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1. 发明申请

WO1997041896A2 INCLUSION COMPLEXES OF ARYL-HETEROCYCLIC SALTS 审中-公开
标题翻译：包含ARYL-HETEROCYCLIC SALTS的复合物
公开(公告)号：WO1997041896A2
公开(公告)日：1997-11-13
申请号：PCT/IB1997000321
申请日：1997-04-01
申请人： PFIZER INC. , JOHNSON, Kevin, Charles , KIM, Yesook , SHANKER, Ravi, Mysore
发明人： PFIZER INC.
IPC分类号： A61K47/48
CPC分类号： B82Y5/00 , A61K31/496 , A61K31/724 , A61K47/6951 , A61K2300/00
摘要： Compositions of matter comprising a pharmaceutically acceptable salt of an aryl-heterocyclic compound, such as ziprasidone, in a cyclodextrin. Preferred cyclodextrins are SBECD and HPBCD. The composition can comprise a dry mixture, a dry inclusion complex or an aqueous solution. The salt/cyclodextrin inclusion complex preferably provides an amount of ziprasidone of at least 2.5 mgA/ml when the complex is dissolved in water at 40 % w/v. A variety of ziprasidone salts are preferred, including the mesylate, esylate, besylate, tartrate, napsylate, and tosylate.
摘要翻译：包含芳环杂环化合物如齐拉西酮的药学上可接受的盐在环糊精中的组合物。优选的环糊精是SBECD和HPBCD。该组合物可以包含干燥混合物，干燥包合络合物或水溶液。当络合物溶于40％w / v的水中时，盐/环糊精包合配合物优选提供至少2.5mgA / ml的量的齐拉西酮。各种齐拉西酮盐是优选的，包括甲磺酸盐，乙磺酸盐，苯磺酸盐，酒石酸盐，萘磺酸盐和甲苯磺酸盐。

2. 发明申请

WO1998030209A1 RAPIDLY RELEASING AND TASTE-MASKING PHARMACEUTICAL DOSAGE FORM 审中-公开
标题翻译：快速释放和吸收药物药物剂型
公开(公告)号：WO1998030209A1
公开(公告)日：1998-07-16
申请号：PCT/IB1997001471
申请日：1997-11-20
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , ITOH, Akinori , NIWA, Toshiyuki
发明人： PFIZER PHARMACEUTICALS INC. , PFIZER INC.
IPC分类号： A61K09/54
CPC分类号： A61K9/5078 , A61K9/1623 , A61K9/1652 , A61K9/5015 , A61K9/5026 , A61K9/5073
摘要： The present invention provides a rapidly releasing and taste-masking pharmaceutical dosage form comprising a core containing a pharmaceutically active ingredient, low-substituted hydroxypropyl cellulose and microcrystalline cellulose, the amount of the microcrystalline cellulose being at least 26.0 weight percent based on the total weight of the core; an inner coating layer formed on the core and containing a water-soluble polymer; and an outer coating layer formed on the inner coating layer and containing a saliva-insoluble polymer. A process for preparing such oral dosage form is also disclosed.
摘要翻译：本发明提供了一种快速释放和掩味的药物剂型，其包含含有药物活性成分，低取代羟丙基纤维素和微晶纤维素的核心，微晶纤维素的量基于总重量的至少26.0重量％核心; 形成在芯上并含有水溶性聚合物的内涂层; 以及形成在内涂层上并含有唾液不溶性聚合物的外涂层。还公开了制备这种口服剂型的方法。

3. 发明申请

WO1998023613A1 FUSED BICYCLIC PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：熔化的双相吡啶衍生物
公开(公告)号：WO1998023613A1
公开(公告)日：1998-06-04
申请号：PCT/IB1997001393
申请日：1997-11-05
申请人： PFIZER INC. , ARNOLD, Lee, Daniel , MOYER, Mikel, Paul , SOBOLOV-JAYNES, Susan, Beth
发明人： PFIZER INC.
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to compounds of formula (I) and to pharmaceutically acceptable salts thereof, wherein R , R and Z are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula (I) and to methods of using said compounds in the treatment of hyperproliferative diseases such as cancer.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，其中R 1，R 2和Z如本文所定义。本发明还涉及含有式（I）化合物的药物组合物以及使用所述化合物治疗过度增殖性疾病如癌症的方法。

4. 发明申请

WO1998023593A1 APO B-SECRETION/MTP INHIBITORY AMIDES 审中-公开
标题翻译： APO B分泌/ MTP抑制剂
公开(公告)号：WO1998023593A1
公开(公告)日：1998-06-04
申请号：PCT/IB1997001368
申请日：1997-11-03
申请人： PFIZER INC. , CHANG, George , QUALLICH, George, Joseph
发明人： PFIZER INC.
IPC分类号： C07D217/04
CPC分类号： C07D401/04 , C07D217/04 , C07D401/06 , C07D405/04 , C07D405/06 , C07D409/06 , C07D417/06
摘要： This invention is directed to compounds of formula (I) or the stereoisomers, pharmaceutically acceptable salts and hydrates thereof. The compounds are Apo B/MTP inhibitors and are useful in the treatment of various disorders and conditions such as atherosclerosis, pancreatitis, obesity, hypercholesteremia, hypertriglyceridemia, hyperlipidemia, and diabetes. The compounds of this invention are also useful in combination with other pharmaceutical agents including cholesterol biosynthesis inhibitors and cholesterol absorption inhibitors, especially HMG-CoA reductase inhibitors and HMG-CoA synthase inhibitors; HMG-CoA reductase gene expression inhibitors; CETP inhibitors; bile acid sequestrants; fibrates; cholesterol absorption inhibitors; ACAT inhibitors, squalene synthetase inhibitors, ion-exchange resins, anti-oxidants and niacin. This invention is also directed to intermediates and processes useful in the preparation of compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物或其立体异构体，其药学上可接受的盐和水合物。这些化合物是Apo B / MTP抑制剂，可用于治疗各种疾病和病症如动脉粥样硬化，胰腺炎，肥胖症，高胆固醇血症，高甘油三酯血症，高脂血症和糖尿病。本发明的化合物还可与其它药剂组合使用，包括胆固醇生物合成抑制剂和胆固醇吸收抑制剂，特别是HMG-CoA还原酶抑制剂和HMG-CoA合成酶抑制剂; HMG-CoA还原酶基因表达抑制剂; CETP抑制剂; 胆汁酸螯合剂贝特类药物; 胆固醇吸收抑制剂; ACAT抑制剂，角鲨烯合成酶抑制剂，离子交换树脂，抗氧化剂和烟酸。本发明还涉及可用于制备式（I）化合物的中间体和方法。

5. 发明申请

WO1998012177A1 PYRROLIDINYL AND PYRROLINYL ETHYLAMINE COMPOUNDS AS KAPPA AGONISTS 审中-公开
标题翻译：吡咯烷酮和吡咯烷酮化合物作为KAPPA激动剂
公开(公告)号：WO1998012177A1
公开(公告)日：1998-03-26
申请号：PCT/IB1997001021
申请日：1997-08-21
申请人： PFIZER INC. , PFIZER PHARMACEUTICALS INC. , ITO, Fumitaka , KONDO, Hiroshi
发明人： PFIZER INC. , PFIZER PHARMACEUTICALS INC.
IPC分类号： C07D207/12
CPC分类号： C07D213/82 , C07D207/10 , C07D207/12 , C07D207/20 , C07D207/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , Y02P20/55
摘要： A compound of formula (I) and the salts thereof, wherein A is halo, hydroxy or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar is optionally substituted phenyl or the like; Ar is aryl or heteroaryl selected from phenyl, naphthyl, pyridyl and the like, the aryl or heteroaryl being optionally substituted; R is hydrogen, hydroxy, C1-C4 alkyl or the like; and R and R are independently selected from optionally substituted C1-C7 alkyl C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl and the like or R and R , together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.
摘要翻译：式（I）化合物及其盐，其中A为卤素，羟基等; 虚线表示任选的双键，条件是如果虚线是双键，则A不存在; Ar 1是任选取代的苯基等; Ar 2是选自苯基，萘基，吡啶基等的芳基或杂芳基，芳基或杂芳基任选被取代; R 1是氢，羟基，C 1 -C 4烷基等; R 2和R 3独立地选自任选取代的C 1 -C 7烷基C 3 -C 6环烷基，C 2 -C 6烯基，C 2 -C 6炔基等或R 2和R 3连同它们所连接的氮原子形成任选取代的吡咯烷，哌啶或吗啉环。这些化合物可用作κ激动剂。

6. 发明申请

WO1998008846A1 SUBSTITUTED 6,6-HETERO-BICYCLIC DERIVATIVES 审中-公开
标题翻译：取代的6,6-杂双环衍生物
公开(公告)号：WO1998008846A1
公开(公告)日：1998-03-05
申请号：PCT/IB1997000904
申请日：1997-07-21
申请人： PFIZER INC. , CHEN, Yuhpyng, Liang
发明人： PFIZER INC.
IPC分类号： C07D471/04
CPC分类号： C07D215/233 , C07D215/18 , C07D215/42 , C07D405/12 , C07D471/04 , C07D475/02
摘要： This invention relates to compounds of formula (I), wherein A, B, D, E, K, G, R and R are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds. Compounds (I) are corticotropin releasing factor (hormone) CRF (CRH) antagonists.
摘要翻译：本发明涉及式（I）化合物，其中A，B，D，E，K，G，R 3和R 5如说明书中所定义，以及这些化合物的药学上可接受的盐。化合物（I）是促肾上腺皮质激素释放因子（激素）CRF（CRH）拮抗剂。

7. 发明申请

WO1998008835A1 SPIROCYCLIC DOPAMINE RECEPTOR SUBTYPE LIGANDS 审中-公开
标题翻译：螺旋多巴胺受体亚型配体
公开(公告)号：WO1998008835A1
公开(公告)日：1998-03-05
申请号：PCT/IB1997000978
申请日：1997-08-08
申请人： PFIZER INC. , BUTLER, Todd, William , FLIRI, Anton, Franz, Joseph
发明人： PFIZER INC.
IPC分类号： C07D307/94
CPC分类号： C07D295/073 , C07D295/112 , C07D295/155 , C07D307/94 , C07D333/50 , C07D333/58
摘要： This invention relates to novel, pharmaceutically active compounds of formula (I) wherein a, b and R through R are defined as in the specification. These compounds exhibit central dopaminergic activity and are useful in the treatment of CNS disorders.
摘要翻译：本发明涉及式（I）的新的药物活性化合物，其中a，b和R 1至R 6如说明书中所定义。这些化合物表现出中枢多巴胺能活性，可用于治疗CNS疾病。

8. 发明申请

WO1998004530A1 PARASITICIDAL PYRAZOLES 审中-公开
公开(公告)号：WO1998004530A1
公开(公告)日：1998-02-05
申请号：PCT/GB1997001925
申请日：1997-07-16
申请人： PFIZER LIMITED , PFIZER INC. , BANKS, Bernard, Joseph
发明人： PFIZER LIMITED , PFIZER INC.
IPC分类号： C07D231/38
CPC分类号： C07D231/38 , A01N43/56 , C07D231/14
摘要： A new group of parasiticidal pyrazoles of formula (I) wherein R is NH2, H, halogen, NH(C1-6alkyl optionally substituted with one or more halogen), NH(allyl optionally substituted with one or more halogen), NH(benzyl optionally substituted with one or more halogen), NHSCF3, or R is C1-6alkyl optionally substituted with one or more halogen; R , R and R are each independently H, halogen, SF5, C1-6alkyl optionally substituted with one or more halogen, C1-6alkoxy optionally substituted with one or more halogen, or S(O)n(C1-6alkyl optionally substituted with one or more halogen) wherein n is 0, 1 or 2; X is O or NOY; Y is H or C1-6alkyl optionally substituted with one or more halogen; R is H, C1-8alkyl optionally substituted with one or more halogen, or C3-8cycloalkyl optionally substituted by one or more halogen, or by one or more C1-4 alkyl optionally substituted with one or more halogen, or by C3-8cycloalkylcarbonyl; and their pharmaceutically- or veterinarily-acceptable acid addition salts are described, together with processes thereto and uses thereof.
摘要翻译：一种新的式（I）的杀虫吡唑，其中R 2是NH 2，H，卤素，NH（任选被一个或多个卤素取代的C 1-6烷基），NH（任选被一个或多个卤素取代的烯丙基），NH （任选被一个或多个卤素取代的苄基），NHSCF 3或R 2是任选被一个或多个卤素取代的C 1-6烷基; R 3，R 5和R 7各自独立地为H，卤素，SF 5，任选被一个或多个卤素取代的C 1-6烷基，任选被一个或多个卤素取代的C 1-6烷氧基或S（O） n（任选被一个或多个卤素取代的C 1-6烷基），其中n为0,1或2; X是O或NOY; Y是H或任选被一个或多个卤素取代的C 1-6烷基; R 8为H，任选被一个或多个卤素取代的C 1-8烷基或任选被一个或多个卤素取代的C 3-8环烷基，或被一个或多个任选被一个或多个卤素取代的C 1-4烷基，或被C 3 -8cycloalkylcarbonyl; 以及它们的药学上或兽医学上可接受的酸加成盐以及其方法及其用途。

9. 发明申请

WO1997042190A1 MESYLATE TRIHYDRATE SALT OF 5-(2-(4-(1,2-BENZISOTHIAZOL-3-YL)-1-PIPERAZINYL)ETHYL)-6-CHLORO-1,3-DIHYDRO-2(1H)-INDOL-2-ONE (=ZIPRASIDONE), ITS PREPARATION AND ITS USE AS DOPAMINE D2 ANTAGONIST 审中-公开
标题翻译： 5-（2-（4-（1,2-BENZISOTHIAZOL-3-YL）-1-哌嗪基）乙基）-6-氯-1,3-二氢-2H-（2H） - 吲哚-2-基] ONE（= ZIPRASIDONE），其制备及其用途DOPAMINE D2 ANTAGONIST
公开(公告)号：WO1997042190A1
公开(公告)日：1997-11-13
申请号：PCT/IB1997000306
申请日：1997-03-26
申请人： PFIZER INC. , BUSCH, Frank, R. , ROSE, Carol, A.
发明人： PFIZER INC.
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： The invention relates to the mesylate trihydrate salt of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one, pharmaceutical compositions containing said mesylate trihydrate salt, and methods of using said mesylate trihydrate salt to treat psychotic disorders.
摘要翻译：本发明涉及5-（2-（4-（1,2-苯并异噻唑-3-基）-1-哌嗪基）乙基）-6-氯-1,3-二氢-2H-吲哚-2-酮的甲磺酸盐三水合物盐， 2-one，含有所述甲磺酸盐三水合物盐的药物组合物，以及使用所述甲磺酸盐三水合盐治疗精神病症的方法。

10. 发明申请

WO1997032873A1 QUINOXALINEDIONES 审中-公开
公开(公告)号：WO1997032873A1
公开(公告)日：1997-09-12
申请号：PCT/EP1997000995
申请日：1997-02-27
申请人： PFIZER RESEARCH AND DEVELOPMENT COMPANY, N.V./S.A. , PFIZER LIMITED , PFIZER INC. , BULL, David, John , CARR, Christopher, Lee , FRAY, Michael, Jonathan , GAUTIER, Elisabeth, Colette, Louise , MOWBRAY, Charles, Eric , STOBIE, Alan
发明人： PFIZER RESEARCH AND DEVELOPMENT COMPANY, N.V./S.A. , PFIZER LIMITED , PFIZER INC.
IPC分类号： C07D401/04
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein R is a 5-membered ring heteroaryl group containing 3 or 4 nitrogen heteroatoms which is linked to the quinoxalinedione ring by a ring carbon or nitrogen atom, or is a 6-membered ring heteroaryl group containing from 1 to 3 nitrogen heteroatoms which is linked to the quinoxalinedione ring by a ring carbon atom, either of said groups being optionally benzo-fused and optionally substituted, including in the benzo-fused portion, by 1 or 2 substituents each independently selected from C1-C4 alkyl, C2-C4 alkenyl, C3-C7 cycloalkyl, halo, hydroxy, C1-C4 alkoxy, C3-C7 cycloalkyloxy, -COOH, C1-C4 alkoxycarbonyl, -CONR R , -NR R , -S(O)p(C1-C4 alkyl), -SO2NR R , aryl, aryloxy, aryl(C1-C4)alkoxy and het, said C1-C4 alkyl being optionally substituted by C3-C7 cycloalkyl, halo, hydroxy, C1-C4 alkoxy, halo(C1-C4)alkoxy, C3-C7 cycloalkyloxy, C3-C7 cycloalkyl(C1-C4)alkoxy, -COOH, C1-C4 alkoxycarbonyl, -CONR R , -NR R , -S(O)p(C1-C4 alkyl), -SO2(aryl), -SO2NR R , morpholino, aryl, aryloxy, aryl(C1-C4)alkoxy or het, and said C2-C4 alkenyl being optionally substituted by aryl; R and R are each independently selected from H, fluoro, chloro, bromo, C1-C4 alkyl and halo(C1-C4)alkyl; R and R are either each independently selected from H and C1-C4 alkyl or, when taken together, are C5-C7 alkylene; p is 0, 1 or 2; together with the preparation of, compositions containing, the uses of and intermediates used in the synthesis of, such compounds. The compounds are useful as NMDA receptor antagonists for treating acute neurodegenerative and chronic neurological disorders.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐，其中R是含有3或4个氮杂原子的5元环杂芳基，其通过环碳或氮原子与喹喔啉二酮环连接，或是含有1至3个氮杂原子的6元环杂芳基，其通过环碳原子与喹喔啉二酮环连接，所述基团任选地被苯并稠合并且任选地被取代，包括苯并稠合部分中的1或 2个独立地选自C 1 -C 4烷基，C 2 -C 4烯基，C 3 -C 7环烷基，卤素，羟基，C 1 -C 4烷氧基，C 3 -C 7环烷氧基，-COOH，C 1 -C 4烷氧羰基，-CONR 3 R R 4，-NR 3 R 4，-S（O）p（C 1 -C 4烷基），-SO 2 NR 3 R 4，芳基，芳氧基，芳基（C 1 -C 4）所述C 1 -C 4烷基任选被C 3 -C 7环烷基，卤素，羟基，C 1 -C 4烷氧基，卤代（C 1 -C 4）烷氧基，C 3 -C 7环烷氧基，C 3 -C 7环烷基（C 1 -C 4）烷氧基，-COOH， C1-C4 烷氧基羰基，-CONR 3 R 4，-NR 3 R 4，-S（O）p（C 1 -C 4烷基），-SO 2（芳基），-SO 2 NR 3 R 4，，吗啉代，芳基，芳氧基，芳基（C 1 -C 4）烷氧基或羟基，所述C 2 -C 4烯基任选被芳基取代; R 1和R 2各自独立地选自H，氟，氯，溴，C 1 -C 4烷基和卤代（C 1 -C 4）烷基; R 3和R 4各自独立地选自H和C 1 -C 4烷基，或者一起是C 5 -C 7亚烷基; p为0,1或2; 以及含有用于合成这些化合物的用途和中间体的组合物的制备。该化合物可用作治疗急性神经变性和慢性神经障碍的NMDA受体拮抗剂。

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