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1. 发明申请

US20160158377A1 BCL-XL Inhibitory Compounds and Antibody Drug Conjugates Including the Same 审中-公开
标题翻译： BCL-XL抑制剂及其抗体药物结合物
公开(公告)号：US20160158377A1
公开(公告)日：2016-06-09
申请号：US14963510
申请日：2015-12-09
申请人： Scott L. Ackler , Nathan B. Bennett , Erwin R. Boghaert , Steve C. Cullen , George Doherty , Robin R. Frey , Anthony R. Haight , Andrew S. Judd , Aaron R. Kunzer , Xiaoqiang Shen , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Xilu Wang , Dennie S. Welch , Michael D. Wendt
发明人： Scott L. Ackler , Nathan B. Bennett , Erwin R. Boghaert , Steve C. Cullen , George Doherty , Robin R. Frey , Anthony R. Haight , Andrew S. Judd , Aaron R. Kunzer , Xiaoqiang Shen , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Xilu Wang , Dennie S. Welch , Michael D. Wendt
IPC分类号： A61K47/48 , C07K16/18 , C07D513/04 , C07D417/14 , C07D487/04
CPC分类号： C07K16/18 , A61K47/6803 , C07D417/14 , C07D487/04 , C07D513/04 , C07K2317/73
摘要： Small molecule Bcl-xL inhibitors and Antibody Drug Conjugates (ADCs) comprising small molecule Bcl-xL inhibitors are disclosed herein. The Bcl-xL inhibitors and ADCs of the disclosure are useful for, among other things, inhibiting anti-apoptotic Bcl-xL proteins as a therapeutic approach towards the treatment of diseases that involve a dysregulated apoptosis pathway.
摘要翻译：本文公开了包含小分子Bcl-xL抑制剂的小分子Bcl-xL抑制剂和抗体药物偶联物（ADC）。本公开的Bcl-xL抑制剂和ADC尤其可用于抑制抗凋亡Bcl-xL蛋白作为治疗涉及失调性凋亡途径的疾病的治疗方法。

2. 发明申请

US20110230459A1 LACTAM ACETAMIDES AS CALCIUM CHANNEL BLOCKERS 有权
标题翻译： LACTAM ACATAMIDES作为钙通道阻断剂
公开(公告)号：US20110230459A1
公开(公告)日：2011-09-22
申请号：US13045010
申请日：2011-03-10
申请人： Irene Drizin , George Doherty , Pramila A. Bhatia , Andrew O. Stewart
发明人： Irene Drizin , George Doherty , Pramila A. Bhatia , Andrew O. Stewart
IPC分类号： A61K31/397 , C07D401/06 , A61K31/4545 , A61K31/496 , C07D471/04 , A61K31/437 , C07D401/02 , C07D487/04 , A61K31/519 , A61K31/497 , A61P25/00 , A61P17/06 , A61P9/00 , A61P17/04 , A61P35/00 , A61P3/10 , A61P15/10 , A61P15/08
CPC分类号： C07D211/76 , C07D401/06 , C07D401/12 , C07D403/06 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04
摘要： The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
摘要翻译：本申请涉及含有式（I）化合物的钙通道抑制剂，其中Ar1，n，R1，X和Y如说明书中所定义。本申请还涉及包含这些化合物的组合物，以及使用这些化合物和组合物治疗病症和病症的方法。

3. 发明申请

US20070043014A1 3,5-Aryl, heteroaryl or cycloalkyl substituted-1,2,4-oxadiazoles as s1p receptor agonists 审中-公开
标题翻译： 3,5-芳基，杂芳基或环烷基取代的-1,2,4-恶二唑作为s1p受体激动剂
公开(公告)号：US20070043014A1
公开(公告)日：2007-02-22
申请号：US10571334
申请日：2004-09-27
申请人： George Doherty , Jeffrey Hale , Irene Legiec , Christopher Lynch , Leslie Toth
发明人： George Doherty , Jeffrey Hale , Irene Legiec , Christopher Lynch , Leslie Toth
IPC分类号： A61K31/506 , A61K31/501 , A61K31/497 , A61K31/4709 , A61K31/4745 , A61K31/4439 , A61K31/4245 , C07D413/04
CPC分类号： C07D413/04 , C07D271/06
摘要： The present invention encompasses compounds of Formula I: (I) as well as the pharmaceutically acceptable salts thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
摘要翻译：本发明包括式I化合物：（I）及其药学上可接受的盐。该化合物可用于治疗免疫介导的疾病和病症，例如骨髓，器官和组织移植排斥反应。包括药物组合物和使用方法。

4. 发明授权

US06943180B2 Substituted N-arylsulfonyl-proline derivatives as potent cell adhesion inhibitors 失效
标题翻译：取代的N-芳基磺酰基 - 脯氨酸衍生物作为有效的细胞粘附抑制剂
公开(公告)号：US06943180B2
公开(公告)日：2005-09-13
申请号：US10472303
申请日：2002-03-15
申请人： George Doherty , Linus S Lin , William K. Hagmann , Ginger Xu-qiang Yang , Linda L. Chang , Shrenik K. Shah , Richard A. Mumford , Theodore Kamenecka
发明人： George Doherty , Linus S Lin , William K. Hagmann , Ginger Xu-qiang Yang , Linda L. Chang , Shrenik K. Shah , Richard A. Mumford , Theodore Kamenecka
IPC分类号： A61K38/00 , A61P1/04 , A61P11/02 , A61P11/06 , A61P25/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D401/12 , C07D401/14 , C07K5/078 , C07D215/20 , A61K31/47
CPC分类号： C07D401/12 , C07D401/14
摘要： Compounds of formula (I) are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, rhinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
摘要翻译：式（I）化合物是VLA-4和/或α4/β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病症。这些化合物可以配制成药物组合物，适用于治疗AIDS相关的痴呆，过敏性结膜炎，过敏性鼻炎，阿尔茨海默病，哮喘，动脉粥样硬化，自体骨髓移植，某些类型的毒性和免疫性肾炎，接触皮肤过敏，包括溃疡性结肠炎和克罗恩病的炎性肠病，炎性肺病，病毒感染的炎症后遗症，脑膜炎，多发性硬化，多发性骨髓瘤，心肌炎，器官移植，牛皮癣，肺纤维化，再狭窄，鼻炎，类风湿性关节炎，败血症关节炎，中风，肿瘤转移，葡萄膜炎和I型糖尿病。

5. 发明申请

US20050070506A1 Selective s1p1/edg1 receptor agonists 审中-公开
标题翻译：选择性s1p1 / edg1受体激动剂
公开(公告)号：US20050070506A1
公开(公告)日：2005-03-31
申请号：US10501176
申请日：2003-01-14
申请人： George Doherty , Michael Forrest , Richard Hajdu , Jeffrey Hale , Li Zhen , Susanne Mandala , Sander Mills , Hugh Rosen , Edward Scolnick
发明人： George Doherty , Michael Forrest , Richard Hajdu , Jeffrey Hale , Li Zhen , Susanne Mandala , Sander Mills , Hugh Rosen , Edward Scolnick
IPC分类号： A61K31/00 , A61K31/66 , G01N33/566
CPC分类号： A61K31/66 , A61K31/00 , G01N33/566 , G01N2500/04
摘要： The present invention encompasses a method of treating an immunoregulatory abnormality in a mammalian patient in need of such treatment comprising administering to said patient a compound which is an agonist of the S1P1/Edg1 receptor in an amount effective for treating said immunoregulatory abnormality, wherein said compound possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor, said compound administered in an amount effective for treating said immunoregulatory abnormality. Pharmaceutical compositions are included. The invention also encompasses a method of identifying candidate compounds that are agonists of the S1P1/Edg1 receptor and which possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor. The invention further encompasses a method of treating a respiratory disease or condition in a mammalian patient in need of such treatment comprising administering to said patient a compound which is an agonist of the S1P1/Edg1 receptor in an amount effective for treating said respiratory disease or condition, wherein said compound possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor.
摘要翻译：本发明包括在需要这种治疗的哺乳动物患者中治疗免疫调节异常的方法，包括以有效治疗所述免疫调节异常的量向所述患者施用作为S1P1 / Edg1受体激动剂的化合物，其中所述化合物对S1P1 / Edg1受体具有S1PR3 / Edg1受体的选择性，所述化合物以有效治疗所述免疫调节异常的量给药。包括药物组合物。本发明还包括鉴定作为S1P1 / Edg1受体的激动剂的候选化合物的方法，并且其具有S1P1 / Edg1受体超过S1PR3 / Edg3受体的选择性。本发明还包括治疗需要这种治疗的哺乳动物患者的呼吸系统疾病或病症的方法，包括向所述患者施用有效治疗所述呼吸系统疾病或病症的S1P1 / Edg1受体激动剂的化合物其中所述化合物对S1P1 / Edg1受体具有超过S1PR3 / Edg3受体的选择性。

6. 发明申请

US20050107345A1 Aminoalkylphosphonates and related compounds as edg receptor agonists 审中-公开
标题翻译：氨基烷基膦酸盐和相关化合物作为edg受体激动剂
公开(公告)号：US20050107345A1
公开(公告)日：2005-05-19
申请号：US10505268
申请日：2003-02-25
申请人： George Doherty , Jeffrey Hale
发明人： George Doherty , Jeffrey Hale
IPC分类号： A61K31/18 , A61K31/197 , A61K31/41 , A61K31/4164 , A61K31/4192 , A61K31/4196 , A61K31/661 , A61K31/662 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/04 , A61P3/10 , A61P5/14 , A61P7/06 , A61P9/10 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P17/10 , A61P17/14 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/06 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/14 , A61P31/18 , A61P31/20 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , C07C229/34 , C07C233/11 , C07C309/24 , C07C311/51 , C07D233/84 , C07D249/04 , C07D249/12 , C07D257/04 , C07D257/06 , C07F9/09 , C07F9/38 , A61K31/433 , A61K31/20 , A61K31/42 , A61K31/4245
CPC分类号： A61K9/4825 , A61K31/66 , C07C229/34 , C07C309/24 , C07C311/51 , C07D233/84 , C07D249/04 , C07D249/12 , C07D257/04 , C07D257/06 , C07F9/094 , C07F9/3808 , C07F9/3826 , C07F9/3882
摘要： The present invention encompasses compounds of formula (II); as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
摘要翻译：本发明包括式（II）的化合物; 以及其药学上可接受的盐和水合物。该化合物可用于治疗免疫介导的疾病和病症，例如骨髓，器官和组织移植排斥反应。包括药物组合物和使用方法。

7. 发明申请

US20050020837A1 N-(benzyl)aminoalkylcarboxylates, phosphinates, phosphonates and tetrazoles as edg receptor agonists 失效
标题翻译： N-（苄基）氨基烷基羧酸盐，次膦酸盐，膦酸盐和四唑作为EDG受体激动剂
公开(公告)号：US20050020837A1
公开(公告)日：2005-01-27
申请号：US10500811
申请日：2003-01-14
申请人： George Doherty , Zhen Li , Jeffrey Hale , Sander Mills
发明人： George Doherty , Zhen Li , Jeffrey Hale , Sander Mills
IPC分类号： A61K31/197 , A61K31/41 , A61K31/4245 , A61K31/662 , A61P1/04 , A61P1/18 , A61P3/10 , A61P11/06 , A61P17/06 , A61P21/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , C07C229/10 , C07C229/14 , C07C229/20 , C07C229/22 , C07D257/04 , C07D333/16 , C07D413/04 , C07F9/30 , C07F9/38 , C07F9/48 , C07F9/59 , C07F9/6553 , C07F9/6558 , C07F9/28 , C07D257/02 , C07C229/34
CPC分类号： C07D413/04 , C07C229/14 , C07C229/20 , C07C229/22 , C07D333/16 , C07F9/301 , C07F9/307 , C07F9/3808 , C07F9/4816 , C07F9/59 , C07F9/655345 , C07F9/65586
摘要： The present invention encompasses compounds of Formula (I) as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
摘要翻译：本发明包括式（I）的化合物及其药学上可接受的盐和水合物。该化合物可用于治疗免疫介导的疾病和病症，例如骨髓，器官和组织移植排斥反应。包括药物组合物和使用方法。

8. 发明授权

US06420418B1 Heterocycle amides as cell adhesion inhibitors 失效
标题翻译：杂环酰胺作为细胞粘附抑制剂
公开(公告)号：US06420418B1
公开(公告)日：2002-07-16
申请号：US09638074
申请日：2000-08-14
申请人： William K. Hagmann , Stephen E. Delaszlo , George Doherty , Linda L. Chang , Ginger X. Yang
发明人： William K. Hagmann , Stephen E. Delaszlo , George Doherty , Linda L. Chang , Ginger X. Yang
IPC分类号： A61K3134
CPC分类号： A61K31/381 , A61K31/341 , A61K31/343 , A61K31/36
摘要： Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
摘要翻译：式I的化合物是VLA-4和/或α4β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。这些化合物可以配制成药物组合物，适用于治疗AIDS相关的痴呆，过敏性结膜炎，过敏性鼻炎，阿尔茨海默病，哮喘，动脉粥样硬化，自体骨髓移植，某些类型的毒性和免疫性肾炎，接触皮肤过敏，包括溃疡性结肠炎和克罗恩病的炎性肠病，炎症性肺病，病毒感染的炎症后遗症，脑膜炎，多发性硬化，多发性骨髓瘤，心肌炎，器官移植，牛皮癣，肺纤维化，再狭窄，视网膜炎，类风湿性关节炎，败血症关节炎，中风，肿瘤转移，葡萄膜炎和I型糖尿病。

9. 发明申请

US20050267018A1 Macrocyclic compounds as inhibitors of viral replication 有权
标题翻译：大环化合物作为病毒复制的抑制剂
公开(公告)号：US20050267018A1
公开(公告)日：2005-12-01
申请号：US11093884
申请日：2005-03-29
申请人： Lawrence Blatt , Steven Andrews , Kevin Condroski , George Doherty , Yutong Jiang , John Josey , April Kennedy , Machender Madduru , Peter Stengel , Steven Wenglowsky , Benjamin Woodard , Laura Woodard
发明人： Lawrence Blatt , Steven Andrews , Kevin Condroski , George Doherty , Yutong Jiang , John Josey , April Kennedy , Machender Madduru , Peter Stengel , Steven Wenglowsky , Benjamin Woodard , Laura Woodard
IPC分类号： A61K31/4709 , A61K38/12
CPC分类号： C07K5/0804
摘要： The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
摘要翻译：实施方案提供了通式I-XIX的化合物，以及包含主题化合物的组合物，包括药物组合物。实施方案还提供治疗方法，包括治疗黄病毒感染的方法，包括丙型肝炎病毒感染和治疗肝纤维化的方法，所述方法通常涉及向有需要的个体施用有效量的主题化合物或组合物。

10. 发明申请

US20100173955A1 4-SUBSTITUTED PHENOXYPHENYLACETIC ACID DERIVATIVES 失效
标题翻译： 4-取代的苯甲酸衍生物
公开(公告)号：US20100173955A1
公开(公告)日：2010-07-08
申请号：US12438112
申请日：2007-08-21
申请人： George Doherty , Adam Cook
发明人： George Doherty , Adam Cook
IPC分类号： A61K31/44 , C07C229/28 , A61K31/195 , C07D213/56 , C07C255/50 , A61K31/277 , C07D333/22 , A61K31/381 , C07D233/54 , A61K31/4164 , A61P37/00 , A61P29/00 , A61P35/00 , A61P17/00 , A61P11/00 , A61P3/10 , A61P1/00
CPC分类号： C07C311/19 , C07C233/75 , C07C233/87 , C07C235/46 , C07C255/57 , C07C271/22 , C07C307/06 , C07C311/06 , C07C317/46 , C07C2601/02 , C07C2601/14 , C07C2602/10 , C07D213/71 , C07D213/81 , C07D213/82 , C07D233/42 , C07D333/16 , Y02P20/55
摘要： Compounds of Formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.
摘要翻译：其中R1，R2，R7，R8，R9，R10和A具有本说明书中给出的含义的式（I）化合物是可用于治疗免疫疾病的DP2受体调节剂。

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