CA2513102C - Substituted pyrazoles, compositions containing such compounds and methods of use - Google Patents
Substituted pyrazoles, compositions containing such compounds and methods of use Download PDFInfo
- Publication number
- CA2513102C CA2513102C CA2513102A CA2513102A CA2513102C CA 2513102 C CA2513102 C CA 2513102C CA 2513102 A CA2513102 A CA 2513102A CA 2513102 A CA2513102 A CA 2513102A CA 2513102 C CA2513102 C CA 2513102C
- Authority
- CA
- Canada
- Prior art keywords
- groups
- optionally substituted
- group
- halo
- phenyl
- 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
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring 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
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US44282803P | 2003-01-27 | 2003-01-27 | |
| US60/442,828 | 2003-01-27 | ||
| PCT/US2004/001927 WO2004069158A2 (en) | 2003-01-27 | 2004-01-23 | Substituted pyrazoles, compositions containing such compounds and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2513102A1 CA2513102A1 (en) | 2004-08-19 |
| CA2513102C true CA2513102C (en) | 2011-03-22 |
Family
ID=32850762
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2513102A Expired - Fee Related CA2513102C (en) | 2003-01-27 | 2004-01-23 | Substituted pyrazoles, compositions containing such compounds and methods of use |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US7572922B2 (OSRAM) |
| EP (1) | EP1590336B1 (OSRAM) |
| JP (2) | JP4560035B2 (OSRAM) |
| AT (1) | ATE490244T1 (OSRAM) |
| AU (2) | AU2004210127B2 (OSRAM) |
| CA (1) | CA2513102C (OSRAM) |
| DE (1) | DE602004030318D1 (OSRAM) |
| WO (1) | WO2004069158A2 (OSRAM) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1590336B1 (en) * | 2003-01-27 | 2010-12-01 | Merck Sharp & Dohme Corp. | Substituted pyrazoles, compositions containing such compounds and methods of use |
| JP2006522130A (ja) | 2003-04-03 | 2006-09-28 | メルク エンド カムパニー インコーポレーテッド | ナトリウムチャンネル遮断薬としてのビアリール置換ピラゾール |
| HRP20080311T3 (hr) * | 2004-06-04 | 2008-07-31 | Merck & Co. Inc. | Derivati pirazola, pripravci koji sadrže takve spojeve i postupci za njihovu primjenu |
| WO2006017055A2 (en) * | 2004-07-07 | 2006-02-16 | Merck & Co., Inc. | Pyrazole amide derivatives, compositions containing such compounds and methods of use |
| US7625938B2 (en) | 2004-07-22 | 2009-12-01 | Merck & Co., Inc. | Substituted pyrazoles, compositions containing such compounds and methods of use |
| WO2006066133A2 (en) | 2004-12-16 | 2006-06-22 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| JP2008533200A (ja) | 2005-03-21 | 2008-08-21 | メルク エンド カムパニー インコーポレーテッド | 置換アリールおよびヘテロアリール誘導体、かかる化合物を含有する組成物および使用法 |
| JP2008540574A (ja) | 2005-05-11 | 2008-11-20 | タケダ サン ディエゴ インコーポレイテッド | ヒストンデアセチラーゼ阻害剤 |
| EP1910308B1 (en) | 2005-06-27 | 2014-09-03 | Exelixis Patent Company LLC | Imidazole based lxr modulators |
| JP2009502923A (ja) * | 2005-07-26 | 2009-01-29 | メルク エンド カムパニー インコーポレーテッド | 置換ピラゾールを合成するための方法 |
| TW200745031A (en) | 2005-10-13 | 2007-12-16 | Merck & Co Inc | Acyl indoles, compositions containing such compounds and methods of use |
| AR056574A1 (es) * | 2005-10-19 | 2007-10-10 | Merck & Co Inc | Derivados de pirazol, composiciones que contienen dichos compuestos y procedimientos de uso |
| US7989472B2 (en) | 2006-03-23 | 2011-08-02 | Merck Sharp & Dohme Corp. | Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use |
| AU2007245059B2 (en) | 2006-03-31 | 2011-07-28 | Novartis Ag | New compounds |
| JP2009537525A (ja) | 2006-05-16 | 2009-10-29 | メルク エンド カムパニー インコーポレーテッド | グルカゴン受容体アンタゴニスト化合物、このような化合物を含む組成物及び使用方法 |
| KR20090094125A (ko) | 2006-12-08 | 2009-09-03 | 엑셀리시스, 인코포레이티드 | Lxr 및 fxr 조절자 |
| WO2008093639A1 (ja) | 2007-01-29 | 2008-08-07 | Takeda Pharmaceutical Company Limited | ピラゾール化合物 |
| KR101538810B1 (ko) | 2007-02-09 | 2015-07-22 | 메타베이시스 테라퓨틱스, 인크. | 글루카곤 수용체의 길항제 |
| EA018328B1 (ru) | 2007-08-02 | 2013-07-30 | Рекордати Айерленд Лимитед | Новые гетероциклические соединения в качестве антагонистов метаботропных глутаматных рецепторов 5-го подтипа (мглу5) |
| WO2009035558A1 (en) * | 2007-09-12 | 2009-03-19 | Merck & Co., Inc. | Process for the production of a crystalline glucagon receptor antagonist compound |
| AR066169A1 (es) | 2007-09-28 | 2009-07-29 | Novartis Ag | Derivados de benzo-imidazoles, utiles para trastornos asociados con la actividad de dgat |
| EP2210876B1 (en) | 2007-11-01 | 2015-05-20 | Takeda Pharmaceutical Company Limited | Heterocyclic compound as glucagon antagonist |
| WO2009082761A1 (en) | 2007-12-26 | 2009-07-02 | Elster Electricity, Llc. | Optimized data collection in a wireless fixed network metering system |
| JP5465658B2 (ja) | 2008-03-05 | 2014-04-09 | 武田薬品工業株式会社 | 複素環化合物 |
| WO2009140342A1 (en) * | 2008-05-16 | 2009-11-19 | Schering Corporation | Glucagon receptor antagonists, compositions, and methods for their use |
| KR20100122513A (ko) | 2008-07-17 | 2010-11-22 | 아사히 가세이 파마 가부시키가이샤 | 질소 함유 복소환 화합물 |
| BRPI0918004B8 (pt) | 2008-08-13 | 2021-05-25 | Metabasis Therapeutics Inc | compostos antagonistas e agonistas inversos de receptores de glucagon, composição farmacêutica e uso dos compostos |
| WO2010030722A1 (en) * | 2008-09-15 | 2010-03-18 | Merck Sharp & Dohme Corp. | Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use |
| JP2012504630A (ja) * | 2008-10-03 | 2012-02-23 | シェーリング コーポレイション | グルカゴン受容体アンタゴニストとしてのスピロイミダゾロン誘導体 |
| US20110178314A1 (en) * | 2008-10-10 | 2011-07-21 | Alain Wellig | Process for preparing 2-alkyl-3-aroyl-5-nitro-benzofurans |
| US8324384B2 (en) | 2009-02-12 | 2012-12-04 | Merck Sharp & Dohme Corp. | Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use |
| WO2010098994A1 (en) | 2009-02-25 | 2010-09-02 | Merck Sharp & Dohme Corp. | Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use |
| US8470773B2 (en) | 2009-06-12 | 2013-06-25 | Merck Sharp & Dohme Corp. | Thiophenes as glucagon receptor antagonists, compositions, and methods for their use |
| EP2480077B1 (en) | 2009-09-22 | 2015-02-18 | Merck Sharp & Dohme Corp. | Pyrrolidines as glucagon receptor antagonists, compositions, and methods for their use |
| WO2011143057A1 (en) | 2010-05-11 | 2011-11-17 | Merck Sharp & Dohme Corp. | Novel prolylcarboxypeptidase inhibitors |
| DK2588465T3 (en) * | 2010-06-30 | 2017-05-01 | Ironwood Pharmaceuticals Inc | SGC stimulators |
| JP5878546B2 (ja) | 2010-11-09 | 2016-03-08 | アイアンウッド ファーマシューティカルズ インコーポレイテッド | sGC刺激剤 |
| KR101506829B1 (ko) | 2010-12-23 | 2015-03-30 | 화이자 인코포레이티드 | 글루카곤 수용체 조절제 |
| KR101585840B1 (ko) | 2011-02-08 | 2016-01-15 | 화이자 인코포레이티드 | 글루카곤 수용체 조절자 |
| BR112014000288A2 (pt) | 2011-07-22 | 2017-01-10 | Pfizer | moduladores do receptor de glucagon de quinolinila |
| EP2797915B1 (en) | 2011-12-27 | 2016-07-13 | Ironwood Pharmaceuticals, Inc. | 2-benzyl-3-(oxazole/thiazole)-5-(pyrimidin-2-yl)-1(H)-pyrazole derivatives as stimulators of the soluble guanylate cyclase (sGC) for the treatment of e.g. hypertension or heart failure |
| US9649294B2 (en) | 2013-11-04 | 2017-05-16 | Merck Sharp & Dohme Corp. | Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use |
| WO2015191900A1 (en) | 2014-06-12 | 2015-12-17 | Ligand Pharmaceuticals, Inc. | Glucagon antagonists |
| TW201811752A (zh) * | 2016-09-06 | 2018-04-01 | 比利時商健生藥品公司 | 用作升糖素受體拮抗劑之吲唑衍生物 |
| TWI757332B (zh) * | 2016-09-06 | 2022-03-11 | 比利時商健生藥品公司 | 使用作為升糖素受體拮抗劑之吲唑衍生物 |
| US12208071B2 (en) | 2018-02-13 | 2025-01-28 | Ligand Pharmaceuticals Incorporated | Glucagon receptor antagonists |
| AU2022417524A1 (en) * | 2021-12-23 | 2024-08-01 | Katholieke Universiteit Leuven | 2-pyrazole anilines and related analogs for inhibiting yap/taz-tead |
| WO2025034531A1 (en) * | 2023-08-04 | 2025-02-13 | The University Of Vermont And State Agricultural College | Small molecule allosteric modulator to pac1 receptor and uses thereof |
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| BRPI0409447A (pt) | 2003-04-14 | 2006-04-18 | Inst For Pharm Discovery Inc | ácidos fenilalcanóicos substituìdos |
| DE10317108A1 (de) | 2003-04-14 | 2004-11-11 | Mutzbauer, Till S., Dr. Dr.med. | Transdermal applizierbares Beruhigungs- und Sedierungsmittel |
| JP2006528687A (ja) | 2003-05-09 | 2006-12-21 | メルク エンド カムパニー インコーポレーテッド | ベンズイミダゾール、こうした化合物を含有する組成物および使用方法 |
| HRP20080311T3 (hr) | 2004-06-04 | 2008-07-31 | Merck & Co. Inc. | Derivati pirazola, pripravci koji sadrže takve spojeve i postupci za njihovu primjenu |
| US7625938B2 (en) * | 2004-07-22 | 2009-12-01 | Merck & Co., Inc. | Substituted pyrazoles, compositions containing such compounds and methods of use |
| AR056574A1 (es) | 2005-10-19 | 2007-10-10 | Merck & Co Inc | Derivados de pirazol, composiciones que contienen dichos compuestos y procedimientos de uso |
-
2004
- 2004-01-23 EP EP04704951A patent/EP1590336B1/en not_active Expired - Lifetime
- 2004-01-23 JP JP2006502975A patent/JP4560035B2/ja not_active Expired - Fee Related
- 2004-01-23 AT AT04704951T patent/ATE490244T1/de not_active IP Right Cessation
- 2004-01-23 DE DE602004030318T patent/DE602004030318D1/de not_active Expired - Lifetime
- 2004-01-23 WO PCT/US2004/001927 patent/WO2004069158A2/en not_active Ceased
- 2004-01-23 US US10/543,290 patent/US7572922B2/en active Active
- 2004-01-23 AU AU2004210127A patent/AU2004210127B2/en not_active Ceased
- 2004-01-23 CA CA2513102A patent/CA2513102C/en not_active Expired - Fee Related
-
2009
- 2009-03-19 US US12/407,184 patent/US7989475B2/en not_active Expired - Lifetime
- 2009-11-26 AU AU2009240856A patent/AU2009240856A1/en not_active Abandoned
-
2010
- 2010-02-10 JP JP2010027448A patent/JP5260569B2/ja not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| AU2004210127A1 (en) | 2004-08-19 |
| CA2513102A1 (en) | 2004-08-19 |
| US20060084681A1 (en) | 2006-04-20 |
| WO2004069158A2 (en) | 2004-08-19 |
| ATE490244T1 (de) | 2010-12-15 |
| JP5260569B2 (ja) | 2013-08-14 |
| AU2009240856A1 (en) | 2009-12-17 |
| DE602004030318D1 (de) | 2011-01-13 |
| US20090215825A1 (en) | 2009-08-27 |
| EP1590336A4 (en) | 2008-12-17 |
| EP1590336A2 (en) | 2005-11-02 |
| AU2004210127B2 (en) | 2009-10-01 |
| US7572922B2 (en) | 2009-08-11 |
| JP2010150267A (ja) | 2010-07-08 |
| JP2006516622A (ja) | 2006-07-06 |
| JP4560035B2 (ja) | 2010-10-13 |
| WO2004069158A3 (en) | 2005-01-20 |
| US7989475B2 (en) | 2011-08-02 |
| EP1590336B1 (en) | 2010-12-01 |
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Legal Events
| Date | Code | Title | Description |
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| EEER | Examination request | ||
| MKLA | Lapsed |
Effective date: 20220124 |