AR006705A1 - Compuestos de 3-[4-(2-fenil-indol-1-ilmetil)-fenil]-acrilamida y 2-fenil-1-[4-(amino-1-il-alqu-1-inil)-bencil]-1h-indol-5-ol, metodo para preparar medicamentos y composiciones farmaceuticas que los contiene - Google Patents
Compuestos de 3-[4-(2-fenil-indol-1-ilmetil)-fenil]-acrilamida y 2-fenil-1-[4-(amino-1-il-alqu-1-inil)-bencil]-1h-indol-5-ol, metodo para preparar medicamentos y composiciones farmaceuticas que los contieneInfo
- Publication number
- AR006705A1 AR006705A1 ARP970101579A ARP970101579A AR006705A1 AR 006705 A1 AR006705 A1 AR 006705A1 AR P970101579 A ARP970101579 A AR P970101579A AR P970101579 A ARP970101579 A AR P970101579A AR 006705 A1 AR006705 A1 AR 006705A1
- Authority
- AR
- Argentina
- Prior art keywords
- phenyl
- alkyl
- compounds
- indol
- group
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/12—Radicals substituted by oxygen atoms
Abstract
Nuevos compuestos de 3-[4-(2-Fenil-Indol-1-ilmetil)-Fenil]-Acrilamida y nuevos compuestos de 2-Fenil-1-[4-(amino-1il-alqu-1-inil)bencil]-1H-indol-5-ol,que son útiles como agentes estrógenos, así como también con composiciones farmacéuticasy métodos de preparación de medicamentos utilizando estoscompuestos, teniendo los compuestos las fórmulas I y II, en donde R1 es seleccionado de H, OH o los alquil éteres o ésteres C1-C4 de los mismos, ohalógeno; R2, R3, R4, R5 y R6 sonindepe ndientemente seleccionados de H, OH o los alquil éteres o ésteres C1-C4 de los mismos, halógeno, ciano, alquilo C1-C6o trifluormetilo, con la condición de que, cuando R1 es H, R2 no es OH; n es 2 o 3 ; X es seleccionado de H, alquiloC1-C6, ciano, nitro trifluormetilo,halógeno; Z es seleccionado de la fórmula III a) la porción -NR7R8en donde R7 y R8 son independientemente seleccionados del grupo de H alquilo C1-C6 fenilo ocombinados por -(CH2)p, en donde p es un entero de desde2 a 6, de mane ra de formar un anillo, siendo el anillo opcionalmente substituido por hasta tressubstituyentes seleccionados del grupo de hidrógeno, hidróxilo, halo, alquilo C1-C4 trihalomelilo, alcoxi, C1-C4, trihalometoxi, alquiltioC1-C4alquilsulfinil C1-C4 , alquilsulfonil C1-C4, hidroxi alquilo (C1-C4)-CO2H-CN- CONHalquilo (C1-C4)-NH2, alquilamino C1-C4, dialquilamino C1-C4-NHOS2alquilo (C1-C4), -NHCOalquilo(C1-C4), y -NO2; b) un heterociclo de cinco, seis o sietemiembros saturado, insaturado o parcialmente insaturado, que contien hasta dosheteroátomos seleccionados del grupo que consiste en -O-, -NH-Nalquilo C1C4)-, N= y -S(O)m en donde m es un entero de desde 0-2 opcionalmente substituido con1-3substituyentes independientemente selecc ionados del grupo que consiste de hidrógeno, hidroxilo, halo, alquilo C1-C4, trihalomelilo, alcoxi C1-C4
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63397296A | 1996-04-19 | 1996-04-19 | |
| US63397696A | 1996-04-19 | 1996-04-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR006705A1 true AR006705A1 (es) | 1999-09-08 |
Family
ID=27092024
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP970101579A AR006705A1 (es) | 1996-04-19 | 1997-04-18 | Compuestos de 3-[4-(2-fenil-indol-1-ilmetil)-fenil]-acrilamida y 2-fenil-1-[4-(amino-1-il-alqu-1-inil)-bencil]-1h-indol-5-ol, metodo para preparar medicamentos y composiciones farmaceuticas que los contiene |
Country Status (24)
| Country | Link |
|---|---|
| EP (1) | EP0802184B1 (es) |
| JP (1) | JPH1036347A (es) |
| KR (1) | KR970069986A (es) |
| CN (1) | CN1103756C (es) |
| AR (1) | AR006705A1 (es) |
| AT (1) | ATE219485T1 (es) |
| AU (1) | AU718888B2 (es) |
| BR (1) | BR9701879A (es) |
| CO (1) | CO4950540A1 (es) |
| CZ (1) | CZ293065B6 (es) |
| DE (1) | DE69713441T2 (es) |
| DK (1) | DK0802184T3 (es) |
| EA (1) | EA000815B1 (es) |
| ES (1) | ES2179273T3 (es) |
| HK (1) | HK1002862A1 (es) |
| HU (1) | HUP9700779A1 (es) |
| ID (1) | ID16618A (es) |
| IL (1) | IL120699A0 (es) |
| NO (1) | NO308214B1 (es) |
| NZ (1) | NZ314595A (es) |
| PT (1) | PT802184E (es) |
| SK (1) | SK282765B6 (es) |
| TW (1) | TW397821B (es) |
| UA (1) | UA47413C2 (es) |
Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1082319B1 (en) * | 1998-05-12 | 2006-09-13 | Wyeth | Benzocarbazole and indenoindole derived estrogenic agents |
| US6069153A (en) * | 1998-05-12 | 2000-05-30 | American Home Products Corporation | Indenoindoles and benzocarbazoles as estrogenic agents |
| PT1076558E (pt) * | 1998-05-15 | 2003-11-28 | Wyeth Corp | 2-fenil-1-¬4-(2-aminoetoxi)-benzil|-indole em combinacao com estrogenios |
| EP1080073A1 (en) * | 1998-05-15 | 2001-03-07 | American Home Products Corporation | Compositions comprising 2-phenyl-indole compounds and estrogen formulations |
| US6479535B1 (en) | 1998-05-15 | 2002-11-12 | Wyeth | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations |
| US7005428B1 (en) | 1998-06-11 | 2006-02-28 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
| US6465445B1 (en) * | 1998-06-11 | 2002-10-15 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
| AU2004200099B2 (en) * | 1998-06-11 | 2006-11-02 | Endorecherche, Inc. | Medical Uses of A Selective Estrogen Receptor Modulator in Combination with Sex Steroid Precursors |
| CN1196708C (zh) * | 1999-09-13 | 2005-04-13 | 惠氏公司 | 2－(4－羟基－苯基)－1－[4－(2－氨－1－基－乙氧基)－苄基]－1h－吲哚－5－酚的吡喃葡糖苷轭合物 |
| AU2001271784A1 (en) * | 2000-07-06 | 2002-01-21 | Wyeth | Therapy for prosthesis-related bone degeneration |
| US6369051B1 (en) | 2000-07-06 | 2002-04-09 | American Home Products Corporation | Combinations of SSRI and estrogenic agents |
| AU2001271781A1 (en) * | 2000-07-06 | 2002-01-21 | Wyeth | Use of substituted indole compounds for treating sphincter incontinence |
| AR030064A1 (es) * | 2000-07-06 | 2003-08-13 | Wyeth Corp | Metodos para inhibir los efectos uterotroficos de los agentes estrogenicos |
| US6376486B1 (en) | 2000-07-06 | 2002-04-23 | American Home Products Corporation | Methods of inhibiting sphincter incontinence |
| AR029538A1 (es) * | 2000-07-06 | 2003-07-02 | Wyeth Corp | Composiciones farmaceuticas de agentes estrogenicos |
| WO2002003986A2 (en) * | 2000-07-06 | 2002-01-17 | Wyeth | Use of substituted indole compounds for treating breast disorders |
| WO2002003991A2 (en) * | 2000-07-06 | 2002-01-17 | Wyeth | Use of substituted indole compounds for increasing nitric oxide synthase activity |
| AR029539A1 (es) | 2000-07-06 | 2003-07-02 | Wyeth Corp | Combinaciones de estatinas y agentes estrogenicos |
| US6455568B2 (en) | 2000-07-06 | 2002-09-24 | Wyeth | Combination therapy for inhibiting sphincter incontinence |
| US6358991B2 (en) | 2000-07-06 | 2002-03-19 | American Home Products Corporation | Methods of treating neuropeptide Y-related conditions |
| WO2002003975A2 (en) * | 2000-07-06 | 2002-01-17 | Wyeth | Combinations of ssri and estrogenic agents |
| EP1656938A1 (en) | 2000-07-06 | 2006-05-17 | Wyeth | Combinations of SSRI and estrogenic agents |
| WO2002003990A2 (en) * | 2000-07-06 | 2002-01-17 | Wyeth | Use of substituted insole compounds for treating excessive intraocular pressure |
| DE60124322T2 (de) * | 2000-08-24 | 2007-05-31 | University Of Tennessee Research Foundation, Knoxville | Selektive modulatoren des androgenrezeptors und methoden zu deren verwendung |
| EP1395563B1 (en) | 2001-05-22 | 2006-03-29 | Eli Lilly And Company | 2-substituted 1,2,3,4-tetrahydroquinolines and derivatives thereof, compositions and methods |
| ES2236536T3 (es) | 2001-05-22 | 2005-07-16 | Eli Lilly And Company | Derivados tetrahidroquinolino para la inhibicion de enfermedades asociadas con la privacion de estrogenos o con una respuesta fisiologica aberrante a estrogenos endogenos. |
| UA86055C2 (ru) | 2004-04-07 | 2009-03-25 | Уайет | Кристаллическая форма в базедоксифена ацетата |
| TWI346105B (en) | 2004-04-07 | 2011-08-01 | Wyeth Corp | Crystalline polymorph of bazedoxifene acetate |
| RU2006132181A (ru) | 2004-04-08 | 2008-05-20 | Вайет (Us) | Базедоксифен аскорбат в качестве селективного модулятора рецептора эстрогена |
| US7868037B2 (en) | 2004-07-14 | 2011-01-11 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| US7772271B2 (en) | 2004-07-14 | 2010-08-10 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| KR20070083484A (ko) | 2004-07-14 | 2007-08-24 | 피티씨 테라퓨틱스, 인크. | Ｃ형 간염 치료 방법 |
| US7781478B2 (en) | 2004-07-14 | 2010-08-24 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| AU2005275182A1 (en) | 2004-07-22 | 2006-02-23 | Ptc Therapeutics, Inc. | Thienopyridines for treating Hepatitis C |
| JP5057983B2 (ja) | 2004-10-20 | 2012-10-24 | アンドルシェルシュ・インコーポレイテッド | 閉経後の女性における膣乾燥および性機能障害の予防および処置のための性ステロイド前駆体単独あるいは選択的エストロゲン受容体モジュレータならびに／またはエストロゲン類および／もしくは５型ｃＧＭＰホスホジエステラーゼ阻害剤の併用 |
| ZA200708179B (en) | 2005-04-22 | 2009-12-30 | Alantos Pharmaceuticals Holding Inc | Dipeptidyl peptidase-IV inhibitors |
| US8268806B2 (en) | 2007-08-10 | 2012-09-18 | Endorecherche, Inc. | Pharmaceutical compositions |
| US20100317635A1 (en) | 2009-06-16 | 2010-12-16 | Endorecherche, Inc. | Treatment of hot flushes, vasomotor symptoms, and night sweats with sex steroid precursors in combination with selective estrogen receptor modulators |
| KR20170127044A (ko) | 2010-06-16 | 2017-11-20 | 앙도르쉐르슈 인코포레이티드 | 에스트로겐-관련 질병의 치료 또는 예방 방법 |
| US9744177B2 (en) | 2014-03-10 | 2017-08-29 | Endorecherche, Inc. | Treatment of male androgen deficiency symptoms or diseases with sex steroid precursor combined with SERM |
| CN107847498B (zh) | 2015-05-29 | 2021-04-13 | 卫材R&D管理有限公司 | 四取代的烯烃化合物及其用途 |
| WO2017059139A1 (en) | 2015-10-01 | 2017-04-06 | Olema Pharmaceuticals, Inc. | TETRAHYDRO-1H-PYRIDO[3,4-b]INDOLE ANTI-ESTROGENIC DRUGS |
| DK3386500T3 (da) | 2015-12-09 | 2022-12-12 | Univ Illinois | Benzothiophen-baserede selektive østrogenreceptor ned-regulatorer |
| EP3434668B1 (en) * | 2016-03-25 | 2020-08-26 | Luoxin Pharmaceutical (Shanghai) Co., Ltd. | Indolo-substituted-piperidine compounds as estrogen receptor degrading agent |
| EP3455218A4 (en) | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| WO2017197036A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| WO2017197055A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| CA3028751A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Pyrimidine-based antiproliferative agents |
| WO2018081168A2 (en) | 2016-10-24 | 2018-05-03 | The Board Of Trustees Of The University Of Illinois | Benzothiophene-based selective mixed estrogen receptor downregulators |
| CA3041986A1 (en) | 2016-11-28 | 2018-05-31 | Eisai R&D Management Co., Ltd. | Salts of indazole derivative and crystals thereof |
| CN110177554B (zh) | 2017-01-06 | 2023-06-02 | G1治疗公司 | 用于治疗癌症的组合疗法 |
| KR20190117582A (ko) | 2017-02-10 | 2019-10-16 | 쥐원 쎄라퓨틱스, 인크. | 벤조티오펜 에스트로겐 수용체 조정제 |
| EP3645001A4 (en) | 2017-06-29 | 2020-12-02 | G1 Therapeutics, Inc. | MORPHIC FORMS OF GIT38 AND THEIR MANUFACTURING PROCESSES |
| CN113453679A (zh) | 2018-12-20 | 2021-09-28 | C4医药公司 | 靶向蛋白降解 |
| WO2024030968A1 (en) | 2022-08-03 | 2024-02-08 | Brystol-Myers Squibb Company | Compounds for modulating ret protein |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3232968A1 (de) * | 1981-09-10 | 1983-06-09 | Degussa Ag, 6000 Frankfurt | Neue 2-(hydroxy-phenyl)-indole und verfahren zu deren herstellung |
| DE3821148A1 (de) * | 1988-06-23 | 1989-12-28 | Erwin Von Dr Angerer | Aminoalkylindole, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate |
| US5395842A (en) * | 1988-10-31 | 1995-03-07 | Endorecherche Inc. | Anti-estrogenic compounds and compositions |
| GB9108811D0 (en) * | 1991-04-24 | 1991-06-12 | Erba Carlo Spa | N-imidazolyl derivatives of substituted indole |
| RU2061694C1 (ru) * | 1991-09-11 | 1996-06-10 | Е.Р.Сквибб энд Санз, Инк., | Производные индола |
| FR2708605A1 (fr) * | 1993-07-30 | 1995-02-10 | Sanofi Sa | Dérivés du N-sulfonylindol-2-one, leur préparation, les compositions pharmaceutiques en contenant. |
| CA2135160A1 (en) * | 1992-05-08 | 1993-11-25 | Masatoshi Inai | Indole derivative |
| GB9326332D0 (en) * | 1993-12-23 | 1994-02-23 | Karo Bio | Indole derivatives |
| DK0746544T3 (da) * | 1994-02-22 | 1999-06-07 | Merrell Pharma Inc | Indolderivater til behandling af østrogenafhængige neoplasmer og sygdomme |
| DE4426625A1 (de) * | 1994-07-27 | 1996-03-14 | Schering Ag | 2-Phenylindole, Verfahren zu deren Herstellung, diese enthaltende pharmazeutische Präparate sowie deren Verwendung zur Herstellung von Arzneimitteln |
-
1997
- 1997-04-09 TW TW086104511A patent/TW397821B/zh active
- 1997-04-14 NZ NZ314595A patent/NZ314595A/xx unknown
- 1997-04-15 DK DK97302577T patent/DK0802184T3/da active
- 1997-04-15 EP EP97302577A patent/EP0802184B1/en not_active Expired - Lifetime
- 1997-04-15 AT AT97302577T patent/ATE219485T1/de not_active IP Right Cessation
- 1997-04-15 PT PT97302577T patent/PT802184E/pt unknown
- 1997-04-15 SK SK471-97A patent/SK282765B6/sk unknown
- 1997-04-15 ES ES97302577T patent/ES2179273T3/es not_active Expired - Lifetime
- 1997-04-15 DE DE69713441T patent/DE69713441T2/de not_active Expired - Fee Related
- 1997-04-17 CO CO97020214A patent/CO4950540A1/es unknown
- 1997-04-17 AU AU18921/97A patent/AU718888B2/en not_active Ceased
- 1997-04-17 ID IDP971302A patent/ID16618A/id unknown
- 1997-04-17 CZ CZ19971176A patent/CZ293065B6/cs not_active IP Right Cessation
- 1997-04-17 UA UA97041832A patent/UA47413C2/uk unknown
- 1997-04-18 KR KR1019970014302A patent/KR970069986A/ko not_active Application Discontinuation
- 1997-04-18 AR ARP970101579A patent/AR006705A1/es not_active Application Discontinuation
- 1997-04-18 JP JP9101557A patent/JPH1036347A/ja active Pending
- 1997-04-18 EA EA199700043A patent/EA000815B1/ru not_active IP Right Cessation
- 1997-04-18 NO NO971814A patent/NO308214B1/no not_active IP Right Cessation
- 1997-04-18 IL IL12069997A patent/IL120699A0/xx unknown
- 1997-04-18 HU HU9700779A patent/HUP9700779A1/hu unknown
- 1997-04-18 CN CN97111251A patent/CN1103756C/zh not_active Expired - Fee Related
- 1997-04-22 BR BR9701879A patent/BR9701879A/pt not_active Application Discontinuation
-
1998
- 1998-03-10 HK HK98101957A patent/HK1002862A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| NZ314595A (en) | 2000-04-28 |
| AU718888B2 (en) | 2000-04-20 |
| CN1103756C (zh) | 2003-03-26 |
| AU1892197A (en) | 1997-10-23 |
| HU9700779D0 (en) | 1997-06-30 |
| CZ293065B6 (cs) | 2004-02-18 |
| SK47197A3 (en) | 1997-11-05 |
| CZ117697A3 (en) | 1997-12-17 |
| EA199700043A1 (ru) | 1997-12-30 |
| HUP9700779A1 (hu) | 1999-09-28 |
| KR970069986A (ko) | 1997-11-07 |
| EP0802184A1 (en) | 1997-10-22 |
| BR9701879A (pt) | 1998-09-29 |
| NO971814D0 (no) | 1997-04-18 |
| JPH1036347A (ja) | 1998-02-10 |
| TW397821B (en) | 2000-07-11 |
| ID16618A (id) | 1997-10-23 |
| EP0802184B1 (en) | 2002-06-19 |
| DK0802184T3 (da) | 2002-09-16 |
| ATE219485T1 (de) | 2002-07-15 |
| IL120699A0 (en) | 1997-08-14 |
| DE69713441D1 (de) | 2002-07-25 |
| DE69713441T2 (de) | 2002-11-07 |
| HK1002862A1 (en) | 1998-09-25 |
| UA47413C2 (uk) | 2002-07-15 |
| EA000815B1 (ru) | 2000-04-24 |
| PT802184E (pt) | 2002-09-30 |
| ES2179273T3 (es) | 2003-01-16 |
| CO4950540A1 (es) | 2000-09-01 |
| SK282765B6 (sk) | 2002-12-03 |
| CN1168373A (zh) | 1997-12-24 |
| NO971814L (no) | 1997-10-20 |
| NO308214B1 (no) | 2000-08-14 |
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