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1. 发明授权

US06780865B1 Compounds having selective hydrolytic potentials 失效
标题翻译：具有选择性水解电位的化合物
公开(公告)号：US06780865B1
公开(公告)日：2004-08-24
申请号：US08932834
申请日：1997-09-18
申请人： David Porubek , Anil M. Kumar , Charles R. Bredl , J. Peter Klein
发明人： David Porubek , Anil M. Kumar , Charles R. Bredl , J. Peter Klein
IPC分类号： C07D47310
CPC分类号： C07D473/04 , C07D473/10
摘要： Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems. The disclosed compounds have a structure of formula I:
摘要翻译：公开了具有选择性水解电位的化合物。所公开的化合物可用作具有选择性稳定性且能够在生物系统中进行程序水解的化合物。所公开的化合物具有式I的结构：

2. 发明授权

US5965564A Enantiomerically pure hydroxylated xanthine compounds 失效
标题翻译：对映体纯的羟基化黄嘌呤化合物
公开(公告)号：US5965564A
公开(公告)日：1999-10-12
申请号：US44976
申请日：1998-03-20
申请人： James A. Bianco , Paul Woodson , David Porubek , Jack Singer
发明人： James A. Bianco , Paul Woodson , David Porubek , Jack Singer
IPC分类号： C07D473/06 , A61K20060101 , A61K31/44 , A61K31/519 , A61K31/52 , A61K31/522 , A61P1/00 , A61P1/02 , A61P1/04 , A61P1/16 , A61P3/10 , A61P5/14 , A61P7/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P15/06 , A61P17/06 , A61P17/14 , A61P19/02 , A61P19/10 , A61P25/20 , A61P29/00 , A61P31/04 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/06 , A61P39/02 , A61P43/00 , C07D473/04 , C07D473/10
CPC分类号： A61K31/522 , A61K31/519 , A61K31/52 , C07D473/10 , Y02P20/582 , Y10S514/814 , Y10S514/866 , Y10S514/921
摘要： There is disclosed compounds and pharmaceutical compositions that are a resolved R or S (preferably R) enantiomer of an .omega.-1 alcohol of a straight chain alkyl (C.sub.5-8) substituted at the 1-position of 3,7-disubstituted xanthine. The inventive compounds are effective in modulating cellular response to external or in situ primary stimuli, as well as to specific modes of administration of such compounds in effective amounts.
摘要翻译：公开了化合物和药物组合物，其是在3,7-二取代的黄嘌呤的1-位取代的直链烷基（C5-8）的ω-1醇的分解的R或S（优选R）对映异构体。本发明化合物有效地调节对外部或原位初级刺激的细胞反应，以及有效量的这些化合物的特定给药模式。

3. 发明授权

US5521315A Olefin substituted long chain compounds 失效
标题翻译：烯烃取代的长链化合物
公开(公告)号：US5521315A
公开(公告)日：1996-05-28
申请号：US59697
申请日：1993-05-10
申请人： Gail Underiner , David Porubek , J. Peter Klein , Elisa Eiseman , Alistair Leigh , Anil Kumar , John Michnick
发明人： Gail Underiner , David Porubek , J. Peter Klein , Elisa Eiseman , Alistair Leigh , Anil Kumar , John Michnick
IPC分类号： C07D239/54 , A61K31/015 , A61K31/047 , A61K31/195 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/505 , A61K31/52 , A61K31/522 , A61P1/00 , A61P1/02 , A61P1/16 , A61P3/00 , A61P3/08 , A61P3/10 , A61P11/00 , A61P13/02 , A61P15/00 , A61P19/10 , A61P25/28 , A61P29/00 , A61P37/00 , A61P43/00 , C07C13/08 , C07C13/16 , C07C15/40 , C07C49/20 , C07C49/647 , C07D209/48 , C07D473/06 , C07D211/88 , C07D239/80
CPC分类号： C07D473/06
摘要： There is disclosed an olefin-substituted compound having the formula:R--(core moiety),wherein R is a straignt chain hydrocarbon having at least one double bond and a carbon chain length of from about 6 to about 18 carbon atoms, wherein multiple double bonds are separated from each other by at least three carbon atoms, wherein the closest double bond to the core moiety is at least five carbon atoms from the core moiety, and wherein the hydrocarbon chain may be substituted by a hydroxyl, halo, keto or dimethylanimo group and/or interrupted by an oxygen atom and salts thereof and pharmaceutical compositions thereof.
摘要翻译：公开了具有下式的烯烃取代的化合物：R-（核心部分），其中R是具有至少一个双键且碳链长度为约6至约18个碳原子的直链烃，其中多个双键彼此分开至少三个碳原子，其中与核心部分最接近的双键是至少五个来自核心部分的碳原子，并且其中烃链可以被羟基，卤素，酮基或二甲基亚胺基取代组和/或被氧原子及其盐和其药物组合物中断。

4. 发明授权

US07053096B2 Compounds having selective hydrolytic potentials 失效
公开(公告)号：US07053096B2
公开(公告)日：2006-05-30
申请号：US10838296
申请日：2004-05-05
申请人： David Porubek , Anil M. Kumar , Charles R. Bredl , J. Peter Klein
发明人： David Porubek , Anil M. Kumar , Charles R. Bredl , J. Peter Klein
IPC分类号： C07D473/10 , A61K31/522
CPC分类号： C07D473/04 , C07D473/10
摘要： Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems.

5. 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。

6. 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。

7. 发明授权

US5648357A Enatiomerically pure hydroxylated xanthine compounds 失效
标题翻译：富含羟基化的黄嘌呤化合物
公开(公告)号：US5648357A
公开(公告)日：1997-07-15
申请号：US307554
申请日：1994-09-16
申请人： James A. Bianco , Paul Woodson , David Porubek , Jack Singer
发明人： James A. Bianco , Paul Woodson , David Porubek , Jack Singer
IPC分类号： A61K31/52 , A61K31/522 , C07D473/10
CPC分类号： C07D473/10 , A61K31/52 , A61K31/522 , Y02P20/582
摘要： There is disclosed compounds and pharmaceutical compositions that are a resolved R or S (preferably R) enantiomer of an .omega.-1 alcohol of a straight chain alkyl (C.sub.5-8) substituted at the 1-position of 3,7-disubstituted xanthine. The inventive compounds are effective in modulating cellular response to external or in situ primary stimuli, as well as to specific modes of administration of such compounds in effective amounts.
摘要翻译：公开了化合物和药物组合物，其是在3,7-二取代的黄嘌呤的1-位取代的直链烷基（C5-8）的ω-1醇的分解的R或S（优选R）对映异构体。本发明化合物有效地调节对外部或原位初级刺激的细胞反应，以及有效量的这些化合物的特定给药模式。

8. 发明授权

US5580873A Enatiomerically pure hydroxylated xanthine compounds to treat proliferative vascular diseases 失效
标题翻译：用于治疗增殖性血管疾病的单体纯羟基化黄嘌呤化合物
公开(公告)号：US5580873A
公开(公告)日：1996-12-03
申请号：US456899
申请日：1995-06-01
申请人： James A. Bianco , Paul Woodson , David Porubek , Jack Singer
发明人： James A. Bianco , Paul Woodson , David Porubek , Jack Singer
IPC分类号： A61K31/52 , A61K31/522 , C07D473/10
CPC分类号： A61K31/52 , A61K31/522 , C07D473/10 , Y02P20/582
摘要： There is disclosed compounds and pharmaceutical compositions that are a resolved R or S (preferably R) enantiomer of an .omega.-1 alcohol of a straight chain alkyl (C.sub.5-8) substituted at the 1-position of 3,7-disubstituted xanthine. The inventive compounds are effective in treating proliferative vascular disease.
摘要翻译：公开了化合物和药物组合物，其是在3,7-二取代的黄嘌呤的1-位取代的直链烷基（C5-8）的ω-1醇的分解的R或S（优选R）对映异构体。本发明化合物可有效治疗增殖性血管疾病。

9. 发明授权

US5792772A Enatiomerically pure hydroxylated xanthine compounds 失效
标题翻译：富含羟基化的黄嘌呤化合物
公开(公告)号：US5792772A
公开(公告)日：1998-08-11
申请号：US458957
申请日：1995-06-01
申请人： James A. Bianco , Paul Woodson , David Porubek , Jack Singer
发明人： James A. Bianco , Paul Woodson , David Porubek , Jack Singer
IPC分类号： C07D473/06 , A61K20060101 , A61K31/44 , A61K31/519 , A61K31/52 , A61K31/522 , A61P1/00 , A61P1/02 , A61P1/04 , A61P1/16 , A61P3/10 , A61P5/14 , A61P7/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P15/06 , A61P17/06 , A61P17/14 , A61P19/02 , A61P19/10 , A61P25/20 , A61P29/00 , A61P31/04 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/06 , A61P39/02 , A61P43/00 , C07D473/04 , C07D473/10
CPC分类号： A61K31/522 , A61K31/519 , A61K31/52 , C07D473/10 , Y02P20/582 , Y10S514/814 , Y10S514/866 , Y10S514/921
摘要： There is disclosed compounds and pharmaceutical compositions that are a resolved R or S (preferably R) enantiomer of an .omega.-1 alcohol of a straight chain alkyl (C.sub.5-8) substituted at the 1-position of 3,7-disubstituted xanthine. The inventive compounds are effective in modulating cellular response to external or in situ primary stimuli, as well as to specific modes of administration of such compounds in effective amounts.
摘要翻译：公开了化合物和药物组合物，其是在3,7-二取代的黄嘌呤的1-位取代的直链烷基（C5-8）的ω-1醇的分解的R或S（优选R）对映异构体。本发明化合物有效地调节对外部或原位初级刺激的细胞反应，以及有效量的这些化合物的特定给药模式。

10. 发明授权

US5629315A Treatment of diseases using enantiomerically pure hydroxylated xanthine compounds 失效
标题翻译：使用对映体纯的羟基化黄嘌呤化合物治疗疾病
公开(公告)号：US5629315A
公开(公告)日：1997-05-13
申请号：US456900
申请日：1995-06-01
申请人： James A. Bianco , Paul Woodson , David Porubek , Jack Singer
发明人： James A. Bianco , Paul Woodson , David Porubek , Jack Singer
IPC分类号： C07D473/06 , A61K20060101 , A61K31/44 , A61K31/519 , A61K31/52 , A61K31/522 , A61P1/00 , A61P1/02 , A61P1/04 , A61P1/16 , A61P3/10 , A61P5/14 , A61P7/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P15/06 , A61P17/06 , A61P17/14 , A61P19/02 , A61P19/10 , A61P25/20 , A61P29/00 , A61P31/04 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/06 , A61P39/02 , A61P43/00 , C07D473/04 , C07D473/10
CPC分类号： A61K31/522 , A61K31/519 , A61K31/52 , C07D473/10 , Y02P20/582 , Y10S514/814 , Y10S514/866 , Y10S514/921
摘要： There is disclosed compounds and pharmaceutical compositions that are a resolved R or S (preferably R) enantiomer of an .omega.-1 alcohol of a straight chain alkyl (C.sub.5-8) substituted at the 1-position of 3,7-disubstituted xanthine. The inventive compounds are effective in modulating cellular response to external or in situ primary stimuli, as well as to specific modes of administration of such compounds in effective amounts.
摘要翻译：公开了化合物和药物组合物，其是在3,7-二取代的黄嘌呤的1-位取代的直链烷基（C5-8）的ω-1醇的分解的R或S（优选R）对映异构体。本发明化合物有效地调节对外部或原位初级刺激的细胞反应，以及有效量的这些化合物的特定给药模式。

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