CN101223166B - 噻唑基mglur5拮抗剂及其应用方法 - Google Patents
噻唑基mglur5拮抗剂及其应用方法 Download PDFInfo
- Publication number
- CN101223166B CN101223166B CN2005800415189A CN200580041518A CN101223166B CN 101223166 B CN101223166 B CN 101223166B CN 2005800415189 A CN2005800415189 A CN 2005800415189A CN 200580041518 A CN200580041518 A CN 200580041518A CN 101223166 B CN101223166 B CN 101223166B
- Authority
- CN
- China
- Prior art keywords
- ethynyl
- thiazole
- methyl isophthalic
- compound
- isophthalic acid
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Fee Related
Links
- OBSLLHNATPQFMJ-UHFFFAOYSA-N Cc1c[s]c(C)n1 Chemical compound Cc1c[s]c(C)n1 OBSLLHNATPQFMJ-UHFFFAOYSA-N 0.000 description 1
Classifications
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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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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
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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
- C07D417/14—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)
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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101223166A CN101223166A (zh) | 2008-07-16 |
| CN101223166B true CN101223166B (zh) | 2011-10-19 |
Family
ID=37968242
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2005800415189A Expired - Fee Related CN101223166B (zh) | 2004-10-07 | 2005-10-06 | 噻唑基mglur5拮抗剂及其应用方法 |
Country Status (9)
| Country | Link |
|---|---|
| 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) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
-
2005
- 2005-10-06 JP JP2007543041A patent/JP5635727B2/ja not_active Expired - Fee Related
- 2005-10-06 AT AT05858618T patent/ATE520692T1/de not_active IP Right Cessation
- 2005-10-06 EP EP05858618A patent/EP1893608B1/en not_active Expired - Lifetime
- 2005-10-06 AU AU2005336513A patent/AU2005336513B2/en not_active Ceased
- 2005-10-06 CA CA2583572A patent/CA2583572C/en not_active Expired - Lifetime
- 2005-10-06 US US11/664,902 patent/US7879882B2/en active Active
- 2005-10-06 ES ES05858618T patent/ES2369783T3/es not_active Expired - Lifetime
- 2005-10-06 WO PCT/US2005/035921 patent/WO2007050050A2/en not_active Ceased
- 2005-10-06 CN CN2005800415189A patent/CN101223166B/zh not_active Expired - Fee Related
- 2005-10-06 EP EP11167527.8A patent/EP2380889B1/en not_active Expired - Lifetime
-
2011
- 2011-01-28 US US13/016,304 patent/US8242143B2/en not_active Expired - Lifetime
-
2012
- 2012-07-26 US US13/558,537 patent/US8609852B2/en not_active Expired - Lifetime
-
2014
- 2014-09-10 JP JP2014184615A patent/JP2015013885A/ja active Pending
Non-Patent Citations (6)
| Title |
|---|
| Jeffrey R.Roppe,et al.5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3"-bipyridine:a highly potent,orally active metabotropic glutamate subtype 5(mGlu5) receptor antagonist with anxiolytic activity.Bioorganic & Medicinal Chemistry Letters.2004,14(15),3993-3996. |
| Jeffrey R.Roppe,et al.5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3"-bipyridine:a highly potent,orally active metabotropic glutamate subtype 5(mGlu5) receptor antagonist with anxiolytic activity.Bioorganic & * |
| Medicinal Chemistry Letters.2003,13(3),351-354. * |
| Medicinal Chemistry Letters.2004,14(15),3993-3996. * |
| Nicholas D.P.Cosford.[3H]-Methoxymethyl-MTEP and [3H]-Methoxy-PEPy:Potent and Selective Radioligands for the Metabotropic Glutamate Subtype 5(mGlu5) Receptor.Bioorganic & Medicinal Chemistry Letters.2003,13(3),351-354. |
| Nicholas D.P.Cosford.[3H]-Methoxymethyl-MTEP and [3H]-Methoxy-PEPy:Potent and Selective Radioligands for the Metabotropic Glutamate Subtype 5(mGlu5) Receptor.Bioorganic & * |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2005336513A1 (en) | 2007-05-17 |
| US8242143B2 (en) | 2012-08-14 |
| US20090203903A1 (en) | 2009-08-13 |
| JP2015013885A (ja) | 2015-01-22 |
| ES2369783T3 (es) | 2011-12-05 |
| JP5635727B2 (ja) | 2014-12-03 |
| 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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