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41. 发明专利

BR0010214A 未知
公开(公告)号：BR0010214A
公开(公告)日：2002-02-13
申请号：BR0010214
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC
发明人： ZHANG PUWEN , TEREFENKO EUGENE A , FENSOME ANDREW , WROBEL JAY E , ZHI LIN , JONES TODD K , TEGLEY CHRISTOPHER M , EDWARDS JAMES P , COLLINS MARK A
IPC分类号： A61K31/535 , A61K31/5355 , A61P15/00 , A61P15/18 , A61P35/00 , A61P43/00 , C07D265/18 , C07D413/04 , A61K31/536
摘要： PROBLEM TO BE SOLVED: To provide novel cyclothiocarbamate derivatives which are agonists of the progesterone receptor.SOLUTION: This invention relates to compounds expressed by the following formula, wherein R is a substituent. The derivatives are useful for: birth control; and treating and preventing progesterone-related disorder.

42. 发明专利

CA2372773A1 CONTRACEPTIVE COMPOSITIONS CONTAINING ANTIPROGESTINIC AND PROGESTINIC 未知
公开(公告)号：CA2372773A1
公开(公告)日：2000-11-09
申请号：CA2372773
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC
发明人： FLETCHER HORACE A , GRUBB GARY S , TEGLEY CHRISTOPHER M , ZHANG PUWEN , TEREFENKO EUGENE A , FENSOME ANDREW , WROBEL JAY E , JONES TODD K , ZHI LIN , EDWARDS JAMES P
IPC分类号： A61K31/567 , A61K20060101 , A61K31/535 , A61K31/5355 , A61K31/536 , A61K31/537 , A61K31/565 , A61K31/57 , A61K45/06 , A61P20060101 , A61P15/18
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 (I): wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic 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, amino, C1 to C6 aminoalkyl, or substituted C1 t o C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a fi ve 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 th e group including H, halogen, CN, NO2 , amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aminoalkyl, CORF, or NRGCORF; or pharmaceutically acceptabl e salt thereof. These methods of treatment may be used for contraception or fo r the treatmentand/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endormetrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention inlcude stimulation of food intake.

43. 发明专利

CA2371632A1 CYCLOCARBAMATE AND CYCLIC AMIDE DERIVATIVES 未知
公开(公告)号：CA2371632A1
公开(公告)日：2000-11-09
申请号：CA2371632
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC
发明人： ZHANG PUWEN , FENSOME ANDREW , ZHI LIN , VIET ANDREW Q , SANTILLI ARTHUR A , TEGLEY CHRISTOPHER M , JONES TODD K , WROBEL JAY E , EDWARDS JAMES P
IPC分类号： C07D495/04 , A61K31/407 , A61K31/429 , A61K31/5365 , A61P15/18 , A61P35/00 , A61P43/00 , C07D498/04 , C07D498/10 , C07D513/04 , C07D513/10 , A61K31/535 , C07D265/00 , C07D333/00
摘要： This invention provides compounds of formula (I) wherein A and B are independent substituents selected from S, CH or N; provided that when A is S , B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N, one N may be optionally substituted with a C1 to C6 alkyl group; R1 and R2 are independent substituents selected from the group of H, C1 to C6 alkyl, substituted C1 to C6 alkyl, C2 to C6 alkyl, C2 t o C6 alkenyl, substituted C2 to C6 alkenyl, C2 to C6 alkynyl, substituted C2 t o C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, CORA, or NRBCORA; or R1 and R2 are fused to form optionally substituted 3 to 8 membered spirocycl ic alkyl, alkenyl or heterocyclic ring, the heterocyclic ring containing one to three heteroatoms selected from the group of O, S and N; or pharmaceutically useful salts thereof. The compounds of this invention are useful as agonists and antagonists of the progesterone receptor and in methods of inducing contraception and in the treatment or prevention of benign or malignant neoplastic diseases.

44. 发明专利

CA2371629A1 3,3-SUBSTITUTED INDOLINE DERIVATIVES 未知
公开(公告)号：CA2371629A1
公开(公告)日：2000-11-09
申请号：CA2371629
申请日：2000-05-01
申请人： LIGAND PHARM INC , AMERICAN HOME PROD
发明人： EDWARDS JAMES P , ULLRICH JOHN W , ZHI LIN , JONES TODD K , TEGLEY CHRISTOPHER M , WROBEL JAY E , FENSOME ANDREW
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 , A61K31/4439 , A61P5/36 , C07D407/04
摘要： A compound of formula (I) and pharmaceutical compositions thereof useful as progesterone receptor antagonist wherein: R1 and R2 are H, OH, OAc, alkylary l, alkylheteroaryl, 1-propynyl, optionally substituted alkyl, O(alkyl), aryl, heteroaryl; or R1 and R2 are joined to form a ring, a double bond to CMe2; C(cycloalkyl), O, C(cycloether); R3 = H, OH, NH2, CORA, or optionally substituted alkenyl or alkynyl; RA = H, optionally substituted alkyl, alkoxy , aminoalkyl; R4 = H, halo, CN, NH2, optionally substituted alkyl, alkoxy, or aminoalkyl; R5 = optionally substituted phenyl, a 5- or 6-membered heterocycle; a 4- or 7-substituted indole or a substituted benzothiophene.

45. 发明专利

SG114650A1 CYCLOCARBAMATE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS 未知
公开(公告)号：SG114650A1
公开(公告)日：2005-09-28
申请号：SG200400080
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC
发明人： ZHANG PUWEN , EUGENE A TEREFENKO , HORACE FLETCHER , ANDREW FENSOME , JAY E WROBEL , ZHI LIN , TODD K JONES , CHRISTOPHER M TEGLEY
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： 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.

46. 发明专利

EA004511B1 ЦИКЛОТИОКАРБАМАТНЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ РЕЦЕПТОРА ПРОГЕСТЕРОНА 未知
公开(公告)号：EA004511B1
公开(公告)日：2004-04-29
申请号：EA200101181
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC
发明人： ZHANG PUWEN , FENSOME ANDREW , TEREFENKO EUGENE A , ZHI LIN , JONES TODD K , TEGLEY CHRISTOPHER M , EDWARDS JAMES P , COLLINS MARK A , WROBEL JAY E
IPC分类号： A61K31/535 , A61K31/5355 , A61P15/00 , A61P15/18 , A61P35/00 , A61P43/00 , C07D265/18 , C07D413/04 , A61K31/536
摘要： Изобретениеотноситсяк соединениямформулыгде Rи Rпредставляютсобойнезависимыезаместители, выбранныеизгруппы, состоящейизН, C-Cалкила, замещенного C-Cалкила, C-Cалкенила, замещенного C-Cалкенила, C-Cалкинила, замещенного C-Cалкинила, C-Cциклоалкила, замещенного C-Cциклоалкила, арила, замещенногоарила, гетероциклила, замещенногогетероциклила, CORи NRCOR, или Rи Rсконденсированыс образованиемнасыщенногоилиненасыщенного 3-8-членногоспироциклическогокольца, необязательносодержащегов своемскелетеотодногодотрехгетероатомов, выбранныхизгруппы, включающейО, S и N, причемкаждоекольцоможетбытьнеобязательнозамещено 1-3 заместителями, выбраннымиизгруппы, состоящейизН и C-Cалкила; Rвыбираютизгруппы, состоящейизН, C-Cалкила, замещенного C-Cалкила, арила, замещенногоарила, C-Cалкокси, замещенного C-Cалкокси, амино, C-Cаминоалкилаи замещенного C-Cаминоалкила; RпредставляетсобойН, C-Cалкилилизамещенный C-Cалкил; RпредставляетсобойН, ОН, NH, C-Cалкил, замещенный C-Cалкил, C-Cалкенил, замещенный C-Cалкенил, алкинил, замещенныйалкинилили COR; Rвыбираютизгруппы, состоящейизН, C-Cалкила, замещенного C-Cалкила, арила, замещенногоарила, C-Cалкокси, замещенного C-Cалкокси, C-Cаминоалкилаилизамещенного C-Cаминоалкила; Rвыбираютизгруппы, состоящейизН, галогена, CN, NO, C-Cалкила, замещенного C-Cалкила, C-Cалкокси, замещенного C-Cалкокси, C-Cаминоалкилаи замещенного C-Cаминоалкила; Rпредставляетсобойзамещенноебензольноекольцо, содержащеезаместители X, Y и Z, определенныев формулеизобретения, илипяти- илишестичленноегетероциклическоекольцос 1, 2 или 3 гетероатомамив кольце, выбраннымиизгруппы, состоящейизО, S, S(O), S(O) и NR, исодержащееодинилидванезависимыхзаместителя, определенныхв формулеизобретения; Rотсутствуетили

47. 发明专利

PL351407A1 THIO-OXINDOLE DERIVATIVES 未知
公开(公告)号：PL351407A1
公开(公告)日：2003-04-22
申请号：PL35140700
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC
发明人： FENSOME ANDREW , ZHANG PUWEN , KOKO MARCI C , ZHI LIN , JONES TODD K , MARSCHKE KEITH B , TEGLEY CHRISTOPHER M
IPC分类号： C07D409/10 , A61K31/404 , A61P1/00 , A61P5/34 , A61P7/00 , A61P7/04 , A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00 , C07D209/08 , C07D209/30 , C07D209/40 , C07D209/96 , A61P5/36
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.

48. 发明专利

SK15912001A3 CYCLOCARBAMATE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS 未知
公开(公告)号：SK15912001A3
公开(公告)日：2002-06-04
申请号：SK15912001
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 , EDWARDS JAMES P , TEGLEY CHRISTOPHER M
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： 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.

49. 发明专利

TR200103288T2 未知
公开(公告)号：TR200103288T2
公开(公告)日：2002-04-22
申请号：TR200103288
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC
发明人： FENSOME ADREW , ZHANG PUWEN , KOKO MARCI C , WROBEL JAY E , MELENSKI EDWARD G , ZHI LIN , JONES TODD K , TEGLEY CHRISTOPHER M , EDWARDS JAMES P
IPC分类号： C07D409/10 , A61K31/404 , A61P1/00 , A61P5/34 , A61P7/00 , A61P7/04 , A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00 , C07D209/08 , C07D209/30 , C07D209/40 , C07D209/96 , A61P5/36
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.

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