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41. 发明授权

US07781591B2 Substituted 3-cyanopyridines as protein kinase inhibitors 有权
标题翻译：取代的3-氰基吡啶作为蛋白激酶抑制剂
公开(公告)号：US07781591B2
公开(公告)日：2010-08-24
申请号：US11818119
申请日：2007-06-13
申请人： Derek Cecil Cole , Diane Harris Boschelli , Yanong Daniel Wang , Magda Asselin , Diane Marie Joseph-McCarthy , Amarnauth Shastrie Prashad , Allan Wissner , Russell Dushin , Biqi Wu , Lawrence Nathan Tumey , Chuan S. Niu , Joan Chen
发明人： Derek Cecil Cole , Diane Harris Boschelli , Yanong Daniel Wang , Magda Asselin , Diane Marie Joseph-McCarthy , Amarnauth Shastrie Prashad , Allan Wissner , Russell Dushin , Biqi Wu , Lawrence Nathan Tumey , Chuan S. Niu , Joan Chen
IPC分类号： C07D401/14
CPC分类号： C07D213/85 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐，水合物和酯，其中R 1，R 2和X如本文所定义。本教导还提供制备式I化合物的方法，以及通过向包括人的哺乳动物施用治疗有效量的式I化合物或化合物来治疗自身免疫性和炎性疾病的方法。

42. 发明申请

US20070287708A1 Substituted 3-cyanopyridines as protein kinase inhibitors 有权
标题翻译：取代的3-氰基吡啶作为蛋白激酶抑制剂
公开(公告)号：US20070287708A1
公开(公告)日：2007-12-13
申请号：US11818119
申请日：2007-06-13
申请人： Derek Cole , Diane Boschelli , Yanong Wang , Magda Asselin , Diane Joseph-McCarthy , Amarnauth Prashad , Allan Wissner , Russell Dushin , Biqi Wu , Lawrence Tumey , Chuan Niu , Joan Chen
发明人： Derek Cole , Diane Boschelli , Yanong Wang , Magda Asselin , Diane Joseph-McCarthy , Amarnauth Prashad , Allan Wissner , Russell Dushin , Biqi Wu , Lawrence Tumey , Chuan Niu , Joan Chen
IPC分类号： A61K31/5377 , A61K31/4439 , C07D413/14 , C07D405/14 , C07D409/14 , C07D403/14
CPC分类号： C07D213/85 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐，水合物和酯，其中R 1，R 2和X如本文所定义。本教导还提供制备式I化合物的方法，以及通过向包括人的哺乳动物施用治疗有效量的式I化合物或化合物来治疗自身免疫性和炎性疾病的方法。

43. 发明授权

US5234918A Certain phosphinyl-oxy-phenyl-methyl-pyridinium-hydroxide inner salts useful as antagonists of PAF 失效
标题翻译：某些氧膦基 - 氧 - 苯基 - 甲基 - 吡啶鎓氢氧化物内盐可用作PAF的拮抗剂
公开(公告)号：US5234918A
公开(公告)日：1993-08-10
申请号：US763714
申请日：1991-09-23
申请人： Allan Wissner , Robert E. Schaub , Phaik-eng Sum
发明人： Allan Wissner , Robert E. Schaub , Phaik-eng Sum
IPC分类号： C07C43/174 , C07C43/178 , C07C59/125 , C07C309/73 , C07D213/20 , C07D215/10 , C07D277/22 , C07D521/00 , C07F9/12 , C07F9/58 , C07F9/60 , C07F9/62 , C07F9/6509 , C07F9/6539
CPC分类号： C07D213/20 , C07C309/73 , C07C43/1745 , C07C43/1785 , C07C59/125 , C07D215/10 , C07D231/12 , C07D233/56 , C07D249/08 , C07D277/22 , C07F9/12 , C07F9/581 , C07F9/60 , C07F9/62 , C07F9/650911 , C07F9/650958 , C07F9/6539
摘要： The invention is a compound of R or S enantiomers or racemic mixtures of compounds of the formula: ##STR1## wherein: (A) is ##STR2## Y is (i) C.sub.1 -C.sub.24(ii) C.sub.1 -C.sub.24 alkoxy;(iii) C.sub.1 -C.sub.24 carboamoyloxy;Y is the divalent radical ##STR3## which are PAF inhibitors.
摘要翻译：本发明是下式化合物的R或S对映异构体或外消旋混合物的化合物：其中：（A）是（i）C 1 -C 24（ⅱ）C 1 -C 24烷氧基; （iii）C 1 -C 24甲酰氧基; Y是PAF抑制剂的二价基团“IMAGE”。

44. 发明授权

US5208247A Pyridinium compounds which are useful as antagonists of platelet activating factor 失效
标题翻译：可用作平板激活因子的拮抗剂的吡啶鎓化合物
公开(公告)号：US5208247A
公开(公告)日：1993-05-04
申请号：US738961
申请日：1991-08-01
申请人： Michael P. Trova , Allan Wissner
发明人： Michael P. Trova , Allan Wissner
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4412 , A61K31/4418 , A61K31/4425 , A61P7/02 , A61P9/00 , C07D213/38 , C07D213/40 , C07D213/56 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/89 , C07D471/04
CPC分类号： C07D213/40 , C07D213/56 , C07D213/75 , C07D213/81 , C07D471/04
摘要： The invention is aryl, amide, imide and carbamate pyridine antagonists of platelet activating factor.

45. 发明授权

US5124147A Method for the treatment of endotoxic shock in a mammal 失效
标题翻译：用于治疗哺乳动物内毒素的方法
公开(公告)号：US5124147A
公开(公告)日：1992-06-23
申请号：US482141
申请日：1990-02-16
申请人： Allan Wissner , Suresh S. Kerwar , Constance Kohler
发明人： Allan Wissner , Suresh S. Kerwar , Constance Kohler
IPC分类号： A61K31/00 , A61K39/395 , A61K39/40 , A61K45/00 , A61P9/00 , A61P31/00 , A61P43/00
CPC分类号： A61K39/395
摘要： The invention is a method of treating endotoxic shock in a mammal which comprises administering to the mammal a therapeutically effective amount of an antagonist to Platelet Activating Factor in combination with a therapeutically effective amount of one or more monoclonal or polyclonal antibodies directed toward either Tumor Necrosis Factor .alpha., Interleukin-1.beta., Gamma Interferon, or bacterial cell wall lipopolysaccharides.

46. 发明授权

US4762942A Antihypertensive phosphate derivatives 失效
标题翻译：抗高血压磷酸盐衍生物
公开(公告)号：US4762942A
公开(公告)日：1988-08-09
申请号：US679788
申请日：1984-12-10
申请人： Allan Wissner , Phaik E. Sum , Robert E. Schaub
发明人： Allan Wissner , Phaik E. Sum , Robert E. Schaub
IPC分类号： C07F9/10
CPC分类号： C07F9/10
摘要： Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is selected from one or more of: (a) C.sub.1 -C.sub.24 branched or straight chain alkyl; (b) C.sub.1 -C.sub.24 branched or straight chain alkoxy; (c) ##STR2## wherein n and m are integers from 0 to 25 and the sum of n and m is less than or equal to 25; phenyl; substituted phenyl wherein the substituents are selected from the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, C.sub.1 -C.sub.20 branched or straight chain alkoxy, halogen, trifluoromethyl, phenyl, and substituted phenyl, phenoxy; and substituted phenoxy, wherein the substituents are selected from the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, halogen, trifluoromethyl, phenyl and substituted phenyl; Q is selected from the group consisting of: ##STR3## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino and wherein R.sub.3 is C.sub.1 -C.sub.4 alkyl, with the proviso that when Q is ##STR4## then R.sub.1 is C.sub.1 -C.sub.4 branched or straight chain alkyl; T is a bivalent radical selected from the group consisting of --(CHR).sub.p -- and ##STR5## wherein p is an integer from 1 to 15, the moiety --(CHR).sub.p -- represents an alkylene chain substituted at any position with one or more C.sub.1 -C.sub.10 alkyl groups or phenyl groups, and the moiety ##STR6## is bound with the oxygen atom attached directly to the aromatic ring; and Z is ##STR7## wherein R.sub.2 is hydrogen or C.sub.1 -C.sub.4 branched or straight chain alkyl and q is an interger from 4 to 7; in either the racemic or optically active forms.
摘要翻译：描述了具有下式的抗高血压磷酸酯衍生物：其中X选自以下中的一种或多种：（a）C 1 -C 24支链或直链烷基; （b）C 1 -C 24支链或直链烷氧基; （c）其中n和m是0至25的整数，n和m的总和小于或等于25; 苯基; 取代基苯基，其中取代基选自C 1 -C 20支链或直链烷基，C 1 -C 20支链或直链烷氧基，卤素，三氟甲基，苯基和取代的苯基，苯氧基; 和取代的苯氧基，其中取代基选自C 1 -C 20支链或直链烷基，卤素，三氟甲基，苯基和取代的苯基; Q选自：其中R 1选自氢，C 1 -C 4支链或直链烷基，C 1 -C 4支链或直链烷氧基和C 1 -C 4支链或直链烷基氨基和其中R 3为C 1 -C 4烷基，条件是当Q为“IMA”时，R 1为C 1 -C 4支链或直链烷基; T是选自 - （CHR）p - 和的二价基团，其中p是1至15的整数， - （CHR）p - 部分代表在任何位置被一个或多个更多的C 1 -C 10烷基或苯基，并且部分“IMAGE”与直接与芳环连接的氧原子结合; 并且Z是，其中R 2是氢或C 1 -C 4支链或直链烷基，q是4至7的整数; 以外消旋或旋光形式。

47. 发明授权

US4762935A Precursors and synthesis of methyl-9-oxo-11.alpha.,16-dihydroxy-16-vinyl-5-cis-13-trans-prostadienoa tes 失效
标题翻译：甲基-9-氧代-11α，16-二羟基-16-乙烯基-5-顺式-13-反 - 前列腺素的前体和合成
公开(公告)号：US4762935A
公开(公告)日：1988-08-09
申请号：US915432
申请日：1986-10-06
申请人： Allan Wissner , Kenneth E. Green , Philip R. Hamann , Jeremy Levin
发明人： Allan Wissner , Kenneth E. Green , Philip R. Hamann , Jeremy Levin
IPC分类号： C07D309/12 , C07C41/00 , C07C41/60 , C07C43/32 , C07C67/00 , C07C401/00 , C07C405/00 , C07F7/18 , C07F7/22
CPC分类号： C07C43/32 , C07C41/60 , C07F7/18
摘要： This disclosure describes novel compounds which are useful as precursors in the synthesis of 9-oxo-11.alpha.,16-dihydroxy-16-vinyl-5-cis-13-trans-prostadienoate esters which possess activity as hypotensive agents and/or as vasodilators.
摘要翻译：本公开描述了在合成具有作为降血压剂和/或血管扩张剂活性的9-氧代-11α，16-二羟基-16-乙烯基-5-顺式-13-反 - 前列腺素酯的9-氧代-11α-十一 - 。

48. 发明授权

US4703130A Antihypertensive phosphate derivatives 失效
标题翻译：抗高血压磷酸盐衍生物
公开(公告)号：US4703130A
公开(公告)日：1987-10-27
申请号：US679789
申请日：1984-12-10
申请人： Allan Wissner
发明人： Allan Wissner
IPC分类号： C07F9/10
CPC分类号： C07F9/10
摘要： Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein W is selected from the group consisting of methyl and phenyl optionally substituted with C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and phenyl; r, n, m and a are integers such that the expression r+(n+1)m+a is also an integer and has a value of 3 to 20; r is greater than or equal to 2; n is greater than or equal to 2; m is greater than or equal to zero and a is greater than or equal to zero; T is selected from the group consisting of hydrogen and ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino; Q is a bivalent radical selected from --(CH.sub.2).sub.p -- and --(CHR).sub.p --, wherein p is an integer 2-12 and the moiety --(CHR).sub.p -- represents an alkylene chain which is substituted by one or more C.sub.1 -C.sub.10 alkyl groups or phenyl groups; Z is selected from the group consisting of ##STR3## wherein R.sub.2 may be the same or different and is selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 branched or straight chain alkyl and q is an integer from 4-7; in either the racemic or optically active forms.
摘要翻译：描述了具有下式的抗高血压磷酸酯衍生物：其中W选自甲基和任选被C 1 -C 3烷基，C 1 -C 3烷氧基和苯基取代的苯基; r，n，m和a是整数，使得表达式r +（n + 1）m + a也是整数，并且具有3至20的值; r大于或等于2; n大于或等于2; m大于或等于零，a大于或等于零; T选自氢和其中R 1选自氢，C 1 -C 4支链或直链烷基，C 1 -C 4支链或直链烷氧基和C 1 -C 4支链或直链烷基氨基 ; Q是选自 - （CH 2）p - 和 - （CHR）p - 的二价基团，其中p是整数2-12，部分 - （CHR）p - 表示被一个或多个C1取代的亚烷基链 -C 10烷基或苯基; Z选自，其中R2可以相同或不同，并且选自氢和C 1 -C 4支链或直链烷基，q是4-7的整数; 以外消旋或旋光形式。

49. 发明授权

US4328359A 15-Deoxy-16-substituted-19-chloro-20-nor-prostane derivatives of the E and F series 失效
标题翻译： E和F系列的15-脱氧-16-取代-19-氯-20-去 - 前列腺衍生物
公开(公告)号：US4328359A
公开(公告)日：1982-05-04
申请号：US233044
申请日：1981-02-10
申请人： Allan Wissner
发明人： Allan Wissner
IPC分类号： C07C29/42 , C07C45/45 , C07C405/00 , C07F7/08 , C07F7/18 , C07F7/22 , C07C177/00
CPC分类号： C07F7/2212 , C07C29/42 , C07C405/00 , C07C405/0025 , C07C45/45 , C07F7/0818 , C07F7/1804
摘要： The invention disclosed herein relates to pharmacologically active prostaglandin derivatives of the E and F series wherein C-16 is substituted with hydrogen, methyl, vinyl or ethynyl and C-19 substituted with chloro and the .beta.-chain consists of 7 carbon atoms.
摘要翻译：本文公开的本发明涉及E和F系列的药理学活性前列腺素衍生物，其中C-16被氢，甲基，乙烯基或乙炔基取代，C-19被氯取代，β-链由7个碳原子组成。

50. 发明授权

US4297516A 1-Substituted-1-oxo-prostane-derivatives of the E, A and F series 失效
标题翻译： E，A和F系列1-取代的1-氧代 - 前列腺衍生物
公开(公告)号：US4297516A
公开(公告)日：1981-10-27
申请号：US46721
申请日：1979-06-07
申请人： Allan Wissner
发明人： Allan Wissner
IPC分类号： C07C29/42 , C07C43/178 , C07C45/00 , C07C45/29 , C07C45/51 , C07C45/63 , C07C45/70 , C07C45/71 , C07C45/75 , C07C47/21 , C07C49/203 , C07C53/50 , C07C62/38 , C07C405/00 , C07D307/54 , C07D317/26 , C07D317/34 , C07F7/22 , C07F9/655 , C07C177/00
CPC分类号： C07F9/65515 , C07C29/42 , C07C405/0025 , C07C43/178 , C07C45/00 , C07C45/29 , C07C45/51 , C07C45/63 , C07C45/70 , C07C45/71 , C07C45/75 , C07C47/21 , C07C49/203 , C07C53/50 , C07C62/38 , C07D307/54 , C07D317/26 , C07D317/34 , C07F7/2212 , C07B2200/09 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要： The invention disclosed herein relates to pharmacologically active prostaglandin derivatives of the E, F, or A series having on the terminal methylene carbon of the alpha chain, a substituent selected from the group consisting of: ##STR1## wherein R is C.sub.1 to C.sub.6 alkyl, and phenyl or phenyl substituted with one or more substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, OR.sub.16, SR.sub.16, F, or Cl, and R.sub.16 is C.sub.1 to C.sub.6 alkyl.
摘要翻译：本文公开的本发明涉及在α链末端亚甲基上具有选自以下的取代基的E，F或A系列的药理学活性前列腺素衍生物：其中R为C1至 C6烷基，苯基或被一个或多个选自C1-C4烷基，OR16，SR16，F或C1的取代基取代的苯基，R16是C1-C6烷基。

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