PE20081487A1 - DERIVADOS DE NICOTINAMIDA COMO INHIBIDORES DE 11ßHSD1 - Google Patents
DERIVADOS DE NICOTINAMIDA COMO INHIBIDORES DE 11ßHSD1Info
- Publication number
- PE20081487A1 PE20081487A1 PE2007001517A PE2007001517A PE20081487A1 PE 20081487 A1 PE20081487 A1 PE 20081487A1 PE 2007001517 A PE2007001517 A PE 2007001517A PE 2007001517 A PE2007001517 A PE 2007001517A PE 20081487 A1 PE20081487 A1 PE 20081487A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- 11ßhsd1
- inhibitors
- cyclohexylcarbamoil
- pyridin
- Prior art date
Links
- DFPAKSUCGFBDDF-UHFFFAOYSA-N Nicotinamide Chemical class NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 101710088194 Dehydrogenase Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical class F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 1
- 208000001145 Metabolic Syndrome Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229960003966 nicotinamide Drugs 0.000 abstract 1
- 235000005152 nicotinamide Nutrition 0.000 abstract 1
- 239000011570 nicotinamide Substances 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
- C07D213/82—Amides; Imides in position 3
-
- 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
-
- 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
- A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- 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
- 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
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE NICOTINAMIDA DE FORMULA (I), EN DONDE Q ES UN ENLACE SIMPLE, -O-, -S- u -N(R15)-; R1 ES ALQUILO(C1-C6), ALQUENILO(C2-C6), CICLOALQUILO(C3-C7), ENTRE OTROS; R2 ES CICLOALQUIL(C3-C7)(CH2)m- Y POLICICLOALQUIL(C6-C12)(CH2)m-, OPCIONALMENTE SUSTITUIDOS, EN DONDE m ES DE 0 A 2; R3 ES H, ALQUILO(C1-C4), ENTRE OTROS; O R2 Y R3 JUNTOS CON EL N AL QUE ESTAN UNIDOS FORMAN UN MONOCICLO SATURADO DE 5 A 6 MIEMBROS CON UN HETEROATOMO DE N, O Y S OPCIONALMENTE SUSTITUIDOS; R4 SON INDEPENDIENTEMENTE HALO, ALQUILO(C1-C2), CIANO, ALCOXI(C1-C2) Y TRIFLUOROMETILO; p ES DE 0 A 2; X ES O, S u -N(R12)-; Y ES UN CICLOALALCDIILO(C3-C7), HETEROCICLIO, ENTRE OTROS. SON SELECCIONADOS: ACIDO 2-[(3R)-1-[5-(CICLOHEXILCARBAMOIL)-6-PROPILSULFANIL-PIRIDIN-2-IL]-3-PIPERIDIL]ACETICO, ACIDO 3-[5-CICLOHEXILCARBAMOIL)-6-PROPILSULFANIL-PIRIDIN-2-IL]SULFANILBENZOICO, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y PROCEDIMIENTO DE PREPARACION. ESTOS COMPUESTOS SON INHIBIDORES DE LA ENZIMA 11-ß-HIDROXIESTEROIDE DESHIDROGENASA DE TIPO 1 (11ßHSD1), SIENDO UTIL EN EL TRATAMIENTO DEL SINDROME METABOLICO, DIABETES TIPO 2, OBESIDAD Y ATEROSCLEROSIS
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US86424706P | 2006-11-03 | 2006-11-03 | |
| US86430306P | 2006-11-03 | 2006-11-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20081487A1 true PE20081487A1 (es) | 2009-01-11 |
Family
ID=39304797
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2007001517A PE20081487A1 (es) | 2006-11-03 | 2007-11-05 | DERIVADOS DE NICOTINAMIDA COMO INHIBIDORES DE 11ßHSD1 |
Country Status (30)
| Country | Link |
|---|---|
| US (3) | US7964618B2 (es) |
| EP (2) | EP2086939B8 (es) |
| JP (1) | JP5165688B2 (es) |
| KR (1) | KR101465275B1 (es) |
| CN (3) | CN101787016B (es) |
| AR (1) | AR063458A1 (es) |
| AT (1) | ATE475649T1 (es) |
| AU (1) | AU2007315955B2 (es) |
| BR (1) | BRPI0717970C1 (es) |
| CA (1) | CA2668006C (es) |
| CL (1) | CL2007003176A1 (es) |
| CO (1) | CO6321130A2 (es) |
| CY (1) | CY1110813T1 (es) |
| DE (1) | DE602007008137D1 (es) |
| DK (1) | DK2086939T3 (es) |
| ES (2) | ES2423206T3 (es) |
| HR (1) | HRP20100522T1 (es) |
| IL (1) | IL198231A0 (es) |
| MX (1) | MX2009004707A (es) |
| NO (1) | NO20091603L (es) |
| NZ (1) | NZ576501A (es) |
| PE (1) | PE20081487A1 (es) |
| PL (1) | PL2086939T3 (es) |
| PT (1) | PT2086939E (es) |
| RS (1) | RS51451B (es) |
| RU (1) | RU2451674C2 (es) |
| SI (1) | SI2086939T1 (es) |
| TW (1) | TW200827346A (es) |
| UY (1) | UY30681A1 (es) |
| WO (1) | WO2008053194A2 (es) |
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| WO2007058346A1 (ja) | 2005-11-21 | 2007-05-24 | Shionogi & Co., Ltd. | I型11βヒドロキシステロイド脱水素酵素阻害活性を有するヘテロ環化合物 |
| TW200827346A (en) * | 2006-11-03 | 2008-07-01 | Astrazeneca Ab | Chemical compounds |
| US8314119B2 (en) | 2006-11-06 | 2012-11-20 | Abbvie Inc. | Azaadamantane derivatives and methods of use |
| TW200836719A (en) * | 2007-02-12 | 2008-09-16 | Astrazeneca Ab | Chemical compounds |
| DK2163543T3 (en) | 2007-05-18 | 2015-04-27 | Shionogi & Co | Nitrogenholdigt heterocyklisk derivat med 11beta-hydroxysteroiddehydrogenase-type 1-inhibitorisk aktivitet |
| EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| EP2202228B1 (en) * | 2007-10-15 | 2014-12-10 | Takeda Pharmaceutical Company Limited | Amide compounds and use of the same |
| WO2009056881A1 (en) * | 2007-10-29 | 2009-05-07 | Astrazeneca Ab | Chemical compounds 313 |
| US7951833B2 (en) * | 2008-02-04 | 2011-05-31 | Astrazeneca Ab | Crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]Benzoic acid 471 |
| MX2010011591A (es) * | 2008-04-22 | 2010-11-09 | Astrazeneca Ab | Pirimidin-5-carboxamidas sustituidas 281. |
| US8507493B2 (en) | 2009-04-20 | 2013-08-13 | Abbvie Inc. | Amide and amidine derivatives and uses thereof |
| EP2440204B1 (en) | 2009-06-12 | 2013-12-18 | Bristol-Myers Squibb Company | Nicotinamide compounds useful as kinase modulators |
| UY32954A (es) * | 2009-10-20 | 2011-05-31 | Astrazeneca Ab | PIRIMIDINAS SUSTITUIDAS CON ADAMANTILIMINOCARBONILO COMO INHIBIDORES DE 11-ß-HSD1 826?. |
| JP5939158B2 (ja) * | 2009-11-24 | 2016-06-22 | アラーガン、インコーポレイテッドAllergan,Incorporated | 治療的有用性を有する受容体調節物質としての新規化合物 |
| US8871208B2 (en) * | 2009-12-04 | 2014-10-28 | Abbvie Inc. | 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors and uses thereof |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| KR20110123657A (ko) * | 2010-05-07 | 2011-11-15 | 에스케이케미칼주식회사 | 피콜린아마이드 및 피리미딘-4-카복사미드 화합물, 이의 제조방법 및 이를 함유하는 약제학적 조성물 |
| EP2582709B1 (de) | 2010-06-18 | 2018-01-24 | Sanofi | Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| SG188307A1 (en) | 2010-09-23 | 2013-04-30 | Abbvie Inc | Monohydrate of an azaadamantane derivative |
| US8471027B2 (en) * | 2011-04-06 | 2013-06-25 | Hoffmann-La Roche Inc. | Adamantyl compounds |
| US8980904B2 (en) * | 2011-07-21 | 2015-03-17 | Xuanzhu Pharma Co., Ltd. | Heterocyclic substituted pyrimidine compound |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| CN102659657B (zh) * | 2012-04-24 | 2014-08-06 | 徐州医学院 | 一种蛋白酶抑制剂pf429242的合成方法 |
| BR112014031108A2 (pt) | 2012-06-20 | 2017-06-27 | Hoffmann La Roche | compostos de pirazol substituído como antagonistas de lpar |
| IN2014DN09348A (es) | 2012-06-20 | 2015-07-17 | Hoffmann La Roche | |
| EP3821892A1 (en) | 2019-11-12 | 2021-05-19 | University of Leeds | (s)-2-(1-(5-(cyclohexylcarbamoyl)-6-(propylthio)pyridin-2-yl)piperidin-3-yl) acetic acid for use in treating wounds |
| GB202216324D0 (en) * | 2022-11-02 | 2022-12-14 | Cerevance Ltd | Novel compounds |
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