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1. 发明授权

US07166725B2 Benzo[d]isoxazol-3-ol DAAO inhibitors 有权
标题翻译：苯并[d]异恶唑-3-醇DAAO抑制剂
公开(公告)号：US07166725B2
公开(公告)日：2007-01-23
申请号：US11024151
申请日：2004-12-28
申请人： Q Kevin Fang , Seth Hopkins , Michele Heffernan , Milan Chytil , Peter Wipf
发明人： Q Kevin Fang , Seth Hopkins , Michele Heffernan , Milan Chytil , Peter Wipf
IPC分类号： C07D261/20 , A61K31/42
CPC分类号： C07D261/20
摘要： Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia, or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutic amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein Z1 is N or CR3; Z2 is N or CR4; Z3is O or S; A is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc or a mixture thereof; R1, R2, R3 and R4 are independently selected from hydrogen, alkyl, hydroxy alkoxy, aryl, acyl, halo, cyano, haloalkyl, NHCOOR5 and SO2NH2; R5 is aryl, arylalkyl, heteroaryl or heteroarylalkyl; at least one of R1, R2, R3 and R4 is other than hydrogen; and at least one of Z1 and Z2 is other than N.
摘要翻译：提高D-丝氨酸浓度和降低D-丝氨酸氧化毒性浓度的方法，用于增强学习，记忆和/或认知，或用于治疗精神分裂症，阿尔茨海默病，共济失调或神经性疼痛，或防止神经功能丧失的方法神经变性疾病的特征包括向需要治疗的受试者施用治疗量的式I化合物或其药学上可接受的盐或溶剂合物：其中Z 1是N或CR 3 ; Z 2是N或CR 4; Z 3是O或S; A是氢，烷基或M + M是铝，钙，锂，镁，钾，钠，锌或它们的混合物; R 1，R 2，R 3和R 4独立地选自氢，烷基，羟基烷氧基，芳基，酰基，卤素，氰基，卤代烷基，NHCOOR 5和SO 2 NH 2。 R 5是芳基，芳基烷基，杂芳基或杂芳基烷基; R 1，R 2，R 3和R 4中的至少一个不是氢; 并且Z 1和Z 2中的至少一个不是N。

2. 发明授权

US10308663B2 Inhibitors of PTP4A3 for the treatment of cancer 有权
公开(公告)号：US10308663B2
公开(公告)日：2019-06-04
申请号：US15737062
申请日：2016-06-16
申请人： John S. Lazo , Elizabeth R. Sharlow , Kelley E. McQueeney , Peter Wipf , Joseph M. Salamoun
发明人： John S. Lazo , Elizabeth R. Sharlow , Kelley E. McQueeney , Peter Wipf , Joseph M. Salamoun
IPC分类号： C07D495/04 , A61K31/4365 , A61P35/00
摘要： The invention provides protein tyrosine phosphatase inhibitor compounds, Their pharmaceutical compositions, uses, and methods of use, such as in the treatment of various cancers, and process for making the compounds. Also disclosed is an improved synthesis of protein tyrosine phosphatase inhibitor and precursor compound thienopyridone (5).

3. 发明申请

US20180170946A1 INHIBITORS OF PTP4A3 FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：US20180170946A1
公开(公告)日：2018-06-21
申请号：US15737062
申请日：2016-06-16
申请人： John S. Lazo , Elizabeth R. Sharlow , Kelley E. McQueeney , Peter Wipf , Joseph M. Salamoun
发明人： John S. Lazo , Elizabeth R. Sharlow , Kelley E. McQueeney , Peter Wipf , Joseph M. Salamoun
IPC分类号： C07D495/04 , A61P35/00
CPC分类号： C07D495/04 , A61K31/4365 , A61P35/00
摘要： The invention provides protein tyrosine phosphatase inhibitor compounds, Their pharmaceutical compositions, uses, and methods of use, such as in the treatment of various cancers, and process for making the compounds. Also disclosed is an improved synthesis of protein tyrosine phosphatase inhibitor and precursor compound thienopyridone (5).

4. 发明授权

US09840515B2 Protein kinase D inhibitors 有权
公开(公告)号：US09840515B2
公开(公告)日：2017-12-12
申请号：US13992546
申请日：2011-12-08
申请人： Peter Wipf , Qiming Jane Wang
发明人： Peter Wipf , Qiming Jane Wang
IPC分类号： A61K31/55 , C07D495/04 , C07D487/04 , C07D491/048 , C07D491/147 , C07D498/04 , C07D513/04 , C07D513/14
CPC分类号： C07D495/04 , C07D487/04 , C07D491/048 , C07D491/147 , C07D498/04 , C07D513/04 , C07D513/14
摘要： Compounds according to Formula (I), are potent inhibitors of protein kinase D (pan-PKD) activity. PKD controls key signaling cascades in cells, affecting cell proliferation, gene transcription, and protein trafficking. Accordingly, pharmaceutically acceptable compositions of the inventive compounds are candidate therapeutics for pathological conditions conditioned by changes in PKD activity.

5. 发明授权

US09216976B2 Targeted nitroxide agents 有权
标题翻译：目标氮氧化物
公开(公告)号：US09216976B2
公开(公告)日：2015-12-22
申请号：US14088233
申请日：2013-11-22
申请人： Peter Wipf , Marie-Celine Frantz
发明人： Peter Wipf , Marie-Celine Frantz
IPC分类号： C07D417/12 , A61K31/454 , A61K47/48 , C07D211/58 , C07D401/12 , C07C237/16 , C07D209/46 , C07D211/94 , C07D221/22
CPC分类号： C07K5/08 , A61K31/454 , A61K47/64 , C07C237/16 , C07D209/44 , C07D209/46 , C07D211/58 , C07D211/94 , C07D221/22 , C07D279/06 , C07D401/12 , C07D417/12 , C07D471/08
摘要： Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
摘要翻译：本文提供了可用于自由基清除的组合物和相关方法，对线粒体具有特别的选择性。化合物包含连接到线粒体靶向基团的含氮氧基的基团。化合物可以交联成二聚体而不损失活性。本文还提供了用于防止，减轻和治疗由辐射引起的损伤的方法。该方法包括以有效预防，减轻或治疗由辐射引起的损伤的量和剂量方案将如本文所述的化合物递送至患者。

6. 发明申请

US20130331460A1 CHRYSOPHAENTIN ANALOGS THAT INHIBIT FTSZ PROTEIN 有权
标题翻译：抑制FTSZ蛋白的CHRYSOPHAENTIN模拟物
公开(公告)号：US20130331460A1
公开(公告)日：2013-12-12
申请号：US14000761
申请日：2012-02-24
申请人： Carole A. Bewley , Peter Wipf
发明人： Carole A. Bewley , Peter Wipf
IPC分类号： C07C39/373 , A61K45/06 , C07C37/14 , A61K31/055
CPC分类号： C07C37/14 , A61K31/055 , A61K31/085 , A61K45/06 , C07C39/373 , C07C43/23 , C07D321/00 , Y02A50/473
摘要： Embodiments of antimicrobial chrysophaentin compounds, pharmaceutical compositions including the chrysophaentin compounds, methods for using the chrysophaentin compounds, and methods for synthesizing the chrysophaentin compounds are disclosed. Certain embodiments of the chrysophaentin compounds inhibit FtsZ protein, thereby inhibiting the growth of clinically relevant bacteria, including drug-resistant strains.
摘要翻译：公开了抗微生物菌素化合物的实施方案，包括辣椒素化合物的药物组合物，使用辣椒素化合物的方法，以及合成辣椒素化合物的方法。辣椒素化合物的某些实施方案抑制FtsZ蛋白，从而抑制临床相关细菌（包括耐药菌株）的生长。

7. 发明授权

US08288551B2 Targeted nitroxide agents 有权
标题翻译：目标氮氧化物
公开(公告)号：US08288551B2
公开(公告)日：2012-10-16
申请号：US12505294
申请日：2009-07-17
申请人： Peter Wipf , Marie Celine Frantz
发明人： Peter Wipf , Marie Celine Frantz
IPC分类号： C07D211/00 , A61K31/445
CPC分类号： C07K5/08 , A61K31/454 , A61K47/64 , C07C237/16 , C07D209/44 , C07D209/46 , C07D211/58 , C07D211/94 , C07D221/22 , C07D279/06 , C07D401/12 , C07D417/12 , C07D471/08
摘要： Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
摘要翻译：本文提供了可用于自由基清除的组合物和相关方法，对线粒体具有特别的选择性。化合物包含连接到线粒体靶向基团的含氮氧基的基团。化合物可以交联成二聚体而不损失活性。本文还提供了用于防止，减轻和治疗由辐射引起的损伤的方法。该方法包括以有效预防，减轻或治疗由辐射引起的损伤的量和剂量方案将如本文所述的化合物递送至患者。

8. 发明授权

US07858657B2 Wortmannin analogs and methods of using same in combination with chemotherapeutic agents 有权
标题翻译：渥曼青霉素类似物及其与化学治疗剂组合使用的方法
公开(公告)号：US07858657B2
公开(公告)日：2010-12-28
申请号：US12235730
申请日：2008-09-23
申请人： Lynn D. Kirkpatrick , Garth Powis , Peter Wipf
发明人： Lynn D. Kirkpatrick , Garth Powis , Peter Wipf
IPC分类号： A61K31/352 , A61K31/4025 , C07D311/78 , C07D405/14
CPC分类号： C07D311/78 , A61K31/337 , A61K31/35 , A61K31/366 , A61K31/40 , A61K31/4025 , A61K31/7072 , A61K33/24 , A61K45/06 , C07D311/94 , A61K2300/00
摘要： Novel wortmannin analogs and their use in inhibiting PI-3-kinase activity in mammals and the treatment or prevention of cancer and tumor formation in a subject are described herein. Preferably, the wortmannin analogs may be administered with other chemotherapeutic agents in the treatment of cancer.
摘要翻译：本文描述了新型渥曼青霉素类似物及其在哺乳动物中抑制PI-3-激酶活性和治疗或预防受试者中癌症和肿瘤形成的用途。优选地，渥曼青霉素类似物可以与其它化学治疗剂一起施用于治疗癌症。

9. 发明申请

US20070161573A1 SELECTIVE TARGETING AGENTS FOR MITOCHONDRIA 有权
标题翻译： MITOCHONDRIA的选择性目标代理
公开(公告)号：US20070161573A1
公开(公告)日：2007-07-12
申请号：US11465162
申请日：2006-08-17
申请人： Peter Wipf , Jingbo Xiao , Mitchell P. Fink , Valerian E. Kagan , Yulia Y. Tyurina
发明人： Peter Wipf , Jingbo Xiao , Mitchell P. Fink , Valerian E. Kagan , Yulia Y. Tyurina
IPC分类号： A61K38/06 , A61K38/05 , A61K31/445
CPC分类号： A61K31/445 , A61K47/55 , A61K47/64
摘要： Compositions and methods are disclosed for treating an illness that is caused or associated with cellular damage or dysfunction which is caused by excessive mitochondrial production of reaction oxygen species (ROS). Compositions which act as mitochondria-selective targeting agents using specific structural signaling features recognizable by cells as mitochondrial targeting sequences are discussed. A method for delivering these agents effectively into cells and mitochondria where they act as electron scavengers by way of certain targeting sequences is also disclosed. Mitochondria dysfunction and cell death by way of apoptosis is inhibited as a result of the ROS-scavenging activity, thereby increasing the survival rate of the patient. In a preferred embodiment, the compositions and methods may be administered therapeutically in the field to patients with profound hemorrhagic shock so that survival could be prolonged until it is feasible to obtain surgical control of the bleeding vessels.
摘要翻译：公开了用于治疗由反应氧物质（ROS）的过量线粒体产生引起的与细胞损伤或功能障碍相关的疾病的组合物和方法。讨论了使用细胞可被线粒体靶向序列识别的特异性结构信号特征作为线粒体选择性靶向剂的组合物。还公开了一种将这些试剂有效地递送到细胞和线粒体中的方法，其中它们通过某些靶向序列作为电子清除剂。由于ROS清除活性，线粒体功能障碍和凋亡细胞死亡被抑制，从而增加患者的存活率。在优选的实施方案中，组合物和方法可以在现场给予具有严重出血性休克的患者的治疗上，使得可以延长存活直到获得出血血管的手术控制。

10. 发明授权

US5925660A Phosphatase inhibitors and methods of use thereof 失效
公开(公告)号：US5925660A
公开(公告)日：1999-07-20
申请号：US917016
申请日：1997-08-22
申请人： John S. Lazo , Robert L. Rice , April Cunningham , Peter Wipf
发明人： John S. Lazo , Robert L. Rice , April Cunningham , Peter Wipf
IPC分类号： A61K31/421 , A61P35/00 , A61P43/00 , C07D263/34 , A61K31/42 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/495
CPC分类号： C07D263/34
摘要： The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B. The invention is further directed to a method of inhibiting a protein phosphatase, a method of inhibiting cell proliferation, and pharmaceutical compositions comprising the subject compounds.

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