EA200101177A1 - Производные индола в качестве антагонистов прогестерона - Google Patents

Производные индола в качестве антагонистов прогестерона

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Publication number
EA200101177A1
EA200101177A1 EA200101177A EA200101177A EA200101177A1 EA 200101177 A1 EA200101177 A1 EA 200101177A1 EA 200101177 A EA200101177 A EA 200101177A EA 200101177 A EA200101177 A EA 200101177A EA 200101177 A1 EA200101177 A1 EA 200101177A1
Authority
EA
Eurasian Patent Office
Prior art keywords
progesterone antagonists
indol derivatives
indol
derivatives
progesterone
Prior art date
Application number
EA200101177A
Other languages
English (en)
Inventor
Эндрю Фенсам
Лори Л. Миллер
Джон У. Уллрих
Рейнхольд Х. У. Бендер
Пувен Жанг
Джей Э. Вроубел
Лин Жи
Тодд К. Джоунс
Кристофер М. Тегли
Джеймс П. Эдвардс
Original Assignee
Америкэн Хоум Продактс Корпорейшн
Лиганд Фармасьютикалз, Инк.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Америкэн Хоум Продактс Корпорейшн, Лиганд Фармасьютикалз, Инк. filed Critical Америкэн Хоум Продактс Корпорейшн
Publication of EA200101177A1 publication Critical patent/EA200101177A1/ru

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    • 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
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32—Oxygen atoms
    • C07D209/34—Oxygen atoms in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • 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
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/96—Spiro-condensed ring systems
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

Abstract

Настоящее изобретение включает соединения формулы (1), которые являются антагонистами рецептора прогестерона, их получение и применение.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200101177A 1999-05-04 2000-05-01 Производные индола в качестве антагонистов прогестерона EA200101177A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US18305899P 1999-05-04 1999-05-04
US09/552,632 US6391907B1 (en) 1999-05-04 2000-04-19 Indoline derivatives
PCT/US2000/011847 WO2000066556A1 (en) 1999-05-04 2000-05-01 Indoline derivatives as progesterone antagonists

Publications (1)

Publication Number Publication Date
EA200101177A1 true EA200101177A1 (ru) 2002-04-25

Family

ID=26878706

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200101177A EA200101177A1 (ru) 1999-05-04 2000-05-01 Производные индола в качестве антагонистов прогестерона

Country Status (21)

Country Link
US (5) US6391907B1 (ru)
EP (1) EP1175398B1 (ru)
JP (1) JP2002543183A (ru)
KR (1) KR20010114252A (ru)
CN (1) CN1141295C (ru)
AT (1) ATE366721T1 (ru)
AU (1) AU4814100A (ru)
BR (1) BR0010215A (ru)
CA (1) CA2371638A1 (ru)
CZ (1) CZ20013953A3 (ru)
DE (1) DE60035496T2 (ru)
DK (1) DK1175398T3 (ru)
EA (1) EA200101177A1 (ru)
ES (1) ES2290035T3 (ru)
HU (1) HUP0200992A3 (ru)
IL (1) IL146281A0 (ru)
MX (1) MXPA01011298A (ru)
NO (1) NO20015379L (ru)
PL (1) PL351954A1 (ru)
WO (1) WO2000066556A1 (ru)
ZA (1) ZA200107631B (ru)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6355648B1 (en) 1999-05-04 2002-03-12 American Home Products Corporation Thio-oxindole derivatives
US6444668B1 (en) 1999-05-04 2002-09-03 Wyeth Combination regimens using progesterone receptor modulators
US6407101B1 (en) * 1999-05-04 2002-06-18 American Home Products Corporation Cyanopyrroles
US6417214B1 (en) * 1999-05-04 2002-07-09 Wyeth 3,3-substituted indoline derivatives
US6391907B1 (en) * 1999-05-04 2002-05-21 American Home Products Corporation Indoline derivatives
US6462032B1 (en) 1999-05-04 2002-10-08 Wyeth Cyclic regimens utilizing indoline derivatives
US6509334B1 (en) 1999-05-04 2003-01-21 American Home Products Corporation Cyclocarbamate derivatives as progesterone receptor modulators
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
UA73119C2 (en) * 2000-04-19 2005-06-15 American Home Products Corpoir Derivatives of cyclic thiocarbamates, pharmaceutical composition including noted derivatives of cyclic thiocarbamates and active ingredients of medicines as modulators of progesterone receptors
DE60139892D1 (de) * 2000-11-15 2009-10-22 Masao Sugamata Makrolidantibiotika für endometriose oder uterusmyome
CA2489813A1 (en) * 2002-06-25 2003-12-31 Wyeth Use of thio-oxindole derivatives in treatment of hormone-related conditions
KR20050012831A (ko) * 2002-06-25 2005-02-02 와이어쓰 피부 질환을 치료하는 데 있어서의 티오-옥스인돌유도체의 용도
AR040782A1 (es) * 2002-10-11 2005-04-20 Ligand Pharm Inc Derivados de 5- cicloalquenil-5h- cromeno [ 3,4- f] quinolina como compuestos mudulares selectivos de receptores de progesterona
AR040783A1 (es) * 2002-10-11 2005-04-20 Ligand Pharm Inc 5-(1',1'-cicloaquil/alquenil) metiliden-1,2 -dihidro-5-h-cromeno [3,4- f] quiinolinas como compuestos moduladores selectivos de receptores de progesterona
WO2004037247A1 (en) * 2002-10-21 2004-05-06 Irm Llc Oxindoles with anti-hiv activity
US7247625B2 (en) 2003-10-09 2007-07-24 Wyeth 6-amino-1,4-dihydro-benzo[d][1,3] oxazin-2-ones and analogs useful as progesterone receptor modulators
US7323455B2 (en) * 2004-03-24 2008-01-29 Wyeth 7-aryl 1,5-dihydro-4,1-benzoxazepin-2(3H)-one derivatives and their use as progesterone receptor modulators
US7414052B2 (en) 2004-03-30 2008-08-19 Wyeth Phenylaminopropanol derivatives and methods of their use
US7517899B2 (en) 2004-03-30 2009-04-14 Wyeth Phenylaminopropanol derivatives and methods of their use
PL1732922T3 (pl) 2004-04-08 2009-03-31 Wyeth Corp Sposób minimalizowania zanieczyszczeń tioamidowych
DE602005010840D1 (de) * 2004-04-08 2008-12-18 Wyeth Corp Thioamidderivate als progesteronrezeptormodulatoren
BRPI0509745A (pt) * 2004-04-08 2007-09-25 Topotarget As compostos de difenil ox-indol-2-ona e seu uso no tratamento de cáncer
AR049631A1 (es) * 2004-04-27 2006-08-23 Wyeth Corp Proceso de acoplamiento para la generacion de derivados reactivos de pirrol -2- carbonitrilo n- sustituidos con contenido de boro para producir biarilos
BRPI0510278A (pt) 2004-04-27 2007-10-30 Wyeth Corp método para produzir compostos, produto, e, composto
US7514466B2 (en) 2004-04-27 2009-04-07 Wyeth Purification of progesterone receptor modulators
GT200500186A (es) * 2004-07-07 2006-03-02 Regimenes anticonceptivos con antagonistas del receptor de progesterona y kits
GT200500183A (es) * 2004-08-09 2006-04-10 Moduladores del receptor de progesterona que comprenden derivados de pirrol-oxindol y sus usos
GT200500185A (es) * 2004-08-09 2006-04-10 Moduladores del receptor de progesterona que comprenden derivados de pirrol-oxindol y sus usos
EP1807425B1 (en) * 2004-10-27 2014-07-30 Janssen Pharmaceutica NV Pyridine imidazoles and aza-indoles as progesterone receptor modulators
US7414142B2 (en) * 2005-09-19 2008-08-19 Wyeth 5-aryl-indan-1-one oximes and analogs useful as progesterone receptor modulators
US7319152B2 (en) * 2005-09-19 2008-01-15 Wyeth 5-Aryl-indan-1-one and analogs useful as progesterone receptor modulators
US20070066628A1 (en) * 2005-09-19 2007-03-22 Wyeth 5-Aryl-indan-1-ol and analogs useful as progesterone receptor modulators
GT200600439A (es) 2005-09-29 2007-09-19 Derivados de propilamina sustituida y metodos para su utilización
US20070213526A1 (en) * 2006-03-07 2007-09-13 Wyeth Purification of progesterone receptor modulators
LT2078032T (lt) 2006-10-24 2017-11-10 Repros Therapeutics Inc. Kompozicijos ir būdai, skirti gimdos gleivinės proliferacijos slopinimui
TW200848021A (en) * 2007-03-06 2008-12-16 Wyeth Corp Sulfonylated heterocycles useful for modulation of the progesterone receptor
US20080312306A1 (en) * 2007-06-15 2008-12-18 Wyeth Polymorphs, solvates, and hydrate of 5-(4'-fluoro-2'-oxo-1',2'-dihydrospiro[cyclopropane-1,3'-indol]-5'-yl)-1-methyl-1h-pyrrole-2-carbonitrile
US20080319204A1 (en) * 2007-06-25 2008-12-25 Wyeth Process for the synthesis of progesterone receptor modulators
EP2205079A4 (en) * 2007-10-04 2010-10-27 Merck Sharp & Dohme N-SUBSTITUTED OXINDOLINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
JP2010540631A (ja) * 2007-10-04 2010-12-24 メルク・シャープ・エンド・ドーム・コーポレイション カルシウムチャネル遮断薬としてのｎ−置換されたオキシインドリン誘導体
JP5315710B2 (ja) * 2008-02-07 2013-10-16 セントラル硝子株式会社 １−ブロモ−３−フルオロ−５−ジフルオロメチルベンゼンの製造方法
TWI539953B (zh) 2008-04-28 2016-07-01 瑞波若斯治療學公司 用於治療乳癌之組成物和方法
WO2010090680A1 (en) * 2008-12-15 2010-08-12 Wyeth Llc Substituted oxindole cb2 agonists
KR20130009990A (ko) 2010-03-22 2013-01-24 레프로스 쎄라피우틱스 아이엔씨. 항프로게스틴의 비독성 전달을 위한 조성물들과 그 방법들
CN102516151B (zh) * 2011-11-11 2013-09-11 华东师范大学 一种3-取代-3-羟基吲哚酮衍生物及其制备方法和应用
WO2014058035A1 (en) * 2012-10-12 2014-04-17 Okinawa Institute Of Science And Technology School Corporation Novel spirooxindole derivative and process for producing the same
CN103242332B (zh) * 2013-05-13 2015-11-04 江西科技师范大学 1-n酰基取代吲哚酮衍生物
CN104530065A (zh) * 2013-05-13 2015-04-22 江西科技师范大学 1-n酰基取代吲哚酮衍生物的应用
WO2015092118A1 (en) * 2013-12-17 2015-06-25 Orion Corporation Spiro[cyclobutane-1,3'-indolin]-2'-one derivatives as bromodomain inhibitors
US10058542B1 (en) 2014-09-12 2018-08-28 Thioredoxin Systems Ab Composition comprising selenazol or thiazolone derivatives and silver and method of treatment therewith
CN106316922B (zh) * 2016-08-17 2019-02-01 华东师范大学 一种含c-3全取代氧化吲哚衍生物及其合成方法和应用
US20200039961A1 (en) * 2016-09-30 2020-02-06 Epizyme, Inc. Substituted fused bi- or tri- heterocyclic compounds as ehmt2 inhibitors
CA3060416A1 (en) 2017-04-21 2018-10-25 Epizyme, Inc. Combination therapies with ehmt2 inhibitors
EP3965884A1 (en) 2019-05-08 2022-03-16 Aligos Therapeutics, Inc. Modulators of thr-beta and methods of use thereof
CN113456631B (zh) * 2021-08-06 2022-06-21 徐州医科大学 一种靶向acsl1的小分子药物及其在治疗子宫内膜癌中的应用

Family Cites Families (105)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3635964A (en) 1969-02-10 1972-01-18 Colgate Palmolive Co 5-morpholinyl-2 1-benzisothiazolines
US3917592A (en) 1974-09-27 1975-11-04 Chevron Res Herbicidal N-haloacetyl-1,2-dihydro-4H-3,1-benzoxazine
IT1039699B (it) 1975-07-03 1979-12-10 Prephar Composizione spermicida a base di derivati benzisotiazolici
US4258185A (en) 1978-10-17 1981-03-24 Yoshitomi Pharmaceutical Industries, Ltd. Pyridazinone compounds
DE3064910D1 (en) 1979-06-12 1983-10-27 Fujisawa Pharmaceutical Co 2-oxo-benzothiazoline, benzoxazoline or indoline derivatives, their preparation, and pharmaceutical compositions comprising such derivatives
US4670566A (en) 1979-07-12 1987-06-02 A. H. Robins Company, Incorporated 3-methyl-hio-4-(5-, 6-, or 7-)phenylindolindolin-2-ones
US4322533A (en) * 1980-03-17 1982-03-30 Lesher George Y 1H-Indole-2,3-dione derivatives
US4440785A (en) 1980-10-30 1984-04-03 A. H. Robins Company, Inc. Methods of using 2-aminobiphenylacetic acids, esters, and metal salts thereof to treat inflammation
US4617302A (en) 1984-10-15 1986-10-14 Eli Lilly And Company Inotropic agents
US4721721A (en) 1984-12-18 1988-01-26 Rorer Pharmaceutical Corporation 6-(4-thiazole) compounds, cardiotonic compositions including the same, and their uses
ATE67185T1 (de) 1985-07-09 1991-09-15 Pfizer Substituierte oxindol-3-carboxamine als entzuendungshemmendes und schmerzstillendes mittel.
US4666913A (en) 1985-11-22 1987-05-19 William H. Rorer, Inc. Hydroxy and aminothiazolyl-benzodiazinone compounds, cardiotonic compositions including the same, and their uses
DE3633861A1 (de) 1986-10-04 1988-04-07 Thomae Gmbh Dr K Neue imidazo-benzoxazinone, ihre herstellung und diese verbindungen enthaltende arzneimittel
JPS63112584A (ja) 1986-10-29 1988-05-17 Yoshitomi Pharmaceut Ind Ltd イミダゾピリジン誘導体
US4822794A (en) 1987-05-08 1989-04-18 Rorer Pharmaceutical Corporation Pyridooxazinone-pyridone compounds, cardiotonic compositions including the same, and their uses
DE3718527A1 (de) 1987-06-03 1988-12-15 Basf Ag Verfahren zur herstellung von 2(5h)-furanonen
AU614965B2 (en) 1987-06-06 1991-09-19 Merck Patent Gesellschaft Mit Beschrankter Haftung Thiadiazinones
EP0303418A3 (en) 1987-08-11 1990-11-07 Smithkline Beecham Laboratoires Pharmaceutiques Substituted indolones, useful in the treatment of heart or asthmatic diseases
DE3733478A1 (de) 1987-10-01 1989-04-13 Schering Ag Antigestagen- und antioestrogenwirksame verbindungen zur geburtseinleitung und zum schwangerschaftsabbruch sowie zur behandlung gynaekologischer stoerungen und hormonabhaengiger tumore
DE3734745A1 (de) 1987-10-09 1989-04-20 Schering Ag Tetrahydropyrrolo(2,1-c)(1,2,4)-thiadiazol-3-ylideniminobenzoxazinone und andere heterocyclisch substituierte azole und azine, verfahren zu ihrer herstellung und ihre verwendung als mittel mit herbizider wirkung
JPH02138183A (ja) 1988-11-17 1990-05-28 Nippon Tokushu Noyaku Seizo Kk 除草性ピロール類
FR2643903A1 (fr) 1989-03-03 1990-09-07 Union Pharma Scient Appl Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux
US5300655A (en) 1989-04-18 1994-04-05 Pfizer Inc. 2-carboxy-thiophene derivatives
US5182282A (en) 1989-04-28 1993-01-26 Roussel Uclaf 4-Benzyl-1H-indole derivatives
FR2646349B1 (fr) 1989-04-28 1994-04-01 Roussel Uclaf Derives du 4-phenylmethyl lh-indole, procede et intermediaires de preparation, application a titre de medicaments et compositions les renfermant
DE3932953A1 (de) 1989-10-03 1991-04-11 Boehringer Mannheim Gmbh Neue 2-bicyclo-benzimidazole, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
DE3935514A1 (de) 1989-10-25 1991-05-02 Boehringer Mannheim Gmbh Neue bicyclo-imidazole, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
KR0164842B1 (ko) 1990-03-24 1999-01-15 손정삼 신규 벤즈옥사진, 벤조티아진 유도체 및 그 제조방법
TW203049B (ru) 1990-04-13 1993-04-01 Yamanouchi Pharma Co Ltd
DE69115221T2 (de) 1990-09-28 1996-08-22 I F L O S A S Di Giorgio E Ald Methode zur Synthese eines Präparats zur Regulation der Empfängnis und des Menstruationszyklus mit onkostatischen antikinetosischen, preventiven und therapeutischen Eigenschaften zur Behandlung von Brustkrebs und Melanomen.
EP0510235A1 (en) 1991-04-26 1992-10-28 Dong-A Pharm. Co., Ltd. Novel benzoxazine or benzothiazine derivatives and process for the preparation of the same
JP3108483B2 (ja) 1991-09-30 2000-11-13 日清製粉株式会社 インドール誘導体およびこれを有効成分とする抗潰瘍薬
SE9103752D0 (sv) 1991-12-18 1991-12-18 Astra Ab New compounds
GB9201038D0 (en) 1992-01-16 1992-03-11 Glaxo Group Ltd Chemical compounds
US5808139A (en) 1992-04-21 1998-09-15 Ligand Pharmaceuticals Incorporated Non-steroid progesterone receptor agonist and antagonist and compounds and methods
DE4242451A1 (de) 1992-12-16 1994-06-23 Basf Ag Verfahren zur Herstellung von 5-Ringheterocyclen
ZA939516B (en) 1992-12-22 1994-06-06 Smithkline Beecham Corp Endothelin receptor antagonists
TW281669B (ru) 1993-02-17 1996-07-21 Chugai Pharmaceutical Co Ltd
FR2702477B1 (fr) 1993-03-08 1995-04-28 Synthelabo Dérivés de benzoxazine, leur préparation et leur application en thérapeutique.
SE9302080D0 (sv) 1993-06-16 1993-06-16 Ab Astra New compounds
DE4330234A1 (de) 1993-09-02 1995-03-09 Schering Ag Verwendung von Gestagenen und kompetitiven Progesteronantagonisten zur Herstellung von Arzneimitteln für die weibliche Fertilitätskontrolle sowie Mittel enthaltend ein Gestagen und einen kompetitiven Progesteronantagonisten
DE4335876A1 (de) 1993-10-17 1995-04-20 Schering Ag Kombination von Progesteronantagonisten und Antiöstrogenen mit partialer agonistischer Wirkung für die Hormonsubstitutions-Therapie für peri- und postmenopausale Frauen
GB9326136D0 (en) 1993-12-22 1994-02-23 Erba Carlo Spa Biologically active 3-substituted oxindole derivatives useful as anti-angiogenic agents
DE4344463A1 (de) 1993-12-22 1995-06-29 Schering Ag Kombinationsprodukt zur Kontrazeption
US5659046A (en) 1993-12-30 1997-08-19 American Cyanamid Company Method for the preparation of 2-perfluoroalkyl-3-oxazolin-5-one
WO1995020389A1 (en) 1994-01-28 1995-08-03 Merck & Co., Inc. Benzoxazinones as inhibitors of hiv reverse transcriptase
US5681817A (en) 1994-02-04 1997-10-28 The Medical College Of Hampton Roads Treatment of ovarian estrogen dependent conditions
US5750471A (en) 1994-06-08 1998-05-12 E. I. Du Pont De Nemours And Company Cyclic sulfonamide herbicides
WO1996015794A1 (en) 1994-11-22 1996-05-30 Balance Pharmaceuticals, Inc. Compositions and methods for contraception and for treatment of benign gynecological disorders
US5521166A (en) 1994-12-19 1996-05-28 Ortho Pharmaceitical Corporation Antiprogestin cyclophasic hormonal regimen
DE69531998T2 (de) 1994-12-22 2004-07-22 Ligand Pharmaceuticals, Inc., San Diego Steroidrezeptor-modulator verbindungen und methoden
US5693647A (en) 1994-12-22 1997-12-02 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods
ZA9510926B (en) 1994-12-23 1996-07-03 Schering Ag Compounds with progesterone-antagonistic and antiestrogenic action to be used together for female contraception
US5552412A (en) 1995-01-09 1996-09-03 Pfizer Inc 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen2-ol compounds which are useful for treating osteoporosis
US5565483A (en) 1995-06-07 1996-10-15 Bristol-Myers Squibb Company 3-substituted oxindole derivatives as potassium channel modulators
WO1997013767A1 (de) 1995-10-09 1997-04-17 Chemisch Pharmazeutische Forschungsgesellschaft Mbh Heterocyclisch substituierte 1-indolcarboxamide als cyclooxygenase-2 inhibitoren
US6500948B1 (en) 1995-12-08 2002-12-31 Agouron Pharmaceuticals, Inc. Metalloproteinase inhibitors-compositions, uses preparation and intermediates thereof
US5659133A (en) * 1996-04-22 1997-08-19 Astropower, Inc. High-temperature optical combustion chamber sensor
TR199802705T2 (xx) 1996-06-25 1999-03-22 Akzo Nobel N.V. Progestojen-anti-progestojen k�r�
GB2315505B (en) * 1996-07-24 1998-07-22 Sofitech Nv An additive for increasing the density of a fluid and fluid comprising such additve
JP2001500865A (ja) 1996-09-13 2001-01-23 ザ ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティ 避妊の非ホルモン法
US5874430A (en) 1996-10-02 1999-02-23 Dupont Pharmaceuticals Company 4,4-disubstitued-1,4-dihydro-2H-3,1-benzoxazin-2-ones useful as HIV reverse transcriptase inhibitors and intermediates and processes for making the same
DE69724630T2 (de) 1996-10-02 2004-07-29 Bristol-Myers Squibb Pharma Co. 4,4-disubstituierte 1,4-dihydro-2h-3,1-benzoxazin-2-one die anwendbar sind als hiv-reverstranskriptase-inhibitoren, zwischenprodukte und verfahren zu ihrer herstellung
US6077840A (en) 1996-12-18 2000-06-20 Meiji Seika Kaisha, Ltd. Tetrahydrobenzindolone derivatives
AU728988B2 (en) 1997-06-05 2001-01-25 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
GB9718913D0 (en) 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
AR015425A1 (es) 1997-09-05 2001-05-02 Smithkline Beecham Corp Compuestos de benzotiazol, composicion farmaceutica que los contiene, su uso en la manufactura de un medicamento, procedimiento para su preparacion,compuestos intermediarios y procedimiento para su preparacion
WO1999015524A1 (en) * 1997-09-23 1999-04-01 Fujisawa Pharmaceutical Co., Ltd. Thiazole derivatives
US5998463A (en) * 1998-02-27 1999-12-07 Pfizer Inc Glycogen phosphorylase inhibitors
NZ506217A (en) 1998-03-06 2002-05-31 Astra Ab Compound for treatment of tuberculosis and other mycobacterial diseases
EP0978279A1 (en) 1998-08-07 2000-02-09 Pfizer Products Inc. Inhibitors of human glycogen phosphorylase
US6339098B1 (en) 1999-05-04 2002-01-15 American Home Products Corporation 2,1-benzisothiazoline 2,2-dioxides
US6399593B1 (en) 1999-05-04 2002-06-04 Wyeth Cyclic regimens using cyclic urea and cyclic amide derivatives
US6380235B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Benzimidazolones and analogues
US6462032B1 (en) 1999-05-04 2002-10-08 Wyeth Cyclic regimens utilizing indoline derivatives
US6358948B1 (en) 1999-05-04 2002-03-19 American Home Products Corporation Quinazolinone and benzoxazine derivatives as progesterone receptor modulators
US6423699B1 (en) 1999-05-04 2002-07-23 American Home Products Corporation Combination therapies using benzimidazolones
US6417214B1 (en) 1999-05-04 2002-07-09 Wyeth 3,3-substituted indoline derivatives
US6407101B1 (en) * 1999-05-04 2002-06-18 American Home Products Corporation Cyanopyrroles
US6380178B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Cyclic regimens using cyclocarbamate and cyclic amide derivatives
US6369056B1 (en) 1999-05-04 2002-04-09 American Home Products Corporation Cyclic urea and cyclic amide derivatives
US6319912B1 (en) 1999-05-04 2001-11-20 American Home Products Corporation Cyclic regimens using 2,1-benzisothiazoline 2,2-dioxides
US6391907B1 (en) 1999-05-04 2002-05-21 American Home Products Corporation Indoline derivatives
US6358947B1 (en) 1999-05-04 2002-03-19 American Home Products Corporation Tetracyclic progesterone receptor modulator compounds and methods
US6355648B1 (en) 1999-05-04 2002-03-12 American Home Products Corporation Thio-oxindole derivatives
US6306851B1 (en) 1999-05-04 2001-10-23 American Home Products Corporation Cyclocarbamate and cyclic amide derivatives
US6444668B1 (en) 1999-05-04 2002-09-03 Wyeth Combination regimens using progesterone receptor modulators
US6329416B1 (en) 1999-05-04 2001-12-11 American Home Products Corporation Combination regimens using 3,3-substituted indoline derivatives
US6498154B1 (en) 1999-05-04 2002-12-24 Wyeth Cyclic regimens using quinazolinone and benzoxazine derivatives
US6509334B1 (en) 1999-05-04 2003-01-21 American Home Products Corporation Cyclocarbamate derivatives as progesterone receptor modulators
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
US6566385B2 (en) * 2000-01-12 2003-05-20 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
UA73119C2 (en) 2000-04-19 2005-06-15 American Home Products Corpoir Derivatives of cyclic thiocarbamates, pharmaceutical composition including noted derivatives of cyclic thiocarbamates and active ingredients of medicines as modulators of progesterone receptors
FR2832233B1 (fr) * 2001-11-13 2004-01-02 France Telecom Reconfiguration de composants programmables dans un appareil electronique
MXPA04012420A (es) 2002-06-25 2005-04-19 Wyeth Corp Derivados de ciclotiocabamativa como moduladores de rp y uso de los mismos para tratamiento de trastornos de la piel.
KR20050012831A (ko) 2002-06-25 2005-02-02 와이어쓰 피부 질환을 치료하는 데 있어서의 티오-옥스인돌유도체의 용도
CA2489813A1 (en) 2002-06-25 2003-12-31 Wyeth Use of thio-oxindole derivatives in treatment of hormone-related conditions
EP1515725A4 (en) 2002-06-25 2005-09-21 Wyeth Corp USE OF CYCLOTHIOCARBAMATE DERIVATIVES IN THE TREATMENT OF HORMONE-RELATED ILLNESSES
TWI223448B (en) * 2003-04-29 2004-11-01 Mosel Vitelic Inc DMOS device having a trenched bus structure
GT200500186A (es) 2004-07-07 2006-03-02 Regimenes anticonceptivos con antagonistas del receptor de progesterona y kits
EP1773344A1 (en) 2004-07-07 2007-04-18 Wyeth a Corporation of the State of Delaware Cyclic progestin regimens and kits
GT200500183A (es) 2004-08-09 2006-04-10 Moduladores del receptor de progesterona que comprenden derivados de pirrol-oxindol y sus usos
GT200500185A (es) 2004-08-09 2006-04-10 Moduladores del receptor de progesterona que comprenden derivados de pirrol-oxindol y sus usos
US7569679B2 (en) 2004-08-13 2009-08-04 Wyeth Tanaproget derivatives, metabolites, and uses thereof

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KR20010114252A (ko) 2001-12-31
US6391907B1 (en) 2002-05-21
NO20015379D0 (no) 2001-11-02
WO2000066556A1 (en) 2000-11-09
EP1175398A1 (en) 2002-01-30
NO20015379L (no) 2002-01-03
EP1175398B1 (en) 2007-07-11
HUP0200992A2 (hu) 2002-07-29
CA2371638A1 (en) 2000-11-09
US20030220388A1 (en) 2003-11-27
CN1141295C (zh) 2004-03-10
DK1175398T3 (da) 2007-11-05
HUP0200992A3 (en) 2004-12-28
US7084168B2 (en) 2006-08-01
US7253203B2 (en) 2007-08-07
DE60035496D1 (de) 2007-08-23
ZA200107631B (en) 2002-05-14
US7645761B2 (en) 2010-01-12
PL351954A1 (en) 2003-07-14
CZ20013953A3 (cs) 2002-06-12
DE60035496T2 (de) 2008-03-13
MXPA01011298A (es) 2003-07-14
IL146281A0 (en) 2002-07-25
ES2290035T3 (es) 2008-02-16
BR0010215A (pt) 2002-02-13
AU4814100A (en) 2000-11-17
US20070259944A1 (en) 2007-11-08
CN1350523A (zh) 2002-05-22
US6608068B2 (en) 2003-08-19
US20060160882A1 (en) 2006-07-20
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US20020086874A1 (en) 2002-07-04
ATE366721T1 (de) 2007-08-15

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