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1. 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。

2. 发明授权

US06503916B2 Treatment of ischemic brain injury 有权
公开(公告)号：US06503916B2
公开(公告)日：2003-01-07
申请号：US10150898
申请日：2002-05-17
申请人： James C Grotta , Roger A Strong , Jaroslaw Adam Aronowski
发明人： James C Grotta , Roger A Strong , Jaroslaw Adam Aronowski
IPC分类号： A61K31522
CPC分类号： A61K31/522 , A61K31/52 , A61K2300/00
摘要： A composition and method adapted for the treatment of ischemic brain injury is disclosed, which includes applying hypothermic conditions to a subject within 5 hours after onset of brain injury and administering to the subject in need thereof a dose of a pharmaceutically effective amount of caffeine and at least a pharmaceutically effective amount of an alcohol or mixtures thereof adapted for the treatment of cerebral ischemia under hypothermic conditions.

3. 发明授权

US06642240B2 Treating emesis in a mammal 有权
标题翻译：化合物
公开(公告)号：US06642240B2
公开(公告)日：2003-11-04
申请号：US10190170
申请日：2002-07-03
申请人： Giuseppe Alvaro , Romano Di Fabio , Riccardo Giovannini , Giuseppe Guercio , Yves St-Denis , Antonella Ursini
发明人： Giuseppe Alvaro , Romano Di Fabio , Riccardo Giovannini , Giuseppe Guercio , Yves St-Denis , Antonella Ursini
IPC分类号： A61K31522
CPC分类号： C07D401/06 , A61K31/135 , A61K31/196 , A61K31/495 , A61K31/496 , C07D241/04 , C07D403/06 , A61K2300/00
摘要： The invention relates to piperazine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their medical use. The novel compounds are antagonists of tachykinins, including substance P and other neurokinins.
摘要翻译：本发明涉及哌嗪衍生物，其制备方法，含有它们的药物组合物及其医疗用途。新化合物是速激肽的拮抗剂，包括物质P和其他神经激肽。

4. 发明授权

US06500834B1 Composition and method for treatment of cerebral ischemia 有权
标题翻译：治疗脑缺血的组合物和方法
公开(公告)号：US06500834B1
公开(公告)日：2002-12-31
申请号：US09552924
申请日：2000-04-20
申请人： James Grotta , Roger Strong , Jaroslaw Aronowski
发明人： James Grotta , Roger Strong , Jaroslaw Aronowski
IPC分类号： A61K31522
CPC分类号： A61K31/52 , A61K31/522 , Y10S514/922 , A61K31/045 , A61K2300/00
摘要： A composition and method for the treatment of cerebral ischemia is disclosed, the composition is a mixture of caffeine and alcohol and is used to treat cerebral ischemia by administering to a subject in need thereof a dose of an effective amount of caffeine and at least a effective amount of an alcohol or mixtures thereof.
摘要翻译：公开了治疗脑缺血的组合物和方法，该组合物是咖啡因和酒精的混合物，并且用于通过向有需要的受试者施用有效量的咖啡因和至少一种有效量的咖啡因来治疗脑缺血醇的量或其混合物。

5. 发明授权

US06693106B2 Pentoxifylline, pioglitazone and metformin are inhibitors of formation of advanced glycation endproducts (AGE's) 有权
标题翻译：己酮可可碱，吡格列酮和二甲双胍是形成晚期糖基化终末产物（AGE）的抑制剂
公开(公告)号：US06693106B2
公开(公告)日：2004-02-17
申请号：US10096579
申请日：2002-03-14
申请人： Samuel Rahbar , Jerry L. Nadler
发明人： Samuel Rahbar , Jerry L. Nadler
IPC分类号： A61K31522
CPC分类号： A61K31/196 , A61K31/155 , A61K31/198 , A61K31/4439 , A61K31/522 , A61K31/606
摘要： Pentoxifylline, pioglitazone and metformin have been found to inhibit the nonenzymatic glycation of proteins which often results in formation of advanced glycation endproducts and crosslinks. The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences. The compounds of the present invention can be used to inhibit this process of nonenzymatic glycation and therefore to inhibit some of the ill effects caused by diabetes or by aging. The compounds are also useful for preventing premature aging, rheumatoid arthritis, Alzheimer's disease, uremia, neurotoxicity, atherosclerosis and spoilage of proteins in food and can prevent discoloration of teeth.
摘要翻译：已经发现己酮可可碱，吡格列酮和二甲双胍抑制蛋白质的非酶糖基化，这通常导致晚期糖基化终产物和交联的形成。蛋白质的非酶糖基化和交联是衰老过程的一部分，其中长寿命蛋白质的糖基化终产物和交联随年龄增长。在血液中和细胞内环境中还原糖浓度升高时，如糖尿病发生，该过程增加。受影响的分子的结构和功能完整性受到这些修饰的干扰，并可能导致严重后果。本发明的化合物可用于抑制非酶糖基化的方法，并因此抑制由糖尿病或老化引起的一些不良作用。该化合物还可用于预防过早衰老，类风湿性关节炎，阿尔茨海默病，尿毒症，神经毒性，动脉粥样硬化和食物中蛋白质的变质，并可防止牙齿变色。

6. 发明授权

US06514980B1 Nucleoside analogs in combination therapy of herpes simplex infections 有权
标题翻译：核苷类似物联合治疗单纯疱疹感染
公开(公告)号：US06514980B1
公开(公告)日：2003-02-04
申请号：US09626015
申请日：2000-07-26
申请人： Malcolm Richard Boyd
发明人： Malcolm Richard Boyd
IPC分类号： A61K31522
CPC分类号： A61K31/57 , A61K31/522 , A61K31/573 , A61K31/66 , A61K31/675 , A61K38/13 , Y10S514/931 , Y10S514/934 , A61K31/52 , A61K2300/00
摘要： A pharmaceutical product comprising a nucleoside analogue active against herpes simplex virus, such as acyclovir/valaciclovir or penciclorivir/famciclovir, and an immunosuppressant, as a combined preparation for simultaneous, separate or sequential use in the treatment and/or prevention of herpes simplex virus infections.
摘要翻译：作为抗单纯疱疹病毒的核苷类似物活性成分的药物制品，例如阿昔洛韦/伐昔洛韦或penciclorivir /泛昔洛韦和免疫抑制剂，作为用于同时，分别或顺序用于治疗和/或预防单纯疱疹病毒感染的组合制剂。

7. 发明授权

US06310205B1 Hypoxathine compounds 失效
标题翻译：低氧化合物
公开(公告)号：US06310205B1
公开(公告)日：2001-10-30
申请号：US09237638
申请日：1999-01-26
申请人： Mark Chasin , Peter Hofer , David Cavalla
发明人： Mark Chasin , Peter Hofer , David Cavalla
IPC分类号： A61K31522
CPC分类号： C07D473/34
摘要： Hypoxanthine compounds of the structure: are disclosed where R3 and R8 are as described herein. The compounds are useful as intermediates to compounds providing PDE IV inhibition activity.
摘要翻译：公开了其中R3和R8如本文所述的结构的次黄嘌呤化合物。该化合物可用作提供PDE IV抑制活性的化合物的中间体。

8. 发明授权

US06727259B2 Remedial agent for neural degeneration 失效
标题翻译：神经变性补救剂
公开(公告)号：US06727259B2
公开(公告)日：2004-04-27
申请号：US09486823
申请日：2000-03-03
申请人： Junichi Shimada , Masako Kurokawa , Ken Ikeda , Fumio Suzuki , Yoshihisa Kuwana
发明人： Junichi Shimada , Masako Kurokawa , Ken Ikeda , Fumio Suzuki , Yoshihisa Kuwana
IPC分类号： A61K31522
CPC分类号： A61K31/52 , A61K31/522 , C07D473/06
摘要： The present invention relates to a therapeutic agent for neurodegenerative disorders, comprising a xanthine derivative represented by formula (I): or a pharmaceutically acceptable salt thereof as an active ingredient wherein X1, X2, R1, R2, R3 and R4 are herein defined.
摘要翻译：本发明涉及一种神经退行性疾病的治疗剂，其包含式（I）表示的黄嘌呤衍生物或其药学上可接受的盐作为活性成分，其中X 1，X 2，R 1，R 本文定义了R 2，R 3和R 4。

9. 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。

10. 发明授权

US06642243B1 Migraine medicine and method for treating same 失效
标题翻译：偏头痛药及其治疗方法
公开(公告)号：US06642243B1
公开(公告)日：2003-11-04
申请号：US09593238
申请日：2000-06-14
申请人： Ashkan Imanzahrai
发明人： Ashkan Imanzahrai
IPC分类号： A61K31522
CPC分类号： A61K31/137 , A61K31/16 , A61K2300/00
摘要： This invention is a safe and effective composition and method for treating acute migraine attacks using pseudoephedrine, acetaminophen, and other agents in an orally administrated form to alleviate the pain and cluster of symptoms characteristic of migraine attacks such as nausea, photophobia, phonophobia, and functional disabilities as well as the prodrome phase of a migraine attack.
摘要翻译：本发明是一种安全有效的组合物和方法，用于以口服给药形式使用伪麻黄碱，对乙酰氨基酚和其他药剂治疗急性偏头痛发作，以缓解偏头痛，畏光，恐慌，功能障碍等特征性症状的疼痛和症状。残疾以及偏头痛发作的前驱阶段。

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