专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明专利

CA2252086A1 6-SUBSTITUTED AMINO-4-OXA-1-AZABICYCLO[3,2,0]HEPTAN-7-ONE DERIVATIVES AS CYSTEINE PROTEASE INHIBITORS 未知
公开(公告)号：CA2252086A1
公开(公告)日：1997-10-16
申请号：CA2252086
申请日：1997-04-09
申请人： MICETICH RONALD GEORGE , SYNPHAR LAB INC , KALETA JADWIGA , ZHOU NIAN E , PURISIMA ENRICO , GUO DEQI , SINGH RAJESHWAR , MENARD ROBERT , CAMERON ALAN , CA NAT RESEARCH COUNCIL
发明人： MICETICH RONALD GEORGE , KALETA JADWIGA , ZHOU NIAN E , PURISIMA ENRICO , GUO DEQI , SINGH RAJESHWAR , MENARD ROBERT , CAMERON ALAN
IPC分类号： C12N9/99 , A61K31/00 , A61K38/00 , A61P9/00 , A61P9/10 , A61P19/00 , A61P19/10 , A61P21/00 , A61P25/00 , A61P31/00 , A61P35/00 , A61P35/04 , C07D503/00 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/08 , A61K38/05 , C07D519/06 , A61K31/42 , A61K31/435 , A61K31/495 , A61K31/535 , A61K31/54
摘要： Novel 6-substituted amino-4-oxa-1-azabicyclo¢3,2,0! heptan-7-one compounds, as well as the pharmaceutically acceptable salts thereof and diastereoisomers thereof, of formula (I) are disclosed, which exhibit excellent cysteine protease inhibitory activity and my be used for treatment of different diseases such as muscular dystrophy, arthritis, myocardial infarction, Alzheimer's disease, bacterial infection, common cold, osteroporosis and cancer metastasis.

2. 发明申请

WO1998025932A1 ANTIBACTERIAL AGENTS 审中-公开
标题翻译：抗菌剂
公开(公告)号：WO1998025932A1
公开(公告)日：1998-06-18
申请号：PCT/US1997022356
申请日：1997-12-05
申请人： WARNER-LAMBERT COMPANY , DOMAGALA, John, Michael , ELLSWORTH, Edmund, Lee , STIER, Michael, Andrew , HUANG, Liren , MICETICH, Ronald, George , SINGH, Rajeshwar , WRIGLEY, Stephen, Keith , WANG, Shouming , ROE, Michael , THORNTON, David, Michael
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D498/04
CPC分类号： C07D487/04 , C07D513/04
摘要： Described are antibacterial agents of formula (I): X is O, S or N-R8; R1, R2, R3 and R8 are independently H, straight or branched alkyl of 1-6 carbons, cycloalkyl of 3-6 carbons, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur, or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR2, NR'COR', CN, CO2R' or CONR2', halogen, CN, CO2R, COR, CON(R)2, CON(R")2, SR, SON, SCO2R or SCON(R)2; R4 is H, straight or branched alkyl of from 1-6 carbon atoms, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR2, NR'COR', CN, CO2R' or CONR2', halogen, CN, NO2, N(R)2, NRCOR, NRCOR", COR, CO2R, CON(R)2, CON(R")2, NRCON(R)2, NRCO2R; R5 is 1-6 straight or branched alkyl, a cycloalkyl of 3-6 carbons, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR2, NR'COR', CN, CO2R' or CONR2', halogen, OR, N(R)2, NRCOR, NRCOR", COR, CON(R)2, CON(R")2, SR or SO2R; R6, R7 are independently H, straight or branched alkyl of 1-6 carbons, cycloalkyl of 3-6 carbons, COR, COR", SO2NR2, CONR2 and these may be optionally substituted by any of the groups listed for R5; R is H, straight or branched alkyl of 1-6 carbon atoms, cycloalkyl of from 3-6 carbon atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur, or pheny, all of which may be optionally substituted by halogen, OR', NR'2, NR'COR', CN, CO2R', CONR'2; R' is H, alkyl of from 1-3 carbon atoms or Ph; R" is part of a naturally occurring amino acid connected via an amide or acyl bond as determined by the formula; halogen is any one of fluoro, chloro, bromo or iodo; or a pharmaceutically acceptable salt.
摘要翻译：描述了式（I）的抗菌剂：X是O，S或N-R8; R1，R2，R3和R8独立地为H，1-6个碳的直链或支链烷基，3-6个碳原子的环烷基，2-6个碳原子的烯基或炔基，5-8个原子的杂环，1-3个杂原子作为氮，氧或硫或苯基，所有这些环可以任选被卤素，OR，NR 2，NR'COR'，CN，CO 2 R'或CONR 2'，卤素，CN，CO 2 R，COR ，CON（R）2，CON（R“）2，SR，SON，SCO 2 R或SCON R 2; R 4是H，1-6个碳原子的直链或支链烷基，2至6的烯基或炔基原子，5-8个原子与1-3个杂原子作为氮原子的杂环，氧或硫或苯基，所有这些环可以任选地被卤素OR，NR 2，NR'COR'，CN， CO 2 R，CONR 2，CON（R“）2，NRCON（R）2，NRCO 2 R; R 5是 1-6个直链或支链烷基，3-6个碳原子的环烷基，2-6个碳原子的烯基或炔基，5-8个原子的杂环和1-3个杂原子作为氮，氧或硫或苯基，所有这些环可以任选被卤素，OR，NR 2，NR'COR'，CN，CO 2 R'或CONR 2'，卤素，OR，N（R） 2，NRCOR，NRCOR“，COR，CON（R）2，CON（R”）2，SR或SO2R; R 6，R 7独立地是H，1-6个碳的直链或支链烷基，3-6个碳的环烷基，COR，COR“，SO2NR2，CONR2，并且它们可以任选被R5所列的任何基团取代; R是H ，1-6个碳原子的直链或支链烷基，3-6个碳原子的环烷基，5-8个原子的杂环，1-3个杂原子作为氮，氧或硫或苯基，所有这些可以是任选的被卤素取代，OR'，NR'2，NR'COR'，CN，CO2R'，CONR'2; R'是H，1-3个碳原子的烷基或Ph; R“是天然存在的氨基通过由式决定的酰胺或酰基键连接酸; 卤素是氟，氯，溴或碘中的任何一种; 或药学上可接受的盐。

3. 发明申请

WO0109169A3 CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：WO0109169A3
公开(公告)日：2001-09-13
申请号：PCT/GB0002830
申请日：2000-07-21
申请人： NAEJA PHARMACEUTICAL INC , SINGH RAJESHWAR , ZHOU NIAN , REDDY ANDHE V N , THOMAS GEORGE , DING QIZHU , KALETA JADWIGA , MICETICH RONALD GEORGE , WHITTAKER MARK
发明人： SINGH RAJESHWAR , ZHOU NIAN , REDDY ANDHE V N , THOMAS GEORGE , DING QIZHU , KALETA JADWIGA , MICETICH RONALD GEORGE , WHITTAKER MARK
IPC分类号： A61K38/00 , A61P9/00 , A61P19/00 , A61P25/00 , A61P31/00 , A61P35/00 , A61P37/00 , C07D207/14 , C07D295/125 , C07D333/38 , C07K5/06 , C07K5/065 , C07K5/062 , A61K31/381 , A61K31/5375 , A61K38/05 , C07D295/12
CPC分类号： C07D295/125 , A61K38/00 , C07D207/14 , C07D333/38 , C07K5/06043 , C07K5/06078
摘要： This invention relates to derivatives of alpha-amino acid amides, to pharmaceutical compositions containing such compounds, and to their use in medicine as inhibitors of cysteine proteases, particularly the cathepsins. A compound of formula (I) is described or a pharmaceutically acceptable salt, hydrate or solvate thereof. Pharmaceutically acceptable salts of the compounds of this invention include the sodium, potassium, magnesium, calcium, hydrogen chloride, tartaric acid, succinic acid, fumaric acid and p-toluenesulfonic acid salts.
摘要翻译：本发明涉及α-氨基酸酰胺的衍生物，含有这些化合物的药物组合物，以及它们在药物中作为半胱氨酸蛋白酶，特别是组织蛋白酶的抑制剂的用途。描述了式（I）化合物或其药学上可接受的盐，水合物或溶剂合物。本发明化合物的药学上可接受的盐包括钠盐，钾盐，镁盐，钙盐，氯化氢盐，酒石酸盐，琥珀酸盐，富马酸盐和对甲苯磺酸盐。

4. 发明申请

WO1998019648A3 N-OXY-NAPHTHALIMIDES AS ANTIBACTERIAL AGENTS 审中-公开
公开(公告)号：WO1998019648A3
公开(公告)日：1998-05-14
申请号：PCT/US1997019872
申请日：1997-10-31
申请人： WARNER-LAMBERT COMPANY , AMEGADZIE, Albert, Kudzoi , CAREY, Maureen, Elizabeth , DOMAGALA, John, Michael , HUANG, Liren , MICETICH, Ronald, George , SINGH, Rajeshwar , STIER, Michael, Andrew , VAISBURG, Arkadii , SANCHEZ, Joseph, Peter
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D221/14

5. 发明申请

WO1993024481A1 7-SUBSTITUTED-6-FLUORO-1,4-DIHYDRO-4-OXO-QUINOLINE-3-CARBOXYLIC ACID COMPOUNDS AND RELATED COMPOUNDS AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译： 7-取代-6-氟-1,4-二氢-4-氧喹啉-3-羧酸化合物及相关化合物作为抗菌剂
公开(公告)号：WO1993024481A1
公开(公告)日：1993-12-09
申请号：PCT/CA1993000231
申请日：1993-05-31
申请人： SYNPHAR LABORATORIES, INC. , SINGH, Rajeshwar , FATHI-AFSHAR, Rakhshandeh , SINGH, Inder, Pal , THOMAS, George , DOERKSEN, Thomas, Roger , SINGH, Maya, Prakash , MICETICH, Ronald, George
发明人： SYNPHAR LABORATORIES, INC.
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D471/04
摘要： Quinoline compounds of formula (I) wherein (A) R is hydrogen or C1-C4 alkyl group; R1 is (i) a C3-C6 cycloalkyl group which may be substituted with one or two halogen atoms, (ii) a phenyl group which may be substituted with one or two halogen atoms, or (iii) a C1-C4 alkyl group which may be substituted with one or two halogen atoms; R2 is hydrogen, a halogen atom, a C1-C4 alkyl group, a hydroxy group or an amino group; R3 is hydrogen, a hydroxy or an amino group; R4 is a 1,2,3-triazol-1-yl group, a 1,2,4-triazol-1-yl group, a 1,2,3,4-tetrazol-1-yl group or a 1,2,3,4-tetrazol-2-yl group, each of which may have 1 to 2 substituents selected from the group consisting of C1-C4 alkyl, COOH, CH2NH2, amino and phenyl groups; and X is N, CH, C-F or C-OCH3; m is 1 or 2; n is 0, 1 or 2; or (B) R1, R2, R3, R4, m and n are as defined above and X and R1 are such that (a) in formula (I) is (b), pharmaceutical compositions using those compounds, methods for treating bacterial infections using those compounds, and methods for disinfecting using those compounds.
摘要翻译：式（I）的喹啉化合物，其中（A）R是氢或C 1 -C 4烷基; R1是（i）可以被一个或两个卤素原子取代的C3-C6环烷基，（ii）可被一个或两个卤素原子取代的苯基，或（iii）C1-C4烷基，可以被一个或两个卤素原子取代; R2是氢，卤素原子，C1-C4烷基，羟基或氨基; R3是氢，羟基或氨基; R 4是1,2,3-三唑-1-基，1,2,4-三唑-1-基，1,2,3,4-四唑-1-基或1,2 3,4-四唑-2-基，其各自可以具有1至2个选自C 1 -C 4烷基，COOH，CH 2 NH 2，氨基和苯基的取代基; X为N，CH，C-F或C-OCH 3; m为1或2; n为0,1或2; 或（B）R 1，R 2，R 3，R 4，m和n如上所定义，X和R 1使得式（I）中的（a）是（b），使用这些化合物的药物组合物，使用这些化合物，以及使用这些化合物进行消毒的方法。

6. 发明申请

WO1999048911A1 MONOBACTAM ENZYME INHIBITORS 审中-公开
标题翻译： MON AM AM ME ME。。。
公开(公告)号：WO1999048911A1
公开(公告)日：1999-09-30
申请号：PCT/IB1999000558
申请日：1999-03-23
申请人： SYNPHAR LABORATORIES INC. , SINGH, Rajeshwar , ZHOU, Nian , REDDY, Andhe, Venkat, Narender , MICETICH, Ronald, George
发明人： SYNPHAR LABORATORIES INC.
IPC分类号： C07K05/065
CPC分类号： C07K5/06078 , A61K38/00
摘要： Monobactam compounds of formula (I) wherein R, R1, R2, R3, R4 and W are as defined in the specification are inhibitors of cysteine proteases such as cathepsins B, L, K and S.
摘要翻译：其中R，R 1，R 2，R 3，R 4和W如说明书中所定义的式（I）的单内酰胺化合物是半胱氨酸蛋白酶如组织蛋白酶B，L，K和S的抑制剂

7. 发明申请

WO9819648A2 ISOQUINOLONES 审中-公开
标题翻译：异喹啉酮
公开(公告)号：WO9819648A2
公开(公告)日：1998-05-14
申请号：PCT/US9719872
申请日：1997-10-31
申请人： WARNER LAMBERT CO , AMEGADZIE ALBERT KUDZOI , CAREY MAUREEN ELIZABETH , DOMAGALA JOHN MICHAEL , HUANG LIREN , MICETICH RONALD GEORGE , SINGH RAJESHWAR , STIER MICHAEL ANDREW , VAISBURG ARKADII , SANCHEZ JOSEPH PETER
发明人： AMEGADZIE ALBERT KUDZOI , CAREY MAUREEN ELIZABETH , DOMAGALA JOHN MICHAEL , HUANG LIREN , MICETICH RONALD GEORGE , SINGH RAJESHWAR , STIER MICHAEL ANDREW , VAISBURG ARKADII , SANCHEZ JOSEPH PETER
IPC分类号： A61K31/473 , A61P31/04 , C07D221/14 , C07D401/04 , C07D491/06 , A61K
CPC分类号： C07D221/14 , C07D401/04 , C07D491/06 , Y02P20/55
摘要： Benzo[de]isoquinoline-1,3-diones which are selective inhibitors of bacterial DNA gyrase and DNA topoisomerase useful in antibacterial agents are described as well as methods for their preparation and formulation. Novel intermediates useful in the preparation of the final products are also described.
摘要翻译：描述了作为细菌DNA促旋酶的选择性抑制剂和可用于抗菌剂的DNA拓扑异构酶的苯并[de]异喹啉-1,3-二酮以及其制备和制剂的方法。还描述了可用于制备最终产品的新型中间体。

8. 发明申请

WO1994001109A1 4-OXA-1-AZABICYCLO [3,2,0] HEPTAN-7-ONE DERIVATIVES AS ANTITUMOR AGENTS 审中-公开
标题翻译： 4-OXA-1-AZABICYCLO [3,2,0] HEPTAN-7-ONE衍生物作为抗肿瘤剂
公开(公告)号：WO1994001109A1
公开(公告)日：1994-01-20
申请号：PCT/GB1993001435
申请日：1993-07-08
申请人： APPLEDENE LIMITED , TAIHO PHARMACEUTICAL CO. LTD. , OTANI, Toshio , OIE, Shinji , MATSUMOTO, Hiroshi , TEMPEST, Mark , MICETICH, Ronald, George , SINGH, Rajeshwar , YAMASHITA, Tomohiro
发明人： APPLEDENE LIMITED , TAIHO PHARMACEUTICAL CO. LTD.
IPC分类号： A61K31/42
CPC分类号： A61K31/42
摘要： The present invention relates to the use of 4-oxa-1-azabicyclo [3,2,0] heptan-7-one derivatives of formula (I) or a pharmaceutically acceptable salt thereof, as antitumor agents, wherein R is -OCOR1 group wherein R1 is hydrogen atom, a C1-9 alkyl group which may be substituted by either one or two substituents selected together from halogen atom, hydroxy, carboxy group or (3RS, 5SR)-(4-oxa-1-azabicyclo[3,2,0]heptan-7-one-3-yl)methyloxycarbonyl, a C2-17 alkenyl group, which may be substituted by carboxy group or (3RS, 5SR)-(4-oxa-1-azabicyclo[3,2,0]heptan-7-one-3-yl)methyloxycarbonyl, a C2-4 alkynyl group, a C3-6 cycloalkyl group which may be substituted by carboxy group or phenyl group which may have 1, 2 or 3 substituents selected from the group consisting of cyano group, halogen atom, C1-6 alkoxy group which may be substituted by carboxy group, C1-6 alkyl group, amino group or hydroxy group. -OR2 wherein R2 is a hydrogen atom or benzyl group which may be substituted by 1 or 2 C1-6 alkoxy group. -S(O)nR3 wherein R3 is phenyl group or a benzyl group which may be substituted by C1-6 alkyl group, n is 0, 1 or 2; or -CH2OH.
摘要翻译：本发明涉及式（I）的4-氧杂-1-氮杂双环[3,2,0]庚-7-酮衍生物或其药学上可接受的盐作为抗肿瘤剂，其中R是-OCOR1基团其中R 1是氢原子，可被卤素原子，羟基，羧基或（3RS，5SR） - （4-氧杂-1-氮杂双环[3，可以被羧基或（3RS，5SR） - （4-氧杂-1-氮杂双环[3,2,2]辛烷基）取代的C 1-7 - 烯基， 0]庚-7-酮-3-基）甲氧基羰基，C2-4炔基，可被羧基取代的C3-6环烷基或可具有1,2或3个选自下列基团的取代基的苯基由氰基，卤素原子，可被羧基取代的C 1-6烷氧基，C 1-6烷基，氨基或羟基组成。 -OR 2，其中R 2是可被1或2个C 1-6烷氧基取代的氢原子或苄基。 -S（O）n R 3，其中R 3为苯基或可被C 1-6烷基取代的苄基，n为0,1或2; 或-CH 2 OH。

9. 发明申请

WO1992013838A1 OLIGOPEPTIDE ANTIRETROVIRAL AGENTS 审中-公开
标题翻译：寡核苷酸抗体代理
公开(公告)号：WO1992013838A1
公开(公告)日：1992-08-20
申请号：PCT/CA1992000051
申请日：1992-02-05
申请人： SYNPHAR LABORATORIES, INC. , LOWN, J., William , MICETICH, Ronald, George
发明人： SYNPHAR LABORATORIES, INC.
IPC分类号： C07D207/34
CPC分类号： C07D401/14 , C07D207/34 , C07D233/90
摘要： Oligopeptide antiretroviral agents are represented by formula (I), wherein A is a moiety bearing a positive charge and of a size which avoids steric inhibition of binding of said compound to nucleic acid sequences associated with the cellular activity of retroviruses; R1 is a moiety derived from a dicarboxylic acid; Het is a five-membered heterocyclic moiety; y and z are independently 0, 1, 2 or 3; and x is 0 or 1. These compounds exhibit antiretroviral activity, especially against Human Immunodeficiency Virus (HIV).
摘要翻译：寡肽抗逆转录病毒剂由式（I）表示，其中A是具有正电荷和大小的部分，其避免空间抑制所述化合物与逆转录病毒细胞活性相关的核酸序列的结合; R1是衍生自二羧酸的部分; Het是五元杂环部分; y和z独立地为0,1,2或3; 这些化合物表现出抗逆转录病毒活性，特别是针对人类免疫缺陷病毒（HIV）。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式