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
- -1 4-CARBAMOYL-3-FLUOROPHENOXY Chemical class 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical group [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- DNUTZBZXLPWRJG-UHFFFAOYSA-N 1-Piperidine carboxylic acid Chemical compound OC(=O)N1CCCCC1 DNUTZBZXLPWRJG-UHFFFAOYSA-N 0.000 abstract 1
- 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 abstract 1
- 101000996752 Homo sapiens Glucose-dependent insulinotropic receptor Proteins 0.000 abstract 1
- 208000031226 Hyperlipidaemia Diseases 0.000 abstract 1
- 208000032382 Ischaemic stroke Diseases 0.000 abstract 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical group C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical group C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- KHUXNRRPPZOJPT-UHFFFAOYSA-N phenoxy radical Chemical compound O=C1C=C[CH]C=C1 KHUXNRRPPZOJPT-UHFFFAOYSA-N 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
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
-
- A—HUMAN NECESSITIES
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- 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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- 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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- 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
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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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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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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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- 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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Physical Education & Sports Medicine (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Reproductive Health (AREA)
- Psychiatry (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Gynecology & Obstetrics (AREA)
- Vascular Medicine (AREA)
- Dermatology (AREA)
- Immunology (AREA)
- Epidemiology (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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| EP2445901A1 (en) | 2009-06-24 | 2012-05-02 | Boehringer Ingelheim International GmbH | New compounds, pharmaceutical composition and methods relating thereto |
| CN102803214A (zh) | 2009-06-24 | 2012-11-28 | 贝林格尔.英格海姆国际有限公司 | 新化合物、与之相关的药物组合物和方法 |
| JP2013522279A (ja) | 2010-03-18 | 2013-06-13 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 糖尿病及び関連状態の治療で用いるｇｐｒ１１９作動薬とｄｄｐ−ｉｖ阻害薬リナグリプチンの組合せ |
| JP5496409B2 (ja) | 2010-03-19 | 2014-05-21 | ファイザー・インク | ２，３ジヒドロ−１ｈ−インデン−１−イル−２，７−ジアザスピロ［３．５］ノナン誘導体およびグレリン受容体のアンタゴニストまたは逆アゴニストとしてのそれらの使用 |
| ES2546465T3 (es) | 2010-10-29 | 2015-09-23 | Pfizer Inc | Inhibidores de N1/N2-lactama acetil-CoA carboxilasa |
| MX2013004083A (es) * | 2010-11-23 | 2013-06-13 | Pfizer | Moduladores de gpr 119. |
| WO2014011926A1 (en) | 2012-07-11 | 2014-01-16 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
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| ES2605565T3 (es) | 2011-08-31 | 2017-03-15 | Pfizer Inc | Compuestos de hexahidropirano [3,4-D][1,3]tiazin-2-amina |
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| HK1206735A1 (en) | 2012-04-06 | 2016-01-15 | 辉瑞公司 | Diacylglycerol acyltransferase 2 inhibitors |
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