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1. 发明申请

US20090099183A1 PYRIMIDINES AND USES THEREOF 审中-公开
标题翻译：吡嗪及其用途
公开(公告)号：US20090099183A1
公开(公告)日：2009-04-16
申请号：US12194192
申请日：2008-08-19
申请人： Rama BHATT , Baoqing GONG , Feng HONG , Scott A. JENKINS , J. Peter KLEIN , Cory T. KOHM , John TULINSKY
发明人： Rama BHATT , Baoqing GONG , Feng HONG , Scott A. JENKINS , J. Peter KLEIN , Cory T. KOHM , John TULINSKY
IPC分类号： A61K31/5377 , C07D239/48 , C12N9/99 , C12N5/00 , A61P35/00 , C07D401/12 , C07D413/12 , A61K31/506 , C07D403/12 , C07D417/12 , A61K31/505
CPC分类号： C07D239/48 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase β (LPAAT-β) activity and/or proliferation of cells such as tumor-cells.
摘要翻译：本发明涉及嘧啶及其用途，包括抑制溶血磷脂酸酰基转移酶β（LPAAT-β）活性和/或细胞例如肿瘤细胞的增殖。

2. 发明授权

US07399860B2 Manufacture of polyglutamate-therapeutic agent conjugates 有权
标题翻译：聚谷氨酸治疗剂缀合物的制造
公开(公告)号：US07399860B2
公开(公告)日：2008-07-15
申请号：US10404152
申请日：2003-04-02
申请人： Anil M. Kumar , J. Peter Klein , Rama Bhatt , Edward Vawter
发明人： Anil M. Kumar , J. Peter Klein , Rama Bhatt , Edward Vawter
IPC分类号： C07D471/00
CPC分类号： A61K47/645
摘要： The invention provides new processes for preparing polyglutamic acid-therapeutic agent conjugates for clinical development and pharmaceutical use, and polyglutamic acid-therapeutic agent conjugates prepared by these processes.
摘要翻译：本发明提供了用于制备用于临床开发和药物用途的聚谷氨酸治疗剂缀合物的新方法，以及通过这些方法制备的聚谷氨酸治疗剂缀合物。

3. 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.

4. 发明授权

US06878715B1 Therapeutic compounds for inhibiting interleukin-12 signals and method for using same 失效
标题翻译：用于抑制白细胞介素-12信号的治疗化合物及其使用方法
公开(公告)号：US06878715B1
公开(公告)日：2005-04-12
申请号：US09544984
申请日：2000-04-07
申请人： J. Peter Klein , Stephen J. Klaus , Anil M. Kumar , Baoqing Gong
发明人： J. Peter Klein , Stephen J. Klaus , Anil M. Kumar , Baoqing Gong
IPC分类号： A61K31/00 , C07D239/54 , C07D473/04 , C07D473/06 , C07D473/10 , C07D487/04 , C07D495/04 , C07D513/04 , A61K31/522
CPC分类号： C07D239/54 , A61K31/00 , C07D473/04 , C07D473/06 , C07D473/10 , C07D487/04 , C07D495/04 , C07D513/04
摘要： Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations associated with disorders affected by Interleukin-12 (“IL-12”) intracellular signaling, such as, for example, Th1 cell-mediated disorders. The therapeutic compounds, pharmaceutically acceptable derivatives (e.g., resolved enantiomers, diastereomers, tautomers, salts and solvates thereof) or prodrugs thereof, have the following general formula: Each X, Y and Z are independently selected from a member of the group consisting of C(R3), N, N(R3) and S. Each R1, R2 and R3 is substituted or unsubstituted and is independently selected from a member of the group consisting of hydrogen, halo, oxo, C(1-20)alkyl, C(1-20)hydroxyalkyl, C(1-20)thioalkyl, C(1-20)alkylamino, C(1-20)alkylaminoalkyl, C(1-20)aminoalkyl, C(1-20)aminoalkoxyalkenyl, C(1-20)aminoalkoxyalkynyl, C(1-20)diaminoalkyl, C(1-20)triaminoalkyl, C(1-20)tetraaminoalkyl, C(5-15)aminotrialkoxyamino, C(1-20)alkylamido, C(1-20)alkylamidoalkyl, C(1-20)amidoalkyl, C(1-20)acetamidoalkyl, C(1-20)alkenyl, C(1-20)alkynyl, C(3-8)alkoxyl, C(1-11)alkoxyalkyl, and C(1-20)dialkoxyalkyl.
摘要翻译：发现具有与五元环结构稠合的六元环结构的新型杂环化合物可用于治疗和预防与受白细胞介素-12（“IL-12”）影响的紊乱相关的症状或表现，，例如，Th1细胞介导的疾病。治疗化合物，药学上可接受的衍生物（例如分解的对映异构体，非对映异构体，互变异构体，其盐和溶剂合物）或其前药具有以下通式：每个X，Y和Z独立地选自C （R 3），N，N（R 3）和S.每个R 1，R 2和R 3是取代或未取代的，并且独立地选自氢，卤素，氧代，C（1-20）烷基，C （1-20）羟基烷基，C（1-20）硫代烷基，C（1-20）烷基氨基，C（1-20）烷基氨基烷基，C（1-20）氨基烷基，C（1-20）氨基烷氧羰基，C（1 （1-20）氨基烷基，C（1-20）四氨基烷基，C（5-15）氨基三烷氧基氨基，C（1-20）烷基酰氨基，C（1-20）烷基氨基烷基，C（1-20））烷基酰氨基烷基，C（1-20）酰氨基烷基，C（1-20）乙酰氨基烷基，C（1-20）烯基，C（1-20）炔基，C（3-8）烷氧基，C（1-11）烷氧基烷基，和C（1-20）二烷氧基烷基。

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

US06469017B1 Method of inhibiting interleukin-12 signaling 失效
标题翻译：抑制白介素12信号传导的方法
公开(公告)号：US06469017B1
公开(公告)日：2002-10-22
申请号：US09008020
申请日：1998-01-16
申请人： Stephen J. Klaus , J. Peter Klein , Anil M. Kumar
发明人： Stephen J. Klaus , J. Peter Klein , Anil M. Kumar
IPC分类号： A61K3152
CPC分类号： C07D473/04 , A61K31/00 , C07D473/06 , C07D487/04 , C07D495/04 , C07D513/04
摘要： A method for blocking IL-12 signaling by administration of the following compound: wherein, R1 is H, CH3, sulfate, phosphate, or salt thereof; R2 is alkyl (C1-12), alkoxyalkyl (C1-11), dialkoxyalkyl, CH2C6H5, —CH2-furan, biotin; and R3 is H, CH3 or CH2C6H5.
摘要翻译：通过给药以下化合物来阻断IL-12信号传导的方法：其中R1是H，CH3，硫酸盐，磷酸盐或其盐; R2是烷基（C1-12），烷氧基烷基（C1-11），二烷氧基烷基，CH2C6H5，-CH2-呋喃，生物素; 并且R 3是H，CH 3或CH 2 C 6 H 5。

7. 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。

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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