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1. 发明授权

US6002008A Substituted 3-cyano quinolines 失效
公开(公告)号：US6002008A
公开(公告)日：1999-12-14
申请号：US49718
申请日：1998-03-27
申请人： Allan Wissner , Bernard D. Johnson , Marvin F. Reich , Middleton B. Floyd, Jr. , Douglas B. Kitchen , Hwei-Ru Tsou
发明人： Allan Wissner , Bernard D. Johnson , Marvin F. Reich , Middleton B. Floyd, Jr. , Douglas B. Kitchen , Hwei-Ru Tsou
IPC分类号： C07D215/54 , C07D215/56 , C07D401/04 , C07D401/12 , C07D409/12 , A01N43/42 , C07D215/16 , C07D215/38
CPC分类号： C07D401/04 , C07D215/54 , C07D215/56 , C07D401/12 , C07D409/12
摘要： This invention provides compounds having the formula: ##STR1## wherein: X is cycloalkyl which may be optionally substituted; or is a pyridinyl, pyrimidinyl, or phenyl ring; wherein the pyridinyl, pyrimidinyl, or phenyl ring may be optionally substituted;n is 0-1;Y is --NH--, --O--, --S--, or --NR--;R is alkyl of 1-6 carbon atoms;R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are each, independently, hydrogen, halogen, alkyl, alkenyl, alkynyl, alkenyloxy, alkynyloxy, hydroxymethyl, halomethyl, alkanoyloxy, alkenoyloxy, alkynoyloxy, alkanoyloxymethyl, alkenoyloxymethyl, alkynoyloxymethyl, alkoxymethyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylsulfonamido, alkenylsulfonamido, alkynylsulfonamido, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy, carboalkyl, phenoxy, phenyl, thiophenoxy, benzyl, amino, hydroxyamino, alkoxyamino, alkylamino, dialkylamino, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, phenylamino, benzylamino, ##STR2## R.sub.5 is alkyl which may be optionally substituted, or phenyl which may be optionally substituted;R.sub.6 is hydrogen, alkyl, or alkenyl;R.sub.7 is chloro or bromoR.sub.8 is hydrogen, alkyl, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, N-cycloalkylaminoalkyl, N-cycloalkyl-N-alkylaminoalkyl, N,N-dicycloalkylaminoalkyl, morpholino-N-alkyl, piperidino-N-alkyl, N-alkyl-piperidino-N-alkyl, azacycloalkyl-N-alkyl, hydroxyalkyl, alkoxyalkyl, carboxy, carboalkoxy, phenyl, carboalkyl+, chloro, fluoro, or bromo;Z is amino, hydroxy, alkoxy, alkylamino, dialkylamino, morpholino, piperazino, N-alkylpiperazino, or pyrrolidino;m=1-4,q=1-3, and p=0-3;any of the substituents R.sub.1, R.sub.2, R.sub.3, or R.sub.4 that are located on contiguous carbon atoms can together be the divalent radical --O--C(R.sub.8).sub.2 --O--;or a pharmaceutically acceptable salt thereof with the proviso that when Y is --NH--, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are hydrogen, and n is 0, X is not 2-methylphenyl, which are inhibitors of protein tyrosine kinase.

2. 发明授权

US5760041A 4-aminoquinazoline EGFR Inhibitors 失效
标题翻译： 4-氨基喹唑啉EGFR抑制剂
公开(公告)号：US5760041A
公开(公告)日：1998-06-02
申请号：US785910
申请日：1997-01-21
申请人： Allan Wissner , Bernard D. Johnson , Middleton B. Floyd, Jr. , Douglas B. Kitchen
发明人： Allan Wissner , Bernard D. Johnson , Middleton B. Floyd, Jr. , Douglas B. Kitchen
IPC分类号： A61K31/505 , A61K31/517 , A61P35/00 , A61P43/00 , C07D239/94
CPC分类号： C07D239/94
摘要： This invention provides a compound having the formula ##STR1## wherein: X is phenyl which is optionally substituted; R and R.sub.1 are each, independently, hydrogen, halogen, alkyl, alkoxy, hydroxy, or trifluoromethyl; R.sub.2 is hydrogen, alkyl, alkoxy, hydroxy, trifluoromethyl; Y is a radical selected from the group consisting of ##STR2## R.sub.3 is independently hydrogen, alkyl, carboxy, carboalkoxy, phenyl, or carboalkyl; n=2-4; or a pharmaceutically acceptable salt thereof, with the proviso that each R.sub.3 of Y may be the same or different which are useful as antineoplastic agents.
摘要翻译：本发明提供了具有下式的化合物：其中：X是任选取代的苯基; R和R 1各自独立地为氢，卤素，烷基，烷氧基，羟基或三氟甲基; R2是氢，烷基，烷氧基，羟基，三氟甲基; Y是选自由下列组成的组的基团：R 3独立地是氢，烷基，羧基，烷氧羰基，苯基或烷基烷基; n = 2-4; 或其药学上可接受的盐，条件是Y的每个R 3可以相同或不同，其可用作抗肿瘤剂。

3. 发明授权

US06288082B1 Substituted 3-cyanoquinolines 有权
公开(公告)号：US06288082B1
公开(公告)日：2001-09-11
申请号：US09406573
申请日：1999-09-24
申请人： Allan Wissner , Hwei-Ru Tsou , Dan M. Berger , Middleton B. Floyd, Jr. , Philip R. Hamann , Nan Zhang , Mark E. Salvati , Philip Frost
发明人： Allan Wissner , Hwei-Ru Tsou , Dan M. Berger , Middleton B. Floyd, Jr. , Philip R. Hamann , Nan Zhang , Mark E. Salvati , Philip Frost
IPC分类号： A61K3147
CPC分类号： C07D401/12 , C07D215/48 , C07D417/12
摘要： This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.

4. 再颁专利

USRE42376E1 Substituted 3-cyanoquinolines 有权
标题翻译：取代的3-氰基喹啉
公开(公告)号：USRE42376E1
公开(公告)日：2011-05-17
申请号：US12785269
申请日：2010-05-21
申请人： Allan Wissner , Hwei-Ru Tsou , Dan M. Berger , Middleton B. Floyd, Jr. , Philip R. Hamann , Nan Zhang , Philip Frost
发明人： Allan Wissner , Hwei-Ru Tsou , Dan M. Berger , Middleton B. Floyd, Jr. , Philip R. Hamann , Nan Zhang , Philip Frost
IPC分类号： A61K31/47 , C07D215/44
CPC分类号： C07D215/54 , C07D215/44 , C07D215/56
摘要： This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.
摘要翻译：本发明提供具有以下结构的式I化合物：其中G1，G2，R1，R4，Z，n和X在本说明书中定义，或其药学上可接受的盐，其可用作抗肿瘤剂和治疗多囊肾病。

5. 发明授权

US06297258B1 Substituted 3-cyanoquinolines 有权
标题翻译：取代的3-氰基喹啉
公开(公告)号：US06297258B1
公开(公告)日：2001-10-02
申请号：US09630270
申请日：2000-08-01
申请人： Allan Wissner , Hwei-Ru Tsou , Dan M. Berger , Middleton B. Floyd, Jr. , Philip R. Hamann , Nan Zhang , Philip Frost
发明人： Allan Wissner , Hwei-Ru Tsou , Dan M. Berger , Middleton B. Floyd, Jr. , Philip R. Hamann , Nan Zhang , Philip Frost
IPC分类号： A61K3147
CPC分类号： C07D215/54 , C07D215/44 , C07D215/56
摘要： This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.
摘要翻译：本发明提供了具有其结构的式I化合物，其中G1，G2，R1，R4，Z，n和X在本说明书或其药学上可接受的盐中定义，其可用作抗肿瘤药物和治疗多囊肾病。

6. 发明授权

US4291175A 1-Hydroxymethyl-11-deoxy-15-hydroxy-prosten-1-ol-derivatives 失效
标题翻译： 1-羟甲基-11-脱氧-15-羟基 - 前列腺-1-醇衍生物
公开(公告)号：US4291175A
公开(公告)日：1981-09-22
申请号：US137082
申请日：1980-04-03
申请人： Allan Wissner , Middleton B. Floyd, Jr.
发明人： Allan Wissner , Middleton B. Floyd, Jr.
IPC分类号： C07C45/59 , C07C59/245 , C07C405/00 , C07D307/32 , C07D307/42 , C07D307/46 , C07D317/16 , C07D317/24 , C07D317/34 , C07F7/18 , C07F9/54 , C07C35/06 , C07C49/597 , C07C49/798
CPC分类号： C07D307/32 , C07C405/0016 , C07C405/0025 , C07C45/59 , C07C59/245 , C07D307/42 , C07D307/46 , C07D317/16 , C07D317/24 , C07D317/34 , C07F7/1856 , C07F9/5407 , Y10S514/822 , Y10S514/929
摘要： Prostaglandin analogs are disclosed that have the .alpha.-chain terminating with the group --CH(OR')OR" wherein R' and R" are the same or different and are hydrogen, C.sub.1 to C.sub.4 alkanoyl or optionally substituted benzoyl, the substituents selected from the group C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, halo and trifluoromethyl. These compounds are useful as hypotensive agents, gastric secretory and platelet aggregation enhibitors and bronchodilators.
摘要翻译：公开前列腺素类似物，其具有以基团-CH（OR'）OR“终止的α-链，其中R'和R”相同或不同，并且是氢，C 1至C 4烷酰基或任选取代的苯甲酰基，取代基选自C1至C4烷基，C1至C4烷氧基，卤素和三氟甲基。这些化合物可用作降压药，胃分泌和血小板聚集抑制剂和支气管扩张剂。

7. 发明授权

US4288630A 1-Hydroxymethyl-11,15-dihydroxy-prosten-1-ol-derivatives 失效
标题翻译： 1-羟甲基-11,15-二羟基 - 前列腺-1-醇衍生物
公开(公告)号：US4288630A
公开(公告)日：1981-09-08
申请号：US137084
申请日：1980-04-03
申请人： Allan Wissner , Middleton B. Floyd, Jr.
发明人： Allan Wissner , Middleton B. Floyd, Jr.
IPC分类号： C07C45/59 , C07C49/743 , C07C59/245 , C07C405/00 , C07D307/42 , C07D307/54 , C07D307/60 , C07D317/16 , C07D317/18 , C07D317/34 , C07F7/18 , C07F9/54 , C07C49/597 , C07C35/06 , C07C49/798
CPC分类号： C07D307/42 , C07C405/0016 , C07C405/0025 , C07C45/59 , C07C49/743 , C07C59/245 , C07D307/54 , C07D307/60 , C07D317/16 , C07D317/18 , C07D317/34 , C07F7/1856 , C07F9/5407
摘要： Prostaglandin analogs are disclosed that have the .alpha.-chain terminating with the group --CH(OR')OR" wherein R' and R" are the same or different and are hydrogen, C.sub.1 to C.sub.4 alkanoyl or optionally substituted benzoyl, the substituents selected from the group C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, halo and trifluoromethyl. These compounds are useful as hypotensive agents, gastric secretory and platelet aggregation enhibitors and bronchodilators.
摘要翻译：公开前列腺素类似物，其具有以基团-CH（OR'）OR“终止的α-链，其中R'和R”相同或不同，并且是氢，C 1至C 4烷酰基或任选取代的苯甲酰基，取代基选自C1至C4烷基，C1至C4烷氧基，卤素和三氟甲基。这些化合物可用作降压药，胃分泌和血小板聚集抑制剂和支气管扩张剂。

8. 发明授权

US4289910A 1-Hydroxymethyl-prosten-1-ol derivatives 失效
标题翻译： 1-羟甲基 - 前列腺-1-醇衍生物
公开(公告)号：US4289910A
公开(公告)日：1981-09-15
申请号：US137029
申请日：1980-04-03
申请人： Allan Wissner , Middleton B. Floyd, Jr.
发明人： Allan Wissner , Middleton B. Floyd, Jr.
IPC分类号： C07C45/59 , C07C59/245 , C07C405/00 , C07D307/32 , C07D307/42 , C07D307/46 , C07D317/16 , C07D317/24 , C07D317/34 , C07F7/18 , C07C35/06 , C07C49/597
CPC分类号： C07D307/32 , C07C405/0016 , C07C405/0025 , C07C45/59 , C07C59/245 , C07D307/42 , C07D307/46 , C07D317/16 , C07D317/24 , C07D317/34 , C07F7/1856
摘要： Prostaglandin analogs are disclosed that have the .alpha.-chain terminating with the group --CH(OR')OR" wherein R' and R" are the same or different and are hydrogen, C.sub.1 to C.sub.4 alkanoyl or optionally substituted benzoyl, the substituents selected from the group C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, halo and trifluoromethyl. These compounds are useful as hypotensive agents, gastric secretory and platelet aggregation enhibitors and bronchodilators.
摘要翻译：公开前列腺素类似物，其具有以基团-CH（OR'）OR“终止的α-链，其中R'和R”相同或不同，并且是氢，C 1至C 4烷酰基或任选取代的苯甲酰基，取代基选自C1至C4烷基，C1至C4烷氧基，卤素和三氟甲基。这些化合物可用作降压药，胃分泌和血小板聚集抑制剂和支气管扩张剂。

9. 发明授权

US4291174A 1-Hydroxymethyl-15-hydroxy-prosten-1-ol derivatives 失效
标题翻译： 1-羟甲基-15-羟基 - 前列腺-1-醇衍生物
公开(公告)号：US4291174A
公开(公告)日：1981-09-22
申请号：US137050
申请日：1980-04-03
申请人： Allan Wissner , Middleton B. Floyd, Jr.
发明人： Allan Wissner , Middleton B. Floyd, Jr.
IPC分类号： C07C45/59 , C07C405/00 , C07D307/42 , C07D307/54 , C07D307/60 , C07D317/16 , C07D317/18 , C07D317/34 , C07F7/18 , C07C49/597 , C07C35/06 , C07C49/798
CPC分类号： C07D307/42 , C07C405/0025 , C07C45/59 , C07D307/54 , C07D307/60 , C07D317/16 , C07D317/18 , C07D317/34 , C07F7/1856 , Y10S514/822 , Y10S514/929
摘要： Prostaglandin analogs are disclosed that have the .alpha.-chain terminating with the group --CH(OR')OR" wherein R' and R" are the same or different and are hydrogen, C.sub.1 to C.sub.4 alkanoyl or optionally substituted benzoyl, the substituents selected from the group C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, halo and trifluoromethyl. These compounds are useful as hypotensive agents, gastric secretory and platelet aggregation inhibitors and bronchodilators.
摘要翻译：公开前列腺素类似物，其具有以基团-CH（OR'）OR“终止的α-链，其中R'和R”相同或不同，并且是氢，C 1至C 4烷酰基或任选取代的苯甲酰基，取代基选自C1至C4烷基，C1至C4烷氧基，卤素和三氟甲基。这些化合物可用作降压药，胃分泌和血小板聚集抑制剂和支气管扩张剂。

10. 发明授权

US4288632A 1-Hydroxymethyl-11,16-dihydroxy-prosten-1-ol derivatives 失效
标题翻译： 1-羟甲基-11,16-二羟基 - 前列腺-1-醇衍生物
公开(公告)号：US4288632A
公开(公告)日：1981-09-08
申请号：US137030
申请日：1980-04-03
申请人： Allan Wissner , Middleton B. Floyd, Jr.
发明人： Allan Wissner , Middleton B. Floyd, Jr.
IPC分类号： C07C45/59 , C07C49/707 , C07C51/09 , C07C405/00 , C07F7/18 , C07F9/54 , C07C35/06 , C07C49/597
CPC分类号： C07F7/1856 , C07C405/0016 , C07C405/0025 , C07C45/59 , C07C49/707 , C07C51/09 , C07F9/5407
摘要： Prostaglandin analogs are disclosed that have the .alpha.-chain terminating with the group --CH(OR')OR" wherein R' and R" are the same or different and are hydrogen, C.sub.1 to C.sub.4 alkanoyl or optionally substituted benzoyl, the substituents selected from the group C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, halo and trifluoromethyl. These compounds are useful as hypotensive agents, gastric secretory and platelet aggregation enhibitors and bronchodilators.
摘要翻译：公开前列腺素类似物，其具有以基团-CH（OR'）OR“终止的α-链，其中R'和R”相同或不同，并且是氢，C 1至C 4烷酰基或任选取代的苯甲酰基，取代基选自C1至C4烷基，C1至C4烷氧基，卤素和三氟甲基。这些化合物可用作降压药，胃分泌和血小板聚集抑制剂和支气管扩张剂。

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