RU93033485A - Производные индола, фармацевтическая композиция, способ лечения - Google Patents
Производные индола, фармацевтическая композиция, способ леченияInfo
- Publication number
- RU93033485A RU93033485A RU93033485/04A RU93033485A RU93033485A RU 93033485 A RU93033485 A RU 93033485A RU 93033485/04 A RU93033485/04 A RU 93033485/04A RU 93033485 A RU93033485 A RU 93033485A RU 93033485 A RU93033485 A RU 93033485A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- aryl
- hydrogen
- compounds
- headaches
- Prior art date
Links
- SIKJAQJRHWYJAI-UHFFFAOYSA-N indole Chemical class C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 206010019233 Headache Diseases 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000002877 alkyl aryl group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 231100000869 headache Toxicity 0.000 claims 2
- 201000011528 vascular disease Diseases 0.000 claims 2
- 206010002855 Anxiety Diseases 0.000 claims 1
- 206010057666 Anxiety disease Diseases 0.000 claims 1
- 210000003169 Central Nervous System Anatomy 0.000 claims 1
- 208000008466 Metabolic Disease Diseases 0.000 claims 1
- 206010027599 Migraine Diseases 0.000 claims 1
- 208000008085 Migraine Disorders Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 239000002220 antihypertensive agent Substances 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 125000005418 aryl aryl group Chemical group 0.000 claims 1
- 125000005518 carboxamido group Chemical group 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 230000000862 serotonergic Effects 0.000 claims 1
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims 1
- 239000000952 serotonin receptor agonist Substances 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000003071 vasodilator agent Substances 0.000 claims 1
Claims (1)
- Предложены соединения формулы
где n = 0, 1 или 2, R1 представляет водород, R2 представляет водород, галоген, циано, OR4, -(CH2)m- (C=O) NR5R6, -(CH2)m- SO2NR5R6, -(CH2)m-NR7(C= O)R8, -(CH2)m-NR7SO2R8, -(CH2)m-S(O)xR8, -(CH2)m-NR2(C= O)NR5R6, -(CH2)m-NR7(C= O)OR9 и -CH=CH(CH2)yR1 0; R3 представляет водород или С1 - 6 -алкил, который может быть линейным или разветвленным, R4 представляет водород, С1 - 6 -алкил или арил, R5 и R6 независимо друг от друга представляют водород, С1 - 6 -алкил, арил или С1 - 3 -алкил-арил или R5 и R6 вместе образуют 4-, 5- или 6-членное кольцо, R7 и R8 независимо друг от друга представляют водород, С1 - 6 -алкил, арил или С1 - 3 -алкил-арил, R9 - водород, С1 - 6 -алкил, арил или С1 - 3 -алкил-арил, R1 0 представляет -C=O)NR5R6 и SO2NR5R6, где R5 и R6 имеют указанные выше значения, а также -NR7(C=O)R8, -NR7SO2R8, -NR7(C= O)NR5R6, -S(O)xR8 и -NR7(C= O)OR9, в которых R7, R8 и R9 имеют указанные выше значения; Y = 0, 1, 2; X = 1 или 2, m = 0, 1, 2 или 3, а упомянутые арильные группы или арильные фрагменты алкиларильных групп - независимые друг от друга фенил и замещенный фенил, причем замещенный фенил может быть замещен на 1 - 3 группы из ряда С1 - 4 -алкила, галогена, гидрокси, циано, карбоксамидо, нитро, а также С1 - 4 -алкокси, и их фармацевтически приемлемые соли. Эти соединения могут применяться как психотерапевтические средства, а также вследствие того, что в их составе содержится 5-НТ1 -агонист серотонина, могут быть использованы для лечения депрессии, чувства страха и беспокойства, нарушения обмена, связанного с сосудистыми расстройствами, тучности, головных болей, мигрени, болевых ощущений, приступов хронических головных болей и головных болей, обусловленных сосудистыми нарушениями, а также других расстройств, связанных с недостаточностью серотонергической нейромедитации. Соединения могут быть полезны также как противогипертонические и сосудорасширяющие средства, действующие на центральную нервную систему.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US59792890A | 1990-10-15 | 1990-10-15 | |
| US597928 | 1990-10-15 | ||
| PCT/US1991/007194 WO1992006973A1 (en) | 1990-10-15 | 1991-10-08 | Indole derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU93033485A true RU93033485A (ru) | 1996-02-27 |
| RU2095360C1 RU2095360C1 (ru) | 1997-11-10 |
Family
ID=24393510
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU9193033485A RU2095360C1 (ru) | 1990-10-15 | 1991-10-08 | Производные индола, их оптические изомеры и фармацевтически приемлемые соли |
Country Status (33)
| Country | Link |
|---|---|
| EP (1) | EP0592438B1 (ru) |
| JP (2) | JP2575272B2 (ru) |
| KR (1) | KR0179053B1 (ru) |
| CN (1) | CN1039322C (ru) |
| AT (1) | ATE157361T1 (ru) |
| AU (1) | AU651637B2 (ru) |
| BG (1) | BG61975B1 (ru) |
| BR (2) | BR9106978A (ru) |
| CA (1) | CA2091562C (ru) |
| DE (3) | DE9190141U1 (ru) |
| DK (1) | DK0592438T5 (ru) |
| EG (1) | EG20224A (ru) |
| ES (1) | ES2104733T3 (ru) |
| FI (1) | FI105812B (ru) |
| GR (1) | GR3025087T3 (ru) |
| HU (2) | HU225055B1 (ru) |
| IE (1) | IE913555A1 (ru) |
| IL (3) | IL115117A (ru) |
| LU (1) | LU90902I2 (ru) |
| MX (1) | MX9101606A (ru) |
| MY (1) | MY111683A (ru) |
| NL (1) | NL300070I2 (ru) |
| NO (3) | NO305121B1 (ru) |
| NZ (2) | NZ240217A (ru) |
| OA (1) | OA09874A (ru) |
| PL (3) | PL168919B1 (ru) |
| PT (1) | PT99218B (ru) |
| RO (1) | RO111767B1 (ru) |
| RU (1) | RU2095360C1 (ru) |
| SG (1) | SG54270A1 (ru) |
| WO (1) | WO1992006973A1 (ru) |
| YU (1) | YU48088B (ru) |
| ZA (1) | ZA918156B (ru) |
Families Citing this family (72)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5559129A (en) * | 1990-10-15 | 1996-09-24 | Pfizer Inc | Indole derivatives |
| US5545644A (en) * | 1990-10-15 | 1996-08-13 | Pfizer Inc. | Indole derivatives |
| US5578612A (en) * | 1990-10-15 | 1996-11-26 | Pfizer Inc. | Indole derivatives |
| US5559246A (en) * | 1990-10-15 | 1996-09-24 | Pfizer Inc. | Indole derivatives |
| US5607951A (en) * | 1990-10-15 | 1997-03-04 | Pfizer Inc | Indole derivatives |
| EP0619805B1 (en) * | 1991-11-25 | 2000-03-15 | Pfizer Inc. | 5-(hetero- or carbocyclylamino)-indole derivatives, their preparation and their use as 5-ht1 agonists |
| TW288010B (ru) * | 1992-03-05 | 1996-10-11 | Pfizer | |
| US5747501A (en) * | 1992-04-07 | 1998-05-05 | Pfizer, Inc. | Indole derivatives |
| GB9207930D0 (en) * | 1992-04-10 | 1992-05-27 | Pfizer Ltd | Indoles |
| UA34452C2 (ru) * | 1992-04-10 | 2001-03-15 | Пфайзер Інк. | Производные ациламиноиндола, проявляющие серотониновую 5-нт1 агонистичную активность и производные аминоиндола как промежуточные соединения |
| GB9208161D0 (en) * | 1992-04-14 | 1992-05-27 | Pfizer Ltd | Indoles |
| GB9210400D0 (en) * | 1992-05-15 | 1992-07-01 | Merck Sharp & Dohme | Therapeutic agents |
| GB9211277D0 (en) | 1992-05-28 | 1992-07-15 | Glaxo Group Inc | Pharmaceutical compositions |
| TW251284B (ru) * | 1992-11-02 | 1995-07-11 | Pfizer | |
| FR2701026B1 (fr) * | 1993-02-02 | 1995-03-31 | Adir | Nouveaux dérivés de l'indole, de l'indazole et du benzisoxazole, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent. |
| IT1271352B (it) * | 1993-04-08 | 1997-05-27 | Boehringer Ingelheim Italia | Derivati dell'indolo utili nel trattamento dei disturbi del sistema nervoso centrale |
| CA2157397C (en) * | 1993-04-22 | 1999-07-06 | Martin James Wythes | Indole derivatives as 5-ht1-like agonists for use in migraine |
| AP486A (en) * | 1993-04-27 | 1996-04-16 | Pfizer | Indole derivatives. |
| ES2070772B1 (es) * | 1993-08-09 | 1996-02-16 | Pfizer | Derivados de acilaminoindol |
| CZ59996A3 (en) * | 1993-08-31 | 1996-06-12 | Pfizer | 5-arylindole derivatives per se and for treating diseases, intermediates for their preparation and pharmaceutical compositions based thereon |
| CA2195850A1 (en) * | 1994-08-03 | 1996-02-15 | Guillaume Lebaut | Substituted indoles |
| GB9417310D0 (en) * | 1994-08-27 | 1994-10-19 | Pfizer Ltd | Therapeutic agents |
| EP0804433B1 (en) * | 1994-10-12 | 2002-09-18 | Pfizer Limited | Indole derivative for the treatment of migraine |
| GB9420529D0 (en) | 1994-10-12 | 1994-11-30 | Pfizer Ltd | Indoles |
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| GB9424471D0 (en) * | 1994-12-03 | 1995-01-18 | Pfizer Ltd | Treatment of emesis |
| JPH11502816A (ja) * | 1995-03-20 | 1999-03-09 | イーライ・リリー・アンド・カンパニー | ５−置換−３−（１，２，３，６−テトラヒドロピリジン−４−イル）−および３−（ピペリジン−４−イル）−１ｈ−インドール類：新規５−ｈｔ▲下１ｆ▼アゴニスト |
| GB9510223D0 (en) * | 1995-05-20 | 1995-07-19 | Pfizer Ltd | Therapeutic agent |
| US5945118A (en) * | 1995-09-29 | 1999-08-31 | Pfizer Inc | Indole derivative for the treatment of migraine |
| GB9714383D0 (en) * | 1997-07-08 | 1997-09-10 | Pfizer Ltd | Improved process |
| WO1999053956A1 (fr) * | 1998-04-16 | 1999-10-28 | Yamanouchi Pharmaceutical Co., Ltd. | Remedes contre l'obesite |
| GB9816556D0 (en) * | 1998-07-30 | 1998-09-30 | Pfizer Ltd | Therapy |
| US5994352A (en) * | 1998-11-13 | 1999-11-30 | Pfizer Inc. | 5-arylindole derivatives |
| GB9825988D0 (en) | 1998-11-27 | 1999-01-20 | Pfizer Ltd | Indole derivatives |
| GB9922963D0 (en) * | 1999-09-28 | 1999-12-01 | Pfizer Ltd | Polymorphic salt |
| JP2000336074A (ja) | 1999-03-24 | 2000-12-05 | Sumitomo Chem Co Ltd | ［２−（アリールスルホニル）エテニル］ベンゼン誘導体の製造方法 |
| GB9915231D0 (en) | 1999-06-29 | 1999-09-01 | Pfizer Ltd | Pharmaceutical complex |
| KR20020035857A (ko) * | 1999-08-26 | 2002-05-15 | 후지야마 아키라 | 인돌 유도체 또는 그의 염의 제조방법 |
| GB9923314D0 (en) * | 1999-10-01 | 1999-12-08 | Pfizer Ltd | Acylation process |
| FR2799463B1 (fr) * | 1999-10-12 | 2004-04-16 | Adir | Nouveaux composes cyano-indoles inhibiteurs de recapture de serotonine, leur procede de preparation et ces compositions pharmaceutiques qui les contiennent |
| US20030166704A1 (en) | 2000-12-20 | 2003-09-04 | Pfizer Inc. | New process |
| GB0031094D0 (en) * | 2000-12-20 | 2001-01-31 | Pfizer Ltd | New Process |
| US8329734B2 (en) | 2009-07-27 | 2012-12-11 | Afgin Pharma Llc | Topical therapy for migraine |
| ES2453164T3 (es) | 2001-08-15 | 2014-04-04 | Pharmacia & Upjohn Company Llc | Cristales que incluyen una sal de ácido málico de N-[2-(dietilamino)etil]-5-[(5-fluoro-1,2-dihidro-2-oxo-3H-indol-3-iliden)metil]-2,4-dimetil-1H-pirrol-3-carboxamida, procedimientos para su preparación y sus composiciones |
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| ATE456557T1 (de) | 2005-06-15 | 2010-02-15 | Pfizer Ltd | Substituierte arylpyrazole zur verwendung gegen parasiten |
| US7645786B2 (en) | 2005-06-15 | 2010-01-12 | Pfizer Inc. | Substituted arylpyrazoles |
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| JP2011526889A (ja) | 2008-06-30 | 2011-10-20 | アフギン ファーマ，エルエルシー | 局所局部的神経作用療法 |
| EP2149573A1 (en) * | 2008-08-01 | 2010-02-03 | Laboratorios Del. Dr. Esteve, S.A. | Substituted indole sulfonamide compounds their preparation and use as medicaments |
| IT1393700B1 (it) | 2009-04-22 | 2012-05-08 | F S I Fabbrica Italiana Sint | Sintesi di 3-{[(2r)-1-metilpirrolidin-2-il]metil}-5-[2-(fenilsulfonil)etil]-1h-indolo |
| WO2011004391A2 (en) | 2009-06-25 | 2011-01-13 | Matrix Laboratories Ltd | An improved process for the preparation of eletriptan and its salt thereof |
| WO2011024039A1 (en) * | 2009-08-25 | 2011-03-03 | Ramesh Babu Potluri | Synthesis of novel 5-(2-(phenylsulfonyl)ethyl)-1h-indole derivatives |
| US8754239B2 (en) | 2010-01-19 | 2014-06-17 | Sms Pharmaceuticals Limited | Process for preparing eletriptan hydrobromide having α-form |
| CN102606426B (zh) * | 2012-03-02 | 2014-05-21 | 王仲彦 | 踏步健身发电装置 |
| WO2014063752A1 (en) | 2012-10-26 | 2014-05-01 | Synthon Bv | Process for making crystalline form alpha of eletriptan hydrobromide |
| JP6440625B2 (ja) | 2012-11-14 | 2018-12-19 | ザ・ジョンズ・ホプキンス・ユニバーシティー | 精神分裂病を処置するための方法および組成物 |
| CN103408535B (zh) * | 2013-08-13 | 2016-03-02 | 张家港威胜生物医药有限公司 | 一种依来曲普坦中间体-5-溴-3-(n-甲基吡咯啉-2-基甲基)-1h-吲哚合成工艺 |
| BR112017018944A2 (pt) | 2015-03-02 | 2018-05-15 | Afgin Pharma Llc | método de tratamento de um estado ou condição de doença em humanos com um medicamento carbinóide, e, método de tratamento de um estado ou condição de doença em um mamífero diferente de um humano com medicamento(s) carbinóide(s) |
| US10383816B2 (en) | 2015-03-02 | 2019-08-20 | Afgin Pharma, Llc | Topical regional neuro-affective therapy with cannabinoid combination products |
| JP2019502761A (ja) | 2016-01-21 | 2019-01-31 | ラボラトリオス レヴィ エセエレ | （（ｒ）−３−［（−１−メチルピロリジン−２−イル）メチル］−５−（２−フェニルスルホニルエチル）−１ｈ−インドールを作製する方法 |
| CN106065008B (zh) * | 2016-06-16 | 2018-06-05 | 黑龙江中医药大学 | 一种具有改善睡眠作用的吲哚-2-酰胺类化合物及其应用 |
| US20180049994A1 (en) | 2016-08-16 | 2018-02-22 | Afgin Pharma, Llc | Topical regional neuro-affective therapy with caryophyllene |
| TR201616365A1 (tr) | 2016-11-14 | 2018-05-21 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Deksketoprofen ve eletri̇ptanin oral farmasöti̇k kompozi̇syonlari |
| TR201619983A2 (tr) | 2016-12-29 | 2018-07-23 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Di̇klofenak ve eletri̇ptanin farmasöti̇k formülasyonlari |
| KR102129947B1 (ko) | 2018-06-08 | 2020-07-03 | 김종창 | 콘크리트 타설을 위한 입체형 와이어 메쉬 |
| EP3766483A1 (en) | 2019-07-19 | 2021-01-20 | BioPharma Synergies, S. L. | Orodispersible powder composition comprising a triptan |
| CA3157466A1 (en) | 2020-01-22 | 2021-07-29 | Diana Sofia CHAPELA DUARTE PIRES | Eletriptan hydrobromide for treatment of spinal cord injury and improvement of locomotor function |
| WO2023150547A2 (en) * | 2022-02-01 | 2023-08-10 | Caamtech, Inc. | Psychedelic compounds and their therapeutic uses |
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|---|---|---|---|---|
| NL74527C (ru) * | ||||
| US2773875A (en) * | 1952-03-28 | 1956-12-11 | Hoffmann La Roche | Indole derivatives and method for producing same |
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| GB8819024D0 (en) * | 1988-08-10 | 1988-09-14 | Glaxo Group Ltd | Chemical compounds |
-
1991
- 1991-10-08 WO PCT/US1991/007194 patent/WO1992006973A1/en active IP Right Grant
- 1991-10-08 BR BR919106978A patent/BR9106978A/pt not_active Application Discontinuation
- 1991-10-08 AU AU89504/91A patent/AU651637B2/en not_active Expired
- 1991-10-08 PL PL91298945A patent/PL168919B1/pl unknown
- 1991-10-08 CA CA002091562A patent/CA2091562C/en not_active Expired - Lifetime
- 1991-10-08 RU RU9193033485A patent/RU2095360C1/ru active
- 1991-10-08 DE DE9190141U patent/DE9190141U1/de not_active Expired - Lifetime
- 1991-10-08 PL PL91310853A patent/PL169987B1/pl unknown
- 1991-10-08 DK DK91920239T patent/DK0592438T5/da active
- 1991-10-08 HU HU9301098A patent/HU225055B1/hu active Protection Beyond IP Right Term
- 1991-10-08 DE DE2002199004 patent/DE10299004I2/de active Active
- 1991-10-08 PL PL91310852A patent/PL170330B1/pl unknown
- 1991-10-08 KR KR1019930701121A patent/KR0179053B1/ko not_active IP Right Cessation
- 1991-10-08 HU HU9301098A patent/HUT64326A/hu unknown
- 1991-10-08 AT AT91920239T patent/ATE157361T1/de active
- 1991-10-08 RO RO93-00511A patent/RO111767B1/ro unknown
- 1991-10-08 EP EP91920239A patent/EP0592438B1/en not_active Expired - Lifetime
- 1991-10-08 DE DE69127468T patent/DE69127468T2/de not_active Expired - Lifetime
- 1991-10-08 ES ES91920239T patent/ES2104733T3/es not_active Expired - Lifetime
- 1991-10-08 JP JP4500646A patent/JP2575272B2/ja not_active Expired - Lifetime
- 1991-10-09 IL IL11511791A patent/IL115117A/en not_active IP Right Cessation
- 1991-10-09 IL IL9970191A patent/IL99701A/en active Protection Beyond IP Right Term
- 1991-10-14 CN CN91109924A patent/CN1039322C/zh not_active Expired - Lifetime
- 1991-10-14 NZ NZ240217A patent/NZ240217A/en not_active IP Right Cessation
- 1991-10-14 ZA ZA918156A patent/ZA918156B/xx unknown
- 1991-10-14 NZ NZ270675A patent/NZ270675A/en not_active IP Right Cessation
- 1991-10-14 PT PT99218A patent/PT99218B/pt not_active IP Right Cessation
- 1991-10-14 YU YU165391A patent/YU48088B/sh unknown
- 1991-10-14 EG EG61791A patent/EG20224A/xx active
- 1991-10-15 MY MYPI91001896A patent/MY111683A/en unknown
- 1991-10-15 MX MX9101606A patent/MX9101606A/es unknown
- 1991-10-16 IE IE355591A patent/IE913555A1/en active Protection Beyond IP Right Term
-
1993
- 1993-04-14 FI FI931667A patent/FI105812B/fi not_active IP Right Cessation
- 1993-04-14 NO NO931378A patent/NO305121B1/no not_active IP Right Cessation
- 1993-04-14 BG BG97632A patent/BG61975B1/bg unknown
- 1993-04-14 OA OA60364A patent/OA09874A/en unknown
-
1995
- 1995-08-31 IL IL11511795A patent/IL115117A0/xx unknown
-
1996
- 1996-03-30 SG SG1996006865A patent/SG54270A1/en unknown
- 1996-06-10 JP JP8147639A patent/JP2677777B2/ja not_active Expired - Lifetime
- 1996-11-12 BR BR1100080-5A patent/BR1100080A/pt active IP Right Grant
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1997
- 1997-10-20 GR GR970402728T patent/GR3025087T3/el unknown
-
1998
- 1998-12-01 NO NO985607A patent/NO985607D0/no unknown
-
2001
- 2001-11-09 NO NO2001019C patent/NO2001019I1/no unknown
- 2001-11-16 NL NL300070C patent/NL300070I2/nl unknown
-
2002
- 2002-03-20 LU LU90902C patent/LU90902I2/fr unknown
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