RU2280034C2 - Соединения, способ их получения, фармацевтическая композиция, селективные антагонисты 5-ht2a рецептора - Google Patents
Соединения, способ их получения, фармацевтическая композиция, селективные антагонисты 5-ht2a рецептора Download PDFInfo
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- RU2280034C2 RU2280034C2 RU2003124077/04A RU2003124077A RU2280034C2 RU 2280034 C2 RU2280034 C2 RU 2280034C2 RU 2003124077/04 A RU2003124077/04 A RU 2003124077/04A RU 2003124077 A RU2003124077 A RU 2003124077A RU 2280034 C2 RU2280034 C2 RU 2280034C2
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- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
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- 125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 description 1
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- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000012071 phase Substances 0.000 description 1
- 150000003016 phosphoric acids Chemical class 0.000 description 1
- URMKJJJRIIGKHL-UHFFFAOYSA-N piperazin-1-yl(quinolin-2-yl)methanone Chemical class C=1C=C2C=CC=CC2=NC=1C(=O)N1CCNCC1 URMKJJJRIIGKHL-UHFFFAOYSA-N 0.000 description 1
- IUGYQRQAERSCNH-UHFFFAOYSA-N pivalic acid Chemical compound CC(C)(C)C(O)=O IUGYQRQAERSCNH-UHFFFAOYSA-N 0.000 description 1
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- 229910000027 potassium carbonate Inorganic materials 0.000 description 1
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- 239000003755 preservative agent Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 150000003141 primary amines Chemical class 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 235000019260 propionic acid Nutrition 0.000 description 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 description 1
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- 125000003373 pyrazinyl group Chemical group 0.000 description 1
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- 125000004943 pyrimidin-6-yl group Chemical group N1=CN=CC=C1* 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- 125000004159 quinolin-2-yl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C([H])C(*)=NC2=C1[H] 0.000 description 1
- JLZCPFISUMNHDT-UHFFFAOYSA-N quinoline-8-carbonyl chloride Chemical compound C1=CN=C2C(C(=O)Cl)=CC=CC2=C1 JLZCPFISUMNHDT-UHFFFAOYSA-N 0.000 description 1
- QRDZFPUVLYEQTA-UHFFFAOYSA-N quinoline-8-carboxylic acid Chemical compound C1=CN=C2C(C(=O)O)=CC=CC2=C1 QRDZFPUVLYEQTA-UHFFFAOYSA-N 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 230000035484 reaction time Effects 0.000 description 1
- 238000010992 reflux Methods 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 125000005920 sec-butoxy group Chemical group 0.000 description 1
- 125000003548 sec-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 150000003335 secondary amines Chemical class 0.000 description 1
- 230000000862 serotonergic effect Effects 0.000 description 1
- 231100000872 sexual dysfunction Toxicity 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 201000002859 sleep apnea Diseases 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
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- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000008347 soybean phospholipid Substances 0.000 description 1
- 238000004611 spectroscopical analysis Methods 0.000 description 1
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- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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- 150000003512 tertiary amines Chemical class 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 239000003053 toxin Substances 0.000 description 1
- 231100000765 toxin Toxicity 0.000 description 1
- 108700012359 toxins Proteins 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- 239000003204 tranquilizing agent Substances 0.000 description 1
- 230000002936 tranquilizing effect Effects 0.000 description 1
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 description 1
- 229960002622 triacetin Drugs 0.000 description 1
- 125000004784 trichloromethoxy group Chemical group ClC(O*)(Cl)Cl 0.000 description 1
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 description 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 230000025033 vasoconstriction Effects 0.000 description 1
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- 230000004584 weight gain Effects 0.000 description 1
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- 239000000080 wetting agent Substances 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
- C07D401/06—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 linked by a carbon chain containing only aliphatic 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A—HUMAN NECESSITIES
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- A61P25/16—Anti-Parkinson drugs
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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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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/22—Anxiolytics
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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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- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- 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]
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
- C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Anesthesiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Addiction (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Quinoline Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10102053.8 | 2001-01-17 | ||
| DE10102053A DE10102053A1 (de) | 2001-01-17 | 2001-01-17 | Piperazinylcarbonylchinoline und -isochinoline |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2003124077A RU2003124077A (ru) | 2005-01-10 |
| RU2280034C2 true RU2280034C2 (ru) | 2006-07-20 |
Family
ID=7670921
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2003124077/04A RU2280034C2 (ru) | 2001-01-17 | 2001-12-24 | Соединения, способ их получения, фармацевтическая композиция, селективные антагонисты 5-ht2a рецептора |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US7329749B2 (enExample) |
| EP (1) | EP1366039B1 (enExample) |
| JP (1) | JP4417624B2 (enExample) |
| KR (1) | KR100854481B1 (enExample) |
| CN (1) | CN1249055C (enExample) |
| AR (1) | AR035682A1 (enExample) |
| AT (1) | ATE304010T1 (enExample) |
| BR (1) | BR0116774A (enExample) |
| CA (1) | CA2434773C (enExample) |
| CZ (1) | CZ304144B6 (enExample) |
| DE (2) | DE10102053A1 (enExample) |
| DK (1) | DK1366039T3 (enExample) |
| ES (1) | ES2248230T3 (enExample) |
| HU (1) | HU230250B1 (enExample) |
| MX (1) | MXPA03006360A (enExample) |
| MY (1) | MY127293A (enExample) |
| PL (1) | PL212087B1 (enExample) |
| RU (1) | RU2280034C2 (enExample) |
| SI (1) | SI1366039T1 (enExample) |
| SK (1) | SK287333B6 (enExample) |
| WO (1) | WO2002057256A1 (enExample) |
| ZA (1) | ZA200306331B (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002057435A2 (en) * | 2001-01-18 | 2002-07-25 | Merck Patent Gmbh | Bifunctional fusion proteins with glucocerebrosidase activity |
| AU2003231032B2 (en) * | 2002-04-22 | 2008-07-10 | Johns Hopkins University School Of Medicine | Modulators of hedgehog signaling pathways, compositions and uses related thereto |
| MXPA04012959A (es) * | 2002-06-29 | 2005-05-16 | Zentaris Gmbh | Arilcarbonilpiperacinas y heteroarilcarbonilpiperacinas y su uso para tratamiento de enfermedades de tumor benigno y maligno. |
| US20090311242A1 (en) * | 2004-07-29 | 2009-12-17 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with 5-hydroxytryptamine 2a receptor (5ht2a) |
| GB2497476B (en) * | 2010-09-06 | 2018-01-10 | Guangzhou Inst Biomed & Health | Amide Compounds |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0320983A2 (en) * | 1987-12-17 | 1989-06-21 | Merrell Dow Pharmaceuticals Inc. | Piperidinyl compounds |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4970714A (en) * | 1989-01-05 | 1990-11-13 | International Business Machines Corp. | Adaptive data link protocol |
| EP0957100B1 (en) * | 1997-07-07 | 2004-10-27 | Kowa Co., Ltd. | Diamine derivatives and pharmaceutical containing the same |
| CA2342251A1 (en) * | 1998-08-28 | 2000-03-09 | Scios Inc. | Use of piperidines and/or piperazines as inhibitors of p38-alpha kinase |
| DE19934433A1 (de) * | 1999-07-22 | 2001-01-25 | Merck Patent Gmbh | N-(Indolcarbonyl-)piperazinderivate |
-
2001
- 2001-01-17 DE DE10102053A patent/DE10102053A1/de not_active Withdrawn
- 2001-12-24 US US10/466,487 patent/US7329749B2/en not_active Expired - Fee Related
- 2001-12-24 BR BR0116774-0A patent/BR0116774A/pt active Search and Examination
- 2001-12-24 CZ CZ20031861A patent/CZ304144B6/cs not_active IP Right Cessation
- 2001-12-24 SK SK865-2003A patent/SK287333B6/sk not_active IP Right Cessation
- 2001-12-24 JP JP2002557935A patent/JP4417624B2/ja not_active Expired - Fee Related
- 2001-12-24 DK DK01273302T patent/DK1366039T3/da active
- 2001-12-24 SI SI200130444T patent/SI1366039T1/sl unknown
- 2001-12-24 PL PL361741A patent/PL212087B1/pl unknown
- 2001-12-24 WO PCT/EP2001/015311 patent/WO2002057256A1/en not_active Ceased
- 2001-12-24 CA CA2434773A patent/CA2434773C/en not_active Expired - Fee Related
- 2001-12-24 DE DE60113300T patent/DE60113300T2/de not_active Expired - Lifetime
- 2001-12-24 KR KR1020037009081A patent/KR100854481B1/ko not_active Expired - Fee Related
- 2001-12-24 EP EP01273302A patent/EP1366039B1/en not_active Expired - Lifetime
- 2001-12-24 CN CNB018220622A patent/CN1249055C/zh not_active Expired - Fee Related
- 2001-12-24 RU RU2003124077/04A patent/RU2280034C2/ru not_active IP Right Cessation
- 2001-12-24 ES ES01273302T patent/ES2248230T3/es not_active Expired - Lifetime
- 2001-12-24 MX MXPA03006360A patent/MXPA03006360A/es active IP Right Grant
- 2001-12-24 AT AT01273302T patent/ATE304010T1/de active
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2002
- 2002-01-14 MY MYPI20020115A patent/MY127293A/en unknown
- 2002-01-16 AR ARP020100135A patent/AR035682A1/es not_active Application Discontinuation
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2003
- 2003-08-14 ZA ZA2003/06331A patent/ZA200306331B/en unknown
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2015
- 2015-10-12 HU HU0401038A patent/HU230250B1/hu not_active IP Right Cessation
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0320983A2 (en) * | 1987-12-17 | 1989-06-21 | Merrell Dow Pharmaceuticals Inc. | Piperidinyl compounds |
Non-Patent Citations (1)
| Title |
|---|
| S.YOUNES et al. EUR. J. MED. CHEM., v.35, January 2000, p.107-121. * |
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Legal Events
| Date | Code | Title | Description |
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| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20171225 |