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1. 发明授权

US07291616B2 Aryl triazines as LPAAT-β inhibitors and uses thereof 失效
标题翻译：芳基三嗪作为LPAAT-β抑制剂及其用途
公开(公告)号：US07291616B2
公开(公告)日：2007-11-06
申请号：US10285364
申请日：2002-10-30
申请人： Rama Bhatt , Baoqing Gong , Feng Hong , Scott A. Jenkins , J. Peter Klein , Anil M. Kumar , John Tulinsky
发明人： Rama Bhatt , Baoqing Gong , Feng Hong , Scott A. Jenkins , J. Peter Klein , Anil M. Kumar , John Tulinsky
IPC分类号： A61K31/53 , C07D251/48
CPC分类号： C07D403/12 , C07D251/16 , C07D251/18 , C07D251/22 , C07D405/12
摘要： The invention relates to aryl triazines 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：本发明涉及芳基三嗪及其用途，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

US06774130B2 Therapeutic compounds for inhibiting interleukin-12 signaling and methods 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：US06774130B2
公开(公告)日：2004-08-10
申请号：US09288556
申请日：1999-04-09
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： A61K31522
CPC分类号： C07D473/04 , A61K31/00 , C07D473/06 , 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。

3. 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。

4. 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。

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

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：

7. 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。

8. 发明授权

US6075029A Xanthine modulators of metabolism of cellular P-450 失效
标题翻译：细胞P-450代谢的黄嘌呤调节剂
公开(公告)号：US6075029A
公开(公告)日：2000-06-13
申请号：US2345
申请日：1998-01-02
申请人： J. Peter Klein , Anil M. Kumar , Paul Woodson
发明人： J. Peter Klein , Anil M. Kumar , Paul Woodson
IPC分类号： C07D473/04 , A61K31/52 , C07D473/06 , C07D473/10
CPC分类号： C07D473/04
摘要： A new class of xanthine compounds, variously substituted at the 1, 3, 7 and 8 positions, is characterized by an ability to modulate the activity of key enzymes involved in drug metabolism. These compounds generally are useful in affecting drug metabolism and, particularly, in extending the circulating half-life of compounds that are metabolized via P-450-mediated pathways.
摘要翻译：在1,3,7和8位各种替代的新一类黄嘌呤化合物的特征在于调节参与药物代谢的关键酶的活性的能力。这些化合物通常可用于影响药物代谢，特别是延长通过P-450介导途径代谢的化合物的循环半衰期。

9. 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。

10. 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。

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