[go: up one dir, main page]

TW200626148A - Heterocyclic derivatives and their use as therapeutic agents - Google Patents

Heterocyclic derivatives and their use as therapeutic agents

Info

Publication number
TW200626148A
TW200626148A TW094132549A TW94132549A TW200626148A TW 200626148 A TW200626148 A TW 200626148A TW 094132549 A TW094132549 A TW 094132549A TW 94132549 A TW94132549 A TW 94132549A TW 200626148 A TW200626148 A TW 200626148A
Authority
TW
Taiwan
Prior art keywords
therapeutic agents
heterocyclic derivatives
mammal
formula
disclosed
Prior art date
Application number
TW094132549A
Other languages
English (en)
Inventor
Rajender Kamboj
Jian-Min Fu
Vishnumurthy Kodumuru
shi-feng Liu
Kashinath Sadalapure
Nagasree Chakka
Duanjie Hou
Shaoyi Sun
Original Assignee
Xenon Pharmaceuticals Inc
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 Xenon Pharmaceuticals Inc filed Critical Xenon Pharmaceuticals Inc
Publication of TW200626148A publication Critical patent/TW200626148A/zh

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • 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
    • A61P17/04Antipruritics
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08Radicals containing only hydrogen and carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
TW094132549A 2004-09-20 2005-09-20 Heterocyclic derivatives and their use as therapeutic agents TW200626148A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US61164604P 2004-09-20 2004-09-20

Publications (1)

Publication Number Publication Date
TW200626148A true TW200626148A (en) 2006-08-01

Family

ID=35623357

Family Applications (1)

Application Number Title Priority Date Filing Date
TW094132549A TW200626148A (en) 2004-09-20 2005-09-20 Heterocyclic derivatives and their use as therapeutic agents

Country Status (11)

Country Link
US (2) US7547698B2 (zh)
EP (1) EP1804792A1 (zh)
JP (2) JP5080256B2 (zh)
CN (1) CN101083986A (zh)
AR (1) AR051294A1 (zh)
AU (1) AU2005286790A1 (zh)
BR (1) BRPI0515477A (zh)
CA (1) CA2580781A1 (zh)
MX (1) MX2007003329A (zh)
TW (1) TW200626148A (zh)
WO (1) WO2006034312A1 (zh)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7517884B2 (en) 1998-03-30 2009-04-14 Kalypsys Inc. Sulfonyl-substituted bicyclic compounds as modulators of PPAR
US20050119251A1 (en) * 2001-12-21 2005-06-02 Jian-Min Fu Nicotinamide derivatives and their use as therapeutic agents
AR051094A1 (es) 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
MX2007003330A (es) * 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
CA2580844A1 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as mediators of stearoyl-coa desaturase
WO2006034441A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
US7919496B2 (en) 2004-09-20 2011-04-05 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-CoA desaturase enzymes
CN101084211A (zh) 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为治疗剂的用途
JP4958785B2 (ja) 2004-09-20 2012-06-20 ゼノン・ファーマシューティカルズ・インコーポレイテッド 複素環誘導体およびステアロイル−CoAデサチュラーゼインヒビターとしてのそれらの使用
US7767677B2 (en) 2004-09-20 2010-08-03 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
DK1805158T3 (en) 2004-10-29 2018-08-06 Kalypsys Inc SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS MODULATORS OF PPAR
EP2540296A1 (en) 2005-06-03 2013-01-02 Xenon Pharmaceuticals Inc. Arminothiazole derivatives as human stearoyl-coa desaturase inhibitors
AU2006255465A1 (en) * 2005-06-09 2006-12-14 Merck Frosst Canada Ltd Azacyclohexane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
EP1940815B1 (en) 2005-10-25 2018-08-15 Kalypsys, Inc. Salts of modulators of ppar and methods of treating metabolic disorders
CA2632936A1 (en) 2005-12-20 2007-06-28 Merck Frosst Canada Ltd. Heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
MX2008015229A (es) 2006-06-05 2008-12-12 Novartis Ag Compuestos organicos.
RU2009110254A (ru) 2006-08-24 2010-09-27 Новартис АГ (CH) Производные 2-(пиразин-2-ил)тиазола и 2-(1н-пиразол-3-ил)тиразола и связанные с ним соединения в качестве ингибиторов стеароил-соа десатуразы для лечения метаболических, сердечно-сосудистых и других нарушений
US20090325956A1 (en) * 2006-10-13 2009-12-31 Takahiko Taniguchi Aromatic amine derivative and use thereof
TW200826936A (en) 2006-12-01 2008-07-01 Merck Frosst Canada Ltd Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
AR064965A1 (es) 2007-01-26 2009-05-06 Merck Frosst Canada Inc Derivados de azacicloalcanos como inhibidores de estearoil - coenzima a delta -9 desaturasa
WO2008096746A1 (ja) 2007-02-06 2008-08-14 Takeda Pharmaceutical Company Limited スピロ化合物およびその用途
EP2152719A4 (en) * 2007-05-23 2011-01-19 Merck Frosst Canada Ltd BICYCLIC HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME-A-DELTA-9-DESATURASE
WO2008157844A1 (en) 2007-06-21 2008-12-24 Forest Laboratories Holdings Limited Novel piperazine derivatives as inhibitors of stearoyl-coa desaturase
TW200920372A (en) * 2007-07-13 2009-05-16 Genelabs Tech Inc Anti-viral compounds, compositions, and methods of use
JP2010533658A (ja) * 2007-07-20 2010-10-28 メルク フロスト カナダ リミテツド ステアロイル補酵素aデルタ−9デサチュラーゼ阻害剤としての二環性へテロ芳香族化合物
WO2009124259A1 (en) * 2008-04-04 2009-10-08 Cv Therapeutics, Inc. Pyrrolotriazinone derivatives for use as stearoyl coa desaturase inhibitors
WO2009137201A1 (en) 2008-04-04 2009-11-12 Cv Therapeutics, Inc. Triazolopyridinone derivatives for use as stearoyl coa desaturase inhibitors
JP5597210B2 (ja) 2009-02-17 2014-10-01 メルク カナダ インコーポレイテッド ステアロイル−補酵素aデルタ−9デサチュラーゼの阻害剤として有用な新規スピロ化合物
US8383643B2 (en) 2009-07-28 2013-02-26 Merck Canada Inc. Spiro compounds useful as inhibitors of stearoyl-coenzyme A delta-9 desaturase
EP2475367A1 (en) 2009-09-10 2012-07-18 Centre National De La Recherche Scientifique NOVEL INHIBITORS OF STEAROYL-CoA-DESATURASE-1 AND THEIR USES
JP5541454B2 (ja) * 2009-09-16 2014-07-09 Jsr株式会社 液晶配向剤および液晶表示素子
BR112012028445A2 (pt) 2010-05-06 2016-07-19 Bristol Myers Squibb Co compostos de heteroarila bicíclica como moduladores de gpr119
CN103096893B (zh) 2010-06-04 2016-05-04 阿尔巴尼分子研究公司 甘氨酸转运体-1抑制剂、其制备方法及其用途
AU2011270754B2 (en) 2010-06-25 2015-04-23 The U.S.A., As Represented By The Secretary, Department Of Health And Human Services Methods of treatment using sterculic acid
EP2766000A2 (en) 2011-10-15 2014-08-20 F.Hoffmann-La Roche Ag Scd1 antagonists for treating cancer
WO2013134546A1 (en) 2012-03-07 2013-09-12 Mayo Foundation For Medical Education And Research Methods and materials for treating cancer
WO2013175474A2 (en) 2012-05-22 2013-11-28 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Selective inhibitors of undifferentiated cells
RU2015122615A (ru) * 2012-12-03 2017-01-10 Ф. Хоффманн-Ля Рош Аг Замещенные соединения амида изоксазола в качестве ингибиторов стеароил-коа-десатуразы 1 (скд1)
SG11201505878UA (en) 2013-02-19 2015-09-29 Pfizer Azabenzimidazole compounds as inhibitors of pde4 isozymes for the treatment of cns and other disorders
JP6713982B2 (ja) 2014-07-24 2020-06-24 ファイザー・インク ピラゾロピリミジン化合物
ES2733502T3 (es) 2014-08-06 2019-11-29 Pfizer Compuestos de imidazopiridazina
EP3177292B1 (en) 2014-08-07 2020-11-25 Mayo Foundation for Medical Education and Research Compounds and methods for treating cancer
CN117777121A (zh) 2016-10-24 2024-03-29 詹森药业有限公司 化合物及其用途
KR20190108118A (ko) 2017-01-06 2019-09-23 유마니티 테라퓨틱스, 인크. 신경계 장애의 치료를 위한 방법
WO2019084157A1 (en) 2017-10-24 2019-05-02 Yumanity Therapeutics, Inc. COMPOUNDS AND USES THEREOF
JP7517992B2 (ja) 2018-03-23 2024-07-17 ヤンセン ファーマシューティカ エヌ.ベー. 化合物及びその使用
BR112021014583A2 (pt) 2019-01-24 2021-10-05 Yumanity Therapeutics, Inc. Compostos e utilizações dos mesmos
EA202192047A1 (ru) 2019-11-13 2021-12-08 Юманити Терапьютикс, Инк. Соединения и их применение
AU2021275233A1 (en) * 2020-05-22 2022-12-08 Vanderbilt University Competitive and noncompetitive inhibitors of the muscarinic acetylcholine receptor M5

Family Cites Families (99)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2985657A (en) * 1959-10-12 1961-05-23 Paul A J Janssen 1-(aroylalkyl)-4-heterocyclylpiperazines
US3830924A (en) * 1966-12-23 1974-08-20 American Cyanamid Co Substituted nitroimidazolyl-thiadiazoles as growth promoting agents
GB1290145A (zh) * 1969-01-21 1972-09-20
AT340933B (de) * 1973-08-20 1978-01-10 Thomae Gmbh Dr K Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze
DE2516040C2 (de) * 1974-06-10 1984-12-20 Dr. Karl Thomae Gmbh, 7950 Biberach Benzimidazole, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel
US4247551A (en) * 1979-09-17 1981-01-27 Gruppo Lepetit S.P.A. N-Pyrrolyl-pyridazineamines and their use as antihypertensive agents
FI70411C (fi) * 1980-12-29 1986-09-19 Pfizer Foerfarande foer framstaellning av nya antihypertensiva 4-amino-6,7-dimetoxi-2-piperazinokinazolin derivat
CH653021A5 (fr) * 1981-04-24 1985-12-13 Delalande Sa Derives piperidino, piperazino et homopiperazino, n-substitues par un groupe heterocyclique aromatique, leur procede de preparation et composition therapeutique les contenant.
DE3139970A1 (de) * 1981-10-08 1983-04-28 Boehringer Mannheim Gmbh, 6800 Mannheim Neue carbonsaeurederivate, verfahren zu ihrer herstellung sowie diese verbindungen enthaltende arzneimittel
US4439606A (en) * 1982-05-06 1984-03-27 American Cyanamid Company Antiatherosclerotic 1-piperazinecarbonyl compounds
US5001125A (en) * 1984-03-26 1991-03-19 Janssen Pharmaceutica N.V. Anti-virally active pyridazinamines
DE3827599A1 (de) * 1988-08-13 1990-02-15 Hoechst Ag Verwendung von optisch aktiven tetrahydrofuran-2-carbonsaeureestern als dotierstoffe in fluessigkristallmischungen, diese enthaltende fluessigkristallmischungen und neue optisch aktive tetrahydrofuran-2-carbonsaeureester
EP0471201A1 (de) * 1990-07-21 1992-02-19 Hoechst Aktiengesellschaft Neue Oxazolidinon-Derivate und ihre Verwendung als Dotierstoffe in Flüssigkristallmischungen
EP0520292A1 (de) * 1991-06-19 1992-12-30 Hoechst Aktiengesellschaft Chirale Azetidinon-Derivate und ihre Verwendung als Dotierstoffe in Flüssigkristallmischungen
EP0524146A1 (de) * 1991-07-19 1993-01-20 Ciba-Geigy Ag Aminosubstituierte Piperazinderivate
DE4124942A1 (de) * 1991-07-27 1993-01-28 Thomae Gmbh Dr K 5-gliedrige heterocyclen, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
JPH05345780A (ja) * 1991-12-24 1993-12-27 Kumiai Chem Ind Co Ltd ピリミジンまたはトリアジン誘導体及び除草剤
DE4236106A1 (de) * 1992-10-26 1994-04-28 Hoechst Ag Azaaromatische Verbindungen, Verfahren zu ihrer Herstellung und ihre Verwendung in flüssigkristallinen Mischungen
US5494908A (en) * 1992-11-23 1996-02-27 Hoechst-Roussel Pharmaceutical Incorporated Substituted 3-(aminoalkylamino)-1,2-benzisoxazoles and related compounds
US5380726A (en) * 1993-01-15 1995-01-10 Ciba-Geigy Corporation Substituted dialkylthio ethers
US5547605A (en) * 1993-12-15 1996-08-20 Hoechst Aktiengesellschaft 2-Aryloxytetrafluoropropionic esters, process for their preparation, and their use in liquid-crystalline mixtures
US5571811A (en) * 1994-07-12 1996-11-05 Janssen Pharmaceutica N.V. Sulfonamide derivatives of azolones
US5637592A (en) * 1994-07-12 1997-06-10 Janssen Pharmaceutica N.V. Acyl derivatives of azolones
US5668148A (en) * 1995-04-20 1997-09-16 Merck & Co., Inc. Alpha1a adrenergic receptor antagonists
DE19517025A1 (de) * 1995-05-10 1996-11-14 Hoechst Ag Trifluortetrahydroisochinolin-Derivate und ihre Verwendung in flüssigkristallinen Mischungen
DE19517038A1 (de) * 1995-05-10 1996-11-14 Hoechst Ag 1,8-Difluorisochinolinderivate und ihre Verwendung in flüssigkristallinen Mischungen
DE19517051A1 (de) * 1995-05-10 1996-11-14 Hoechst Ag 1-Fluor-6,7-dihydro-5H-isochinolin-8-on-Derivate und ihre Verwendung in flüssigkristallinen Mischungen
DE19517056A1 (de) * 1995-05-10 1996-11-14 Hoechst Ag 1-Fluor-5,6,7,8-tetrahydroisochinolin-Derivate und ihre Verwendung in flüssigkristallinen Mischungen
DE19517060A1 (de) * 1995-05-10 1996-11-14 Hoechst Ag 1-Fluorisochinolinderivate und ihre Verwendung in flüssigkristallinen Mischungen
ZA969622B (en) * 1995-12-13 1998-05-15 Upjohn Co Oxazolidinone antibacterial agents having a six-membered heteroaromatic ring.
EP0929553B1 (en) * 1996-10-02 2005-03-16 Novartis AG Pyrimidine derivatives and processes for the preparation thereof
DE59707681D1 (de) * 1996-10-28 2002-08-14 Rolic Ag Zug Vernetzbare, photoaktive Silanderivate
ES2125206B1 (es) * 1997-07-21 1999-11-16 Esteve Labor Dr Derivados de acil-piperazinil-pirimidinas, su preparacion y su aplicacion como medicamentos.
AU3819099A (en) * 1998-04-20 1999-11-08 Basf Aktiengesellschaft Heterocyclically substituted amides used as calpain inhibitors
US6562847B1 (en) * 1998-08-25 2003-05-13 Ortho-Mcneil Pharmaceutical, Inc. Pyridyl ethers and thioethers as ligands for nicotinic acetylcholine receptor and its therapeutic application
KR20010087738A (ko) * 1998-10-21 2001-09-21 다케다 야쿠힌 고교 가부시키가이샤 축합 피리다진 유도체, 이의 제조 방법 및 용도
FR2792314B1 (fr) * 1999-04-15 2001-06-01 Adir Nouveaux composes aminotriazoles, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
GB9912413D0 (en) * 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
US6127382A (en) * 1999-08-16 2000-10-03 Allergan Sales, Inc. Amines substituted with a tetrahydroquinolinyl group an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
US6677452B1 (en) * 1999-09-30 2004-01-13 Lion Bioscience Ag Pyridine carboxamide or sulfonamide derivatives and combinatorial libraries thereof
US6987001B2 (en) 2000-02-24 2006-01-17 Xenon Pharmaceuticals Inc. Methods and compositions using stearoyl-CoA desaturase to identify triglyceride reducing therapeutic agents
US20020045613A1 (en) * 2000-04-27 2002-04-18 Heinz Pauls 1-aroyl-piperidinyl benzamidines
ES2292607T3 (es) * 2000-07-27 2008-03-16 Eli Lilly And Company Amidas heterociclicas sustituidas.
JP2004505975A (ja) * 2000-08-08 2004-02-26 サノフィ−サンテラボ ベンズイミダゾール誘導体、その製造及び治療上の使用
US6738895B1 (en) * 2000-08-31 2004-05-18 Micron Technology, Inc. Method and system for substantially registerless processing
ATE402262T1 (de) 2000-09-26 2008-08-15 Xenon Pharmaceuticals Inc Verfahren und zusammensetzungen, die eine stearoyl-coa desuturase-hscd5 verwenden
FR2815032B1 (fr) * 2000-10-10 2003-08-08 Pf Medicament Nouveaux derives d'aminophenyle piperazine ou d'amino phenyle piperide inhibiteurs de proteines prenyl transferase ainsi que leurs preparations
DE10060412A1 (de) * 2000-12-05 2002-06-06 Bayer Ag DELTA1-Pyrroline
EE200300439A (et) * 2001-03-15 2003-12-15 Astrazeneca Ab Metalloproteinaasi inhibiitorid
FR2823209B1 (fr) * 2001-04-04 2003-12-12 Fournier Lab Sa Nouvelles thiohydantoines et leur utilisation en therapeutique
US6911447B2 (en) * 2001-04-25 2005-06-28 The Procter & Gamble Company Melanocortin receptor ligands
PL367205A1 (en) * 2001-06-15 2005-02-21 Yamanouchi Pharmaceutical Co, Ltd. Phenylpyridine carbonyl piperazine derivative
JP2004536113A (ja) * 2001-07-03 2004-12-02 カイロン コーポレイション チロシンキナーゼおよびセリン/スレオニンキナーゼのインヒビターとしてのインダゾールベンズイミダゾール化合物
US7115607B2 (en) * 2001-07-25 2006-10-03 Amgen Inc. Substituted piperazinyl amides and methods of use
FR2829926B1 (fr) * 2001-09-26 2004-10-01 Oreal Composition pour la teinture des fibres keratiniques comprenant un colorant diazoique dicationique particulier
US6916812B2 (en) * 2001-10-09 2005-07-12 Bristol-Myers Squibb Company Alpha-aminoamide derivatives as melanocortin agonists
US6824707B2 (en) * 2001-10-23 2004-11-30 Clariant International Ltd. Active matrix liquid crystal device and smectic liquid crystal mixture
JPWO2003037862A1 (ja) * 2001-10-30 2005-02-17 日本新薬株式会社 アミド誘導体及び医薬
GB0127008D0 (en) 2001-11-09 2002-01-02 Novartis Ag Organic compounds
US6620811B2 (en) * 2001-11-19 2003-09-16 Hoffmann-La Roche Inc. Isonicotin- and nicotinamide derivatives of benzothiazoles
FR2833261B1 (fr) * 2001-12-06 2004-07-02 Yang Ji Chemical Company Ltd Nouveaux composes inhibiteurs specifiques de la phospholipase a2 secretee non pancreatique humaine du groupe ii
US20050119251A1 (en) * 2001-12-21 2005-06-02 Jian-Min Fu Nicotinamide derivatives and their use as therapeutic agents
US7390813B1 (en) * 2001-12-21 2008-06-24 Xenon Pharmaceuticals Inc. Pyridylpiperazines and aminonicotinamides and their use as therapeutic agents
US20030166932A1 (en) * 2002-01-04 2003-09-04 Beard Richard L. Amines substituted with a dihydronaphthalenyl, chromenyl, or thiochromenyl group, an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
IL162859A0 (en) 2002-02-05 2005-11-20 Novo Nordisk As Novel aryl-and heteroarylpiperazines
DE10217006A1 (de) * 2002-04-16 2003-11-06 Merck Patent Gmbh Substituierte Indole
JP2005289816A (ja) * 2002-05-14 2005-10-20 Banyu Pharmaceut Co Ltd ベンズイミダゾール誘導体
EP1551811A1 (en) 2002-10-17 2005-07-13 Amgen Inc. Benzimidazole derivatives and their use as vanilloid receptor ligands
US20040097492A1 (en) * 2002-11-01 2004-05-20 Pratt John K Anti-infective agents
DE10259382A1 (de) * 2002-12-18 2004-07-01 Abbott Gmbh & Co. Kg 3-Substituierte 3,4-Dihydro-thieno[2,3-d]pyrimidin-4-on-Derivate, ihre Herstellung und Verwendung
US20050130989A1 (en) * 2003-01-28 2005-06-16 Aventis Pharma S. A. N-arylheteroaromatic products compositions containing them and use thereof
US6861422B2 (en) * 2003-02-26 2005-03-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
PE20050226A1 (es) * 2003-06-04 2005-05-18 Aventis Pharma Sa Productos aril-heteroaromaticos y composiciones que los contienen
CN1812981A (zh) * 2003-06-27 2006-08-02 万有制药株式会社 杂芳氧基含氮饱和杂环衍生物
FR2857966A1 (fr) * 2003-07-24 2005-01-28 Aventis Pharma Sa Produits aryl-heteroaromatiques, compositions les contenant et utilisation
WO2005011654A2 (en) * 2003-07-29 2005-02-10 Xenon Pharmaceuticals Inc. Pyridyl derivatives and their use as therapeutic agents
WO2005011657A2 (en) 2003-07-30 2005-02-10 Xenon Pharmaceuticals Inc. Piperazine derivatives and their use as therapeutic agents
AU2004261252C1 (en) * 2003-07-30 2009-09-17 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
US7754711B2 (en) * 2003-07-30 2010-07-13 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
DK1656361T3 (da) * 2003-08-11 2008-05-05 Hoffmann La Roche Piperazin med OR-substitueret phenylgruppe og anvendelse deraf som GLYT1-inhibitorer
JPWO2005021550A1 (ja) * 2003-08-29 2006-10-26 大日本住友製薬株式会社 二環性ピラゾール誘導体
CN100522171C (zh) * 2003-09-09 2009-08-05 弗·哈夫曼-拉罗切有限公司 作为甘氨酸摄取抑制剂、用于治疗精神病的1-苯甲酰基哌嗪衍生物
US7399765B2 (en) * 2003-09-19 2008-07-15 Abbott Laboratories Substituted diazabicycloalkane derivatives
US20050124660A1 (en) * 2003-10-27 2005-06-09 Jochen Antel Novel medical uses of compounds showing CB1-antagonistic activity and combination treatment involving said compounds
US7345043B2 (en) * 2004-04-01 2008-03-18 Miikana Therapeutics Inhibitors of histone deacetylase
AR048523A1 (es) * 2004-04-07 2006-05-03 Kalypsys Inc Compuestos con estructura de aril sulfonamida y sulfonilo como moduladores de ppar y metodos para tratar trastornos metabolicos
FR2868780B1 (fr) * 2004-04-13 2008-10-17 Sanofi Synthelabo Derives de la 1-amino-phthalazine, leur preparation et leur application en therapeutique
AR051094A1 (es) * 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
JP4958785B2 (ja) * 2004-09-20 2012-06-20 ゼノン・ファーマシューティカルズ・インコーポレイテッド 複素環誘導体およびステアロイル−CoAデサチュラーゼインヒビターとしてのそれらの使用
US7919496B2 (en) * 2004-09-20 2011-04-05 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-CoA desaturase enzymes
WO2006034441A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
CA2580844A1 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as mediators of stearoyl-coa desaturase
US7767677B2 (en) * 2004-09-20 2010-08-03 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
CN101084211A (zh) * 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为治疗剂的用途
MX2007003330A (es) * 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
MX2007008189A (es) * 2005-01-07 2007-08-07 Hoffmann La Roche Derivados de [4-(heteroaril)piperazin-1-il]-(fenilo 2,5-sustituido) metanona como inhibidores del transportador de glicina 1(glyt-1) para el tratamiento de trastornos neurologicos y neuropsiquiatricos.
EP2540296A1 (en) * 2005-06-03 2013-01-02 Xenon Pharmaceuticals Inc. Arminothiazole derivatives as human stearoyl-coa desaturase inhibitors
US7662819B2 (en) * 2007-04-09 2010-02-16 Gilead Palo Alto, Inc. Pteridinone derivatives for use as stearoyl CoA desaturase inhibitors
UA100192C2 (en) * 2008-11-11 2012-11-26 УАЙТ ЭлЭлСи 1-(arylsulfonyl)-4-(piperazin-1-yl)-1h-benzimidazoles as 5-hydroxytryptamine-6 ligands

Also Published As

Publication number Publication date
CN101083986A (zh) 2007-12-05
CA2580781A1 (en) 2006-03-30
US20070219211A1 (en) 2007-09-20
JP2008513498A (ja) 2008-05-01
EP1804792A1 (en) 2007-07-11
MX2007003329A (es) 2007-06-05
US7547698B2 (en) 2009-06-16
JP2012193188A (ja) 2012-10-11
AR051294A1 (es) 2007-01-03
WO2006034312A1 (en) 2006-03-30
US20090291957A1 (en) 2009-11-26
JP5080256B2 (ja) 2012-11-21
AU2005286790A1 (en) 2006-03-30
BRPI0515477A (pt) 2008-07-22
US20110009414A9 (en) 2011-01-13

Similar Documents

Publication Publication Date Title
TW200626148A (en) Heterocyclic derivatives and their use as therapeutic agents
TW200626592A (en) Heterocyclic derivatives and their use as therapeutic agents
TW200626139A (en) Heterocyclic derivatives and their use as therapeutic agents
TW200626155A (en) Heterocyclic derivatives and their use as therapeutic agents
TW200626153A (en) Heterocyclic derivatives and their use as therapeutic agents
TW200624427A (en) Heterocyclic derivatives and their use as therapeutic agents
TW200626154A (en) Heterocyclic derivatives and their use as therapeutic agents
TW200626572A (en) Heterocyclic derivatives and their use as therapeutic agents
TW200626138A (en) Heterocyclic derivatives and their use as therapeutic agents
TW200638935A (en) Pyridazine derivatives and their use as therapeutic agents
TNSN06032A1 (en) Pyridazine derivatives and their use as therapeutic agents
TNSN06034A1 (en) Pyridazine derivatives and their use as therapeutic agents
IL173397A0 (en) Pyridyl derivatives and their use as therapeutic agents
TNSN06033A1 (en) Piperazine derivatives and their use as therapeutic agents
MX2007000028A (es) Derivados de nicotinamida y su uso como agentes terapeuticos.
MXPA05012466A (es) Derivados de quinolina como inhibidores de fosfodiesterasa.
TNSN06036A1 (en) Pyridyl derivatives and their use as therapeutic agents
WO2007046868A3 (en) Thiazolidine derivatives and their uses as therapeutic agents
WO2007046867A3 (en) Piperidine derivatives and their uses as therapeutic agents
WO2006125194A3 (en) Piperazine derivatives and their uses as therapeutic agents
MY144229A (en) Pyridazine derivatives and their use as therapeutic agents
JO2829B1 (en) Pyridazine derivatives and their use as therapeutic agents