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1. 发明申请

WO2005014539A3 PYRROLE-BASED HMG-COA REDUCTASE INHIBITORS 审中-公开
标题翻译：基于PYRROLE的HMG-COA还原抑制剂
公开(公告)号：WO2005014539A3
公开(公告)日：2005-05-12
申请号：PCT/IB2004002540
申请日：2004-07-30
申请人： WARNER LAMBERT CO , KENNEDY ROBERT MICHAEL , PARK WILLIAM KEUN-CHAN , ROTH BRUCE DAVID , SONG YUNTAO , TRIVEDI BHARAT KALIDAS
发明人： KENNEDY ROBERT MICHAEL , PARK WILLIAM KEUN-CHAN , ROTH BRUCE DAVID , SONG YUNTAO , TRIVEDI BHARAT KALIDAS
IPC分类号： C07C303/40 , C07C311/13 , C07D207/32 , C07D207/33 , C07D207/34 , C07D207/36 , C07D319/06 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , A61K31/40 , A61K31/4025 , A61P3/06 , C07C311/11
CPC分类号： C04B35/632 , C07C303/40 , C07C311/13 , C07D207/33 , C07D207/34 , C07D207/36 , C07D319/06 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14
摘要： HMGCo-A reductase inhibitor compounds of formula (I) useful as hypocholesterolemic and hypolipidemic compounds are provided. Also provided are pharmaceutical compositions of the compounds. Methods of making and methods of using the compounds are also provided.
摘要翻译：提供了可用作低胆固醇血症和降血脂化合物的式（I）的HMGCo-A还原酶抑制剂化合物。还提供了化合物的药物组合物。还提供了制备方法和使用该化合物的方法。

2. 发明申请

WO1998009940A1 BIPHENYL BUTYRIC ACIDS AND THEIR DERIVATIVES AS INHIBITORS OF MATRIX METALLOPROTEINASES 审中-公开
标题翻译：二苯基丁酸及其作为基质金属蛋白酶抑制剂的衍生物
公开(公告)号：WO1998009940A1
公开(公告)日：1998-03-12
申请号：PCT/US1997014852
申请日：1997-08-22
申请人： WARNER-LAMBERT COMPANY , PURCHASE, Claude, Forsey, Jr. , ROTH, Bruce, David , WHITE, Andrew, David , SCHIELKE, Gerald, Paul , WALKER, Lary, Craswell
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07C251/48
CPC分类号： C07C323/63 , C07C59/56 , C07C59/84 , C07C59/88 , C07C59/90 , C07C69/738 , C07C251/48 , C07C251/86 , C07C255/64
摘要： Biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.
摘要翻译：描述了联苯丁酸化合物和衍生物以及用于制备的酸法和其药物组合物，其可用作基质金属蛋白酶抑制剂，特别是明胶酶A（72kD明胶酶）和基质溶素-1和用于治疗多发性硬化症，动脉粥样硬化斑块破裂，主动脉瘤，心力衰竭，再狭窄，牙周病，角膜溃疡，烧伤治疗，褥疮性溃疡，伤口愈合，癌症，炎症，疼痛，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病症，其他活化的迁移细胞，急性和慢性神经变性疾病，包括中风，头部创伤，脊髓损伤，阿尔茨海默病，肌萎缩性侧索硬化，脑淀粉样血管病，艾滋病，帕金森病，亨廷顿病，朊病毒疾病，重症肌无力和杜氏肌营养不良症。

3. 发明申请

WO1989007598A2 IMPROVED PROCESS FOR TRANS-6-[2-(SUBSTITUTED-PYRROL-1-YL)ALKYL]PYRAN-2-ONE INHIBITORS OF CHOLESTEROL SYNTHESIS 审中-公开
标题翻译：改进方法TRANS-6- [2-（取代的吡咯-1-基）烷基]吡喃-2-酮抑制剂胆固醇的合成
公开(公告)号：WO1989007598A2
公开(公告)日：1989-08-24
申请号：PCT/US1989000719
申请日：1989-02-22
申请人： WARNER-LAMBERT COMPANY , BUTLER, Donald, Eugene , DEERING, Carl, Francis , MILLAR, Alan , NANNINGA, Thomas, Norman , ROTH, Bruce, David
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D405/06
CPC分类号： C07D319/08 , C07C235/80 , C07D207/34 , C07D319/06 , C07D405/06
摘要： An improved process for the preparation of trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where 1,6-heptadien-4-ol is converted in eight operations to the desired products, as well as an improved process for the preparation of (2R-trans) and trans-(U)-5-(4-fluoro-phenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide by a novel synthesis where 4-methyl-3-oxo-N-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-alpha-[2-methyl-1-oxopropyl]-gamma-oxo-N,beta-diphenylbenzenebutaneamide is converted in one step to the desired product, and additionally, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide from (R)-4-cyano-3-[[(1,1-dimethylethyl)dimethylsilyl]oxy]butanoic acid, as well as other valuable intermediates used in the processes.
摘要翻译：它已经开发了一种改进的方法，用于反式-6-的制备[2-（取代的吡咯-1-基）烷基]吡喃-2-酮由一个新的合成装置，用于将1,6-heptadiène- 在所需产品中进行8次操作。制备（2R-反式）和反式 - （U）-5-（4-氟 - 苯基）-2-（1-甲基乙基）-N，4-二苯基-1的改进方法也被开发出来。 [2-（四氢-4-羟基-6-氧代-2H-吡喃-2-基）乙基]使用新的合成用于将4-甲基-3-氧代-1H-吡咯-3-甲酰胺 -N苯基戊酰胺在八个操作中，期望的产物或在另一个实施方案中变换4-氟-α-[2-甲基-1-氧代丙基〕-gamma氧代-N，β-diphénylbenzènebutaneamide在一个步骤中在期望的产品中。已经进一步开发出一种方法，用于制备式（2R-反式）-5-（4-flurophényle）-2-（1-甲基乙基）-N，4-二苯基-1- [2-（四氢 4-羟基-6-氧代-2H-吡喃-2-基）乙基]从（R）-4-氰基-3- -1H-吡咯-3-甲酰胺 - [[（1,1-二甲乙基）二甲基甲硅烷 ]氧]丁酸，以及在该方法中使用的其他有价值的中间体。

4. 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.

5. 发明申请

WO2005014539A2 NOVEL PYRROLE-BASED HMG-COA REDUCTASE INHIBITORS 审中-公开
标题翻译：基于PYRROLE的HMG-COA还原抑制剂
公开(公告)号：WO2005014539A2
公开(公告)日：2005-02-17
申请号：PCT/IB2004/002540
申请日：2004-07-30
申请人： WARNER-LAMBERT COMPANY LLC , KENNEDY, Robert, Michael , PARK, William, Keun-Chan , ROTH, Bruce, David , SONG, Yuntao , TRIVEDI, Bharat, Kalidas
发明人： KENNEDY, Robert, Michael , PARK, William, Keun-Chan , ROTH, Bruce, David , SONG, Yuntao , TRIVEDI, Bharat, Kalidas
IPC分类号： C07D207/00
CPC分类号： C04B35/632 , C07C303/40 , C07C311/13 , C07D207/33 , C07D207/34 , C07D207/36 , C07D319/06 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14
摘要： HMGCo-A reductase inhibitor compounds useful as hypocholesterolemic and hypolipidemic compounds are provided. Also provided are pharmaceutical compositions of the compounds. Method of making and methods of using the compounds are also provided.
摘要翻译：提供了可用作低胆固醇血症和降血脂化合物的HMGCo-A还原酶抑制剂化合物。还提供了化合物的药物组合物。还提供了制备方法和使用该化合物的方法。

6. 发明申请

WO1998016505A1 SULFONAMIDE INTERLEUKIN-1'beta' CONVERTING ENZYME INHIBITORS 审中-公开
标题翻译： SULFONAMIDE INTERLEUKIN-1 beta转化酶抑制剂
公开(公告)号：WO1998016505A1
公开(公告)日：1998-04-23
申请号：PCT/US1997018396
申请日：1997-10-09
申请人： WARNER-LAMBERT COMPANY , ALBRECHT, Hans, P. , ALLEN, Hamish, John , BRADY, Kenneth, Dale , HARTER, William, Glen , KOSTLAN, Catherine, Rose , ROTH, Bruce, David , WALKER, Nigel
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07C311/13
CPC分类号： C07K5/1024 , A61K38/00 , C07C311/06 , C07C311/19 , C07C2601/14 , C07C2602/08 , C07C2602/42 , C07C2603/18 , C07D217/24 , C07K5/06026 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06104 , C07K5/06139 , C07K5/0804 , C07K5/0812 , C07K5/0815 , C07K5/0819 , C07K5/0821 , C07K5/1005 , C07K5/1016 , C07K5/1019 , C07K5/1021
摘要： The present invention relates to compounds that are inhibitors of interleukin-1 beta converting enzyme that have the Formula (I). This invention also relates to a method of treatment of stroke, reperfusion injury, Alzheimer's disease, shigellosis, inflammatory diseases, and septic shock 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）的白细胞介素-1β转换酶抑制剂的化合物。本发明还涉及治疗中风，再灌注损伤，阿尔茨海默病，志贺氏菌病，炎性疾病和败血性休克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

WO8804657A3 TRANS-6-(2-(2-(SUBSTITUTED-PHENYL)-2-(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）-2-（OR-4-）杂芳基-5-取代-1H-吡咯-1-基） - 乙基）四氢-4-羟基-2H-吡喃 2-酮胆固醇生物合成抑制剂
公开(公告)号：WO8804657A3
公开(公告)日：1988-12-01
申请号：PCT/US8703047
申请日：1987-11-23
申请人： WARNER LAMBERT CO , ROTH BRUCE DAVID , SLISKOVIC DRAGO ROBERT
发明人： ROTH BRUCE DAVID , SLISKOVIC DRAGO ROBERT
IPC分类号： C07D405/14 , C07D409/14
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.

8. 发明申请

WO0042045A3 FUNCTIONALIZED HETEROCYCLES AS CHEMOKINE RECEPTOR MODULATORS 审中-公开
标题翻译：作为化学受体调节剂的功能化杂环化合物
公开(公告)号：WO0042045A3
公开(公告)日：2000-11-09
申请号：PCT/US9930434
申请日：1999-12-20
申请人： WARNER LAMBERT CO , HARRIMAN GERALDINE C , KOLZ CHRISTINE NYLUND , LULY JAY R , ROTH BRUCE DAVID , SONG YUNTAO , TRIVEDI BHARAT KALIDAS
发明人： HARRIMAN GERALDINE C , KOLZ CHRISTINE NYLUND , LULY JAY R , ROTH BRUCE DAVID , SONG YUNTAO , TRIVEDI BHARAT KALIDAS
IPC分类号： C07D491/147 , A61K31/437 , A61K31/4375 , A61P31/18 , C07D455/02 , C07D491/14 , C07D491/22 , A61K31/436 , A61K31/438
CPC分类号： C07D491/14 , C07D455/02
摘要： The present invention is a novel series of functionalized heterocycles as chemokine receptor modulators of Formula (I) useful as modulators of chemokine receptor activity. The compounds are useful in the treatment and prevention of the AIDS virus. Intermediates useful in the prepartion of the final products, pharmaceutical compositions containing the final products are also taught.
摘要翻译：本发明是用作趋化因子受体活性调节剂的式（I）的趋化因子受体调节剂的新一系列官能化杂环。该化合物可用于治疗和预防艾滋病病毒。还介绍了可用于最终产品制备的中间体，含有最终产品的药物组合物。

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

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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