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11. 发明授权

US5641783A Substituted amino alcohol compounds 失效
标题翻译：取代氨基醇化合物
公开(公告)号：US5641783A
公开(公告)日：1997-06-24
申请号：US303842
申请日：1994-09-08
申请人： J. Peter Klein , Gail E. Underiner , Anil M. Kumar
发明人： J. Peter Klein , Gail E. Underiner , Anil M. Kumar
IPC分类号： A61K31/45 , A61K31/47 , A61K31/513 , A61K31/519 , A61K31/522 , C07C215/08 , C07C215/56 , C07C217/62 , C07C217/64 , C07C229/22 , C07C233/36 , C07C233/78 , C07C233/91 , C07D207/40 , C07D207/404 , C07D209/48 , C07D211/76 , C07D211/88 , C07D217/24 , C07D239/54 , C07D239/90 , C07D239/96 , C07D295/13 , C07D473/10 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/52
CPC分类号： C07D207/404 , A61K31/45 , A61K31/47 , A61K31/513 , A61K31/519 , A61K31/522 , C07C215/08 , C07C215/56 , C07C217/62 , C07C217/64 , C07C229/22 , C07C233/36 , C07C233/78 , C07C233/91 , C07D209/48 , C07D211/76 , C07D211/88 , C07D217/24 , C07D239/54 , C07D239/90 , C07D239/96 , C07D295/13 , C07D473/10
摘要： Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.4 is a terminal moiety comprising a substituted or unsubstituted, oxidized or reduced ring system, the ring system having a single ring or two to three fused rings, a ring comprising from three to seven ring atoms. The disclosed compounds are effective agents to inhibit undesirable responses to cell stimuli.
摘要翻译：公开了具有式I的直链或支链脂族烃结构的化合物：一至四，m为四至二十的整数。独立地，R 1和R 2是氢，直链或支链烷基，链烯基或长链多至20个碳原子的炔基或 - （CH 2）w R 5。如果R 1或R 2是 - （CH 2）w R 5，则w可以是1-20的整数，R 5可以是羟基，卤素，C 1-8烷氧基或取代或未取代的碳环或杂环。或者，R 1和R 2可以共同形成具有4-8个碳原子的取代或未取代的饱和或不饱和杂环，N是所得杂环的杂原子。 R3可以是氢或C1-3。在化合物中，包含R 1或R 2，（CH 2）n和（CH 2）m的碳原子总和不超过40个。 R4是包含取代或未取代的氧化或还原环系的末端部分，该环系具有单环或二至三个稠环，包含3-7个环原子的环。所公开的化合物是抑制对细胞刺激的不良反应的有效试剂。

12. 发明授权

US5807861A Amine substituted xanthinyl compounds 失效
标题翻译：胺取代的黄原胶化合物
公开(公告)号：US5807861A
公开(公告)日：1998-09-15
申请号：US476911
申请日：1995-06-07
申请人： J. Peter Klein , Gail E. Underiner , Anil M. Kumar , Lance H. Ridgers , Glenn C. Rice , David W. Leung
发明人： J. Peter Klein , Gail E. Underiner , Anil M. Kumar , Lance H. Ridgers , Glenn C. Rice , David W. Leung
IPC分类号： C07D239/54 , C07D473/04 , C07D473/06 , C07D487/04 , C07D513/04 , A61K31/52
CPC分类号： C07D239/54 , C07D473/04 , C07D473/06 , C07D487/04 , C07D513/04
摘要： A method for treating a disease caused by an undesirable cell response mediated by a proliferative intracellular signaling pathway is provided wherein an effective amount of a compound is administered. The compound, resolved enantiomers, diastereomers, hydrates, salts, solvates and mixtures thereof, has the formula CORE MOIETY--(R).sub.j wherein j is an integer from one to three; the core moiety is xanthinyl; and R is independently selected from the group consisting of amine, hydrogen, halogen, hydroxyl, C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, 2-bromopropyl, 4-chloropentyl, cyclohexyl, cyclopentyl, 3-dimethylaminobutyl, 2-hydroxyethyl, 5-hydroxyhexyl, 3-hydroxy-n-butyl, 3-hydroxypropyl, 2-methoxyethyl, 4-methoxy-n-butyl, phenyl, and formula I, at least one R comprising formula I ##STR1## wherein (CH.sub.2).sub.n is optionally substituted; n is an integer from five to twenty; each R.sub.1 or R.sub.2 is independently hydrogen or an optionally substituted group that is herein defined; and wherein, when the (CH.sub.2).sub.n, R.sub.1 or R.sub.2 is substituted, a substituent is selected from the group consisting of carbamoyl, primary, secondary and tertiary amino, C.sub.(2-8) alkenyl, C.sub.(1-8) alkyl, C.sub.(1-8) alkoxyl, C.sub.(1-8) hydroxyalkyl, azido, carbonato, carbonyl, carboxyl, cyano, C.sub.(1-8) haloalkyl, isocyano, isomercaptocyano, phospho, phosphonato, sulfonato, alkylsulfonyl, alkylsulfoxidyl, mercaptocarbonyl, mercaptocarbonato, thioureido and ureido.
摘要翻译：提供了治疗由增殖性细胞内信号传导途径介导的不良细胞应答引起的疾病的方法，其中施用有效量的化合物。化合物，拆分的对映体，非对映异构体，水合物，盐，溶剂合物及其混合物具有式CORE MOIETY-（R）j，其中j是1至3的整数; 核心部分是xanthinyl; 并且R独立地选自胺，氢，卤素，羟基，C（1-10）烷基，C（2-10）烯基，2-溴丙基，4-氯戊基，环己基，环戊基，3-二甲基氨基丁基， 2-羟基乙基，5-羟基己基，3-羟基 - 正丁基，3-羟基丙基，2-甲氧基乙基，4-甲氧基 - 正丁基，苯基和式I，至少一个R包括式I其中（CH 2）n任选被取代; n是从5到20的整数; 每个R 1或R 2独立地为氢或本文定义的任选取代的基团; 并且其中当（CH 2）n，R 1或R 2被取代时，取代基选自氨基甲酰基，伯，仲和叔氨基，C（2-8）烯基，C（1-8）烷基， C（1-8）烷氧基，C（1-8）羟基烷基，叠氮基，碳酸根，羰基，羧基，氰基，C（1-8）卤代烷基，异氰基，异构体巯基，磷酸根，膦酸根，磺酸根，烷基磺酰基，烷基亚砜基，巯基羰基，巯基羰基，硫脲基和脲基。

13. 发明授权

US5801182A Amine substituted compounds 失效
标题翻译：胺取代的化合物
公开(公告)号：US5801182A
公开(公告)日：1998-09-01
申请号：US485777
申请日：1995-06-07
申请人： J. Peter Klein , Gail E. Underiner , Anil M. Kumar , Lance H. Ridgers
发明人： J. Peter Klein , Gail E. Underiner , Anil M. Kumar , Lance H. Ridgers
IPC分类号： C07D239/54 , C07D473/04 , C07D473/06 , C07D487/04 , C07D513/04 , A61K31/505 , C07D239/02
CPC分类号： C07D239/54 , C07D473/04 , C07D473/06 , C07D487/04 , C07D513/04
摘要： Compounds and pharmaceutical compositions, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, have the formula: CORE MOIETY --(R).sub.j In these compounds, j is an integer from one to three; the core moiety is a cyclic core, the cyclic core being non-cyclic or at least one five- to seven-member non-heterocyclic ring or heterocycle; and R is selected from the group consisting of amine, hydrogen, halogen, hydroxyl, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, cyclic or heterocyclic group or formula I. At least one R having formula I: ##STR1## In formula I, n is an integer from four to twenty; and each R.sub.1 or R.sub.2 is independently hydrogen, substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or cyclic or heterocyclic group. The compounds are useful in treating or preventing, for example, sepsis syndrome, hematopoietic or organ toxicity, cancer, viral activity, AIDS and AIDS-related indications, allopecia caused by cytotoxic therapies, and progression of an inflammatory or autoimmune disease.
摘要翻译：化合物和药物组合物，包括拆分的对映异构体和/或非对映异构体，水合物，盐，溶剂合物及其混合物，具有下式：CORE MOIETY - （R）j在这些化合物中，j是1至3的整数; 核心部分是环核心，环核心是非环状的或至少一个五至七元的非杂环环或杂环; 并且R选自胺，氢，卤素，羟基，取代或未取代的C（1-10）烷基，C（2-10）烯基，环状或杂环基或式I化合物。至少一种具有式 I： I在式I中，n是4至20的整数; 并且每个R 1或R 2独立地为氢，取代或未取代的C 1-20烷基，C（1-20）烷氧基，C（2-20）烯基或环状或杂环基。该化合物可用于治疗或预防例如败血症综合征，造血或器官毒性，癌症，病毒活性，AIDS和AIDS相关适应症，由细胞毒性疗法引起的脱发，以及炎性或自身免疫性疾病的进展。

14. 发明授权

US5750575A Substituted amino alcohol compounds 失效
标题翻译：取代氨基醇化合物
公开(公告)号：US5750575A
公开(公告)日：1998-05-12
申请号：US475721
申请日：1995-06-07
申请人： J. Peter Klein , Gail E. Underiner , Anil M. Kumar
发明人： J. Peter Klein , Gail E. Underiner , Anil M. Kumar
IPC分类号： A61K31/45 , A61K31/47 , A61K31/513 , A61K31/519 , A61K31/522 , C07C215/08 , C07C215/56 , C07C217/62 , C07C217/64 , C07C229/22 , C07C233/36 , C07C233/78 , C07C233/91 , C07D207/40 , C07D207/404 , C07D209/48 , C07D211/76 , C07D211/88 , C07D217/24 , C07D239/54 , C07D239/90 , C07D239/96 , C07D295/13 , C07D473/10 , A61K31/165 , A61K31/135 , C07C215/20 , C07C233/35
CPC分类号： C07D207/404 , A61K31/45 , A61K31/47 , A61K31/513 , A61K31/519 , A61K31/522 , C07C215/08 , C07C215/56 , C07C217/62 , C07C217/64 , C07C229/22 , C07C233/36 , C07C233/78 , C07C233/91 , C07D209/48 , C07D211/76 , C07D211/88 , C07D217/24 , C07D239/54 , C07D239/90 , C07D239/96 , C07D295/13 , C07D473/10
摘要： Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.4 is a carbocycle comprising a substituted or unsubstituted ring system, the ring system having a single ring or two fused rings, a ring comprising from three to seven ring atoms. The disclosed compounds are effective agents to inhibit undesirable responses to cell stimuli.
摘要翻译：公开了具有式I的直链或支链脂族烃结构的化合物：一至四，m为四至二十的整数。独立地，R 1和R 2是氢，直链或支链烷基，链烯基或长链多至20个碳原子的炔基或 - （CH 2）w R 5。如果R 1或R 2是 - （CH 2）w R 5，则w可以是1-20的整数，R 5可以是羟基，卤素，C 1-8烷氧基或取代或未取代的碳环或杂环。或者，R 1和R 2可以共同形成具有4-8个碳原子的取代或未取代的饱和或不饱和杂环，N是所得杂环的杂原子。 R3可以是氢或C1-3。在化合物中，包含R 1或R 2，（CH 2）n和（CH 2）m的碳原子总和不超过40个。 R4是包含取代或未取代的环系的碳环，所述环体系具有单环或两个稠环，包含3-7个环原子的环。所公开的化合物是抑制对细胞刺激的不良反应的有效试剂。

15. 发明授权

US5824677A Substituted amino alcohol compounds 失效
标题翻译：取代氨基醇化合物
公开(公告)号：US5824677A
公开(公告)日：1998-10-20
申请号：US474816
申请日：1995-06-07
申请人： J. Peter Klein , Gail E. Underiner , Anil M. Kumar
发明人： J. Peter Klein , Gail E. Underiner , Anil M. Kumar
IPC分类号： A61K31/45 , A61K31/47 , A61K31/513 , A61K31/519 , A61K31/522 , C07C215/08 , C07C215/56 , C07C217/62 , C07C217/64 , C07C229/22 , C07C233/36 , C07C233/78 , C07C233/91 , C07D207/40 , C07D207/404 , C07D209/48 , C07D211/76 , C07D211/88 , C07D217/24 , C07D239/54 , C07D239/90 , C07D239/96 , C07D295/13 , C07D473/10 , A61K31/385 , A61K31/445 , A61K31/505
CPC分类号： C07D207/404 , A61K31/45 , A61K31/47 , A61K31/513 , A61K31/519 , A61K31/522 , C07C215/08 , C07C215/56 , C07C217/62 , C07C217/64 , C07C229/22 , C07C233/36 , C07C233/78 , C07C233/91 , C07D209/48 , C07D211/76 , C07D211/88 , C07D217/24 , C07D239/54 , C07D239/90 , C07D239/96 , C07D295/13 , C07D473/10
摘要： Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.4 is a hetorocycle comprising a substituted or unsubstituted, oxidized or reduced ring system, the ring system having a single ring or two to three fused rings, a ring comprising from three to seven ring atoms. The disclosed compounds are effective agents to inhibit undesirable responses to cell stimuli.
摘要翻译：公开了具有式I的直链或支链脂族烃结构的化合物：一至四，m为四至二十的整数。独立地，R 1和R 2是氢，直链或支链烷基，链烯基或长链多至20个碳原子的炔基或 - （CH 2）w R 5。如果R 1或R 2是 - （CH 2）w R 5，则w可以是1-20的整数，R 5可以是羟基，卤素，C 1-8烷氧基或取代或未取代的碳环或杂环。或者，R 1和R 2可以共同形成具有4-8个碳原子的取代或未取代的饱和或不饱和杂环，N是所得杂环的杂原子。 R3可以是氢或C13。在化合物中，包含R 1或R 2，（CH 2）n和（CH 2）m的碳原子总和不超过40个。 R4是包含取代或未取代的氧化或还原环体系的环状环，所述环体系具有单环或二至三个稠环，包含3-7个环原子的环。所公开的化合物是抑制对细胞刺激的不良反应的有效试剂。

16. 发明授权

US5777117A Method for preparing substituted amino alcohol compounds 失效
标题翻译：取代氨基醇化合物的制备方法
公开(公告)号：US5777117A
公开(公告)日：1998-07-07
申请号：US472569
申请日：1995-06-07
申请人： J. Peter Klein , Gail E. Underiner , Anil M. Kumar
发明人： J. Peter Klein , Gail E. Underiner , Anil M. Kumar
IPC分类号： A61K31/45 , A61K31/47 , A61K31/513 , A61K31/519 , A61K31/522 , C07C215/08 , C07C215/56 , C07C217/62 , C07C217/64 , C07C229/22 , C07C233/36 , C07C233/78 , C07C233/91 , C07D207/40 , C07D207/404 , C07D209/48 , C07D211/76 , C07D211/88 , C07D217/24 , C07D239/54 , C07D239/90 , C07D239/96 , C07D295/13 , C07D473/10 , C07D211/94 , C07D239/80
CPC分类号： C07D207/404 , A61K31/45 , A61K31/47 , A61K31/513 , A61K31/519 , A61K31/522 , C07C215/08 , C07C215/56 , C07C217/62 , C07C217/64 , C07C229/22 , C07C233/36 , C07C233/78 , C07C233/91 , C07D209/48 , C07D211/76 , C07D211/88 , C07D217/24 , C07D239/54 , C07D239/90 , C07D239/96 , C07D295/13 , C07D473/10
摘要： Disclosed is a process for preparing compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.4 is a terminal moiety comprising a substituted or unsubstituted, oxidized or reduced ring system, the ring system having a single ring or two to three fused rings, a ring comprising from three to seven ring atoms. The disclosed compounds are effective agents to inhibit undesirable responses to cell stimuli.
摘要翻译：公开了一种制备具有式I的直链或支链脂族烃结构的化合物的方法：在式I中，n是1-4的整数，m是4至20的整数。独立地，R 1和R 2是氢，直链或支链烷基，链烯基或长链多至20个碳原子的炔基或 - （CH 2）w R 5。如果R 1或R 2是 - （CH 2）w R 5，则w可以是1-20的整数，R 5可以是羟基，卤素，C 1-8烷氧基或取代或未取代的碳环或杂环。或者，R 1和R 2可以共同形成具有4-8个碳原子的取代或未取代的饱和或不饱和杂环，N是所得杂环的杂原子。 R3可以是氢或C1-3。在化合物中，包含R 1或R 2，（CH 2）n和（CH 2）m的碳原子总和不超过40个。 R4是包含取代或未取代的氧化或还原环系的末端部分，该环系具有单环或二至三个稠环，包含3-7个环原子的环。所公开的化合物是抑制对细胞刺激的不良反应的有效试剂。

17. 发明授权

US5470878A Cell signaling inhibitors 失效
标题翻译：细胞信号传导抑制剂
公开(公告)号：US5470878A
公开(公告)日：1995-11-28
申请号：US164081
申请日：1993-12-08
申请人： John Michnick , Gail E. Underiner , J. Peter Klein , Glenn C. Rice
发明人： John Michnick , Gail E. Underiner , J. Peter Klein , Glenn C. Rice
IPC分类号： A61K31/404 , A61K31/45 , A61K31/47 , A61K31/513 , A61K31/519 , A61K31/522 , C07C215/08 , C07C215/56 , C07C217/62 , C07C229/22 , C07C233/36 , C07C233/78 , C07C233/91 , C07D207/40 , C07D207/404 , C07D209/48 , C07D211/76 , C07D211/88 , C07D217/24 , C07D239/54 , C07D239/90 , C07D239/96 , C07D295/13 , C07D473/10 , A61K31/20 , C07C233/00
CPC分类号： C07D207/404 , A61K31/404 , A61K31/45 , A61K31/47 , A61K31/513 , A61K31/519 , A61K31/522 , C07C215/08 , C07C215/56 , C07C217/62 , C07C229/22 , C07C233/36 , C07C233/78 , C07C233/91 , C07D209/48 , C07D211/76 , C07D211/88 , C07D217/24 , C07D239/54 , C07D239/90 , C07D239/96 , C07D295/13 , C07D473/10
摘要： Therapeutic compounds have the formula:(X)j-(non-cyclic core moiety),j being an integer from one to three, the core moiety is non-cyclic and X is a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkane or alkene of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy. Or jointly, R.sub.1 and R.sub.2 form a substituted or unsubstituted, saturated or unsaturated heterocyclic group having from four to eight carbon atoms, N being a hetero atom. R.sub.3 is a hydrogen or C.sub.1-3. Or, therapeutic compounds may also have the formula: ##STR2## R.sub.4 is a hydrogen, a straight or branched chain alkane or alkene of up to eight carbon atoms in length, --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy, or a substituted or unsubstituted, saturated or unsaturated heterocyclic group having from four to eight carbon atoms. r and s are independently integers from one to four, the sum (r+s) not being greater than five. t is an integer from one to fourteen and one or more carbon atoms of (CH.sub.2).sub.s or (CH.sub.2).sub.t may be substituted by a keto or hydroxy group.
摘要翻译：治疗化合物具有下式：（X）j-（非环核心部分），j为1至3的整数，核心部分为非环状，X为外消旋混合物，R或S对映异构体，溶剂合物，水合物或其盐：C是手性碳原子，n是1-4的整数（优选1至3），（CH 2）n的一个或多个碳原子可被酮或羟基取代组，m是从1到14的整数。独立地，R 1和R 2可以是氢，长或多至十二个碳原子的直链或支链烷烃或烯烃，或 - （CH 2）w R 5，w为2至14的整数，R 5为单 - ，二 - 或三取代或未取代的芳基，R 5上的取代基是羟基，氯，氟，溴或C 1-6烷氧基。或者共同地，R 1和R 2形成具有4至8个碳原子的取代或未取代的饱和或不饱和杂环基，N是杂原子。 R3是氢或C1-3。或者，治疗性化合物也可以具有下式：R 4是氢，长或多至八个碳原子的直链或支链烷烃或烯烃， - （CH 2）w R 5，w是2至14的整数， R5是一个，二或三取代或未取代的芳基，R 5上的取代基是羟基，氯，氟，溴或C 1-6烷氧基，或取代或未取代的饱和或不饱和杂环基，八个碳原子。 r和s独立为从1到4的整数，并且（r + s）不大于5。 t是1至14的整数，（CH 2）s或（CH 2）t的一个或多个碳原子可以被酮基或羟基取代。

18. 发明授权

US5801181A Amino alcohol substituted cyclic compounds 失效
标题翻译：氨基醇取代的环状化合物
公开(公告)号：US5801181A
公开(公告)日：1998-09-01
申请号：US474820
申请日：1995-06-07
申请人： John Michnick , Gail E. Underiner , J. Peter Klein , Glenn C. Rice
发明人： John Michnick , Gail E. Underiner , J. Peter Klein , Glenn C. Rice
IPC分类号： A61K31/404 , A61K31/45 , A61K31/47 , A61K31/513 , A61K31/519 , A61K31/522 , C07C215/08 , C07C215/56 , C07C217/62 , C07C229/22 , C07C233/36 , C07C233/78 , C07C233/91 , C07D207/40 , C07D207/404 , C07D209/48 , C07D211/76 , C07D211/88 , C07D217/24 , C07D239/54 , C07D239/90 , C07D239/96 , C07D295/13 , C07D473/10 , A01N43/00 , A01N43/42 , A01N43/58 , A01N43/90
CPC分类号： C07D207/404 , A61K31/404 , A61K31/45 , A61K31/47 , A61K31/513 , A61K31/519 , A61K31/522 , C07C215/08 , C07C215/56 , C07C217/62 , C07C229/22 , C07C233/36 , C07C233/78 , C07C233/91 , C07D209/48 , C07D211/76 , C07D211/88 , C07D217/24 , C07D239/54 , C07D239/90 , C07D239/96 , C07D295/13 , C07D473/10
摘要： Therapeutic compounds have the formula: (X)j--(core moiety), J being an integer from one to three, the core moiety having at least one, five- to seven-membered ring and X being a racemic mixture, R or S enantiomer, slovate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkane or alkene of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy. Or jointly, R.sub.1 and R.sub.2 form a substituted or unsubstituted, saturated or unsaturated heterocyclic group having from four to eight carbon atoms, N being a hetero atom. R.sub.3 is a hydrogen or C.sub.1-3. Or, therapeutic compounds may also have the formula: ##STR2## R.sub.4 is a hydrogen, a straight or branched chain alkane or alkene of up to eight carbon atoms in length, --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy, or a substituted or unsubstituted, saturated or unsaturated heterocyclic group having from four to eight carbon atoms, N being a hetero atom. r and s are independently integers from one to four, the sum (r+s) not being greater than five. t is an integer from one to fourteen and one or more carbon atoms of (CH.sub.2).sub.s or (CH.sub.2).sub.t may be substituted by a keto or hydroxy group.
摘要翻译：治疗性化合物具有下式：（X）j-（核心部分），J为1至3的整数，核心部分具有至少一个五至七元环，X为外消旋混合物，R或S 对映异构体，疏水盐，水合物或盐：C是手性碳原子，n是1至4（优选1至3）的整数，（CH 2）n的一个或多个碳原子可以被取代通过酮或羟基，m是1至14的整数。独立地，R 1和R 2可以是氢，长或多至十二个碳原子的直链或支链烷烃或烯烃，或 - （CH 2）w R 5，w为2至14的整数，R 5为单 - ，二 - 或三取代或未取代的芳基，R 5上的取代基是羟基，氯，氟，溴或C 1-6烷氧基。或者共同地，R 1和R 2形成具有4至8个碳原子的取代或未取代的饱和或不饱和杂环基，N是杂原子。 R3是氢或C1-3。或者，治疗性化合物也可以具有下式：R 4是氢，长或多至八个碳原子的直链或支链烷烃或烯烃， - （CH 2）w R 5，w是2至14的整数， R5是一个，二或三取代或未取代的芳基，R 5上的取代基是羟基，氯，氟，溴或C 1-6烷氧基，或取代或未取代的饱和或不饱和杂环基，八个碳原子，N是杂原子。 r和s独立为从1到4的整数，并且（r + s）不大于5。 t是1至14的整数，（CH 2）s或（CH 2）t的一个或多个碳原子可以被酮基或羟基取代。

19. 发明授权

US5780476A Hydroxyl-containing xanthine compounds 失效
标题翻译：含羟基黄嘌呤化合物
公开(公告)号：US5780476A
公开(公告)日：1998-07-14
申请号：US468660
申请日：1995-06-06
申请人： Gail E. Underiner , David Porubek , J. Peter Klein , Paul Woodson
发明人： Gail E. Underiner , David Porubek , J. Peter Klein , Paul Woodson
IPC分类号： A61K31/519 , A61K31/522 , A61K31/52 , C07D473/04
CPC分类号： A61K31/522 , A61K31/519
摘要： Disclosed are therapeutic compounds having the formula: (R)j - (core moiety), including resolved enantiomers, diastereomers, hydrates, salts, solvates and mixtures thereof. j is an integer from one to three, the core moiety is either non-cyclic or comprises at least one five- to seven-membered ring structure, R may be selected from the group consisting of hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted benzyl, C.sub.1-6 alkyl or C.sub.1-6 alkenyl, and at least one R has the formula I: ##STR1## n is an integer from seven to twenty and at least one of X or Y is --OH. The other of X or Y, which is not --OH, is hydrogen, CH.sub.3 --, CH.sub.3 --CH.sub.2 --, CH.sub.3 --(CH.sub.2).sub.2 -- or (CH.sub.3).sub.2 --CH.sub.2 --, and each W.sub.1, W.sub.2, and W.sub.3 is independently hydrogen, CH.sub.3 --, CH.sub.3 --CH.sub.2 --, CH.sub.3 --(CH.sub.2).sub.2 -- or (CH.sub.3).sub.2 --CH.sub.2 --. The X, Y, W.sub.1, W.sub.2, or W.sub.3 alkyl groups may be unsubstituted or substituted by an hydroxyl, halo or dimethylamino group. The disclosed compounds and therapeutic compositions thereof are useful in treating individuals having a disease or treatment-induced toxicity, mediated by second messenger activity.
摘要翻译：公开了具有下式的治疗化合物：（R）j-（核心部分），包括拆分的对映异构体，非对映体，水合物，盐，溶剂合物及其混合物。 j是1至3的整数，核心部分是非环状的或包含至少一个五至七元环结构，R可以选自氢，卤素，羟基，氨基，取代或未取代的苄基，C 1-6烷基或C 1-6烯基，并且至少一个R具有式I：I是7至20的整数，X或Y中的至少一个是-OH。不是-OH的X或Y中的另一个是氢，CH 3 - ，CH 3 -CH 2 - ，CH 3 - （CH 2）2 - 或（CH 3）2 -CH 2 - ，并且每个W 1，W 2和W 3独立地氢，CH 3 - ，CH 3 -CH 2 - ，CH 3 - （CH 2）2 - 或（CH 3）2 -CH 2 - 。 X，Y，W1，W2或W3烷基可以是未取代的或被羟基，卤素或二甲基氨基取代。所公开的化合物及其治疗组合物可用于治疗由第二信使活性介导的患有疾病或治疗诱导的毒性的个体。

20. 发明授权

US5804584A Therapeutic compounds containing a monocyclic five- to six- membered ring structure having one to two nitrogen atoms 失效
标题翻译：含有1至2个氮原子的单环五至六元环结构的治疗化合物
公开(公告)号：US5804584A
公开(公告)日：1998-09-08
申请号：US468659
申请日：1995-06-06
申请人： Gail E. Underiner , David Porubek , J. Peter Klein , Paul Woodson
发明人： Gail E. Underiner , David Porubek , J. Peter Klein , Paul Woodson
IPC分类号： A61K31/519 , A61K31/522 , C07D239/54 , A61K31/52
CPC分类号： A61K31/522 , A61K31/519
摘要： Disclosed are therapeutic compounds having the formula: (R)j-(core moiety), including resolved enantiomers, diastereomers, hydrates, salts, solvates and mixtures thereof. j is an integer from one to three, the core moiety is either non-cyclic or comprises at least one five- to seven-membered ring structure, R may be selected from the group consisting of hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted benzyl, C.sub.1-6 alkyl or C.sub.1-6 alkenyl, and at least one R has the formula I: ##STR1## n is an integer from seven to twenty and at least one of X or Y is --OH. The other of X or Y, which is not --OH, is hydrogen, CH.sub.3 --, CH.sub.3 --CH.sub.2 --, CH.sub.3 --(CH.sub.2).sub.2 -- or (CH.sub.3).sub.2 --CH.sub.2 --, and each W.sub.1, W.sub.2, and W.sub.3 is independently hydrogen, CH.sub.3 --, CH.sub.3 --CH.sub.2 --, CH.sub.3 --(CH.sub.2).sub.2 -- or (CH.sub.3).sub.2 --CH.sub.2 --. The X, Y, W.sub.1, W.sub.2, or W.sub.3 alkyl groups may be unsubstituted or substituted by an hydroxyl, halo or dimethylamino group. The disclosed compounds and therapeutic compositions thereof are useful in treating individuals having a disease or treatment-induced toxicity, mediated by second messenger activity.
摘要翻译：公开了具有下式的治疗化合物：（R）j-（核心部分），包括拆分的对映异构体，非对映体，水合物，盐，溶剂合物及其混合物。 j是1至3的整数，核心部分是非环状的或包含至少一个五至七元环结构，R可以选自氢，卤素，羟基，氨基，取代或未取代的苄基，C 1-6烷基或C 1-6烯基，并且至少一个R具有式I：I是7至20的整数，X或Y中的至少一个是-OH。不是-OH的X或Y中的另一个是氢，CH 3 - ，CH 3 -CH 2 - ，CH 3 - （CH 2）2 - 或（CH 3）2 -CH 2 - ，并且每个W 1，W 2和W 3独立地氢，CH 3 - ，CH 3 -CH 2 - ，CH 3 - （CH 2）2 - 或（CH 3）2 -CH 2 - 。 X，Y，W1，W2或W3烷基可以是未取代的或被羟基，卤素或二甲基氨基取代。所公开的化合物及其治疗组合物可用于治疗由第二信使活性介导的患有疾病或治疗诱导的毒性的个体。

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