JP5635727B2 - チアゾリルｍｇｌｕｒ５アンタゴニスト及びそれらの使用のための方法 - Google Patents

チアゾリルｍｇｌｕｒ５アンタゴニスト及びそれらの使用のための方法 Download PDF

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Publication number
JP5635727B2
JP5635727B2 JP2007543041A JP2007543041A JP5635727B2 JP 5635727 B2 JP5635727 B2 JP 5635727B2 JP 2007543041 A JP2007543041 A JP 2007543041A JP 2007543041 A JP2007543041 A JP 2007543041A JP 5635727 B2 JP5635727 B2 JP 5635727B2
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thiazol
methyl
ethynyl
mmol
disorder
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JP2008516004A (ja
JP2008516004A5 (enExample
Inventor
コスフオード，ニコラス・デイー
サイダーズ，トーマス・ジエイ
ペイン，ジヨウジフ
ロツペ，ジエフリー・アール
ホアン，ドーホア
スミス，ニコラス・デイー
プーン，ステイーブ・エフ
キング，クリス
イーストマン，ブライアン・ダブリユ
ワン，ボウイ
アルーダ，ジーニー・エム
ベルニエ，ジヤン−ミツシエル
チヤオ，シオウミン
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/06—Antiasthmatics
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    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
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    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
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    • A61P25/08—Antiepileptics; Anticonvulsants
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P25/34—Tobacco-abuse
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Addiction (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Psychology (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
JP2007543041A 2004-10-07 2005-10-06 チアゾリルｍｇｌｕｒ５アンタゴニスト及びそれらの使用のための方法 Expired - Fee Related JP5635727B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US61680504P 2004-10-07 2004-10-07
US60/616,805 2004-10-07
PCT/US2005/035921 WO2007050050A2 (en) 2004-10-07 2005-10-06 Thiazolyl mglur5 antagonists and methods for their use

Related Child Applications (1)

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JP2014184615A Division JP2015013885A (ja) 2004-10-07 2014-09-10 チアゾリルｍｇｌｕｒ５アンタゴニスト及びそれらの使用のための方法

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JP2008516004A JP2008516004A (ja) 2008-05-15
JP2008516004A5 JP2008516004A5 (enExample) 2014-10-30
JP5635727B2 true JP5635727B2 (ja) 2014-12-03

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JP2014184615A Pending JP2015013885A (ja) 2004-10-07 2014-09-10 チアゾリルｍｇｌｕｒ５アンタゴニスト及びそれらの使用のための方法

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US (3) US7879882B2 (enExample)
EP (2) EP1893608B1 (enExample)
JP (2) JP5635727B2 (enExample)
CN (1) CN101223166B (enExample)
AT (1) ATE520692T1 (enExample)
AU (1) AU2005336513B2 (enExample)
CA (1) CA2583572C (enExample)
ES (1) ES2369783T3 (enExample)
WO (1) WO2007050050A2 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
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JP2015013885A (ja) * 2004-10-07 2015-01-22 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． チアゾリルｍｇｌｕｒ５アンタゴニスト及びそれらの使用のための方法

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US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
TW201124391A (en) * 2009-10-20 2011-07-16 Lundbeck & Co As H 2-substituted-ethynylthiazole derivatives and uses of same
WO2011092293A2 (en) 2010-02-01 2011-08-04 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
US20120295942A1 (en) 2010-02-01 2012-11-22 Nicholas James Devereux Pyrazolo[5,1b]oxazole Derivatives as CRF-1 Receptor Antagonists
JP5748777B2 (ja) 2010-02-02 2015-07-15 ノバルティス アーゲー Ｃｒｆ受容体アンタゴニストとしてのシクロヘキシルアミド誘導体
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
US8772300B2 (en) * 2011-04-19 2014-07-08 Hoffmann-La Roche Inc. Phenyl or pyridinyl-ethynyl derivatives
EP2702050B1 (en) * 2011-04-26 2016-05-18 F.Hoffmann-La Roche Ag Pyrazolidin-3-one derivatives
MX337443B (es) * 2011-04-26 2016-03-07 Hoffmann La Roche Derivados de etinilo como moduladores alostericos positivos del receptor de glutamato metabotropico del subtipo 5 (mglur5).
WO2014121883A1 (en) 2013-02-07 2014-08-14 Merck Patent Gmbh Substituted acetylene derivatives and their use as positive allosteric modulators of mglur4
UA116023C2 (uk) * 2013-07-08 2018-01-25 Ф. Хоффманн-Ля Рош Аг Етинільні похідні як антагоністи метаботропного глутаматного рецептора
WO2015188368A1 (en) 2014-06-13 2015-12-17 Merck Sharp & Dohme Corp. Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles
CR20170536A (es) 2015-06-03 2018-02-01 Hoffmann La Roche Derivados de etinilo
SG10202002990XA (en) 2017-08-04 2020-05-28 Skyhawk Therapeutics Inc Methods and compositions for modulating splicing
KR20210135241A (ko) 2019-02-05 2021-11-12 스카이호크 테라퓨틱스, 인코포레이티드 스플라이싱을 조절하는 방법 및 조성물
KR20210135507A (ko) 2019-02-06 2021-11-15 스카이호크 테라퓨틱스, 인코포레이티드 스플라이싱을 조절하는 방법 및 조성물

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US6774138B2 (en) 1999-08-31 2004-08-10 Merck & Co., Inc. Thiazolyl(pyridyl)ethyne compounds
US7462619B2 (en) * 1999-08-31 2008-12-09 Merck & Co., Inc. Pyridazine, pyrimidine and pyrazine ethyne compounds
US7365074B2 (en) * 1999-08-31 2008-04-29 Merck & Co., Inc. Pyridazine, pyrimidine and pyrazine ethyne compounds
CA2383524C (en) * 1999-08-31 2010-09-28 Merck & Co., Inc. Thiazolyl alkynyl compounds and methods of use thereof
US6956049B1 (en) * 1999-08-31 2005-10-18 Merck & Co., Inc. Methods of modulating processes mediated by excitatory amino acid receptors
US6903005B1 (en) * 2000-08-30 2005-06-07 Micron Technology, Inc. Method for the formation of RuSixOy-containing barrier layers for high-k dielectrics
US6551270B1 (en) 2000-08-30 2003-04-22 Snowden Pencer, Inc. Dual lumen access port
US20070060618A1 (en) * 2002-10-24 2007-03-15 Merck & Co., Inc. Alkyne derivatives as tracers for metabotropic glutamate receptor binding
JP5635727B2 (ja) * 2004-10-07 2014-12-03 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． チアゾリルｍｇｌｕｒ５アンタゴニスト及びそれらの使用のための方法

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015013885A (ja) * 2004-10-07 2015-01-22 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． チアゾリルｍｇｌｕｒ５アンタゴニスト及びそれらの使用のための方法

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AU2005336513A1 (en) 2007-05-17
US8242143B2 (en) 2012-08-14
US20090203903A1 (en) 2009-08-13
CN101223166B (zh) 2011-10-19
JP2015013885A (ja) 2015-01-22
ES2369783T3 (es) 2011-12-05
US7879882B2 (en) 2011-02-01
EP1893608A2 (en) 2008-03-05
EP2380889A2 (en) 2011-10-26
EP1893608A4 (en) 2009-04-22
EP2380889A3 (en) 2012-01-18
WO2007050050A2 (en) 2007-05-03
ATE520692T1 (de) 2011-09-15
WO2007050050A3 (en) 2008-02-07
CA2583572A1 (en) 2006-04-07
EP1893608B1 (en) 2011-08-17
AU2005336513B2 (en) 2012-08-09
EP2380889B1 (en) 2013-06-26
US8609852B2 (en) 2013-12-17
CA2583572C (en) 2016-07-12
US20110230526A1 (en) 2011-09-22
JP2008516004A (ja) 2008-05-15
US20120289696A1 (en) 2012-11-15
CN101223166A (zh) 2008-07-16
AU2005336513A8 (en) 2009-01-08

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