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91. 发明专利

CA2372279A1 COMPOSITIONS CONTAINING BENZIMIDAZOLONES AND PROGESTOGENS 未知
公开(公告)号：CA2372279A1
公开(公告)日：2000-11-09
申请号：CA2372279
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC
发明人： JONES TODD K , TEGLEY CHRISTOPHER M , ZHI LIN , GRUBB GARY S , EDWARDS JAMES P , WROBEL JAY E , BENDER REINHOLD H W , ZHANG PUWEN
IPC分类号： C07D277/68 , A61K31/415 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4985 , A61K31/535 , A61K31/54 , A61K31/5415 , A61K31/56 , A61K31/57 , A61K38/22 , A61K45/00 , A61K45/06 , A61P15/18 , A61P43/00 , C07D235/26 , C07D241/44 , C07D263/58 , C07D279/16 , A61K31/41 , A61K31/495 , A61K31/565
摘要： This invention relates to cyclic combination therapies and regimens utilizin g substituted indoline derivative compounds which are antagonists of the progesterone receptor having general structure (1) wherein: A is O, S, or NR 4; B is a bond between A and C=Q, or the moiety CR5R6; R4, R5, R6 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 t o C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to form a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substitut ed C1 to C6 alkenyl, alkynyl, substituted alkynyl, -COH, or optionally substituted -CO(C1 to C3 alkyl), -CO(aryl), -CO(C1 to C3 alkoxy), or -CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionall y substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstituted benzene ring; or a 5- or 6-membered heteroaromatic ring containing 1 or 2 substituents; or a pharmaceutically acceptable salt thereof, in combination with a progestational agent, an estrogen, or both or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium , ovary, breast, colon, prostate. These combinations may also be used in metho ds of contraception, to stimulate food intake or for minimization of side effec ts or cyclic menstrual bleeding.

92. 发明专利

CA2259031C ANDROGEN RECEPTOR MODULATOR COMPOUNDS AND METHODS 未知
公开(公告)号：CA2259031C
公开(公告)日：2006-10-24
申请号：CA2259031
申请日：1997-06-26
申请人： LIGAND PHARM INC
发明人： JONES TODD , HIGUCHI ROBERT , EDWARDS JAMES P , HAMANN LAWRENCE G
IPC分类号： C07D471/04 , C07D491/052 , A61K31/47 , C07D455/03 , C07D471/14 , C07D471/16 , C07D491/044 , C07D491/147 , C07D495/04 , C07D495/14 , C07D498/16
摘要： Non-steroidal compounds which are high affinity, high selectivity modulato rs for androgen receptors are disclosed, having the formula: (see formula I, III, IV, V) (see formula VI) Also disclosed are pharmaceutical compositions incorporating such compound s, methods for employing the disclosed compounds and compositions for treating patients requiring androgen receptor agonist, partial agonist or antagonist therapy, intermediates usefully in the preparation of the compounds and processes for the preparation of the androgen receptor modulator compounds.

93. 发明专利

DK1173433T3 未知
公开(公告)号：DK1173433T3
公开(公告)日：2006-05-15
申请号：DK00932005
申请日：2000-05-01
申请人： WYETH CORP , LIGAND PHARM INC
发明人： COLLINS MARK A , MACKNER VALERIE A , ZHI LIN , JONES TODD K , TEGLEY CHRISTOPHER M , WROBEL JAY E , EDWARDS JAMES P
IPC分类号： C07D403/04 , C07D413/04 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/536 , A61K31/5415 , A61P5/34 , A61P13/08 , A61P15/00 , A61P15/14 , A61P15/16 , A61P15/18 , A61P35/00 , A61P43/00
摘要： This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein, T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain -CH2(CH2)nCH2-, -CH2CH2CMe2CH2CH2-, -O(CH2)pCH2-, -O(CH2)qO-, -CH2CH2OCH2CH2-, or -CH2CH2NR7CH2CH2-; n=1-5; p=1-4; q=1-4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB; RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof.

94. 发明专利

NO321361B1 未知
公开(公告)号：NO321361B1
公开(公告)日：2006-05-02
申请号：NO20015378
申请日：2001-11-02
申请人： LIGAND PHARM INC , WYETH CORP
发明人： FLETCHER III HORACE , EDWARDS JAMES P , ZHANG PUWEN , TEREFENKO EUGENE A , FENSOME ANDREW , WROBEL JAY E , TEGLEY CHRISTOPHER M , JONES TODD KEVIN , ZHI LIN
IPC分类号： C07D265/12 , C07D265/18 , A61K31/536 , A61K31/537 , A61P15/00 , A61P15/18 , A61P35/00 , A61P43/00 , C07D413/04 , C07D413/10 , C07D417/04 , C07F9/6533
摘要： 1. Technical Result Increase in efficiency of treatment of progesterone-related maladies. 2. Essence This invention provides compounds of Formula wherein R1 and R2 may be single substituents or fused to form spirocyclic or heterospirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, CORc; Rc is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy , substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, NO2, amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aminoalkyl, CORF, or NRGCORF; and pharmaceutical compositions containing them for treatment progesterone-related maladies. 3. Field of Application Medicine.

95. 发明专利

EA004512B1 ЦИКЛОКАРБАМАТНЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ РЕЦЕПТОРА ПРОГЕСТЕРОНА 未知
公开(公告)号：EA004512B1
公开(公告)日：2004-04-29
申请号：EA200101176
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC
发明人： ZHANG PUWEN , TEREFENKO EUGENE A , FLETCHER HORACE III , FENSOME ANDREW , WROBEL JAY E , ZHI LIN , JONES TODD K , TEGLEY CHRISTOPHER M , EDWARDS JAMES P
IPC分类号： C07D265/12 , A61K31/536 , A61K31/537 , A61P15/18 , A61P35/00 , A61P43/00 , C07D265/18 , C07D413/04 , C07D413/10 , C07D417/04 , C07F9/6533 , A61P15/00
摘要： Изобретениеотноситсяк соединениямформулыгде Rи Rпредставляютсобойнезависимыезаместители, выбранныеизгруппы, включающейН, C-Cалкил, замещенный C-Cалкил, C-Cалкенил, замещенный C-Cалкенил, C-Cалкинил, замещенный C-Cалкинил, C-Cциклоалкил, замещенный C-Cциклоалкил, арил, замещенныйарил, гетероциклил, замещенныйгетероциклил CORили NRCOR; или Rи Rсконденсированыс образованиемнасыщенногоилиненасыщенного 3-8-членногоспироциклическогокольца, необязательносодержащегов своемскелетеотодногодотрехгетероатомов, выбранныхизгруппы, включающейО, S и N; причемкольцоможетбытьнеобязательнозамещено 1-4 заместителями, выбраннымиизгруппы, включающейфтор, C-Cалкил, C-Cалкокси, C-Cтиоалкил, CF, ОН, CN, NH, NH(C-Cалкил) или N(C-Cалкил); RвыбираютизН, C-Cалкила, замещенного C-Cалкила, арила, замещенногоарила, C-Cалкокси, замещенного C-Cалкокси, C-Cаминоалкилаилизамещенного C-Cаминоалкила; RпредставляетсобойН, C-Cалкилилизамещенный C-Cалкил; RпредставляетсобойН, ОН, NH, C-Cалкил, замещенный C-Cалкил, C-Cалкенил, замещенный C-Cалкенил, алкинил, замещенныйалкинил, или COR; RпредставляетсобойН, C-Cалкил, замещенный C-Cалкил, арил, замещенныйарил, C-Cалкокси, замещенный C-Cалкокси, C-Cаминоалкилилизамещенный C-Cаминоалкил; RпредставляетсобойН, галоген, CN, NO, C-Cалкил, замещенный C-Cалкил, алкинил, замещенныйалкинил, C-Cалкокси, замещенный C-Cалкокси, амино, C-Cаминоалкилилизамещенный C-Cаминоалкил; Rвыбираютизгруппы, включающейзамещенноебензольноекольцо, содержащеезаместители X, Y и Z, определенныев формулеизобретения, илипятиилишестичленноекольцос 1,2 или 3 гетероатомамив кольце, выбраннымиизгруппы, включающейО, S, SO, SOили NR, содержащееодинилидванезависимыхзаместителя, определенныхв формулеизобретения; RотсутствуетилипредставляетсобойН, О,

96. 发明专利

BR0207543A 未知
公开(公告)号：BR0207543A
公开(公告)日：2004-04-27
申请号：BR0207543
申请日：2002-02-23
申请人： LIGAND PHARM INC
发明人： HIGUCHI ROBERT I , ZHI LIN , KARANEWSKY DONALD S , THOMPSON ANTHONY W , CAFERRO THOMAS R , MANI NEELAKANDHA S , CHEN JYUN-HUNG , CUMMINGS MARQUIS L , EDWARDS JAMES P , ADAMS MARK E , DECKHUT CHARLOTTE L F
IPC分类号： G01N33/50 , A61K31/5383 , A61P5/00 , A61P5/26 , A61P5/28 , A61P13/08 , A61P15/08 , A61P15/10 , A61P17/00 , A61P17/10 , A61P17/14 , A61P19/10 , A61P35/00 , A61P43/00 , C07D498/04 , C07D498/14 , A61K31/5365
摘要： Non-steroidal tricyclic quinolinone and tricyclic quinoline compounds and compositions that are agonists, partial agonists and/or antagonists for androgen receptors (AR), their preparation and their uses are described.

97. 发明专利

GEP20043266B Thio-Oxindole Derivatives 未知
公开(公告)号：GEP20043266B
公开(公告)日：2004-01-12
申请号：GEAP2000004531
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC
发明人： ZHANG PUWEN , FENSOME ANDREW , WROBEL JAY E , ZHI LIN , JONES TODD K , TEGLEY CHRISTOPHER M , EDWARDS JAMES P , KOKO MARCI C , MELENSKI EDWARD G
IPC分类号： C07D209/08 , C07D409/10 , A61K31/404 , A61P1/00 , A61P5/34 , A61P5/36 , A61P7/00 , A61P7/04 , A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00 , C07D209/30 , C07D209/40 , C07D209/96
摘要： 1. Technical Result Improvement of medicinal properties and increase in treatment efficiency. 2. Essence A compound of the formula (1) wherein R1-R5 and Q have the values indicated in the description or a pharmaceutically acceptable salt thereof and their use for mammals to obtain the medicament for treatment carcinomas and adenocarcinomas of endometrium, ovary, mammary gland, colon or prostatitis, dysfunctional haemorrhage and menopause after substitution hormonotherapy 3. Field of Application Medicine.

98. 发明专利

HK1043986A1 3,3-Substituted indoline derivatives. 未知
公开(公告)号：HK1043986A1
公开(公告)日：2002-10-04
申请号：HK02104852
申请日：2002-06-28
申请人： WYETH CORP , LIGAND PHARM INC
发明人： ULLRICH JOHN W , FENSOME ANDREW , ZHI LIN , JONES TODD K , WROBEL JAY E , TEGLEY CHRISTOPHER M , EDWARDS JAMES P
IPC分类号： C07D401/04 , A61K31/403 , A61K31/404 , A61K31/4427 , A61K31/506 , A61P1/00 , A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00 , C07D209/08 , C07D209/86 , C07D209/96 , C07D403/04 , C07D405/04 , C07D409/04 , C07D , A61K , A61P

99. 发明专利

PT918774E 未知
公开(公告)号：PT918774E
公开(公告)日：2002-05-31
申请号：PT97931460
申请日：1997-06-26
申请人： LIGAND PHARM INC
发明人： EDWARDS JAMES P , HIGUCHI ROBERT , JONES TODD
IPC分类号： C07D491/052 , A61K31/4738 , A61K31/4745 , A61P5/26 , C07D471/04 , C07D471/14 , C07D471/16 , C07D487/02 , C07D487/04 , C07D487/12 , C07D491/044 , C07D491/147 , C07D498/12 , C07D498/16 , A61K31/47 , C07D491/06

100. 发明专利

ZA200107633B Cyclothiocarbamate derivatives as progesterone receptor modulators. 未知
公开(公告)号：ZA200107633B
公开(公告)日：2002-05-14
申请号：ZA200107633
申请日：2001-09-17
申请人： AMERICAN HOME PROD , LIGAND PHARM INC
发明人： ZHANG PUWEN , FENSOME ANDREW , TEREFENKO EUGENE A , WROBEL JAY E , EDWARDS JAMES P , JONES TODD K , TEGLEY CHRISTOPHER M , ZHI LIN , COLLINS MARK A
IPC分类号： A61K20060101 , A61P20060101 , C07D20060101 , A61K , A61P , C07D

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