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公开(公告)号:US4749698A
公开(公告)日:1988-06-07
申请号:US752695
申请日:1985-07-08
申请人: Edward S. Neiss , John T. Suh , John R. Regan , Jerry W. Skiles , Jeffrey N. Barton , James J. Mencel , Paul Menard
发明人: Edward S. Neiss , John T. Suh , John R. Regan , Jerry W. Skiles , Jeffrey N. Barton , James J. Mencel , Paul Menard
IPC分类号: A61K38/00 , C07K5/02 , C07K5/06 , C07D207/12 , A61K31/40 , A61K31/495 , A61K31/505 , A61K31/54 , C07D207/14 , C07D207/24 , C07D403/12 , C07D417/12
CPC分类号: C07K5/0222 , C07K5/06026 , C07K5/06191 , A61K38/00
摘要: Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.
摘要翻译: 具有一般结构
的化合物及其药学上可接受的盐,其中本文定义的取代基表现出抗高血压活性。 -
公开(公告)号:US4746676A
公开(公告)日:1988-05-24
申请号:US649797
申请日:1984-09-12
申请人: Edward S. Neiss , John T. Suh , John R. Regan , Jerry W. Skiles , Jeffrey N. Barton , Paul Menard
发明人: Edward S. Neiss , John T. Suh , John R. Regan , Jerry W. Skiles , Jeffrey N. Barton , Paul Menard
IPC分类号: C07D207/16 , A61K31/40 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/54 , A61K38/00 , A61K38/55 , A61P7/10 , A61P9/12 , A61P27/02 , A61P43/00 , C07D207/22 , C07D209/42 , C07D405/12 , C07D417/12 , C07K5/02 , C07K5/06 , C12N9/99 , C07D207/14
CPC分类号: C07K5/0222 , C07K5/06026 , C07K5/06191 , A61K38/00
摘要: Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.
摘要翻译: 具有一般结构
的化合物及其药学上可接受的盐,其中本文定义的取代基表现出抗高血压活性。 -
公开(公告)号:US4666906A
公开(公告)日:1987-05-19
申请号:US756530
申请日:1985-07-19
申请人: John J. Piwinski , John T. Suh , Paul Menard , Howard Jones , Edward S. Neiss , John R. Regan
发明人: John J. Piwinski , John T. Suh , Paul Menard , Howard Jones , Edward S. Neiss , John R. Regan
IPC分类号: A61K38/00 , C07K5/02 , A61K31/54 , C07D285/22
CPC分类号: C07K5/0222 , A61K38/00
摘要: Compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are as defined herein, having antihypertensive activity.
摘要翻译: 式IMA的化合物及其药学上可接受的盐,其中取代基如本文所定义,具有抗高血压活性。
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公开(公告)号:US4596791A
公开(公告)日:1986-06-24
申请号:US690387
申请日:1985-01-10
申请人: John J. Piwinski , John T. Suh , Paul Menard , Howard Jones , Edward S. Neiss
发明人: John J. Piwinski , John T. Suh , Paul Menard , Howard Jones , Edward S. Neiss
CPC分类号: C07K5/0222 , A61K38/00 , Y10S530/80
摘要: Compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are as defined herein, having antihypertensive activity.
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公开(公告)号:US4696939A
公开(公告)日:1987-09-29
申请号:US802921
申请日:1985-11-29
申请人: John T. Suh , John J. Piwinski , Howard Jones , Edward S. Neiss
发明人: John T. Suh , John J. Piwinski , Howard Jones , Edward S. Neiss
IPC分类号: C07D231/56 , C07D239/90 , C07D285/14 , C07D285/30 , A61K31/41
CPC分类号: C07D231/56 , C07D239/90 , C07D285/14 , C07D285/30
摘要: Compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are as defined herein, having antihypertensive activity.
摘要翻译: 式IMA的化合物及其药学上可接受的盐,其中取代基如本文所定义,具有抗高血压活性。
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公开(公告)号:US4576941A
公开(公告)日:1986-03-18
申请号:US584576
申请日:1984-02-29
申请人: John T. Suh , John J. Piwinski , Howard Jones , Edward S. Neiss
发明人: John T. Suh , John J. Piwinski , Howard Jones , Edward S. Neiss
IPC分类号: A61K31/165 , A61K31/17 , A61K31/18 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/265 , A61K31/415 , A61K31/433 , A61K31/505 , A61K31/517 , A61P7/10 , A61P9/00 , A61P9/12 , A61P43/00 , C07C67/00 , C07C313/00 , C07C323/60 , C07D231/56 , C07D239/90 , C07D285/06 , C07D285/14 , C07D285/24 , C07D285/30 , C07D521/00 , A61K31/54 , C07D401/12 , C07D413/12 , C07D417/12
CPC分类号: C07D231/56 , C07D239/90 , C07D285/14 , C07D285/30
摘要: Compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are as defined herein, having antihypertensive activity.
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公开(公告)号:US4650854A
公开(公告)日:1987-03-17
申请号:US741936
申请日:1985-06-06
申请人: Edward S. Neiss , David Stevenson , Laurence L. Ho , Robert C. Liu , John T. Suh
发明人: Edward S. Neiss , David Stevenson , Laurence L. Ho , Robert C. Liu , John T. Suh
IPC分类号: A61K38/00 , C07K14/585 , C07K7/36
CPC分类号: C07K14/585 , A61K38/00
摘要: New peptides are disclosed which have biological activity of the same type as known calcitonins and which are amide analogs of natural calcitonins.
摘要翻译: 公开了具有与已知降钙素相同类型的生物活性并且是天然降钙素的酰胺类似物的新肽。
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公开(公告)号:US4804742A
公开(公告)日:1989-02-14
申请号:US938671
申请日:1986-12-05
申请人: Edward S. Neiss , David Stevenson , Laurence L. Ho , Robert C. Liu , John T. Suh
发明人: Edward S. Neiss , David Stevenson , Laurence L. Ho , Robert C. Liu , John T. Suh
IPC分类号: A61K38/00 , C07K14/585 , C07C103/52
CPC分类号: C07K14/585 , A61K38/00
摘要: New peptides are disclosed which have biological activity of the same type as known calcitonins and which are amide analogs of natural calcitonins.
摘要翻译: 公开了具有与已知降钙素相同类型的生物活性并且是天然降钙素的酰胺类似物的新肽。
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公开(公告)号:US4661515A
公开(公告)日:1987-04-28
申请号:US821201
申请日:1986-01-17
申请人: Edward S. Neiss , John T. Suh , John J. Piwinski
发明人: Edward S. Neiss , John T. Suh , John J. Piwinski
IPC分类号: C07D307/52 , A61K31/265 , A61K31/34 , C07C153/017 , C07D307/54
CPC分类号: C07D307/52
摘要: Novel compounds possessing both angiotensin enzyme inhibitory activity and diuretic activity are disclosed. The compounds are represented by the general formula ##STR1## in which X is ##STR2## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, and cycloalkyl, and may be the same or different; n is an integer from 0 to 4 inclusive; M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cyloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl, or M and R.sub.6 taken together with the nitrogen to which M is bonded and the carbon to which R.sub.6 is bonded form a saturated unsubstituted heterocyclic group containing 3 or 4 ring carbon atoms; Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy; Z.sub.1 and Z.sub.2 each is a chemical bond, the group X.sub.3 --(CH.sub.2).sub.m, an amino acid group or the group X.sub.3 --(CH.sub.2).sub.m --X.sub.3 wherein X.sub.3 is oxygen, sulfur or NH and m is an integer from 0 to 4 inclusive; A and B each is the same as R.sub.1 or halogen, trifluoromethyl, OR.sub.1, NO.sub.2, NR.sub.1 R.sub.2, SO.sub.2 NH.sub.2, CN, SR.sub.1, SOR.sub.1, SO.sub.2 R.sub.1, CONR.sub.1 R.sub.2, COOR.sub.1 ; C is hydrogen alkyl, heteroallyl, amino, --CR.sub.1 .dbd.CR.sub.2 --, ##STR3## aminoalkyl, furfurylmethylamino, aminoaryl or aminobenzyl; X.sub.1 and X.sub.2 are each S, SO, SO.sub.2, NR.sub.1, O, chemical bond, (CR.sub.9 R.sub.10).sub.m, --CR.sub.9 .dbd.CR.sub.10 --, and CHOH, with the proviso that at least one of X.sub.1 and X.sub.2 be (CR.sub.9 R.sub.10).sub.m, wherein R.sub.9 and R.sub.10 are each hydrogen or lower alkyl, and m is an integer from 1 to 5; Ar is a divalent arylene or heteroarylene; and R.sub.7 and R.sub.8 are each hydrogen, alkyl, halo, cyano, hydroxy, alkoxy, amino, alkylamino, dialkylamino, mercapto, alkylmercapto, nitro, trifluoromethyl, carboxy, carbalkoxy, COY and NHCONHR.sub.1 wherein R.sub.1 and Y are as hereindefined; and pharmaceutically-acceptable salts thereof.
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公开(公告)号:US4364940A
公开(公告)日:1982-12-21
申请号:US237234
申请日:1981-02-23
申请人: Edward S. Neiss , Bernard Loev
发明人: Edward S. Neiss , Bernard Loev
IPC分类号: A61K31/60 , A61K8/38 , A61K31/235 , A61K33/40 , A61P17/00 , A61Q19/00 , C07C409/34
CPC分类号: A61Q19/00 , A61K8/38 , Y10S514/859
摘要: A composition for the treatment of acne in the form of a solution, lotion or cream containing from about 1 to 10% by weight of a compound of the formula ##STR1## wherein R is an alkyl having up to 6 carbon atoms or aryl having up to 10 carbon atoms and R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl having up to 6 carbon atoms, phenyl, phenyl-lower alkyl, lower alkylphenyl, halogen, halophenyl, trifluoromethyl, trifluoromethylphenyl, lower alkoxy, methylenedioxy, and lower alkoxyphenyl.
摘要翻译: 用于治疗痤疮形式的组合物,其含有约1-10重量%的下式化合物,其中R是具有至多6个碳原子的烷基或具有至多6个碳原子的芳基 至10个碳原子,R 1和R 2独立地为氢,具有至多6个碳原子的低级烷基,苯基,苯基 - 低级烷基,低级烷基苯基,卤素,卤代苯基,三氟甲基,三氟甲基苯基,低级烷氧基,亚甲二氧基和低级烷氧基苯基。
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