CZ281511B6 - Benzimidazolonové deriváty jako 5-HT1A a 5-HT2 antagonisté - Google Patents
Benzimidazolonové deriváty jako 5-HT1A a 5-HT2 antagonisté Download PDFInfo
- Publication number
- CZ281511B6 CZ281511B6 CZ94170A CZ17094A CZ281511B6 CZ 281511 B6 CZ281511 B6 CZ 281511B6 CZ 94170 A CZ94170 A CZ 94170A CZ 17094 A CZ17094 A CZ 17094A CZ 281511 B6 CZ281511 B6 CZ 281511B6
- Authority
- CZ
- Czechia
- Prior art keywords
- dihydro
- benzimidazol
- compound
- carbon atoms
- piperazin
- Prior art date
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- 239000000852 hydrogen donor Substances 0.000 description 1
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- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- ZLVXBBHTMQJRSX-VMGNSXQWSA-N jdtic Chemical compound C1([C@]2(C)CCN(C[C@@H]2C)C[C@H](C(C)C)NC(=O)[C@@H]2NCC3=CC(O)=CC=C3C2)=CC=CC(O)=C1 ZLVXBBHTMQJRSX-VMGNSXQWSA-N 0.000 description 1
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- XDPPELXCFSPXJH-UHFFFAOYSA-N n-[4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl]-2-nitroaniline Chemical compound COC1=CC=CC=C1N1CCN(CCCCNC=2C(=CC=CC=2)[N+]([O-])=O)CC1 XDPPELXCFSPXJH-UHFFFAOYSA-N 0.000 description 1
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- 150000005623 oxindoles Chemical class 0.000 description 1
- RMYUPIFLALKWOD-UHFFFAOYSA-N oxiran-2-ylmethyl n-[2-[dimethyl(trimethylsilyl)silyl]ethyl]carbamate Chemical compound C[Si](C)(C)[Si](C)(C)CCNC(=O)OCC1CO1 RMYUPIFLALKWOD-UHFFFAOYSA-N 0.000 description 1
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- 239000011736 potassium bicarbonate Substances 0.000 description 1
- 235000015497 potassium bicarbonate Nutrition 0.000 description 1
- 229910000028 potassium bicarbonate Inorganic materials 0.000 description 1
- TYJJADVDDVDEDZ-UHFFFAOYSA-M potassium hydrogencarbonate Chemical compound [K+].OC([O-])=O TYJJADVDDVDEDZ-UHFFFAOYSA-M 0.000 description 1
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- 239000003215 serotonin 5-HT2 receptor antagonist Substances 0.000 description 1
- 235000015424 sodium Nutrition 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- UIIMBOGNXHQVGW-UHFFFAOYSA-M sodium bicarbonate Substances [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 1
- HYHCSLBZRBJJCH-UHFFFAOYSA-M sodium hydrosulfide Chemical compound [Na+].[SH-] HYHCSLBZRBJJCH-UHFFFAOYSA-M 0.000 description 1
- 239000007962 solid dispersion Substances 0.000 description 1
- 239000011877 solvent mixture Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- IIACRCGMVDHOTQ-UHFFFAOYSA-N sulfamic acid group Chemical group S(N)(O)(=O)=O IIACRCGMVDHOTQ-UHFFFAOYSA-N 0.000 description 1
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- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000001302 tertiary amino group Chemical group 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- XJDNKRIXUMDJCW-UHFFFAOYSA-J titanium tetrachloride Chemical compound Cl[Ti](Cl)(Cl)Cl XJDNKRIXUMDJCW-UHFFFAOYSA-J 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
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Classifications
-
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
- C07D235/26—Oxygen atoms
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Compositions Of Macromolecular Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ITMI912118A IT1251144B (it) | 1991-07-30 | 1991-07-30 | Derivati del benzimidazolone |
| PCT/IT1992/000088 WO1993003016A1 (en) | 1991-07-30 | 1992-07-30 | Benzimidazolone derivatives as 5-ht1a and 5-ht2 antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CZ17094A3 CZ17094A3 (en) | 1994-05-18 |
| CZ281511B6 true CZ281511B6 (cs) | 1996-10-16 |
Family
ID=11360463
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CZ94170A CZ281511B6 (cs) | 1991-07-30 | 1992-07-30 | Benzimidazolonové deriváty jako 5-HT1A a 5-HT2 antagonisté |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US5576318A (enExample) |
| EP (1) | EP0526434B1 (enExample) |
| JP (1) | JP2989667B2 (enExample) |
| KR (1) | KR100263495B1 (enExample) |
| AT (1) | ATE191910T1 (enExample) |
| AU (1) | AU665366B2 (enExample) |
| CA (1) | CA2114542C (enExample) |
| CZ (1) | CZ281511B6 (enExample) |
| DE (1) | DE69230926T2 (enExample) |
| DK (1) | DK0526434T3 (enExample) |
| EE (1) | EE03070B1 (enExample) |
| ES (1) | ES2144412T3 (enExample) |
| FI (1) | FI111460B (enExample) |
| GR (1) | GR3033947T3 (enExample) |
| HU (2) | HUT70195A (enExample) |
| IE (1) | IE922464A1 (enExample) |
| IL (1) | IL102665A (enExample) |
| IT (1) | IT1251144B (enExample) |
| MX (1) | MX9204139A (enExample) |
| NO (1) | NO304070B1 (enExample) |
| NZ (1) | NZ243777A (enExample) |
| PH (1) | PH30998A (enExample) |
| PL (1) | PL171329B1 (enExample) |
| PT (1) | PT526434E (enExample) |
| RU (1) | RU2096411C1 (enExample) |
| SG (1) | SG52407A1 (enExample) |
| SK (1) | SK279292B6 (enExample) |
| TW (1) | TW209862B (enExample) |
| UA (1) | UA42684C2 (enExample) |
| WO (1) | WO1993003016A1 (enExample) |
| ZA (1) | ZA925682B (enExample) |
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| CN104926734B (zh) * | 2015-07-07 | 2017-04-05 | 苏州立新制药有限公司 | 氟班色林的制备方法 |
| WO2017076213A1 (zh) * | 2015-11-02 | 2017-05-11 | 苏州旺山旺水生物医药有限公司 | 苯并咪唑类化合物、其制备方法及用途 |
| WO2017076356A1 (zh) * | 2015-11-05 | 2017-05-11 | 苏州晶云药物科技有限公司 | 氟班色林的新晶型及其制备方法 |
| CN106749038A (zh) * | 2015-11-25 | 2017-05-31 | 山东诚创医药技术开发有限公司 | 一种氟班色林的制备方法 |
| CN106866546A (zh) * | 2015-12-10 | 2017-06-20 | 常州爱诺新睿医药技术有限公司 | 氟班色林或其药学上可接受的盐与药用辅料的固体分散体及其制备方法 |
| CN108699007A (zh) | 2016-01-31 | 2018-10-23 | 孟晓明 | 氟班色林的新晶型及其制备方法及其用途 |
| CN108349908B (zh) * | 2016-02-02 | 2021-07-20 | 深圳市塔吉瑞生物医药有限公司 | 一种取代的苯并咪唑酮化合物及包含该化合物的组合物 |
| CN107235913B (zh) * | 2016-03-29 | 2020-07-10 | 苏州科伦药物研究有限公司 | 工业规模高效制造优质氟班色林的方法 |
| CN106866582A (zh) * | 2017-01-10 | 2017-06-20 | 广州隽沐生物科技有限公司 | 一种氟班色林中间体的制备方法 |
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| US3406178A (en) * | 1964-02-04 | 1968-10-15 | Monsanto Chem Australia Ltd | Preparation of 2-substituted benzimidazoles |
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| IT1176613B (it) * | 1984-08-14 | 1987-08-18 | Ravizza Spa | Derivati piperazinici farmacologicamente attivi e processo per la loro preparazione |
| IE58370B1 (en) * | 1985-04-10 | 1993-09-08 | Lundbeck & Co As H | Indole derivatives |
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| US4954503A (en) * | 1989-09-11 | 1990-09-04 | Hoechst-Roussel Pharmaceuticals, Inc. | 3-(1-substituted-4-piperazinyl)-1H-indazoles |
| IT1251144B (it) * | 1991-07-30 | 1995-05-04 | Boehringer Ingelheim Italia | Derivati del benzimidazolone |
-
1991
- 1991-07-30 IT ITMI912118A patent/IT1251144B/it active IP Right Grant
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1992
- 1992-07-15 MX MX9204139A patent/MX9204139A/es unknown
- 1992-07-28 TW TW081105974A patent/TW209862B/zh not_active IP Right Cessation
- 1992-07-28 IL IL10266592A patent/IL102665A/en not_active IP Right Cessation
- 1992-07-29 IE IE246492A patent/IE922464A1/en not_active IP Right Cessation
- 1992-07-29 PH PH44739A patent/PH30998A/en unknown
- 1992-07-29 ZA ZA925682A patent/ZA925682B/xx unknown
- 1992-07-30 DK DK92830427T patent/DK0526434T3/da active
- 1992-07-30 WO PCT/IT1992/000088 patent/WO1993003016A1/en not_active Ceased
- 1992-07-30 PT PT92830427T patent/PT526434E/pt unknown
- 1992-07-30 AT AT92830427T patent/ATE191910T1/de active
- 1992-07-30 SG SG1996004034A patent/SG52407A1/en unknown
- 1992-07-30 KR KR1019940700293A patent/KR100263495B1/ko not_active Expired - Lifetime
- 1992-07-30 EP EP92830427A patent/EP0526434B1/en not_active Expired - Lifetime
- 1992-07-30 PL PL92302163A patent/PL171329B1/pl unknown
- 1992-07-30 HU HU9400255A patent/HUT70195A/hu unknown
- 1992-07-30 UA UA94005462A patent/UA42684C2/uk unknown
- 1992-07-30 CA CA002114542A patent/CA2114542C/en not_active Expired - Lifetime
- 1992-07-30 NZ NZ243777A patent/NZ243777A/en unknown
- 1992-07-30 AU AU24275/92A patent/AU665366B2/en not_active Expired
- 1992-07-30 RU RU9294015171A patent/RU2096411C1/ru active
- 1992-07-30 SK SK101-94A patent/SK279292B6/sk unknown
- 1992-07-30 ES ES92830427T patent/ES2144412T3/es not_active Expired - Lifetime
- 1992-07-30 DE DE69230926T patent/DE69230926T2/de not_active Expired - Lifetime
- 1992-07-30 CZ CZ94170A patent/CZ281511B6/cs not_active IP Right Cessation
- 1992-07-30 JP JP50345393A patent/JP2989667B2/ja not_active Expired - Lifetime
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1994
- 1994-01-28 FI FI940420A patent/FI111460B/fi not_active IP Right Cessation
- 1994-01-28 NO NO940306A patent/NO304070B1/no not_active IP Right Cessation
- 1994-03-23 US US08/216,742 patent/US5576318A/en not_active Expired - Lifetime
- 1994-11-23 EE EE9400396A patent/EE03070B1/xx unknown
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1995
- 1995-06-20 HU HU95P/P00292P patent/HU211256A9/hu unknown
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2000
- 2000-07-12 GR GR20000401632T patent/GR3033947T3/el unknown
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| IF00 | In force as of 2000-06-30 in czech republic | ||
| MK4A | Patent expired |
Effective date: 20120730 |