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21. 发明申请

WO1997008191A1 POLYMORPHS OF THE PRODRUG 6-N-(L-ALA-L-ALA)-TROVAFLOXACIN 审中-公开
标题翻译： PR-6-N-（L-ALA-L-ALA）-TROVAFLOXACIN的多聚体
公开(公告)号：WO1997008191A1
公开(公告)日：1997-03-06
申请号：PCT/IB1996000653
申请日：1996-07-05
申请人： PFIZER INC. , NORRIS, Timothy , MCGARRY, James, J. , ALLEN, Douglas, J., M.
发明人： PFIZER INC.
IPC分类号： C07K05/02
CPC分类号： C07D471/04 , A61K38/00 , C07K5/06191
摘要： A prodrug of trovafloxacin having formula (I), which is selected from its polymorph PII and the monohydrate PII.M and pseudomorphs PII.PS thereof, and processes for their preparation. Polymorph PII and the monohydrate PII.M and pseudomorph PII.PS thereof are described in said formula. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds of the invention for treatment of bacterial infections in mammals.
摘要翻译：具有式（I）的曲伐沙星的前体药物，其选自其多晶型物质PII和一水合物PII.M及其假构型PII.PS及其制备方法。所述式中描述了多晶型PII和一水合物PII.M及其假构型PII.PS。本发明还涉及使用和药物组合物的方法，所述组合物包含用于治疗哺乳动物细菌感染的本发明化合物。

22. 发明申请

WO1997006161A1 ANTICOCCIDIAL 8-AMINOQUINOLINE DERIVATIVES 审中-公开
标题翻译：抗焦虑的8-氨基喹啉衍生物
公开(公告)号：WO1997006161A1
公开(公告)日：1997-02-20
申请号：PCT/EP1996003324
申请日：1996-07-26
申请人： PFIZER LIMITED , PFIZER INC. , ARMER, Richard, Edward , DUTTON, Christopher, James , THONG, Kam, Wah , TOMMASINI, Ivan
发明人： PFIZER LIMITED , PFIZER INC.
IPC分类号： C07D405/12
CPC分类号： C07D405/12 , C07D215/40 , C07D409/12
摘要： Compounds of formula (I) non-toxic salts thereof, and non-toxic solvates of either entity, wherein A is C2-C10 alkylene, C4-C6 alkenylene, C4-C6 alkynylene or C5-C7 cycloalkylene; B is a direct link or C1-C6 alkylene; W is O, S, SO or SO2; R is OH, C1-C4 alkoxy or C1-C4 alkyl; R is H; halo; OH; C1-C4 alkoxy; C1-C4 alkylamino; di C1-C4 alkylamino; C2-C4 alkenyl optionally substituted with phenyl, CO2(C1-C4 alkyl), CN or CONH2; or phenyl or phenoxy optionally substituted with one or two substituents selected from C1-C4 alkyl, C1-C4 alkoxy, halo, CF3 and amino; R is H; halo; C2-C4 alkenyl optionally substituted with phenyl, CO2(C1-C4 alkyl), CN or CONH2; phenyl optionally substituted with one or two substituents selected from C1-C4 alkyl, C1-C4 alkoxy, halo, CF3 and amino; thienyl; furyl or pyridyl; R is H or C1-C4 alkyl; R is H; C1-C4 alkyl; C1-C4 alkoxy; halo; C2-C4 alkenyl optionally substituted with phenyl, CO2(C1-C4 alkyl), CN or CONH2; phenyl or phenoxy optionally substituted with one or two substituents selected from C1-C4 alkyl, C1-C4 alkoxy, halo, CF3 and amino; thienyl; furyl or pyridyl; R is H or C1-C4 alkyl; R is H or C1-C4 alkoxy; m is 1, 2 or 3; n is 0, 1, 2, 3 or 4; and p is 0 or 1; have broad spectrum anticoccidial activity and thus are useful in the treatment or prevention of coccidiosis, and also for performance enhancement, in animals.
摘要翻译：其中A为C 2 -C 10亚烷基，C 4 -C 6亚烯基，C 4 -C 6亚炔基或C 5 -C 7亚环烷基的任何一个实体的无毒溶剂化物; B是直链或C1-C6亚烷基; W是O，S，SO或SO2; R 1是OH，C 1 -C 4烷氧基或C 1 -C 4烷基; R 2是H; 光环; 哦; C1-C4烷氧基; C1-C4烷基氨基; 二C1-C4烷基氨基; 任选被苯基，CO 2（C 1 -C 4烷基），CN或CONH 2取代的C 2 -C 4烯基; 或任选被一个或两个选自C 1 -C 4烷基，C 1 -C 4烷氧基，卤素，CF 3和氨基的取代基取代的苯基或苯氧基; R 3为H; 光环; 任选被苯基，CO 2（C 1 -C 4烷基），CN或CONH 2取代的C 2 -C 4烯基; 任选被一个或两个选自C 1 -C 4烷基，C 1 -C 4烷氧基，卤素，CF 3和氨基的取代基取代的苯基; 噻吩; 呋喃基或吡啶基; R 4是H或C 1 -C 4烷基; R 5为H; C 1 -C 4烷基; C1-C4烷氧基; 光环; 任选被苯基，CO 2（C 1 -C 4烷基），CN或CONH 2取代的C 2 -C 4烯基; 任选被一个或两个选自C 1 -C 4烷基，C 1 -C 4烷氧基，卤素，CF 3和氨基的取代基取代的苯基或苯氧基; 噻吩; 呋喃基或吡啶基 R 6是H或C 1 -C 4烷基; R 7是H或C 1 -C 4烷氧基; m为1,2或3; n为0,1,2,3或4; p为0或1; 具有广谱抗球虫活性，因此可用于治疗或预防球虫病，以及用于动物中的表现增强。

23. 发明申请

WO1997003066A1 SUBSTITUTED BENZOLACTAM COMPOUNDS AS SUBSTANCE P ANTAGONISTS 审中-公开
标题翻译：替代苯甲酸酯化合物作为物质P ANTAGONISTS
公开(公告)号：WO1997003066A1
公开(公告)日：1997-01-30
申请号：PCT/IB1996000434
申请日：1996-05-09
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , WAKABAYASHI, Hiroaki , IKUNAKA, Masaya
发明人： PFIZER PHARMACEUTICALS INC. , PFIZER INC.
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D211/56 , C07D413/12 , C07D417/12 , C07D453/02 , C07D471/08
摘要： This invention provides a compound of general formula (I) and its pharmaceutically acceptable salts, wherein: W is methylene, ethylene, propylene, vinylene, -CH2-O-, -O-CH2-, -CH2-S- or -S-CH2-; R , R and R are independently hydrogen, C1-C3 alkyl, C1-C3 alkoxy or halo C1-C3 alkyl, provided that when W is methylene, both R and R are not hydrogen; X is halo, C1-C3 alkoxy, C1-C3 alkyl, halo C1-C3 alkoxy or C1-C3 alkenyl; Y is imino or oxy; Q is oxygen or sulfur; and T is (2S,3S)-2-diphenylmethylquinuclidin-3-yl, (2S,3S)-2-phenylpiperidin-3-yl or (2S,3S)-2-diphenylmethyl-1-azanorbornan-3-yl. These compounds are useful in the treatment of treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, emesis, urinary incontinence, pain, migraine, angiogensis or the like in a mammaliam subject, especially humans. Also, intermediates of the above compounds are disclosed.
摘要翻译：本发明提供通式（I）的化合物及其药学上可接受的盐，其中：W是亚甲基，亚乙基，亚丙基，亚乙烯基，-CH 2 -O-，-O-CH 2 - ， - CH 2 -S-或-S- CH2-; R 1，R 2和R 3独立地是氢，C 1 -C 3烷基，C 1 -C 3烷氧基或卤代C 1 -C 3烷基，条件是当W是亚甲基时，R 2和R 3 >不是氢; X是卤素，C 1 -C 3烷氧基，C 1 -C 3烷基，卤代C 1 -C 3烷氧基或C 1 -C 3烯基; Y是亚氨基或氧基; Q是氧或硫; 并且T是（2S，3S）-2-二苯基甲基奎宁环-3-基，（2S，3S）-2-苯基哌啶-3-基或（2S，3S）-2-二苯基甲基-1-氮杂咯烷-3-基。这些化合物可用于治疗哺乳动物受试者，特别是人类的治疗胃肠疾病，中枢神经系统疾病，炎性疾病，呕吐，尿失禁，疼痛，偏头痛，血管生成等。另外，公开了上述化合物的中间体。

24. 发明申请

WO1997000268A1 PROCESS FOR PREPARING DERIVATIVES OF AZABICYCLO NAPHTHYRIDINE CARBOXYLIC ACID COMPRISING A DIPEPTIDE 审中-公开
标题翻译：制备包含哌啶酮的亚硫酰基萘甲酸羧酸衍生物的方法
公开(公告)号：WO1997000268A1
公开(公告)日：1997-01-03
申请号：PCT/IB1996000257
申请日：1996-03-27
申请人： PFIZER INC. , BRAISH, Tamim, F. , CASTALDI, Michael, J. , WATSON, Harry, A., Jr.
发明人： PFIZER INC.
IPC分类号： C07K01/06
CPC分类号： C07K5/06191 , Y02P20/55
摘要： A novel process for preparing a prodrug acid, viz., 7-[(1 alpha , 6 alpha , 7 alpha )-6-(L-Ala-L-Ala-amino)-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, in the form of a pharmaceutically acceptable acid addition salt, is disclosed, which involves (1) treating an N-protected 7-[(1 alpha , 5 alpha , 6 alpha )-6-amino-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid C1-C4 alkyl ester, wherein the nitrogen-protecting group is benzyloxycarbonyl, C1-C4 alkoxycarbonyl or C1-C4 alkanoyl, with a strongly-protic acid to selectively remove the N-protecting group; (2) then condensing the resulting free amino ester compound with an N-protected L-alanyl-L-alanine dipeptide compound, wherein the N-protecting group is as previously defined, in the presence of a standard dehydrating agent to form the corresponding N-protected prodrug ester compound as the desired condensation product; and (3) thereafter hydrolyzing the intermediate N-protected prodrug ester in the presence of a pharmaceutically-acceptable strong acid to convert said N-protected prodrug ester to the desired naphthyridinone L-Ala-L-Ala prodrug acid final product, in the form of the corresponding pharmaceutically acceptable acid addition salt, indicated above. The latter prodrug acid final product is especially useful in the form of the corresponding methanesulfonic acid addition salt, which serves as a water-soluble prodrug companion to a known antibacterial agent, viz., 7-[(1 alpha , 5 alpha , 6 alpha )-6-amino-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1-naphthyridine-3-carboxylic acid.
摘要翻译：制备前体药物酸，即7 - [（1α，6α，7α）-6-（L-Ala-L-Ala-氨基）-3-氮杂双环[3.1.0] 吡啶-3-基] -6-氟-1-（2,4-二氟苯基）-1,4-二氢-4-氧代-1,8-二氮杂萘-3-羧酸，其为药学上可接受的酸加成盐，其涉及（1）处理N-保护的7 - [（1α，5α，6α）-6-氨基-3-氮杂双环[3.1.0]己-3-基] -6-氟 -1-（2,4-二氟苯基）-1,4-二氢-4-氧代-1,8-二氮杂萘-3-羧酸C1-C4烷基酯，其中氮保护基是苄氧羰基，C1-C4烷氧基羰基或C 1 -C 4烷酰基，用强质子酸选择性除去N-保护基; （2）然后将所得游离氨基酯化合物与N-保护的L-丙氨酰-L-丙氨酸二肽化合物缩合，其中N-保护基团如前所定义，在标准脱水剂存在下形成相应的N 保护的前药酯化合物作为所需的缩合产物; 和（3）然后在药学上可接受的强酸存在下水解中间体N-保护的前药酯，以将所述N-保护的前药酯转化为所需的萘啶酮L-Ala-L-Ala前药酸最终产物，形式的上述相应的药学上可接受的酸加成盐。后一种前药酸最终产物特别可用于相应的甲磺酸加成盐的形式，其用作已知抗菌剂的水溶性前体药物，即7 - [（1α，5α，6α 基）-6-氨基-3-氮杂双环[3.1.0]己-3-基] -6-氟-1-（2,4-二氟苯基）-1,4-二氢-4-氧代-1-萘-3- -羧酸。

25. 发明申请

WO1996040234A1 IN OVO VACCINATION AGAINST COCCIDIOSIS 审中-公开
标题翻译：在反贪污的OVO疫苗中
公开(公告)号：WO1996040234A1
公开(公告)日：1996-12-19
申请号：PCT/IB1995000446
申请日：1995-06-07
申请人： PFIZER INC. , EVANS, Nigel, A. , FINDLY, R., Craig , WEBER, Frederick, H.
发明人： PFIZER INC.
IPC分类号： A61K39/012
CPC分类号： A61K39/012 , A61K2039/51 , A61K2039/522 , A61K2039/55
摘要： The invention relates to a method of vaccinating a domesticated bird against coccidiosis comprising administering in ovo an effective immunizing dose of live Eimeria sporozoites or merozoites, or a mixture thereof. In a preferred embodiment, the domesticated bird that is vaccinated is a chicken or turkey.
摘要翻译：本发明涉及一种针对球虫病接种家禽的方法，其中包括以卵内施用有效免疫剂量的活艾美球虫子孢子或裂殖子或其混合物。在优选的实施方案中，接种的驯养的禽鸟是鸡或火鸡。

26. 发明申请

WO1996040233A1 IN OVO VACCINATION AGAINST COCCIDIOSIS 审中-公开
标题翻译：在对OVC疫苗接种疫苗
公开(公告)号：WO1996040233A1
公开(公告)日：1996-12-19
申请号：PCT/IB1995000445
申请日：1995-06-07
申请人： PFIZER INC. , EVANS, Nigel, A. , FINDLY, R., Craig , WEBER, Frederick, H.
发明人： PFIZER INC.
IPC分类号： A61K39/012
CPC分类号： A61K39/012
摘要： The invention relates to a method of vaccinating a domesticated bird against coccidiosis comprising administering in ovo an effective immunizing dose of live Eimeria sporocysts or oocysts, or a mixture thereof.
摘要翻译：本发明涉及一种针对球虫病接种驯养的禽类的方法，其包括在卵内施用有效免疫剂量的活艾美球虫孢子囊或卵囊或其混合物。

27. 发明申请

WO1996039408A1 TRICYCLIC 5,6-DIHYDRO-9H-PYRAZOLO[3,4-c]-1,2,4-TRIAZOLO[4,3-'alpha']PYRIDINES 审中-公开
标题翻译：三酮5,6-二氢-9H-吡唑并[3,4-c] -1,2,4-三唑[4,3-α]吡啶
公开(公告)号：WO1996039408A1
公开(公告)日：1996-12-12
申请号：PCT/IB1995000429
申请日：1995-06-06
申请人： PFIZER INC. , DUPLANTIER, Allen, J. , COOPER, Kelvin
发明人： PFIZER INC.
IPC分类号： C07D471/14
CPC分类号： C07D471/14
摘要： A compound of formula (I), wherein R , R , R , R and R are as defined in the description. The compound of formula (I) and the pharmaceutically acceptable salts thereof are useful in inhibiting phosphodiesterase (PDE) Type IV and the production of tumor necrosis factor (TNF) and in the treatment of asthma, arthritis, bronchitis, chronic obstructive airways disease, psoriasis, allergic rhinitis, dermatitis and other inflammatory diseases characterized by phosphodiesterase (PDE) Type IV activity as well as AIDS, sepsis, septic shock and other diseases, such as cachexia, involving the production of TNF.
摘要翻译：式（I）化合物，其中R 1，R 2，R 3，R 9和R 10如说明书中所定义。式（I）化合物及其药学上可接受的盐可用于抑制IV型磷酸二酯酶（PDE）和肿瘤坏死因子（TNF）的产生以及治疗哮喘，关节炎，支气管炎，慢性阻塞性气道疾病，牛皮癣，过敏性鼻炎，皮炎和其他以磷酸二酯酶（PDE）IV型活性为特征的炎性疾病以及艾滋病，败血症，败血性休克等涉及TNF产生的恶病质等疾病。

28. 发明申请

WO1996038466A1 STEROIDAL GLYCOSIDES 审中-公开
标题翻译：灭菌糖尿病
公开(公告)号：WO1996038466A1
公开(公告)日：1996-12-05
申请号：PCT/IB1995000409
申请日：1995-05-29
申请人： PFIZER INC. , DENINNO, Michael, Paul , McCARTHY, Peter, Andrew
发明人： PFIZER INC.
IPC分类号： C07J71/00
CPC分类号： C07J41/0055 , C07J17/005 , C07J21/005 , C07J41/0016 , C07J41/0038 , C07J71/0005 , C07J71/0094 , Y10S514/824
摘要： The invention relates to certains steroidal glycoside derivatives useful as hypocholesterolemic agents and antiatherosclerosis agents. The present invention is also directed to pharmaceutical compositions comprising such derivatives and use of such derivatives in treating hypercholesterolemia or atherosclerosis.
摘要翻译：本发明涉及可用作低胆固醇血症药和抗动脉粥样硬化剂的某些甾体糖苷衍生物。本发明还涉及包含这些衍生物的药物组合物和这些衍生物在治疗高胆固醇血症或动脉粥样硬化中的用途。

29. 发明申请

WO1996036632A1 PYRROLIDINYL METHYL INDOLE SALT 审中-公开
标题翻译：吡咯烷基甲基吲哚盐
公开(公告)号：WO1996036632A1
公开(公告)日：1996-11-21
申请号：PCT/EP1996001560
申请日：1996-04-10
申请人： PFIZER RESEARCH AND DEVELOPMENT COMPANY, N.V./S.A. , PFIZER LIMITED , PFIZER INC. , WYTHES, Martin, James
发明人： PFIZER RESEARCH AND DEVELOPMENT COMPANY, N.V./S.A. , PFIZER LIMITED , PFIZER INC.
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： The fumarate salt of (R)-5-(methylaminosulphonylmethyl)-3-(N-methylpyrrolidin-2-ylmethyl)-1 H-indole, useful in the treatment of migraine.
摘要翻译：（R）-5-（甲基氨基磺酰基甲基）-3-（N-甲基吡咯烷-2-基甲基）-1H-吲哚的富马酸盐，可用于治疗偏头痛。

30. 发明申请

WO1996033172A1 ARYLSULFONYL HYDROXAMIC ACID DERIVATIVES AS MMP AND TNF INHIBITORS 审中-公开
标题翻译：作为MMP和TNF抑制剂的ARYLSULFONYL羟基酸衍生物
公开(公告)号：WO1996033172A1
公开(公告)日：1996-10-24
申请号：PCT/IB1995000279
申请日：1995-04-20
申请人： PFIZER INC. , PISCOPIO, Anthony, D. , RIZZI, James, P.
发明人： PFIZER INC.
IPC分类号： C07D211/96
CPC分类号： C07D295/24 , C07D211/96 , C07D241/04 , C07D241/08
摘要： A compound of formula (I) wherein R , R , R , R , R , R , R , R , R and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis and other diseases characterized by matrix metalloproteinase activity, as well as AIDS, sepsis, septic shock and other diseases involving the production of TNF.
摘要翻译：式（I）的化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8， 9＆gt;和Ar如上所定义，可用于治疗选自关节炎，癌症，组织溃疡，再狭窄，牙周病，大疱性表皮松解症，巩膜炎和其他以基质金属蛋白酶活性为特征的疾病的病症，以及艾滋病，败血症，败血性休克等涉及TNF产生的疾病。

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