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2. 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

3. 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。

4. 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。

5. 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。

6. 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。

7. 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。

8. 发明申请

WO1997046539A1 AMIDE DERIVATIVES OF SUBSTITUTED QUINOXALINE 2,3-DIONES AS GLUTAMATE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：取代的喹喔啉2,3-二酮作为谷氨酸受体拮抗剂的酰胺衍生物
公开(公告)号：WO1997046539A1
公开(公告)日：1997-12-11
申请号：PCT/US1997008525
申请日：1997-05-20
申请人： WARNER-LAMBERT COMPANY , NIKAM, Sham, S.
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D241/44
CPC分类号： C07D405/12 , C07D241/44 , C07D409/12
摘要： A novel series of substituted quinoxaline 2,3-diones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate receptor antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, seizure disorders, pain, Alzheimer's, Parkinson's, and Huntington's Diseases.
摘要翻译：教导了一系列用作神经保护剂的取代喹喔啉2,3-二酮。还教导了新的中间体，制备方法和含有这些化合物的药物组合物。这些化合物是谷氨酸受体拮抗剂，可用于治疗由血栓栓塞或出血性脑卒中，脑血管痉挛，低血糖症，心脏骤停，癫痫持续状态，围产期窒息，缺氧，癫痫发作，疼痛，阿尔茨海默氏症等引起的脑卒中，脑缺血或脑梗塞。，帕金森病和亨廷顿疾病。

9. 发明申请

WO1997045021A1 SUGAR COATED PRODUCTS AND PROCESS FOR PREPARING THE SAME 审中-公开
标题翻译：糖包衣制品及其制备方法
公开(公告)号：WO1997045021A1
公开(公告)日：1997-12-04
申请号：PCT/US1997008098
申请日：1997-05-13
申请人： WARNER-LAMBERT COMPANY , HAKAMATA, Tetsuya , MOCHIZUKI, Yasuhiro , NODA, Yasuo
发明人： WARNER-LAMBERT COMPANY
IPC分类号： A23G03/00
CPC分类号： A23G3/54 , A23G3/343 , A23G4/06 , A23G4/10 , A23G4/20 , A23G2200/00 , A23G2200/06
摘要： Improved sugar coated products having a hard coating of a fruity taste which are prepared by applying a hard coating composed of a sugar alcohol over the surface of an edible core material, a layer of said hard coating containing a sour agent.
摘要翻译：通过将由糖醇组成的硬涂层涂覆在可食用芯材的表面上的硬糖皮层，含有酸性试剂的所述硬涂层制成的具有水果味硬涂层的改进的糖衣制品。

10. 发明申请

WO1997044314A1 N-ACYL SULFAMIC ACID ESTERS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS 审中-公开
标题翻译： N-乙酰基硫酸酯有机物作为高效液相色谱
公开(公告)号：WO1997044314A1
公开(公告)日：1997-11-27
申请号：PCT/US1997006725
申请日：1997-04-21
申请人： WARNER-LAMBERT COMPANY , LEE, Helen, Tsenwhei , PICARD, Joseph, Armand , ROARK, William, Howard , ROTH, Bruce, David , SLISKOVIC, Drago, Robert
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07C307/02
CPC分类号： C07C307/02 , C07C311/08 , C07C311/44 , C07C323/60 , C07D209/20
摘要： The instant invention is new compounds of formula (I), wherein R is -CN, -(CH2)0-1-NR R , -O-(CH2)1-10-Z wherein Z is -NR R , OR , or CO2R , -OC(=O)R , -SR , -SCN, -S(CH2)1-10Z, -S(O)1-2R wherein R is hydroxy, alkoxy, alkyl, (CH2)1-10Z or NR R , -C(=O)XR , -CH2-R wherein R is (CH2)0-5-Y-(CH2)0-5Z, or alkyl with from 1-3 double bonds, which alkyl is optionally substituted by one or more selected from -CN, NO2, halogen, OR , NR R , and CO2R ; their use as cerebrovascular agents in diseases such as stroke, peripheral vascular disease, restenosis, and as agents for regulating plasma cholesterol concentrations, for treating hypercholesterolemia and atherosclerosis, and for lowering the serum or plasma level of Lp(a). A pharmaceutical composition is also claimed.
摘要翻译：本发明是新的式（I）化合物，其中R 6是-CN， - （CH 2）0-1 -NR 7 R 8，-O-（CH 2）1-10 -Z，其中 Z是-NR 9 R 10，OR 1或CO 2 R 1，-OC（= O）R 11，-SR 11，-SCN，-S（CH 2） 10Z，-S（O）1-2R 12其中R 12是羟基，烷氧基，烷基，（CH 2）1-10Z或NR 7 R 8，-C（= O）X R 11 其中R 13为（CH 2）0-5-Y-（CH 2）0-5Z，或具有1-3个双键的烷基，该烷基任选被一个或多个选自-CN，NO 2，卤素，OR 1，NR 9 R 10和CO 2 R 1; 它们用作中风，外周血管疾病，再狭窄等疾病中的脑血管因子，以及用于调节血浆胆固醇浓度的药剂，用于治疗高胆固醇血症和动脉粥样硬化，以及降低Lp（a）的血清或血浆水平。还要求药物组合物。

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