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1. 发明申请

WO2002089806A1 HETEROBICYCLES FKBP-LIGANDS 审中-公开
标题翻译：杂环化合物FKBP-LIGANDS
公开(公告)号：WO2002089806A1
公开(公告)日：2002-11-14
申请号：PCT/US2002/014966
申请日：2002-05-10
申请人： AGOURON PHARMACEUTICALS, INC. , GUO, Chuangxing , AUGELLI-SZAFRAN, Corinne, E. , BARTA, Nancy, Sue , BENDER, Steven, Lee , BIGGE, Christopher, Franklin , CAPRATHE, Bradley, William , CHATTERJEE, Arindam , DEAL, Judith , DONG, Liming , FAY, Lorraine, Kathleen , HOU, Xinjun , HUDACK, Raymond, Andrew, Jr. , WARNER-LAMBERT COMPANY
发明人： GUO, Chuangxing , AUGELLI-SZAFRAN, Corinne, E. , BARTA, Nancy, Sue , BENDER, Steven, Lee , BIGGE, Christopher, Franklin , CAPRATHE, Bradley, William , CHATTERJEE, Arindam , DEAL, Judith , DONG, Liming , FAY, Lorraine, Kathleen , HOU, Xinjun , HUDACK, Raymond, Andrew, Jr. , WARNER-LAMBERT COMPANY
IPC分类号： A61K31/4995
CPC分类号： C07D471/08 , C07C57/58 , C07C59/64
摘要： Diazabicyclo[3.3.1]nonane derivatives that inhibit the peptidyl-prolyl isomerase enzyme activity associated with FK-506 binding proteins (FKBP) are described for treating neurological disorders. Also described are compounds useful for preparing such inhibitors.
摘要翻译：描述了抑制与FK-506结合蛋白（FKBP）相关的肽基 - 脯氨酰异构酶活性的二氮杂双环[3.3.1]壬烷衍生物用于治疗神经障碍。还描述了可用于制备这种抑制剂的化合物。

2. 发明申请

WO2003018553A1 ORAL ANTIDIABETIC AGENTS 审中-公开
标题翻译：口服抗生素
公开(公告)号：WO2003018553A1
公开(公告)日：2003-03-06
申请号：PCT/IB2002/002843
申请日：2002-07-15
申请人： WARNER-LAMBERT COMPANY LLC , BIGGE, Christopher, Franklin , BRIDGES, Alexander, James , CASIMIRO-GARCIA, Agustin , FAKHOURY, Stephen, Alan , LEE, Helen, Tsenwhei , REED, Jessica, Elizabeth , SCHAUM, Robert, Philipp , SCHLOSSER, Kevin, Matthew , SEXTON, Karen, Elaine , ZHOU, Hairong
发明人： BIGGE, Christopher, Franklin , BRIDGES, Alexander, James , CASIMIRO-GARCIA, Agustin , FAKHOURY, Stephen, Alan , LEE, Helen, Tsenwhei , REED, Jessica, Elizabeth , SCHAUM, Robert, Philipp , SCHLOSSER, Kevin, Matthew , SEXTON, Karen, Elaine , ZHOU, Hairong
IPC分类号： C07D207/32
CPC分类号： C07D207/325 , C07D207/327 , C07D207/34 , C07D209/08 , C07D263/32 , C07D263/58 , C07D277/26 , C07D309/38 , C07D401/10 , C07D401/12 , C07D403/12 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention provides compounds of Formula (I): f I wherein A, X, Q, Y, B, D, Z, and E have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful as antidiabetic agents. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, process for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.
摘要翻译：本发明提供式（I）的化合物：其中A，X，Q，Y，B，D，Z和E具有说明书中定义的任何值及其药学上可接受的盐，其可用作抗糖尿病药。还公开了包含一种或多种式I化合物，制备式I化合物的方法和可用于制备式I化合物的中间体的药物组合物。

3. 发明申请

WO2003045912A1 INHIBITORS OF FACTOR XA AND OTHER SERINE PROTEASES INVOLVED IN THE COAGULATION CASCADE 审中-公开
标题翻译：因子XA和其他丝氨酸蛋白酶在混合级联中的抑制剂
公开(公告)号：WO2003045912A1
公开(公告)日：2003-06-05
申请号：PCT/IB2002/004757
申请日：2002-11-14
申请人： WARNER-LAMBERT COMPANY LLC , BIGGE, Christopher, Franklin , DUDLEY, Danette, Andrea , EDMUNDS, Jeremy, John , VAN HUIS, Chad, Alan , CASIMIRO-GARCIA, Agustin , FILIPSKI, Kevin, James , KOHRT, Jeffrey, Thomas
发明人： BIGGE, Christopher, Franklin , DUDLEY, Danette, Andrea , EDMUNDS, Jeremy, John , VAN HUIS, Chad, Alan , CASIMIRO-GARCIA, Agustin , FILIPSKI, Kevin, James , KOHRT, Jeffrey, Thomas
IPC分类号： C07D207/16
CPC分类号： C07D231/12 , C07D207/16 , C07D207/20 , C07D207/22 , C07D207/24 , C07D207/26 , C07D207/27 , C07D211/76 , C07D213/64 , C07D231/06 , C07D233/56 , C07D237/14 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12
摘要： The present invention provides compounds of Formula (I), wherein A, B, C, G, and W 1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula (I), processes for preparing compounds of Formula (I), and intermediates useful for preparing compounds of Formula (I).
摘要翻译：本发明提供了式（I）的化合物，其中A，B，C，G和W 1具有本说明书中定义的任何值，并且是药学上可接受的它们可用于治疗血栓形成疾病。还公开了包含一种或多种式（I）化合物的药物组合物，制备式（I）化合物的方法和可用于制备式（I）化合物的中间体。

4. 发明申请

WO2003082276A1 ANTIDIABETIC AGENTS 审中-公开
标题翻译：抗真菌剂
公开(公告)号：WO2003082276A1
公开(公告)日：2003-10-09
申请号：PCT/IB2003/001131
申请日：2003-03-25
申请人： WARNER-LAMBERT COMPANY LLC , BIGGE, Christopher, Franklin , SCHAUM, Robert, Philipp
发明人： BIGGE, Christopher, Franklin , SCHAUM, Robert, Philipp
IPC分类号： A61K31/422
CPC分类号： C07D413/06
摘要： Compounds of formula (I): wherein X, Y, B, E, J, K, L, Z, and R 9 -R 12 have any of the meanings described herein, their pharmaceutically acceptable salts, lower blood glucose levels and are useful for treating diseases in mammals such as Non-Insulin Dependent Diabetes Mellitus. Also disclosed are pharmaceutical compositions, process for preparing compounds of formula (I) and intermediates useful for preparing compounds of formula (I).
摘要翻译：式（I）化合物：其中X，Y，B，E，J，K，L，Z和R9-R12具有本文所述的任何含义，其药学上可接受的盐，较低的血糖水平，并且可用于治疗哺乳动物疾病如非胰岛素依赖性糖尿病。还公开了药物组合物，制备式（I）化合物的方法和可用于制备式（I）化合物的中间体。

5. 发明申请

WO2008084303A1 COMPOUNDS HAVING BOTH ANGIOTENSIN II RECEPTOR ANTAGONISM AND PPARY ACTIVATING ACTIVITIES 审中-公开
标题翻译：具有两种血管紧张素II受体拮抗剂和药物活性的化合物
公开(公告)号：WO2008084303A1
公开(公告)日：2008-07-17
申请号：PCT/IB2007/003844
申请日：2007-12-03
申请人： PFIZER PRODUCTS INC. , BIGGE, Christopher, Franklin , CASIMIRO-GARCIA, Agustin , LEE, Chitase , RISLEY, Hud, Lawrence , SCHAUM, Robert, Philip
发明人： BIGGE, Christopher, Franklin , CASIMIRO-GARCIA, Agustin , LEE, Chitase , RISLEY, Hud, Lawrence , SCHAUM, Robert, Philip
IPC分类号： C07D471/04 , A61K31/437 , A61P3/10
CPC分类号： C07D471/04
摘要： Compounds of following formula (I) are provided that have both angiontensin Il receptor antagonist activity and PPARy agonist activity. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment of diseases with the compounds including type 2 diabetes, insulin resistance, hyperinsulinemia, hyperlipidemia, hypertriglyceridemia, metabolic syndrome, congestive heart failure, and hypertension.
摘要翻译：提供具有两种血管紧张素II受体拮抗剂活性和PPARγ激动剂活性的下式（I）的化合物。还提供了包含该化合物的药物组合物和用包括2型糖尿病，胰岛素抵抗，高胰岛素血症，高脂血症，高甘油三酯血症，代谢综合征，充血性心力衰竭和高血压的化合物治疗疾病的方法。

6. 发明申请

WO1993004688A1 PHARMACEUTICAL PREPARATION CONTAINING AN URICOSURIC AND AN EXCITATORY AMINO ACID ANTAGONIST 审中-公开
标题翻译：含有尿素酶和激素氨基酸拮抗剂的药物制剂
公开(公告)号：WO1993004688A1
公开(公告)日：1993-03-18
申请号：PCT/US1992007540
申请日：1992-09-02
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , BIGGE, Christopher, Franklin , JOHNSON, Graham , TAYLOR, Charles, Price, Jr. , WELTY, Devin, Franklin
IPC分类号： A61K31/675
CPC分类号： A61K31/675 , A61K31/18 , A61K31/47 , A61K31/495 , A61K45/06 , A61K31/19 , A61K2300/00
摘要： The present invention is a pharmaceutical composition having a combination of an uricosuric agent such as probenecid or the like and an excitatory amino acid antagonist useful for treating a disease advantageously affected by treatment with an excitatory amino acid antagonist.
摘要翻译：本发明是具有尿酸润滑剂如丙磺舒等的组合物和可用于治疗有利于用兴奋性氨基酸拮抗剂治疗影响的疾病的兴奋性氨基酸拮抗剂的药物组合物。

7. 发明申请

WO1994009000A1 QUINOXALINEDIONE DERIVATIVES AS EAA ANTAGONISTS 审中-公开
标题翻译：喹喔啉衍生物作为EAA拮抗剂
公开(公告)号：WO1994009000A1
公开(公告)日：1994-04-28
申请号：PCT/US1993009667
申请日：1993-10-08
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , BIGGE, Christopher, Franklin , MALONE, Thomas, Charles , WÄTJEN, Frank
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D217/04 , C07D487/04 , C07F9/6561
摘要： A compound having formula (I) or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or hydroxy; R is hydrogen, alkyl, arylalkyl, (CH2)nOH or (CH2)nNR R ; R and R are each independently hydrogen, halogen, NO2, CN, CF3, SO2NR R , PO3R R , alkyl, alkenyl, alkynyl, (CH2)nCONR R , (CH2)nCO2R , NHCOR , wherein R and R are each independently hydrogen or alkyl or together R and R form a ring of from three to seven atoms, R is hydrogen or alkyl, R is hydrogen or alkyl, R is hydrogen or alkyl, and n is an integer of from zero to four; A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b, and formed by the following bivalent radicals: a-NR -CHR -CHR -b, a-CHR -CHR -NR -b, a-CHR -NR -CHR -b, a-CHR -CH2-NR -CHR -b, a-CHR -NR -CH2-CHR -b, a-CH2-CH2-CHR -NR -b, a-NR -CHR -CH2-CH2-b, a-CH2-CH2-NR -CH2-CH2-b, a-CH2-CH2-CH2-NR -CH2-b, a-CH2-NR -CH2-CH2-CH2-b, a-CH2-CH2-CH2-CH2-NR -b, a-NR -CH2-CH2-CH2-CH2-b, wherein R is hydrogen, CH2CH2OH, or alkyl, and R and R are each independently hydrogen, CN, CONH2, CH2NH2, CH2OH, alkyl, arylalkyl, alkenyl or CO2R , wherein R is hydrogen or alkyl. The compounds are useful in the treatment of disorders of mammals, responsive to the blockade of glutamic and aspartic acid receptors. Processes for preparing the compounds and novel intermediate useful in the processes are also included.
摘要翻译：具有式（I）的化合物或其药学上可接受的盐，其中R是氢或羟基; R 1是氢，烷基，芳基烷基，（CH 2）n OH或（CH 2）n NR 7 R 8; R 5和R 6各自独立地为氢，卤素，NO 2，CN，CF 3，SO 2 NR 7，PO 3 R 9，R 10，烷基，烯基，炔基，（CH 2）nCONR R 8，（CH 2）n CO 2 R 10，NHCOR 11，其中R 7和R 8各自独立地为氢或烷基或一起R 7和R 8形成三个至七个原子的环，R 9是氢或烷基，R 10是氢或烷基，R 11是氢或烷基，n是0-4的整数; A是在标记a和b的位置与苯并环稠合的5至7个原子的环，并由以下二价基团形成：a-NR 12 -CHR 13 -CHR 14，a -CHR 13 -CHR 14 -NR 12 -b，a-CHR 13 -NR 12 -CHR 14 -b，a-CHR 14 -CH 2 -NR 12， -CHR 13 -b，a-CHR 13 -NR 12 -CH 2 -CHR 14，a-CH 2 -CH 2 -CHR 13 -NR 12 -b，-OR -CHR 13 -CH 2 -CH 2 -B，a-CH 2 -CH 2 -NR 12 -CH 2 -CH 2 -B，a-CH 2 -CH 2 -CH 2 -NR 12 -CH 2 -B，a -CH2-NR12 -CH2-CH2-CH2-b，a-CH2-CH2-CH2-CH2-NR12-b，-NR12 -CH2-CH2-CH2-CH2-b，其中R 12是氢，CH 2 CH 2 OH或烷基，R 13和R 14各自独立地是氢，CN，CONH 2，CH 2 NH 2，CH 2 OH，烷基，芳基烷基，烯基或CO 2 R 15， 15>是氢或烷基。该化合物可用于治疗对谷氨酸和天冬氨酸受体的阻断作用的哺乳动物疾病的治疗。还包括用于制备化合物的方法和用于该方法的新型中间体。

8. 发明申请

WO1992016205A2 NOVEL DERIVATIVES OF 2-CARBOXYNDOLES HAVING PHARMACEUTICAL ACTIVITY 审中-公开
标题翻译：具有药物活性的2-羧基嘌呤衍生物的新颖衍生物
公开(公告)号：WO1992016205A2
公开(公告)日：1992-10-01
申请号：PCT/US1992001699
申请日：1992-03-04
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , BIGGE, Christopher, Franklin , JOHNSON, Graham , YUEN, Po-wai
IPC分类号： A61K31/40
CPC分类号： C07D209/42
摘要： The present invention relates to novel 3-substituted-2-carboxyindoles; including as 3-substituents amides of hydroxamic acids and derivatives thereof or urea and carbonyl, carboxyl or phosphonic acids or ester amides, or 2-acylsulfon amides thereof; and including also as 3-substituents unsaturated acids and their further ester and amide derivatives. These 2-carboxyindoles are useful as pharmaceutical agents, therefore, the present invention is also pharmaceutical compositions and pharmaceutical methods of treatment therefor. The compounds of the present invention are useful in the treatment of neurodegenerative disorders including cerebrovascular disorders.
摘要翻译：本发明涉及在3-位取代的新颖的2-羧基吲哚化合物，其包含异羟肟酸酰胺和这些酸的衍生物或脲和羰基，羧基或膦酸或酯酰胺或它们的2-酰基砜酰胺，并且其在3位不饱和酸及其其他酯和酰胺衍生物中也含有取代基。这些2-羧基吲哚可用作药物，因此本发明还涉及使用这些组合物的药物组合物和治疗方法。所公开的化合物可用于治疗神经变性疾病，例如脑血管疾病。

9. 发明申请

WO1996028445A1 NOVEL GLUTAMATE (AMPA/KAINATE) RECEPTOR ANTAGONISTS: N-SUBSTITUTED FUSED AZACYCLOALKYLQUINOXALINEDIONES 审中-公开
标题翻译：新型谷氨酸（AMPA / KAINATE）受体拮抗剂：N-取代的熔融氮杂环丁烷氧基
公开(公告)号：WO1996028445A1
公开(公告)日：1996-09-19
申请号：PCT/US1995016306
申请日：1995-12-08
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , BIGGE, Christopher, Franklin , MALONE, Thomas, Charles , SCHELKUN, Robert, Michael , YI, Chung, Stephen
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D217/02 , C07D217/04 , C07D217/06
摘要： Novel N-substituded azacycloalkyl ring fused 2,3-quinoxalinediones of formula (I), pharmaceutical compositions containing the same and the method of using the same, for the blockade of glutamate receptors, including either or both N-methyl-D-aspartate (NMDA) receptors and non-NMDA receptors such as the alpha -amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor and the kainate receptor, are described. Method of preparing the N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones are also described. Novel intermediates of the inventive quinoxalinediones are disclosed. The novel N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones may be used, for example, as neuroprotective agents, for treatment of chronic neurodegenerative disorders, as anticonvulsants and in the treatment of schizophrenia, epilepsy, anxiety, pain and drug addiction. In formula (I) m and n are independently 0,1 or 2 provided that m + n is > 1. R is hydrogen, an alkyl or an alkylaryl; X and Y are independently hydrogen, halogen, nitro, cyano, trifluoromethyl, COOH, CONR R , SO2CF3, SO2R , SONR R , alkyl, alkenyl, (CH2)zCONR R , (CH2)zCOOR , or NHCOR , wherein R and R are independently hydrogen, alkyl having 1 to 6 carton atoms, cycloalkyl or alkylaryl, and z is an integer from 0 to 4; R is alkylCOOR , alkylamine, alkylquanidine, aryl, alkylaryl, COalkyl, COalkylaryl, CONR alkyl, CONR aryl, CONR alkylaryl, CSNR alkyl, CSNR alkylaryl or a common amino acid moiety joined by an amide bond, wherein R is hydrogen, alkyl or alkylaryl.
摘要翻译：新型N-取代的氮杂环烷基环稠合式（I）的2,3-喹喔啉二酸盐，含有它们的药物组合物及其使用方法，用于封闭谷氨酸受体，包括N-甲基-D-天冬氨酸（或 NMDA）受体和非NMDA受体，例如α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体和红藻氨酸受体。还描述了制备N-取代的氮杂环烷基环稠合的2,3-喹喔啉的方法。公开了本发明喹喔啉的新型中间体。新的N-取代的氮杂环烷基环稠合的2,3-喹喔啉酮可以用作例如神经保护剂，用于治疗慢性神经变性疾病，作为抗惊厥药，以及治疗精神分裂症，癫痫，焦虑，疼痛和药物成瘾。在式（I）中，如果m + n> 1，则m和n分别为0,1或2，R 1是氢，烷基或烷基芳基; X和Y独立地是氢，卤素，硝基，氰基，三氟甲基，COOH，CONR 4 R 5，SO 2 CF 3，SO 2 R 4，SONR 4 R 5，烷基，烯基，（CH 2） R 5，（CH 2）z COOR 4或NHCOR 4，其中R 4和R 5独立地是氢，具有1-6个碳原子的烷基，环烷基或烷芳基，z 是从0到4的整数; R 2是烷基COOR 3，烷基胺，烷基喹啉，芳基，烷基芳基，CO烷基，CO烷基芳基，CONR 3烷基，CONR 3芳基，CONR 3烷基芳基，CSNR 3烷基，CSNR 3，烷基芳基或通过酰胺键连接的常见氨基酸部分，其中R 3是氢，烷基或烷基芳基。

10. 发明申请

WO1996017832A1 NOVEL GLUTAMATE RECEPTOR ANTAGONISTS: FUSED CYCLOALKYLQUINOXALINEDIONES 审中-公开
标题翻译：新型谷氨酸受体拮抗剂：融合的环丙基胆碱酯
公开(公告)号：WO1996017832A1
公开(公告)日：1996-06-13
申请号：PCT/US1995014571
申请日：1995-11-07
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , BIGGE, Christopher, Franklin , RETZ, Daniel, Martin
IPC分类号： C07D241/38
CPC分类号： C07D241/38 , C07C211/60 , C07C215/44 , C07C229/50 , C07C233/25 , C07C233/41 , C07C233/43 , C07C233/54 , C07C247/14 , C07C309/66 , C07C2602/10
摘要： Novel substituted alicyclic fused ring 2,3-quinoxalinediones, pharmaceutical compositions containing the same and the method of using the same, for the blockade of glutamate receptors, including either or both N-methyl-D-aspartate (NMDA) receptors and non-NMDA receptors such as the alpha -amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor and the kainate receptor, are described. Methods of preparing the substituted alicyclic fused ring 2,3-quinoxalinediones are also described. Novel intermediates of the inventive quinoxalinediones are disclosed. The novel substituted alicyclic fused ring 2,3-quinoxalinediones may be used, for example, as neuroprotective agents, for treatment of chronic neurodegenerative disorders, as anticonvulsants and in the treatment of schizophrenia, epilepsy, anxiety, pain and drug addiction.
摘要翻译：新型取代的脂环稠合环2,3-喹喔啉二酸盐，含有它们的药物组合物及其使用方法，用于封闭谷氨酸受体，包括N-甲基-D-天冬氨酸（NMDA）受体和非NMDA 描述了α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体和红藻氨酸受体等受体。还描述了制备取代的脂环稠合环2,3-喹喔啉的方法。公开了本发明喹喔啉的新型中间体。新型取代的脂环稠合环2,3-喹喔啉二醇可用作例如神经保护剂，用于治疗慢性神经变性疾病，抗惊厥药和治疗精神分裂症，癫痫，焦虑，疼痛和药物成瘾。

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