TW201036951A - Quinazolinone derivatives useful as vanilloid antagonists - Google Patents

Quinazolinone derivatives useful as vanilloid antagonists Download PDF

Info

Publication number
TW201036951A
TW201036951A TW099100721A TW99100721A TW201036951A TW 201036951 A TW201036951 A TW 201036951A TW 099100721 A TW099100721 A TW 099100721A TW 99100721 A TW99100721 A TW 99100721A TW 201036951 A TW201036951 A TW 201036951A
Authority
TW
Taiwan
Prior art keywords
formula
compound
group
alkyl
salt
Prior art date
Application number
TW099100721A
Other languages
English (en)
Chinese (zh)
Inventor
Weichun Chen
Hong-Yong Kim
Jessica Liang
Michael Mutz
Mahavir Prashad
Christopher Towler
Ruo-Qiu Wu
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=42167396&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TW201036951(A) "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 TW201036951A publication Critical patent/TW201036951A/zh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/90—Oxygen atoms with acyclic radicals attached in position 2 or 3

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
TW099100721A 2009-01-13 2010-01-12 Quinazolinone derivatives useful as vanilloid antagonists TW201036951A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US14425009P 2009-01-13 2009-01-13

Publications (1)

Publication Number Publication Date
TW201036951A true TW201036951A (en) 2010-10-16

Family

ID=42167396

Family Applications (1)

Application Number Title Priority Date Filing Date
TW099100721A TW201036951A (en) 2009-01-13 2010-01-12 Quinazolinone derivatives useful as vanilloid antagonists

Country Status (28)

Country Link
US (2) US8349852B2 (cg-RX-API-DMAC10.html)
EP (1) EP2387440B1 (cg-RX-API-DMAC10.html)
JP (1) JP2012515150A (cg-RX-API-DMAC10.html)
KR (1) KR20110104996A (cg-RX-API-DMAC10.html)
CN (1) CN102281920A (cg-RX-API-DMAC10.html)
AR (1) AR075006A1 (cg-RX-API-DMAC10.html)
AU (1) AU2010206233B2 (cg-RX-API-DMAC10.html)
BR (1) BRPI1006909A2 (cg-RX-API-DMAC10.html)
CA (2) CA2749529C (cg-RX-API-DMAC10.html)
CO (1) CO6400202A2 (cg-RX-API-DMAC10.html)
CR (1) CR20110369A (cg-RX-API-DMAC10.html)
CU (1) CU20110148A7 (cg-RX-API-DMAC10.html)
EA (1) EA201101063A1 (cg-RX-API-DMAC10.html)
EC (1) ECSP11011195A (cg-RX-API-DMAC10.html)
ES (1) ES2614612T3 (cg-RX-API-DMAC10.html)
IL (1) IL213869A0 (cg-RX-API-DMAC10.html)
MA (1) MA32957B1 (cg-RX-API-DMAC10.html)
MX (1) MX2011007444A (cg-RX-API-DMAC10.html)
NZ (1) NZ593877A (cg-RX-API-DMAC10.html)
PE (1) PE20110776A1 (cg-RX-API-DMAC10.html)
PL (1) PL2387440T3 (cg-RX-API-DMAC10.html)
PT (1) PT2387440T (cg-RX-API-DMAC10.html)
SG (1) SG172808A1 (cg-RX-API-DMAC10.html)
TN (1) TN2011000326A1 (cg-RX-API-DMAC10.html)
TW (1) TW201036951A (cg-RX-API-DMAC10.html)
UY (1) UY32381A (cg-RX-API-DMAC10.html)
WO (1) WO2010084050A2 (cg-RX-API-DMAC10.html)
ZA (1) ZA201104873B (cg-RX-API-DMAC10.html)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0412769D0 (en) 2004-06-08 2004-07-07 Novartis Ag Organic compounds
EP2755944B1 (en) 2011-09-16 2017-06-14 Sanofi Biarylderivatives,their preparation and their therapeutic application
KR101789430B1 (ko) 2016-06-28 2017-10-25 동국대학교 산학협력단 Smo 저해 활성을 갖는 신규 화합물 및 이를 유효성분으로 포함하는 암 예방 또는 치료용 조성물
CN108863949B (zh) * 2018-07-09 2021-01-15 湖南博隽生物医药有限公司 一种用于治疗慢性炎性痛的辣椒素受体拮抗剂及合成方法
US20200261456A1 (en) * 2019-02-15 2020-08-20 Novartis Ag Methods for treating ocular surface pain
JP6994061B2 (ja) * 2019-02-15 2022-01-14 ノバルティス アーゲー 4-(7-ヒドロキシ-2-イソプロピル-4-オキソ-4h-キナゾリン-3-イル)-ベンゾニトリルの製剤
JP2022520410A (ja) * 2019-02-15 2022-03-30 ノバルティス アーゲー 4-(7-ヒドロキシ-2-イソプロピル-4-オキソ-4h-キナゾリン-3-イル)-ベンゾニトリルの結晶形態及びその製剤
WO2021009664A1 (en) 2019-07-15 2021-01-21 Novartis Ag Methods for treating meibomian gland dysfunction with liver x receptor agonists
SI4073065T1 (sl) 2019-12-10 2025-06-30 F. Hoffmann-La Roche Ag Novi derivati metilkinazolinona
US12459902B2 (en) 2020-08-06 2025-11-04 Bausch + Lomb Ireland Limited Crystalline forms of 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile and formulations thereof
TW202222298A (zh) 2020-10-07 2022-06-16 瑞士商諾華公司 含有可溶解的眼部插入物之藥物及其使用方法
US20230416207A1 (en) * 2020-11-17 2023-12-28 Crystal Pharmatech Co., Ltd. Crystalline forms of quinazolinone compound and process for preparing the same

Family Cites Families (169)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
DE19735879A1 (de) 1997-08-19 1999-02-25 Hoechst Schering Agrevo Gmbh Verfahren zur Herstellung von 2-Carboxy-5-nitro-benzolsulfonsäure und deren Salzen durch Oxidation
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
CZ20032561A3 (cs) 2001-03-26 2003-12-17 Novartis Ag Deriváty pyridinu, způsob jejich přípravy a farmaceutický prostředek, který je obsahuje
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
AR042206A1 (es) 2002-11-26 2005-06-15 Novartis Ag Acidos fenilaceticos y derivados
GB0302876D0 (en) 2003-02-07 2003-03-12 Novartis Ag Organic compounds
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
US7476653B2 (en) 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
US7491695B2 (en) 2003-06-18 2009-02-17 Tranzyme Pharma Inc. Methods of using macrocyclic modulators of the ghrelin receptor
EP1505064A1 (en) 2003-08-05 2005-02-09 Bayer HealthCare AG 2-Aminopyrimidine derivatives
CN100398524C (zh) 2003-08-12 2008-07-02 弗·哈夫曼-拉罗切有限公司 作为crf拮抗剂的四氢喹唑啉衍生物
WO2005013997A1 (en) 2003-08-12 2005-02-17 F. Hoffmann-La Roche Ag Spiro-substituted tetrahydroquinazolines as corticotropin releasing factor (cfr) antagonists
EP1664010A1 (en) 2003-08-29 2006-06-07 Vernalis (R&D) Limited Sulfonamides antagonising n-type calcium channels
PL1664036T3 (pl) 2003-09-03 2012-04-30 Pfizer Związki benzimidazolonu wykazujące działanie agonistyczne względem receptora 5-ht4
AU2004274403A1 (en) 2003-09-03 2005-03-31 Aventis Pharmaceuticals Inc. 5-aryl-Pyrazolo(4,3-d)pyrimidines, pyridines, and pyrazines and related compounds
EA200600372A1 (ru) 2003-09-05 2006-08-25 Ньюроджин Корпорейшн Конденсированные с гетероарилом пиридины, пиразины и пиримидины в качестве лигандов рецептора кортикотропин-рилизинг-фактора (crf 1)
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
BRPI0414238A (pt) 2003-09-09 2006-10-31 Ono Pharmaceutical Co antagonistas de crf e compostos heterobicìclicos
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
AR045955A1 (es) 2003-09-30 2005-11-16 Janssen Pharmaceutica Nv Compuestos benzoimidazolicos
EP1670774A1 (en) 2003-09-30 2006-06-21 Janssen Pharmaceutica N.V. Quinoxaline compounds
WO2005044266A1 (en) 2003-10-31 2005-05-19 Astrazeneca Ab Alkynes i
US7714009B2 (en) 2003-10-31 2010-05-11 Takeda Pharmaceutical Company Limited Nitrogen-containing fused heterocyclic compounds
AU2004289694B2 (en) 2003-11-10 2010-05-13 Merck Sharp & Dohme Corp. 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
EP1713791B1 (en) 2003-12-19 2008-04-30 AstraZeneca AB 5-fluoro- and chloro-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
CA2551686C (en) 2004-01-07 2014-09-23 Ian Irwin Stereoisomeric compounds and methods for the treatment of gastrointestinal and central nervous system disorders
TW200530181A (en) 2004-01-13 2005-09-16 Bristol Myers Squibb Co Heterocyclic compounds useful as growth hormone secretagogues
CA2555258C (en) 2004-01-29 2009-04-28 Pfizer Inc. 1-isopropyl-2-oxo-1,2-dihydropyridine-3-carboxamide derivatives having 5-ht4 receptor agonistic activity
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
WO2005080356A1 (en) 2004-02-18 2005-09-01 Astrazeneca Ab Tetrazole compounds and their use as metabotropic glutamate receptor antagonits
AU2005214376A1 (en) 2004-02-18 2005-09-01 Astrazeneca Ab Acetylinic piperazine compounds and their use as metabotropic glutamate receptor antagonists
SG149900A1 (en) 2004-02-18 2009-02-27 Astrazeneca Ab Polyheterocyclic compounds and their use as metabotropic glutamate receptor antagonists
ATE402935T1 (de) 2004-02-18 2008-08-15 Astrazeneca Ab Kondensierte heterocyclische verbindungen und deren verwendung als antagonisten des metabotropen rezeptors zur behandlung von gastrointestinalen erkrankungen
TW200533348A (en) 2004-02-18 2005-10-16 Theravance Inc Indazole-carboxamide compounds as 5-ht4 receptor agonists
AU2005214375A1 (en) 2004-02-18 2005-09-01 Astrazeneca Ab Triazole compounds and their use as metabotropic glutamate receptor antagonists
US7585881B2 (en) 2004-02-18 2009-09-08 Astrazeneca Ab Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
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
JP5162236B2 (ja) 2004-03-25 2013-03-13 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ イミダゾール化合物
WO2005097136A1 (en) 2004-03-29 2005-10-20 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
EA200801607A1 (ru) 2004-06-15 2008-10-30 Пфайзер Инк. Производные бензимидазолонкарбоновой кислоты
AR049300A1 (es) 2004-06-15 2006-07-12 Schering Corp Compuestos triciclicos antagonistas de mglur1 como agentes terapeuticos
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
KR101042490B1 (ko) 2004-07-15 2011-06-16 니뽄 다바코 산교 가부시키가이샤 축합 벤즈아미드 화합물 및 바닐로이드 수용체 1형(vr1)활성 저해제
WO2006008082A1 (en) 2004-07-19 2006-01-26 Institut De Recherche Pour Le Developpement Pharmaceutical compositions for the treatment of leishmaniasis
WO2006010629A1 (en) 2004-07-28 2006-02-02 Glaxo Group Limited Piperazine derivatives useful for the treatment of gastrointestinal disorders
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
WO2006031852A1 (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
SE0402284D0 (sv) 2004-09-21 2004-09-21 Astrazeneca Ab New heterocyclic amides
CN101039942A (zh) 2004-09-27 2007-09-19 伊利舍医药品公司 磺酰胺类及其用途
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
AU2005336513B2 (en) 2004-10-07 2012-08-09 Merck Sharp & Dohme Llc Thiazolyl mGluR5 antagonists and methods for their use
WO2006038871A1 (en) 2004-10-08 2006-04-13 Astrazeneca Ab New hydroxymethylbenzothiazoles amides
US8143425B2 (en) 2004-10-12 2012-03-27 Bristol-Myers Squibb Company Heterocyclic aromatic compounds useful as growth hormone secretagogues
AU2005295752A1 (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
GB0519957D0 (en) 2005-09-30 2005-11-09 Sb Pharmco Inc Chemical compound
CA2584167A1 (en) 2004-10-22 2006-05-04 Amgen Inc. Substituted nitrogen-containing heterocycles as vanilloid receptor ligands and their uses as medicament
EP1809620B1 (en) 2004-11-04 2010-12-29 Addex Pharma SA Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
DE602005014566D1 (de) 2004-11-05 2009-07-02 Theravance Inc Chinolinon-carboxamid-verbindungen
DE602005016446D1 (de) 2004-11-05 2009-10-15 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
CN102161653A (zh) 2004-11-24 2011-08-24 雅培制药有限公司 抑制香草素受体亚型1(vr1)受体的苯并二氢吡喃基脲化合物及其用途
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
SE0403118D0 (sv) 2004-12-21 2004-12-21 Astrazeneca Ab New compounds 2
SE0403117D0 (sv) 2004-12-21 2004-12-21 Astrazeneca Ab New compounds 1
ATE469897T1 (de) 2004-12-22 2010-06-15 Theravance Inc Indazolcarbonsäureamidverbindungen
SE0403171D0 (sv) 2004-12-23 2004-12-23 Astrazeneca Ab New compounds
CA2593482A1 (en) 2005-01-14 2006-07-20 Neurogen Corporation Heteroaryl substituted quinolin-4-ylamine analogues
ES2346685T3 (es) 2005-01-14 2010-10-19 F. Hoffmann-La Roche Ag Deribados de tiazol-4-carboxamida como antagonistas de mglur5.
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
US20060183901A1 (en) 2005-02-17 2006-08-17 Theravance, Inc. Crystalline form of an indazole-carboxamide compound
GB0503646D0 (en) 2005-02-22 2005-03-30 Novartis Ag Organic compounds
ES2346147T3 (es) 2005-03-03 2010-10-11 Janssen Pharmaceutica Nv Derivados de oxa-diaza-espiro-(5.5)-undecanona sustituidos y su uso como antagonistas de las neuroquininas.
EP1858865B1 (en) 2005-03-10 2009-09-16 Pfizer Inc. Substituted n-sulfonylaminophenylethyl-2-phenoxy acetamide compounds
US20060211710A1 (en) 2005-03-17 2006-09-21 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
WO2006102645A1 (en) 2005-03-24 2006-09-28 Janssen Pharmaceutica, N.V. Biaryl derived amide modulators of vanilloid vr1 receptor
GB0506147D0 (en) 2005-03-24 2005-05-04 Merck Sharp & Dohme Therapeutic agents
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
US20060235036A1 (en) 2005-04-15 2006-10-19 Doherty Elizabeth M Vanilloid receptor ligands and their use in treatments
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
GB0508318D0 (en) 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0508314D0 (en) 2005-04-25 2005-06-01 Novartis Ag Organic compounds
US7504520B2 (en) 2005-05-11 2009-03-17 Abbott Laboratories Antagonists of the vanilloid receptor subtype 1 (VR1) and use thereof
GB0509573D0 (en) 2005-05-11 2005-06-15 Merck Sharp & Dohme Therapeutic compounds
AU2006244027A1 (en) 2005-05-11 2006-11-16 Merck Sharp & Dohme Limited 2,3-substituted fused bicyclic pyrimidin-4(3H)-ones modulating the function of the vanilloid-1 receptor (VR1)
US20060281718A1 (en) 2005-05-12 2006-12-14 Bannon Anthony W Treatment of VR1-antagonist-induced increase in body temperature with an antipyretic agent
DE102005038947A1 (de) 2005-05-18 2006-11-30 Grünenthal GmbH Substituierte Benzo[d]isoxazol-3-yl-amin-Verbindungen und deren Verwendung in Arzneimitteln
WO2006123255A2 (en) 2005-05-18 2006-11-23 Addex Pharma Sa Substituted oxadiazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
GB0510141D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B3
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
DE102005023588A1 (de) 2005-05-18 2006-11-23 Grünenthal GmbH Salze substituierter Allophansäureester und deren Verwendung in Arzneimitteln
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
DE102005044813A1 (de) 2005-05-19 2007-10-04 Grünenthal GmbH Substituierte Spiro-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
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
CN101208327A (zh) 2005-06-23 2008-06-25 阿斯利康(瑞典)有限公司 作为神经激肽受体拮抗剂用于治疗胃肠疾病的新氮杂环丁烷衍生物
CN101203511A (zh) 2005-06-23 2008-06-18 阿斯利康(瑞典)有限公司 作为神经激肽受体拮抗剂用于治疗胃肠疾病的新氮杂环丁烷衍生物
JP2009500419A (ja) 2005-07-05 2009-01-08 アリックス セラピューティクス、インコーポレイテッド 立体異性体のピリジル及びピリドニル化合物並びに消化管障害及び中枢神経系障害の治療方法
US20090170872A1 (en) 2005-07-05 2009-07-02 Orchid Research Laboratories Limited Compounds and Their Pharmaceutical Use
WO2007007018A1 (en) 2005-07-12 2007-01-18 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
WO2007010390A1 (en) 2005-07-22 2007-01-25 Pfizer Japan Inc. Indazolecarboxamide derivatives as 5ht4 receptor agonists
EP1757290A1 (en) 2005-08-16 2007-02-28 Zentaris GmbH Novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors
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
JP2009507855A (ja) 2005-09-08 2009-02-26 スミスクライン・ビーチャム・コーポレイション 非環式1,4−ジアミンおよびその使用
US20090306038A1 (en) 2005-09-13 2009-12-10 Carceller Gonzalez Elena 2-Aminopyrimidine derivatives as modulators of the histamine H4 receptor activity
AR057828A1 (es) 2005-09-29 2007-12-19 Astrazeneca Ab Compuestos derivados de azetidina, su preparacion y composicion farmaceuutica
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
HUP0500921A2 (en) 2005-10-05 2007-07-30 Richter Gedeon Nyrt Tetrazole derivatives, process for their preparation and their use
HUP0500920A2 (en) 2005-10-05 2007-07-30 Richter Gedeon Nyrt Oxadiazole derivatives, process for their preparation and their use
EP1931681B1 (en) 2005-10-07 2012-11-14 Glenmark Pharmaceuticals S.A. Substituted benzofused derivatives and their use as vanilloid receptor ligands
US20070088073A1 (en) 2005-10-19 2007-04-19 Allergan, Inc. Method for treating pain
US7902251B2 (en) 2005-10-19 2011-03-08 Allergan, Inc. Method for treating pain
WO2007045462A2 (de) 2005-10-19 2007-04-26 Grünenthal GmbH Neue vanilloid-rezeptor liganden und ihre verwendung zur herstellung von arzneimitteln
AU2006306146A1 (en) 2005-10-28 2007-05-03 Abbott Laboratories Indazole derivatives that inhibit TRPV1 receptor
US20070105920A1 (en) 2005-11-08 2007-05-10 Akzo Nobel N.V. 2-(Benzimidazol-1-Yl)-N-(4-phenylthiazol-2-yl) acetamide derivatives
GB0525068D0 (en) 2005-12-08 2006-01-18 Novartis Ag Organic compounds
NL2000323C2 (nl) 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine-derivaten.
EP1829879A1 (en) 2006-02-10 2007-09-05 Cellzome (UK) Ltd. Amino pyrimidine compounds for the treatment of inflammatory disorders
WO2007090853A1 (en) 2006-02-10 2007-08-16 Cellzome (Uk) Ltd. Enantiomers of 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
WO2007113202A1 (en) 2006-03-31 2007-10-11 Glaxo Group Limited Piperazine derivatives as growth hormone secretagogue (ghs) receptor agonists
ATE478067T1 (de) 2006-03-31 2010-09-15 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyridine und pyrazine als modulatoren des histamin-h4-rezeptors
AU2007235577B2 (en) 2006-03-31 2011-09-15 Janssen Pharmaceutica N.V. Benzoimidazol-2-yl pyridines as modulators of the histamine H4 receptor
WO2007117401A2 (en) 2006-04-07 2007-10-18 Janssen Pharmaceutica N.V. Indoles and benzoimidazoles as modulators of the histamine h4 receptor
WO2007118852A1 (en) 2006-04-13 2007-10-25 Glaxo Group Limited Aryl and heteroaryl sulphonamides as growth hormone secretagogue receptor agonists

Also Published As

Publication number Publication date
US20130060029A1 (en) 2013-03-07
EP2387440A2 (en) 2011-11-23
US8349852B2 (en) 2013-01-08
EP2387440B1 (en) 2016-11-09
SG172808A1 (en) 2011-08-29
WO2010084050A2 (en) 2010-07-29
CN102281920A (zh) 2011-12-14
EA201101063A1 (ru) 2012-02-28
MA32957B1 (fr) 2012-01-02
KR20110104996A (ko) 2011-09-23
AU2010206233B2 (en) 2012-07-26
CR20110369A (es) 2011-08-26
PT2387440T (pt) 2017-01-17
CA2749529A1 (en) 2010-07-29
WO2010084050A3 (en) 2011-01-27
US20100197705A1 (en) 2010-08-05
BRPI1006909A2 (pt) 2016-02-16
CU20110148A7 (es) 2012-02-15
CA2749529C (en) 2017-04-04
NZ593877A (en) 2012-11-30
AR075006A1 (es) 2011-03-02
CO6400202A2 (es) 2012-03-15
PE20110776A1 (es) 2011-11-04
AU2010206233A1 (en) 2011-07-28
MX2011007444A (es) 2011-08-12
ECSP11011195A (es) 2011-08-31
CA2946304A1 (en) 2010-07-29
ES2614612T3 (es) 2017-06-01
JP2012515150A (ja) 2012-07-05
ZA201104873B (en) 2012-07-25
UY32381A (es) 2010-08-31
TN2011000326A1 (en) 2012-12-17
PL2387440T3 (pl) 2017-09-29
IL213869A0 (en) 2011-07-31

Similar Documents

Publication Publication Date Title
AU2010206233B2 (en) Quinazolinone derivatives useful as vanilloid antagonists
CN110003204B (zh) 一种bet蛋白抑制剂、其制备方法及用途
TW201706249A (zh) 製造喹啉化合物之方法及包含該化合物之醫藥組合物
CN106866571B (zh) 杂环脲类化合物及其药物组合物和应用
JP2006521288A (ja) {6,7−ビス(2−メトキシ−エトキシ)−キナゾリン−4−イル}−(3e)の多形体
WO2022095910A1 (zh) 用作激酶抑制剂的化合物及其应用
TW200410695A (en) Quinazolinone derivatives useful as anti-hyperalgesic agents
JP2008539278A (ja) 結晶性ロスバスタチンカルシウム
WO2021164793A1 (zh) 用作激酶抑制剂的化合物及其应用
CN101356160A (zh) 作为辣椒素受体拮抗剂的三取代的喹唑啉酮衍生物
CA2723989C (en) Fumarate salt of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(n-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline
CN107793363B (zh) 一种取代芳胺基芳杂环类化合物及其作为抗肿瘤药物的应用
TW202216667A (zh) 經取代n-苯基乙醯胺
CN106749045A (zh) 一种新型d‑氨基酸氧化酶抑制剂及其制法和应用
JP2004511486A (ja) デルタ−オピオイドアゴニストおよびアンタゴニストとしてのモルフィノイド誘導体
CN112912373B (zh) 血管生成抑制剂、其制备方法和应用
AU2022383160A1 (en) Compounds for the treatment of kinase-dependent disorders
WO2014000686A1 (zh) 嘧啶并苯并氮杂卓类化合物及其作为抗肿瘤药物的应用
WO2013159698A1 (zh) 稠环喹唑啉羟肟酸类化合物及其作为抗肿瘤药物的应用
CN108864063A (zh) 一种治疗癌症的药物溶剂合物及其制备方法
AU2012241083A1 (en) Quinazolinone derivatives useful as vanilloid antagonists
KR20190128671A (ko) 중수소화 벤즈이미다졸 화합물 및 그의 의약 용도
WO2026103775A1 (zh) 一种苯甲酰胺类衍生物及其用途
JP3484115B2 (ja) 縮合ピリダジン誘導体、その製造法および用途
JPH083162A (ja) イミダゾピリジン誘導体及びその製法