ZA200402099B - Novel 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity. - Google Patents
Novel 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity. Download PDFInfo
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- ZA200402099B ZA200402099B ZA200402099A ZA200402099A ZA200402099B ZA 200402099 B ZA200402099 B ZA 200402099B ZA 200402099 A ZA200402099 A ZA 200402099A ZA 200402099 A ZA200402099 A ZA 200402099A ZA 200402099 B ZA200402099 B ZA 200402099B
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- South Africa
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- MCGBIXXDQFWVDW-UHFFFAOYSA-N 4,5-dihydro-1h-pyrazole Chemical class C1CC=NN1 MCGBIXXDQFWVDW-UHFFFAOYSA-N 0.000 title description 4
- 230000000694 effects Effects 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims description 39
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 22
- -1 trifluoromethoxy, nitro, amino Chemical group 0.000 claims description 22
- 125000000217 alkyl group Chemical group 0.000 claims description 21
- 229930003827 cannabinoid Natural products 0.000 claims description 17
- 239000003557 cannabinoid Substances 0.000 claims description 17
- 208000035475 disorder Diseases 0.000 claims description 16
- 229910052757 nitrogen Inorganic materials 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 13
- 239000000203 mixture Substances 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 10
- 125000001544 thienyl group Chemical group 0.000 claims description 10
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- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 9
- 125000000623 heterocyclic group Chemical group 0.000 claims description 8
- 125000000468 ketone group Chemical group 0.000 claims description 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 239000000126 substance Substances 0.000 claims description 7
- 125000003342 alkenyl group Chemical group 0.000 claims description 6
- 125000003545 alkoxy group Chemical group 0.000 claims description 6
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 6
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- 125000001153 fluoro group Chemical group F* 0.000 claims description 6
- 229920006395 saturated elastomer Polymers 0.000 claims description 6
- 125000001424 substituent group Chemical group 0.000 claims description 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 6
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 5
- 229910052760 oxygen Inorganic materials 0.000 claims description 5
- 230000005062 synaptic transmission Effects 0.000 claims description 5
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims description 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 4
- 230000002490 cerebral effect Effects 0.000 claims description 4
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 4
- 125000001624 naphthyl group Chemical group 0.000 claims description 4
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- 125000005344 pyridylmethyl group Chemical group [H]C1=C([H])C([H])=C([H])C(=N1)C([H])([H])* 0.000 claims description 3
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- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 2
- 125000002393 azetidinyl group Chemical group 0.000 claims description 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 2
- 150000001602 bicycloalkyls Chemical group 0.000 claims description 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 2
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 claims description 2
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- 150000002367 halogens Chemical class 0.000 claims description 2
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- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
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- 229940002612 prodrug Drugs 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000005034 trifluormethylthio group Chemical group FC(S*)(F)F 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 description 10
- 229940044551 receptor antagonist Drugs 0.000 description 8
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- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 6
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- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
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- SUZLHDUTVMZSEV-UHFFFAOYSA-N Deoxycoleonol Natural products C12C(=O)CC(C)(C=C)OC2(C)C(OC(=O)C)C(O)C2C1(C)C(O)CCC2(C)C SUZLHDUTVMZSEV-UHFFFAOYSA-N 0.000 description 2
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
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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
-
- 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
-
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
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- Diabetes (AREA)
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Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01203850 | 2001-09-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200402099B true ZA200402099B (en) | 2005-04-26 |
Family
ID=8181043
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200402099A ZA200402099B (en) | 2001-09-21 | 2004-03-16 | Novel 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity. |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US7528162B2 (ru) |
| EP (1) | EP1429761B1 (ru) |
| JP (1) | JP4313671B2 (ru) |
| KR (1) | KR100903760B1 (ru) |
| CN (2) | CN101659639A (ru) |
| AR (1) | AR036596A1 (ru) |
| AT (1) | ATE344663T1 (ru) |
| AU (1) | AU2002333852B2 (ru) |
| BR (1) | BR0212044A (ru) |
| CA (1) | CA2456606C (ru) |
| DE (1) | DE60215960T2 (ru) |
| DK (1) | DK1429761T3 (ru) |
| ES (1) | ES2272809T3 (ru) |
| HR (1) | HRP20040085A2 (ru) |
| HU (1) | HUP0401567A3 (ru) |
| IL (2) | IL160081A0 (ru) |
| MX (1) | MXPA04002583A (ru) |
| NO (1) | NO20041176L (ru) |
| PL (1) | PL368441A1 (ru) |
| PT (1) | PT1429761E (ru) |
| RU (1) | RU2299199C2 (ru) |
| SI (1) | SI1429761T1 (ru) |
| UA (1) | UA78523C2 (ru) |
| WO (1) | WO2003026647A1 (ru) |
| ZA (1) | ZA200402099B (ru) |
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| US6117889A (en) * | 1994-04-01 | 2000-09-12 | University Of Virginia | 7-Azabicyclo-[2.2.1]-heptane and -heptene derivatives as analgesics and anti-inflammatory agents |
| US5616601A (en) * | 1994-07-28 | 1997-04-01 | Gd Searle & Co | 1,2-aryl and heteroaryl substituted imidazolyl compounds for the treatment of inflammation |
| US6103708A (en) * | 1998-05-12 | 2000-08-15 | American Home Products Corporation | Furans, benzofurans, and thiophenes useful in the treatment of insulin resistance and hyperglycemia |
| FR2789079B3 (fr) * | 1999-02-01 | 2001-03-02 | Sanofi Synthelabo | Derive d'acide pyrazolecarboxylique, sa preparation, les compositions pharmaceutiques en contenant |
| CO5170501A1 (es) | 1999-04-14 | 2002-06-27 | Novartis Ag | AZOLES SUSTITUIDOS UTILES PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR TNFa eIL-1 Y ENFERMEDADES DEL METABOLISMO OSEO |
| DZ3335A1 (fr) * | 2000-03-23 | 2001-09-27 | Solvay Pharm Bv | Derives de 4,5-dihydro-1h-pyrazole ayant une activite antagoniste de cb1 |
| IL160081A0 (en) | 2001-09-21 | 2004-06-20 | Solvay Pharm Bv | Novel 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity |
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2002
- 2002-09-17 IL IL16008102A patent/IL160081A0/xx unknown
- 2002-09-17 DK DK02799408T patent/DK1429761T3/da active
- 2002-09-17 CN CN200910141766A patent/CN101659639A/zh active Pending
- 2002-09-17 AT AT02799408T patent/ATE344663T1/de active
- 2002-09-17 DE DE60215960T patent/DE60215960T2/de not_active Expired - Lifetime
- 2002-09-17 MX MXPA04002583A patent/MXPA04002583A/es active IP Right Grant
- 2002-09-17 PT PT02799408T patent/PT1429761E/pt unknown
- 2002-09-17 RU RU2004107131/04A patent/RU2299199C2/ru not_active IP Right Cessation
- 2002-09-17 ES ES02799408T patent/ES2272809T3/es not_active Expired - Lifetime
- 2002-09-17 AU AU2002333852A patent/AU2002333852B2/en not_active Ceased
- 2002-09-17 JP JP2003530284A patent/JP4313671B2/ja not_active Expired - Fee Related
- 2002-09-17 CA CA2456606A patent/CA2456606C/en not_active Expired - Fee Related
- 2002-09-17 KR KR1020047004003A patent/KR100903760B1/ko not_active IP Right Cessation
- 2002-09-17 WO PCT/EP2002/010433 patent/WO2003026647A1/en active IP Right Grant
- 2002-09-17 SI SI200230448T patent/SI1429761T1/sl unknown
- 2002-09-17 PL PL02368441A patent/PL368441A1/xx unknown
- 2002-09-17 EP EP02799408A patent/EP1429761B1/en not_active Expired - Lifetime
- 2002-09-17 HU HU0401567A patent/HUP0401567A3/hu unknown
- 2002-09-17 UA UA20040402982A patent/UA78523C2/uk unknown
- 2002-09-17 BR BR0212044-5A patent/BR0212044A/pt not_active IP Right Cessation
- 2002-09-17 CN CNA028181891A patent/CN1555262A/zh active Pending
- 2002-09-17 US US10/490,291 patent/US7528162B2/en not_active Expired - Fee Related
- 2002-09-18 AR ARP020103506A patent/AR036596A1/es unknown
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2004
- 2004-01-27 IL IL160081A patent/IL160081A/en not_active IP Right Cessation
- 2004-01-28 HR HR20040085A patent/HRP20040085A2/hr not_active Application Discontinuation
- 2004-03-16 ZA ZA200402099A patent/ZA200402099B/en unknown
- 2004-03-19 NO NO20041176A patent/NO20041176L/no not_active Application Discontinuation
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