公开(公告)号：US20240059686A1

公开(公告)日：2024-02-22

申请号：US18085500

申请日：2022-12-20

Applicant: Arvinas Operations, Inc.

Inventor： Andrew P. CREW ,  Hanqing DONG ,  Jing WANG ,  Xin CHEN ,  Yimin QIAN ,  Craig M. CREWS ,  Michael BERLIN ,  Meizhong JIN

IPC: C07D417/14 ,  C07D413/14 ,  C07D417/12 ,  C07D413/12 ,  C07D233/86 ,  C07D401/04 ,  C07D491/107 ,  C07D471/10 ,  A61K45/06 ,  C07K5/078 ,  A61P35/00 ,  A61P25/28

CPC classification number: C07D417/14 ,  C07D413/14 ,  C07D417/12 ,  C07D413/12 ,  C07D233/86 ,  A61P25/28 ,  C07D491/107 ,  C07D471/10 ,  A61K45/06 ,  C07K5/06165 ,  A61P35/00 ,  C07D401/04

Abstract: The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.

公开(公告)号：US20180346780A1

公开(公告)日：2018-12-06

申请号：US15778923

申请日：2016-11-29

Applicant: Hindustan Petroleum Corporation LTD.

Inventor： Raman Ravishankar ,  Chinthalapati Sivakesava Raju ,  Bhaskar Pramanlk ,  Tanmoy Kar ,  Peddy Rao ,  Nettem Venkateswarlu Choudary

IPC: C09K3/32 ,  C07C237/22 ,  B01D17/02

CPC classification number: C09K3/32 ,  B01D17/02 ,  C07C237/22 ,  C07K5/06017 ,  C07K5/06052 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/06165

Abstract: In accordance with the present subject matter there is provided a compound of Formula I wherein, R1 is substituted C1 to C10 alkyl; and R2 is substituted C1 to C10 alkyl, a process for preparing a compound of Formula I, and a gel comprising a compound of Formula I. There is also provided a process for separating a hydrophobic material from a mixture of hydrophobic and hydrophilic material using a compound of Formula I.

公开(公告)号：US20180134748A1

公开(公告)日：2018-05-17

申请号：US15861300

申请日：2018-01-03

Applicant: Shanghai Lumosa Therapeutics Co., Ltd.

Inventor： Shi-Qi PENG ,  Ming ZHAO ,  Jian-Hui WU ,  Yu-Ji WANG ,  Qi-Qi FENG

IPC: C07K5/097 ,  C07K5/11 ,  C07K5/078 ,  C07K5/02 ,  A61K47/54 ,  C07D217/00 ,  A61K47/55 ,  A61K38/00

CPC classification number: C07K5/0821 ,  A61K38/00 ,  A61K47/545 ,  A61K47/55 ,  C07D217/00 ,  C07K5/0215 ,  C07K5/06165 ,  C07K5/1019

Abstract: The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula I shown below: wherein the definitions of T, Q, R1 and R2 are described herein. The compound of the present invention simultaneously has triple functions of thrombolysis, free radical scavenging and thrombus-targeting/antithrombosis. The present invention also relates to a pharmaceutical composition comprising the compound, and a preparation method and a nanostructure of the compound.

公开(公告)号：US20170247324A1

公开(公告)日：2017-08-31

申请号：US15457220

申请日：2017-03-13

Applicant: New York University

Inventor： Paramjit S. Arora ,  Monika Raj ,  Huabin Wu

IPC: C07C391/02 ,  C07K7/06 ,  C07D207/16 ,  C07K5/083 ,  C07K5/062 ,  C07K1/107

CPC classification number: C07C391/02 ,  C07C231/10 ,  C07C231/12 ,  C07C245/08 ,  C07C319/12 ,  C07C2603/10 ,  C07D207/16 ,  C07D209/20 ,  C07D233/64 ,  C07K1/1075 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06052 ,  C07K5/06078 ,  C07K5/06165 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/1008 ,  C07K7/06 ,  C07C237/22 ,  C07C323/59

Abstract: The present invention relates to ligation agents and their use in making an amide ligation product. Methods of making the ligation agents are also disclosed.

公开(公告)号：US09676785B2

公开(公告)日：2017-06-13

申请号：US14331161

申请日：2014-07-14

Applicant: Celgene CAR LLC

Inventor： Deqiang Niu ,  Russell C. Petter ,  Juswinder Singh ,  Arthur F. Kluge ,  Lixin Qiao

IPC: C07D403/14 ,  C07D487/16 ,  C07K5/078 ,  C07K5/083 ,  C07K5/087 ,  C07K5/08 ,  A61K31/4035 ,  A61K31/407 ,  A61K31/506 ,  A61K45/06 ,  C07D403/12 ,  C07D487/04 ,  A61K38/00

CPC classification number: C07D487/16 ,  A61K31/4035 ,  A61K31/407 ,  A61K31/506 ,  A61K38/00 ,  A61K45/06 ,  C07D403/12 ,  C07D403/14 ,  C07D487/04 ,  C07K5/06165 ,  C07K5/0806 ,  C07K5/0812 ,  C07K5/0827

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

公开(公告)号：US20160326216A1

公开(公告)日：2016-11-10

申请号：US15222592

申请日：2016-07-28

Applicant: Celgene Avilomics Research, Inc.

Inventor： Deqiang Niu ,  Russell C. Petter ,  Lixin Qiao ,  Juswinder Singh

IPC: C07K7/06 ,  C07K5/08 ,  C12N9/50 ,  A61K38/06 ,  A61K38/08 ,  C12N9/99 ,  C07K5/093 ,  A61K45/06

CPC classification number: C07K7/06 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4439 ,  A61K31/4965 ,  A61K31/506 ,  A61K38/00 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K45/06 ,  C07D209/52 ,  C07D401/12 ,  C07D403/12 ,  C07K5/06165 ,  C07K5/0802 ,  C07K5/0804 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/081 ,  C07K5/0812 ,  C07K5/0817 ,  C07K5/0819 ,  C07K5/0821 ,  C07K5/0827 ,  C07K5/1016 ,  C12N9/506 ,  C12N9/99 ,  C12Y304/21098

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

公开(公告)号：US09464110B2

公开(公告)日：2016-10-11

申请号：US14628752

申请日：2015-02-23

Applicant: AJINOMOTO CO., INC.

Inventor： Takanori Sugimoto

IPC: C07K5/078 ,  A61K8/44 ,  A61K8/64 ,  A61Q19/00 ,  A61K8/49

CPC classification number: C07K5/06165 ,  A61K8/44 ,  A61K8/4913 ,  A61K8/64 ,  A61Q19/00

Abstract: An acyl dipeptide derivative represented by the formula (1): wherein an acyl group represented by R1—CO— is a saturated or unsaturated, straight or branched chain acyl group having 2-24 carbon atoms, R2 and R3 are each independently a hydrogen atom, an OH group or an OR5 group, R5 is a saturated or unsaturated, straight or branched chain hydrocarbon group having 1-6 carbon atoms, and R4 is a hydrogen atom, or a saturated or unsaturated, straight or branched chain hydrocarbon group having 1-6 carbon atoms, or a salt thereof has a superior antimicrobial effect, and a composition containing the compound is superior in the sensory feel.

公开(公告)号：US20160052965A1

公开(公告)日：2016-02-25

申请号：US14884263

申请日：2015-10-15

Applicant: TetraLogic Birinapant UK Ltd.

Inventor： Stephen M. Condon ,  Matthew G. Laporte ,  Yijun Deng ,  Susan R. Rippin

IPC: C07K5/078

CPC classification number: C07K5/06165 ,  A61K38/00 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D487/14 ,  C07K5/06026 ,  C07K5/0606 ,  Y02A50/411 ,  Y02A50/414

Abstract: Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes. In various embodiments of the invention the Smac mimetics of the invention are combined with chemotherapeutic agents, including, but not limited to topoisomerase inhibitors, kinase inhibitors, NSAIDs, taxanes and platinum containing compounds use broader language

公开(公告)号：US09187496B2

公开(公告)日：2015-11-17

申请号：US13675787

申请日：2012-11-13

Applicant: Idenix Pharmaceuticals, Inc.

Inventor： Cyril B. Dousson ,  David Dukhan ,  Christophe Claude Parsy ,  Claire Pierra ,  Francois-Rene Alexandre ,  Guillaume Brandt ,  Daniel Da Costa ,  Houcine Rahali ,  Jean-Laurent Paparin ,  Michel Derock ,  Thierry Convard ,  Dominique Surleraux

IPC: A61K31/4178 ,  A61K31/381 ,  C07D513/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  A61K31/4184 ,  A61K31/429 ,  A61K31/5377 ,  A61K31/7056 ,  A61K38/05 ,  A61K38/20 ,  A61K38/21 ,  C07K5/078

CPC classification number: C07D513/04 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/429 ,  A61K31/5377 ,  A61K31/7056 ,  A61K38/05 ,  A61K38/20 ,  A61K38/21 ,  A61K38/212 ,  A61K38/215 ,  A61K38/217 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07K5/06165

Abstract: Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.

Abstract translation: 本文提供的是5,5-稠合亚磺酰丙型肝炎病毒抑制剂化合物，例如式I，IA或IB，包含该化合物的药物组合物及其制备方法。 还提供了它们用于在有需要的宿主中治疗HCV感染的方法。

公开(公告)号：US20150315237A1

公开(公告)日：2015-11-05

申请号：US14162328

申请日：2014-01-23

Applicant: Northwestern University

Inventor： Joseph R. Moskal ,  M. Amin Khan

IPC: C07K5/103 ,  A61K38/07

CPC classification number: C07K5/1013 ,  A61K38/00 ,  A61K38/07 ,  C07D403/06 ,  C07K5/06165 ,  C07K5/0823

Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorders, such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

Abstract translation: 公开了具有增强NMDA受体活性调节效力的化合物。 预期这些化合物可用于治疗疾病和病症，例如学习，认知活动和止痛，特别是在缓解和/或减少神经性疼痛方面。 还公开了可口服制剂和其它药学上可接受的化合物递送形式，包括静脉内制剂。