PE20120399A1 - Derivados del l-(piperidin-4-il)-pirazol como moduladores de gpr 119 - Google Patents
Derivados del l-(piperidin-4-il)-pirazol como moduladores de gpr 119Info
- Publication number
- PE20120399A1 PE20120399A1 PE2011002028A PE2011002028A PE20120399A1 PE 20120399 A1 PE20120399 A1 PE 20120399A1 PE 2011002028 A PE2011002028 A PE 2011002028A PE 2011002028 A PE2011002028 A PE 2011002028A PE 20120399 A1 PE20120399 A1 PE 20120399A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- methyl
- piperidin
- cyane
- pirazol
- Prior art date
Links
Classifications
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- 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
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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- A—HUMAN NECESSITIES
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- 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
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- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A—HUMAN NECESSITIES
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
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- 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
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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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- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
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- A61P27/12—Ophthalmic agents for cataracts
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- 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
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- 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
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- 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
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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)
- Physical Education & Sports Medicine (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Endocrinology (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Emergency Medicine (AREA)
- Immunology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
REFERIDA A UN COMPUESTO DERIVADO DE PIPERIDINIL-PIRAZOL DE FORMULA (I), DONDE X ES UN COMPUESTO DEL GRUPO (a) O (b); Y ES O, CH(R5) O NR5; Z ES C(O)-O-R6 O PIRIMIDINA SUSTITUIDA CON ALQUILO C1-C4, CF3, HALOGENO, ENTRE OTROS; m ES 1, 2 O 3; n ES 0, 1 O 2; R1 ES H, ALQUILO C1-C4, CICLOALQUILO C3-C6; R2a ES H, F, ALQUILO C1-C4; R2b ES H O F; R3 ES OH, HALOGENO, CIANO, ALQUILO C1-C4, ENTRE OTROS; R5 ES H O ALQUILO C1-C4; R6 ES ALQUILO C1-C4 O CICLOALQUILO C3-C6 OPCIONALMENTE SUSTITUIDO CON METILO O ETILO. SON COMPUESTOS PREFERIDOS: 4-{4-[(4-CARBAMOIL-3-FLUOROFENOXI)METIL]-5-CIANO-1H-PIRAZOL-1-IL}PIPERIDIN-1-CARBOXILATO DE 1-METILCICLOPROPILO, 4-{4-[(4-CARBAMOIL-2-FLUOROFENOXI)METIL]-5-CIANO-1H-PIRAZOL-1-IL}PIPERIDIN-1-CARBOXILATO DE 1-METILCICLOPROPILO, 4-(5-CIANO-4-{[4-(1H-PIRAZOL-1-IL)FENOXI]METIL}-1H-PIRAZOL-1-IL)PIPERIDIN-1-CARBOXILATO DE ISOPROPILO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS MODULAN LA ACTIVIDAD DEL RECEPTOR ACOPLADO A PROTEINA G, GPR119 Y SON UTILES EN EL TRATAMIENTO DE LA DIABETES MELLITUS TIPO I Y II, HIPERLIPIDEMIA, ICTUS ISQUEMICO, CARDIOPATIA CORONARIA, ENTRE OTROS
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18435509P | 2009-06-05 | 2009-06-05 | |
| US25762109P | 2009-11-03 | 2009-11-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20120399A1 true PE20120399A1 (es) | 2012-04-24 |
Family
ID=42358441
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011002028A PE20120399A1 (es) | 2009-06-05 | 2010-05-27 | Derivados del l-(piperidin-4-il)-pirazol como moduladores de gpr 119 |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US20110020460A1 (es) |
| EP (1) | EP2438051A1 (es) |
| JP (1) | JP2012528847A (es) |
| KR (1) | KR20120061063A (es) |
| CN (1) | CN102459222B (es) |
| AP (1) | AP2799A (es) |
| AR (1) | AR076985A1 (es) |
| AU (1) | AU2010255422B2 (es) |
| BR (1) | BRPI1014636A2 (es) |
| CA (1) | CA2764021C (es) |
| CL (1) | CL2011003085A1 (es) |
| CO (1) | CO6470897A2 (es) |
| CR (1) | CR20110623A (es) |
| CU (1) | CU20110225A7 (es) |
| DO (1) | DOP2011000371A (es) |
| EA (1) | EA020106B1 (es) |
| EC (1) | ECSP11011493A (es) |
| GE (1) | GEP20135907B (es) |
| GT (1) | GT201100308A (es) |
| HN (1) | HN2011003195A (es) |
| IL (1) | IL216772A0 (es) |
| MA (1) | MA33334B1 (es) |
| MX (1) | MX2011013034A (es) |
| NI (1) | NI201100204A (es) |
| NZ (1) | NZ596467A (es) |
| PE (1) | PE20120399A1 (es) |
| SG (1) | SG175995A1 (es) |
| SV (1) | SV2011004063A (es) |
| TN (1) | TN2012000073A1 (es) |
| TW (1) | TWI411611B (es) |
| UY (1) | UY32683A (es) |
| WO (1) | WO2010140092A1 (es) |
| ZA (1) | ZA201108481B (es) |
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| EP2547339A1 (en) | 2010-03-18 | 2013-01-23 | Boehringer Ingelheim International GmbH | Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions |
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| DK2699576T3 (en) | 2011-04-22 | 2016-02-15 | Pfizer | Pyrazolospiroketon derivatives for use as acetyl-CoA carboxylase inhibitors |
| CN103958495B (zh) | 2011-06-09 | 2018-06-22 | 理森制药股份公司 | 作为gpr-119的调节剂的化合物 |
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| TW202115086A (zh) | 2019-06-28 | 2021-04-16 | 美商輝瑞大藥廠 | Bckdk抑制劑 |
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| KR20030076716A (ko) | 2001-02-28 | 2003-09-26 | 머크 앤드 캄파니 인코포레이티드 | 멜라노코르틴-4 수용체 효능제로서 아실화 피페리딘 유도체 |
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| DOP2006000009A (es) * | 2005-01-13 | 2006-08-15 | Arena Pharm Inc | Procedimiento para preparar eteres de pirazolo [3,4-d] pirimidina |
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| BRPI0617207A2 (pt) * | 2005-09-29 | 2011-07-19 | Sanofi Aventis | derivados de fenil-1,2,4-oxadiazolona, processos para sua preparação e seu uso como produtos farmacêuticos |
| GB0522846D0 (en) | 2005-11-09 | 2005-12-21 | Peakdale Molecular Ltd | Process |
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| KR20100134659A (ko) * | 2008-03-31 | 2010-12-23 | 메타볼렉스, 인코포레이티드 | 옥시메틸렌 아릴 화합물 및 그것의 사용 |
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