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1. 发明申请

US20050261252A1 LPA receptor agonists and antagonists and methods of use 审中-公开
标题翻译： LPA受体激动剂和拮抗剂及其使用方法
公开(公告)号：US20050261252A1
公开(公告)日：2005-11-24
申请号：US11067884
申请日：2005-02-28
申请人： Duane Miller , Gabor Tigyi , James Dalton , Vineet Sardar , Don Elrod , Huiping Xu , Daniel Baker , Dean Wang , Karoly Liliom , David Fischer , Tamas Virag , Nora Nusser
发明人： Duane Miller , Gabor Tigyi , James Dalton , Vineet Sardar , Don Elrod , Huiping Xu , Daniel Baker , Dean Wang , Karoly Liliom , David Fischer , Tamas Virag , Nora Nusser
IPC分类号： C12N15/09 , A61K31/27 , A61K31/66 , A61K31/685 , A61P17/02 , A61P35/00 , A61P43/00 , C07F9/09 , C07F9/10 , C07F9/11 , C07F9/17 , C07F9/22 , C07F9/38 , C07F9/40 , A61K31/675 , A61K31/663 , C07F9/28
摘要： The present invention relates to compounds according to formula (I) as disclosed herein as well as pharmaceutical compositions which include those compounds. Also disclosed are methods of using such compounds, which have activity as agonists or as antagonists of LPA receptors; such methods including inhibiting LPA activity on an LPA receptor, modulating LPA receptor activity, treating cancer, enhancing cell proliferation, and treating a wound.
摘要翻译：本发明涉及本文公开的式（I）化合物以及包括那些化合物的药物组合物。还公开了使用这些化合物的方法，其具有活性作为LPA受体的激动剂或拮抗剂; 这些方法包括抑制LPA受体的LPA活性，调节LPA受体活性，治疗癌症，增强细胞增殖和治疗伤口。

2. 发明申请

US20080090783A1 LPA Receptor Agonists and Antagonists and Methods of Use 有权
标题翻译： LPA受体激动剂和拮抗剂及其使用方法
公开(公告)号：US20080090783A1
公开(公告)日：2008-04-17
申请号：US11748331
申请日：2007-05-14
申请人： Duane Miller , Gabor Tigyi , Gangadhar Durgam , Tamas Virag , Michelle Walker , Ryoko Tsukahara
发明人： Duane Miller , Gabor Tigyi , Gangadhar Durgam , Tamas Virag , Michelle Walker , Ryoko Tsukahara
IPC分类号： A61K31/661 , A61K31/675 , A61P43/00
CPC分类号： C07F9/11 , A61K31/661 , A61K31/675 , C07F9/113 , C07F9/1651 , C07F9/1653 , C07F9/17 , C07F9/173 , C07F9/3808 , C07F9/4006
摘要： Disclosed are compounds according to formula (I) as well as pharmaceutical compositions which include those compounds. Also disclosed are methods of using such compounds, which have activity as agonists or as antagonists of LPA receptors; such methods including inhibiting LPA activity on an LPA receptor, modulating LPA receptor activity, treating cancer, enhancing cell proliferation, treating a wound, treating apoptosis or preserving or restoring function in a cell, tissue, or organ, culturing cells, preserving organ or tissue function, and treating a dermatological condition.
摘要翻译：公开了根据式（I）的化合物以及包括这些化合物的药物组合物。还公开了使用这些化合物的方法，其具有活性作为LPA受体的激动剂或拮抗剂; 这样的方法包括抑制LPA受体的LPA活性，调节LPA受体活性，治疗癌症，增强细胞增殖，治疗伤口，治疗细胞，组织或器官中的凋亡或维持或恢复功能，培养细胞，保存器官或组织功能，治疗皮肤病。

3. 发明申请

US20060009507A1 LPA receptor agonists and antagonists and methods of use 有权
公开(公告)号：US20060009507A1
公开(公告)日：2006-01-12
申请号：US10963085
申请日：2004-10-12
申请人： Duane Miller , Gabor Tigyi , Gangadhar Durgam , Tamas Virag , Michelle Walker , Ryoko Tsukahara
发明人： Duane Miller , Gabor Tigyi , Gangadhar Durgam , Tamas Virag , Michelle Walker , Ryoko Tsukahara
IPC分类号： A61K31/40 , C07D207/02
CPC分类号： C07F9/11 , A61K31/661 , A61K31/675 , C07F9/113 , C07F9/1651 , C07F9/1653 , C07F9/17 , C07F9/173 , C07F9/3808 , C07F9/4006
摘要： The present invention relates to compounds according to formula (I) as disclosed herein as well as pharmaceutical compositions which include those compounds. Also disclosed are methods of using such compounds, which have activity as agonists or as antagonists of LPA receptors; such methods including inhibiting LPA activity on an LPA receptor, modulating LPA receptor activity, treating cancer, enhancing cell proliferation, treating a wound, treating apoptosis or preserving or restoring function in a cell, tissue, or organ, culturing cells, preserving organ or tissue function, and treating a dermatological condition.

4. 发明申请

US20060270634A1 Acetal phosphate-derived LPA mimics, PPARgamma activators, and autotaxin inhibitors 审中-公开
标题翻译：乙酸磷酸酯衍生的LPA模拟物，PPARγ激活剂和自体贴剂抑制剂
公开(公告)号：US20060270634A1
公开(公告)日：2006-11-30
申请号：US11418561
申请日：2006-05-06
申请人： Duane Miller , Gabor Tigyi , Veeresa Gududuru , Yuko Fujiwara , Daniel Baker , Michelle Walker , Gangadar Durgam
发明人： Duane Miller , Gabor Tigyi , Veeresa Gududuru , Yuko Fujiwara , Daniel Baker , Michelle Walker , Gangadar Durgam
IPC分类号： A61K31/665
CPC分类号： A61K31/665
摘要： Disclosed are compositions that modulate the effects of extracellular LPA receptors, the intracellular PPARγ receptor, and autotaxin, and methods for their use.
摘要翻译：公开了调节细胞外LPA受体，细胞内PPARγ受体和自体调节素的作用的组合物及其使用方法。

5. 发明申请

US20050137172A1 Haloacetamide and azide substituted compounds and methods of use thereof 审中-公开
标题翻译：卤代乙酰胺和叠氮化物取代的化合物及其使用方法
公开(公告)号：US20050137172A1
公开(公告)日：2005-06-23
申请号：US10963761
申请日：2004-10-14
申请人： James Dalton , Duane Miller , Vipin Nair , Huiping Xu
发明人： James Dalton , Duane Miller , Vipin Nair , Huiping Xu
IPC分类号： A61K31/165 , A61K31/21 , A61K31/277 , A61K31/655 , A61K31/66 , C07C235/24 , C07C255/60 , C07D207/44 , C07D207/452 , A61K31/195 , A61K31/32 , A61K31/4015
CPC分类号： C07D207/452 , C07C235/24 , C07C255/60
摘要： The present invention relates to a novel class of anti-cancer compounds, which contain a haloacetamide or azide moiety and are, in one embodiment, alkylating agents. These agents, either alone or in a composition, are useful for treating cancer, preventing cancer, delaying the progression of cancer, treating and/or preventing the recurrence of cancer, suppressing, inhibiting or reducing the incidence of cancer, or inducing apoptosis in a cancer cell. Accordingly, the present invention provides a) methods of treating cancer in a subject; b) methods of preventing cancer in a subject; c) methods of delaying the progression of cancer in a subject; d) methods of treating the recurrence of cancer in a subject; e) methods of preventing the recurrence of cancer in a subject; f) methods of suppressing, inhibiting or reducing the incidence of cancer in a subject; and g) methods of inducing apoptosis in a cancer cell; by administering to the subject an anti-cancer compound of the present invention or an analog or metabolite thereof, its N-oxide, ester, pharmaceutically acceptable salt, hydrate, or any combination thereof as described herein.
摘要翻译：本发明涉及一类新的抗癌化合物，其含有卤代乙酰胺或叠氮化物部分，在一个实施方案中是烷化剂。这些药物单独或组合物可用于治疗癌症，预防癌症，延缓癌症进展，治疗和/或预防癌症复发，抑制，抑制或降低癌症发生率或诱导癌细胞凋亡癌细胞。因此，本发明提供了a）在受试者中治疗癌症的方法; b）预防受试者癌症的方法; c）延缓受试者癌症进展的方法; d）治疗患者癌症复发的方法; e）预防受试者癌症复发的方法; f）抑制或抑制受试者癌症发病率的方法; 和g）诱导癌细胞凋亡的方法; 通过向受试者施用本文所述的抗癌化合物或其类似物或代谢物，其N-氧化物，酯，药学上可接受的盐，水合物或其任何组合。

6. 发明申请

US20050085449A1 Haloacetamide and azide substituted compounds and methods of use thereof 审中-公开
公开(公告)号：US20050085449A1
公开(公告)日：2005-04-21
申请号：US10684582
申请日：2003-10-15
申请人： James Dalton , Duane Miller , Huiping Xu , Vipin Nair
发明人： James Dalton , Duane Miller , Huiping Xu , Vipin Nair
IPC分类号： A61K31/165 , A61K31/21 , A61K31/277 , A61K31/655 , A61K31/66 , C07C235/24 , C07C255/60 , C07D207/44 , C07D207/452
CPC分类号： C07D207/452 , A61K31/165 , A61K31/21 , A61K31/277 , A61K31/655 , A61K31/66 , C07C235/24 , C07C255/60
摘要： The present invention relates to a novel class of anti-cancer compounds, which contain a haloacetamide or azide moiety and are, in one embodiment, alkylating agents. These agents, either alone or in a composition, are useful for treating cancer, preventing cancer, delaying the progression of cancer, treating and/or preventing the recurrence of cancer, suppressing, inhibiting or reducing the incidence of cancer, or inducing apoptosis in a cancer cell. Accordingly, the present invention provides a) methods of treating cancer in a subject; b) methods of preventing cancer in a subject; c) methods of delaying the progression of cancer in a subject; d) methods of treating the recurrence of cancer in a subject; e) methods of preventing the recurrence of cancer in a subject; f) methods of suppressing, inhibiting or reducing the incidence of cancer in a subject; and g) methods of inducing apoptosis in a cancer cell; by administering to the subject an anti-cancer compound of the present invention or an analog or metabolite thereof, its N-oxide, ester, pharmaceutically acceptable salt, hydrate, or any combination thereof as described herein.

7. 发明申请

US20070078111A1 LPA2 receptor agonist inhibitors of CFTR 审中-公开
标题翻译： CFTR的LPA2受体激动剂抑制剂
公开(公告)号：US20070078111A1
公开(公告)日：2007-04-05
申请号：US11489062
申请日：2006-07-19
申请人： Gabor Tigyi , Duane Miller , Leonard Johnson , Veeresa Gududuru , Anjaparavanda Naren , Chunying Li , Wenlin Deng , Gangadhar Durgam
发明人： Gabor Tigyi , Duane Miller , Leonard Johnson , Veeresa Gududuru , Anjaparavanda Naren , Chunying Li , Wenlin Deng , Gangadhar Durgam
IPC分类号： A61K31/685 , A61K31/665 , A61K31/66
CPC分类号： A61K31/661 , A61K31/66 , A61K31/665 , A61K31/685 , A61K45/06 , Y02A50/471 , Y02A50/473 , A61K2300/00
摘要： Methods and compositions for treating or preventing diarrhea are disclosed. The methods comprise administering to an individual a therapeutically effective amount of an LPA2 receptor agonist for treating or preventing diarrhea. Also disclosed is a method of inhibiting CFTR activation by administering at least one LPA2 receptor agonist in an amount effective to inhibit formation of a macromolecular complex between the LPA2 receptor, CFTR, and a Na+/H+ exchange regulatory factor-2 (NHERF-2).
摘要翻译：公开了治疗或预防腹泻的方法和组合物。所述方法包括向个体施用治疗有效量的用于治疗或预防腹泻的LPA 2受体激动剂。还公开了通过施用至少一种LPA 2受体激动剂来抑制CFTR活化的方法，所述激动剂的量有效抑制LPA 2受体CFTR之间的大分子复合物的形成，和Na + + / H +交换调节因子-2（NHERF-2）。

8. 发明申请

US20070265290A1 Heterocyclic selective androgen receptor modulators and methods of use thereof 审中-公开
标题翻译：杂环选择性雄激素受体调节剂及其使用方法
公开(公告)号：US20070265290A1
公开(公告)日：2007-11-15
申请号：US11723957
申请日：2007-03-22
申请人： James Dalton , Duane Miller
发明人： James Dalton , Duane Miller
IPC分类号： A61K31/505 , A61K31/16 , A61K31/40 , A61K31/41 , C07D221/22 , C07D239/00 , C07D277/00 , C07D401/00 , C07D263/02 , C07D233/00 , A61K31/506 , A61K31/4164 , A61K31/44
CPC分类号： C07D213/75 , C07D213/84 , C07K14/721
摘要： This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.
摘要翻译：本发明提供一类雄激素受体靶向剂（ARTA）。这些药剂定义了一种新的化合物亚类，它们是选择性雄激素受体调节剂（SARM）。已经发现几种SARM化合物对雄激素受体具有非甾类化合物的意想不到的雄激素和合成代谢活性。已经发现其他SARM化合物对雄激素受体具有非甾类配体的意想不到的抗雄激素活性。 SARM化合物，单独或作为组合物，可用于a）男性避孕; b）治疗各种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血，肥胖，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; c）治疗与男性雄激素降低相关的病症（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌营养不良，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌癌症，子宫癌和卵巢癌; d）治疗和/或预防急性和/或慢性肌肉消瘦病症; e）预防和/或治疗干眼症状; f）口服雄激素替代疗法; g）降低前列腺癌的发生率，停止或导致消退; 和/或h）诱导癌细胞中的细胞凋亡。

9. 发明申请

US20060111441A1 Treating wasting disorders with selective androgen receptor modulators 有权
标题翻译：用选择性雄激素受体调节剂治疗浪费障碍
公开(公告)号：US20060111441A1
公开(公告)日：2006-05-25
申请号：US11220414
申请日：2005-09-07
申请人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
发明人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
IPC分类号： A61K31/277
CPC分类号： A61K31/277
摘要： This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, by administering to the subject a selective androgen receptor modulator (SARM) and/or an analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, impurity or crystal of said SARM compound, or any combination thereof.
摘要翻译：本发明提供：1）治疗患有肌肉消瘦障碍的受试者的方法; 2）预防受试者的肌肉消瘦障碍的方法; 3）治疗，预防，抑制，抑制或减轻患有肌肉消瘦障碍的受试者的肌肉损失的方法; 4）一种治疗，预防，抑制，减少或抑制患有肌肉消瘦障碍的受试者的肌肉消瘦的方法; 和/或5）通过向受试者施用选择性雄激素受体调节剂（SARM）和/或类似物衍生物，治疗，预防，抑制，减少或抑制患有肌肉消瘦疾病的受试者的肌肉蛋白分解代谢的方法，所述SARM化合物的异构体，代谢物，药学上可接受的盐，药物产品，水合物，N-氧化物，前药，多晶型物，杂质或晶体，或其任何组合。

10. 发明申请

US20060040998A1 Thiazolidinone amides, thiazolidine carboxylic acid amides, methods of making, and uses thereof 有权
标题翻译：噻唑烷酮酰胺，噻唑烷羧酸酰胺，其制备方法和用途
公开(公告)号：US20060040998A1
公开(公告)日：2006-02-23
申请号：US10992175
申请日：2004-11-18
申请人： Duane Miller , Veeresa Gududuru , James Dalton , Eunju Hurh
发明人： Duane Miller , Veeresa Gududuru , James Dalton , Eunju Hurh
IPC分类号： A61K31/427 , C07D417/02
CPC分类号： C07D277/06 , C07D277/14 , C07D277/20 , C07D277/34 , C07D277/56 , C07D417/04
摘要： Substituted thiazolidinone carboxylic acid amides and substituted thiazolidine carboxylic acid amides according to formulae (I) and (II) are disclosed where the various substituent groups are as defined in the specification. Methods of making these compounds, pharmaceutical compositions containing the compounds, and their use, particularly for treating or preventing cancer, are also disclosed.
摘要翻译：公开了根据式（I）和（II）的取代的噻唑烷酮羧酸酰胺和取代的噻唑烷羧酸酰胺，其中各种取代基如说明书中所定义。还公开了制备这些化合物的方法，含有这些化合物的药物组合物及其用途，特别是用于治疗或预防癌症的方法。

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