CN1141295C - 作为黄体酮拮抗剂的二氢吲哚衍生物 - Google Patents

作为黄体酮拮抗剂的二氢吲哚衍生物 Download PDF

Info

Publication number
CN1141295C
CN1141295C CNB008071411A CN00807141A CN1141295C CN 1141295 C CN1141295 C CN 1141295C CN B008071411 A CNB008071411 A CN B008071411A CN 00807141 A CN00807141 A CN 00807141A CN 1141295 C CN1141295 C CN 1141295C
Authority
CN
China
Prior art keywords
indoles
spiral shell
hexanaphthene
dihydro
ketone
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.)
Expired - Fee Related
Application number
CNB008071411A
Other languages
English (en)
Chinese (zh)
Other versions
CN1350523A (zh
Inventor
A�����߶���ɭ
A·芬森
L·L·米勒
���ڶ���
J·W·乌尔里克
W
R·H·W·本德
张普文
J·E·弗罗贝尔
»
智林
��ظ�
T·K·琼斯
J·P·爱德华兹
C·M·特格利
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Hui Shi
Original Assignee
Ligand Pharmaceuticals Inc
American Home Products Corp
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 Ligand Pharmaceuticals Inc, American Home Products Corp filed Critical Ligand Pharmaceuticals Inc
Publication of CN1350523A publication Critical patent/CN1350523A/zh
Application granted granted Critical
Publication of CN1141295C publication Critical patent/CN1141295C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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
    • C07D209/30—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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Steroid Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CNB008071411A 1999-05-04 2000-05-01 作为黄体酮拮抗剂的二氢吲哚衍生物 Expired - Fee Related CN1141295C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US18305899P 1999-05-04 1999-05-04
US60/183,058 1999-05-04
US09/552,632 2000-04-19
US09/552,632 US6391907B1 (en) 1999-05-04 2000-04-19 Indoline derivatives

Publications (2)

Publication Number Publication Date
CN1350523A CN1350523A (zh) 2002-05-22
CN1141295C true CN1141295C (zh) 2004-03-10

Family

ID=26878706

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB008071411A Expired - Fee Related CN1141295C (zh) 1999-05-04 2000-05-01 作为黄体酮拮抗剂的二氢吲哚衍生物

Country Status (21)

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

Families Citing this family (56)

* 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
US6462032B1 (en) 1999-05-04 2002-10-08 Wyeth Cyclic regimens utilizing indoline derivatives
US6444668B1 (en) 1999-05-04 2002-09-03 Wyeth Combination regimens using progesterone receptor modulators
US6509334B1 (en) * 1999-05-04 2003-01-21 American Home Products Corporation Cyclocarbamate derivatives as progesterone receptor modulators
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
US6391907B1 (en) 1999-05-04 2002-05-21 American Home Products Corporation Indoline derivatives
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
JP3836790B2 (ja) * 2000-11-15 2006-10-25 昌雄 菅又 子宮内膜症の予防又は治療薬
AU2003245637A1 (en) 2002-06-25 2004-01-06 Wyeth Use of thio-oxindole derivatives in treatment of hormone-related conditions
CN1662206A (zh) 2002-06-25 2005-08-31 惠氏公司 硫代－2－羟基吲哚衍生物在治疗皮肤病中的用途
EP1558618A1 (en) * 2002-10-11 2005-08-03 Ligand Pharmaceuticals, Inc. 5-(1 ,1 -CYCLOALKYL/ALKENYL)METHYLIDENE 1,2-DIHYDRO- 5H /-CHROMENO[3,4-f ] QUINOLINES AS SELECTIVE PROGESTERONE RECEPTOR MODULATOR COMPOUNDS
AU2003258050A1 (en) * 2002-10-11 2004-05-04 Ligand Pharmaceuticals Incorporated 5-cycloalkenyl 5h-chromeno(3,4-f)quinoline derivatives as selective progesterone receptor modulator compounds
AU2003286604A1 (en) * 2002-10-21 2004-05-13 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
US7517899B2 (en) 2004-03-30 2009-04-14 Wyeth Phenylaminopropanol derivatives and methods of their use
US7414052B2 (en) 2004-03-30 2008-08-19 Wyeth Phenylaminopropanol derivatives and methods of their use
US20070299102A1 (en) * 2004-04-08 2007-12-27 Topo Target A/S Diphenyl Ox-Indol-2-One Compounds and Their Use in the Treatment of Cancer
JP4869221B2 (ja) * 2004-04-08 2012-02-08 ワイス・エルエルシー プロゲステロン受容体調節剤としてのチオアミド誘導体
ATE409699T1 (de) * 2004-04-08 2008-10-15 Wyeth Corp Verfahren zur minimierung von thioamidverunreinigungen
AU2005238520B2 (en) 2004-04-27 2011-09-08 Wyeth Cyanopyrrole containing cyclic carbamate and thiocarbamate biaryls and methods for preparing the same
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
AU2005237520B2 (en) 2004-04-27 2012-01-19 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
EP2502925A1 (en) * 2004-10-27 2012-09-26 Janssen Pharmaceutica NV Pyridine imidazoles and aza-indoles 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
US7414142B2 (en) * 2005-09-19 2008-08-19 Wyeth 5-aryl-indan-1-one oximes 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
PE20070584A1 (es) 2005-09-29 2007-07-09 Wyeth Corp Derivados de propilamina sustituidas que mejoran la recaptacion de monoaminas
US20070213526A1 (en) * 2006-03-07 2007-09-13 Wyeth Purification of progesterone receptor modulators
EP2078032B1 (en) 2006-10-24 2017-08-02 Repros Therapeutics Inc. Compositions and methods for suppressing endometrial proliferation
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
US8273749B2 (en) * 2007-10-04 2012-09-25 Merck Sharp & Dohme Corp. N-substituted oxindoline derivatives as calcium channel blockers
JP2010540628A (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
PH12012501812A1 (en) 2010-03-22 2012-12-10 Allergan Pharmaceuticals Int Ltd Compositions and methods for non-toxic delivery of antiprogestins
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
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
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
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
WO2018064557A1 (en) * 2016-09-30 2018-04-05 Epizyme, Inc. Substituted fused bi- or tri- heterocyclic compounds as ehmt2 inhibitors
EP3612181A4 (en) 2017-04-21 2021-01-06 Epizyme, Inc. Combination therapies with ehmt2 inhibitors
SG11202111552YA (en) 2019-05-08 2021-11-29 Aligos Therapeutics Inc MODULATORS OF THR-ß 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
WO2025013907A1 (en) * 2023-07-10 2025-01-16 Okinawa Institute Of Science And Technology School Corporation Use of spirooxindole oxirane derivative for modifying peptide and/or protein

Family Cites Families (107)

* 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
JPH0452299Y2 (enExample) 1987-01-14 1992-12-09
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
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
US5182282A (en) * 1989-04-28 1993-01-26 Roussel Uclaf 4-Benzyl-1H-indole derivatives
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 (enExample) 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
JP3419539B2 (ja) * 1993-02-17 2003-06-23 中外製薬株式会社 インドリン−２−オン誘導体
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
AU1694295A (en) 1994-01-28 1995-08-15 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
EP0765324A1 (en) 1994-06-08 1997-04-02 E.I. Du Pont De Nemours And Company Cyclic sulfonamide herbicides
DE69532894T2 (de) 1994-11-22 2004-09-02 Balance Pharmaceuticals, Inc., Pacific Palisades Verfahren zur empfängnisverhütung
US5521166A (en) 1994-12-19 1996-05-28 Ortho Pharmaceitical Corporation Antiprogestin cyclophasic hormonal regimen
ATE269336T1 (de) 1994-12-22 2004-07-15 Ligand Pharm Inc Steroidrezeptor-modulator verbindungen und methoden
US5693646A (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
ES2174265T3 (es) 1996-06-25 2002-11-01 Akzo Nobel Nv Regimenes de progestogeno-anti-progestogeno.
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
WO1998014436A1 (en) 1996-10-02 1998-04-09 Dupont Pharmaceuticals Company 4,4-disubstituted-1,4-dihydro-2h-3,1-benzoxazin-2-ones useful as hiv reverse transcriptase inhibitors and intermediates and processes for making the same
WO1998027059A1 (en) 1996-12-18 1998-06-25 Meiji Seika Kaisha, Ltd. Novel tetrahydrobenzindolone derivatives
JP2002502427A (ja) 1997-06-05 2002-01-22 メルク エンド カンパニー インコーポレーテッド ゴナドトロピン放出ホルモンの拮抗薬
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
US6319912B1 (en) 1999-05-04 2001-11-20 American Home Products Corporation Cyclic regimens using 2,1-benzisothiazoline 2,2-dioxides
US6423699B1 (en) * 1999-05-04 2002-07-23 American Home Products Corporation Combination therapies using benzimidazolones
US6509334B1 (en) 1999-05-04 2003-01-21 American Home Products Corporation Cyclocarbamate derivatives as progesterone receptor modulators
US6380235B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Benzimidazolones and analogues
US6329416B1 (en) * 1999-05-04 2001-12-11 American Home Products Corporation Combination regimens using 3,3-substituted indoline derivatives
US6358947B1 (en) * 1999-05-04 2002-03-19 American Home Products Corporation Tetracyclic progesterone receptor modulator compounds and methods
US6369056B1 (en) 1999-05-04 2002-04-09 American Home Products Corporation Cyclic urea and cyclic amide derivatives
US6380178B1 (en) * 1999-05-04 2002-04-30 American Home Products Corporation Cyclic regimens using cyclocarbamate and cyclic amide derivatives
US6358948B1 (en) 1999-05-04 2002-03-19 American Home Products Corporation Quinazolinone and benzoxazine derivatives as progesterone receptor modulators
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
US6399593B1 (en) * 1999-05-04 2002-06-04 Wyeth Cyclic regimens using cyclic urea and cyclic amide derivatives
US6462032B1 (en) * 1999-05-04 2002-10-08 Wyeth Cyclic regimens utilizing indoline derivatives
US6391907B1 (en) 1999-05-04 2002-05-21 American Home Products Corporation Indoline derivatives
US6339098B1 (en) 1999-05-04 2002-01-15 American Home Products Corporation 2,1-benzisothiazoline 2,2-dioxides
US6306851B1 (en) 1999-05-04 2001-10-23 American Home Products Corporation Cyclocarbamate and cyclic amide derivatives
US6417214B1 (en) * 1999-05-04 2002-07-09 Wyeth 3,3-substituted indoline derivatives
US6498154B1 (en) * 1999-05-04 2002-12-24 Wyeth Cyclic regimens using quinazolinone and benzoxazine derivatives
US6355648B1 (en) 1999-05-04 2002-03-12 American Home Products Corporation Thio-oxindole derivatives
JP2003525796A (ja) 1999-08-26 2003-09-02 オートモーティブ システムズ ラボラトリー インコーポレーテッド 磁気センサ
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
IL165397A0 (en) 2002-06-25 2006-01-15 Wyeth Corp Cyclothiocarbamative derivatives as pr modulators and use thereof for treatment of skin disorders
AU2003245637A1 (en) 2002-06-25 2004-01-06 Wyeth Use of thio-oxindole derivatives in treatment of hormone-related conditions
CN1662206A (zh) 2002-06-25 2005-08-31 惠氏公司 硫代－2－羟基吲哚衍生物在治疗皮肤病中的用途
CN1662241A (zh) 2002-06-25 2005-08-31 惠氏公司 环硫代氨基甲酸酯衍生物在治疗与激素有关的病症中的用途
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
AR049707A1 (es) 2004-07-07 2006-08-30 Wyeth Corp Regimenes y kits de progestina ciclica
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
MX2007001812A (es) 2004-08-13 2007-03-26 Wyeth Corp Derivados de tanaproget, metabolitos, y usos de los mismos.

Also Published As

Publication number Publication date
US6391907B1 (en) 2002-05-21
US20030220388A1 (en) 2003-11-27
NO20015379L (no) 2002-01-03
US7645761B2 (en) 2010-01-12
ZA200107631B (en) 2002-05-14
DE60035496T2 (de) 2008-03-13
US20060160882A1 (en) 2006-07-20
CN1350523A (zh) 2002-05-22
HUP0200992A3 (en) 2004-12-28
EP1175398A1 (en) 2002-01-30
IL146281A0 (en) 2002-07-25
US20070259944A1 (en) 2007-11-08
BR0010215A (pt) 2002-02-13
KR20010114252A (ko) 2001-12-31
MXPA01011298A (es) 2003-07-14
US7084168B2 (en) 2006-08-01
EA200101177A1 (ru) 2002-04-25
US6608068B2 (en) 2003-08-19
EP1175398B1 (en) 2007-07-11
ES2290035T3 (es) 2008-02-16
ATE366721T1 (de) 2007-08-15
WO2000066556A1 (en) 2000-11-09
JP2002543183A (ja) 2002-12-17
PL351954A1 (en) 2003-07-14
AU4814100A (en) 2000-11-17
DK1175398T3 (da) 2007-11-05
NO20015379D0 (no) 2001-11-02
CZ20013953A3 (cs) 2002-06-12
CA2371638A1 (en) 2000-11-09
HUP0200992A2 (hu) 2002-07-29
DE60035496D1 (de) 2007-08-23
US7253203B2 (en) 2007-08-07
US20020086874A1 (en) 2002-07-04

Similar Documents

Publication Publication Date Title
CN1141295C (zh) 作为黄体酮拮抗剂的二氢吲哚衍生物
CN1152020C (zh) 苯并咪唑酮和类似物以及它们作为黄体酮配体的用途
CN1215067C (zh) 哒嗪酮醛糖还原酶抑制剂
CN1282640C (zh) N－芳基苯乙酰胺衍生物及包含所述化合物的药物组合物
CN1113236A (zh) 非肽基速激肽受体拮抗剂
CN1349413A (zh) 含喹唑啉酮和苯并噁嗪衍生物的避孕组合物
CN1898205A (zh) 吲哚满酮衍生物及其在治疗疾病状态如癌症中的用途
CN1106804A (zh) 1-苯碘酰-1，3-二氢-2h-苯并咪唑-2-酮衍生物
CN1823046A (zh) 苯基喹啉及其作为雌激素受体调节剂的用途
CN1505613A (zh) 取代的吲哚、含这类吲哚的药物组合物及它们作为PPAR-γ结合剂的用途
CN1699347A (zh) 用于治疗炎症的取代的吡唑基苯磺酰胺类化合物
CN1703403A (zh) 趋代谢的谷氨酸盐受体拮抗剂
CN1495170A (zh) 用于治疗炎症的取代的吡唑基苯磺酰胺类化合物
CN1173497A (zh) 含杂环碳酸衍生物
CN1349537A (zh) 环脲和环酰胺衍生物
CN1993321A (zh) 作为单胺再摄取抑制剂的3－氨基－1－芳基丙基吲哚类化合物
CN1201820C (zh) 含苯并咪唑酮和孕激素的组合物
CN1993343A (zh) 作为雌激素配体的四环化合物
CN1131856C (zh) 作为黄体酮受体调节剂的环硫代氨基甲酸酯衍生物
CN1069974A (zh) 三唑基取代的叔胺化合物及其盐
CN1599737A (zh) 稠环吡唑衍生物
CN1589268A (zh) 作为选择性雌激素受体－β激动剂的取代的苯并吡喃类化合物
CN1249057C (zh) 用作抗菌剂的色烯基甲基嘧啶二胺
CN1179753C (zh) 含有抗孕激素和孕激素的避孕组合物
CN1124026A (zh) 新型哌啶基硫代吲哚衍生物，它们的制备方法，和含有它们的药物组合物，作为止痛药的用途

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
C56 Change in the name or address of the patentee

Owner name: WYETH CORP.; LEGA PHARMACY CO.,LTD.

Free format text: FORMER NAME OR ADDRESS: AMERICAN HOME PRODUCTS CORP.; LEGA PHARMACY CO.,LTD.

CP01 Change in the name or title of a patent holder

Patentee after: Wyeth Corp.

Patentee after: Ligand Pharmaceuticals, Inc.

Patentee before: American Home Products Corp.

Patentee before: Ligand Pharmaceuticals, Inc.

ASS Succession or assignment of patent right

Owner name: WYETH(AMERICAN HOME PRODUCTS)

Free format text: FORMER OWNER: WYETH(AMERICAN HOME PRODUCTS); LEGA PHARMACY CO.,LTD.

Effective date: 20061208

C41 Transfer of patent application or patent right or utility model
TR01 Transfer of patent right

Effective date of registration: 20061208

Address after: new jersey

Patentee after: Hui Shi

Address before: new jersey

Co-patentee before: Ligand Pharmaceuticals, Inc.

Patentee before: Hui Shi

C17 Cessation of patent right
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20040310

Termination date: 20100501