PE20060427A1 - Derivados de pirazol como inhibidores de la union del glucagon y composiciones - Google Patents
Derivados de pirazol como inhibidores de la union del glucagon y composicionesInfo
- Publication number
- PE20060427A1 PE20060427A1 PE2005000624A PE2005000624A PE20060427A1 PE 20060427 A1 PE20060427 A1 PE 20060427A1 PE 2005000624 A PE2005000624 A PE 2005000624A PE 2005000624 A PE2005000624 A PE 2005000624A PE 20060427 A1 PE20060427 A1 PE 20060427A1
- Authority
- PE
- Peru
- Prior art keywords
- pirazole
- derivatives
- compositions
- alkyl
- binding inhibitors
- Prior art date
Links
- 102000051325 Glucagon Human genes 0.000 title abstract 2
- 108060003199 Glucagon Proteins 0.000 title abstract 2
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 title abstract 2
- 229960004666 glucagon Drugs 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title 1
- 229940000635 beta-alanine Drugs 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical class F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical compound C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
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
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- 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
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
-
- 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
-
- 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
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
SE REFIERE A COMPUESTOS DE PIRAZOL QUE TIENEN UN GRUPO NAFTILO UNIDO, DE FORMULA (I), EN DONDE R1 ES H, Y EL OTRO ES HALO, OH, ALQUILO(C1-C4), O-ALQUILO(C1-C4) OPCIONALMENTE SUSTITUIDOS CON HALO, ENTRE OTROS; CADA R2 SE SELECCIONA DE R1, O DOS GRUPOS R2 JUNTOS PUEDEN FORMAR UNA ESTRUCTURA CICLICA; R3 ES H O ALQUILO(C1-C3). SON PREFERIDOS: N-(4-{(1S)-1-[3-(3,5-DICLOROFENIL)-5-(6-METOXI-2-NAFTIL)-1H-PIRAZOL-1-IL]ETIL}BENZOIL)-ß-ALANINA, N-4-{(1S)-1-[3-[2-FLUORO-5-(TRIFLUOROMETIL)FENIL]-5-(6-METOXI-2-NAFTIL)-1H-PIRAZOL-1-IL]ETIL}BENZOIL)-ß-ALANINA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON INHIBIDORES DE LA UNION DEL GLUCAGON POR LO QUE SON UTILES EN EL TRATAMIENTO DE DIABETES DE TIPO 2
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US57711604P | 2004-06-04 | 2004-06-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20060427A1 true PE20060427A1 (es) | 2006-06-19 |
Family
ID=35335786
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2005000624A PE20060427A1 (es) | 2004-06-04 | 2005-06-02 | Derivados de pirazol como inhibidores de la union del glucagon y composiciones |
Country Status (34)
| Country | Link |
|---|---|
| US (2) | US7598285B2 (es) |
| EP (1) | EP1756064B1 (es) |
| JP (2) | JP4108739B2 (es) |
| CN (1) | CN1964947A (es) |
| AR (2) | AR049291A1 (es) |
| AT (1) | ATE395338T1 (es) |
| AU (2) | AU2005252183B2 (es) |
| BR (1) | BRPI0511703B8 (es) |
| CA (1) | CA2566945C (es) |
| CR (1) | CR8766A (es) |
| CY (1) | CY1108544T1 (es) |
| DE (1) | DE602005006806D1 (es) |
| DK (1) | DK1756064T3 (es) |
| EA (1) | EA012431B1 (es) |
| EC (1) | ECSP067062A (es) |
| ES (1) | ES2306165T3 (es) |
| GE (1) | GEP20094605B (es) |
| HR (1) | HRP20080311T3 (es) |
| IL (1) | IL179754A (es) |
| MA (1) | MA28673B1 (es) |
| MX (1) | MXPA06014084A (es) |
| MY (1) | MY143599A (es) |
| NI (1) | NI200600290A (es) |
| NO (1) | NO339149B1 (es) |
| NZ (1) | NZ551405A (es) |
| PE (1) | PE20060427A1 (es) |
| PL (1) | PL1756064T3 (es) |
| PT (1) | PT1756064E (es) |
| SI (1) | SI1756064T1 (es) |
| TN (1) | TNSN06397A1 (es) |
| TW (1) | TWI293952B (es) |
| UA (1) | UA85884C2 (es) |
| WO (1) | WO2005121097A2 (es) |
| ZA (1) | ZA200609489B (es) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE490244T1 (de) | 2003-01-27 | 2010-12-15 | Merck Sharp & Dohme | Substituierte pyrazole, zusammensetzungen,die solche verbindungen enthalten, und anwendungsverfahren |
| SI1756064T1 (sl) | 2004-06-04 | 2008-12-31 | Merck & Co Inc | Derivati pirazola, sestavki vsebujoäśi takĺ ne sestavine in postopki uporabe |
| AU2005269792B9 (en) * | 2004-07-22 | 2008-11-27 | Merck Sharp & Dohme Corp. | Substituted pyrazoles, compositions containing such compounds and methods of use |
| WO2007015999A2 (en) * | 2005-07-26 | 2007-02-08 | Merck & Co., Inc. | Process for synthesizing a substituted pyrazole |
| AR056574A1 (es) * | 2005-10-19 | 2007-10-10 | Merck & Co Inc | Derivados de pirazol, composiciones que contienen dichos compuestos y procedimientos de uso |
| EP2114891A1 (en) * | 2007-01-17 | 2009-11-11 | Laboratorios Del. Dr. Esteve, S.A. | Substituted pyrazoline compounds with acat inhibition activity |
| KR101538810B1 (ko) | 2007-02-09 | 2015-07-22 | 메타베이시스 테라퓨틱스, 인크. | 글루카곤 수용체의 길항제 |
| EP2170337A4 (en) * | 2007-06-28 | 2013-12-18 | Abbvie Inc | NEW TRIAZOLOPYRIDAZINE |
| US8232413B2 (en) * | 2007-09-12 | 2012-07-31 | Merck Sharp & Dohme Corp. | Process for the production of a crystalline glucagon receptor antagonist compound |
| BRPI0912245A2 (pt) | 2008-03-05 | 2019-09-24 | Takeda Pharmaceuticals Co | composto, prodroga, medicamento, métodos de suprimir produção de açúcar em um mamífero e para a profilaxia ou o tratamento de diabetes em um mamífero, e, uso do composto |
| WO2009113522A1 (ja) | 2008-03-11 | 2009-09-17 | あすか製薬株式会社 | 固体分散体とその医薬組成物、並びにそれらの製造方法 |
| CA2724294A1 (en) | 2008-05-16 | 2009-11-19 | Schering Corporation | Glucagon receptor antagonists, compositions, and methods for their use |
| CN102292316B (zh) | 2008-08-13 | 2015-07-01 | 症变治疗公司 | 胰高血糖素拮抗剂 |
| RU2008135294A (ru) * | 2008-08-29 | 2010-03-10 | Дик Корпорейшн (Jp) | Нафталиновые производные |
| WO2010030722A1 (en) * | 2008-09-15 | 2010-03-18 | Merck Sharp & Dohme Corp. | Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use |
| CA2738663A1 (en) * | 2008-10-03 | 2010-04-08 | Schering Corporation | Spiro-imidazolone derivatives as glucagon receptor antagonists |
| US8324384B2 (en) | 2009-02-12 | 2012-12-04 | Merck Sharp & Dohme Corp. | Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use |
| US8318667B2 (en) | 2009-02-25 | 2012-11-27 | 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 |
| AU2011346670B2 (en) | 2010-12-23 | 2015-05-07 | Pfizer Inc. | Glucagon receptor modulators |
| CA2825102C (en) | 2011-02-08 | 2016-03-08 | Pfizer Inc. | Glucagon receptor modulators |
| AU2012288493B2 (en) | 2011-07-22 | 2015-08-06 | Pfizer Inc. | Quinolinyl glucagon receptor modulators |
| TW201427658A (zh) | 2012-12-10 | 2014-07-16 | Merck Sharp & Dohme | 藉由投予升糖素受體拮抗劑及膽固醇吸收抑制劑治療糖尿病之方法 |
| US9649294B2 (en) | 2013-11-04 | 2017-05-16 | Merck Sharp & Dohme Corp. | Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use |
| CN103933032B (zh) * | 2013-12-30 | 2019-08-23 | 北京赛林泰医药技术有限公司 | 作为抗癌药物的吡唑类衍生物的使用方法和用途 |
| WO2015191900A1 (en) | 2014-06-12 | 2015-12-17 | Ligand Pharmaceuticals, Inc. | Glucagon antagonists |
| WO2018044903A1 (en) | 2016-08-30 | 2018-03-08 | Regeneron Pharmaceuticals, Inc. | Methods of treating severe insulin resistance by interfering with glucagon receptor signaling |
| TWI763705B (zh) * | 2016-09-06 | 2022-05-11 | 比利時商健生藥品公司 | 可作為升糖素受體拮抗劑之吲哚衍生物 |
| EP3529278A1 (en) | 2016-10-20 | 2019-08-28 | Regeneron Pharmaceuticals, Inc. | Methods of lowering blood glucose levels |
| EP3672620A1 (en) | 2017-08-22 | 2020-07-01 | Regeneron Pharmaceuticals, Inc. | Methods of treating urea cycle disorders by interfering with glucagon receptor signaling |
| US12208071B2 (en) | 2018-02-13 | 2025-01-28 | Ligand Pharmaceuticals Incorporated | Glucagon receptor antagonists |
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| WO2002040444A1 (en) | 2000-11-17 | 2002-05-23 | Novo Nordisk A/S | Glucagon antagonists/inverse agonists |
| ITMI20010733A1 (it) | 2001-04-05 | 2002-10-05 | Recordati Chem Pharm | Uso di inibitori dell'isoenzina cox-2 per il trattamento dell'incontinenza urinaria |
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| WO2003053938A1 (en) | 2001-12-20 | 2003-07-03 | Novo Nordisk A/S | Benzimidazols and indols as glucagon receptor antagonists/inverse agonisten |
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| ATE384526T1 (de) * | 2003-04-14 | 2008-02-15 | Inst For Pharm Discovery Inc | N-(((((1,3-thiazol-2- yl)amino)carbonyl)phenyl)sulphonyl)phenylalanin derivate und verwandte verbindungen zur behandlung von diabetes |
| EP1626717A4 (en) * | 2003-05-09 | 2009-09-09 | Merck & Co Inc | BENZIMIDAZOLE, COMPOSITIONS AND METHOD OF ADMINISTRATION CONTAINING SUCH COMPOUNDS |
| SI1756064T1 (sl) | 2004-06-04 | 2008-12-31 | Merck & Co Inc | Derivati pirazola, sestavki vsebujoäśi takĺ ne sestavine in postopki uporabe |
| AU2005269792B9 (en) * | 2004-07-22 | 2008-11-27 | Merck Sharp & Dohme Corp. | 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 |
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