RU2004109586A - Диарилциклоалкильные производные, способ их получения и их применение в качестве ppar-активаторов - Google Patents
Диарилциклоалкильные производные, способ их получения и их применение в качестве ppar-активаторов Download PDFInfo
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- RU2004109586A RU2004109586A RU2004109586/04A RU2004109586A RU2004109586A RU 2004109586 A RU2004109586 A RU 2004109586A RU 2004109586/04 A RU2004109586/04 A RU 2004109586/04A RU 2004109586 A RU2004109586 A RU 2004109586A RU 2004109586 A RU2004109586 A RU 2004109586A
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- Prior art keywords
- alkyl
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- medicament
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- treatment
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- 238000004519 manufacturing process Methods 0.000 title claims 16
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 title 1
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 title 1
- 239000012190 activator Substances 0.000 title 1
- YCWSUKQGVSGXJO-NTUHNPAUSA-N nifuroxazide Chemical compound C1=CC(O)=CC=C1C(=O)N\N=C\C1=CC=C([N+]([O-])=O)O1 YCWSUKQGVSGXJO-NTUHNPAUSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 29
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 21
- 239000003814 drug Substances 0.000 claims 15
- 125000004432 carbon atom Chemical group C* 0.000 claims 10
- 125000004430 oxygen atom Chemical group O* 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 239000000825 pharmaceutical preparation Substances 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000006553 (C3-C8) cycloalkenyl group Chemical group 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 3
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000031229 Cardiomyopathies Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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
- A61P1/04—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
-
- 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
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- 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
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P3/06—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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- 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
- C07D413/12—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 chain containing hetero atoms as chain links
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (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)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (23)
1. Соединение формулы
в которой кольцо A представляет (C3-C8)-циклоалкил или (C3-C8)-циклоалкенил, и в этих циклоалкильных или циклоалкенильных кольцах один или несколько атомов углерода могут быть заменены атомами кислорода;
R1, R2, R4, R5, независимо друг от друга, представляют H, F, Cl, Br, OH, NO2, CF3, OCF3, (С1-C6)-алкил или O-(С1-C6)-алкил;
R3 представляет H или (C1-C6)-алкил;
X представляет (C1-С6)-алкил, где один или несколько атомов углерода в алкильной группе могут быть заменены атомами кислорода;
Y представляет (C1-С6)-алкил, где один или несколько атомов углерода в алкильной группе могут быть заменены атомами кислорода;
и его физиологически приемлемые соли.
2. Соединение формулы I по п.1, где
кольцо А представляет (C3-C8)-циклоалкил или (C3-C8)-циклоалкенил, и в этих циклоалкильных или циклоалкенильных кольцах один или несколько атомов углерода могут быть заменены атомами кислорода;
R1, R2, R4, независимо друг от друга, представляют H, F, Cl, Br, OH, NO2, CF3, OCF3, (C1-C6)-алкил или O-(C1-C6)-алкил;
R5 представляет (C1-C6)-алкил;
R3 представляет H или (C1-C6)-алкил;
X представляет (C1-C6)-алкил, где один или несколько атомов углерода в алкильной группе заменены атомами кислорода;
Y представляет (C1-C6)-алкил, где один или несколько атомов углерода в алкильной группе могут быть заменены атомами кислорода;
и его физиологически приемлемые соли.
3. Соединение формулы I по п.1 или 2, где
кольцо А представляет (C3-C8)-циклоалкил или (C3-C8)-циклоалкенил;
R1, R2, независимо друг от друга, представляют H, F, Cl, Br, OH, NO2, CF3, OCF3, (C1-C6)-алкил или O-(C1-C6)-алкил;
R3 представляет H или (C1-C6)-алкил;
X представляет (C1-C6)-алкил, где один или несколько атомов углерода в алкильной группе заменены атомами кислорода;
Y представляет (C1-C6)-алкил, где один или несколько атомов углерода в алкильной группе заменены атомами кислорода;
и его физиологически приемлемые соли.
4. Соединение формулы I по п.1 или 2, имеющее структуру Ia
кольцо А представляет циклогексил;
R1, R2, независимо друг от друга, представляют H, F, Cl, Br, OH, NO2, CF3, OCF3, (C1-C6)-алкил или O-(C1-C6)-алкил;
R3 представляет H или (C1-C6)-алкил;
X представляет (C1-C6)-алкил, где один или несколько атомов углерода в алкильной группе заменены атомами кислорода;
Y представляет (C1-C6)-алкил, где один или несколько атомов углерода в алкильной группе заменены атомами кислорода;
и его физиологически приемлемые соли.
5. Фармацевтический препарат, включающий одно или несколько соединений по одному или нескольким из пп.1-4.
6. Фармацевтический препарат, включающий одно или несколько соединений по одному или нескольким из пп.1-4 и одно или несколько активных соединений.
7. Фармацевтический препарат, включающий одно или несколько соединений по пп.1-4 и одно или несколько липид- или триглицеридпонижающих активных соединений.
8. Применение соединений по одному или нескольким из пп.1-4 для получения лекарственного средства для лечения нарушений липидного обмена.
9. Применение соединений по одному или нескольким из пп.1-4 для получения лекарственного средства для лечения диабета типа II.
10. Применение соединений по одному или нескольким из пп.1-4 для получения лекарственного средства для лечения синдрома X.
11. Применение соединений по одному или нескольким из
пп.1-4 для получения лекарственного средства для лечения нарушенной толерантности к глюкозе.
12. Применение соединений по одному или нескольким из пп.1-4 для получения лекарственного средства для лечения нарушений, связанных с принятием пищи.
13. Применение соединений по одному или нескольким из пп.1-4 для получения лекарственного средства для лечения ожирения.
14. Применение соединений по одному или нескольким из пп.1-4 для получения лекарственного средства для лечения кардиомиопатии.
15. Применение соединений по одному или нескольким из пп.1-4 для получения лекарственного средства для лечения сердечной недостаточности.
16. Применение соединений по одному или нескольким из пп.1-4 для получения лекарственного средства для лечения остеопороза.
17. Применение соединений по одному или нескольким из пп.1-4 для получения лекарственного средства для лечения атеросклероза.
18. Применение соединений по одному или нескольким из пп.1-4 для получения лекарственного средства для лечения болезни Альцгеймера.
19. Применение соединений по одному или нескольким из пп.1-4 для получения лекарственного средства для лечения воспалений.
20. Применение соединений по одному или нескольким из пп.1-4 в сочетании с, по крайней мере, одним дополнительным активным соединением для получения лекарственного средства для лечения нарушений липидного обмена.
21. Применение соединений по одному или нескольким из пп.1-4 в сочетании с, по крайней мере, одним дополнительным активным соединением для получения лекарственного средства для лечения диабета типа II.
22. Применение соединений по одному или нескольким из пп.1-4 в сочетании с, по крайней мере, одним дополнительным активным соединением для получения лекарственного средства для лечения синдрома Х.
23. Способ получения фармацевтического препарата, включающего одно или несколько соединений по одному или нескольким из пп.1-4, который включает смешение активного соединения с фармацевтически приемлемым носителем и придание этой смеси формы, подходящей для введения.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10142734A DE10142734A1 (de) | 2001-08-31 | 2001-08-31 | Diarylcycloalkylderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| DE10142734.4 | 2001-08-31 | ||
| DE10223273.3 | 2002-05-24 | ||
| DE2002123273 DE10223273A1 (de) | 2002-05-24 | 2002-05-24 | Diarylcycloalkylderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2004109586A true RU2004109586A (ru) | 2005-04-20 |
| RU2330846C2 RU2330846C2 (ru) | 2008-08-10 |
Family
ID=26010044
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2004109586/04A RU2330846C2 (ru) | 2001-08-31 | 2002-08-17 | Диарилциклоалкильные производные, способ их получения и их применение в качестве ppar-активаторов |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US6624185B2 (ru) |
| EP (1) | EP1425014B1 (ru) |
| JP (1) | JP4436129B2 (ru) |
| KR (1) | KR100915108B1 (ru) |
| CN (1) | CN1255103C (ru) |
| AR (1) | AR039063A1 (ru) |
| AT (1) | ATE347890T1 (ru) |
| AU (1) | AU2002333456B2 (ru) |
| BG (1) | BG108598A (ru) |
| BR (1) | BR0212158A (ru) |
| CA (1) | CA2458210C (ru) |
| CO (1) | CO5560562A2 (ru) |
| CR (1) | CR7261A (ru) |
| CY (1) | CY1106378T1 (ru) |
| DE (1) | DE50208960D1 (ru) |
| DK (1) | DK1425014T3 (ru) |
| EE (1) | EE05418B1 (ru) |
| ES (1) | ES2278077T3 (ru) |
| HR (1) | HRP20040199A2 (ru) |
| HU (1) | HUP0401564A3 (ru) |
| IL (2) | IL160556A0 (ru) |
| MA (1) | MA27134A1 (ru) |
| MX (1) | MXPA04001850A (ru) |
| MY (1) | MY132789A (ru) |
| NZ (1) | NZ531440A (ru) |
| OA (1) | OA12656A (ru) |
| PE (1) | PE20030414A1 (ru) |
| PL (1) | PL208515B1 (ru) |
| PT (1) | PT1425014E (ru) |
| RS (1) | RS50889B (ru) |
| RU (1) | RU2330846C2 (ru) |
| TN (1) | TNSN04039A1 (ru) |
| TW (1) | TWI305724B (ru) |
| UA (1) | UA76773C2 (ru) |
| WO (1) | WO2003020269A1 (ru) |
Families Citing this family (93)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001090087A1 (fr) * | 2000-05-26 | 2001-11-29 | Nippon Shinyaku Co., Ltd. | Composes heterocycliques |
| US6884812B2 (en) * | 2001-08-31 | 2005-04-26 | Aventis Pharma Deutschland Gmbh | Diarylcycloalkyl derivatives, processes for their preparation and their use as pharmaceuticals |
| US7399777B2 (en) * | 2001-08-31 | 2008-07-15 | Sanofi-Aventis Deutschland Gmbh | Diarylcycloalkyl derivatives, processes for their preparation and their use as pharmceuticals |
| US7078404B2 (en) * | 2002-04-11 | 2006-07-18 | Sanofi-Aventis Deutschland Gmbh | Acyl-3-carboxyphenylurea derivatives, processes for preparing them and their use |
| US7049341B2 (en) * | 2002-06-07 | 2006-05-23 | Aventis Pharma Deutschland Gmbh | N-benzoylureidocinnamic acid derivatives, processes for preparing them and their use |
| US7262220B2 (en) * | 2002-07-11 | 2007-08-28 | Sanofi-Aventis Deutschland Gmbh | Urea- and urethane-substituted acylureas, process for their preparation and their use |
| US7208504B2 (en) | 2002-10-12 | 2007-04-24 | Sanofi-Aventis Deutschland Gmbh | Bicyclic inhibitors of hormone sensitive lipase |
| DE10258008B4 (de) * | 2002-12-12 | 2006-02-02 | Sanofi-Aventis Deutschland Gmbh | Heterocyclische Fluorglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel |
| DE10258007B4 (de) * | 2002-12-12 | 2006-02-09 | Sanofi-Aventis Deutschland Gmbh | Aromatische Fluorglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel |
| US20040242583A1 (en) * | 2003-01-20 | 2004-12-02 | Aventis Pharma Deutschland Gmbh | Pyrimido[5,4-e][1,2,4]triazine-5,7-diones, processes for preparing them and their use |
| US7179941B2 (en) | 2003-01-23 | 2007-02-20 | Sanofi-Aventis Deutschland Gmbh | Carbonylamino-substituted acyl phenyl urea derivatives, process for their preparation and their use |
| US7196114B2 (en) * | 2003-02-17 | 2007-03-27 | Sanofi-Aventis Deutschland Gmbh | Substituted 3-(benzoylureido) thiophene derivatives, processes for preparing them and their use |
| US7148246B2 (en) | 2003-02-27 | 2006-12-12 | Sanofi-Aventis Deutschland Gmbh | Cycloalkyl derivatives having bioisosteric carboxylic acid groups, processes for their preparation and their use as pharmaceuticals |
| DE10308350B4 (de) * | 2003-02-27 | 2006-06-01 | Sanofi-Aventis Deutschland Gmbh | Verfahren zur Herstellung der enantiomeren Formen von cis-konfigurierten 1,3-Cyclohexandiol-Derivaten |
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