CN102753527B - 用作crf受体拮抗剂的环己基酰胺衍生物 - Google Patents

用作crf受体拮抗剂的环己基酰胺衍生物 Download PDF

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CN102753527B
CN102753527B CN201180007786.4A CN201180007786A CN102753527B CN 102753527 B CN102753527 B CN 102753527B CN 201180007786 A CN201180007786 A CN 201180007786A CN 102753527 B CN102753527 B CN 102753527B
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chloro
methyl
trans
cyclohexyl
ylmethyl
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CN102753527A (zh
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D·贝蒂
I·布鲁斯
A-O·科尔森
A·J·库尔尚
T·夏普
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Novartis AG
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Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10703722B2 (en) 2010-04-27 2020-07-07 Calcimedica, Inc. Compounds that modulate intracellular calcium
RS65839B1 (sr) 2014-01-21 2024-09-30 Neurocrine Biosciences Inc Crf1 receptor antagonisti za tretman kongenitalne adrenalne hiperplazije
EP3778595B1 (en) 2015-02-27 2021-08-25 Calcimedica, Inc. Pancreatitis treatment
CA2995094A1 (en) 2015-08-07 2017-02-16 Calcimedica, Inc. Use of crac channel inhibitors for the treatment of stroke and traumatic brain injury
JOP20170153A1 (ar) 2016-07-15 2019-01-30 Lilly Co Eli نظائر urocortin-2 جديدة معدلة بحمض دهني لعلاج داء السكري وأمراض الكلى المزمنة
EP3661500B1 (en) 2017-07-31 2026-01-07 Novartis AG Use of mavoglurant in the reduction of cocaine use or in preventing relapse into cocaine use
EP3716972A4 (en) 2017-11-29 2021-08-25 The Rockefeller University PYRANOPYRAZOLE AND PYRAZOLOPYRIDINE IMMUNOMODULATORS FOR THE TREATMENT OF AUTOIMMUNE DISEASES
WO2019118785A2 (en) 2017-12-13 2019-06-20 Praxis Biotech LLC Inhibitors of integrated stress response pathway
EP3774739B1 (en) * 2018-04-09 2022-05-11 RaQualia Pharma Inc. Fused cyclic urea derivatives as crhr2 antagonist
WO2019236710A1 (en) 2018-06-05 2019-12-12 Praxis Biotech LLC Inhibitors of integrated stress response pathway
US20220023266A1 (en) 2018-12-07 2022-01-27 Neurocrine Biosciences, Inc. Crf1 receptor antagonist, pharmaceutical formulations and solid forms thereof for the treatment of congenital adrenal hyperplasia
MX2021015210A (es) * 2019-06-12 2022-01-18 Praxis Biotech LLC Inhibidores de la via de respuesta al estres integrada.
JP2022536663A (ja) 2019-06-12 2022-08-18 プラクシス バイオテック エルエルシー 統合的ストレス応答経路のモジュレーター
JP7623365B2 (ja) 2019-09-27 2025-01-28 ニューロクライン バイオサイエンシーズ，インコーポレイテッド Ｃｒｆ受容体アンタゴニストおよび使用方法
TW202140480A (zh) * 2020-01-15 2021-11-01 日商拉夸里亞創藥股份有限公司 作為crhr2拮抗劑之螺雜環衍生物
JP2023528537A (ja) 2020-03-20 2023-07-04 カルシメディカ，インク． 急性肺傷害及び急性呼吸窮迫症候群を処置するための方法及び組成物
JP2023545256A (ja) 2020-09-30 2023-10-27 ラクオリア創薬株式会社 Ｃｒｈｒ２拮抗薬としての３－ヒドロキシオキシインドール誘導体
CA3198798A1 (en) 2020-11-13 2022-05-19 Kenneth Stauderman Improved synthesis of crac channel inhibitors

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006044958A1 (en) * 2004-10-19 2006-04-27 Sb Pharmco Puerto Rico Inc. Pyrazolo [1,5-alpha] pyrimidinyl derivatives useful as corticotropin-releasing factor (crf) receptor antagonists
CN1938309A (zh) * 2003-12-22 2007-03-28 Sb药物波多黎各公司 Crf受体拮抗剂及其相关方法
WO2008086047A1 (en) * 2007-01-03 2008-07-17 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
WO2009146539A1 (en) * 2008-06-02 2009-12-10 Neuromed Pharmaceuticals Ltd. 4-(aminomethyl)cyclohexanamine derivatives as calcium channel blockers
WO2009151800A1 (en) * 2008-05-07 2009-12-17 Merck & Co., Inc. Soluble epoxide hydrolase inhibitors, compositions containing such compounds and methods of treatment
WO2009153720A1 (en) * 2008-06-18 2009-12-23 Pfizer Limited Nicotinamide derivatives
WO2010015655A1 (en) * 2008-08-07 2010-02-11 Novartis Ag Cyclohexyl amide derivatives and their use as crf-1 receptor antagonists

Family Cites Families (191)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
US6403599B1 (en) 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
TW544448B (en) 1997-07-11 2003-08-01 Novartis Ag Pyridine derivatives
GB9802251D0 (en) 1998-02-03 1998-04-01 Ciba Geigy Ag Organic compounds
ID29095A (id) 1998-10-02 2001-07-26 Novartis Ag Cs Antagonis mglur5 untuk pengobatan rasa sakit dan kegelisahan
US6525203B1 (en) 1999-03-12 2003-02-25 Bristol-Myers Squibb Company Heterocyclic aromatic compounds useful as growth hormone secretagogues
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.
CA2905585C (en) 2001-03-29 2020-02-18 Bausch Health Ireland Limited Guanylate cyclase receptor agonists for the treatment and/or prevention of cancer or polyps
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
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
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
GB0302876D0 (en) 2003-02-07 2003-03-12 Novartis Ag Organic compounds
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
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
JP2007501866A (ja) 2003-06-13 2007-02-01 マイクロバイア インコーポレイテッド 胃腸疾患の治療のための方法および組成物
US7491695B2 (en) 2003-06-18 2009-02-17 Tranzyme Pharma Inc. Methods of using macrocyclic modulators of the ghrelin receptor
US7476653B2 (en) 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
EP1505064A1 (en) 2003-08-05 2005-02-09 Bayer HealthCare AG 2-Aminopyrimidine derivatives
JP2007501822A (ja) 2003-08-12 2007-02-01 エフ．ホフマン−ラ　ロシュ　アーゲー コルチコトロピン放出性因子（ｃｒｆ）アンタゴニストとしてのスピロ置換テトラヒドロキナゾリン
ES2293317T3 (es) 2003-08-12 2008-03-16 F. Hoffmann-La Roche Ag Derivados de tetrahidroquinazolina com antagonistas de cfr.
WO2005068448A1 (en) 2003-08-29 2005-07-28 Ionix Pharmaceuticals Limited Sulfonamides antagonising n-type calcium channels
CA2537916A1 (en) 2003-09-03 2005-03-31 Neurogen Corporation 5-aryl-pyrazolo[4,3-d]pyrimidines, pyridines, and pyrazines and related compounds
UA86204C2 (uk) 2003-09-03 2009-04-10 Пфайзер Инк. Сполуки бензімідазолону, які мають 5-нт4 рецепторну агоністичну активність
AR045582A1 (es) 2003-09-05 2005-11-02 Neurogen Corp Piridinas pirazinas y pirimidinas heteroarilo fusionadas como ligandos receptores de crf1
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
AU2004272437A1 (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
KR20060111466A (ko) 2003-09-30 2006-10-27 얀센 파마슈티카 엔.브이. 퀴녹살린 화합물
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
RU2006110561A (ru) 2003-09-30 2007-10-10 Янссен Фармацевтика Н.В. (Be) Соединения бензоимидазола
EP1677791A4 (en) 2003-10-31 2007-08-15 Takeda Pharmaceutical NITROGENIC CONDENSED HETEROCYCLIC COMPOUNDS
EP1677789A1 (en) 2003-10-31 2006-07-12 AstraZeneca AB Alkynes i
CN1922156A (zh) 2003-11-10 2007-02-28 默克公司 作为钠通道阻断剂的取代的三唑
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
CA2548039A1 (en) 2003-12-19 2005-07-21 Astrazenca Ab 5-fluoro-, chloro- and cyano-pyridin-2-yl-tetrazoles as ligands of the metabotropic glutamate receptor-5
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
RU2374244C2 (ru) 2004-01-07 2009-11-27 Арикс Терапьютикс Стереоизомерные соединения и способы лечения желудочно-кишечных расстройств и расстройств центральной нервной системы
TW200530181A (en) 2004-01-13 2005-09-16 Bristol Myers Squibb Co Heterocyclic compounds useful as growth hormone secretagogues
DE602005005167T2 (de) 2004-01-29 2009-04-30 Pfizer Inc. 1-isopropyl-2-oxo-1,2-dihydropyridin-3-carbonsäureamidderivate mit agonistischer wirkung am 5-ht4-rezeptor
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
US20070185100A1 (en) 2004-02-18 2007-08-09 Astrazeneca Ab Poly-heterocyclic compounds and their use as metabotropic glutamate receptor antagonists
TW200531694A (en) 2004-02-18 2005-10-01 Astrazeneca Ab Acetylinic piperazine compounds and their use as metabotropic glutamate receptor antagonists
DE602005008558D1 (de) 2004-02-18 2008-09-11 Astrazeneca Ab Kondensierte heterocyclische verbindungen und deren verwendung als antagonisten des metabotropen reznkungen
WO2005080356A1 (en) 2004-02-18 2005-09-01 Astrazeneca Ab Tetrazole compounds and their use as metabotropic glutamate receptor antagonits
US7585881B2 (en) 2004-02-18 2009-09-08 Astrazeneca Ab Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
RU2006127575A (ru) 2004-02-18 2008-03-27 Астразенека Аб (Se) Соединение триазола и их применение в качестве антагонистов метаботропного рецептора глутамата
TW200533348A (en) 2004-02-18 2005-10-16 Theravance Inc Indazole-carboxamide compounds as 5-ht4 receptor agonists
TW200538108A (en) 2004-02-19 2005-12-01 Astrazeneca Ab Fused heterocyclic compounds and their use as metabotropic glutamate receptor antagonists
TW200538180A (en) 2004-02-20 2005-12-01 Astrazeneca Ab New compounds
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
US7087749B2 (en) 2004-03-11 2006-08-08 Adolor Corporation Substituted piperidine compounds and methods of their use
AU2005226729B2 (en) 2004-03-25 2010-01-28 Janssen Pharmaceutica N.V. Imidazole compounds
EP1732564A1 (en) 2004-03-29 2006-12-20 Merck & Co., Inc. Biaryl substituted pyrazinones as sodium channel blockers
WO2005097788A2 (en) 2004-04-02 2005-10-20 Elixir Pharmaceuticals, Inc. Sulfonamides and uses thereof
TWI351282B (en) 2004-04-07 2011-11-01 Theravance Inc Quinolinone-carboxamide compounds as 5-ht4 recepto
EP1734820A4 (en) 2004-04-16 2008-01-23 Neurogen Corp Imidazopyrrazine, imidazopyridine, and imidazo-pyrimidine 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
CA2569654C (en) 2004-06-15 2010-12-21 Pfizer Inc. Benzimidazolone carboxylic acid derivatives
PE20060526A1 (es) 2004-06-15 2006-07-13 Schering Corp Compuestos triciclicos como antagonistas de mglur1
SE0401653D0 (sv) 2004-06-24 2004-06-24 Astrazeneca Ab New compounds
WO2006006740A1 (ja) 2004-07-14 2006-01-19 Japan Tobacco Inc. ３−アミノベンズアミド化合物及びバニロイド受容体１型(ｖｒ１)活性阻害剤
MX2007000480A (es) 2004-07-15 2007-03-29 Japan Tobacco Inc Compuesto de benzamida fusionado e inhibidor de actividad de receptor de vainilloide 1.
US20080039430A1 (en) 2004-07-19 2008-02-14 Ali Ouaissi Pharmaceutical Compositions For The Treatment Of Leishmaniasis
PE20060574A1 (es) 2004-07-28 2006-06-24 Glaxo Group Ltd Derivados de arilpiperazina sulfonamida como agonistas de los receptores de secretagogos de la hormona del crecimiento (ghs)
ITMI20041566A1 (it) 2004-07-30 2004-10-30 Indena Spa "trpv1 agonisti, formulazioni che li contengono e loro usi"
WO2006016218A1 (en) 2004-08-03 2006-02-16 Pfizer Japan Inc. Aryl or heteroaryl carbonyl derivatives derivatives useful as vanilloid receptor 1 (vr1) antagonists
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
AU2005284904A1 (en) 2004-09-13 2006-03-23 Amgen Inc. Vanilloid receptor ligands and their use in treatments
GB0420424D0 (en) 2004-09-14 2004-10-20 Ionix Pharmaceuticals Ltd Therapeutic compounds
US20060063792A1 (en) 2004-09-17 2006-03-23 Adolor Corporation Substituted morphinans and methods of their use
SE0402284D0 (sv) 2004-09-21 2004-09-21 Astrazeneca Ab New heterocyclic amides
EP1797090A4 (en) 2004-09-27 2009-11-11 Elixir Pharmaceuticals Inc SULFONAMIDES AND USES THEREOF
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
CA2583572C (en) 2004-10-07 2016-07-12 Merck & Co., Inc. Thiazolyl mglur5 antagonists and methods for their use
JP2008515884A (ja) 2004-10-08 2008-05-15 アストラゼネカ・アクチエボラーグ 新規なヒドロキシメチルベンゾチアゾールアミド
US8143425B2 (en) 2004-10-12 2012-03-27 Bristol-Myers Squibb Company Heterocyclic aromatic compounds useful as growth hormone secretagogues
WO2006044527A1 (en) 2004-10-15 2006-04-27 Amgen Inc. Imidazole derivatives as vanilloid receptor ligands
US7652035B2 (en) 2004-10-19 2010-01-26 Neurocrine Bioscience, Inc. CRF receptor antagonists and methods relating thereto
EP1807418A2 (en) 2004-10-22 2007-07-18 Amgen, Inc Substituted nitrogen-containing heterocycles as vanilloid receptor ligands and their uses as medicament
WO2006048771A1 (en) 2004-11-04 2006-05-11 Addex Pharmaceuticals Sa Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
EP1807423B1 (en) 2004-11-05 2009-05-20 Theravance, Inc. Quinolinone-carboxamide compounds
ATE441646T1 (de) 2004-11-05 2009-09-15 Theravance Inc 5-ht4-rezeptoragonistenverbindungen
EP1812113A1 (en) 2004-11-11 2007-08-01 Argenta Discovery Limited Pyrimidine compounds as histamine modulators
US20060111416A1 (en) 2004-11-24 2006-05-25 Lane Charlotte A L Octahydropyrrolo[3,4-C]pyrrole derivatives
NZ555318A (en) 2004-11-24 2011-01-28 Abbott Lab Chromanylurea compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor and uses thereof
WO2006058338A2 (en) 2004-11-29 2006-06-01 Janssen Pharmaceutica N.V. 4 - piperidinecarboxamide derivatives as modulators of vanilloid vr1 receptor
US7875627B2 (en) 2004-12-07 2011-01-25 Abbott Laboratories Thienopyridyl compounds that inhibit vanilloid receptor subtype 1 (VR1) and uses thereof
US20060128710A1 (en) 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
US7615570B2 (en) 2004-12-13 2009-11-10 Abbott Laboratories Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
SE0403117D0 (sv) 2004-12-21 2004-12-21 Astrazeneca Ab New compounds 1
SE0403118D0 (sv) 2004-12-21 2004-12-21 Astrazeneca Ab New compounds 2
ATE469897T1 (de) 2004-12-22 2010-06-15 Theravance Inc Indazolcarbonsäureamidverbindungen
SE0403171D0 (sv) 2004-12-23 2004-12-23 Astrazeneca Ab New compounds
BRPI0606644A2 (pt) 2005-01-14 2009-07-14 Hoffmann La Roche derivados de 4-carboxamida tiazola
EP1836203A2 (en) 2005-01-14 2007-09-26 Neurogen Corporation Heteroaryl substituted quinolin-4-ylamine analogues
US7429608B2 (en) 2005-01-20 2008-09-30 Amgen Inc. Benzo[d]imidazol analogs as vanilloid receptor ligands and their use in treatments
US7301022B2 (en) 2005-02-15 2007-11-27 Amgen Inc. Vanilloid receptor ligands and their use in treatments
WO2006088988A1 (en) 2005-02-17 2006-08-24 Theravance, Inc. Crystalline form of an indazole-carboxamide compound
GB0503646D0 (en) 2005-02-22 2005-03-30 Novartis Ag Organic compounds
DE602006014531D1 (de) 2005-03-03 2010-07-08 Janssen Pharmaceutica Nv Substituierte oxadiazaspiro-ä5.5ü-undecanonderivate und ihre verwendung als neurokininantagonisten
ES2331153T3 (es) 2005-03-10 2009-12-22 Pfizer Inc. Compuestos de n-sulfonilaminofeniletil-2-fenoxiacetamida sustituidos.
US20060211710A1 (en) 2005-03-17 2006-09-21 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
GB0506147D0 (en) 2005-03-24 2005-05-04 Merck Sharp & Dohme Therapeutic agents
WO2006102645A1 (en) 2005-03-24 2006-09-28 Janssen Pharmaceutica, N.V. Biaryl derived amide modulators of vanilloid vr1 receptor
WO2006105117A2 (en) 2005-03-28 2006-10-05 Dynogen Pharmaceuticals, Inc. Method of treating disorders and conditions using peripherally-restricted antagonists and inhibitors
TWI377206B (en) 2005-04-06 2012-11-21 Theravance Inc Crystalline form of a quinolinone-carboxamide compound
WO2006113769A1 (en) 2005-04-15 2006-10-26 Amgen Inc. Vanilloid receptor ligands and their use in treatments
GB0508314D0 (en) 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0508318D0 (en) 2005-04-25 2005-06-01 Novartis Ag Organic compounds
US20060241296A1 (en) 2005-04-25 2006-10-26 Doherty Elizabeth M Vanilloid receptor ligands and their use in treatments
GB0508319D0 (en) 2005-04-25 2005-06-01 Novartis Ag Organic compounds
AU2006243987B2 (en) 2005-05-11 2011-11-24 Abbott Laboratories Antagonists of the vanilloid receptor subtype 1 (VR1) and uses thereof
US20090298856A1 (en) 2005-05-11 2009-12-03 Rebecca Elizabeth Brown 2,3 Substituted fused bicyclic pyrimidin-4(3H)-ones modulating the function of the vanilliod-1receptor (VR1)
GB0509573D0 (en) 2005-05-11 2005-06-15 Merck Sharp & Dohme Therapeutic compounds
WO2006124753A2 (en) 2005-05-12 2006-11-23 Amgen Inc. Antipyretic agents against vr1-antagonist-induced increases in body temperature
EP1893606A2 (en) 2005-05-18 2008-03-05 Addex Pharma SA Substituted oxadiazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
DE102005023588A1 (de) 2005-05-18 2006-11-23 Grünenthal GmbH Salze substituierter Allophansäureester und deren Verwendung in Arzneimitteln
DE102005038947A1 (de) 2005-05-18 2006-11-30 Grünenthal GmbH Substituierte Benzo[d]isoxazol-3-yl-amin-Verbindungen und deren Verwendung in Arzneimitteln
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
GB0510142D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds A1
GB0510141D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B3
GB0510140D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B2
DE102005044814A1 (de) 2005-05-19 2006-11-23 Grünenthal GmbH Substituierte Sprio-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln
DE102005023784A1 (de) 2005-05-19 2006-11-30 Grünenthal GmbH Substituierte Spiro-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln
DE102005044813A1 (de) 2005-05-19 2007-10-04 Grünenthal GmbH Substituierte Spiro-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln
DE102005024012A1 (de) 2005-05-20 2006-11-23 Grünenthal GmbH Verwendung von 2,5-disubstituierten Thiazol-4-on-Derivaten in Arzneimitteln
US7582611B2 (en) 2005-05-24 2009-09-01 Pfizer Inc. Motilide compounds
MY147756A (en) 2005-05-25 2013-01-15 Theravance Inc Benzimidazole-carboxamide compounds as 5-ht4 receptor agonists
US7317022B2 (en) 2005-06-07 2008-01-08 Theravance, Inc. Benzoimidazolone-carboxamide compounds as 5-HT4 receptors agonists
CN101248042A (zh) 2005-06-10 2008-08-20 伊利舍医药品公司 磺酰胺类化合物及其用途
US20100069346A1 (en) 2005-06-23 2010-03-18 Sara Holmqvist New Azetidine Derivatives as Neurokinin Receptor Antagonists for the Treatment of Gastrointestinal Diseases
JP2008546768A (ja) 2005-06-23 2008-12-25 アストラゼネカ・アクチエボラーグ 胃腸疾患を治療するためのニューロキニン受容体アンタゴニストとしての新規なアゼチジン誘導体
US20090170872A1 (en) 2005-07-05 2009-07-02 Orchid Research Laboratories Limited Compounds and Their Pharmaceutical Use
WO2007005951A2 (en) 2005-07-05 2007-01-11 Aryx Therapeutics, Inc. Stereoisomeric pyridyl and pyridonyl compounds and methods for the treatment of gastrointestinal and central nervous system disorders
EP1902022A1 (en) 2005-07-12 2008-03-26 Glaxo Group Limited Piperazine heteroaryl derivates as gpr38 agonists
RU2416612C9 (ru) 2005-07-22 2012-03-27 Ипсен Фарма С.А.С. Стимуляторы секреции гормона роста
CA2615611C (en) 2005-07-22 2011-09-27 Pfizer Inc. Indazole derivatives
SI1907374T1 (sl) 2005-07-26 2012-11-30 Glaxo Group Ltd Derivati benzilpiperazina uporabni za zdravljenje gastrointestinalnih motenj
EP1757290A1 (en) 2005-08-16 2007-02-28 Zentaris GmbH Novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors
WO2007022531A2 (en) 2005-08-19 2007-02-22 Microbia, Inc. Methods and compositions for the treatment of gastrointestinal disorders
WO2007023242A1 (en) 2005-08-24 2007-03-01 Merz Pharma Gmbh & Co. Kgaa Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors
EP1943247A1 (en) 2005-08-25 2008-07-16 Merz Pharma GmbH & Co.KGaA Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors
WO2007030761A2 (en) 2005-09-08 2007-03-15 Smithkline Beecham Corporation Acyclic 1,4-diamines and uses thereof
CA2622372A1 (en) 2005-09-13 2007-03-22 Palau Pharma, S.A. 2-aminopyrimidine derivatives as modulators of the histamine h4 receptor activity
AR056087A1 (es) 2005-09-29 2007-09-19 Astrazeneca Ab Derivados de azetidina como antagonistas de receptores de neuroquina nk
UY29796A1 (es) 2005-09-29 2007-04-30 Astrazeneca Ab Nuevos compuestos para el tratamiento de trastornos neurológicos, psiquiátricos o del dolor
AR057828A1 (es) 2005-09-29 2007-12-19 Astrazeneca Ab Compuestos derivados de azetidina, su preparacion y composicion farmaceuutica
HUP0500920A2 (en) 2005-10-05 2007-07-30 Richter Gedeon Nyrt Oxadiazole derivatives, process for their preparation and their use
HUP0500921A2 (en) 2005-10-05 2007-07-30 Richter Gedeon Nyrt Tetrazole derivatives, process for their preparation and their use
JP2009511465A (ja) 2005-10-07 2009-03-19 グレンマーク・ファーマシューティカルズ・エスエー 置換ベンゾ縮合誘導体およびバニロイド受容体リガンドとしてのその使用
DK1940821T3 (da) 2005-10-19 2013-06-10 Gruenenthal Gmbh Nye vanilloid-receptorligander og deres anvendelse til fremstilling af lægemidler.
US7902251B2 (en) 2005-10-19 2011-03-08 Allergan, Inc. Method for treating pain
US20070088073A1 (en) 2005-10-19 2007-04-19 Allergan, Inc. Method for treating pain
US7538110B2 (en) 2005-10-27 2009-05-26 Adolor Corporation Opioid antagonists
CN101365684A (zh) 2005-10-28 2009-02-11 艾博特公司 抑制trpv1受体的吲唑衍生物
WO2007048643A1 (en) 2005-10-28 2007-05-03 Glaxo Group Limited Novel compound
JP2007122605A (ja) 2005-10-31 2007-05-17 Fujitsu Ltd インピーダンス回路、電源装置
US20070105920A1 (en) 2005-11-08 2007-05-10 Akzo Nobel N.V. 2-(Benzimidazol-1-Yl)-N-(4-phenylthiazol-2-yl) acetamide derivatives
GB0525661D0 (en) 2005-12-16 2006-01-25 Glaxo Group Ltd Novel compounds
NL2000323C2 (nl) 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine-derivaten.
WO2007090853A1 (en) 2006-02-10 2007-08-16 Cellzome (Uk) Ltd. Enantiomers of amino pyrimidine compounds for the treatment of inflammatory disorders
EP1829879A1 (en) 2006-02-10 2007-09-05 Cellzome (UK) Ltd. Amino pyrimidine compounds for the treatment of inflammatory disorders
WO2007090854A1 (en) 2006-02-10 2007-08-16 Cellzome (Uk) Ltd. Azetidine amino pyrimidine compounds for the treatment of inflammatory disorders
GB0603550D0 (en) 2006-02-22 2006-04-05 Glaxo Group Ltd Novel compounds
WO2007101158A2 (en) 2006-02-24 2007-09-07 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
WO2007101161A2 (en) 2006-02-24 2007-09-07 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
US8597562B2 (en) 2006-03-30 2013-12-03 GM Global Technology Operations LLC Composite products and methods of making the same
PE20080176A1 (es) 2006-03-31 2008-04-25 Glaxo Group Ltd Compuestos de arilpiperazina sulfonamida como agonista de los receptores de secretagogos de la hormona de crecimiento (ghs)
PL2007752T3 (pl) 2006-03-31 2011-02-28 Janssen Pharmaceutica Nv Benzoimidazol-2-ilopirymidyny i pirazyny jako modulatory receptora histaminowego H4
DE602007008859D1 (de) 2006-03-31 2010-10-14 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyridine als modulatoren des histamin-h4-rezeptors
EP2010172B1 (en) 2006-04-07 2012-08-29 Janssen Pharmaceutica N.V. Indoles and benzoimidazoles as modulators of the histamine h4 receptor
EP2007716A1 (en) 2006-04-13 2008-12-31 Glaxo Group Limited Aryl and heteroaryl sulphonamides as growth hormone secretagogue receptor agonists
MX2009000110A (es) 2006-06-28 2009-01-23 Glaxo Group Ltd Derivados de piperazinilo utiles en el tratamiento de enfermedades mediadas por el receptor grp38.
US8088733B2 (en) 2006-07-06 2012-01-03 Tranzyme Pharma Inc. Methods of using macrocyclic agonists of the ghrelin receptor for treatment of gastrointestinal motility disorders
CN101657436A (zh) 2007-02-09 2010-02-24 特兰齐姆制药公司 大环生长素释放肽受体调节剂及其使用方法
ES2390195T3 (es) 2007-08-27 2012-11-07 Theravance, Inc. Compuestos de amidoalquil-8-azabiciclo(3,2,1)octano, como antagonistas del receptor opioide mu
EP2195313B1 (en) 2007-08-27 2014-04-02 Theravance, Inc. Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
ATE502939T1 (de) 2007-08-27 2011-04-15 Theravance Inc Disubstituierte alkyl-8-azabicycloä3.2.1üoktan- verbindungen als mu-opioid-rezeptorantagonisten
TWI423801B (zh) 2007-08-27 2014-01-21 Theravance Inc 作為μ類鴉片受體拮抗劑之８－氮雜雙環〔３．２．１〕辛基－２－羥基苯甲醯胺化合物
US20110021538A1 (en) 2008-04-02 2011-01-27 Arena Pharmaceuticals, Inc. Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1938309A (zh) * 2003-12-22 2007-03-28 Sb药物波多黎各公司 Crf受体拮抗剂及其相关方法
WO2006044958A1 (en) * 2004-10-19 2006-04-27 Sb Pharmco Puerto Rico Inc. Pyrazolo [1,5-alpha] pyrimidinyl derivatives useful as corticotropin-releasing factor (crf) receptor antagonists
WO2008086047A1 (en) * 2007-01-03 2008-07-17 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
WO2009151800A1 (en) * 2008-05-07 2009-12-17 Merck & Co., Inc. Soluble epoxide hydrolase inhibitors, compositions containing such compounds and methods of treatment
WO2009146539A1 (en) * 2008-06-02 2009-12-10 Neuromed Pharmaceuticals Ltd. 4-(aminomethyl)cyclohexanamine derivatives as calcium channel blockers
WO2009153720A1 (en) * 2008-06-18 2009-12-23 Pfizer Limited Nicotinamide derivatives
WO2010015655A1 (en) * 2008-08-07 2010-02-11 Novartis Ag Cyclohexyl amide derivatives and their use as crf-1 receptor antagonists

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Corticotrophin-releasing factor receptor antagonists;Thomas E Christos，等;《Expert Opinion on Therapeutic Patents 》;20081231;第8卷(第2期);第143-152页 *

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