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1. 发明授权

US6100271A Therapeutic compounds containing xanthinyl 失效
标题翻译：含有黄原素的治疗化合物
公开(公告)号：US6100271A
公开(公告)日：2000-08-08
申请号：US483871
申请日：1995-06-07
申请人： J. Peter Klein , Alistair J. Leigh , Gail E. Underiner , Anil M. Kumar
发明人： J. Peter Klein , Alistair J. Leigh , Gail E. Underiner , Anil M. Kumar
IPC分类号： C07D239/54 , A61K31/42 , A61K31/421 , A61K31/496 , A61K31/505 , A61K31/52 , A61K31/522 , A61P9/10 , A61P9/14 , A61P11/16 , A61P13/02 , A61P15/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/04 , A61P37/08 , A61P43/00 , C07C47/198 , C07C47/277 , C07C49/175 , C07C49/255 , C07C57/46 , C07C59/64 , C07C65/21 , C07C69/06 , C07C69/14 , C07C69/24 , C07C69/608 , C07C69/612 , C07C225/06 , C07C233/01 , C07D239/56 , C07D241/18 , C07D263/30 , C07D473/04 , C07D473/06 , C07D473/10 , C07D487/04 , C07D513/04 , C07D521/00
CPC分类号： C07D487/04 , C07D473/04 , C07D473/06 , C07D473/10 , C07D513/04
摘要： Therapeutic compounds with at least one carboxylic acid, ester or amide-substituted side chain have the formula:CORE MOIETY --(R).sub.jwherein j is an integer from one to three. The core moiety is non-cyclic or cyclic (carbocyclic or heterocyclic). R may be selected from among hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, carbocyclic or heterocyclic groups and at least one R has the formula I: ##STR1## wherein: one or two p are the integer one, otherwise p is two; and n is an integer from three to twenty; R.sub.1 is selected from the group consisting of substituted and unsubstituted CH.sub.2 ; NR.sub.3, R.sub.3 being hydrogen, substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or C.sub.(1-20) hydroxyalkyl, or carbocyclic or heterocyclic group; O; --CHR.sub.4 O--, R.sub.4 being substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl, C.sub.(1-20) hydroxyalkyl, or R.sub.2 and R.sub.4 join to form a substituted or unsubstituted heterocycle having four to seven ring atoms, the ether group --O-- of --CHR.sub.4 O-- being a member of the heterocycle. R.sub.2 is selected from the group consisting of hydrogen; halogen; substituted or unsubstituted C.sub.(1-10) alkyl; C.sub.(1-10) alkoxyl; C.sub.(2-10) alkenyl; C.sub.(1-10) hydroxyallyl; --A(R.sub.5).sub.m, A being N or O, m being one or two and R.sub.5 being hydrogen, a substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(1-10) alkoxyl, C.sub.(2-10) alkenyl or C.sub.(1-10) hydroxyalkyl), or carbocyclic or heterocyclic group. At least one of R.sub.1 is NR.sub.3, O or --CHR.sub.4 O--, or R.sub.2 is --A(R.sub.5).sub.m. The compounds and pharmaceutical compositions thereof are useful as therapies for diseases advanced via intracellular signaling through specific intracellular signaling pathways by mediating a signaling response to an external stimuli.
摘要翻译：具有至少一个羧酸，酯或酰胺取代的侧链的治疗化合物具有下式：CORE MOIETY - （R）j，其中j是1至3的整数。核心部分是非环状或环状的（碳环或杂环）。 R可以选自氢，卤素，羟基，氨基，取代或未取代的C（1-10）烷基，C（2-10）烯基，碳环或杂环基，并且至少一个R具有式I：其中：或两个p为整数，否则p为2; n为3〜20的整数。 R1选自取代和未取代的CH 2; NR 1，R 3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C（1-20）羟基烷基或碳环或杂环基; O; -CHR4O-，R4是取代或未取代的C（1-20）烷基，C（1-20）烷氧基，C（2-20）烯基，C（1-20）羟基烷基或R2和R4连接形成取代的或具有4-7个环原子的未取代的杂环，-CHR4O-的醚基-O-是杂环的成员。 R2选自氢; 卤素; 取代或未取代的C（1-10）烷基; C（1-10）烷氧基; C（2-10）烯基; C（1-10）羟基烯基; -A（R5）m，A是N或O，m是一个或两个，R5是氢，取代或未取代的C（1-10）烷基，C（1-10）烷氧基，C（2-10）烯基或C（1-10）羟烷基）或碳环或杂环基。 R 1中的至少一个为NR 3，O或-CHR 4 O-，或R 2为-A（R 5）m。这些化合物及其药物组合物可用作通过介导对外部刺激的信号反应的特异性细胞内信号通路的细胞内信号传导的疾病的治疗。

2. 发明授权

US5985926A Method for inhibiting intracellular viral replication 失效
标题翻译：抑制细胞内病毒复制的方法
公开(公告)号：US5985926A
公开(公告)日：1999-11-16
申请号：US797326
申请日：1997-02-10
申请人： David W. Leung , Gail E. Underiner , Jack W. Singer
发明人： David W. Leung , Gail E. Underiner , Jack W. Singer
IPC分类号： A61K31/4035 , A61K31/445 , A61K31/472 , A61K31/513 , A61K31/522 , C12N15/48 , A61K31/20
CPC分类号： A61K31/522 , A61K31/4035 , A61K31/445 , A61K31/472 , A61K31/513
摘要： There is disclosed a method of preventing or delaying the occurrence of acquired immunodeficiency syndrome (AIDS) in human immunodeficiency virus (HIV) seropositive humans by administering an effective amount of a compound that inhibits cellular signaling through a specific phospholipid-based cellular signaling and signal amplification pathway. The invention further provides a method for preventing or delaying clinical symptoms of a group of viral diseases wherein the viral disease is mediated by host cell viral replication. The invention provides an advantage by attacking host cellular signaling mechanisms to prevent the development of drug resistance from rapidly mutating viruses.
摘要翻译：公开了通过施用有效量的抑制细胞信号传导的化合物通过特定的基于磷脂的细胞信号传导和信号扩增来预防或延迟人类免疫缺陷病毒（HIV）血清阳性人类中的获得性免疫缺陷综合征（AIDS）的发生的方法途径。本发明还提供了一种用于预防或延缓一组病毒性疾病的临床症状的方法，其中所述病毒性疾病由宿主细胞病毒复制介导。本发明通过攻击宿主细胞信号传导机制来提供一个优点，以防止快速突变病毒对耐药性的发展。

3. 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。

4. 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。

5. 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。

6. 发明授权

US6103730A Amine substituted compounds 失效
标题翻译：胺取代的化合物
公开(公告)号：US6103730A
公开(公告)日：2000-08-15
申请号：US486264
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 , A61K31/522 , C07D473/10
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.jIn 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。至少一个具有式 I：式I中，n为4〜20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。

7. 发明授权

US06693105B1 Hydroxyl-containing compounds 失效
标题翻译：含羟基的化合物
公开(公告)号：US06693105B1
公开(公告)日：2004-02-17
申请号：US09361145
申请日：1999-07-27
申请人： Gail E. Underiner , David Porubek , J. Peter Klein , Paul Woodson , Stephen J. Klaus , Anil M. Kumar , John Tulinsky
发明人： Gail E. Underiner , David Porubek , J. Peter Klein , Paul Woodson , Stephen J. Klaus , Anil M. Kumar , John Tulinsky
IPC分类号： A61K31522
CPC分类号： C07D209/48 , A61K31/00 , A61K31/519 , A61K31/522 , C07C233/91 , C07C317/18 , C07D211/76 , C07D211/88 , C07D215/22 , C07D239/54 , C07D239/88 , C07D239/96 , C07D295/088 , C07D473/04 , C07D473/06 , C07D473/08 , C07D473/10 , C07D475/02 , C07D487/04 , C07D495/04 , C07D513/04 , Y10T436/147777
摘要： Disclosed are therapeutic compounds having the formula: (R)j—(CORE MOIETY), including resolved enantiomers, diastereomers, hydrates, salts, solvates or mixtures thereof where j is an integer from one to three. The core moiety is a bicyclic ring structure having at least one heterocyclic ring that contains five to six ring atoms and up to two nitrogen heteroatoms. R is selected from the group consisting of hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted benzyl, C1-6 alkyl or C1-6 alkenyl, and at least one R has the formula I: n is an integer from 1 to 20, at least one of X or Y is —OH. Another of X or Y, which is not —OH, is hydrogen, CH3—, CH3—CH2—, CH3—(CH2)2—or (CH3)2—CH2—, and each W1, W2, and W3 is independently hydrogen, CH3—, CH3—CH2—, CH3—(CH2)2— or (CH3)2—CH2—. The X, Y, W1, W2, or W3 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：包括拆分的对映异构体，非对映异构体，水合物，盐，溶剂合物或其混合物，其中j是1至3的整数。核心部分是具有至少一个含有5至6个环原子和至多2个氮杂原子的杂环的双环结构。 R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，至少一个R具有式I：n为1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独立地是氢，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。

8. 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。

9. 发明授权

US5756511A Method for treating symptoms of a neurodegenerative condition 失效
标题翻译：治疗神经退行性疾病症状的方法
公开(公告)号：US5756511A
公开(公告)日：1998-05-26
申请号：US416270
申请日：1995-04-03
申请人： James W. West , David W. Leung , J. Peter Klein , Gail E. Underiner , Anil M. Kumar
发明人： James W. West , David W. Leung , J. Peter Klein , Gail E. Underiner , Anil M. Kumar
IPC分类号： A61K31/522 , A01N43/90
CPC分类号： A61K31/522
摘要： A method for treating symptoms of Alzheimer's Disease by administering an effective amount of a compound, racemate, isolated R or S enantionmer, solvate, hydrate or salt having the formula: X--terminal heterocyclic moiety. In the above formula, the terminal heterocyclic moiety is a 3,7-dimethylxanthinyl, 3-methylxanthinyyl or xanthinyl moiety and X is: ##STR1## n is zero or an integer from one to four; and m is an integer from seven to fourteen. For compounds useful in the inventive method, 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. w may be an integer from one to twenty and R.sub.5 is preferably an hydroxyl, halo C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. R.sub.3 in compounds useful in the inventive method may be either an hydroxyl group, an oxygen atom, the single bond represented being instead a double bond, or --O--R.sub.4, R.sub.4 being a C.sub.1-6 oxoalkyl.
摘要翻译：通过施用有效量的具有下式的化合物，外消旋物，分离的R或S对映体，溶剂合物，水合物或盐，来治疗阿尔茨海默病症状的方法：在上式中，末端杂环部分为 3,7-二甲基黄烷基，3-甲基黄嘌呤基或xanthinyl部分，X为：n为0或1至4的整数; m为7〜14的整数。对于可用于本发明方法的化合物，R 1和R 2是氢，直链或支链烷基，链烯基或炔基，其长度为至多20个碳原子或 - （CH 2）w R 5。 w可以是从一到二十的整数，R 5优选为羟基，卤代C 1-8烷氧基或取代或未取代的碳环或杂环。可用于本发明方法的化合物中的R 3可以是羟基，氧原子，所表示的单键代替双键，或-O-R4，R4是C1-6氧代烷基。

10. 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。

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