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1. 发明申请

WO1998009957A1 COMPOUNDS FOR AND A METHOD OF INHIBITING MATRIX METALLOPROTEINASES 审中-公开
标题翻译：用于抑制基质金属蛋白酶的方法和方法
公开(公告)号：WO1998009957A1
公开(公告)日：1998-03-12
申请号：PCT/US1997015444
申请日：1997-09-02
申请人： WARNER-LAMBERT COMPANY , PICARD, Joseph, Armand , SLISKOVIC, Drago, Robert
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D307/91
CPC分类号： C07D307/91 , C07C311/19 , C07D333/76
摘要： The present invention relates to compounds of formula (I) that inhibit matrix metalloproteinases and to a method of inhibiting matrix metalloproteinases using the compounds, wherein Q is an un-natural amino acid. More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal diseases, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disases dependent upon tissue invasion by leukocytes.
摘要翻译：本发明涉及抑制基质金属蛋白酶的式（I）化合物和使用其中Q是非天然氨基酸的化合物抑制基质金属蛋白酶的方法。更具体地，本发明涉及一种治疗涉及基质金属蛋白酶的疾病的方法，例如多发性硬化，动脉粥样硬化斑块破裂，再狭窄，主动脉瘤，心力衰竭，牙周病，角膜溃疡，烧伤，褥疮性溃疡，慢性溃疡或慢性溃疡伤口，癌症转移，肿瘤血管发生，关节炎或依赖于白细胞组织侵袭的其他自身免疫性或炎症性疾病。

2. 发明申请

WO1998009934A1 MATRIX METALLOPROTEINASE INHIBITORS AND THEIR THERAPEUTIC USES 审中-公开
标题翻译：基质金属蛋白酶抑制剂及其治疗用途
公开(公告)号：WO1998009934A1
公开(公告)日：1998-03-12
申请号：PCT/US1997014859
申请日：1997-08-22
申请人： WARNER-LAMBERT COMPANY , O'BRIEN, Patrick, Michael , PICARD, Joseph, Armand , SLISKOVIC, Drago, Robert , WHITE, Andrew, David
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07C35/38
CPC分类号： C07D307/91 , A61K31/343 , A61K31/381 , C07C311/19 , C07C2603/18 , C07D333/76
摘要： The present invention relates to a method of inhibiting matrix metalloproteinases using compounds that are dibenzofuran sulfonamide derivatives having Formula (I). More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.
摘要翻译：本发明涉及使用具有式（I）的二苯并呋喃磺酰胺衍生物的化合物抑制基质金属蛋白酶的方法。更具体地，本发明涉及一种治疗涉及基质金属蛋白酶的疾病的方法，例如多发性硬化，动脉粥样硬化斑块破裂，再狭窄，主动脉瘤，心力衰竭，牙周病，角膜溃疡，烧伤，褥疮性溃疡，慢性溃疡或慢性溃疡伤口，癌症转移，肿瘤血管生成，关节炎或依赖于白细胞组织侵袭的其他自身免疫性或炎性疾病。

3. 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。

4. 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。

5. 发明申请

WO1988004657A2 TRANS-6-[2-[2-(SUBSTITUTED-PHENYL)-3- (or 4-) HETEROARYL-5-SUBSTITUTED-1H-PYRROL-1-YL]-ETHYL]TETRAHYDRO-4-HYDROXY-2H-PYRAN-2-ONE INHIBITORS OF CHOLESTEROL BIOSYNTHESIS 审中-公开
标题翻译：反式-6- [2- [2-（取代的苯基）-3-（或4-）取代的5-取代的1H-吡咯-1-基] - 乙基]四氢-4-羟基-2H- 胆碱醇生物合成2-ONE抑制剂
公开(公告)号：WO1988004657A2
公开(公告)日：1988-06-30
申请号：PCT/US1987003047
申请日：1987-11-23
申请人： WARNER-LAMBERT COMPANY , ROTH, Bruce, David , SLISKOVIC, Drago, Robert
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D405/14
CPC分类号： C07D405/14
摘要： Certain trans-6-[2-[2-(substituted-phenyl)-3- (or 4-)heteroaryl-5-substituted-1H-pyrrol-1-yl]ethyl]tetrahydro-4-hydroxy-2H-pyran-2-ones and the corresponding lactone-ring-opened acids are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG CoA reductase) and are thus useful hypolipidemic or hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of inhibiting the biosynthesis of cholesterol employing such pharmaceutical compositions are also disclosed.

7. 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

8. 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。

9. 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。

10. 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。

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