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1. 发明申请

WO1989001933A2 4-QUINOLINE-3-CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译： 4-QUINOLIN-3-羧酸衍生物及其作为抗菌剂的用途
公开(公告)号：WO1989001933A2
公开(公告)日：1989-03-09
申请号：PCT/US1988002938
申请日：1988-08-23
申请人： WARNER-LAMBERT COMPANY , CULBERTSON, Townley, Payne , DOMAGALA, John, Michael , HAGEN, Susan, Elizabeth , SANCHEZ, Josheph, Peter
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D215/56
CPC分类号： C07D207/08 , C07D207/09 , C07D207/12 , C07D207/20 , C07D211/34 , C07D211/52 , C07D211/70 , C07D215/56 , C07D401/04
摘要： A novel series of quinoline-, naphthyridine- and benzoxazine-carboxylic acids (I), useful as antibacterial agents is described. Novel methods for preparing the compounds as well as novel intermediates are also described as are methods for their formulation and the use thereof in treating bacterial infections. In formula (I), where Z is (II), wherein one endocyclic double bond may be present between any two consecutive ring positions or two alternating or nonalternating endocyclic double bonds may be present in the ring; wherein n, n', n''', and n"" are each independently 0, 1, or 2; n'' is 0, 1, 2, or 3; y is 0 or 1; x is 0 or 1; A and B are each independently CH, CH2, NR7 wherein R7 is hydrogen or R7 is R8CO wherein R8 is alkyl of from one to ten carbon atoms, arylalkyl, aryl wherein the aryl or alkyl may be substituted by hydroxy, halogen, COOH, or CONHR9 where R9 is hydrogen or alkyl of from one to four carbon atoms and when A is NR7, B can be O or S or when B is NR7, A can be absent; (CR13R14)n''' wherein R13 and R14 are each independently hydrogen or lower alkyl and E is hydrogen, alkyl, OR10 wherein R10 is hydrogen or alkyl, NR11R12 wherein R11 and R12 are each independently hydrogen, lower alkyl, cycloalkyl, alkylaryl, alkylheteroaryl, alkanoyl, amidine, peptide, urethane, or R11 and R14 when taken together with the nitrogen to which they are attached form a ring of from three to six carbon atoms or (a), (b), or (c).
摘要翻译：描述了一系列可用作抗菌剂的喹啉 - ，萘啶 - 和苯并恶嗪羧酸（I）。还公开了制备这些化合物的新方法以及新的中间体。还描述了它们的制剂方法和它们在治疗细菌感染中的用途。这些新的酸具有其中Z是由式（II）表示，其中桥环双键可以是连续的周期的任何两个位置，或两个双键内环交替或之间存在的式（I）不交替可目前的周期; 其中n，n'，n''和n“'独立地为0,1或2; n“是0,1,2或3; y是0或1; x是0或1; A和B各自独立地为CH，CH 2，NR 7，其中R 7为氢或R 7为R 8 CO，其中R 8为1-10个碳原子的烷基，芳基烷基，芳基，芳基等。该烷基可以被羟基，卤素，COOH或CONHR9取代，其中R9是氢或具有1至4个碳原子的烷基，并且当A是NR7时，B是O或S，或者当B是 NR7，A可能不存在; 其中R 13和R 14各自独立地为氢或低级烷基，E为氢，烷基，OR 10，其中R 10为氢或烷基，NR 11 R 12，其中R 11和R 12各自独立地为氢，低级烷基，环烷基，烷基芳基，烷基杂芳基，生物碱，脒，肽，氨基甲酸酯或R 11和R 14与它们所连接的氮一起形成环（a），（b）或（c）。

3. 发明申请

WO1989006649A2 ANTIBACTERIAL AGENTS 审中-公开
标题翻译：抗菌剂
公开(公告)号：WO1989006649A2
公开(公告)日：1989-07-27
申请号：PCT/US1989000278
申请日：1989-01-23
申请人： WARNER-LAMBERT COMPANY , DOMAGALA, John, Michael , HAGEN, Susan, Elizabeth , KIELY, John, Steven
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D215/56
CPC分类号： C07D263/10 , C07D215/56 , C07D401/04 , C07D451/04 , C07D471/04 , C07D471/08 , C07D487/08 , C07F7/0812
摘要： Novel naphthyridine-, and quinolinecarboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.

4. 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。

5. 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

6. 发明申请

WO1998016504A2 SULFONAMIDE SUBSTITUTED ASPARTIC ACID INTERLEUKIN-1'beta' CONVERTING ENZYME INHIBITORS 审中-公开
标题翻译：磺酰胺取代的ASPARTIC ACID INTERLEUKIN-1 beta转化酶抑制剂
公开(公告)号：WO1998016504A2
公开(公告)日：1998-04-23
申请号：PCT/US1997018406
申请日：1997-10-09
申请人： WARNER-LAMBERT COMPANY , ALLEN, Hamish, John , BRADY, Kenneth, Dale , HARTER, William, Glen , LUNNEY, Elizabeth, Ann , PLUMMER, Mark, Stephen , SAWYER, Tomi , SHAHRIPOUR, Aurash , WALKER, Nigel
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07C311/00
CPC分类号： C07D307/12 , C07C311/19 , C07C311/29 , C07C311/46 , C07C323/67 , C07C2601/14 , C07C2602/10
摘要： The present invention relates to compounds that are inhibitors of interleukin-1 beta converting enzyme that have Formula (I, II or III). This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock, reperfusion injury, Alzheimer's disease, and shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1 beta converting enzyme.
摘要翻译：本发明涉及具有式（I，II或III）的白细胞介素-1β转换酶的抑制剂的化合物。本发明还涉及治疗中风，炎性疾病，败血性休克，再灌注损伤，阿尔茨海默病和志贺氏菌病的方法，以及含有作为白细胞介素-1β转换酶抑制剂的化合物的药学上可接受的组合物。

7. 发明申请

WO1998011090A2 3-ALKYL-3-PHENYL-PIPERIDINES 审中-公开
标题翻译： 3-烷基-3-苯基 - 哌啶
公开(公告)号：WO1998011090A2
公开(公告)日：1998-03-19
申请号：PCT/US1997015443
申请日：1997-09-02
申请人： WARNER-LAMBERT COMPANY , CHEN, Michael, Huai, Gu , CHUNG, Fu-Zon , LEE, Helen, Tsenwhei
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D401/00
CPC分类号： C07D401/14 , C07D211/22 , C07D211/26 , C07D211/48 , C07D211/52 , C07D309/12 , C07D405/06
摘要： The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.
摘要翻译：本发明的小非肽是速激肽拮抗剂。这些化合物是高度选择性和功能性的NK3拮抗剂，预期可用于治疗疼痛，抑郁症，焦虑症，恐慌症，精神分裂症，神经痛，成瘾症，炎性疾病，胃肠道疾病，血管疾病和神经病理学疾病。

8. 发明申请

WO1998006711A1 BUTYRIC ACID MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：丁酸基金属蛋白酶抑制剂
公开(公告)号：WO1998006711A1
公开(公告)日：1998-02-19
申请号：PCT/US1997012389
申请日：1997-07-16
申请人： WARNER-LAMBERT COMPANY , SLISKOVIC, Drago, Robert , PICARD, Joseph, Armand
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D307/91
CPC分类号： C07D307/91 , C07D405/12 , C07D407/12 , C07D409/12
摘要： Compounds of formula (I) wherein R1 and R2 include hydrogen, alkyl, substituted alkyl, halo, and arylalkyl; R3 is hydroxy, alkoxy, or hydroxyamino; X is O, S, or NOH; and R4 and R5 include hydrogen, alkyl, and aryl, are useful for inhibiting matrix metalloproteinase enzymes in animals, and as such, prevent and treat diseases resulting from the breakdown of connective tissues.
摘要翻译：其中R1和R2包括氢，烷基，取代的烷基，卤素和芳基烷基的式（Ⅰ）化合物; R3是羟基，烷氧基或羟基氨基; X是O，S或NOH; R4和R5包括氢，烷基和芳基，可用于抑制动物中的基质金属蛋白酶，从而预防和治疗由结缔组织破坏引起的疾病。

9. 发明申请

WO1998006703A1 2-PHENYL BENZIMIDAZOLE DERIVATIVES AS MCP-1 ANTAGONISTS 审中-公开
标题翻译：作为MCP-1拮抗剂的2-苯基苯并咪唑衍生物
公开(公告)号：WO1998006703A1
公开(公告)日：1998-02-19
申请号：PCT/US1997013870
申请日：1997-08-06
申请人： WARNER-LAMBERT COMPANY , CONNOR, David, Thomas , GLASE, Shelly, Ann , PURCHASE, Terri, Stoeber , ROTH, Bruce, David , TRIVEDI, Bharat, Kalidas
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D235/18
CPC分类号： C07D235/02 , C07D235/18
摘要： Benzimidazole derivatives of formula (I) or a pharmaceutically acceptable salt thereof are MCP-1 antagonists and are thus useful in the treatment of inflammation, artherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection wherein A is N or CH; where W, X, Y and Z can be independently C-R2, C-R3, C-R4, C-R5, or N; no more than two of W, X, Y and Z can be N in any one structure, R2, R3, R4 and R5 can be independently H, C1-20 alkyl, halogen, nitro, -SO2NR8R9, alkoxy of from 1-4 carbon atoms; -S(O)pR where p is an integer from 0 to 2; -(CH2)mOR, -(CH2)mCOOR, -(CH2)mNR8R9, -(CH2)mCONR8R9, -(CH2)mCOR, or -CF3; m is an integer of from 0 to 4, R is hydrogen, lower alkyl of from 1-4 carbon atoms, aryl of from 6-10 carbon atoms, or benzyl; R1 can be H, lower alkyl of from 1-4 carbon atoms, or -(CH2)m-Ph; R6 is alkyl of from 1-6 carbon atoms or R7; R7 is (CH2)nNR10R11; n is an integer from 2 to 6; R8 and R9 can be independently hydrogen, lower alkyl of from 1-4 carbon atoms, or can be taken together to form a ring of from 3-8 atoms having up to one additional heteroatom as O, S, SO2, or N-R12; R10 and R11 can independently be lower alkyl, -(CH2)mPh, unsubstituted or substituted with up to three R2 substituents, or R10 and R11 can be taken together to form a ring of from 3-8 atoms which may contain oxygen or NR12; R12 is hydrogen, lower alkyl, -(CH2)tPh, where Ph is phenyl unsubstituted or substituted with up to three R2 substituents; t is an integer of from 0 to 2.
摘要翻译：式（I）的苯并咪唑衍生物或其药学上可接受的盐是MCP-1拮抗剂，因此可用于治疗炎症，动脉粥样硬化，再狭窄和免疫疾病如关节炎和移植排斥，其中A是N或CH; 其中W，X，Y和Z可以独立地为C-R2，C-R3，C-R4，C-R5或N; 不超过两个W，X，Y和Z可以是任何一个结构中的N，R2，R3，R4和R5可以独立地是H，C1-20烷基，卤素，硝基，-SO2NR8R9，1-4的烷氧基碳原子 -S（O）p R，其中p是0至2的整数; - （CH 2）m COOR， - （CH 2）m COOR， - （CH 2）m NR 8 R 9， - （CH 2）m CONR 8 R 9， - （CH 2）m -COR或-CF 3; m为0-4的整数，R为氢，1-4个碳原子的低级烷基，6-10个碳原子的芳基或苄基; R1可以是H，1-4个碳原子的低级烷基，或 - （CH2）m-Ph; R6是1-6个碳原子的烷基或R7; R7是（CH2）nNR10R11; n为2-6的整数; R 8和R 9可以独立地为氢，1-4个碳原子的低级烷基，或者可以一起形成具有至多一个另外的杂原子的3-8个原子的环作为O，S，SO2或N-R12 ; R 10和R 11可以独立地为低级烷基， - （CH 2）m Ph，未被取代或被至多三个R 2取代基取代，或者R 10和R 11可以一起形成可含有氧或NR 12的3-8个原子的环; R 12是氢，低级烷基， - （CH 2）t Ph，其中Ph是未被取代或被至多三个R 2取代基取代的苯基; t是0到2的整数。

10. 发明申请

WO1998002160A1 METHOD FOR TREATING AND PREVENTING NEURODEGENERATIVE DISORDERS BY ADMINISTERING A THIAZOLIDINONE 审中-公开
标题翻译：通过管理噻唑烷酮治疗和预防神经损伤性疾病的方法
公开(公告)号：WO1998002160A1
公开(公告)日：1998-01-22
申请号：PCT/US1997011586
申请日：1997-07-01
申请人： WARNER-LAMBERT COMPANY , CARROLL, Richard, Thomas , DYER, Richard, Dennis , ROBICHAUD, Lillian, Jane , SHIVERS, Brenda, De Rae
发明人： WARNER-LAMBERT COMPANY
IPC分类号： A61K31/425
CPC分类号： A61K31/426
摘要： Neurodegenerative disorders such as Alzheimer's disease, stroke, multiple sclerosis, and head trauma are treated and prevented with 5-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]-2-imino-4-thiazolidinone or a pharmaceutically acceptable salt thereof.
摘要翻译：使用5 - [[3,5-双（1,1-二甲基乙基）-4-羟基苯基]亚甲基] -2-亚氨基-4-甲基苯酚处理和预防神经变性疾病如阿尔茨海默病，中风，多发性硬化和头部外伤，噻唑烷酮或其药学上可接受的盐。

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