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11. 发明授权

US06328855B1 Method for producing (+)-exo-6-phenyl-3-azabicyclo-[3.2.0]heptanes 失效
标题翻译：（+） - 外-6-苯基-3-氮杂双环[3.2.0]庚烷的制备方法
公开(公告)号：US06328855B1
公开(公告)日：2001-12-11
申请号：US09807218
申请日：2001-04-11
申请人： Norbert Bischof , Ernst Buschmann , Michael Henningsen , Georg Arnold Krei , Rainer Munschauer , Thomas Pfeiffer , Gerd Steiner , Wolfgang Viergutz
发明人： Norbert Bischof , Ernst Buschmann , Michael Henningsen , Georg Arnold Krei , Rainer Munschauer , Thomas Pfeiffer , Gerd Steiner , Wolfgang Viergutz
IPC分类号： C07D20952
CPC分类号： C07D209/52
摘要： A process for preparing (+)-exo-6-phenyl-3-azabicyclo[3.2.0]heptanes of the formula I where R is hydrogen, chlorine, bromine, fluorine or methoxy, which comprises photocyclizing a bisallylammonium salt of the formula II where R has the meanings given above and X− is an anion, in an inert solvent in a glass apparatus with addition of sensitizer and precipitating using (−)-ditoluoyltartaric acid the desired (+)-exo-isomer I as ditoluoyltartrate from the resulting mixture, with or without recrystallization of this tartrate from an alcohol/water mixture.
摘要翻译：制备式I的（+） - 外-6-苯基-3-氮杂双环[3.2.0]庚烷的方法，其中R是氢，氯，溴，氟或甲氧基，其包括将式II的双烯丙基铵盐光环化，其中R 具有上述含义，X-是阴离子，在玻璃装置的惰性溶剂中，加入敏化剂并使用（ - ） - 二甲酰基酒石酸从所得混合物中将所需的（+） - 外异构体I作为二异氰酸甲酯酒石酸盐沉淀，有或没有酒石酸盐与酒精/水混合物重结晶。

12. 发明授权

US07863444B2 4-aminopyrrolopyrimidines as kinase inhibitors 有权
标题翻译： 4-氨基吡咯并嘧啶作为激酶抑制剂
公开(公告)号：US07863444B2
公开(公告)日：2011-01-04
申请号：US09399083
申请日：1999-09-17
申请人： David Calderwood , Lee Arnold , Hormoz Mazdiyasni , Gavin C. Hirst , Bojuan B. Deng , David N. Johnston , Paul Rafferty , Gerald B. Tometzki , Helen L. Twigger , Rainer Munschauer
发明人： David Calderwood , Lee Arnold , Hormoz Mazdiyasni , Gavin C. Hirst , Bojuan B. Deng , David N. Johnston , Paul Rafferty , Gerald B. Tometzki , Helen L. Twigger , Rainer Munschauer
IPC分类号： C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： Chemical compounds having structural formula I and physiologically acceptable salts thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the kinases whose activity is inhibited by these compounds are involved in immunologic, hyperproliferative or angiogenic processes. Thus, these compounds can ameliorate disase states where angiogenesis or endothelial cell hyperproliferaton is a factor. These compounds can be used to treat cancer, hyperproliferative disorders, rheumatoid artheritis, disorders of the immune system, transplant rejection, and inflammatory disorders.
摘要翻译：具有结构式I的化合物及其生理上可接受的盐是丝氨酸/苏氨酸和酪氨酸激酶活性的抑制剂。活性被这些化合物抑制的几种激酶参与免疫学，过度增殖或血管发生过程。因此，这些化合物可以改善其中血管生成或内皮细胞过度膨胀是一个因素的疾病状态。这些化合物可用于治疗癌症，过度增殖性疾病，类风湿性关节炎，免疫系统紊乱，移植排斥和炎症性疾病。

13. 发明授权

US06713474B2 Pyrrolopyrimidines as therapeutic agents 有权
标题翻译：吡咯并嘧啶作为治疗剂
公开(公告)号：US06713474B2
公开(公告)日：2004-03-30
申请号：US09537167
申请日：2000-03-29
申请人： Gavin C. Hirst , David Calderwood , Rainer Munschauer , Lee D. Arnold , David N. Johnston , Paul Rafferty
发明人： Gavin C. Hirst , David Calderwood , Rainer Munschauer , Lee D. Arnold , David N. Johnston , Paul Rafferty
IPC分类号： C07D48704
CPC分类号： C07D487/04 , C07F9/6561 , C07F9/65842
摘要： Chemical compounds having structural formula I and physiologically acceptable salts and metabolites thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the kinases, whose activity is inhibited by these chemical compounds, are involved in immunologic, hyperproliferative, or angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyper proliferative disorders, rheumatiod arthritis, disorders of the immune system, trasplant rejections and imflammatory disorders.
摘要翻译：具有结构式I的化合物及其生理上可接受的盐及其代谢物是丝氨酸/苏氨酸和酪氨酸激酶活性的抑制剂。其活性被这些化合物抑制的几种激酶参与免疫学，过度增殖或血管发生过程。因此，这些化合物可以改善其中血管生成或内皮细胞过度增殖是一个因素的疾病状态。这些化合物可用于治疗癌症和高增殖性疾病，风湿性关节炎，免疫系统疾病，寄生虫排斥和炎症性疾病。

14. 发明授权

US6001839A Substituted 4-amino-7H-pyrrolo [2,3,-d]-pyrimidines as PTK inhibitors 失效
标题翻译：取代的4-氨基-7H-吡咯并[2,3，-d] - 嘧啶作为PTK抑制剂
公开(公告)号：US6001839A
公开(公告)日：1999-12-14
申请号：US42702
申请日：1998-03-17
申请人： David J. Calderwood , David N. Johnston , Paul Rafferty , Helen L. Twigger , Rainer Munschauer , Lee Arnold
发明人： David J. Calderwood , David N. Johnston , Paul Rafferty , Helen L. Twigger , Rainer Munschauer , Lee Arnold
IPC分类号： A61K31/519 , A61P35/00 , A61P37/02 , A61P43/00 , C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： Compounds of formula I ##STR1## including pharmaceutically acceptable salts thereof in which R.sub.1 represents hydrogen, 2-phenyl-1,3-dioxan-5-yl, a C.sub.1-6 alkyl group, a C.sub.3-8 cycloalkyl group, a C.sub.5-7 cycloalkenyl group or an (optionally substituted phenyl)C.sub.1-6 alkyl group wherein the alkyl, cycloalkyl and cycloalkenyl groups are optionally substituted by one or more groups of formula OR.sub.A in which R.sub.A represents H or a C.sub.1-6 alkyl group provided that a group of formula OR.sub.A is not located on the carbon attached to nitrogen;R.sub.2 represents hydrogen, a C.sub.1-6 alkyl group, a C.sub.3-8 cycloalkyl group, halo, hydroxy, an (optionally substituted phenyl)C.sub.1-6 alkyl group, optionally substituted phenyl or R.sub.4 ; andR.sub.3 represents a group of formula (a) ##STR2## in which the phenyl ring is additionally optionally substituted and A represents NH, O, NHSO.sub.2, SO.sub.2 NH, a C.sub.1-4 alkylene chain, NHCO, NHCO.sub.2, CONH, NHCONH, CO.sub.2 or S(O).sub.p in which p is 0, 1 or 2, or A is absent and R.sub.5 is attached directly to the phenyl ring;and R.sub.5 represents optionally substituted phenyl and, additionally, when A is absent R.sub.5 represents a) a phthalimido group optionally substituted by halo or b) a pyrazolylamino group in which the pyrazole ring is optionally substituted by one or more of the following: hydroxy or optionally substituted phenyl;R.sub.4 represents a heterocyclic group; are described which are useful in treating proliferative diseases and disorders of the immune system in mammals. Processes to prepare these compounds and pharmaceutical compositions containing these compound are also described.
摘要翻译：式I化合物，其包括其药学上可接受的盐，其中R 1表示氢，2-苯基-1,3-二恶烷-5-基，C 1-6烷基，C 3-8环烷基，C 5-7环烯基或（任选取代的苯基）C 1-6烷基，其中烷基，环烷基和环烯基任选被一个或多个RAA代表H或C 1-6烷基的式ORA基团取代，条件是式ORA基团为不位于附着在氮上的碳上; R 2表示氢，C 1-6烷基，C 3-8环烷基，卤素，羟基，（任选取代的苯基）C 1-6烷基，任选取代的苯基或R 4; 并且R 3表示式（a）的基团，其中苯环另外被任意取代，A代表NH，O，NHSO 2，SO 2 NH，C 1-4亚烷基链，NHCO，NHCO 2，CONH，NHCONH，CO 2或S ）p，其中p是0,1或2，或A不存在，R 5直接连接到苯环上; 并且另外，当A不存在时，R 5表示a）任选被卤素取代的苯二甲酰亚氨基，或b）吡唑基氨基，其中吡唑环任选被一个或多个下述取代基取代：羟基或任选地取代的苯基; R4表示杂环基; 被描述为可用于治疗哺乳动物免疫系统的增殖性疾病和病症。还描述了制备这些化合物的方法和含有这些化合物的药物组合物。

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