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11. 发明申请

US20020132836A1 Compounds and methods for modulating CCR4 function 审中-公开
标题翻译：调节CCR4功能的化合物和方法
公开(公告)号：US20020132836A1
公开(公告)日：2002-09-19
申请号：US09975567
申请日：2001-10-11
申请人： ChemoCentryx Inc.
发明人： Daniel J. Dairaghi , Brian E. McMaster , Thomas J. Schall
IPC分类号： A61K031/426 , A61K031/4245 , A61K031/381 , A61K031/357 , A61K031/341 , A61K031/18
CPC分类号： C07D417/12 , A61K31/00 , A61K31/18 , A61K31/265 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/4245 , A61K31/426 , C07D277/42 , C07D277/82 , C07D513/04
摘要： Compounds and compositions are provided that bind to the CCR4 chemokine receptor and which are useful for treating diseases associated with CCR4 activity, such as contact hypersensitivity.
摘要翻译：提供了结合CCR4趋化因子受体的化合物和组合物，其可用于治疗与CCR4活性相关的疾病，例如接触性超敏反应。

12. 发明申请

US20020094960A1 Anticonvulsant derivatives useful for the treatment of depression 失效
标题翻译：用于治疗抑郁症的抗惊厥药物
公开(公告)号：US20020094960A1
公开(公告)日：2002-07-18
申请号：US09916742
申请日：2001-07-27
发明人： Carlos R. Plata-Salaman , Josue Bacaltchuk , Pedro A.S. Prado-Lima
IPC分类号： A61K031/7024 , A61K031/35 , A61K031/357 , A61K031/255
CPC分类号： A61K31/7048 , A61K31/255 , A61K31/35 , A61K31/357 , A61K31/7024
摘要： Anticonvulsant derivatives useful for treating depression as monotherapy or combination therapy are disclosed.
摘要翻译：公开了用于治疗抑郁症作为单一疗法或组合疗法的抗惊厥药物。

13. 发明申请

US20020035143A1 Application of 2,3,7,8-tetrachlorodibenzo-para-dioxin (TCDD) as a promoter blocker of cancer 失效
公开(公告)号：US20020035143A1
公开(公告)日：2002-03-21
申请号：US09925449
申请日：2001-08-10
发明人： Gary Michael Kayajanian
IPC分类号： A61K031/357
CPC分类号： A61K31/357 , Y10S514/908
摘要： This Invention relates to the use of low levels of the chemical compound 2,3,7,8-tetrachlorodibenzo-para-dioxin (TCDD) as a promoter blocker of specific identified cancers in men, specific identified cancers in women, prostate cancers in black men, and total cancers in each sex.

14. 发明申请

US20020133009A1 Method for opening potassium channels 审中-公开
标题翻译：钾通道开放方法
公开(公告)号：US20020133009A1
公开(公告)日：2002-09-19
申请号：US10090085
申请日：2002-03-04
发明人： George N. Lambrou , Anna Ottlecz , Christine Percicot , Michael Wiederholt
IPC分类号： A61K031/497 , A61K031/4965 , A61K031/506 , A61K031/443 , A61K031/357 , A61K031/5575
CPC分类号： A61K31/4965 , A61K8/37 , A61K31/357 , A61K31/443 , A61K31/497 , A61K31/506 , A61K31/5575 , A61Q7/00
摘要： The present invention relates to a method for opening potassium channels in mammalian cells by administering to a mammal effective amounts of potassium channel-opening keto compounds as described herein.
摘要翻译：本发明涉及通过向哺乳动物施用有效量的本文所述的钾通道开放酮化合物来打开哺乳动物细胞中钾通道的方法。

15. 发明申请

US20020055528A1 Artemisinin analogs having antimalarial, antiproliferative, and antitumor activities and chemoselective methods of making the same 有权
标题翻译：具有抗疟疾，抗增殖和抗肿瘤活性的青蒿素类似物和制备相同的化学选择性方法
公开(公告)号：US20020055528A1
公开(公告)日：2002-05-09
申请号：US09887922
申请日：2001-06-22
发明人： Gary H. Posner , Hardwin O'Dowd , Suji Xie , Theresa A. Shapiro , Christopher Murray
IPC分类号： A61K031/428 , A61K031/427 , A61K031/357 , C07D493/22
CPC分类号： C07D493/18 , C07D519/00
摘要： Methods for producing novel artemisinin analogs and artemisinin dimers having antimalarial, antiproliferative and antitumor activities are described herein. These novel artemisinin analogs and artemisinin dimers have the following structure 1 or diastereomers thereof, having antimalarial, and antiproliferative and antitumor activities wherein, the monomers of the present invention are formed when n is I and R is alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl. The dimers of the present invention are formed when n is 2 and R is a linker including, but not limited to, alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl.
摘要翻译：本文描述了具有抗疟疾，抗增殖和抗肿瘤活性的新型青蒿素类似物和青蒿素二聚体的生产方法。这些新颖的青蒿素类似物和青蒿素二聚体具有以下结构或非对映异构体，具有抗疟疾和抗增殖和抗肿瘤活性，其中当n是I且R是烷基，环烷基，杂烷基，杂环烷基，烯基，炔基，芳基或杂芳基。本发明的二聚体在n为2时形成，R为包括但不限于烷基，环烷基，杂烷基，杂环烷基，烯基，炔基，芳基或杂芳基的连接体。

16. 发明申请

US20020049249A1 PPAR receptor activator compounds for treating cutaneous disorders/afflictions 审中-公开
标题翻译：用于治疗皮肤疾病/病症的PPAR受体激活剂化合物
公开(公告)号：US20020049249A1
公开(公告)日：2002-04-25
申请号：US09933818
申请日：2001-08-22
发明人： Jean-Michel Bernardon , Serge Michel
IPC分类号： A61K031/385 , A61K031/39 , A61K031/357 , A61K031/352 , A61K031/195 , A61K031/192
CPC分类号： A61K31/382 , A61K8/368 , A61K8/447 , A61K31/12 , A61K31/13 , A61K31/185 , A61K31/21 , A61K31/352 , A61K31/357 , A61K31/39 , A61K31/435 , A61K31/498 , A61K2800/70 , A61Q17/00 , A61Q19/00
摘要： Compounds of formula (I): 1 characteristically activators of receptors of PPAR type, are well suited for treating cutaneous disorders/afflictions, notably disorders of the barrier function of the skin, more particularly disorders of the secretion of epidermal lipids, photodermatoses or ulcers, and/or disorders of the metabolism of lipids.
摘要翻译：式（I）化合物：特征为PPAR受体的激活剂，非常适合于治疗皮肤疾病/病症，特别是皮肤屏障功能障碍，更特别是分泌表皮脂质，光皮质病或溃疡的病症，以及 /或脂质代谢紊乱。

17. 发明申请

US20020032177A1 Use of D-chiro-inositol in the treatment of conditions associated with hypothalamic gene expression 审中-公开
标题翻译：使用D-手性肌醇治疗与下丘脑基因表达相关的病症
公开(公告)号：US20020032177A1
公开(公告)日：2002-03-14
申请号：US09844292
申请日：2001-04-30
申请人： Insmed Pharmaceuticals, Inc.
发明人： Geoffrey Allan , Charles V. Mobbs
IPC分类号： A61K031/715 , A61K031/66 , A61K031/357 , A61K031/28 , A61K031/215 , A61K031/075 , A61K031/047
CPC分类号： A61K31/715 , A61K31/047 , A61K31/075 , A61K31/215 , A61K31/28 , A61K31/357 , A61K31/66 , A61K31/00 , A61K2300/00
摘要： The present invention relates to the use of D-chiro-inositol (DCI) as a regulator of hypothalamic gene expression and, more particularly, to the use of DCI and derivatives and metabolites thereof to treat neuroendocrine impairments such as obesity, polycystic ovarian syndrome (PCOS), impaired regulation of hormones during aging and to correct such neuroendocrine impairments and associated functions.
摘要翻译：本发明涉及D-手性肌醇（DCI）作为下丘脑基因表达的调节剂的用途，更具体地说，涉及使用DCI及其衍生物及其代谢物来治疗神经内分泌障碍如肥胖，多囊卵巢综合征 PCOS），老化期间激素的调节受损，并纠正这种神经内分泌障碍和相关功能。

18. 发明申请

US20020022652A1 Methylnogarol compositions and uses thereof 审中-公开
标题翻译：甲基乳剂组合物及其用途
公开(公告)号：US20020022652A1
公开(公告)日：2002-02-21
申请号：US09834180
申请日：2001-04-12
发明人： Dennis M. Brown
IPC分类号： A61K033/24 , A61K031/357 , A61K031/337
CPC分类号： A61K31/357 , A61K31/337 , A61K31/4745 , A61K33/24 , A61K2300/00
摘要： A method of treatment of a host with a cellular proliferative disease, comprising contacting the host with a methylnogarol and an antiproliferative agent, each in an amount sufficient to modulate said cellular proliferative disease, is described. In some embodiments the methylnogarol comprises menogaril (7-O-Methylnogarol; 7-Con-O-Methylnogarol; U-52047; 2,6-Epoxy-2H-naphthacenonull1,2-bnulloxocin-9,16-dione, 4-(dimethylamino)-3,4,5,6,11,12,13,14-octahydro-3,5,8,10,13-pentahydroxy-11-methoxy-6,13 -dimethyl, -(2alpha,3beta,4alpha,5beta,6alpha, 11 alpha, 13alpha)-, (P)-; 2,6-Epoxy-2H-naphthacenonull1,2-bnulloxocin-9,16-dione,4-(dimethylamino)-3,4,5,6,11,12,13,14-octahydro-3,5,8,10,13-pentahydroxy-11-methoxy-6,13-dimethyl-; 7(R)-O-Methylnogarol; 7-OMEN). Antiproliferative agents of the invention comprise alkylating agents, intercalating agents, metal coordination complexes, pyrimidine nucleosides, purine nucleosides, inhibitors of nucleic acid associated enzymes and proteins, and agents affecting structural proteins and cytoplasmic enzymes. The invention comprises the described methods as well as compositions comprising a methylnogarol and an antiproliferative agent.
摘要翻译：描述了一种治疗具有细胞增殖性疾病的宿主的方法，包括使宿主与甲基孕激素和抗增殖剂接触，各自以足以调节所述细胞增殖性疾病的量。在一些实施方案中，甲基头孢菌素包含衣康定（7-O-甲基诺考罗; 7-Con-O-甲基诺考罗尔; U-52047; 2,6-环氧-2H-氢萘并[1,2-b]氧杂环丁烷-9,16-二酮， 4-（二甲基氨基）-3,4,5,6,11,12,13,14-八氢-3,5,8,10,13-五羟基-11-甲氧基-6,13-二甲基 - （2α， 3β，4α，5β，6α，11α，13α） - ，（P） - ; 2,6-环氧-2H-并四氮烯[1,2-b]生物素-9,16-二酮，4-（二甲基氨基） 3,4,5,6,11,12,13,14-八氢-3,5,8,10,13-五羟基-11-甲氧基-6,13-二甲基 - ; 7（R）-O-甲基吗啉; 7-OMEN）。本发明的抗增殖剂包括烷化剂，嵌入剂，金属配位络合物，嘧啶核苷，嘌呤核苷，核酸相关酶和蛋白质的抑制剂以及影响结构蛋白和细胞质酶的试剂。本发明包括所述方法以及包含甲基胃酸和抗增殖剂的组合物。

19. 发明申请

US20020016357A1 Novel discalamide compounds and their use as anti-proliferative agents 失效
标题翻译：新型的discalamide化合物及其作为抗增殖剂的用途
公开(公告)号：US20020016357A1
公开(公告)日：2002-02-07
申请号：US09835692
申请日：2001-04-16
发明人： Sarath P. Gunasekera , Ross E. Longley , Gopal K. Paul , Richard A. Isbrucker , Shirley A. Pomponi
IPC分类号： A61K031/357 , C07D319/14
CPC分类号： C07D493/04 , A61K31/70
摘要： The subject invention provides novel biologically active compounds which are useful for inhibiting cellular proliferation. Because of the biological activity of these compounds, they can be used for immunomodulation and/or treating cancer. In a preferred embodiment, the novel compounds, compositions and methods of use of the subject invention can advantageously be used to inhibit the growth of tumor cells in a mammalian host. More particularly, the subject compounds can be used for inhibiting in a human the growth of tumor cells, including cells of breast, colon, CNS, ovarian, renal, prostate, bone, gastrointestinal, stomach, testicular, or lung tumors, as well as human leukemia or melanoma cells. Specifically exemplified are discalamides A and B.
摘要翻译：本发明提供了可用于抑制细胞增殖的新型生物活性化合物。由于这些化合物的生物活性，它们可用于免疫调节和/或治疗癌症。在优选的实施方案中，本发明的新颖化合物，组合物和使用方法可有利地用于抑制哺乳动物宿主中肿瘤细胞的生长。更具体地，本发明化合物可用于在人体中抑制肿瘤细胞（包括乳腺，结肠，CNS，卵巢，肾，前列腺，骨，胃肠，胃，睾丸或肺肿瘤）的生长，以及人白血病或黑素瘤细胞。具体举例说明的是甲酰胺A和B.

20. 发明申请

US20010056117A1 Oxygen-containing heterocyclic compounds 失效
标题翻译：含氧杂环化合物
公开(公告)号：US20010056117A1
公开(公告)日：2001-12-27
申请号：US09795093
申请日：2001-03-01
发明人： Etsuo Ohshima , Koji Yanagawa , Haruhiko Manabe , Ichiro Miki , Yoshiaki Masuda
IPC分类号： C07D319/16 , A61K031/357
CPC分类号： C07D405/04 , C07D317/46 , C07D319/20 , C07D407/04 , C07D407/08
摘要： The present invention relates to oxygen-containing heterocyclic compounds represented by the following formula (I): 1 wherein m represents an integer of 0 to 4; R1, R2, R3 and R4 independently represent a hydrogen atom, substituted or unsubstituted lower alkyl, etc.; R5 represents substituted or unsubstituted lower alkoxy etc.; R6 represents a hydrogen atom etc.; and Y represents the following formula (II): 2 wherein R9 represents cyano etc., R10 represents a hydrogen atom etc., R1 represents carboxy etc., and R2 represents a hydrogen atom etc.; and the like; or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及由下式（I）表示的含氧杂环化合物：其中m表示0至4的整数; R1，R2，R3和R4独立地表示氢原子，取代或未取代的低级烷基等; R5表示取代或未取代的低级烷氧基等。 R6表示氢原子等。 Y表示下式（II）：其中，R9表示氰基等，R10表示氢原子等，R1表示羧基等，R2表示氢原子等。等等; 或其药学上可接受的盐。

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