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21. 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。

22. 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。

23. 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。

24. 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。

25. 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。

26. 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。

27. 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。

28. 发明申请

WO1996027583A1 ARYLSULFONYLAMINO HYDROXAMIC ACID DERIVATIVES 审中-公开
标题翻译：芳基磺酰胺羟基酸衍生物
公开(公告)号：WO1996027583A1
公开(公告)日：1996-09-12
申请号：PCT/US1996002679
申请日：1996-03-07
申请人： PFIZER INC. , ROBINSON, Ralph, P. , RIZZI, James, P.
发明人： PFIZER INC.
IPC分类号： C07C311/29
CPC分类号： C07D213/40 , C07C311/29 , C07D207/12 , C07D241/08 , C07D295/185
摘要： A compound of formula (I), wherein n, X, 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, AIDS, sepsis, septic shock and other diseases involving the production of TNF.
摘要翻译：式（I）化合物，其中n，X，R 3，R 4和Ar如上所定义，可用于治疗选自关节炎，癌症，组织溃疡，再狭窄的病症，牙周病，大疱性表皮松解症，巩膜炎等特征为基质金属蛋白酶活性的疾病，AIDS，败血症，败血性休克等涉及TNF产生的疾病。

29. 发明申请

WO1996026209A1 STABLE HYDRATES OF A CEPHALOSPORIN CHLORIDE SALT 审中-公开
标题翻译： CEPHOROSPORIN氯化物盐的稳定水合物
公开(公告)号：WO1996026209A1
公开(公告)日：1996-08-29
申请号：PCT/GB1996000373
申请日：1996-02-19
申请人： PFIZER INC. , WEBSTER, Richard, Andrew, Bentley
发明人： PFIZER INC.
IPC分类号： C07D501/36
CPC分类号： C07D501/00
摘要： The cephalosporin compound [6R, 7R]-7-[2-(2-amino-4-thiazolyl)-2-(Z)-(methoxyimino)acetamido]-3-[1-(methylamino)pyridinium-4-thiomethyl]-ceph-3-em-4-carboxylic acid chloride hydrochloride is provided as a mono-, di- or tri-hydrate. The hydrates are produced by treating an aqueous solution of the corresponding carboxylate with hydrogen chloride and have been found to possess unexpectedly superior stability properties over other forms of the compound. The hydrates may be used in the treatment and/or prevention of bacterial infections in humans and animals.
摘要翻译：头孢菌素化合物[6R，7R] -7- [2-（2-氨基-4-噻唑基）-2-（Z） - （甲氧基亚氨基）乙酰氨基] -3- [1-（甲基氨基）吡啶鎓-4-硫代甲基] - 顺式-3-烯-4-羧酰氯盐酸盐以单 - ，二 - 或三 - 水合物的形式提供。通过用氯化氢处理相应的羧酸盐的水溶液来生产水合物，并且已经发现其具有比其它形式的化合物出人意料的优异的稳定性。水合物可用于治疗和/或预防人和动物的细菌感染。

30. 发明申请

WO1996012720A1 BICYCLIC TETRAHYDRO PYRAZOLOPYRIDINES AND THEIR USE AS MEDICAMENTS 审中-公开
标题翻译：双羟基四氢吡喃并吡啶并用作药物
公开(公告)号：WO1996012720A1
公开(公告)日：1996-05-02
申请号：PCT/IB1995000847
申请日：1995-10-06
申请人： PFIZER INC. , DUPLANTIER, Allen, J.
发明人： PFIZER INC.
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Compounds of formula (I) wherein R , R , R and X are as defined. The compounds 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, AIDS, septic shock and other diseases involving the production of TNF.
摘要翻译：其中R 1，R 2，R 3和X的式（I）化合物如上所定义。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，皮炎等炎性疾病，艾滋病，败血性休克等涉及TNF产生的疾病。

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