公开(公告)号：US20030036208A1

公开(公告)日：2003-02-20

申请号：US10271661

申请日：2002-10-16

申请人： University of Utah Research Foundation, a Utah corporation

发明人： Andreas Rohrwasser ,  Terry Morgan ,  Jean-Marc Lalouel

IPC分类号： G01N033/536

CPC分类号： G01N33/74 ,  C12Q1/6883 ,  C12Q2600/158 ,  G01N2333/96466 ,  G01N2333/96472 ,  G01N2410/02 ,  G01N2500/00 ,  Y10S530/86

摘要： The present invention relates to a method for screening drugs for use in treating hypertension using the tubular renin-angiotensinogen system identified by the present invention. The invention further relates to a method to diagnose sodium status and sensitivity in an individual by measuring urinary angiotensinogen or angiotensin-I.

公开(公告)号：US5008402A

公开(公告)日：1991-04-16

申请号：US497718

申请日：1990-03-22

申请人： Thomas Meul

发明人： Thomas Meul

IPC分类号： C07D207/36 ,  C07D207/38

CPC分类号： C07D207/38 ,  Y10S530/86

摘要： A process for the production of 5-alkyl tetramic acids from 4-alkoxy-3-pyrrolin-2-ones and aldehydes or ketones. By basic catalysis, 5-alkylidene-4-alkoxy-3-pyrrolin-2-ones are first formed, which are converted into the target compounds by cleavage of the alkoxy group and catalytic hydrogenation.

公开(公告)号：US4985407A

公开(公告)日：1991-01-15

申请号：US280330

申请日：1988-12-06

申请人： Michael W. Foxton ,  Barry E. Ayres ,  Anthony W. J. Cooper

发明人： Michael W. Foxton ,  Barry E. Ayres ,  Anthony W. J. Cooper

IPC分类号： C12N9/99 ,  A61K38/55 ,  A61P5/38 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P27/02 ,  A61P27/06 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K14/81

CPC分类号： C07K5/0227 ,  C07K5/0207 ,  Y10S530/86

摘要： There are described new compounds of formula (1) ##STR1## wherein R.sup.1 represents an acyl group;X.sup.1 represents phenylalanine or p-methoxyphenylalanine bonded N-terminally to R.sup.1 and C-terminally to X.sup.2 ;X.sup.2 represents histidine or N-methylhistidine bonded N-terminally to X.sup.1 and C-terminally to the group --NH--;R.sup.2 represents a C.sub.4-6 cycloalkyl group;R.sup.3 represents a group CHR.sup.6 R.sup.7 is a hydrogen atom and R.sup.7 is a phenyl group, or R.sup.6 is a methyl group and R.sup.7 is a hydrogen atom or a methyl or ethyl group;X.sup.3 represents a C.sub.2-6 alkylene chain optionally substituted by one or more C.sub.1-4 alkyl groups;R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a C.sub.1-4 alkyl group, or NR.sup.4 R.sup.5 may form a 5- or 6- membered polymethylenimine ring;and salts and solvates thereof.The new compounds have been found to exhibit activity as renin inhibitors, combining good duration of action with significant oral potency.Compositions containing the compounds of formula (1) and processes for preparing the compounds are also described.

公开(公告)号：US4914129A

公开(公告)日：1990-04-03

申请号：US405372

申请日：1989-09-08

申请人： Peter Buhlmayer ,  James L. Stanton ,  Walter Fuhrer ,  Richard Goschke ,  Vittorio Rasetti ,  Heinrich Rueger

发明人： Peter Buhlmayer ,  James L. Stanton ,  Walter Fuhrer ,  Richard Goschke ,  Vittorio Rasetti ,  Heinrich Rueger

IPC分类号： C07D233/54 ,  C07D233/64 ,  C07D233/84 ,  C07D401/12 ,  C07D417/12

CPC分类号： C07D233/64 ,  C07D233/84 ,  C07D401/12 ,  C07D417/12 ,  Y10S530/86

摘要： Compounds of the formula ##STR1## in which R.sub.1 represents acyl substituted by a thio, sulphinyl or sulphonyl group, A represents an optionally N-alkylated .alpha.-amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy, optionally substituted mercapto, sulphinyl or sulphonyl, and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups, inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.

公开(公告)号：US4906613A

公开(公告)日：1990-03-06

申请号：US795282

申请日：1985-11-05

申请人： Robert W. Watkins

发明人： Robert W. Watkins

IPC分类号： A61K38/00 ,  A61K38/55 ,  A61K45/00 ,  C07K5/02

CPC分类号： C07K5/0227 ,  A61K38/553 ,  Y10S530/86

摘要： The present invention relates to ophthalmological pharmaceutical compositions comprising a renin inhibitor and to methods for using said composition in the treatment of glaucoma.

公开(公告)号：US4904660A

公开(公告)日：1990-02-27

申请号：US160173

申请日：1988-02-25

申请人： Kohji Nakano ,  Takashi Fujikura ,  Ryuichiro Hara ,  Masato Ichihara ,  Yukiko Fukunaga ,  Masayuki Shibasaki

发明人： Kohji Nakano ,  Takashi Fujikura ,  Ryuichiro Hara ,  Masato Ichihara ,  Yukiko Fukunaga ,  Masayuki Shibasaki

IPC分类号： A61K38/00 ,  C07D233/54 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/12 ,  C07K5/02 ,  C07K5/065

CPC分类号： C07D233/64 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/12 ,  C07K5/0227 ,  C07K5/06078 ,  A61K38/00 ,  Y10S530/86

摘要： Novel compounds of the following formula (I) and their salts: A compound of the formula (I) ##STR1## These compounds are expected to be useful for renin inhibitors. Thus, the compounds are useful medical agents, in particular, anti-hypertensive agents.

公开(公告)号：US4857650A

公开(公告)日：1989-08-15

申请号：US879741

申请日：1986-06-27

申请人： Kinji Iizuka ,  Tetsuhide Kamijo ,  Tetsuhiro Kubota ,  Kenji Akahane ,  Hideaki Umeyama ,  Yoshiaki Kiso

发明人： Kinji Iizuka ,  Tetsuhide Kamijo ,  Tetsuhiro Kubota ,  Kenji Akahane ,  Hideaki Umeyama ,  Yoshiaki Kiso

IPC分类号： C07D233/54 ,  C07D233/61 ,  C07D233/64 ,  C07D403/12

CPC分类号： C07D233/64 ,  C07D403/12 ,  Y10S530/86

摘要： New renin inhibitory amino acid derivatives represented by formula (I): ##STR1## wherein A represents an alkoxycarbonyl group having 2 to 7 carbon atoms, ##STR2## wherein R.sup.1 and R.sup.2 are defined as in the specification below or ##STR3## wherein X and Y are defined as in the specification herein below, n represents zero or one, Z represents --O-- or --NH--, and R represents a straight- or branched chain alkyl group having 1 to 7 carbon atoms, and pharmaceutically acceptable salts thereof, useful as a therapeutic agent are disclosed. The amino acid derivatives have a renin inhibitory effect when administered orally and are useful for treatment of hypertension, especially renin-associated hypertension.

摘要翻译： 由式（I）表示的新的肾素抑制性氨基酸衍生物：其中A表示碳原子数2〜7的烷氧基羰基，其中R1和R2如下面的说明书所定义， 其中X和Y如下面的说明书中所定义，n表示0或1，Z表示-O-或-NH-，R表示具有1至7个碳原子的直链或支链烷基， 公开了可用作治疗剂的盐。 当口服给药时，氨基酸衍生物具有肾素抑制作用，可用于治疗高血压，特别是肾素相关性高血压。

公开(公告)号：US4855303A

公开(公告)日：1989-08-08

申请号：US206079

申请日：1988-06-10

申请人： Dennis J. Hoover

发明人： Dennis J. Hoover

IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K5/06

CPC分类号： C07K5/0227 ,  C07K5/06191 ,  A61K38/00 ,  Y10S530/86

摘要： Polypeptides containing fluorinated cyclostatine derivatives as antihypertensive agents.

摘要翻译： 含有氟化环状星素衍生物作为抗高血压药的多肽。

公开(公告)号：US4853463A

公开(公告)日：1989-08-01

申请号：US283694

申请日：1988-12-13

申请人： Kinji Iizuka ,  Tetsuhide Kamijo ,  Tetsuhiro Kubota ,  Kenji Akahane ,  Hideaki Umeyama ,  Yoshiaki Kiso

发明人： Kinji Iizuka ,  Tetsuhide Kamijo ,  Tetsuhiro Kubota ,  Kenji Akahane ,  Hideaki Umeyama ,  Yoshiaki Kiso

IPC分类号： C07C233/51 ,  C07D207/16 ,  C07D295/185

CPC分类号： C07D295/185 ,  C07C233/51 ,  C07D207/16 ,  Y10S530/86

摘要： Novel amino acid derivatives useful as a therapeutic agent are disclosed. These amino acid derivatives and the pharmaceutically acceptable salts thereof have a human renin inhibitory effect when administered orally and are useful for treatment of hypertension, especially renin-associated hypertension.

摘要翻译： 公开了可用作治疗剂的新型氨基酸衍生物。 这些氨基酸衍生物及其药学上可接受的盐在口服给药时具有人肾素抑制作用，可用于治疗高血压，特别是肾素相关性高血压。

公开(公告)号：US4812555A

公开(公告)日：1989-03-14

申请号：US171973

申请日：1988-03-22

申请人： Peter Raddatz ,  Gunter Holzemann ,  Alfred Jonczyk ,  Claus J. Schmitges ,  Klaus O. Minck

发明人： Peter Raddatz ,  Gunter Holzemann ,  Alfred Jonczyk ,  Claus J. Schmitges ,  Klaus O. Minck

IPC分类号： C07K7/06 ,  A61K38/00 ,  A61K38/55 ,  A61P9/12 ,  A61P43/00 ,  C07C67/00 ,  C07C231/00 ,  C07C237/12 ,  C07C237/22 ,  C07C239/00 ,  C07C269/00 ,  C07C301/00 ,  C07C303/40 ,  C07C309/18 ,  C07C313/00 ,  C07D233/54 ,  C07K1/113 ,  C07K5/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/08 ,  C07K5/10 ,  C07K14/81 ,  A61K37/02

CPC分类号： C07D233/64 ,  C07K5/00 ,  C07K5/0227 ,  Y10S530/86

摘要： New peptides of the formula IX--Z--NR.sup.2 --CHR.sup.3 --CHOH--(CHR.sup.4).sub.n --CO--Ewherein X, Z, R.sup.2, R.sup.3, R.sup.4, E and n are as defined herein and their salts inhibit the activity of human plasma renin.

摘要翻译： 式XZ-NR2-CHR3-CHOH-（CHR4）n-CO-E的新肽，其中X，Z，R2，R3，R4，E和n如本文所定义，并且它们的盐抑制人血浆肾素的活性 。