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1. 发明授权

US5866576A Epoxide-containing compounds 失效
标题翻译：含环氧化物的化合物
公开(公告)号：US5866576A
公开(公告)日：1999-02-02
申请号：US778563
申请日：1997-01-03
申请人： Gail Underiner , J. Peter Klein , John Michnick , Alistair Leigh , Anil Kumar
发明人： Gail Underiner , J. Peter Klein , John Michnick , Alistair Leigh , Anil Kumar
IPC分类号： C07D303/36 , C07D405/06 , C07D473/10 , A61K31/505 , C07D239/02
CPC分类号： C07D405/06 , C07D303/36 , C07D473/10
摘要： Disclosed are enantiomers, diastereomers, salts, solvates, hydrates and mixtures thereof, of formula I: ##STR1## The core moiety is a monocyclic ring structure having five to six ring atoms and two nitrogen atoms at the 1 and 3 positions, n is an integer from 4 to 16, R.sub.1 and R.sub.2 are hydrogen, halogen or C.sub.1-12 alkyl or alkenyl, and (CH.sub.2).sub.n may be optionally substituted by a hydroxyl, halogen, oxygen, a C.sub.1-4 alkyl group or a dimethylamino group. The compounds and pharmaceutical composition thereof are useful in methods for treating an individual having a disease or treatment-induced toxicity mediated through a second messenger.
摘要翻译：公开了式I的对映异构体，非对映异构体，盐，溶剂化物，水合物及其混合物：核心部分是在1和3位具有5至6个环原子和2个氮原子的单环环结构，n为 4至16的整数，R 1和R 2是氢，卤素或C 1-12烷基或链烯基，和（CH 2）n可任选被羟基，卤素，氧，C 1-4烷基或二甲基氨基取代。化合物及其药物组合物可用于治疗患有通过第二信使介导的疾病或治疗诱导的毒性的个体的方法。

2. 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。

3. 发明授权

US6121270A Epoxide-containing compounds 失效
标题翻译：含环氧化物的化合物
公开(公告)号：US6121270A
公开(公告)日：2000-09-19
申请号：US98473
申请日：1998-06-17
申请人： Gail Underiner , J. Peter Klein , John Michnick , Alistair Leigh , Anil Kumar
发明人： Gail Underiner , J. Peter Klein , John Michnick , Alistair Leigh , Anil Kumar
IPC分类号： C07D303/36 , C07D405/06 , C07D473/10 , A61K31/52 , C07D473/04
CPC分类号： C07D405/06 , C07D303/36 , C07D473/10
摘要： Disclosed are enantiomers diastereomers, salts, solvates, hydrates and mixtures thereof, of formula I: ##STR1## The core moiety is non-cyclic or at least one five- to seven-membered ring, n is an integer from about 4 to about 16, R.sub.1 and R.sub.2 are hydrogen, halogen or C.sub.1-12 alkyl or alkenyl, and (CH.sub.2).sub.n may be substituted by a hydroxyl, halogen, oxygen, a (C.sub.1-4) alkyl group or a dimethylamino group. The compounds and pharmaceutical composition thereof are useful in methods for treating an individual having a disease or treatment-induced toxicity, mediated by second messenger activity.
摘要翻译：公开了式I的对映体非对映异构体，盐，溶剂合物，水合物及其混合物：核心部分是非环状或至少一个五至七元环，n是约4至约16的整数，R 1和 R2是氢，卤素或C1-12烷基或烯基，（CH2）n可以被羟基，卤素，氧，（C1-4）烷基或二甲氨基取代。所述化合物及其药物组合物可用于治疗由第二信使活性介导的具有疾病或治疗诱导的毒性的个体的方法。

4. 发明授权

US5340813A Substituted aminoalkyl xanthine compounds 失效
标题翻译：取代的氨基烷基黄嘌呤化合物
公开(公告)号：US5340813A
公开(公告)日：1994-08-23
申请号：US973804
申请日：1992-11-09
申请人： J. Peter Klein , Gail Underiner , Alistair Leigh
发明人： J. Peter Klein , Gail Underiner , Alistair Leigh
IPC分类号： C07D251/00 , A61K31/44 , A61K31/4402 , A61K31/505 , A61K31/517 , A61K31/52 , A61K31/522 , A61P1/00 , A61P1/16 , A61P3/00 , A61P7/00 , A61P9/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P31/00 , A61P37/00 , A61P43/00 , C07D213/64 , C07D239/54 , C07D239/62 , C07D239/72 , C07D471/02 , C07D473/04 , C07D473/06 , C07D473/08 , C07D473/10 , C07D473/30
CPC分类号： A61K31/522 , A61K31/52 , C07D473/04
摘要： Compounds of the formula ##STR1## wherein each of one or two R is independently ##STR2## wherein n is an integer from 4 to 18, each R.sub.1 ' and R.sub.2 ' is independently H, alkyl (1-4C) or alkenyl (1-4C); and R.sub.3 ' and R.sub.4 ' are independently H or CH.sub.3 ; and wherein the alkyl or alkenyl may be substituted by a hydroxyl, halo or dimethylamino group and/or interrupted by an oxygen atom, H or alkyl (1-4C), including resolved enantiomers and/or diastereomers and mixtures thereof. Preferably, n is from 6 to 10, R.sub.1 ' and R.sub.2 ' are independently H or methyl and R.sub.3 ' and R.sub.4 ' are H. In particular, the compounds lower elevated levels of unsaturated, non-arachidonate phosphatidic acid (PA) and diacylglycerol (DAG) derived from said PA within seconds of the primary stimulus and their contact with said cells. The modulatory effect depends on the nature of the target cell and the stimulus applied.
摘要翻译：式1的化合物，其中一个或两个R各自独立地为其中n为4至18的整数，每个R 1'和R 2'独立地为H，烷基（1-4C）或链烯基（ 1-4C）; 且R 3'和R 4'独立地为H或CH 3; 并且其中所述烷基或链烯基可以被羟基，卤素或二甲基氨基取代和/或被氧原子H或烷基（1-4C）中断，包括拆分的对映异构体和/或非对映异构体及其混合物。优选地，n为6至10，R 1'和R 2'独立地为H或甲基，且R 3'和R 4'为H.特别地，该化合物降低不饱和，非花生四烯酸酯磷脂酸（PA）和二酰基甘油 DAG），其在主刺激的几秒钟内从所述PA衍生并与所述细胞接触。调节作用取决于靶细胞的性质和应用的刺激。

5. 发明授权

US6020337A Electronegative-substituted long chain xanthine compounds 失效
标题翻译：电负性取代长链黄嘌呤化合物
公开(公告)号：US6020337A
公开(公告)日：2000-02-01
申请号：US950810
申请日：1997-09-16
申请人： Alistair J. Leigh , John Michnick , Anil M. Kumar , J. Peter Klein , Gail Underiner
发明人： Alistair J. Leigh , John Michnick , Anil M. Kumar , J. Peter Klein , Gail Underiner
IPC分类号： C07D209/48 , C07D239/54 , C07D239/96 , C07D473/10 , A61K31/52 , C07D473/00
CPC分类号： C07D209/48 , C07D239/54 , C07D239/96 , C07D473/10
摘要： Therapeutic compounds, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, having a formula: ##STR1## wherein R.sub.0 is selected from the group consisting of hydrogen, halo, hydroxyl, amino, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, cyclic or heterocyclic groups, wherein the substituents of substituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl are other than halo; n is an integer from one to sixteen; R.sub.1, R.sub.2, and R.sub.3 are independently selected from the group consisting of a halo; haloacetoxy; hydrogen; hydroxy; oxo; --N.dbd.C.dbd.S; --N.dbd.C.dbd.O; --0--C.tbd.N; --C.tbd.N; --N.dbd.N.dbd.N; and --C--(R.sub.5).sub.3, R.sub.5 being independently a halo or hydrogen, at least one R.sub.5 being halo, at least one of R.sub.1, R.sub.2, and R.sub.3 being halo, cyano, isocyano, isothiocyano, azide or haloacetoxy group; R.sub.4 is hydrogen, C.sub.(1-6) alkyl, C.sub.(1-6) alkenyl, cyclo C.sub.(4-6) alkyl, or phenyl; one or more hydrogen atoms of (CH.sub.2).sub.n --CH.sub.a --CH.sub.b --CH.sub.c may be replaced with: i) at least one of halogen atom, hydroxyl, oxo, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(1-10) alkoxyalkyl, or C.sub.(2-10) alkenyl; or ii) one or more unsaturated bonds; and any two adjacent carbon atoms of (CH.sub.2).sub.n --CH.sub.a --CH.sub.b --CH.sub.c may be instead separated by at least one oxygen atom. These compounds are useful in treating or preventing diseases by inhibiting selective second messenger pathways.
摘要翻译：具有下式的治疗化合物，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，其中R 0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，环状或杂环基团，其中取代的C（1-10）烷基，C（2-10）烯基的取代基不是卤素; n是从1到16的整数; R 1，R 2和R 3独立地选自卤素; 卤代乙酰氧基; 氢; 羟基; 氧代 -N = C = S; -N = C = O; -0-C 3BOND N; -C 3BOND N; -N = N = N; 和 - （R 5）3，R 5独立地为卤素或氢，至少一个R 5为卤素，R 1，R 2和R 3中的至少一个为卤素，氰基，异氰基，异硫氰基，叠氮基或卤代乙酰氧基; R4是氢，C（1-6）烷基，C（1-6）烯基，环C（4-6）烷基或苯基; （CH 2）n -CH-CHB-CHc的一个或多个氢原子可以被：i）卤素原子，羟基，氧代，取代或未取代的C（1-10）烷基，C（1-10 ）烷氧基烷基或C（2-10）烯基; 或ii）一个或多个不饱和键; 并且（CH 2）n -CH CH-CH c CH 2的任何两个相邻的碳原子可以被至少一个氧原子隔开。这些化合物可用于通过抑制选择性第二信使途径来治疗或预防疾病。

6. 发明授权

US5473070A Substituted long chain alcohol xanthine compounds 失效
标题翻译：取代长链醇黄嘌呤化合物
公开(公告)号：US5473070A
公开(公告)日：1995-12-05
申请号：US976353
申请日：1992-11-16
申请人： Gail Underiner , David Porubek , J. Peter Klein , Paul Woodson
发明人： Gail Underiner , David Porubek , J. Peter Klein , Paul Woodson
IPC分类号： A61K31/519 , C07C233/91 , C07C317/18 , C07D209/48 , C07D211/76 , C07D211/88 , C07D215/22 , C07D239/54 , C07D239/88 , C07D239/96 , C07D295/088 , C07D473/06 , C07D473/08 , C07D473/10 , C07D475/02 , C07D473/04 , A61K31/52
CPC分类号： C07D209/48 , A61K31/519 , C07C233/91 , C07C317/18 , C07D211/76 , C07D211/88 , C07D215/22 , C07D239/54 , C07D239/88 , C07D239/96 , C07D295/088 , C07D473/06 , C07D473/08 , C07D473/10 , C07D475/02
摘要： There is disclosed compounds and pharmaceutical compositions comprising compounds of the formula: ##STR1## wherein each of one or two R is independently ##STR2## wherein n is an integer from 7 to 20, at least one of X or Y is --OH and if one of X or Y is --OH then the other X or Y is H, 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 W.sub.1, W.sub.2, and W.sub.3 is independently H, 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 wherein the alkyl groups may be substituted by a hydroxyl, halo or dimethylamino group and/or interrupted by an oxygen atom, H or alkyl (1-4C), including resolved enantiomers and/or diastereomers, salts and mixtures thereof. In particular, the compounds lower elevated levels of unsaturated, non-arachidonate phosphatidic acid (PA) and diacylglycerol (DAG) derived from said PA within seconds of the primary stimulus and their contact with said cells. The modulatory effect depends on the nature of the target cell and the stimulus applied.
摘要翻译：公开了包含下式化合物的化合物和药物组合物：独立地为：其中n为7至20的整数，X或Y中的至少一个为-OH，如果X或Y中的一个为-OH，则其它X或Y是H，CH 3，CH 3 -CH 2，CH 3 - （CH 2）2 - 或（CH 3）2 -CH 2 - ，W 1，W 2和W 3独立地为H，CH 3，CH 3 -CH 2， CH 2）2 - 或（CH 3）2 -CH 2 - ，并且其中烷基可以被羟基，卤素或二甲基氨基取代和/或被氧原子H或烷基（1-4C）中断，包括拆分的对映异构体和/或非对映体，其盐和混合物。特别地，所述化合物在主刺激的几秒钟内与所述细胞的接触降低了源自所述PA的不饱和，非花生四烯酸磷脂酸（PA）和二酰基甘油（DAG）的升高水平。调节作用取决于靶细胞的性质和应用的刺激。

7. 发明授权

US5354756A Olefin-substituted long chain xanthine compounds 失效
标题翻译：烯烃取代的长链黄嘌呤化合物
公开(公告)号：US5354756A
公开(公告)日：1994-10-11
申请号：US3372
申请日：1993-01-12
申请人： Gail Underiner , David Porubek , J. Peter Klein
发明人： Gail Underiner , David Porubek , J. Peter Klein
IPC分类号： C07D473/06 , A61K31/52 , C07D473/02
CPC分类号： C07D473/06
摘要： There is disclosed compounds and pharmaceutical compositions having a xanthine core and one or two hydrocarbon side chains bonded to a ring nitrogen atom, wherein the hydrocarbon side chains are independently a straight chain hydrocarbon having at least one double bond in a carbon chain length of from about 4 to about 18 carbon atoms in length, wherein multiple double bonds are separated from each other by at least three carbon atoms, and wherein the hydrocarbon chain may be substituted by a hydroxyl, halo or dimethylamino group and/or interrupted by an oxygen atom. The compounds lower elevated levels of unsaturated, non-arachidonate phosphatidic acid (PA) and diacylglycerol (DAG) derived from said PA within seconds of the primary stimulus and their contact with cells. The modulatory effect depends on the nature of the target cell and the stimulus applied.
摘要翻译：公开了具有与环氮原子键合的黄嘌呤核和一个或两个烃侧链的化合物和药物组合物，其中烃侧链独立地为具有至少一个双键的碳链长度为约 4至约18个碳原子，其中多个双键彼此分开至少三个碳原子，并且其中烃链可以被羟基，卤素或二甲基氨基取代和/或被氧原子中断。该化合物在主要刺激的几秒钟内和与细胞接触的情况下，降低了源自所述PA的不饱和，非花生四烯酸磷脂酸（PA）和二酰基甘油（DAG）的升高水平。调节作用取决于靶细胞的性质和应用的刺激。

8. 发明授权

US5770595A Oxime substituted therapeutic compounds 失效
标题翻译：肟取代的治疗化合物
公开(公告)号：US5770595A
公开(公告)日：1998-06-23
申请号：US193344
申请日：1994-02-07
申请人： J. Peter Klein , Alistair Leigh
发明人： J. Peter Klein , Alistair Leigh
IPC分类号： A61K31/15 , A61K31/52 , C07D473/10
CPC分类号： A61K31/52 , A61K31/15 , C07D473/10
摘要： Oxime-substituted compounds are preferably cyclic or heterocyclic compounds. The oxime-substituted compounds and pharmaceutical compositions thereof have the formula: CORE MOIETY--(R).sub.j including resolved enantiomers (both syn and anti forms) and/or diastereomers, hydrates, salts, solvates and mixtures thereof. j is an integer from one to three, the core moiety is non-cyclic or cyclic and R may be selected from among: hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted C.sub.(1-10), alkyl, C.sub.(2-10) alkenyl, cyclic or heterocyclic groups, and formula I. At least one R has the formula I: --(CH.sub.2).sub.n --C--(R.sub.1).sub.p, I wherein n is an integer from three to twenty; p is two or three; R.sub.1 is selected from among hydrogen; halogen; hydroxide; substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(1-10) alkoxy, C.sub.(2-10) alkenyl, cyclic or heterocyclic group; =N--OR.sub.2, R.sub.2 being hydrogen or a substitute or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, cyclic or heterocyclic group; and --(CH.sub.2).sub.s --C(R.sub.3).sub.t (wherein s is zero or an integer from one to ten, t is two or three, R.sub.3 is hydrogen, halogen, hydroxide, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(1-10) alkoxy, C(.sub.2-10) alkenyl, cyclic or heterocyclic group, or .dbd.N--OR.sub.2, R.sub.2 being defined above). At least one R.sub.1 or one R.sub.3 is .dbd.N--OR.sub.2, p or t corresponding to the at least one R.sub.1 or one R.sub.3 is two, and a second R.sub.1 or second R.sub.3, bonded to the same --C as the at least one R.sub.1 or one R.sub.3, is other than .dbd.N--OR.sub.2. These disclosed compounds are useful in a large variety of therapeutic indications for treating or preventing disease mediated by intracellular signaling through specific intracellular signaling pathways.
摘要翻译：肟取代的化合物优选为环状或杂环化合物。肟取代的化合物及其药物组合物具有下式：包括拆分的对映异构体（顺式和反式）和/或非对映异构体，水合物，盐，溶剂合物及其混合物。 j是1至3的整数，核心部分是非环状或环状的，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- 至少一个R具有式I： - （CH 2）n C - （R 1）p，其中n是3至20的整数; p是两三个; R1选自氢; 卤素; 氢氧化物; 取代或未取代的C（1-10）烷基，C（1-10）烷氧基，C（2-10）烯基，环或杂环基; = N-OR2，R2为氢或取代或未取代的C（1-10）烷基，C（2-10）烯基，环状或杂环基; 和（CH 2）s C（R 3）t（其中s为0或1至10的整数，t为2或3，R 3为氢，卤素，氢氧化物，取代或未取代的C（1-10）烷基，C（ 1-10）烷氧基，C（2-10）烯基，环状或杂环基，或= N-OR2，R2如上所定义）。至少一个R1或一个R3为= N-OR2，p或t对应于至少一个R 1或一个R 3为两个，第二个R 1或第二个R 3，与至少一个R 1或一个R3不是= N-OR2。这些公开的化合物可用于治疗或预防通过特定细胞内信号传导途径通过细胞内信号转导介导的疾病的各种各样的治疗适应症。

9. 发明申请

US20100189726A1 LPAAT-BETA INHIBITORS AND USES THEREOF 审中-公开
标题翻译： LPAAT-BETA抑制剂及其用途
公开(公告)号：US20100189726A1
公开(公告)日：2010-07-29
申请号：US12569639
申请日：2009-09-29
申请人： Lynn BONHAM , J. Peter Klein , Robert E. Finney , David M. Hollenback , Scott A. Shaffer , Norina M. Tang , Thayer H. White , David W. Leung , Baoqing Gong , John Tulinsky
发明人： Lynn BONHAM , J. Peter Klein , Robert E. Finney , David M. Hollenback , Scott A. Shaffer , Norina M. Tang , Thayer H. White , David W. Leung , Baoqing Gong , John Tulinsky
IPC分类号： A61K31/53 , C07D251/50 , C07D405/12 , C07D251/52 , A61K39/00 , A61P35/00
CPC分类号： C07D251/70 , C07D251/50 , C07D251/52 , C07D251/54 , C07D251/58
摘要： The invention relates to triazines and the use thereof to inhibit lysophosphatidic acid acyltransferase β (LPAAT-β) activity. The invention further relates to methods of treating cancer using said triazines. The invention also relates to methods for screening for LPAAT-β activity.
摘要翻译：本发明涉及三嗪及其用于抑制溶血磷脂酰基转移酶的用途。（LPAAT-＆bgr）活动。本发明还涉及使用所述三嗪治疗癌症的方法。本发明还涉及用于筛选LPAAT-＆bgr的方法; 活动。

10. 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：

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