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1. 发明申请

WO02092622A2 DIPEPTIDE DERIVATIVES 审中-公开
标题翻译：替代衍生物
公开(公告)号：WO02092622A2
公开(公告)日：2002-11-21
申请号：PCT/EP0205293
申请日：2002-05-14
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , FINK CYNTHIA ANNE
发明人： FINK CYNTHIA ANNE
IPC分类号： C12N9/99 , A61K38/00 , A61P9/00 , A61P9/12 , A61P43/00 , C07K5/06 , C07K5/062 , C07K5/00
CPC分类号： A61K31/235 , A61K38/05 , A61K45/06 , C07K5/06026 , C07K5/06034 , C07K5/06191 , A61K2300/00
摘要： Compounds of formula (I) wherein R, R1, COOR2, R3-R7, alk, and X have meaning as defined, such being useful as dual inhibitors of angiotensin converting enzyme and neutral endopeptidase, as well as inhibitors of endothelin converting enzyme. In a preferred embodiment, R and R5 represent hydrogen; R1 represents benzyl; R3 represents hydrogen, acetyl or methoxyacetyl; R4 represents isopropyl or tert-butyl; R6 and R7 represent methyl; X represents -O-; alk represents methylene; and COOR2 represents carboxyl or ethoxycarbonyl.
摘要翻译：其中R，R1，COOR2，R3-R7，alk和X具有定义的含义的式（I）化合物，可用作血管紧张素转换酶和中性肽链内切酶的双重抑制剂，以及内皮素转化酶的抑制剂。在优选的实施方案中，R和R 5表示氢; R1表示苄基; R3表示氢，乙酰基或甲氧基乙酰基; R4代表异丙基或叔丁基; R6和R7代表甲基; X表示-O-; 烷基代表亚甲基; COOR2代表羧基或乙氧基羰基。

2. 发明申请

WO02092622A8 DIPEPTIDE DERIVATIVES HAVING A N-TERMINAL 2-THIOACYL GROUP AS VASOPEPTIDASE INHIBITORS 审中-公开
标题翻译：具有作为血管生成抑制剂的N-末端2-硫代酸基团的二肽衍生物
公开(公告)号：WO02092622A8
公开(公告)日：2004-01-22
申请号：PCT/EP0205293
申请日：2002-05-14
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FINK CYNTHIA ANNE
发明人： FINK CYNTHIA ANNE
IPC分类号： C12N9/99 , A61K38/00 , A61P9/00 , A61P9/12 , A61P43/00 , C07K5/06 , C07K5/062 , A61K38/04
CPC分类号： A61K31/235 , A61K38/05 , A61K45/06 , C07K5/06026 , C07K5/06034 , C07K5/06191 , A61K2300/00
摘要： Compounds of formula (I) wherein R, R1, COOR2, R3-R7, alk, and X have meaning as defined, such being useful as dual inhibitors of angiotensin converting enzyme and neutral endopeptidase, as well as inhibitors of endothelin converting enzyme. In a preferred embodiment, R and R5 represent hydrogen; R1 represents benzyl; R3 represents hydrogen, acetyl or methoxyacetyl; R4 represents isopropyl or tert-butyl; R6 and R7 represent methyl; X represents -O-; alk represents methylene; and COOR2 represents carboxyl or ethoxycarbonyl.
摘要翻译：其中R，R1，COOR2，R3-R7，alk和X具有定义的含义的式（I）化合物，可用作血管紧张素转换酶和中性肽链内切酶的双重抑制剂，以及内皮素转化酶的抑制剂。在优选的实施方案中，R和R 5表示氢; R1表示苄基; R3表示氢，乙酰基或甲氧基乙酰基; R4代表异丙基或叔丁基; R6和R7代表甲基; X表示-O-; 烷基代表亚甲基; COOR2代表羧基或乙氧基羰基。

3. 发明专利

HU226645B1 CERTAIN CYCLIC THIO SUBSTITUTED ACYLAMINOACID AMIDE DERIVATIVES 未知
公开(公告)号：HU226645B1
公开(公告)日：2009-05-28
申请号：HU0002122
申请日：1998-03-18
申请人： NOVARTIS AG
发明人： FINK CYNTHIA ANNE
IPC分类号： C07C327/32 , C07D295/14 , A61K31/16 , A61K31/198 , A61K31/265 , A61K31/38 , A61K31/381 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/5375 , A61K31/625 , A61P19/02 , A61P25/00 , A61P29/00 , A61P35/00 , C07C323/53 , C07C323/60 , C07C327/22 , C07C327/26 , C07D211/34 , C07D211/96 , C07D213/56 , C07D213/75 , C07D213/81 , C07D213/82 , C07D213/83 , C07D333/20 , C07D333/24 , C07D333/36 , C07D333/38
摘要： Disclosed are compound of formula I wherein R represents hydrogen, lower alkyl, cycloalkyl, bicycloalkyl, adamantyl, aryl, biaryl, or mono- or di-(cycloalkyl, aryl or biaryl)-lower alkyl, di-(lower alkyl or aryl-lower alkyl)amino-lower alkyl, or (piperidino, morpholino, pyrrolidino)-lower alkyl; R1 represents hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, or (cycloalkyl, aryl or biaryl)-lower alkyl; R2 represents hydrogen, lower alkyl, lower alkoxy, aryl-lower alkyl, aryl-lower alkoxy, amino, mono- or di-(lower alkyl or aryl-lower alkyl)-amino, acylamino, or (lower alkyl or aryl-lower alkyl)-(thio, sulfinyl or sulfonyl); R3 represents hydrogen, lower alkyl, cycloalkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or C2-C7-alkyl interrupted by S, SO, SO2, O or N-R5; R4 represents hydrogen or acyl; R5 represents hydrogen, lower alkyl, aryl-lower alkyl, acyl, or (lower alkyl, aryl or aryl-lower alkyl)-sulfonyl; A together with the carbon to which it is attached forms a ring and represents a bivalent radical of the formula (CH2)P which may be interrupted by S, SO, SO2, O, or N-R5; n represents an integer from zero to four; p represents an integer from 2 to 6; any pharmaceutically acceptable salts thereof; and disulfides corresponding to said compounds of formula I wherein R4 is hydrogen; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinases in mammals using such compounds.

4. 发明专利

CO5540347A2 DERIVADOS DE DIPEPTIDO QUE CONTIENE UN GRUPO 2-TIOACILO N-TERMINAL COMO INHIBIDORES DE VASOPEPTIDASA 未知
公开(公告)号：CO5540347A2
公开(公告)日：2005-07-29
申请号：CO03105928
申请日：2003-12-02
申请人： NOVARTIS AG
发明人： FINK CYNTHIA ANNE
IPC分类号： C12N9/99 , A61K38/00 , A61P9/00 , A61P9/12 , A61P43/00 , C07K5/06 , C07K5/062
摘要： 1.- Compuestos de la fórmula:en donde R, R1, COOR2, R3-R7, alk, y X tienen los significados como se definen, siendo éstos útiles como inhibidores dobles de la enzima convertidora de angiotensina y de la endopeptidasa neutra, así como inhibidores de la enzima convertidora de endotelina. En una modalidad preferida R y R5 representan hidrógeno; R1 representa bencilo; R3 representa hidrógeno, acetilo o metoxiacetilo; R4 representa isopropilo o butilo terciario; R6 y R7 representan metilo; X representa -O-;alk representa metileno; y COOR2 representa carboxilo o etoxicarbonilo.

5. 发明专利

BR0212899A 未知
公开(公告)号：BR0212899A
公开(公告)日：2004-11-03
申请号：BR0212899
申请日：2002-09-20
申请人： NOVARTIS AG
发明人： FINK CYNTHIA ANNE
IPC分类号： C12N9/99 , A61K38/00 , A61K38/04 , A61K38/55 , A61K45/00 , A61P9/04 , A61P9/12 , A61P13/12 , A61P43/00 , C07K5/04 , C07K5/06 , C07K5/065 , C07D309/06 , C07D405/12 , C07D409/14 , A61K31/35 , A61K31/40 , A61K31/44
摘要： Compounds of the formula wherein R, R 1 -R 7 and alk have meaning as defined, pharmaceutical compositions thereof, and use thereof for the treatment and/or prevention of cardiovascular disorders responsive to ACE and NEP inhibition and/or ECE inhibition.

6. 发明专利

SK14032003A3 Dipeptide derivatives having a N-terminal 2-thioacyl group as vasopeptidase inhibitors 未知
公开(公告)号：SK14032003A3
公开(公告)日：2004-06-08
申请号：SK14032003
申请日：2002-05-14
申请人： NOVARTIS AG
发明人： FINK CYNTHIA ANNE
IPC分类号： C12N9/99 , A61K38/00 , A61P9/00 , A61P9/12 , A61P43/00 , C07K5/06 , C07K5/062
摘要： Compounds of the formula wherein, R to R 7 and alk-X have meaning as defined, such being useful as dual inhibitors of angiotensin converting enzyme and neutral endopeptidase, as well as inhibitors of endothelin converting enzyme.

7. 发明专利

NO20035084A 未知
公开(公告)号：NO20035084A
公开(公告)日：2004-01-15
申请号：NO20035084
申请日：2003-11-14
申请人： NOVARTIS AG
发明人： FINK CYNTHIA ANNE
IPC分类号： C12N9/99 , A61K38/00 , A61P9/00 , A61P9/12 , A61P43/00 , C07K5/06 , C07K5/062 , C07K
CPC分类号： A61K31/235 , A61K38/05 , A61K45/06 , C07K5/06026 , C07K5/06034 , C07K5/06191 , A61K2300/00

8. 发明专利

NO314079B1 未知
公开(公告)号：NO314079B1
公开(公告)日：2003-01-27
申请号：NO994482
申请日：1999-09-16
申请人： NOVARTIS AG
发明人： FINK CYNTHIA ANNE
IPC分类号： C07D295/14 , A61K31/16 , A61K31/198 , A61K31/265 , A61K31/381 , A61K31/4402 , A61K31/4406 , A61K31/5375 , A61P19/02 , A61P29/00 , A61P35/00 , C07C323/53 , C07C323/60 , C07C327/22 , C07C327/26 , C07C327/32 , C07D213/56 , C07D213/75 , C07D213/81 , C07D213/82 , C07D333/20 , C07D333/24 , C07D333/38 , A61K31/44
摘要： Disclosed are compound of formula I wherein R represents hydrogen, lower alkyl, cycloalkyl, bicycloalkyl, adamantyl, aryl, biaryl, or mono- or di-(cycloalkyl, aryl or biaryl)-lower alkyl, di-(lower alkyl or aryl-lower alkyl)amino-lower alkyl, or (piperidino, morpholino, pyrrolidino)-lower alkyl; R1 represents hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, or (cycloalkyl, aryl or biaryl)-lower alkyl; R2 represents hydrogen, lower alkyl, lower alkoxy, aryl-lower alkyl, aryl-lower alkoxy, amino, mono- or di-(lower alkyl or aryl-lower alkyl)-amino, acylamino, or (lower alkyl or aryl-lower alkyl)-(thio, sulfinyl or sulfonyl); R3 represents hydrogen, lower alkyl, cycloalkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or C2-C7-alkyl interrupted by S, SO, SO2, O or N-R5; R4 represents hydrogen or acyl; R5 represents hydrogen, lower alkyl, aryl-lower alkyl, acyl, or (lower alkyl, aryl or aryl-lower alkyl)-sulfonyl; A together with the carbon to which it is attached forms a ring and represents a bivalent radical of the formula (CH2)P which may be interrupted by S, SO, SO2, O, or N-R5; n represents an integer from zero to four; p represents an integer from 2 to 6; any pharmaceutically acceptable salts thereof; and disulfides corresponding to said compounds of formula I wherein R4 is hydrogen; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinases in mammals using such compounds.

9. 发明专利

NO311224B1 未知
公开(公告)号：NO311224B1
公开(公告)日：2001-10-29
申请号：NO944364
申请日：1994-11-15
申请人： NOVARTIS AG
发明人： FINK CYNTHIA ANNE
IPC分类号： A61K38/55 , A61K38/00 , A61P3/06 , A61P7/10 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , C07K5/065 , C07K5/078 , C07K14/81 , A61K38/05 , A61P9/00
摘要： Disclosed are the compounds of formula I wherein R represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl-lower alkyl or cycloalkyl-lower alkyl; R1 represents hydrogen, lower alkyl, cycloalkyl, carbocyclic aryl or heterocyclic aryl, or biaryl; R3 represents hydrogen or acyl; R4 represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, biaryl or biaryl-lower alkyl; R5 represents hydrogen or lower alkyl; or R4 and R5 together with the carbon atom to which they are attached represent cycloalkylidene or benzo-fused cycloalkylidene; A together with the carbon atom to which it is attached represents 3 to 10 membered cycloalkylidene or 5 to 10 membered cycloalkenylidene radical which may be substituted by lower alkyl or aryl-lower alkyl or may be fused to a saturated or unsaturated carbocyclic 5-7-membered ring; or A together with the carbon to which it is attached represents 5 or 6 membered oxacycloalkylidene, thiacycloalkylidene or azacycloalkylidene optionally substituted by lower alkyl or aryl-lower alkyl; or A together with the carbon atom to which it is attached represents 2,2-norbornylidene; m is 0, 1, 2 or 3; and COOR2 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester; disulfide derivatives derived from said compounds wherein R3 is hydrogen; and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for preparation of said compounds; intermediates; and methods of treating disorders in mammals which are responsive to ACE and NEP inhibition by administration of said compounds to mammals in need of such treatment.

10. 发明专利

SK15812000A3 CERTAIN THIOL INHIBITORS OF ENDOTHELIN-CONVERTING ENZYME 未知
公开(公告)号：SK15812000A3
公开(公告)日：2001-03-12
申请号：SK15812000
申请日：1999-04-21
申请人： NOVARTIS AG
发明人： DE LOMBAERT STEPHANE , FINK CYNTHIA ANNE , FIROOZNIA FARIBORZ , HOYER DENTON WADE , JENG ARCO YINGCHEU
IPC分类号： A61K38/00 , C07K5/065 , C07K5/078 , A61K38/05
摘要： Disclosed as endothelin converting enzyme inhibitors are the compounds of formula (I), wherein the variables have the meanings as defined hereinbefore.

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