公开(公告)号：US5773420A

公开(公告)日：1998-06-30

申请号：US531142

申请日：1995-10-20

申请人： Thomas T. Nguyen ,  John W. Ellingboe

发明人： Thomas T. Nguyen ,  John W. Ellingboe

IPC分类号： C07H15/203 ,  A61K31/70 ,  C07H17/00

CPC分类号： C07H15/203

摘要： This invention relates to acylated benzylglycosides and a method for their use as smooth muscle cell proliferation inhibitors and as therapeutic compositions for treating diseases and conditions which are characterize by excessive smooth muscle proliferation, such as restenosis. The acylated benzylglycosides of this invention are those of formula I, below: ##STR1## wherein X is ##STR2## R.sup.1 is H, alkyl having 1 to 6 carbon atoms, chloro, bromo, or alkoxy having 1 to 6 carbon atoms; R.sup.2 is H, an acyl group having 1 to 6 carbon atoms, phenylsulfonyl, or substituted phenylsulfonyl; and R.sup.3 is an acyl group having 1 to 8 carbon atoms, benzoyl, substituted benzoyl, alkylsulfonyl having 1 to 6 carbon atoms, phenylsulfonyl, or substituted phenylsulfonyl; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are each, independently, an acyl group having 1 to 6 carbon atoms; and R.sup.10 and R.sup.11 are each, independently, an acyl group having 1 to 6 carbon atoms, or the R.sup.10 and R.sup.11 groups on the 4' and 6' positions of the maltose or the 4 and 6 positions of the glucose form an isopropylidene group; or pharmaceutically acceptable salts thereof. R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are each, independently, an acyl group having 1 to 6 carbon atoms; and R.sup.10 and R.sup.11 are each, independently, an acyl group having 1 to 6 carbon atoms, or the R.sup.10 and R.sup.11 groups on the 4' and 6' positions of the maltose or the 4 and 6 positions of the glucose form an isopropylidene group; or a pharmaceutically acceptable salt thereof a pharmaceutically acceptable agent.

摘要翻译： 本发明涉及酰化苄基鹅糖苷及其作为平滑肌细胞增殖抑制剂和作为用于治疗以过度平滑肌增生为特征的疾病和病症如再狭窄的治疗组合物的方法。 本发明的酰化苄基鹅糖苷是下式I的化合物：其中X是R或R 1是H，具有1-6个碳原子的烷基，氯，溴或具有1-6个碳原子的烷氧基 碳原子 R2是H，具有1-6个碳原子的酰基，苯基磺酰基或取代的苯基磺酰基; 并且R 3是具有1至8个碳原子的酰基，苯甲酰基，取代的苯甲酰基，具有1至6个碳原子的烷基磺酰基，苯基磺酰基或取代的苯基磺酰基; R4，R5，R6，R7，R8和R9各自独立地为具有1至6个碳原子的酰基; R10和R11各自独立地为具有1至6个碳原子的酰基，或麦芽糖4'和6'位上的R 10和R 11基团或葡萄糖的4和6位形成异丙叉基; 或其药学上可接受的盐。 R4，R5，R6，R7，R8和R9各自独立地为具有1至6个碳原子的酰基; R10和R11各自独立地为具有1至6个碳原子的酰基，或麦芽糖4'和6'位上的R 10和R 11基团或葡萄糖的4和6位形成异丙叉基; 或其药学上可接受的盐是药学上可接受的试剂。

公开(公告)号：US5498775A

公开(公告)日：1996-03-12

申请号：US335278

申请日：1994-11-07

申请人： Sarah T. A. Novak ,  Richard M. Soll ,  John W. Ellingboe ,  Thomas T. Nguyen

发明人： Sarah T. A. Novak ,  Richard M. Soll ,  John W. Ellingboe ,  Thomas T. Nguyen

IPC分类号： C07H15/18 ,  A61K31/70 ,  A61K31/7028 ,  A61P9/00 ,  A61P43/00 ,  C07H15/22 ,  C07H15/00

CPC分类号： C07H15/22

摘要： This invention relates to the use of polyanionic benzylglycosides as smooth muscle cell proliferation inhibitors and as therapeutic compositions for treating diseases and conditions which are characterized by excessive smooth muscle proliferation, such as restenosis. The compounds of this invention are those of formula I ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are, independently, H, SO.sub.3 M, or ##STR2## and each oligosaccharide group contains 1 to 3 sugar groups; M is lithium, sodium, potassium, or ammonium;n is 1 or 2;X is a halogen, lower alkyl having 1 to 6 carbon atoms, or lower alkoxy having 1 to 6 carbon atoms;Y is carbonyl or sulfonyl;Z is alkyl from 1 to 12 carbon atoms, ##STR3## and X is as defined above; or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及聚阴离子苄基糖苷类作为平滑肌细胞增殖抑制剂的用途，以及用于治疗以过度平滑肌增生为特征的疾病和病症如再狭窄的治疗组合物。 本发明的化合物是式I的化合物，其中R 1，R 2，R 3和R 4各自独立地是H，SO 3 M或者每个寡糖基团含有1至3个糖基团 ; M是锂，钠，钾或铵; n为1或2; X是卤素，具有1至6个碳原子的低级烷基或具有1至6个碳原子的低级烷氧基; Y是羰基或磺酰基; Z是1至12个碳原子的烷基，X如上定义; 或其药学上可接受的盐。

公开(公告)号：US06503917B1

公开(公告)日：2003-01-07

申请号：US09703508

申请日：2000-11-01

申请人： Chingfan Chiu ,  Zhilian Tang ,  John W. Ellingboe

发明人： Chingfan Chiu ,  Zhilian Tang ,  John W. Ellingboe

IPC分类号： C07D21324

CPC分类号： C07D213/30 ,  C07D405/04 ,  C07D409/14

摘要： The present invention relates to novel substituted pyridine compounds of Formula (I) wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.

摘要翻译： 本发明涉及式（I）的新型取代的吡啶化合物，其中Z，R1，R2和R3如本文所定义，具有雌激素活性，其制备方法，组合文库和制备文库的固相方法 的化合物，利用用于药物发现的化合物的文库，治疗方法及其药物组合物。

公开(公告)号：US5451583A

公开(公告)日：1995-09-19

申请号：US353428

申请日：1994-12-09

申请人： John W. Ellingboe

发明人： John W. Ellingboe

IPC分类号： C07D235/08 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  A61K31/415 ,  C07D235/06

CPC分类号： C07D401/10 ,  C07D235/08 ,  C07D401/14 ,  C07D403/10

摘要： There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are defined in the specification; n is 1 to 3;Y is ##STR2## wherein R.sup.3 is hydrogen, perfluoro alkyl of 1-6 carbon atoms, trifluoromethylalkyl of 1-6 carbon atoms, or alkyl of 1-6 carbon atoms; and R.sup.4 is hydrogen or alkyl of 1-6 carbon atoms;with the proviso that when R.sup.1 is ##STR3## then R.sup.2 cannot be ##STR4## wherein X is as defined above; and the pharmaceutically acceptable salts thereof, which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension and congestive heart-failure.

摘要翻译： 公开了式（I）的化合物，其中R1和R2在说明书中定义; n为1〜3; Y为，其中R 3为氢，1-6个碳原子的全氟烷基，1-6个碳原子的三氟甲基烷基或1-6个碳原子的烷基; R4为氢或1-6个碳原子的烷基; 条件是当R1是时，则R2不能是，其中X如上所定义; 及其药学上可接受的盐，其由于其拮抗血管紧张素II的能力可用于治疗高血压和充血性心力衰竭。

公开(公告)号：US5283242A

公开(公告)日：1994-02-01

申请号：US975198

申请日：1992-11-12

申请人： John W. Ellingboe

发明人： John W. Ellingboe

IPC分类号： C07D235/08 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D241/04 ,  A61K31/495 ,  A61K31/50 ,  C07D239/94

CPC分类号： C07D401/10 ,  C07D235/08 ,  C07D401/14 ,  C07D403/10

摘要： There are disclosed compounds of the formula ##STR1## wherein R.sup.1 is ##STR2## R.sup.2 is ##STR3## wherein X is ##STR4## wherein R.sup.5 is hydrogen, alkyl of 1-6 carbon atoms, benzyl, triphenylmethyl, or Sn(alkyl of 1-6 carbon atoms).sub.3 ;n is 1 to 3;Y is ##STR5## wherein R.sup.3 is hydrogen, perfluoro alkyl of 1-6 carbon atoms, trifluoromethylalkyl of 1-6 carbon atoms, or alkyl of 1-6 carbon atoms; and R.sup.4 is hydrogen or alkyl of 1-6 carbon atoms;with the proviso that when R.sup.1 is ##STR6## then R.sup.2 cannot be ##STR7## wherein X is as defined above; and the pharmaceutically acceptable salts thereof, which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension and congestive heart-failure.

摘要翻译： 公开了下式的化合物，其中R 1是其中X是H，其中R 5是氢，1-6个碳原子的烷基，苄基，三苯基甲基， 或Sn（1-6个碳原子的烷基）3; n为1〜3; Y为，其中R 3为氢，1-6个碳原子的全氟烷基，1-6个碳原子的三氟甲基烷基或1-6个碳原子的烷基; R4为氢或1-6个碳原子的烷基; 条件是当R1是时，则R2不能是，其中X如上所定义; 及其药学上可接受的盐，其由于其拮抗血管紧张素II的能力可用于治疗高血压和充血性心力衰竭。

公开(公告)号：US4895860A

公开(公告)日：1990-01-23

申请号：US341514

申请日：1989-04-21

申请人： Thomas R. Alessi ,  John W. Ellingboe

发明人： Thomas R. Alessi ,  John W. Ellingboe

IPC分类号： C07D291/04 ,  C07D419/06

CPC分类号： C07D291/04 ,  C07D419/06

摘要： This invention relates to novel substituted 3H-1,2,3,5-oxathiadiazole 2-oxides, to the processes for their preparation, to methods for using the compounds, and to pharmaceutical compositions thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.

摘要翻译： 本发明涉及新的取代的3H-1,2,3,5-氧硫杂二唑2-氧化物，其制备方法，使用该化合物的方法及其药物组合物。 这些化合物具有药物性质，使其有益于治疗糖尿病和相关病症。

公开(公告)号：US06384057B1

公开(公告)日：2002-05-07

申请号：US09703386

申请日：2000-11-01

申请人： Chingfan Chiu ,  Zhilian Tang ,  John W. Ellingboe

发明人： Chingfan Chiu ,  Zhilian Tang ,  John W. Ellingboe

IPC分类号： A61K31444

CPC分类号： C07D213/30 ,  C07D405/04 ,  C07D409/14

摘要： The present invention relates to novel substituted pyridine compounds of Formula (I) wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.

摘要翻译： 本发明涉及式（I）的新型取代的吡啶化合物，其中Z，R1，R2和R3如本文所定义，具有雌激素活性，其制备方法，组合文库和制备文库的固相方法 的化合物，利用用于药物发现的化合物的文库，治疗方法及其药物组合物。

公开(公告)号：US5256654A

公开(公告)日：1993-10-26

申请号：US901485

申请日：1992-06-25

申请人： John W. Ellingboe ,  Madelene Nikaido ,  Jehan Bagli

发明人： John W. Ellingboe ,  Madelene Nikaido ,  Jehan Bagli

IPC分类号： A61K31/505 ,  C07D207/333 ,  C07D211/40 ,  C07D239/30 ,  C07D471/04 ,  C07D487/04 ,  A61K31/55

CPC分类号： C07D471/04 ,  C07D487/04

摘要： This invention relates to pyrrolo-, pyrido-, azepino-, and azocinopyrimidines of the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently H, lower alkyl containing 1 to 6 carbon atoms, or perfluoroalkyl containing 1 to 6 carbon atoms; R.sup.5 is H or when n is 1 R.sup.5 taken together with R.sup.3 comprises a double bond; n is 0 to 1; p is 0 to 2; m is 0 to 3; Ar.sup.1 is ##STR2## wherein W is H, lower alkyl containing 1 to 6 carbon atoms, halogen, hydroxy, or lower alkoxy containing 1 to 6 carbon atoms; Ar.sup.2 is ##STR3## wherein X is ##STR4## wherein R.sup.6 is H, tert-butyl, tri-n-butylstannyl, or triphenylmethyl; and the pharmaceutically acceptable salts thereof which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension, congestive heart failure, and restenosis. The compounds are also useful for reducing lipid levels in the blood plasma and are thus useful for treating hyperlipidemia and hypercholesterolemia. Also disclosed are processes for the production of said compounds and pharmaceutical compositions containing said compounds.

摘要翻译： 本发明涉及通式I的吡咯并，吡啶并，吖辛因和偶氮嘧啶，其中R 1，R 2，R 3和R 4独立地为H，含有1至6个碳原子的低级烷基或含有1个 至6个碳原子; R5为H或当n为1时，R5与R3一起包含双键; n为0至1; p为0〜2; m为0〜3; Ar1为其中W为H，含有1至6个碳原子的低级烷基，卤素，羟基或含有1至6个碳原子的低级烷氧基; Ar2是其中X是，其中R6是H，叔丁基，三正丁基甲锡烷基或三苯基甲基; 及其药学上可接受的盐由于其拮抗血管紧张素II的能力可用于治疗高血压，充血性心力衰竭和再狭窄。 所述化合物还可用于降低血浆中的脂质水平，因此可用于治疗高脂血症和高胆固醇血症。 还公开了用于生产所述化合物和含有所述化合物的药物组合物的方法。

公开(公告)号：US5149699A

公开(公告)日：1992-09-22

申请号：US782025

申请日：1991-10-24

申请人： John W. Ellingboe ,  Madelene Nikaido ,  Jehan Bagli

发明人： John W. Ellingboe ,  Madelene Nikaido ,  Jehan Bagli

IPC分类号： A61K31/519 ,  A61P9/12 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D471/04

摘要： This invention relates to pyrrolo-, pyrido-, azepino-, and azocinopyrimidines of the general formula I ##STR1## useful for treating hypertension and congestive heart failure, to pharmaceutical compositions, and to methods for production thereof.

摘要翻译： 本发明涉及可用于治疗高血压和充血性心力衰竭的通式I的吡咯并，吡啶并，氮杂嘧啶并嘧啶并嘧啶以及其制备方法。

公开(公告)号：US4906753A

公开(公告)日：1990-03-06

申请号：US221586

申请日：1988-07-20

申请人： Jehan F. Bagli ,  John W. Ellingboe ,  Thomas R. Alessi

发明人： Jehan F. Bagli ,  John W. Ellingboe ,  Thomas R. Alessi

IPC分类号： C07D239/56

CPC分类号： C07D239/56

摘要： Disclosed herein are 2,6-disubstituted-5-cyano-4-pyrimidinyloxyacetic acids and pharmaceutically acceptable salts thereof and methods of their preparation. The compounds are new aldose reductase inhibitors useful for the treatment of prevention of diabetic complications.

摘要翻译： 本文公开了2,6-二取代-5-氰基-4-嘧啶氧基乙酸及其药学上可接受的盐及其制备方法。 该化合物是用于治疗预防糖尿病并发症的新的醛糖还原酶抑制剂。