JPH1036346A5 - - Google Patents
Info
- Publication number
- JPH1036346A5 JPH1036346A5 JP1997101563A JP10156397A JPH1036346A5 JP H1036346 A5 JPH1036346 A5 JP H1036346A5 JP 1997101563 A JP1997101563 A JP 1997101563A JP 10156397 A JP10156397 A JP 10156397A JP H1036346 A5 JPH1036346 A5 JP H1036346A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- azepan
- indol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63397496A | 1996-04-19 | 1996-04-19 | |
| US08/833,271 US5998402A (en) | 1996-04-19 | 1997-04-04 | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents |
| US08/833271 | 1997-04-04 | ||
| US08/633974 | 1997-04-04 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JPH1036346A JPH1036346A (ja) | 1998-02-10 |
| JPH1036346A5 true JPH1036346A5 (OSRAM) | 2008-02-14 |
| JP4093611B2 JP4093611B2 (ja) | 2008-06-04 |
Family
ID=27092026
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP10156397A Expired - Lifetime JP4093611B2 (ja) | 1996-04-19 | 1997-04-18 | エストロゲン剤 |
Country Status (26)
| Country | Link |
|---|---|
| EP (1) | EP0802183B1 (OSRAM) |
| JP (1) | JP4093611B2 (OSRAM) |
| KR (1) | KR100480193B1 (OSRAM) |
| CN (1) | CN1106383C (OSRAM) |
| AR (1) | AR011503A1 (OSRAM) |
| AT (1) | ATE206701T1 (OSRAM) |
| AU (1) | AU710149B2 (OSRAM) |
| BR (1) | BRPI9715334B8 (OSRAM) |
| CO (1) | CO4900051A1 (OSRAM) |
| CY (2) | CY2325B1 (OSRAM) |
| CZ (1) | CZ291701B6 (OSRAM) |
| DE (2) | DE122009000061I1 (OSRAM) |
| DK (1) | DK0802183T3 (OSRAM) |
| EA (1) | EA001448B1 (OSRAM) |
| ES (1) | ES2162198T3 (OSRAM) |
| FR (1) | FR09C0048I2 (OSRAM) |
| HU (1) | HU227077B1 (OSRAM) |
| IL (1) | IL120701A (OSRAM) |
| LU (1) | LU91608I2 (OSRAM) |
| MX (1) | MX9702865A (OSRAM) |
| NL (1) | NL300416I2 (OSRAM) |
| NO (2) | NO309564B1 (OSRAM) |
| NZ (1) | NZ314601A (OSRAM) |
| PT (1) | PT802183E (OSRAM) |
| SK (1) | SK281737B6 (OSRAM) |
| UA (1) | UA48148C2 (OSRAM) |
Families Citing this family (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6172100B1 (en) | 1997-04-30 | 2001-01-09 | Eli Lilly And Company | Antithrombotic agents |
| WO1998048800A1 (en) | 1997-05-01 | 1998-11-05 | Eli Lilly And Company | Antithrombotic agents |
| ID24568A (id) * | 1997-11-06 | 2000-07-27 | American Home Prod | Kontrasepsi oral yang mengandung anti-estrogen plus progestin |
| US6069153A (en) * | 1998-05-12 | 2000-05-30 | American Home Products Corporation | Indenoindoles and benzocarbazoles as estrogenic agents |
| ATE339415T1 (de) * | 1998-05-12 | 2006-10-15 | Wyeth Corp | Benzocarbazol und indenoindole derivate als östrogene agentien |
| US6479535B1 (en) | 1998-05-15 | 2002-11-12 | Wyeth | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations |
| BR9911040A (pt) * | 1998-05-15 | 2001-02-13 | American Home Prod | 2-fenil-1-[4-(2-aminoetóxi)-benzil]-indol em combinação com estrogêneos |
| EP1080073A1 (en) * | 1998-05-15 | 2001-03-07 | American Home Products Corporation | Compositions comprising 2-phenyl-indole compounds 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 |
| ATE258934T1 (de) | 1998-10-30 | 2004-02-15 | Lilly Co Eli | Azaindol derivate und ihre verwendung als antithrombotische wirkstoffe |
| US6358943B1 (en) | 1999-03-04 | 2002-03-19 | American Home Products Corporation | N-substituted indolines as estrogenic agents |
| US6380185B1 (en) | 1999-03-04 | 2002-04-30 | American Home Products Corporation | N-substituted benzoyl indoles as estrogenic agents |
| TWI220898B (en) * | 1999-03-04 | 2004-09-11 | Wyeth Corp | N-substituted indolines as estrogenic agents |
| AU3859400A (en) * | 1999-03-04 | 2000-09-21 | American Home Products Corporation | N-substituted benzoyl indoles as estrogenic agents |
| TWI287018B (en) * | 1999-09-13 | 2007-09-21 | Wyeth Corp | Glucopyranosides conjugates of 2-(4-hydroxy-phenyl)-3-methyl-1-[4-(2-amin-1-yl-ethoxy)-benzyl]-1H-indol-5-ols |
| US6380166B1 (en) | 1999-09-13 | 2002-04-30 | American Home Products Corporation | Glucopyranosides conjugates of 2-(4-hydroxy-phenyl)-3-methyl-1-[4-(2-amin-1-yl-ethoxy)-benzyl]-1H-indol-5-ols |
| CN1400904A (zh) * | 2000-01-28 | 2003-03-05 | 恩多研究公司 | 与雌激素联合的选择性雌激素受体调节剂 |
| US20020013327A1 (en) * | 2000-04-18 | 2002-01-31 | Lee Andrew G. | Compositions and methods for treating female sexual dysfunction |
| EP1656938A1 (en) | 2000-07-06 | 2006-05-17 | Wyeth | Combinations of SSRI and estrogenic agents |
| AR030064A1 (es) * | 2000-07-06 | 2003-08-13 | Wyeth Corp | Metodos para inhibir los efectos uterotroficos de los agentes estrogenicos |
| EP1990051A1 (en) | 2000-07-06 | 2008-11-12 | Wyeth | Combinations of SSRI and estrogenic agents |
| WO2002003992A2 (en) * | 2000-07-06 | 2002-01-17 | Wyeth | Use of substituted indole compounds for treating prosthesis-related bone degeneration |
| US6358991B2 (en) * | 2000-07-06 | 2002-03-19 | American Home Products Corporation | Methods of treating neuropeptide Y-related conditions |
| JP2004502734A (ja) * | 2000-07-06 | 2004-01-29 | ワイス | 一酸化窒素シンターゼ活性の増強方法 |
| AU2001271781A1 (en) * | 2000-07-06 | 2002-01-21 | Wyeth | Use of substituted indole compounds for treating sphincter incontinence |
| WO2002003986A2 (en) * | 2000-07-06 | 2002-01-17 | Wyeth | Use of substituted indole compounds for treating breast disorders |
| AR029538A1 (es) | 2000-07-06 | 2003-07-02 | Wyeth Corp | Composiciones farmaceuticas de agentes estrogenicos |
| AU2001271782A1 (en) | 2000-07-06 | 2002-01-21 | Wyeth | Use of substituted insole compounds for treating excessive intraocular pressure |
| EP1177787A3 (en) * | 2000-07-28 | 2003-09-10 | Pfizer Products Inc. | Use of an estrogen agonist/antagonist for treating cataracts |
| WO2002094788A1 (en) | 2001-05-22 | 2002-11-28 | Eli Lilly And Company | 2-substituted 1,2,3,4-tetrahydroquinolines and derivatives thereof, compositions and methods |
| PT1401446E (pt) | 2001-05-22 | 2005-05-31 | Lilly Co Eli | Derivados de tetrahidroquinolina para a inibicao de doencas associadas com a privacao de estrogenio ou com uma resposta fisiologica aberrante ao estrogenio endogeno |
| EP1531807A4 (en) * | 2002-06-13 | 2007-10-31 | Wyeth Corp | Bazedoxifene TREATMENT SCHEMES |
| BR0312675A (pt) | 2002-07-22 | 2005-05-03 | Lilly Co Eli | Composto ou um sal de adição de ácido farmacêutico do mesmo,m e, métodos para tratar endometriose, e para tratar leiomioma uterino |
| EP1577288B1 (en) | 2002-12-26 | 2014-07-23 | Eisai R&D Management Co., Ltd. | Selective estrogen receptor modulators |
| US7250440B2 (en) * | 2003-08-12 | 2007-07-31 | Wyeth | (Hydroxyphenyl)-1H-indole-3-carbaldehyde oxime derivatives as estrogenic agents |
| BRPI0509257A (pt) | 2004-04-07 | 2007-09-11 | Wyeth Corp | polimorfo cristalino de acetato de bazedoxifeno, composição, processo para preparar um polimorfo e para aumentar a proporção de acetato de bazedoxifeno forma b em uma composição, métodos de tratar um mamìfero, cáncer de mama e uma mulher em pós-menopausa para um ou mais distúrbios vasomotores, de abaixar colesterol e de inibir perda óssea em um mamìfero e uso de um polimorfo |
| EP1732890A1 (en) | 2004-04-07 | 2006-12-20 | Wyeth | Crystalline polymorph of a bazedoxifene acetate |
| JP2007532556A (ja) | 2004-04-08 | 2007-11-15 | ワイス | 選択的エストロゲン受容体調節剤としてのアスコルビン酸バゼドキシフェン |
| US7772271B2 (en) | 2004-07-14 | 2010-08-10 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| US7868037B2 (en) | 2004-07-14 | 2011-01-11 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| US7781478B2 (en) | 2004-07-14 | 2010-08-24 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| JP2008506702A (ja) | 2004-07-14 | 2008-03-06 | ピーティーシー セラピューティクス,インコーポレーテッド | C型肝炎を治療するための方法 |
| NZ553329A (en) | 2004-07-22 | 2010-09-30 | Ptc Therapeutics Inc | Thienopyridines for treating hepatitis C |
| CN1993322A (zh) * | 2004-08-05 | 2007-07-04 | 惠氏公司 | 哌多昔芬盐酸盐一水合物的结晶多晶型物 |
| SG155258A1 (en) | 2004-10-20 | 2009-09-30 | Endorech Inc | Sex steroid precursors alone or in combination with a selective estrogen receptor modulator and/or with estrogens and/or a type 5 cgmp phosphodiesterase inhibitor for the prevention and treatment of vaginal dryness and sexual dysfunction in postmenopausa |
| FR2880625B1 (fr) * | 2005-01-07 | 2007-03-09 | Sanofi Aventis Sa | Derives de n-(heteroaryl)-1h-indole-2-carboxamides, leur preparation et leur application en therapeutique |
| US20100087661A1 (en) * | 2007-02-12 | 2010-04-08 | Josef Jirman | Method for the preparation of 5-benzyloxy-2-(4-benzyloxphenyl)-3-methyl-1h-indole |
| US8268806B2 (en) | 2007-08-10 | 2012-09-18 | Endorecherche, Inc. | Pharmaceutical compositions |
| CA2714494A1 (en) * | 2008-02-11 | 2009-08-20 | Wyeth Llc | Methods of preparing polymorphic form a of bazedoxifene acetate |
| EP2276732B1 (en) | 2008-04-16 | 2015-05-20 | Karo Bio Ab | Novel estrogen receptor ligands |
| CN102395561A (zh) * | 2009-04-13 | 2012-03-28 | 桑多斯股份公司 | 合成巴多昔芬乙酸酯及其中间体的方法 |
| 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 |
| ITMI20091109A1 (it) * | 2009-06-23 | 2010-12-24 | Wyeth Corp | Forma polimorfa d di bazedoxifene acetato e metodi per la sua preparazione |
| SG186333A1 (en) | 2010-06-16 | 2013-01-30 | Endorech Inc | Methods of treating or preventing estrogen-related diseases |
| US7968732B1 (en) | 2010-09-07 | 2011-06-28 | Divi's Laboratories, Ltd. | Process for the preparation of 5-benzyloxy-2-(4-benzyloxyphenyl)-3-methyl-1H-indole |
| WO2012037187A2 (en) | 2010-09-14 | 2012-03-22 | Dr. Reddy's Laboratories Ltd. | Preparation of crystalline bazedoxifene and its salts |
| US8569483B2 (en) | 2011-06-21 | 2013-10-29 | Divi's Laboratories, Ltd. | Process for the preparation of bazedoxifene acetate and intermediates thereof |
| CN102690225B (zh) * | 2012-04-11 | 2014-12-24 | 南京友杰医药科技有限公司 | 巴多昔芬的合成方法 |
| US9751835B2 (en) * | 2013-05-15 | 2017-09-05 | Indiana University Research And Technology Corporation | Processes and intermediates for preparing indole pharmaceuticals |
| 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 |
| US9421264B2 (en) | 2014-03-28 | 2016-08-23 | Duke University | Method of treating cancer using selective estrogen receptor modulators |
| FI3834824T3 (fi) | 2014-03-28 | 2025-12-05 | Univ Duke | Estrogeenireseptoripositiivisen rintasyövän hoito selektiivisellä estrogeenireseptorin modulaattorilla |
| WO2016097071A1 (en) * | 2014-12-18 | 2016-06-23 | F. Hoffmann-La Roche Ag | Estrogen receptor modulators and uses thereof |
| KR20190110400A (ko) | 2018-03-20 | 2019-09-30 | 엠에프씨 주식회사 | 새로운 중간체를 이용한 바제독시펜의 제조방법 |
| IT201800006562A1 (it) * | 2018-06-21 | 2019-12-21 | Procedimento e intermedi utili per la preparazione di indoli | |
| IT201900001923A1 (it) | 2019-02-11 | 2020-08-11 | Erregierre Spa | Sali di bazedoxifene utili per la preparazione di bazedoxifene acetato |
| US11246874B1 (en) | 2021-04-20 | 2022-02-15 | Oxygen Biotech LLC | Treatment of COVID-19 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SU373940A3 (OSRAM) * | 1970-01-21 | 1973-03-12 | ||
| DE2557342A1 (de) * | 1975-12-19 | 1977-06-30 | Hoechst Ag | Basisch substituierte indolderivate und verfahren zu ihrer herstellung |
| US4656187A (en) * | 1981-08-03 | 1987-04-07 | Eli Lilly And Company | Treatment of mammary cancer |
| DE3232968A1 (de) * | 1981-09-10 | 1983-06-09 | Degussa Ag, 6000 Frankfurt | Neue 2-(hydroxy-phenyl)-indole und verfahren zu deren herstellung |
| CA1241660A (en) * | 1984-06-25 | 1988-09-06 | Yvan Guindon | Indole-2-alkanoic acids |
| GB8707051D0 (en) * | 1986-04-15 | 1987-04-29 | Ici America Inc | Heterocyclic carboxamides |
| 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 |
| GB9004301D0 (en) * | 1990-02-26 | 1990-04-18 | Fujisawa Pharmaceutical Co | Indolebutyric acid derivatives and process for preparation thereof |
| US5051442A (en) * | 1990-04-25 | 1991-09-24 | Merrell Dow Pharmaceuticals Inc. | 3-indolyl thioacetate derivatives and NMDA receptor antagonistic use thereof |
| AU665690B2 (en) * | 1992-05-08 | 1996-01-11 | Otsuka Pharmaceutical Factory, Inc. | Indole derivative |
| ATE188377T1 (de) * | 1993-06-29 | 2000-01-15 | Takeda Chemical Industries Ltd | Chinoline oder chinazolin-derivate und deren verwendung zur herstellung eines medikaments für die behandlung von osteoporose |
| GB9326332D0 (en) * | 1993-12-23 | 1994-02-23 | Karo Bio | Indole derivatives |
| 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
- 1997-04-15 SK SK472-97A patent/SK281737B6/sk not_active IP Right Cessation
- 1997-04-15 ES ES97302576T patent/ES2162198T3/es not_active Expired - Lifetime
- 1997-04-15 AT AT97302576T patent/ATE206701T1/de active
- 1997-04-15 DE DE122009000061C patent/DE122009000061I1/de active Pending
- 1997-04-15 EP EP97302576A patent/EP0802183B1/en not_active Expired - Lifetime
- 1997-04-15 DK DK97302576T patent/DK0802183T3/da active
- 1997-04-15 NZ NZ314601A patent/NZ314601A/en not_active IP Right Cessation
- 1997-04-15 PT PT97302576T patent/PT802183E/pt unknown
- 1997-04-15 DE DE69707189T patent/DE69707189T2/de not_active Expired - Lifetime
- 1997-04-17 CZ CZ19971175A patent/CZ291701B6/cs not_active IP Right Cessation
- 1997-04-17 UA UA97041833A patent/UA48148C2/uk unknown
- 1997-04-17 AU AU18920/97A patent/AU710149B2/en not_active Expired
- 1997-04-18 HU HU9700777A patent/HU227077B1/hu active Protection Beyond IP Right Term
- 1997-04-18 MX MX9702865A patent/MX9702865A/es unknown
- 1997-04-18 JP JP10156397A patent/JP4093611B2/ja not_active Expired - Lifetime
- 1997-04-18 AR ARP970101580A patent/AR011503A1/es active IP Right Grant
- 1997-04-18 EA EA199700044A patent/EA001448B1/ru not_active IP Right Cessation
- 1997-04-18 KR KR1019970014894A patent/KR100480193B1/ko not_active Expired - Lifetime
- 1997-04-18 IL IL12070197A patent/IL120701A/xx active Protection Beyond IP Right Term
- 1997-04-18 CO CO97020584A patent/CO4900051A1/es unknown
- 1997-04-18 NO NO971815A patent/NO309564B1/no not_active IP Right Cessation
- 1997-04-18 CN CN97113496A patent/CN1106383C/zh not_active Expired - Lifetime
- 1997-04-22 BR BRPI9715334A patent/BRPI9715334B8/pt not_active IP Right Cessation
-
2003
- 2003-04-08 CY CY0300038A patent/CY2325B1/xx unknown
-
2009
- 2009-09-23 LU LU91608C patent/LU91608I2/fr unknown
- 2009-09-28 NL NL300416C patent/NL300416I2/nl unknown
- 2009-09-30 CY CY2009016C patent/CY2009016I1/el unknown
- 2009-09-30 FR FR09C0048C patent/FR09C0048I2/fr active Active
- 2009-11-09 NO NO2009025C patent/NO2009025I2/no unknown
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