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公开(公告)号:US5773646A
公开(公告)日:1998-06-30
申请号:US825086
申请日:1997-03-27
申请人: Nizal Chandrakumar , Barbara B. Chen , Helen Y. Chen , Michael Clare , Alan F. Gasiecki , Richard A. Haack , James W. Malecha , Peter G. Ruminski , Mark A. Russell
发明人: Nizal Chandrakumar , Barbara B. Chen , Helen Y. Chen , Michael Clare , Alan F. Gasiecki , Richard A. Haack , James W. Malecha , Peter G. Ruminski , Mark A. Russell
IPC分类号: A61K31/00 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/216 , A61K31/415 , A61K31/4164 , A61K31/4168 , A61K31/4184 , A61K31/496 , A61K31/505 , A61P1/00 , A61P1/02 , A61P19/00 , A61P19/08 , A61P19/10 , A61P27/00 , A61P27/02 , A61P35/00 , A61P43/00 , C07C45/67 , C07C49/796 , C07C205/35 , C07C205/45 , C07C205/56 , C07C205/57 , C07C257/16 , C07C257/18 , C07C259/18 , C07C275/42 , C07C279/18 , C07C279/24 , C07C279/28 , C07C311/46 , C07C311/47 , C07C317/42 , C07C317/44 , C07C323/44 , C07C323/56 , C07C335/16 , C07C335/22 , C07C335/32 , C07D223/06 , C07D233/50 , C07D233/88 , C07D235/30 , C07D239/14 , C07D311/18 , C07D311/20 , C07D405/12 , C07C241/00 , C07C205/00 , C07C229/00 , C07C321/00
CPC分类号: C07C45/673 , C07C205/35 , C07C205/45 , C07C205/56 , C07C205/57 , C07C257/16 , C07C259/18 , C07C275/42 , C07C279/18 , C07C279/24 , C07C279/28 , C07C311/46 , C07C311/47 , C07C317/42 , C07C323/44 , C07C335/16 , C07C335/22 , C07C335/32 , C07C49/796 , C07D223/06 , C07D233/50 , C07D233/88 , C07D235/30 , C07D239/14 , C07D311/18 , C07D311/20 , C07D405/12
摘要: The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.
摘要翻译: 本发明涉及一类由式I表示的化合物或其药学上可接受的盐,包含式I化合物的药物组合物和选择性抑制或拮抗αvβ3整联蛋白的方法。
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公开(公告)号:US06251944B1
公开(公告)日:2001-06-26
申请号:US09288742
申请日:1999-04-08
申请人: Barbara B. Chen , Helen Y. Chen , Glen J. Gesicki , Richard A. Haack , James W. Malecha , Thomas D. Penning , Joseph G. Rico , Thomas E. Rogers , Peter G. Ruminski , Mark A. Russell , Stella S. Yu
发明人: Barbara B. Chen , Helen Y. Chen , Glen J. Gesicki , Richard A. Haack , James W. Malecha , Thomas D. Penning , Joseph G. Rico , Thomas E. Rogers , Peter G. Ruminski , Mark A. Russell , Stella S. Yu
IPC分类号: A61K3119
CPC分类号: C07D271/07 , A61K31/155 , C07C275/42 , C07C279/18 , C07C279/22 , C07C279/24 , C07C279/28 , C07C311/06 , C07C311/13 , C07C311/19 , C07C311/64 , C07C317/44 , C07C323/52 , C07D223/12 , C07D231/12 , C07D233/50 , C07D233/56 , C07D233/88 , C07D239/14 , C07D249/08 , C07D249/14 , C07D295/215
摘要: The present invention relates to a class of compounds represented by Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 integrin.
摘要翻译: 本发明涉及一类由式I表示的化合物或其药学上可接受的盐,包含式I化合物的药物组合物,以及选择性抑制或拮抗α-角蛋白3整联蛋白的方法。
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公开(公告)号:US5952381A
公开(公告)日:1999-09-14
申请号:US826244
申请日:1997-03-27
申请人: Barbara B. Chen , Helen Y. Chen , Glen J. Gesicki , Richard A. Haack , James W. Malecha , Thomas D. Penning , Joseph G. Rico , Thomas E. Rogers , Peter G. Ruminski , Mark A. Russell , Stella S. Yu
发明人: Barbara B. Chen , Helen Y. Chen , Glen J. Gesicki , Richard A. Haack , James W. Malecha , Thomas D. Penning , Joseph G. Rico , Thomas E. Rogers , Peter G. Ruminski , Mark A. Russell , Stella S. Yu
IPC分类号: A61K31/155 , A61K31/166 , A61K31/17 , A61K31/18 , A61K31/216 , A61K31/4168 , A61K31/4192 , A61K31/4453 , A61K31/505 , A61K31/5375 , A61P9/14 , A61P19/08 , A61P19/10 , A61P27/02 , A61P35/00 , C07C257/18 , C07C259/18 , C07C275/42 , C07C279/18 , C07C279/22 , C07C279/24 , C07C279/28 , C07C311/06 , C07C311/13 , C07C311/19 , C07C311/47 , C07C311/64 , C07C317/44 , C07C323/52 , C07D223/12 , C07D233/50 , C07D233/88 , C07D239/14 , C07D249/14 , C07D271/06 , C07D271/07 , C07D295/20 , C07D295/215 , C07D521/00 , C07C229/00 , A61K31/19 , C07C205/00
CPC分类号: C07D271/07 , A61K31/155 , C07C275/42 , C07C279/18 , C07C279/22 , C07C279/24 , C07C279/28 , C07C311/06 , C07C311/13 , C07C311/19 , C07C311/64 , C07C317/44 , C07C323/52 , C07D223/12 , C07D231/12 , C07D233/50 , C07D233/56 , C07D233/88 , C07D239/14 , C07D249/08 , C07D249/14 , C07D295/215
摘要: The present invention relates to a class of compounds represented by Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.
摘要翻译: 本发明涉及一类由式I表示的化合物或其药学上可接受的盐,包含式I化合物的药物组合物和选择性抑制或拮抗αvβ3整联蛋白的方法。
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公开(公告)号:US5585492A
公开(公告)日:1996-12-17
申请号:US321183
申请日:1994-10-11
申请人: Nizal S. Chandrakumar , Barbara B. Chen , Michael Clare , Bipinchandra N. Desai , Stevan W. Djuric , Stephen H. Docter , Alan F. Gasiecki , Richard A. Haack , Chi-Dean Liang , Julie M. Miyashiro , Thomas D. Penning , Mark A,. Russell , Stella S. Yu
发明人: Nizal S. Chandrakumar , Barbara B. Chen , Michael Clare , Bipinchandra N. Desai , Stevan W. Djuric , Stephen H. Docter , Alan F. Gasiecki , Richard A. Haack , Chi-Dean Liang , Julie M. Miyashiro , Thomas D. Penning , Mark A,. Russell , Stella S. Yu
IPC分类号: C07D295/08 , A61K31/09 , A61K31/135 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/27 , A61K31/336 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/425 , A61K31/426 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61K31/46 , A61K31/495 , A61K31/535 , A61K31/55 , A61K31/695 , A61P17/00 , A61P29/00 , A61P43/00 , C07C217/16 , C07C217/18 , C07C229/08 , C07C229/12 , C07C237/06 , C07C271/44 , C07D207/06 , C07D207/08 , C07D207/12 , C07D207/16 , C07D209/12 , C07D209/52 , C07D211/34 , C07D211/58 , C07D211/60 , C07D211/62 , C07D211/74 , C07D213/30 , C07D213/55 , C07D213/56 , C07D213/61 , C07D213/69 , C07D213/73 , C07D213/74 , C07D213/75 , C07D215/12 , C07D223/02 , C07D225/02 , C07D235/08 , C07D277/20 , C07D277/24 , C07D277/34 , C07D295/092 , C07D295/12 , C07D295/14 , C07D295/18 , C07D295/185 , C07D295/215 , C07D295/22 , C07D295/26 , C07D303/02 , C07D307/42 , C07D307/81 , C07D311/58 , C07D317/54 , C07D333/16 , C07D333/32 , C07D401/04 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D417/12 , C07D451/02 , C07D471/04 , C07D471/08 , C07D473/00 , C07D473/28 , C07D491/048 , C07D491/107 , C07D207/10 , C07D207/14
CPC分类号: C07D295/185 , C07C217/16 , C07C229/12 , C07C237/06 , C07D277/24 , C07D295/088 , C07D295/215 , C07D295/26
摘要: The present invention provides compounds of the formula Ar.sup.1 --Q--Ar.sup.2 --Y--R--Z and pharmaceutically acceptable salts thereof wherein Ar.sup.1 and Ar.sup.2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD and asthma.
摘要翻译: 本发明提供式Ar1-Q-Ar2-YRZ的化合物及其药学上可接受的盐,其中Ar1和Ar2是任选取代的芳基部分,Z是任选取代的含氮部分,其可以是无环的,环状的或双环的胺,或 任选取代的单环或双环含氮杂芳基部分; Q是能够连接两个芳基的连接基团; R是亚烷基部分; Y是能够将芳基连接到亚烷基部分并且其中Z通过氮原子与R键合的连接部分。 本发明的化合物和药物组合物可用于治疗由LTB4产生介导的炎性疾病,例如牛皮癣,溃疡性结肠炎,IBD和哮喘。
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公开(公告)号:US5508309A
公开(公告)日:1996-04-16
申请号:US271381
申请日:1994-07-01
IPC分类号: C07C43/215 , C07C63/64 , C07C63/66 , C07C65/32 , C07C65/34 , C07C65/38 , C07C65/40 , C07D213/79 , C07D257/04 , C07D307/68 , C07D333/38 , C07F7/08 , A61K31/19 , A61K31/235 , A61K31/215
CPC分类号: C07F7/0818 , C07C43/215 , C07C63/64 , C07C63/66 , C07C65/32 , C07C65/34 , C07C65/38 , C07C65/40 , C07D213/79 , C07D257/04 , C07D307/68 , C07D333/38
摘要: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, --CH.dbd.CH--, or --CH.dbd.N--;wherein R.sup.1 is --CO.sub.2 R.sup.2 or tetrazole;wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbons or a pharmaceutically acceptable cation;wherein R is an alkyl of from 1 to 20 carbons, --(CH.sub.2).sub.p CF.sub.3 or --(CH.sub.2).sub.q R.sup.3 wherein R.sup.3 is alkoxy, phenoxy or alkoxy substituted phenoxy wherein the alkoxy group has from 1 to 8 carbons;wherein p and q are integers from 0 to 20;wherein n is 0 or 1; andwherein m is 0, 1, 2, or 3.
摘要翻译: 本发明涉及下式的化合物或其药学上可接受的盐,其中X是氧,硫,-CH = CH-或-CH = N-; 其中R 1是-CO 2 R 2或四唑; 其中R2是氢,1至6个碳的烷基或药学上可接受的阳离子; 其中R是1至20个碳的烷基, - (CH 2)p CF 3或 - (CH 2)q R 3,其中R 3是烷氧基,苯氧基或烷氧基取代的苯氧基,其中烷氧基具有1至8个碳; 其中p和q为0至20的整数; 其中n为0或1; 并且其中m为0,1,2或3。
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公开(公告)号:US4791133A
公开(公告)日:1988-12-13
申请号:US67526
申请日:1987-06-26
IPC分类号: C07C59/48 , C07D307/54 , C07D309/30 , C07D333/24 , A61K31/38 , A61K31/34 , C07C69/76 , C07C103/26 , C07D211/08 , C07D333/22 , C07D409/00
CPC分类号: C07D309/30 , C07C59/48 , C07D307/54 , C07D333/24
摘要: This invention relates to leukotriene B.sub.4 antagonists having the structure ##STR1## and the pharmaceutically acceptable addition salts thereof; wherein R.sup.1 is lower alkyl having 1-10 carbon atoms; or lower alkenyl or alkynyl having 2-10 carbon atoms; or lower alkadienyl having 3-10 carbon atoms; or lower alkadiynyl or alkenynyl having 4-10 carbon atoms;wherein R.sup.2 and R.sup.3 are the same or different and represent hydrogen or lower alkyl having 1-6 carbon atoms;wherein X is CH.dbd.CH, S, or O;wherein Y is CH.dbd.CH or C.tbd.C;wherein Z is OR.sup.4 or NR.sup.5 R.sup.6, and wherein R.sup.4 represent H, lower alkyl having 1-6 carbon atoms, or a pharmaceutically acceptable cation, and wherein R.sup.5 and R.sup.6 act independently and represent H or lower alkyl having 1-6 carbon atoms, or R.sup.5 and R.sup.6 may act together with N to form a cycloamine of the formula: ##STR2## wherein q is an integer from 2-5; wherein m and n are the same or different and either 1 or 0; andwherein p is an integer from 1 to 5.
摘要翻译: 本发明涉及具有以下结构的白细胞三烯B4拮抗剂及其药学上可接受的加成盐; 其中R1是具有1-10个碳原子的低级烷基; 或具有2-10个碳原子的低级烯基或炔基; 或具有3-10个碳原子的低级链二烯基; 或具有4-10个碳原子的低级炔二炔基或烯炔基; 其中R2和R3相同或不同并且表示氢或具有1-6个碳原子的低级烷基; 其中X为CH = CH,S或O; 其中Y为CH = CH或C 3BOND C; 其中Z是OR 4或NR 5 R 6,并且其中R 4表示H,具有1-6个碳原子的低级烷基或药学上可接受的阳离子,并且其中R5和R6独立地表示H代表具有1-6个碳原子的低级烷基或R5 并且R6可以与N一起起作用以形成下式的环胺:其中q是2-5的整数; 其中m和n相同或不同,为1或0; 并且其中p为1至5的整数。
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公开(公告)号:US4970234A
公开(公告)日:1990-11-13
申请号:US390579
申请日:1989-08-07
申请人: Stevan W. Djuric , Richard A. Haack , Stella S. Yu
发明人: Stevan W. Djuric , Richard A. Haack , Stella S. Yu
IPC分类号: C07C57/60 , C07C57/66 , C07C57/68 , C07C59/48 , C07C59/64 , C07C59/88 , C07C59/90 , C07D307/87 , C07D333/16 , C07D333/22 , C07D333/28 , C07F7/08 , C07F7/22
CPC分类号: C07D307/87 , C07C57/60 , C07C57/66 , C07C57/68 , C07C59/48 , C07C59/64 , C07C59/88 , C07C59/90 , C07D333/16 , C07D333/22 , C07D333/28 , C07F7/0818 , C07F7/2212
摘要: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, or --CH.dbd.CH--;wherein Z is OR.sup.1 or --NR.sup.4 R.sup.5 ;wherein R.sup.1 is hydrogen, lower alkyl, or a pharmaceutically acceptable cation;wherein R.sup.2 is H, --CH.sub.3 or --C.sub.2 H.sub.5 ;wherein R.sup.3 is OH, H or --O;wherein R.sup.4 and R.sup.5 may independently be hydrogen, or lower alkyl having 1-6 carbon atoms, or R.sup.4 and R.sup.5 may act together with N to form a cyclic amide of the formula: ##STR2## wherein n is an integer from 4-5; and m is an integer from 0-4. More particularly, this invention relates to compounds of the above formula which have utility as LTB.sub.4 antagonists.
摘要翻译: 本发明涉及下式的化合物或其药学上可接受的盐,其中X是氧,硫或-CH = CH-; 其中Z是OR 1或-NR 4 R 5; 其中R1是氢,低级烷基或药学上可接受的阳离子; 其中R2是H,-CH3或-C2H5; 其中R3是OH,H或-O; 其中R 4和R 5可以独立地是氢或具有1-6个碳原子的低级烷基,或者R 4和R 5可以与N一起起作用以形成下式的环酰胺:其中n是4-5的整数; m为0-4的整数。 更具体地说,本发明涉及可用作LTB4拮抗剂的上式化合物。
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公开(公告)号:US5356919A
公开(公告)日:1994-10-18
申请号:US707522
申请日:1991-05-30
IPC分类号: C07C43/215 , C07C63/64 , C07C63/66 , C07C65/32 , C07C65/34 , C07C65/38 , C07C65/40 , C07D213/79 , C07D257/04 , C07D307/68 , C07D333/38 , C07F7/08 , A61K31/41
CPC分类号: C07F7/0818 , C07C43/215 , C07C63/64 , C07C63/66 , C07C65/32 , C07C65/34 , C07C65/38 , C07C65/40 , C07D213/79 , C07D257/04 , C07D307/68 , C07D333/38
摘要: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, --CH.dbd.CH--, or --CH.dbd.N--; wherein R.sup.1 is --CO.sub.2 R.sup.2 or tetrazole; wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbons or a pharmaceutically acceptable cation; wherein R is an alkyl of from 1 to 20 carbons, --(CH.sub.2).sub.p CF.sub.3 or --(CH.sub.2).sub.q R.sup.3 wherein R.sup.3 is alkoxy, phenoxy or alkoxy substituted phenoxy wherein the alkoxy group has from 1 to 8 carbons; wherein p and q are integers from 0 to 20; wherein n is 0 or 1; and wherein m is 0, 1, 2, or 3.
摘要翻译: 本发明涉及下式的化合物或其药学上可接受的盐,其中X是氧,硫,-CH = CH-或-CH = N-; 其中R 1是-CO 2 R 2或四唑; 其中R2是氢,1至6个碳的烷基或药学上可接受的阳离子; 其中R是1至20个碳的烷基, - (CH 2)p CF 3或 - (CH 2)q R 3,其中R 3是烷氧基,苯氧基或烷氧基取代的苯氧基,其中烷氧基具有1至8个碳; 其中p和q为0至20的整数; 其中n为0或1; 并且其中m为0,1,2或3。
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公开(公告)号:US5179123A
公开(公告)日:1993-01-12
申请号:US787273
申请日:1991-11-04
IPC分类号: C07C59/70 , C07C59/74 , C07C65/19 , C07C65/30 , C07C65/38 , C07C311/51 , C07D213/79 , C07D257/04 , C07D307/68 , C07D333/38
CPC分类号: C07D213/79 , C07C311/51 , C07C59/70 , C07C59/74 , C07C65/19 , C07C65/30 , C07C65/38 , C07D257/04 , C07D307/68 , C07D333/38
摘要: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxgen, sulfur, --CH.dbd.CH--or --CH.dbd.N--; wherein R.sub.1 is alkyl, alkenyl or alkynyl of about 1 to 20 carbon atoms; wherein R is --CO.sub.2 R.sup.2, tetrazole, methylsulfonamide or benzenesulfonamide, wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbon atoms or a pharmaceutically acceptable cation and R.sup.3 is hydroxyl or halogen, having utility as LTB.sub.4 synthesis inhibitors.
摘要翻译: 本发明涉及下式的化合物或其药学上可接受的盐,其中X是氧,硫,-CH = CH-或-CH = N-; 其中R1是约1-20个碳原子的烷基,烯基或炔基; 其中R为-CO 2 R 2,四唑,甲基磺酰胺或苯磺酰胺,其中R 2为氢,1至6个碳原子的烷基或药学上可接受的阳离子,R 3为羟基或卤素,可用作LTB4合成抑制剂。
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公开(公告)号:US5086067A
公开(公告)日:1992-02-04
申请号:US452138
申请日:1989-12-18
IPC分类号: A61K31/18 , A61K31/19 , A61K31/235 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P1/04 , A61P29/00 , A61P43/00 , C07C59/70 , C07C59/74 , C07C65/19 , C07C65/30 , C07C65/32 , C07C65/38 , C07C69/712 , C07C69/76 , C07C311/51 , C07D213/76 , C07D213/79 , C07D257/04 , C07D307/66 , C07D307/68 , C07D333/34 , C07D333/38 , C07D401/04 , C07D405/04 , C07D409/04
CPC分类号: C07D213/79 , C07C311/51 , C07C59/70 , C07C59/74 , C07C65/19 , C07C65/30 , C07C65/38 , C07D257/04 , C07D307/68 , C07D333/38
摘要: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, --CH.dbd.CH-- or --CH.dbd.N--; wherein R.sub.1 is alkyl, alkenyl or alkynyl of about 1 to 20 carbon atoms; wherein R is --CO.sub.2 R.sup.2, tetrazole, methylsulfonamide or benzenesulfonamide, wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbon atoms or a pharmaceutically acceptable cation and R.sup.3 is hydroxyl or halogen, having utility as LTB.sub.4 synthesis inhibitors.
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