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PE20140610A1 - Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina - Google Patents

Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina

Info

Publication number
PE20140610A1
PE20140610A1 PE2013002562A PE2013002562A PE20140610A1 PE 20140610 A1 PE20140610 A1 PE 20140610A1 PE 2013002562 A PE2013002562 A PE 2013002562A PE 2013002562 A PE2013002562 A PE 2013002562A PE 20140610 A1 PE20140610 A1 PE 20140610A1
Authority
PE
Peru
Prior art keywords
alkyl
cycloalkyl
oxo
phenyl
piperidine
Prior art date
Application number
PE2013002562A
Other languages
English (en)
Inventor
Ameet Vijay Ambarkhane
Gurdip Bhalay
Martin Beckett
James Dale
Ahmed Hamadi
Alessandro Mazzacani
Jeffrey Mckenna
Cristopher Thomson
Original Assignee
Novartis 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46317469&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20140610(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20140610A1 publication Critical patent/PE20140610A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/10Laxatives
    • 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
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • 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
    • C07D487/10Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Nutrition Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE PIPERIDINA 3-ESPIROCICLICA DE FORMULA (I) DONDE X1 ES (CRx1H)n, NRx1 O N, EN DONDE Rx1 ES H O ALQUILO(C1-C6); n ES 0 O 1; X2 ES CH, N O C; m ES 1 O 2; p ES 0 O 1; Y ES NR1 U O, EN DONDE R1 ES H, ALQUILO(C1-C6), HALOALQUILO(C1-C6), CICLOALQUILO(C3-C6), ENTRE OTROS; R2a ES -A-FENILO, -A-HETEROARILO DE 5 A 6 MIEMBROS, -A-CICLOALQUILO(C5-C6), ENTRE OTROS, EN DONDE A ES UN ENLACE, ENTRE OTROS; R2b ES H O ALQUILO(C1-C4); R3 Y R4 SON CADA UNO H, ALQUILO(C1-C6), CICLOALQUILO(C3-C6), ENTRE OTROS; R6 Y R7 SON CADA UNO H, ALQUILO(C1-C6), HIDROXIALQUILO(C1-C6) O HALOALQUILO(C1-C6); R5 ES FENILO, HETEROARILO DE 5 A 6 MIEMBROS; CICLOALQUILO(C3-C6), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-AMINO-N-[(R)-1-BENCILOXIMETIL-2-(2-METIL-1-OXO-4-FENIL-2,7-DIAZA-ESPIRO[4.5]DEC-7-IL)-2-OXO-ETIL]-2-METIL-PROPIONAMIDA; 2-AMINO-N-((2R)-3-(BENCILOXI)-1-(4-(4-FLUOROFENIL)-2-METIL-1-OXO-2,7-DIAZAESPIRO[4.5]DECAN-7-IL)-1-OXOPROPAN-2-IL)-2-METILPROPANAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON AGONISTAS DE RECEPTORES DE LA GHRELINA SIENDO UTILES EN EL TRATAMIENTO DE GASTROPARESIA, DISPEPSIA FUNCIONAL, SINDROME DEL INTESTINO CORTO
PE2013002562A 2011-05-27 2012-05-25 Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina PE20140610A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161490848P 2011-05-27 2011-05-27
US201161560960P 2011-11-17 2011-11-17
US201261642116P 2012-05-03 2012-05-03

Publications (1)

Publication Number Publication Date
PE20140610A1 true PE20140610A1 (es) 2014-05-31

Family

ID=46317469

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2013002562A PE20140610A1 (es) 2011-05-27 2012-05-25 Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina

Country Status (22)

Country Link
US (2) US8546416B2 (es)
EP (1) EP2714690A1 (es)
JP (1) JP2014515369A (es)
KR (1) KR20140023399A (es)
CN (1) CN103562206A (es)
AP (1) AP2013007234A0 (es)
AR (1) AR086554A1 (es)
AU (1) AU2012264305A1 (es)
BR (1) BR112013030391A2 (es)
CA (1) CA2835916A1 (es)
CL (1) CL2013003211A1 (es)
CO (1) CO6811856A2 (es)
CR (1) CR20130625A (es)
EA (1) EA201391797A1 (es)
IL (1) IL229320A0 (es)
MX (1) MX355072B (es)
PE (1) PE20140610A1 (es)
PH (1) PH12013502204A1 (es)
SG (1) SG194616A1 (es)
TW (1) TW201302749A (es)
UY (1) UY34094A (es)
WO (1) WO2012164473A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2867043A1 (en) * 2012-05-03 2013-11-07 Novartis Ag L-malate salt of 2,7-diaza-spiro[4.5]dec-7-yle derivatives and crystalline forms thereof as ghrelin receptor agonists
CN104768544B (zh) * 2012-08-09 2017-06-16 迪纳米斯治疗公司 包括葡甲胺或其盐的组合物在制备减少或预防甘油三酯水平增加的药物中的应用
WO2015154023A1 (en) 2014-04-04 2015-10-08 X-Rx Discovery, Inc. Substituted spirocydic inhibitors of autotaxin
WO2016067638A1 (en) * 2014-10-31 2016-05-06 Raqualia Pharma Inc. Tetrahydropyrazolopyridine derivatives as ghrelin receptor agonists
CA3062880A1 (en) * 2017-05-12 2018-11-15 Millennium Pharmaceuticals, Inc. Treatment of gastroparesis with triazaspiro[4.5]decanone
CN111175387B (zh) * 2018-11-13 2022-06-07 成都康弘药业集团股份有限公司 一种米那普仑异构体的检测方法
CN113125583B (zh) * 2019-12-30 2022-06-21 成都百裕制药股份有限公司 一种注射用泮托拉唑钠中基因毒性杂质含量的检测方法
WO2022109363A1 (en) * 2020-11-23 2022-05-27 Enanta Pharmaceuticals, Inc. Novel spiropyrrolidine derived antiviral agents
CN116806150A (zh) * 2021-01-05 2023-09-26 载度思生命科学有限公司 新的自分泌运动因子抑制剂
US12398147B2 (en) 2021-05-11 2025-08-26 Enanta Pharmaceuticals, Inc. Macrocyclic spiropyrrolidine derived antiviral agents
US12479854B2 (en) 2021-07-29 2025-11-25 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
WO2023107417A1 (en) 2021-12-08 2023-06-15 Enanta Pharmaceuticals, Inc. Heterocyclic antiviral agents
US11993600B2 (en) * 2021-12-08 2024-05-28 Enanta Pharmaceuticals, Inc. Saturated spirocyclics as antiviral agents
WO2023196307A1 (en) 2022-04-05 2023-10-12 Enanta Pharmaceuticals, Inc. Novel spiropyrrolidine derived antiviral agents

Family Cites Families (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SK282166B6 (sk) * 1992-12-11 2001-11-06 Merck & Co., Inc. Spiropiperidínové deriváty, spôsob ich výroby a farmaceutický prostriedok s ich obsahom
US5578593A (en) 1992-12-11 1996-11-26 Merck & Co., Inc. Spiro piperidines and homologs promote release of growth hormone
CA2220055C (en) 1995-05-08 2001-04-24 Pfizer Inc. Dipeptides which promote release of growth hormone
US6403599B1 (en) 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
AU7169696A (en) * 1995-09-26 1997-04-17 Merck & Co., Inc. 3-spirolactam, 3-spiroamino, 3-spirolactone and 3-spirobenzopyran piperidines and pyrrolidines promote release of growth hormone
WO1997044042A1 (en) 1996-05-22 1997-11-27 Arch Development Corporation Sleep quality improvement using a growth hormone secretagogue
UA64751C2 (uk) 1997-06-25 2004-03-15 Пфайзер Продактс Інк. Спосіб лікування інсулінової толерантності речовинами, які посилюють секрецію гормону росту (варіанти) та фармацевтична композиція (варіанти)
ES2283055T3 (es) * 1997-06-25 2007-10-16 Pfizer Inc. Derivados dipeptidos como secretagogos de la hormona de crecimiento.
TW544448B (en) 1997-07-11 2003-08-01 Novartis Ag Pyridine derivatives
ZA987385B (en) 1997-08-19 2000-04-18 Lilly Co Eli Growth hormone secretagogues.
US6329342B1 (en) 1997-08-19 2001-12-11 Eli Lilly And Company Treatment of congestive heart failure with growth hormone secretagogues
GB9802251D0 (en) 1998-02-03 1998-04-01 Ciba Geigy Ag Organic compounds
WO2000020001A1 (en) 1998-10-02 2000-04-13 Novartis Ag Mglur5 antagonists for the treatment of pain and anxiety
US6194578B1 (en) 1998-11-20 2001-02-27 Pfizer Inc. Dipeptide derivatives
SI1004583T1 (en) 1998-11-23 2004-12-31 Pfizer Products Inc. Process and hydantoin intermediates for the synthesis of growth hormone secretagogues
GB9913079D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
DOP2001000154A (es) 2000-05-25 2002-05-15 Pfizer Prod Inc Combinación de secretagogos de hormona del crecimiento y antidepresivos
DE60140285D1 (de) 2000-05-31 2009-12-10 Pfizer Prod Inc Verwendung von Wachstumshormonsekretagoga zur Förderung der Beweglichkeit des Verdauungstrakts
IL143690A0 (en) 2000-06-19 2002-04-21 Pfizer Prod Inc The use of growth hormone secretagogues to treat systemic lupus erythematosus and inflammatory bowel disease
GB0028702D0 (en) 2000-11-24 2001-01-10 Novartis Ag Organic compounds
PL363907A1 (en) 2001-03-26 2004-11-29 Novartis Ag Fused pyridine derivatives for use as vanilloid receptor antagonists for treating pain.
CA2443721A1 (en) 2001-05-14 2002-11-21 Novartis Ag Sulfonamide derivatives
JP3894035B2 (ja) 2001-07-04 2007-03-14 東レ株式会社 炭素繊維強化基材、それからなるプリフォームおよび複合材料
TW200306839A (en) 2002-02-06 2003-12-01 Novartis Ag Quinazolinone derivatives and their use as CB agonists
AU2003218273A1 (en) 2002-04-10 2003-10-27 Eli Lilly And Company Stereoselective process for the synthesis of (d)-2-amino-5-phenylpentanoic or alkyl ester thereof
US6696468B2 (en) 2002-05-16 2004-02-24 Dainippon Pharmaceutical Co., Ltd. (s)-4-amino-5-chloro-2-methoxy-n-[1-[1-(2-tetrahydrofuryl-carbonyl)-4-piperidinylmethyl]-4-piperidinyl]benzamide, process for the preparation thereof, pharmaceutical composition containing the same, and intermediate therefor
SE0201940D0 (sv) 2002-06-20 2002-06-20 Astrazeneca Ab New combination II
DOP2003000703A (es) 2002-09-20 2004-03-31 Pfizer Compuestos de imidazopiradina como agonistas del receptor 5-ht4
GB0223730D0 (en) 2002-10-11 2002-11-20 Novartis Ag Organic compounds
PE20040844A1 (es) 2002-11-26 2004-12-30 Novartis Ag Acidos fenilaceticos y derivados como inhibidores de la cox-2
GB0302876D0 (en) 2003-02-07 2003-03-12 Novartis Ag Organic compounds
EP1631260A2 (en) 2003-02-28 2006-03-08 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
JP2004277318A (ja) 2003-03-14 2004-10-07 Dainippon Pharmaceut Co Ltd 1−(1−置換カルボニル−4−ピペリジニルメチル)ピペリジン誘導体およびそれを含有する医薬組成物
JP2004277319A (ja) 2003-03-14 2004-10-07 Dainippon Pharmaceut Co Ltd 1−(4−ピペリジニルメチル)ピペリジニルアミド誘導体およびそれを含有する医薬組成物
EA009215B1 (ru) 2003-05-21 2007-12-28 Прозидион Лимитед Ингибиторы гликогенфосфорилазы, представляющие собой амиды пирролопиридин-2-карбоновых кислот
EP1505064A1 (en) 2003-08-05 2005-02-09 Bayer HealthCare AG 2-Aminopyrimidine derivatives
CN1835753A (zh) 2003-08-12 2006-09-20 弗·哈夫曼-拉罗切有限公司 作为促皮质释放素(cfr)拮抗剂的螺-取代的四氢喹唑啉
EP1656354B1 (en) 2003-08-12 2007-09-26 F.Hoffmann-La Roche Ag Tetrahydroquinazoline derivatives as cfr antagonists
WO2005068448A1 (en) 2003-08-29 2005-07-28 Ionix Pharmaceuticals Limited Sulfonamides antagonising n-type calcium channels
AU2004274403A1 (en) 2003-09-03 2005-03-31 Aventis Pharmaceuticals Inc. 5-aryl-Pyrazolo(4,3-d)pyrimidines, pyridines, and pyrazines and related compounds
KR100738784B1 (ko) 2003-09-03 2007-07-12 화이자 인코포레이티드 5-ht4 수용체 효능 활성을 갖는 벤즈이미다졸론
JP2005082508A (ja) 2003-09-05 2005-03-31 Dainippon Pharmaceut Co Ltd 2−アルコキシ−6−アミノ−5−ハロゲノ−n−(1−置換−4−ピペリジニル)ピリジン−3−カルボキサミド誘導体およびそれを含有する医薬組成物
AP2006003559A0 (en) 2003-09-05 2006-04-30 Neurogen Corp Ventis Pharmaceuticals Inc Heteroaryl fused pyridines, pyrazines and pyrimidines as CRF 1 receptor ligands
CA2538026A1 (en) 2003-09-09 2005-03-24 Ono Pharmaceutical Co., Ltd. Crf antagonists and heterobicyclic compounds
GB0322612D0 (en) 2003-09-26 2003-10-29 Novartis Ag Organic compounds
JP2005104896A (ja) 2003-09-30 2005-04-21 Dainippon Pharmaceut Co Ltd 2−アルコキシ−6−アミノ−5−ハロゲノピリジン−3−カルボキサミド誘導体およびそれを含有する医薬組成物
AU2004278372B2 (en) 2003-09-30 2010-02-18 Janssen Pharmaceutica N.V. Quinoxaline compounds
BRPI0414918A (pt) 2003-09-30 2006-11-07 Janssen Pharmaceutica Nv compostos de benzoimidazola
CA2543707A1 (en) 2003-10-31 2005-05-19 Takeda Pharmaceutical Company Limited Nitrogen-containing fused heterocyclic compounds
NZ547044A (en) 2003-11-10 2010-05-28 Merck Sharp & Dohme Substituted triazoles as sodium channel blockers
US7208596B2 (en) 2003-11-25 2007-04-24 Bristol-Myers Squibb Pharma Company Processes for the preparation of pyrazolo[1,5-a]-1,3,5-triazines and intermediates thereof
WO2005054239A1 (en) 2003-12-05 2005-06-16 Bayer Healthcare Ag 2-aminopyrimidine derivatives
US7211568B2 (en) 2003-12-18 2007-05-01 Kosan Biosciences Incorporated 9-Desoxoerythromycin compounds as prokinetic agents
JP2005206590A (ja) 2003-12-25 2005-08-04 Mitsubishi Pharma Corp ナトリウムチャネルサイト2選択的阻害剤
DK2194053T3 (da) 2004-01-07 2013-07-01 Armetheon Inc Methoxypiperidinderivater til brug i behandling af gastrointestinale forstyrrelser og forstyrrelser i centralnervesystemet.
EP1713797B1 (en) 2004-01-29 2008-03-05 Pfizer, Inc. 1-isopropyl-2-oxo-1,2-dihydropyridine-3-carboxamide derivatives having 5-ht4 receptor agonistic activity
TW200533348A (en) 2004-02-18 2005-10-16 Theravance Inc Indazole-carboxamide compounds as 5-ht4 receptor agonists
WO2005092882A1 (en) 2004-03-01 2005-10-06 Pfizer Japan, Inc. 4-amino-5-halogeno-benzamide derivatives as 5-ht4 receptor agonists for the treatment of gastrointestinal, cns, neurological and cardiovascular disorders
EP1574478A1 (de) 2004-03-08 2005-09-14 Solvay Fluor GmbH Herstellung von Carbonylfluorid
EP1737297B1 (en) 2004-03-25 2012-12-19 Janssen Pharmaceutica NV Imidazole compounds
US20080280873A1 (en) 2004-03-29 2008-11-13 Jun Liang Biaryl Substituted Pyrazinones as Sodium Channel Blockers
TWI351282B (en) 2004-04-07 2011-11-01 Theravance Inc Quinolinone-carboxamide compounds as 5-ht4 recepto
US20080015196A1 (en) 2004-04-16 2008-01-17 Neurogen Corporation Imidazopyrazines, Imidazopyridines, and Imidazopyrimidines as Crf1 Receptor Ligands
GB0412769D0 (en) 2004-06-08 2004-07-07 Novartis Ag Organic compounds
GB0412768D0 (en) 2004-06-08 2004-07-07 Novartis Ag Organic compounds
AU2005254800B2 (en) 2004-06-15 2010-12-09 Pfizer Inc. Benzimidazolone carboxylic acid derivatives
SE0401653D0 (sv) 2004-06-24 2004-06-24 Astrazeneca Ab New compounds
WO2006023757A2 (en) 2004-08-19 2006-03-02 University Of Virginia Patent Foundation Novel tricyclic, bicyclic, monocyclic, and acyclic amines as potent sodium channel blocking agents
GB0420424D0 (en) 2004-09-14 2004-10-20 Ionix Pharmaceuticals Ltd Therapeutic compounds
WO2006038594A1 (ja) 2004-10-04 2006-04-13 Ono Pharmaceutical Co., Ltd. N型カルシウムチャネル阻害薬
GB0519957D0 (en) 2005-09-30 2005-11-09 Sb Pharmco Inc Chemical compound
ES2332808T3 (es) 2004-11-05 2010-02-12 Theravance, Inc. Compuestos agonistas del receptor 5-ht4.
JP5042028B2 (ja) 2004-11-05 2012-10-03 セラヴァンス, インコーポレーテッド キノリノン−カルボキサミド化合物
AU2005303893A1 (en) 2004-11-11 2006-05-18 Argenta Discovery Ltd Pyrimidine compounds as histamine modulators
US20060111416A1 (en) 2004-11-24 2006-05-25 Lane Charlotte A L Octahydropyrrolo[3,4-C]pyrrole derivatives
MX2007007818A (es) 2004-12-22 2007-09-11 Theravance Inc Compuestos de indazol-carboxamida.
EP1818061A1 (en) 2005-12-02 2007-08-15 Charite-Universitätsmedizin Berlin Use of ghrelin for stimulating hair growth
US7601844B2 (en) 2006-01-27 2009-10-13 Bristol-Myers Squibb Company Piperidinyl derivatives as modulators of chemokine receptor activity
AU2008241532A1 (en) 2007-02-09 2008-10-30 Tranzyme Pharma, Inc. Macrocyclic ghrelin receptor modulators and methods of using the same
US7994203B2 (en) 2008-08-06 2011-08-09 Novartis Ag Organic compounds
US8273900B2 (en) 2008-08-07 2012-09-25 Novartis Ag Organic compounds
EP2482813A4 (en) 2009-09-30 2013-02-27 Tranzyme Pharma Inc SALTS, SOLVATES AND PHARMACEUTICAL COMPOSITIONS OF GHRELIN RECEPTOR MACROCYCLIC AGONISTS AND METHODS OF USE

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SG194616A1 (en) 2013-12-30
US20130331369A1 (en) 2013-12-12
AR086554A1 (es) 2014-01-08
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CR20130625A (es) 2014-02-04
EA201391797A1 (ru) 2014-04-30
MX355072B (es) 2018-04-04
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WO2012164473A1 (en) 2012-12-06
US8546416B2 (en) 2013-10-01
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JP2014515369A (ja) 2014-06-30
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AU2012264305A1 (en) 2013-11-21

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