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51. 发明授权

US5527907A Macrolide immunomodulators 失效
标题翻译：大环内酯类免疫调节剂
公开(公告)号：US5527907A
公开(公告)日：1996-06-18
申请号：US327391
申请日：1994-10-26
申请人： Yat S. Or , Jay R. Luly , Rolf Wagner
发明人： Yat S. Or , Jay R. Luly , Rolf Wagner
IPC分类号： C07D498/18 , C07D491/16 , A61K31/395
CPC分类号： C07D498/18
摘要： Novel macrolide compounds of the formula ##STR1## and pharmaceutically acceptable salts, esters, amides and prodrugs thereof, processes for the preparation of the compounds of the invention, intermediates useful in these processes, a pharmaceutical composition, and a method of treating immunomodulatory disorders are disclosed.
摘要翻译：下式的新型大环内酯类化合物及其药学上可接受的盐，酯，酰胺和前药，本发明化合物的制备方法，用于这些方法的中间体，药物组合物和治疗免疫调节性疾病的方法是披露

52. 发明授权

US5508397A Activated macrolactams 失效
标题翻译：活化的大环内酰胺
公开(公告)号：US5508397A
公开(公告)日：1996-04-16
申请号：US357568
申请日：1994-12-16
申请人： Yat S. Or , Jay R. Luly
发明人： Yat S. Or , Jay R. Luly
IPC分类号： A61K31/435 , A61P37/06 , C07D498/18 , C07F7/18 , C07D498/16 , C12P17/18
CPC分类号： C07D498/18 , C07F7/1856
摘要： Activated macrolactam compounds having the formula ##STR1## wherein n is zero or one, R.sup.101 is selected from the group consisting of methyl, ethyl, allyl, propyl and cyclopropylmethyl;R.sup.102 is hydrogen, and R.sup.103 is selected from the group consisting of hydrogen, hydroxy and a protected hydroxy group or, taken together, R.sup.102 and R.sup.103 form a bond;R.sup.104 and R.sup.105 are chosen such that one is hydrogen while the other is -OS(O).sub.2 F; andR.sup.106 is selected from the group consisting of hydrogen, a protected hydroxy group, loweralkyl, alkenyl, cycloalkyl, aryl and arylalkyl,as well as processes for making such compounds and methods for their use in the preparation of C-32-modified derivatives of ascomycin or the congeners or analogs thereof.
摘要翻译：具有式“IMAGE”的活性大环内酰胺化合物，其中n为0或1，R 101选自甲基，乙基，烯丙基，丙基和环丙基甲基; R 102是氢，R 103选自氢，羟基和保护的羟基，或者R 102和R 103一起形成一个键; 选择R104和R105使得一个是氢，而另一个是-OS（O）2 F; R 106选自氢，保护的羟基，低级烷基，烯基，环烷基，芳基和芳基烷基，以及制备这些化合物的方法及其用于制备C-32修饰的衍生物的方法子囊霉素或其同系物或类似物。

53. 发明授权

US5457111A Macrocyclic immunomodulators 失效
标题翻译：大环免疫调节剂
公开(公告)号：US5457111A
公开(公告)日：1995-10-10
申请号：US149416
申请日：1993-11-09
申请人： Jay R. Luly , Megumi Kawai , Yat S. Or , Paul Wiedeman , Rolf Wagner
发明人： Jay R. Luly , Megumi Kawai , Yat S. Or , Paul Wiedeman , Rolf Wagner
IPC分类号： C07D487/14 , C07D491/20 , C07D498/04 , C07D498/14 , C07D498/18 , C07D498/22 , C07D513/14 , C07D513/18 , C07F7/18 , C07F9/6561 , C07H19/01 , A61K31/435
CPC分类号： C07D498/18 , C07D487/14 , C07D513/14 , C07F7/1856 , C07F9/6561 , C07H19/01
摘要： Immunomodulatory macrocyclic compounds having the formula ##STR1## and pharmaceutically acceptable salts, esters, amides and prodrugs thereof, wherein X is selected from one of the formulae ##STR2## as well as pharmaceutical compositions containing the same.
摘要翻译：具有下式（VII）的免疫调节大环化合物及其药学上可接受的盐，酯，酰胺和前药，其中X选自下列之一：IMAGE＆lt; IMAGE＆gt;以及含有该化合物的药物组合物。

54. 发明授权

US5386011A Hexapeptide anaphylatoxin-receptor ligands 失效
标题翻译：六肽过敏毒素受体配体
公开(公告)号：US5386011A
公开(公告)日：1995-01-31
申请号：US634641
申请日：1990-12-27
申请人： Paul E. Wiedeman , Megumi Kawai , Jay R. Luly , Yat S. Or , Rolf Wagner
发明人： Paul E. Wiedeman , Megumi Kawai , Jay R. Luly , Yat S. Or , Rolf Wagner
IPC分类号： A61K38/00 , A61P37/08 , C07K5/02 , C07K5/06 , C07K5/08 , C07K5/10 , C07K7/02 , C07K7/06 , C07K14/47 , A61K37/00 , C07K5/00 , C07K7/00 , A61K37/02
CPC分类号： C07K14/472 , A61K38/00
摘要： Oligopeptide compounds or oligopeptide analogue compounds of the formula A-B-D-E-G-J-L-M-Q are ligands for the anaphylatoxin receptor and are useful in the treatment of inflammatory disease states.Also disclosed are anaphylatoxin receptor ligand compositions and a method for modulating anaphylatoxin activity.
摘要翻译：式A-B-D-E-G-J-L-M-Q的寡肽化合物或寡肽类似物化合物是过敏毒素受体的配体，可用于治疗炎性疾病状态。还公开了过敏毒素受体配体组合物和调节过敏毒素活性的方法。

55. 发明授权

US5091575A Peptidylaminodiols 失效
标题翻译：肽基氨基二醇
公开(公告)号：US5091575A
公开(公告)日：1992-02-25
申请号：US713644
申请日：1991-06-10
申请人： Jay R. Luly , Jacob J. Plattner , Dale J. Kempf
发明人： Jay R. Luly , Jacob J. Plattner , Dale J. Kempf
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078
CPC分类号： C07K5/0227 , C07K5/06043 , C07K5/06078 , C07K5/06139 , A61K38/00
摘要： A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is C.dbd.O or CHOH; U is CH.sub.2 or NR.sup.2, provided that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, .alpha.,.alpha.-dimethylbenzyl, 1-benzyloxyethyl; phenethyl, phenoxy, thiophenoxy or anilino; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl; lowerakenyl, benzyl or heterocyclic ring substituted methyl; R.sub.4 is loweralkyl, cycloalkylmethyl or benzyl; R.sub.5 is vinyl, formyl, hydroxymethyl or hydrogen; R.sub.7 is hydrogen or loweralkyl; R.sub.8 and R.sub.9 are independently selected from OH and NH.sub.2 ; and R.sub.6 is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R.sub.5 and R.sub.7 are both hydrogen and R.sub.8 and R.sub.9 are OH, the carbon bearing R.sub.5 is of the "R" configuration and the carbon bearing R.sub.6 is of the "S" configuration; or pharmaceutically acceptable salts or esters thereof. Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.
摘要翻译：下式的肾素抑制化合物：其中A是取代基; W是C = O或CHOH; U是CH 2或NR 2，条件是当W是CHOH时，U是CH 2; R1是低级烷基，环烷基甲基，苄基，4-甲氧基苄基，卤代苄基，（1-萘基）甲基，（2-萘基）甲基，（4-咪唑基）甲基，α，α-二甲基苄基，1-苄氧基乙基; 苯乙基，苯氧基，硫代苯氧基或苯胺基; R2是氢或低级烷基; R3是低级烷基，[（烷氧基）烷氧基]烷基，（硫代烷氧基）烷基; 苄基或杂环取代的甲基; R4是低级烷基，环烷基甲基或苄基; R5是乙烯基，甲酰基，羟甲基或氢; R7是氢或低级烷基; R8和R9独立地选自OH和NH2; 和R6是氢，低级烷基，乙烯基或芳基烷基; 条件是当R 5和R 7均为氢且R 8和R 9为OH时，碳原子的R 5为“R”构型，碳原子的R 6为“S”构型; 或其药学上可接受的盐或酯。还公开了肾素抑制组合物，治疗高血压的方法，制备肾素抑制化合物的方法和可用于制备肾素抑制化合物的中间体。

56. 发明授权

US5032577A Peptidylaminodiols 失效
标题翻译：肽基氨基二醇
公开(公告)号：US5032577A
公开(公告)日：1991-07-16
申请号：US132356
申请日：1987-12-18
申请人： Anthony K. L. Fung , Dale J. Kempf , Jay R. Luly , Saul H. Rosenberg , Jacob J. Plattner
发明人： Anthony K. L. Fung , Dale J. Kempf , Jay R. Luly , Saul H. Rosenberg , Jacob J. Plattner
IPC分类号： C12N9/99 , A61K31/165 , A61K31/44 , A61K31/4406 , A61K38/00 , A61P9/12 , C07C67/00 , C07C235/06 , C07C235/08 , C07C235/10 , C07C235/34 , C07C235/74 , C07C235/78 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/00 , C07C271/20 , C07C271/24 , C07C313/00 , C07C317/44 , C07C323/60 , C07C325/00 , C07C327/20 , C07C333/02 , C07D213/00 , C07D213/71 , C07D213/78 , C07D233/54 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/08 , C07K5/083 , C07K5/097 , C07K14/81
CPC分类号： C07D233/64 , C07K5/0202 , C07K5/0227 , C07K5/06026 , C07K5/06078 , C07K5/0802 , C07K5/0806 , C07K5/0808 , C07K5/0821 , C07K5/0823 , A61K38/00
摘要： A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is C.dbd.O or CHOH; U is CH.sub.2 or NR.sub.2, provided that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, (alpha,alpha)-dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkenyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, lowerakenyl, benzyl or heterocyclic ring substituted methyl; R.sub.4 is loweralkyl, cycloalkylmethyl or benzyl; R.sub.5 is vinyl, formyl, hydroxymethyl or hydrogen; R.sub.7 is hydrogen or loweralkyl; R.sub.8 and R.sub.9 are independently selected from OH and NH.sub.2 ; and R.sub.6 is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R.sub.5 and R.sub.7 are both hydrogen and R.sub.8 and R.sub.9 are OH, the carbon bearing R.sub.5 is of the "R" configuration and the carbon bearing R.sub.6 is of the "S" configuration, or pharmaceutically acceptable salts or esters thereof. Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.
摘要翻译：下式的肾素抑制化合物：其中A是取代基; W是C = O或CHOH; U是CH 2或NR 2，条件是当W是CHOH时，U是CH 2; （1-萘基）甲基，（2-萘基）甲基，（4-咪唑基）甲基，（α，α） - 二甲基苄基，1-苄氧基乙基，苯乙基，苯氧基，噻吩氧基或苯胺基; R2是氢或低级烷基; R3是低级烯基，[（烷氧基）烷氧基]烷基，（硫代烷氧基）烷基，低级，苄基或杂环取代的甲基; R4是低级烷基，环烷基甲基或苄基; R5是乙烯基，甲酰基，羟甲基或氢; R7是氢或低级烷基; R8和R9独立地选自OH和NH2; 和R6是氢，低级烷基，乙烯基或芳基烷基; 条件是当R 5和R 7均为氢且R 8和R 9为OH时，含碳的R 5为“R”构型，并且含碳的R 6为“S”构型，或其药学上可接受的盐或酯。还公开了肾素抑制组合物，治疗高血压的方法，制备肾素抑制化合物的方法和可用于制备肾素抑制化合物的中间体。

57. 发明授权

US4977277A Functionalized peptidyl aminodiols and -triols 4-amino-5-cyclohexyl-3-hydroxy-1,2-oxopentane and derivatives thereof 失效
标题翻译：官能化肽基氨基二醇和三醇4-氨基-5-环己基-3-羟基-1,2-氧代戊烷及其衍生物
公开(公告)号：US4977277A
公开(公告)日：1990-12-11
申请号：US361522
申请日：1989-06-05
申请人： Saul H. Rosenberg , Jay R. Luly , Jacob J. Plattner
发明人： Saul H. Rosenberg , Jay R. Luly , Jacob J. Plattner
IPC分类号： A61K38/00 , C07C271/16 , C07C271/20 , C07D231/38 , C07D295/215 , C07D303/36 , C07F7/18 , C07K5/02 , C07K5/06 , C07K5/065
CPC分类号： C07D231/38 , C07C271/16 , C07C271/20 , C07D295/215 , C07D303/36 , C07F7/1856 , C07K5/0227 , C07K5/06043 , C07K5/06078 , A61K38/00 , C07C2101/14 , Y10S530/86
摘要： The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; OR.sub.8 or SR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or aminoalkyl; NR.sub.9 R.sub.10 wherein R.sub.9 and R.sub.10 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; ##STR2## wherein B is NH, alkylamino, S, O, CH.sub.2 or CHOH and R.sub.11 is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, carboxylic acid-substituted alkyl, alkoxycarbonylalkyl, aminoalkyl, N-protected aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, (N-protected)-(alkyl)aminoalkyl, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, .alpha.-methylbenzyl, .alpha., .alpha.-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)-methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R.sub.1 is phenoxy, thiophenoxy or anilino, B is CH.sub.2 or CHOH or A is hydrogen; R.sub.3 is loweralkyl, benzyl or heterocyclic ring-substituted methyl; R.sub.4 is lower-alkyl, cycloalkyl- methyl or benzyl; R.sub.2, R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl; X is O, NH or S; R.sub.7 is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl ##STR3## wherein R.sub.12 and R.sub.13 are independently hydrogen or loweralkyl, n is 0-2 and R.sub.14 is substituted or unsubstituted phenyl or heterocyclic; or XR.sub.7 together are loweralkylsulfonyl, N.sub.3 or Cl, and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及下式的肾素抑制化合物：其中A是氢; 低级烷基芳烷基 OR 8或SR 8，其中R 8是氢，低级烷基或氨基烷基; NR 9 R 10其中R 9和R 10独立地选自氢，低级烷基，氨基烷基，氰基烷基和羟烷基; 其中B是NH，烷基氨基，S，O，CH 2或CHOH，R 11是低级烷基，环烷基，芳基，芳基烷基，烷氧基，烯氧基，羟基烷氧基，二羟基烷氧基，芳基烷氧基，芳基烷氧基烷基，氨基，烷基氨基，二烷基氨基，（羟基烷基）烷基）氨基，（二羟基烷基）（烷基）氨基，羧酸取代的烷基，烷氧基羰基烷基，氨基烷基，N-保护的氨基烷基，烷基氨基烷基，二烷基氨基烷基，（N-保护的） - （烷基）氨基烷基，（杂环）烷基或取代或未取代的杂环; R1是低级烷基，环烷基甲基，苄基，α-甲基苄基，α，α-二甲基苄基，4-甲氧基苄基，卤代苄基，（1-萘基） - 甲基，（2-萘基）甲基，（4-咪唑基）甲基，苯乙基，苯氧基，噻吩氧基或苯胺基; 如果R1是苯氧基，硫代苯氧基或苯胺基，B是CH 2或CHOH或A是氢; R3是低级烷基，苄基或杂环取代的甲基; R4是低级烷基，环烷基 - 甲基或苄基; R2，R5和R6独立地是氢或低级烷基; X是O，NH或S; R 7为氢，低级烷基，烷酰基，烷基磺酰基，其中R 12和R 13独立地为氢或低级烷基，n为0-2，R 14为取代或未取代的苯基或杂环基; 或XR7一起是低级烷基磺酰基，N 3或Cl，及其药学上可接受的盐。

58. 发明授权

US4725584A Peptidyl-1-amino-2,4-diols 失效
标题翻译：肽基-1-氨基-2,4-二醇
公开(公告)号：US4725584A
公开(公告)日：1988-02-16
申请号：US830614
申请日：1986-02-19
申请人： Jay R. Luly , Jacob J. Plattner , Hing L. Sham
发明人： Jay R. Luly , Jacob J. Plattner , Hing L. Sham
IPC分类号： A61K38/00 , C07K5/065 , A61K31/65 , A61K37/43 , C07C103/20 , C07C125/06 , C07K5/06 , C07K7/02
CPC分类号： C07K5/06078 , A61K38/00 , Y02P20/55 , Y10S530/86
摘要： The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is an N-protecting group; R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are independently selected from loweralkyl or lipophilic or aromatic amino acid side chains; and R.sub.4 is hydrogen, loweralkyl, loweralkylmercapto or loweralkylsulfonyl.
摘要翻译：本发明涉及下式的肾素抑制化合物，其中A是N-保护基; R1，R2，R3和R5独立地选自低级烷基或亲油或芳族氨基酸侧链; R4是氢，低级烷基，低级烷基巯基或低级烷基磺酰基。

59. 发明授权

US4645759A Renin inhibiting compounds 失效
标题翻译：肾素抑制化合物
公开(公告)号：US4645759A
公开(公告)日：1987-02-24
申请号：US735491
申请日：1985-05-17
申请人： Jay R. Luly , John J. Plattner , Joseph F. Dellaria
发明人： Jay R. Luly , John J. Plattner , Joseph F. Dellaria
IPC分类号： A61K38/00 , C07K5/02 , C07K5/065 , A61K37/43 , C07K5/08
CPC分类号： C07K5/06078 , C07K5/0227 , A61K38/00 , Y02P20/55 , Y10S530/86
摘要： The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is an N-protecting group; n is 0 or 1; B is hydrogen, hydroxy, NH, loweralkyl or arylalkyl; with the proviso that when A is an N-protecting group, B is NH and when n is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R.sub.1, R.sub.3 and R.sub.5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R.sub.2, R.sub.4, R.sub.7, R.sub.8 and R.sub.9 are hydrogen or loweralkyl and may be the same or different; X is NH, O, S, SO or SO.sub.2 ; and R.sub.6 is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protecting group, with the proviso that R.sub.6 may be an N-protecting group when X is NH.
摘要翻译：本发明涉及下式的肾素抑制化合物，其中A是N-保护基; n为0或1; B是氢，羟基，NH，低级烷基或芳基烷基; 条件是当A是N-保护基时，B是NH，当n是0时，B是氢，羟基，低级烷基或芳基烷基; R 1，R 3和R 5是低级烷基或亲水性，亲油性或芳族氨基酸侧链，可以相同或不同; R2，R4，R7，R8和R9是氢或低级烷基，可以相同或不同; X是NH，O，S，SO或SO 2; 并且R 6为低级烷基，环烷基，环烷基烷基，芳基，芳烷基或N-保护基，条件是当X为NH时，R 6可为N-保护基。

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