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ATE554085T1 - Neue inhibitoren von glutaminylcyclase - Google Patents

Neue inhibitoren von glutaminylcyclase

Info

Publication number
ATE554085T1
ATE554085T1 AT07847471T AT07847471T ATE554085T1 AT E554085 T1 ATE554085 T1 AT E554085T1 AT 07847471 T AT07847471 T AT 07847471T AT 07847471 T AT07847471 T AT 07847471T AT E554085 T1 ATE554085 T1 AT E554085T1
Authority
AT
Austria
Prior art keywords
alkyl
carbocyclyl
heteroaryl
glutaminyl cyclase
new inhibitors
Prior art date
Application number
AT07847471T
Other languages
English (en)
Inventor
Mirko Buchholz
Andre J Niestroj
Ulrich Heiser
Daniel Ramsbeck
Stephan Schilling
Original Assignee
Probiodrug Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Probiodrug Ag filed Critical Probiodrug Ag
Application granted granted Critical
Publication of ATE554085T1 publication Critical patent/ATE554085T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Reproductive Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Anesthesiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
AT07847471T 2006-11-30 2007-11-28 Neue inhibitoren von glutaminylcyclase ATE554085T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US86784506P 2006-11-30 2006-11-30
PCT/EP2007/062953 WO2008065141A1 (en) 2006-11-30 2007-11-28 Novel inhibitors of glutaminyl cyclase

Publications (1)

Publication Number Publication Date
ATE554085T1 true ATE554085T1 (de) 2012-05-15

Family

ID=39133797

Family Applications (1)

Application Number Title Priority Date Filing Date
AT07847471T ATE554085T1 (de) 2006-11-30 2007-11-28 Neue inhibitoren von glutaminylcyclase

Country Status (7)

Country Link
US (1) US9126987B2 (de)
EP (1) EP2091948B1 (de)
JP (1) JP5523107B2 (de)
AT (1) ATE554085T1 (de)
DK (1) DK2091948T3 (de)
SI (1) SI2091948T1 (de)
WO (1) WO2008065141A1 (de)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8420684B2 (en) * 2006-11-09 2013-04-16 Probiodrug Ag Inhibitors of glutaminyl cyclase
JP5599614B2 (ja) * 2006-11-09 2014-10-01 プロビオドルグ エージー グルタミニルシクラーゼの新規阻害剤
WO2008055945A1 (en) * 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
US7803810B2 (en) * 2007-03-09 2010-09-28 Probiodrug Ag Inhibitors
DK2160380T3 (da) * 2007-04-18 2014-06-30 Probiodrug Ag Cyano-guanidin derivater som glutaminyl cyclase inhibitorer
WO2008128986A1 (en) * 2007-04-18 2008-10-30 Probiodrug Ag Urea derivatives as glutaminyl cyclase inhibitors
ES2468551T3 (es) * 2007-04-18 2014-06-16 Probiodrug Ag Derivados de nitrovinil-diamina como inhibidores de la glutaminil ciclasa
US9034907B2 (en) * 2007-04-18 2015-05-19 Probiodrug Ag Inhibitors of glutaminyl cyclase
ES2473621T3 (es) * 2007-04-18 2014-07-07 Probiodrug Ag Derivados de nitrovinil-diamina como inhibidores de glutaminil ciclasa
JP5667440B2 (ja) * 2007-04-18 2015-02-12 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体
JP5676249B2 (ja) * 2007-04-20 2015-02-25 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのアミノピリジン誘導体
JP2011501652A (ja) * 2007-09-12 2011-01-13 プロビオドルグ エージー トランスジェニックマウス
EP2238252B1 (de) * 2008-01-14 2013-07-31 Probiodrug AG Mausmodelle mit einer knockout-mutation des glutaminyl-cyclase-gens
CN105481980A (zh) 2008-07-21 2016-04-13 前体生物药物股份公司 诊断抗体测定
MX2011000975A (es) * 2008-07-25 2011-05-25 Abbott Lab Analogos de peptido b amiloide, oligomeros de los mismos, procedimientos para preparar y composiciones que comprenden dichos analogos u oligomeros, y sus usos.
CN102695546B (zh) 2009-09-11 2014-09-10 前体生物药物股份公司 作为谷氨酰胺酰环化酶抑制剂的杂环衍生物
US20110152341A1 (en) 2009-12-22 2011-06-23 Probiodrug Ag Cleavage of b-amyloid precursor protein
CN102947705A (zh) 2010-02-18 2013-02-27 前体生物药物股份公司 通过确定焦谷氨酸修饰的mcp-1诊断炎性疾病的方法和谷氨酰胺酰基环化酶抑制剂的筛选方法
US9181233B2 (en) 2010-03-03 2015-11-10 Probiodrug Ag Inhibitors of glutaminyl cyclase
US8269019B2 (en) 2010-03-10 2012-09-18 Probiodrug Ag Inhibitors
JP5945532B2 (ja) 2010-04-21 2016-07-05 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体
CN101914094B (zh) * 2010-07-29 2012-08-22 南京大学 1,3,4-噁二唑衍生物及其制法与在制备抗肿瘤药物中的应用
EP2606129B1 (de) 2010-08-19 2015-03-25 Probiodrug AG Glutaminylcyclase-kristallstruktur
AU2012228236B2 (en) 2011-03-16 2016-10-27 Vivoryon Therapeutics N.V. Diagnostic antibody assay
US8530670B2 (en) 2011-03-16 2013-09-10 Probiodrug Ag Inhibitors
JP2018501482A (ja) 2014-12-19 2018-01-18 プロビオドルグ エージー pGlu−Abetaペプチドの検出のための新規の方法
CN105384692B (zh) * 2015-10-26 2018-06-29 深圳大学 一种谷氨酰胺酰基环化酶抑制剂
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
EP3521308B1 (de) 2018-01-31 2024-03-13 Vivoryon Therapeutics N.V. Humanisierte und deimmunisierte antikörper
CN111320617A (zh) * 2018-12-17 2020-06-23 华中科技大学 苯基噁二唑类衍生物及其制备方法与应用
CN111362930B (zh) * 2020-04-15 2023-02-03 安徽医科大学 一种1,2,4-噁二唑-吡啶类化合物及其应用

Family Cites Families (466)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5736816A (ja) 1980-08-14 1982-02-27 Toshiba Corp Chodendokoirunoseizohoho
JPS57192573A (en) 1981-05-25 1982-11-26 Hochiki Co Fire fighting agent
JPS60165712A (ja) 1984-02-08 1985-08-28 パイオニア株式会社 可変調整部品の自動調整方法
JPS6126111A (ja) 1984-07-16 1986-02-05 Shin Meiwa Ind Co Ltd 産業用ロボツト
JPS6137764A (ja) 1984-07-31 1986-02-22 Suntory Ltd 抗プロリルエンドペプチダ−ゼ活性を有する新規生理活性化合物
JPS6152021A (ja) 1984-08-22 1986-03-14 Fujitsu Ltd スケルチ回路
JPS6172439A (ja) 1984-09-18 1986-04-14 Sanyo Electric Co Ltd デ−タ転送方式
JPH0623190B2 (ja) 1985-04-16 1994-03-30 サントリー株式会社 インヒビタ−活性を有するn−アシルピロリジン誘導体及びその製法並びに用途
CA1309805C (en) 1985-04-16 1992-11-03 Naoki Higuchi Dipeptide derivative and synthesis and use thereof
DE3684633D1 (de) 1985-04-16 1992-05-07 Suntory Ltd Dipeptid-derivate von fettsaeure, verfahren zu ihrer herstellung, heilmittel, das sie enthaelt und anwendung.
JPS62114957A (ja) 1985-11-13 1987-05-26 Suntory Ltd プロリルエンドペプチダ−ゼ阻害作用を有する新規ピロリジン誘導体およびその製法並びに用途
JPH0714878B2 (ja) 1985-11-14 1995-02-22 サントリー株式会社 ピロリジンアミドを有効成分とするプロリルエンドペプチダーゼ阻害剤
JPH0764834B2 (ja) 1985-11-29 1995-07-12 サントリー株式会社 プロリルエンドペプチダーゼ阻害活性を有する新規ピロリジンアミド誘導体およびその製法並びに用途
CA1320734C (en) 1986-02-04 1993-07-27 Suntory Limited Pyrrolidineamide derivative of acylamino acid and pharmaceutical composition containing the same
US5198458A (en) 1986-02-04 1993-03-30 Suntory Limited Pyrrolidineamide derivatives of acylamino acid and pharmaceutical composition containing the same
JPS6386485A (ja) 1986-09-30 1988-04-16 Agency Of Ind Science & Technol トンネル型ジヨセフソン接合素子
JPH08806B2 (ja) 1986-11-18 1996-01-10 サントリー株式会社 プロリルエンドペプチダ−ゼ阻害作用を有する新規ピロリジンアミド誘導体
US5254550A (en) 1986-11-20 1993-10-19 Ono Pharmaceutical Co., Ltd. Prolinal derivatives and pharmaceutical compositions thereof
DE3786229T2 (de) 1986-11-20 1993-10-07 Ono Pharmaceutical Co Prolinalderivate.
JPS63162672A (ja) 1986-12-25 1988-07-06 Ono Pharmaceut Co Ltd 新規なプロリナ−ル誘導体、それらの製造方法およびそれらを含有する抗健忘症剤
US5262431A (en) 1986-12-29 1993-11-16 Ono Pharmaceutical Co., Ltd. Prolinal derivatives and pharmaceutical compositions thereof
ATE84787T1 (de) 1986-12-29 1993-02-15 Ono Pharmaceutical Co Prolin-derivate.
JPH089591B2 (ja) 1986-12-29 1996-01-31 小野薬品工業株式会社 新規なプロリナール誘導体
DE3879522T2 (de) 1987-02-04 1993-09-02 Ono Pharmaceutical Co Prolinalderivate.
ATE151760T1 (de) 1987-02-23 1997-05-15 Ono Pharmaceutical Co Thiazolidin-derivate
JPS6442465A (en) 1987-08-07 1989-02-14 Wakunaga Pharma Co Ltd N-acylprolylpyrrolidine derivative, production and use thereof
US4857524A (en) 1987-08-08 1989-08-15 Kissei Pharmaceutical Co., Ltd. Thiazolidine compounds and therapeutic method
JP2649237B2 (ja) 1988-03-07 1997-09-03 キッセイ薬品工業 株式会社 チアゾリジン誘導体
JP2515558B2 (ja) 1987-09-10 1996-07-10 株式会社ヤクルト本社 新規なペプチドおよびそれを有効成分とする抗健忘症剤
JPH0742309B2 (ja) 1987-11-30 1995-05-10 キッセイ薬品工業株式会社 チアゾリジン誘導体
JPH01250370A (ja) 1987-12-23 1989-10-05 Zeria Pharmaceut Co Ltd 新規アミノ酸イミド誘導体、製法ならびに用途
US5053414A (en) 1988-04-08 1991-10-01 Ono Pharmaceutical Co., Ltd. Heterocyclic compounds
US5328899A (en) 1988-07-15 1994-07-12 The Salk Institute For Biological Studies NPY peptide analogs
ZA896374B (en) 1988-08-26 1990-05-30 Merrell Dow Pharma Neuropeptide y antagonists
ZA896376B (en) 1988-08-26 1990-05-30 Merrell Dow Pharma Neuropeptide y agonists
JP2531989B2 (ja) 1988-09-14 1996-09-04 吉富製薬株式会社 ピリジン化合物
CA2004028C (en) 1988-12-08 1998-09-22 Motoki Torizuka Condensed benzene derivative
JPH02207070A (ja) 1989-02-07 1990-08-16 Zeria Pharmaceut Co Ltd アミノ酸イミド誘導体、それを含有する医薬及び該化合物の製造中間体
EP0419683A4 (en) 1989-04-13 1992-03-11 Japan Tobacco Inc. New amino acid derivatives having prolylendopeptidase inhibitor activity
DE3939797A1 (de) 1989-12-01 1991-06-06 Basf Ag Neue vom neuropeptid y abgeleitete peptide
US4985560A (en) 1990-01-12 1991-01-15 American Home Products Corporation Pyridazino(4,5-b)indolizines
JPH04211648A (ja) 1990-07-27 1992-08-03 Nippon Kayaku Co Ltd ケト酸アミド誘導体
JPH03255080A (ja) 1990-03-05 1991-11-13 Yoshitomi Pharmaceut Ind Ltd ベンゼン化合物
US5073549A (en) 1990-03-22 1991-12-17 Bristol-Myers Squibb Company BU-4164E - A and B, prolyl endopeptidase inhibitors and their methods of use
US4999349A (en) 1990-03-22 1991-03-12 Bristol-Myers Squibb Co. BU-4164E - A and B, prolyl endopeptidase inhibitors
EP0536163A1 (de) 1990-06-04 1993-04-14 Pfizer Inc. Aromatische pyrrolidin- und thiazolidinamide
US5407950A (en) 1990-06-07 1995-04-18 Zeria Pharmaceutical Co., Ltd. Arylalkanoylamine derivative and drug containing the same
US5506256A (en) 1990-07-27 1996-04-09 Yoshitomi Pharmaceutical Industries, Ltd. Proline derivatives possessing prolyl endopeptidase-inhibitory activity
JPH05186498A (ja) 1991-12-27 1993-07-27 Japan Tobacco Inc プロリン誘導体
EP0468469A2 (de) 1990-07-27 1992-01-29 Japan Tobacco Inc. Prolinderivate
JPH04235162A (ja) 1990-08-09 1992-08-24 Zeria Pharmaceut Co Ltd 新規コハク酸アミド誘導体およびそれを含有する医薬
JPH04208299A (ja) 1990-11-30 1992-07-29 Ajinomoto Co Inc プロリルエンドペプチターゼ阻害ペプチド
US5104880A (en) 1991-05-01 1992-04-14 Mayo Foundation For Medical Education And Research Huperzine a analogs as acetylcholinesterase inhibitors
WO1992021333A2 (en) 1991-05-24 1992-12-10 Pharmavene, Inc. Treatment of drug withdrawal symptoms and drug craving with type b monoamine oxidase inhibitors
DE69222142T2 (de) 1991-06-20 1998-04-09 Snow Brand Milk Products Co., Ltd., Sapporo, Hokkaido Neuartige prolyl-endopeptidase-inhibitoren sna-115 und sna-115t, ihre herstellung, und hierbei verwendete stämme
HUT66324A (en) 1991-07-29 1994-11-28 Warner Lambert Co Quinazoline derivatives as acetylcholinesterase inhibitors and pharmaceutical compositions containing them
WO1993012139A1 (en) 1991-12-19 1993-06-24 Garvan Institute Of Medical Research A novel molecule which inhibits neuropeptide tyrosine biological function
JPH05301826A (ja) 1991-12-24 1993-11-16 Snow Brand Milk Prod Co Ltd プロリルエンドペプチダーゼ阻害剤
JPH05201970A (ja) 1992-01-24 1993-08-10 Japan Tobacco Inc 新規プロリン誘導体
JP3318622B2 (ja) 1992-05-27 2002-08-26 独立行政法人産業技術総合研究所 プロリルエンドペプチダーゼ阻害剤
GB9212308D0 (en) 1992-06-10 1992-07-22 Ici Plc Therapeutic compositions
GB9213215D0 (en) 1992-06-20 1992-08-05 Wellcome Found Peptides
JPH06116284A (ja) 1992-10-02 1994-04-26 Yamanouchi Pharmaceut Co Ltd 新規ペプチド
WO1994007890A1 (fr) 1992-10-05 1994-04-14 Ube Industries, Ltd. Compose pyrimidine
US5260286A (en) 1992-10-16 1993-11-09 Japan Tobacco, Inc. 2-piperidinecarboxylic acid derivatives useful as NMDA receptor antagonists
CA2149892C (en) 1992-11-20 1998-12-08 Koji Kobayashi Compound having prolyl endopeptidase inhibitory activity and pharmaceutical use thereof
US5354758A (en) 1992-12-16 1994-10-11 Japan Tobacco Inc. Benzomorphans useful as NMDA receptor antagonists
JPH06192298A (ja) 1992-12-24 1994-07-12 Mitsui Toatsu Chem Inc 新規機能性ペプチド
DE4326465A1 (de) 1993-01-20 1995-02-09 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
JPH06234693A (ja) 1993-02-09 1994-08-23 Snow Brand Milk Prod Co Ltd 新規イソテトラセノン系物質及びその製造法
FR2701480B1 (fr) 1993-02-15 1995-05-24 Sanofi Elf Composés à groupe sulfamoyle et amidino, leur procédé de préparation et les compositions pharmaceutiques les contenant.
EP0611769A1 (de) 1993-02-16 1994-08-24 Merrell Dow Pharmaceuticals Inc. Silytierte acetylcholinesterase Inhibitoren
AU4982293A (en) 1993-03-02 1994-09-26 Fujisawa Pharmaceutical Co., Ltd. Novel heterocyclic compound
FR2702150B1 (fr) 1993-03-03 1995-04-07 Rhone Poulenc Rorer Sa Application de dérivés de 2H-1,2-4-benzothiadiazine-3(4H)-one-1,1-dioxyde comme antagonistes non compétitifs du récepteur NMDA.
FR2703050B1 (fr) 1993-03-24 1995-04-28 Adir Nouveaux dérivés bicycliques azotés, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent.
EP0627400A1 (de) 1993-06-04 1994-12-07 Merrell Dow Pharmaceuticals Inc. Aromatische Inhibitoren von Acetylcholinesterase
WO1995000161A1 (en) 1993-06-18 1995-01-05 University Of Cincinnati Neuropeptide y antagonists and agonists
WO1995001352A1 (en) 1993-06-30 1995-01-12 Zeria Pharmaceutical Co., Ltd. Thiazolidine derivative and medicine containing the same
FR2707643B1 (fr) 1993-07-16 1995-08-11 Rhone Poulenc Rorer Sa Dérivés d'imidazo[1,2-a]pyrazine-4-one, leur préparation et les médicaments les contenant.
FR2707645B1 (fr) 1993-07-16 1995-08-11 Rhone Poulenc Rorer Sa Dérivés d'imidazo[1,2-a]pirazine-4-one, leur préparation et les médicaments les contenant.
DE69428703T2 (de) 1993-07-23 2002-05-29 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai, Tokio/Tokyo Pyrrolidin derivate
JPH0741485A (ja) * 1993-07-30 1995-02-10 Katayama Seiyakushiyo:Kk セフェム誘導体およびそれを含有する抗菌剤
FR2711993B1 (fr) 1993-11-05 1995-12-01 Rhone Poulenc Rorer Sa Médicaments contenant des dérivés de 7H-imidazol[1,2-a]pyrazine-8-one, les nouveaux composés et leur préparation.
WO1995015310A1 (en) 1993-12-02 1995-06-08 Merrell Pharmaceuticals Inc. Prolyl endopeptidase inhibitors
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
FR2717812B1 (fr) 1994-03-28 1996-05-10 Rhone Poulenc Rorer Sa Indeno[1,2-e]pyrazine-4-ones, leur préparation et les médicaments les contenant.
FR2717813B1 (fr) 1994-03-28 1996-05-10 Rhone Poulenc Rorer Sa Dérivés d'imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one, leur préparation et les médicaments les contenant .
FR2717805B1 (fr) 1994-03-28 1996-05-10 Rhone Poulenc Rorer Sa Dérivés de 5H-indeno[1,2-b]pyrazine-2,3-dione, leur préparation et les médicaments les contenant .
FR2717811B1 (fr) 1994-03-28 1996-04-26 Rhone Poulenc Rorer Sa Dérivés d'imidazo[1,2-a]pyrazine-4-one, leur préparation et les médicaments les contenant.
JPH07267988A (ja) 1994-03-31 1995-10-17 Yamanouchi Pharmaceut Co Ltd 新規ペプチド
GB9410320D0 (en) 1994-05-24 1994-07-13 Fisons Corp Novel therapeutic method
GB9418443D0 (en) 1994-09-13 1994-11-02 Pfizer Ltd Therapeutic agents
US6562862B1 (en) 1994-10-20 2003-05-13 Eli Lilly And Company Methods of inhibiting physiological conditions associated with an excess of neuropeptide Y
IL115613A0 (en) 1994-10-20 1996-01-19 Lilly Co Eli Bicyclic neuropeptide y receptor antagonists
US5663192A (en) 1994-10-20 1997-09-02 Eli Lilly And Company Heterocyclic neuropeptide Y receptor antagonists
FR2726275B1 (fr) 1994-11-02 1996-12-06 Rhone Poulenc Rorer Sa Spiro heterocycle-imidazo(1,2-a)indeno(1,2-e)pyrazine)-4'- ones, leur preparation et les medicaments les contenants
IL116584A0 (en) 1994-12-29 1996-03-31 Res Dev Foundation Novel flavin adenine dinucleotide analogue inhibitors of monoamine oxidase
US5691368A (en) 1995-01-11 1997-11-25 Hoechst Marion Roussel, Inc. Substituted oxazolidine calpain and/or cathepsin B inhibitors
GB9500601D0 (en) 1995-01-12 1995-03-01 Wellcome Found Modified peptides
US5552411A (en) 1995-05-26 1996-09-03 Warner-Lambert Company Sulfonylquinolines as central nervous system and cardiovascular agents
US5635503A (en) 1995-06-07 1997-06-03 Bristol-Myers Squibb Company Dihydropyridine npy antagonists: piperazine derivatives
US5554621A (en) 1995-06-07 1996-09-10 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: nitrogen heterocyclic derivatives
US5668151A (en) 1995-06-07 1997-09-16 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: piperidine derivatives
IL117997A0 (en) 1995-06-07 1996-10-31 Pfizer Neuropeptide Y1 specific ligands
JP3727383B2 (ja) 1995-07-31 2005-12-14 月桂冠株式会社 プロリルエンドペプチダーゼ阻害剤
MX9703186A (es) 1995-09-01 1997-07-31 Lilly Co Eli Antagonistas del receptor del neuropeptido y de indolilo.
WO1997012613A1 (en) 1995-10-05 1997-04-10 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
ES2100129B1 (es) 1995-10-11 1998-02-16 Medichem Sa Nuevos compuestos aminopiridinicos policiclicos inhibidores de acetilcolinesterasa, procedimiento para su preparacion y su utilizacion.
DE19544685A1 (de) 1995-11-30 1997-06-05 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE19544686A1 (de) 1995-11-30 1997-06-05 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE19544687A1 (de) 1995-11-30 1997-06-05 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
WO1997019682A1 (en) 1995-12-01 1997-06-05 Synaptic Pharmaceutical Corporation Aryl sulfonamide and sulfamide derivatives and uses thereof
AU7692996A (en) 1995-12-01 1997-06-27 Ciba-Geigy Ag Receptor antagonists
WO1997020822A1 (en) 1995-12-01 1997-06-12 Novartis Ag Quinazolin-2,4-diazirines as npy receptor antagonist
AU7626496A (en) 1995-12-01 1997-06-27 Ciba-Geigy Ag Heteroaryl compounds
WO1997020821A1 (en) 1995-12-01 1997-06-12 Novartis Ag Heteroaryl derivatives
JPH09157253A (ja) 1995-12-12 1997-06-17 Yamanouchi Pharmaceut Co Ltd 新規アミノ酸誘導体
ZA9610736B (en) 1995-12-22 1997-06-27 Warner Lambert Co 2-Substituted piperidine analogs and their use as subtypeselective nmda receptor antagonists
ZA9610741B (en) 1995-12-22 1997-06-24 Warner Lambert Co 4-Substituted piperidine analogs and their use as subtype selective nmda receptor antagonists
ZA9610745B (en) 1995-12-22 1997-06-24 Warner Lambert Co 4-Subsituted piperidine analogs and their use as subtype selective nmda receptor antagonists
WO1997025041A1 (en) 1996-01-09 1997-07-17 Eli Lilly And Company Benzimidzolyl neuropeptide y receptor antagonists
GB9605027D0 (en) 1996-03-09 1996-05-08 Pfizer Ltd Quinoxalinediones
US5662723A (en) 1996-03-22 1997-09-02 Libbey Glass Inc. Apparatus and method for forming a decorative pattern on glassware having an edge
ES2165586T3 (es) 1996-04-12 2002-03-16 Aventis Pharma Inc Derivados de isatina como inhibidores de acetilcolinesterasa y analgesicos.
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
WO1997046250A1 (en) 1996-06-04 1997-12-11 Synaptic Pharmaceutical Corporation Methods of modifying feeding behavior, compounds useful in such methods, and dna encoding a hypothalamic atypical neuropeptide y/peptide yy receptor (y5)
EP0942751B1 (de) 1996-07-05 2002-09-25 The WWK Trust Zusammensetzungen zur behandlung der peripheren neuropathie, die antidepressiven verbindungen und/oder monoamino-oxidaseinhibitoren und/oder vitamin b12 und/oder neurotransmitter-vorläufer oder induktoren enthalten
WO1998003493A1 (en) 1996-07-23 1998-01-29 Neurogen Corporation Certain substituted benzylamine derivatives; a new class of neuropeptide-y1 specific ligands
ATE230403T1 (de) 1996-07-23 2003-01-15 Neurogen Corp Einige amido- und ammo- substituierte benzylaminderivate: eine neue klasse von neuropeptid y1 spezifische ligande
PT918761E (pt) 1996-07-23 2003-09-30 Neurogen Corp Algumas amidas e aminas substituidas com derivados de benzilamina uma nova classe de ligandos especificos do neuropeptido y1
WO1998005337A1 (en) 1996-08-01 1998-02-12 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
WO1998006703A1 (en) 1996-08-14 1998-02-19 Warner-Lambert Company 2-phenyl benzimidazole derivatives as mcp-1 antagonists
CA2268051A1 (en) 1996-08-23 1998-02-26 Alanex Corporation Neuropeptide-y ligands
JP3880664B2 (ja) 1996-09-04 2007-02-14 月桂冠株式会社 プロリルエンドペプチダーゼ阻害ペプチド
AU4424697A (en) 1996-09-11 1998-04-02 Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services, The The use of functional n-methyl-d-aspartate antagonists to ameliorate or prevent aminoglycoside-induced ototoxicity
AU4944297A (en) 1996-10-08 1998-05-05 Novartis Ag Modulation of apoptosis
FR2754709B1 (fr) 1996-10-23 1999-03-05 Sanofi Sa Composition cosmetique contenant un antagoniste des recepteurs du neuropeptide gamma et alpha 2 antagonistes susceptibles d'etre incorpores dans une telle composition
US6011155A (en) 1996-11-07 2000-01-04 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
WO1998030243A1 (en) 1997-01-08 1998-07-16 Warner-Lambert Company Acetylcholinesterase inhibitors in combination with muscarinic agonists for the treatment of alzheimer's disease
AU6417198A (en) 1997-03-13 1998-09-29 Bioresearch Ireland a division of Eolas - The Irish Science and Technology Agency Cytoprotective agents comprising monoamine oxidase inhibitors
CA2286660A1 (en) 1997-04-16 1998-10-22 Arqule, Inc. Synthesis and use of .alpha.-ketoamide derivatives and arrays
JP2001527554A (ja) 1997-05-07 2001-12-25 アルゴス ファーマシューティカル コーポレーション 抗うつ薬とnmdaレセプター拮抗薬とを組み合わせる神経障害痛の治療用組成物及び治療方法
AU7472798A (en) 1997-05-07 1998-11-27 Algos Pharmaceutical Corporation Cox-2 inhibitors in combination with nmda-blockers for treating pain
HU226110B1 (en) 1997-06-30 2008-04-28 Merz Pharma Gmbh & Co Kgaa 1-amino-alkylcyclohexane nmda receptor antagonists, pharmaceutical compositions containing and their use
GB9716657D0 (en) 1997-08-07 1997-10-15 Zeneca Ltd Chemical compounds
GB9716879D0 (en) 1997-08-08 1997-10-15 Shire Int Licensing Bv Treatment of attention deficit disorders
AU7696098A (en) 1997-08-11 1999-03-01 Algos Pharmaceutical Corporation Substance p inhibitors in combination with nmda-blockers for treating pain
SE9703376D0 (sv) 1997-09-18 1997-09-18 Astra Ab A new combination
SE9703414D0 (sv) 1997-09-23 1997-09-23 Astra Ab New compounds
CA2819705C (en) 1998-02-02 2014-07-08 Trustees Of Tufts College Method of regulating glucose metabolism, and reagents related thereto
JP2002506075A (ja) 1998-03-09 2002-02-26 フォンダテッヒ・ベネルクス・ナムローゼ・フェンノートシャップ セリンペプチダーゼ調節剤
US6007841A (en) 1998-03-13 1999-12-28 Algos Pharmaceutical Corporation Analgesic composition and method for treating pain
GB9805561D0 (en) 1998-03-16 1998-05-13 Merck Sharp & Dohme A combination of therapeutic agents
US6541208B1 (en) 1998-03-17 2003-04-01 University Of Maryland Biotechnology Institute Diagnostic method for distinguishing HIV-associated dementia from other forms of dementia
DE19812331A1 (de) 1998-03-20 1999-09-23 Merck Patent Gmbh Piperidinderivate
US6054451A (en) 1998-04-21 2000-04-25 Algos Pharmaceutical Corporation Analgesic composition and method for alleviating pain
AU3786299A (en) 1998-05-04 1999-11-23 Neotherapeutics, Inc. Novel serotonin-like 9-substituted hypoxanthine and methods of use
WO1999057119A1 (en) 1998-05-04 1999-11-11 Neotherapeutics, Inc. Novel dopamine-like 9-substituted hypoxanthine and methods of use
DE19823831A1 (de) 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
DE19828114A1 (de) 1998-06-24 2000-01-27 Probiodrug Ges Fuer Arzneim Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV
DE19828113A1 (de) 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV
PE20000728A1 (es) 1998-06-26 2000-08-21 Cocensys Inc Heterociclos 4-bencil piperidina alquilsulfoxido y su uso como antagonistas receptores subtipo-selectivo nmda
US6262081B1 (en) 1998-07-10 2001-07-17 Dupont Pharmaceuticals Company Composition for and method of treating neurological disorders
DE69911975T2 (de) 1998-07-31 2004-09-09 Novo Nordisk A/S In-vitro stimulation von beta zellen vermehrung
DE19834591A1 (de) 1998-07-31 2000-02-03 Probiodrug Ges Fuer Arzneim Verfahren zur Steigerung des Blutglukosespiegels in Säugern
US6218383B1 (en) 1998-08-07 2001-04-17 Targacept, Inc. Pharmaceutical compositions for the prevention and treatment of central nervous system disorders
IL125809A (en) 1998-08-17 2005-08-31 Finetech Lab Ltd Process and intermediates for production of donepezil and related compounds
IT1304904B1 (it) 1998-09-11 2001-04-05 Eisai Co Ltd Derivati anticolinesterasici per il trattamento delle sindromidolorose funzionali e/o organiche
HUP0103781A3 (en) 1998-10-16 2003-09-29 Janssen Pharmaceutica Nv Pharmaceutical compositions comprising atypical antiphsychotic agent in combination with acetylcholinesterase inhibitor for improving cognition
AU1408699A (en) 1998-11-12 2000-06-05 Algos Pharmaceutical Corporation Cox-2 inhibitors in combination with nmda-blockers for treating pain
WO2000030446A1 (en) 1998-11-23 2000-06-02 Bonnie Davis Dosage formulations for acetylcholinesterase inhibitors
WO2000030674A1 (en) 1998-11-26 2000-06-02 Ferring Bv Neuropeptide y y4 agents in the treatment of reproductive disorders
ATE306264T1 (de) 1998-12-11 2005-10-15 Bonnie M Davis Verwendung von acetylcholinesterase inhibitoren zur modulierung der hypothalamus-hypophysen- gonadenachse
GB9902453D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902459D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902455D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902461D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902452D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
JP2002540098A (ja) 1999-03-23 2002-11-26 住友製薬株式会社 三環性インドール−2−カルボン酸化合物
US6121311A (en) 1999-04-28 2000-09-19 Japan Tobacco Inc. Method for treating cocainism
MXPA01011321A (es) 1999-05-05 2003-08-01 Johnson & Johnson Neuropeptidos y ligandos de receptores 3a, 4, 5, 9b-tetrahidro-1h-benz(e)indol-2-il amino derivados utiles en el tratamiento de obesidad y otros trastornos.
JP3148739B2 (ja) 1999-05-19 2001-03-26 ドーマー株式会社 プロリルエンドペプチダーゼ阻害剤
US6172081B1 (en) 1999-06-24 2001-01-09 Novartis Ag Tetrahydroisoquinoline 3-carboxamide derivatives
US6110949A (en) 1999-06-24 2000-08-29 Novartis Ag N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6107317A (en) 1999-06-24 2000-08-22 Novartis Ag N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
AU6053900A (en) 1999-06-25 2001-01-31 Morris Notelovitz Compositions for treating or preventing neurodegeneration and cognitive decline
DE19936521A1 (de) 1999-08-06 2001-02-15 Gruenenthal Gmbh Substituierte Pyrrolidin-2,3,4-trion-3-oxim-Derivate
DE19936719A1 (de) 1999-08-06 2001-02-15 Gruenenthal Gmbh Substituierte 1,5-Dihydropyrrol-2-on-Derivate
EP1078632A1 (de) 1999-08-16 2001-02-28 Sanofi-Synthelabo Verwendung von Monoamin Oxydase Inhibitoren zu Herstellung eines Medikaments zur Behandlung der Fettleibigkeit
DE19940130A1 (de) 1999-08-24 2001-03-01 Probiodrug Ges Fuer Arzneim Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung
TWI292316B (en) 1999-10-11 2008-01-11 Sod Conseils Rech Applic Pharmaceutical composition of thiazole derivatives intended to inhibit mao and/or lipidic peroxidation and/or to act as modulators of sodium channels and the use thereof
UA72558C2 (uk) 1999-11-01 2005-03-15 Мерц Фарма Гмбх Унд Ко. Кгаа 1-аміноалкілциклогексанові антагоністи рецептора nmda
CA2390231A1 (en) 1999-11-12 2001-05-17 Paul Jackson Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors
UA75055C2 (uk) 1999-11-30 2006-03-15 Пфайзер Продактс Інк. Похідні бензоімідазолу, що використовуються як антипроліферативний засіб, фармацевтична композиція на їх основі
GB9928330D0 (en) 1999-11-30 2000-01-26 Ferring Bv Novel antidiabetic agents
AU779875B2 (en) 2000-01-24 2005-02-17 Merck Sharp & Dohme Limited Gamma-secretase inhibitors
JP2003520849A (ja) 2000-01-24 2003-07-08 ノボ ノルディスク アクティーゼルスカブ 酵素dpp−ivの阻害剤であるn−置換2−シアノピロールおよび−ピロリン
JP4398620B2 (ja) 2000-02-03 2010-01-13 ミレニアム・ファーマシューティカルズ・インコーポレイテッド ヒト化抗ccr−2抗体およびその使用方法
GB0005251D0 (en) 2000-03-03 2000-04-26 Merck Sharp & Dohme Therapeutic compounds
US20030144255A1 (en) 2000-03-06 2003-07-31 Bain Allen I Compositions for prevention and treatment of dementia
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
DE60124080T2 (de) 2000-03-23 2007-03-01 Elan Pharmaceuticals, Inc., San Francisco Verbindungen und verfahren zur behandlung der alzheimerschen krankheit
US6992081B2 (en) 2000-03-23 2006-01-31 Elan Pharmaceuticals, Inc. Compounds to treat Alzheimer's disease
GB0008710D0 (en) 2000-04-07 2000-05-31 Merck Sharp & Dohme Therapeutic compounds
US6706741B2 (en) 2000-04-13 2004-03-16 Eisai Co., Ltd. Acetylcholinesterase inhibitors containing 1-benzyl-pyridinium salts
GB0010183D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
HUP0300600A2 (hu) 2000-04-26 2003-08-28 Warner-Lambert Co. Ciklohexil-amin-származékok mint altípus-szelektív NMDA receptor antagonisták és ezeket tartalmazó gyógyszerkészítmények
GB0010188D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
US20010036949A1 (en) 2000-05-09 2001-11-01 Coe Jotham Wadsworth Pharmaceutical composition and method of treatment of diseases of cognitive dysfunction in a mammal
AU2001261487A1 (en) 2000-06-01 2001-12-11 Warner Lambert Company Cyclohexylamine derivatives as subtype selective nmda receptor antagonists
US6683101B2 (en) 2000-06-06 2004-01-27 Warner-Lambert Company Bicyclic cyclohexylamines and their use as NMDA receptor antagonists
EP1299374B1 (de) 2000-06-22 2006-12-27 Pharmos Corporation Neue nicht psychotropische cannabinoide
GB0015488D0 (en) 2000-06-23 2000-08-16 Merck Sharp & Dohme Therapeutic agents
US6713276B2 (en) 2000-06-28 2004-03-30 Scios, Inc. Modulation of Aβ levels by β-secretase BACE2
US6686449B2 (en) 2000-06-30 2004-02-03 Pharmacia & Upjohn Company Mutant presenilin 1 polypeptides
MXPA02012560A (es) 2000-06-30 2003-05-14 Elan Pharm Inc Compuestos para tratar la enfermedad de alzheimer.
JP2004502690A (ja) 2000-07-04 2004-01-29 ノボ ノルディスク アクティーゼルスカブ 酵素dpp−ivのインヒビターである複素環式化合物
GB0016681D0 (en) 2000-07-06 2000-08-23 Merck Sharp & Dohme Therapeutic compounds
US6556971B1 (en) 2000-09-01 2003-04-29 Snap-On Technologies, Inc. Computer-implemented speech recognition system training
WO2002027418A2 (en) 2000-09-25 2002-04-04 Motorwiz, Inc. Model-based machine diagnostics and prognostics using theory of noise and communications
US20020151591A1 (en) 2000-10-17 2002-10-17 Anabella Villalobos Combination use of acetylcholinesterase inhibitors and GABAa inverse agonists for the treatment of cognitive disorders
HU227197B1 (en) 2000-10-24 2010-10-28 Richter Gedeon Nyrt Nmda receptor antagonist carboxylic acid amide derivatives and pharmaceutical compositions containing them
EP1334085B1 (de) 2000-11-02 2005-08-24 Merck Sharp & Dohme Ltd. Sulfamide als gamma-secretase-inhibitoren
TWI243162B (en) 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
US6670364B2 (en) 2001-01-31 2003-12-30 Telik, Inc. Antagonists of MCP-1 function and methods of use thereof
TWI245761B (en) 2001-03-01 2005-12-21 Telik Inc Antagonists of MCP-1 function and methods of use thereof
IL157638A0 (en) * 2001-03-01 2004-03-28 Shionogi & Co Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity
EP1436258A4 (de) 2001-03-08 2005-03-23 Univ Emory Ph-wert-abhängige nmda-rezeptorantagonisten
US6649196B2 (en) 2001-03-12 2003-11-18 Mayo Foundation For Medical Education And Research Methods of reducing β-amyloid polypeptides
US6677365B2 (en) 2001-04-03 2004-01-13 Telik, Inc. Antagonists of MCP-1 function and methods of use thereof
US6573287B2 (en) 2001-04-12 2003-06-03 Bristo-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method
FR2824825B1 (fr) 2001-05-15 2005-05-06 Servier Lab Nouveaux derives d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
SI20922A (sl) 2001-05-18 2002-12-31 Krka Tovarna Zdravil, D.D., Novo Mesto Monoklonsko protitelo, ki nevtralizira aktivnost katepsina B, in njegove uporabe
US6562783B2 (en) 2001-05-30 2003-05-13 Neurologic, Inc. Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors
MXPA03011046A (es) 2001-06-01 2004-06-25 Elan Pharm Inc Hidroxialquilaminas.
WO2003000180A2 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
WO2003000181A2 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
DE10154689A1 (de) 2001-11-09 2003-05-22 Probiodrug Ag Substituierte Aminoketonverbindungen
DE60223920T2 (de) 2001-06-27 2008-11-13 Smithkline Beecham Corp. Pyrrolidine als dipeptidyl-peptidase-inhibitoren
WO2003072556A1 (en) 2001-06-27 2003-09-04 Prosidion Ltd. Glutaminyl based dpiv inhibitors
ATE374181T1 (de) 2001-06-27 2007-10-15 Smithkline Beecham Corp Fluorpyrrolidine als dipeptidylpeptidaseinhibitoren
WO2003002553A2 (en) 2001-06-27 2003-01-09 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
US6982264B2 (en) 2001-06-27 2006-01-03 Elan Pharmaceuticals, Inc. Substituted alcohols useful in treatment of Alzheimer's disease
DE10150203A1 (de) 2001-10-12 2003-04-17 Probiodrug Ag Peptidylketone als Inhibitoren der DPIV
RU2299066C2 (ru) 2001-06-27 2007-05-20 Пробиодруг Аг Новые ингибиторы дипептидилпептидазы iv и их применение в качестве противораковых агентов
JP2005502624A (ja) 2001-07-03 2005-01-27 ノボ ノルディスク アクティーゼルスカブ 糖尿病を治療するための、dpp−ivを阻害するプリン誘導体
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
SK287726B6 (en) 2001-07-24 2011-07-06 Richter Gedeon Vegyeszet Carboxylic acid amide derivatives, their preparation, pharmaceutical compositions containing them and process for preparing pharmaceutical compositions
US6948038B2 (en) * 2001-07-24 2005-09-20 Microsoft Corporation System and method for backing up and restoring data
PL372212A1 (en) 2001-08-03 2005-07-11 Schering Corporation Novel gamma secretase inhibitors
JP2005504042A (ja) 2001-08-03 2005-02-10 シェーリング コーポレイション γセクレターゼインヒビターのようなスルホンアミド誘導体
EP1423127A1 (de) 2001-08-30 2004-06-02 Ortho-Mcneil Pharmaceutical, Inc. Behandlung von dementia und erinnerungsstörungen mit anticonvulsants und acetylcholinesterasehemmer
CN100341862C (zh) 2001-09-14 2007-10-10 三菱制药株式会社 噻唑烷衍生物及其医药用途
EP1463727A2 (de) 2001-09-19 2004-10-06 Novo Nordisk A/S Heterocyclische verbindungen, bei denen es sich um inhibitoren des enzyms dpp-iv handelt
GB0125446D0 (en) 2001-10-23 2001-12-12 Ferring Bv Novel anti-diabetic agents
GB0125445D0 (en) 2001-10-23 2001-12-12 Ferring Bv Protease Inhibitors
CA2464736A1 (en) 2001-10-23 2003-05-15 Oklahoma Medical Research Foundation Beta-secretase inhibitors and methods of use
US6861440B2 (en) 2001-10-26 2005-03-01 Hoffmann-La Roche Inc. DPP IV inhibitors
US7304040B2 (en) 2001-11-02 2007-12-04 Kensuke Egashira Suppression of post-transplant arteriosclerosis
HRP20040550A2 (en) 2001-11-19 2006-11-30 Elan Pharmaceuticals 3,4-disubstituted, 3,5-disubstituted and 3,4,5-substituted piperidines and piperazines
US7727964B2 (en) 2001-11-26 2010-06-01 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
RU2004121898A (ru) 2001-12-19 2006-01-20 Атеродженикс, Инк. (Us) Производные халкона и их применение для лечения заболеваний
WO2003057144A2 (en) 2001-12-26 2003-07-17 Guilford Pharmaceuticals Change inhibitors of dipeptidyl peptidase iv
US6727261B2 (en) 2001-12-27 2004-04-27 Hoffman-La Roche Inc. Pyrido[2,1-A]Isoquinoline derivatives
WO2003057204A2 (en) 2002-01-08 2003-07-17 Nordic Bioscience A/S Modulation of iamt (pimt or pcmt) in immune system
CA2473441A1 (en) 2002-01-18 2003-07-24 The Genetics Company Inc. Beta-secretase inhibitors
TW200302717A (en) 2002-02-06 2003-08-16 Schering Corp Novel gamma secretase inhibitors
US20040171614A1 (en) 2002-02-06 2004-09-02 Schering-Plough Corporation Novel gamma secretase inhibitors
BR0307665A (pt) 2002-02-13 2005-01-04 Hoffmann La Roche Compostos, processo para a sua manufatura, composições farmacêuticas que compreendem os mesmos, método para o tratamento e/ou profilaxia de enfermidades associadas com dpp iv e utilização dos compostos
ES2252656T3 (es) 2002-02-13 2006-05-16 F. Hoffmann-La Roche Ag Nuevos derivados de piridina y quinolina.
HUP0200849A2 (hu) 2002-03-06 2004-08-30 Sanofi-Synthelabo N-aminoacetil-2-ciano-pirrolidin-származékok, e vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra
JP2005526811A (ja) 2002-03-25 2005-09-08 メルク エンド カムパニー インコーポレーテッド 糖尿病の治療または予防用β−アミノ複素環式ジペプチジルペプチダーゼ阻害剤
JP4405811B2 (ja) 2002-03-29 2010-01-27 エーザイ・アール・アンド・ディー・マネジメント株式会社 (1−インダノン)−(1,2,3,6−テトラヒドロピリジン)誘導体
US6996738B2 (en) 2002-04-15 2006-02-07 Broadcom Corporation Robust and scalable de-skew method for data path skew control
JP4404643B2 (ja) 2002-04-24 2010-01-27 啓 森 ガンマセクレターゼ阻害剤
MXPA04010552A (es) 2002-04-26 2005-01-25 Schering Corp Antagonistas muscarinicos.
WO2003099202A2 (en) 2002-05-17 2003-12-04 Merck & Co., Inc. Beta-secretase inhibitors
DE60324788D1 (de) 2002-05-31 2009-01-02 Lundbeck & Co As H Kombination aus einem nmda-antagonist und acetylcholinesterase-hemmern zur behandlung der alzheimer-krankheit
WO2003101958A2 (en) 2002-06-04 2003-12-11 Pfizer Products Inc. Flourinated cyclic amides as dipeptidyl peptidase iv inhibitors
AU2003233010A1 (en) 2002-06-04 2003-12-19 Pfizer Products Inc. Process for the preparation of 3,3,4,4-tetrafluoropyrrolidine and derivatives thereof
EP1514552A4 (de) 2002-06-06 2008-04-02 Eisai R&D Man Co Ltd Neues kondensiertes imidazolderivativ
US20050171300A1 (en) 2002-06-19 2005-08-04 Luc Moens Semi-gloss powder coating compositions
AU2003248259A1 (en) 2002-07-10 2004-02-02 Yamanouchi Pharmaceutical Co., Ltd. Novel azetidine derivative or salt thereof
ATE451369T1 (de) 2002-07-15 2009-12-15 Merck & Co Inc Piperidinopyrimidindipeptidylpeptidaseinhibitor n zur behandlung von diabetes
US20040019118A1 (en) 2002-07-19 2004-01-29 Khalid Iqbal NMDA receptor antagonists and their use in inhibiting abnormal hyperphosphorylation of microtubule associated protein tau
US7557137B2 (en) 2002-08-05 2009-07-07 Bristol-Myers Squibb Company Gamma-lactams as beta-secretase inhibitors
EA016166B1 (ru) 2002-08-21 2012-02-28 Бёрингер Ингельхайм Фарма Гмбх & Ко. Кг 8-[3-аминопиперидин-1-ил]ксантины, способ их получения и их применение в качестве лекарственных средств
DE10238470A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
DE10238477A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Purinderivate, deren Herstellung und deren Verwendung als Arzneimittel
AU2003262051B2 (en) 2002-09-12 2008-09-25 Juridical Foundation The Chemo-Sero-Therapeutic Research Institute Human antihuman MCP-1 antibody and antibody fragment thereof
MXPA05003091A (es) 2002-09-19 2005-05-27 Abbott Lab Composiciones farmaceuticas como inhibidores de peptidasa de dipeptidilo-iv de (dpp-iv).
US20050282871A1 (en) 2002-09-20 2005-12-22 Burrill Ii Leland C 3-(3,5-Disubstituted-4-hydroxyphenyl)propionamide derivatives as cathepsin b inhibitors
US7273889B2 (en) 2002-09-25 2007-09-25 Innovative Drug Delivery Systems, Inc. NMDA receptor antagonist formulation with reduced neurotoxicity
GB0223038D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
GB0223039D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
AU2003275404A1 (en) 2002-10-07 2004-05-04 Merck & Co., Inc. Antidiabetic beta-amino heterocyclic dipeptidyl peptidase inhibitors
WO2004033455A2 (en) 2002-10-08 2004-04-22 Novo Nordisk A/S Hemisuccinate salts of heterocyclic dpp-iv inhibitors
GB0223494D0 (en) 2002-10-09 2002-11-13 Neuropharma Sa Dual binding site acetylcholinesterase inhibitors for the treatment of alzheimer's disease
AU2003298596B2 (en) 2002-10-18 2008-12-18 Merck Sharp & Dohme Corp. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP1556019A2 (de) 2002-10-24 2005-07-27 Merz Pharma GmbH & Co. KGaA Kombinationstherapie unter verwendung von 1-aminocyclohexan derivaten und acetylcholinesterase inhibitoren
US20040082543A1 (en) 2002-10-29 2004-04-29 Pharmacia Corporation Compositions of cyclooxygenase-2 selective inhibitors and NMDA receptor antagonists for the treatment or prevention of neuropathic pain
AU2003285296A1 (en) 2002-10-30 2004-05-25 Nordic Bioscience A/S Coumpounds modulating the activity of gapdh and/or iamt
WO2004041795A1 (en) 2002-10-30 2004-05-21 Guilford Pharmaceuticals Inc. Novel inhibitors of dipeptidyl peptidase iv
GB0225474D0 (en) 2002-11-01 2002-12-11 Merck Sharp & Dohme Therapeutic agents
BR0315796A (pt) 2002-11-07 2005-09-13 Merck & Co Inc Composto, composição farmacêutica, e, métodos para tratar diabetes, para tratar hiperglicemia, e para tratar obesidade em um mamìfero
CA2505098A1 (en) 2002-11-12 2004-05-27 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
AU2002952946A0 (en) 2002-11-27 2002-12-12 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
CA2508487A1 (en) 2002-12-04 2004-06-17 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7420079B2 (en) 2002-12-09 2008-09-02 Bristol-Myers Squibb Company Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof
AU2003293376A1 (en) 2002-12-10 2004-06-30 Imclone Systems Incorporated Anti-angiogenic compounds and their use in cancer treatment
WO2004056727A2 (en) 2002-12-19 2004-07-08 Atherogenics, Inc. Process of making chalcone derivatives
AU2003297219A1 (en) 2002-12-20 2004-07-22 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
CA2512111A1 (en) 2003-01-07 2004-07-29 Merck And Co., Inc. Macrocyclic beta-secretase inhibitors for treatment of alzheimer's disease
JP4564952B2 (ja) 2003-01-17 2010-10-20 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病の治療および予防のためのジペプチジルペプチダーゼ阻害薬としての3−アミノ−4−フェニルブタン酸誘導体
EP1592689A4 (de) 2003-01-31 2008-12-24 Merck & Co Inc 3-amino-4-phenylbutansäurederivate als dipeptidylpeptidase-hemmer zur behandlung oder vorbeugung von diabetes
EP1592684B1 (de) 2003-02-04 2008-07-30 F. Hoffmann-La Roche Ag Malonamidderivate als gamma-secretaseinhibitoren
WO2004071454A2 (en) 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
CN1777436A (zh) 2003-02-18 2006-05-24 罗斯坎普研究有限责任公司 β和γ分泌酶抑制剂的抗血管生成和抗肿瘤性
WO2004076434A1 (en) 2003-02-28 2004-09-10 Aic Dipeptidyl peptidase inhibitors
WO2004076433A1 (en) 2003-02-28 2004-09-10 Aic Dipeptidyl peptidase inhibitors
EP1454627A1 (de) 2003-03-06 2004-09-08 MyoContract Ltd. Alpha-Keto-Carbonyl-Verbindungen als Calpainhemmer
WO2004084830A2 (en) 2003-03-21 2004-10-07 Buck Institute Method for treating alzheimer’s dementia
US20040191334A1 (en) 2003-03-24 2004-09-30 Pang-Chui Shaw Use of transhinone derivates as cholinesterase inhibitors in treating related diseases
US20040242566A1 (en) 2003-03-25 2004-12-02 Syrrx, Inc. Dipeptidyl peptidase inhibitors
WO2004087158A2 (en) 2003-03-28 2004-10-14 Acadia Pharmaceuticals Inc. Muscarinic m1 receptor agonists for pain management
AR044013A1 (es) 2003-04-09 2005-08-24 Wyeth Corp Derivados de acido [2-(8,9-dioxo-2,6-diazabiciclo [5.2.0.] non-1 (7)-en-2-il)alquil]fosfonico, metodos para su uso, composicion y procedimiento de preparacion
GB0308382D0 (en) 2003-04-10 2003-05-21 Univ Cambridge Tech Therapeutic methods and means
GB0308318D0 (en) 2003-04-10 2003-05-14 Merck Sharp & Dohme Therapeutic agents
WO2004089362A1 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S 2-cyanopyrroles and their analogues as ddp-iv inhibitors
US7732162B2 (en) 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
US7371871B2 (en) 2003-05-05 2008-05-13 Probiodrug Ag Inhibitors of glutaminyl cyclase
KR20110059664A (ko) 2003-05-05 2011-06-02 프로비오드룩 아게 글루타미닐 및 글루타메이트 사이클라제의 이펙터의 용도
US8338120B2 (en) 2003-05-05 2012-12-25 Probiodrug Ag Method of treating inflammation with glutaminyl cyclase inhibitors
EP1622870A2 (de) 2003-05-05 2006-02-08 Prosidion Ltd. Glutaminylbasierte dp-iv-inhibitoren
AU2003902260A0 (en) 2003-05-09 2003-05-29 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
MXPA05012268A (es) 2003-05-13 2006-02-10 Schering Corp N-arilsulfonilpiperidinas enlazadas como inhibidores de la gamma-secretasa.
DE602004023932D1 (de) 2003-05-14 2009-12-17 Merck & Co Inc 3-amino-4-phenylbutansäurederivate als dipeptidylpeptidase-hemmer zur behandlung oder vorbeugung von diabetes
EP1625122A1 (de) 2003-05-14 2006-02-15 Takeda San Diego, Inc. Dipeptidylpeptidase-hemmer
ATE386028T1 (de) 2003-05-16 2008-03-15 Merck Sharp & Dohme Zyklohexylsulfone als gamma-sekretase-inhibitoren
KR20070104480A (ko) 2003-05-27 2007-10-25 포레스트 래보러토리즈, 인코포레이티드 우울증 및 그 밖의 기분장애의 치료를 위한 nmda수용체 길항제 및 선택적 세로토닌 재흡수 억제제의 배합물
AU2003902828A0 (en) 2003-06-05 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
AU2004247068A1 (en) 2003-06-06 2004-12-23 Merck & Co., Inc. Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
AU2003902946A0 (en) 2003-06-12 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
JP4579239B2 (ja) 2003-06-17 2010-11-10 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病の治療または予防するためのジペプチジルペプチダーゼ阻害剤としてのシクロヘキシルグリシン誘導体
BRPI0411509A (pt) 2003-06-20 2006-07-25 Hoffmann La Roche compostos, processo para a sua manufatura, composições farmacêuticas que compreendem os mesmos, método para tratamento e/ou profilaxia de enfermidades que estão associadas com dpp-iv e sua utilização
MXPA05013904A (es) 2003-06-20 2006-02-24 Hoffmann La Roche Derivados de pirido[2,1-a] isoquinolinas como inhibidores de dipeptidil-peptidasa iv(dpp-iv).
CN100430377C (zh) 2003-06-30 2008-11-05 麦克公司 用于治疗阿尔茨海默病的N-烷基苯基甲酰胺β分泌酶抑制剂
EP1643986A4 (de) 2003-07-01 2009-04-08 Merck & Co Inc Phenylcarboxylat-beta-secretase-hemmer zur behandlung von morbus alzheimer
WO2005007614A1 (en) 2003-07-03 2005-01-27 The Government Of The United States Of America As Represented By The Secretary, Department Of Health And Human Services 6011 Monoamine oxidase inhibitors
US20050036994A1 (en) 2003-07-16 2005-02-17 Koichiro Mihara Compounds and methods for downregulating the effects of TGF-beta
EP1671129A1 (de) 2003-07-21 2006-06-21 Angiogenetics Sweden AB Verbindungen und verfahren zur förderung der angiogenese durch verwendung eines gamma-secretase-inhibitors oder hemmen des gamma-secretase-wegs
EP1660058A2 (de) 2003-07-28 2006-05-31 Merz Pharma GmbH & Co. KGaA Verwendung von 1-amino-alkylcyclohexan-verbindungen bei der behandlung von schmerzüberempfindlichkeit
US7259160B2 (en) 2003-07-31 2007-08-21 Merck & Co., Inc. Hexahydrodiazepinones as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
GB0318447D0 (en) 2003-08-05 2003-09-10 Merck Sharp & Dohme Therapeutic agents
CA2535619A1 (en) 2003-08-13 2005-02-24 Takeda Pharmaceutical Company Limited 4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors
EP1656359B1 (de) 2003-08-14 2012-11-28 Merck Sharp & Dohme Corp. Makrocyclische beta-sekretaseinhibitoren zur behandlung der alzheimer-krankheit
WO2005023762A1 (en) 2003-09-04 2005-03-17 Abbott Laboratories Pyrrolidine-2-carbonitrile derivatives and their use as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
JP2007505121A (ja) 2003-09-08 2007-03-08 武田薬品工業株式会社 ジペプチジルぺプチダーゼ阻害剤
EP1697342A2 (de) 2003-09-08 2006-09-06 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitoren
TW200530157A (en) 2003-09-09 2005-09-16 Japan Tobacco Inc Dipeptidyl peptidase iv inhibitor
GB0322140D0 (en) 2003-09-22 2003-10-22 Pfizer Ltd Combinations
WO2005030731A1 (en) 2003-09-24 2005-04-07 Merck Sharp & Dohme Limited Gamma-secretase inhibitors
US7829597B2 (en) 2003-10-03 2010-11-09 Merck, Sharp & Dohme, Inc. Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease
EP1682540A1 (de) 2003-10-06 2006-07-26 Alangudi Sankaranarayanan Azolidincarbonitrile und ihre verwendung als dpp-iv hemmer
AU2004283803B2 (en) 2003-10-06 2010-06-24 F. Hoffmann-La Roche Ag Substituted dibenzo-azepine and benzo-diazepine derivatives useful as gamma-secretase inhibitors
MXPA06004038A (es) 2003-10-08 2006-06-28 Pfizer Compuestos de 1-'2-(4-hidroxifenil)-2-hidroxietil-piperidin-4-ol como antagonsitas del receptor n-metil-d-aspartato.
CN1867324A (zh) 2003-10-15 2006-11-22 前体生物药物股份公司 谷氨酰胺酰基环化酶效应物和谷氨酸环化酶效应物的应用
DK1675591T3 (da) 2003-10-16 2011-11-14 Neurosearch As Farmaceutisk sammensætning omfattende en monoamin-neurotransmitter-genoptagelseshæmmer og en acetylcholinesterase-hæmmer
GB0324236D0 (en) 2003-10-16 2003-11-19 Astrazeneca Ab Chemical compounds
TW200519105A (en) 2003-10-20 2005-06-16 Lg Life Science Ltd Novel inhibitors of DPP-IV, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent
WO2005079779A1 (en) 2003-10-22 2005-09-01 Merz Pharma Gmbh & Co. Kgaa THE USE OF 1-AMINOCYCLOHEXANE DERIVATIVES TO MODIFY DEPOSITION OF FIBRILLOGENIC Aß PEPTIDES IN AMYLOIDOPATHIES
US20050171112A1 (en) 2003-11-03 2005-08-04 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
US7667044B2 (en) 2003-11-03 2010-02-23 Probiodrug Ag Compounds for the treatment of neurological disorders
WO2005049027A2 (en) 2003-11-03 2005-06-02 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
EP1824846A2 (de) 2003-11-03 2007-08-29 Probiodrug AG Neue verbindungen zur behandlung neurologischer erkrankungen
CA2541212A1 (en) 2003-11-04 2005-05-19 Wallace T. Ashton Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
RU2367666C2 (ru) 2003-11-11 2009-09-20 Ф.Хоффманн-Ля Рош Аг Производные фосфиновой кислоты, ингибиторы бета-секретазы, предназначенные для лечения болезни альцгеймера
WO2005047297A1 (en) 2003-11-12 2005-05-26 Phenomix Corporation Heterocyclic boronic acid compounds
JP4576386B2 (ja) 2003-11-24 2010-11-04 メルク・シャープ・エンド・ドーム・コーポレイション アルツハイマー病治療用のベンジルエーテルおよびベンジルアミノ系β−セクレターゼ阻害薬
DE10355304A1 (de) 2003-11-27 2005-06-23 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 8-(Piperazin-1-yl)-und 8-([1,4]Diazepan-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
UY28650A1 (es) 2003-12-05 2005-02-28 Forest Laboratories Memantina para la prevencion o disminucion de la conducta suicida y para el tratamiento de la depresion mayor asociada con esta conducta
EP1541148A1 (de) 2003-12-09 2005-06-15 Graffinity Pharmaceuticals Aktiengesellschaft Dpp-iv inhibitoren
EP1541143A1 (de) 2003-12-09 2005-06-15 Graffinity Pharmaceuticals Aktiengesellschaft Dpp-iv inhibitoren
WO2005058849A1 (en) 2003-12-15 2005-06-30 Glenmark Pharmaceuticals Ltd. New dipeptidyl peptidase in inhibitors; process for their preparation and compositions containing them
AU2004311749A1 (en) 2003-12-19 2005-07-21 Merck & Co., Inc. Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease
WO2005070429A1 (en) 2004-01-22 2005-08-04 Neurosearch A/S Pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor and an n-methyl-d-aspartate (nmda) receptors antagonist
US20050245617A1 (en) 2004-01-29 2005-11-03 Meyerson Laurence R Methods and compositions for the treatment of CNS-related conditions
WO2005075426A1 (en) 2004-02-03 2005-08-18 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
BRPI0507485A (pt) 2004-02-05 2007-07-10 Probiodrug Ag inibidores novos de glutaminil ciclase
WO2005079756A2 (en) 2004-02-13 2005-09-01 Neuromolecular, Inc. Combination of a nmda receptor antagonist and an anti-depressive drug mao-inhibitor or a gadph-inhibitor for the treatment of psychiatric conditions
US20050182044A1 (en) 2004-02-17 2005-08-18 Bruinsma Gosse B. Combinatorial therapy with an acetylcholinesterase inhibitor and (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3,-b]indol-5-yl phenylcarbamate
JP4733058B2 (ja) 2004-02-18 2011-07-27 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 8−[3−アミノ−ピペリジン−1−イル]−キサンチン、その製造及びそのdpp−ivインヒビターの形態での使用
RU2379315C2 (ru) 2004-02-23 2010-01-20 Трастиз Оф Тафтс Колледж Ингибиторы дипептидилпептидазы iv
EP1593671A1 (de) 2004-03-05 2005-11-09 Graffinity Pharmaceuticals AG DPP-IV Inhibitoren
WO2005087235A1 (en) 2004-03-09 2005-09-22 National Health Research Institutes Pyrrolidine compounds
GEP20094679B (en) 2004-03-15 2009-05-10 Takeda Pharmaceuticals Co Dipeptidyl peptidase inhibitors
US20070213388A1 (en) 2004-03-19 2007-09-13 Bruinsma Gosse B Acetylcholinesterase Inhibitors and N-Methyl-D-Aspartate Antagonists Useful in the Treatment of of Cognitive Disorders
WO2005095339A1 (en) 2004-03-31 2005-10-13 Pfizer Products Inc. Dicyanopyrrolidines as dipeptidyl peptidase iv inhibitors
WO2005097103A2 (en) 2004-04-01 2005-10-20 Axys Pharmaceuticals, Inc. Diabetes and metabolic syndrome therapy utilizing cathepsin b inhibitors
JP2007531742A (ja) 2004-04-05 2007-11-08 シェーリング コーポレイション 新規のγセクレターゼインヒビター
WO2005103020A1 (en) 2004-04-20 2005-11-03 Merck & Co., Inc. 1,3,5-substituted phenyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
US7968571B2 (en) 2004-04-20 2011-06-28 Merck, Sharp & Dohme, Corp. 2,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's Disease
WO2005102390A2 (en) 2004-04-22 2005-11-03 Pfizer Japan, Inc. Combinations comprising alpha-2-delta ligands and nmda receptor antagonists
WO2005105133A2 (en) 2004-04-23 2005-11-10 Massachusetts Eye And Ear Infirmary Methods and compositions for preserving the viability of photoreceptor cells
CN1950349A (zh) 2004-05-04 2007-04-18 默克公司 作为用于治疗或预防糖尿病的二肽基肽酶-ⅳ抑制剂的1,2,4-噁二唑衍生物
CA2566108C (en) 2004-05-12 2010-04-06 Pfizer Products Inc. Proline derivatives and their use as dipeptidyl peptidase iv inhibitors
EP1756040A4 (de) 2004-05-13 2008-04-30 Merck & Co Inc Als -sekretaseinhibitoren zur behandlung von alzheimer-krankheit geeignete phenylcarbonsäureamidverbindungen
CN1960990A (zh) 2004-05-18 2007-05-09 默克公司 作为用于治疗或预防糖尿病的二肽基肽酶-ⅳ抑制剂的环己基丙氨酸衍生物
EP1598341A1 (de) 2004-05-21 2005-11-23 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV-Hemmer
US7687638B2 (en) 2004-06-04 2010-03-30 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
EP1604989A1 (de) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV-Hemmer
EP1604662A1 (de) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft 1-[(3R)-Amino-4-(2-fluoro-phenyl)-butyl]-pyrrolidin-(2R)-carbonsäure-benzylamine-Derivate und verwandte Verbindungen als Dipeptidyl-Peptidase IV (DPP-IV) Inhibitoren zur Behandlung von Typ 2 Diabetes Mellitus
EP1604980A1 (de) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV-Hemmer
CN1968924B (zh) 2004-06-15 2011-08-03 默沙东公司 作为β-分泌酶抑制剂用于治疗阿尔茨海默氏病的吡咯烷-3-基化合物
GB0413389D0 (en) 2004-06-16 2004-07-21 Astrazeneca Ab Chemical compounds
WO2006009886A1 (en) 2004-06-21 2006-01-26 Merck & Co., Inc. Aminocyclohexanes as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2006085961A2 (en) 2004-06-30 2006-08-17 Centocor, Inc. Anti-mcp-1 antibodies, compositions, methods and uses
EP1789404B1 (de) 2004-06-30 2010-03-24 Schering Corporation Substituierte n-arylsulfonylheterocyclische amine als gamma-sekretase-hemmer
EP1778220A1 (de) 2004-07-12 2007-05-02 Phenomix Corporation Eingezwängte cyano-verbindungen
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
ATE491693T1 (de) 2004-07-22 2011-01-15 Schering Corp Substituierte amide als inhibitoren der beta- sekretase
JP2008508289A (ja) 2004-07-28 2008-03-21 シェーリング コーポレイション 大環状βセクレターゼ阻害剤
HUP0401523A3 (en) 2004-07-29 2007-05-02 Richter Gedeon Vegyeszet Indole-2-carboxamide derivatives, pharmaceutical compositions containing them and process for producing them
EP1623983A1 (de) 2004-08-05 2006-02-08 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft Heterozyklische Verbindungen verwendbar als DDP-IV-Inhibitoren
ATE473742T1 (de) 2004-08-23 2010-07-15 Merck Sharp & Dohme Kondensierte triazolderivate als dipeptidylpeptidase-iv-hemmer zur behandlung bzw. prävention von diabetes
AU2005276631A1 (en) 2004-08-25 2006-03-02 Santhera Pharmaceuticals (Schweiz) Ag Alpha-keto carbonyl calpain inhibitors
CA2578006A1 (en) 2004-08-25 2006-03-02 Santhera Pharmaceuticals (Schweiz) Ag Alpha-keto carbonyl calpain inhibitors
US7388007B2 (en) 2004-08-26 2008-06-17 Bristol-Myers Squibb Company Gamma-lactams as beta-secretase inhibitors
WO2006029850A1 (en) 2004-09-14 2006-03-23 The Genetics Company, Inc. Hydrazone derivatives and their use as beta secretase inhibitors
CA2580238A1 (en) 2004-09-17 2006-03-30 Comentis, Inc. Bicyclic compounds which inhibit beta-secretase activity and methods of use thereof
US7659289B2 (en) 2004-09-17 2010-02-09 Comentis, Inc. Hydroxyethylene-based β-secretase inhibitors and use thereof
AU2005292134B2 (en) 2004-10-01 2010-12-23 Merck Sharp & Dohme Corp. Aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
WO2006042103A2 (en) 2004-10-05 2006-04-20 Axys Pharmaceuticals, Inc. Reversible inhibitors of cathepsin b
CA2580266A1 (en) 2004-10-08 2006-04-20 Novartis Ag Combination of organic compounds
US9186345B2 (en) 2004-10-12 2015-11-17 Hakon Hakonarson Method of treating skin diseases
CA2583342A1 (en) 2004-10-13 2006-04-27 Merck And Co., Inc. Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of alzhermer's disease
US20090004302A1 (en) 2004-10-15 2009-01-01 Biopharmacopae Design International Inc. Methods and Therapeutic Compositions Comprising Plant Extracts for the Treatment of Cancer
US20090253752A1 (en) 2004-10-25 2009-10-08 Bryan Burkey Combination of dpp-iv inhibitor, ppar antidiabetic and metmorfin
GB0423673D0 (en) 2004-10-25 2004-11-24 Glaxo Group Ltd Compounds
US7932275B2 (en) 2004-10-29 2011-04-26 Merck, Sharp & Dohme Corp. 2-aminopyridine compounds useful as β-secretase inhibitors for the treatment of alzheimer's disease
CA2587083A1 (en) 2004-11-17 2006-05-26 Merck & Co., Inc. Macrocyclic tertiary amine beta-secretase inhibitors for the treatment of alzheimer's disease
CA2587256A1 (en) 2004-11-23 2006-06-01 Merck & Co., Inc. Macrocyclic aminopyridyl beta-secretase inhibitors for the treatment of alzheimer's disease
US8394837B2 (en) 2004-11-23 2013-03-12 Merck, Sharp & Dohme, Corp. 2,3,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
RU2404750C2 (ru) 2004-11-23 2010-11-27 Адамас Фармасьютикалс, Инк. Композиция, содержащая основу или покрытие для замедленного высвобождения и антагонист nmda рецептора, способ введения такого nmda антагониста субъекту
CA2588296A1 (en) 2004-11-24 2006-06-01 Neuromolecular Pharmaceuticals, Inc. Composition comprising an nmda receptor antagonist and levodopa and use thereof for treating neurological disease
AU2005309606B2 (en) 2004-11-29 2011-01-06 Merck Sharp & Dohme Corp. Fused aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
BRPI0516667A (pt) 2004-11-30 2008-09-16 Hoffmann La Roche compostos, processo para a manufatura dos mesmos, composições farmacêuticas que os compreendem, método para o tratamento e/ou profilaxia de enfermidades que estão associadas com dpp-iv e utilização desses compostos
WO2006060473A2 (en) 2004-12-03 2006-06-08 Mucosal Therapeutics Llc Methods of treatment of injured or diseased joints with lubricin compositions
GB0427267D0 (en) 2004-12-13 2005-01-12 Maria Teresa De Magistris Peptide adjuvants
WO2006064189A1 (en) * 2004-12-14 2006-06-22 Astrazeneca Ab Oxadiazole derivatives as dgat inhibitors
WO2006064375A2 (en) * 2004-12-16 2006-06-22 Ab Science Aminoaryl substituted five-membered ring heterocyclic compounds for the treatment of diseases
US7411093B2 (en) 2004-12-20 2008-08-12 Hoffman-La Roche Inc. Aminocycloalkanes as DPP-IV inhibitors
RU2396257C2 (ru) 2004-12-20 2010-08-10 Ф.Хоффманн-Ля Рош Аг Производные 4-аминопиперидина
US7872124B2 (en) 2004-12-21 2011-01-18 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
AU2005322611A1 (en) 2004-12-23 2006-07-06 Voyager Pharmaceutical Corporation Leuprolide acetate and acetylcholinesterase inhibitors or NMDA receptor antagonists for the treatment of Alzheimer's disease
WO2006070394A1 (en) 2004-12-28 2006-07-06 Council Of Scientific And Industrial Research Substituted carbamic acid quinolin-6-yl esters useful as acetylcholinesterase inhibitors
EP1855673A4 (de) 2005-01-06 2008-03-12 Merck & Co Inc Heilmittelkombinationstherapie und pharmazeutische zusammensetzungen zur behandlung von entzündungen
CA2594943A1 (en) 2005-01-19 2006-07-27 Merck & Co., Inc. Aminomethyl beta-secretase inhibitors for the treatment of alzheimer's disease
US20060216331A1 (en) 2005-02-28 2006-09-28 Lines Thomas C Composition for treating mental health disorders
EP1858501A1 (de) 2005-03-07 2007-11-28 Michael Hermanussen Nmda-rezeptor-antagonisten bei der medizinischen intervention von stoffwechselerkrankungen
US7745470B2 (en) 2005-03-10 2010-06-29 Bristol-Myers Squibb Company Isophthalates as beta-secretase inhibitors
FR2883285B1 (fr) 2005-03-17 2007-05-18 Sanofi Aventis Sa Sel besylate de la 7-(2-(4-(3-trifluoromethyl-phenyl) -1,2,3,6-tetrahudro-pyrid-1-yl)ethyl) isoquinoleine, sa preparation et son utilisation en therapeutique
PA8675801A1 (es) 2005-05-19 2006-12-07 Centocor Inc Anticuerpos anti-mcp-1, composiciones, metodos y usos
NZ575727A (en) 2006-09-21 2011-12-22 Probiodrug Ag Novel genes related to glutaminyl cyclase

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JP2010511013A (ja) 2010-04-08
SI2091948T1 (sl) 2012-07-31
WO2008065141A1 (en) 2008-06-05
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US20080214620A1 (en) 2008-09-04
DK2091948T3 (da) 2012-07-23

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