公开(公告)号：US20240287009A1

公开(公告)日：2024-08-29

申请号：US18411304

申请日：2024-01-12

Applicant: Infineum International Limited

Inventor： Evan A. HAIDASZ ,  Robert A. Clarkson ,  Michael A. Collins ,  BENJAMIN G. N. CHAPPELL

IPC: C07D295/03 ,  C07C211/21 ,  C07C211/27 ,  C07C211/45 ,  C07C217/08 ,  C07C217/40 ,  C07C217/76 ,  C07D209/08 ,  C07D217/04 ,  C07D295/033 ,  C07D295/195 ,  C08F36/14

CPC classification number: C07D295/03 ,  C07C211/21 ,  C07C211/27 ,  C07C211/45 ,  C07C217/08 ,  C07C217/40 ,  C07C217/76 ,  C07D209/08 ,  C07D217/04 ,  C07D295/033 ,  C07D295/195 ,  C08F36/14

Abstract: Disclosed herein are addition-polymerizable monomer composition including an amine-derivatized alpha-methyl styrene (ADAMS) monomer according to structure (I) and/or an aminated conjugated aliphatic methylated polyene (ACAMP) monomer according to structure (II):




with k, R1, R2, R3, and R4 defined herein. Difunctional monomers of these types with two polymerizable loci and/or two amine loci are also disclosed herein. Further disclosed herein are methods for making such compositions.

公开(公告)号：US20230365539A1

公开(公告)日：2023-11-16

申请号：US18226638

申请日：2023-07-26

Applicant: QATAR UNIVERSITY

Inventor： Ashraf KHALIL ,  Ala-Eddin AL MOUSTAFA ,  Dana H. ELKHALIFA ,  Feras ALALI

IPC: C07D405/10 ,  A61P35/00 ,  C07D295/033 ,  C07C225/22 ,  C07C317/30 ,  C07D413/10

CPC classification number: C07D405/10 ,  A61P35/00 ,  C07D295/033 ,  C07C225/22 ,  C07C317/30 ,  C07D413/10 ,  A61K45/06

Abstract: Provided herein are compounds, compositions, and methods useful for the treatment of breast cancer, particularly triple negative breast cancers. In certain aspects, provided herein are compounds of formula (I):




or a pharmaceutically acceptable salt or solvate thereof. In certain aspects, provided herein are compositions comprising any of the compounds provided herein. In certain aspects, provided herein are methods for the treatment of cancer in a subject in need thereof comprising administering to the subject an effective amount of any of the compounds or compositions provided herein.

公开(公告)号：US10562872B2

公开(公告)日：2020-02-18

申请号：US16072596

申请日：2017-02-06

Applicant: H. Lundbeck A/S

Inventor： Frederik Diness ,  Morten Meldal ,  Christian Borch Jacobsen

IPC: C07D295/096 ,  C07D333/70 ,  C07D491/113 ,  C07D295/073 ,  C07C209/10 ,  C07D265/30 ,  C07D295/033 ,  C07D413/10 ,  C07C211/52

Abstract: The invention relates to a method for synthesis of 1-[2-(2,4-Dimethyl-phenylsulfanyl)-phenyl]piperazine in the presence of a strong base.

公开(公告)号：US10287260B2

公开(公告)日：2019-05-14

申请号：US14780616

申请日：2014-03-28

Applicant: Japan Science and Technology Agency ,  Furuya Metal Co., Ltd.

Inventor： Mitsuhiro Arisawa ,  Satoshi Shuto ,  Naoyuki Hoshiya ,  Satoshi Arai

IPC: B01J23/44 ,  B01J23/46 ,  B01J23/52 ,  B01J23/75 ,  B01J31/06 ,  B01J31/16 ,  B01J31/28 ,  B01J35/00 ,  B82Y30/00 ,  C07B37/04 ,  B01J23/745 ,  B01J23/755 ,  C07D295/023 ,  C07D295/033

Abstract: Provided is a material that, when compared with SAPd, exhibits the similar activity in cross-coupling (CC) reactions, can decrease the amount of catalytic metal that is mixed into the reaction product, and increases the number of times use can be repeated. Provided are a catalyst and a catalyst precursor that use a catalytic metal other than Pd and that exhibit the CC reaction activity similar to when Pd is used. Provided are a catalyst and a catalyst precursor that exhibit the similar CC reaction activity when using Pd or a catalytic metal other than Pd, without using a carrier such as metal and without using piranha solution. A composite wherein catalytic metal nanoparticles are dispersed in a continuous phase comprising a polymer having C2-6 alkylene group units and phenylene group units (an alkylene group unit being bonded to at least the first and fourth position of the phenylene group unit). The particle diameter of the catalytic metal nanoparticles is at most 20 nm. A composite structure including a substrate, and the aforementioned composite provided to the surface of the substrate. A method for manufacturing the composite structure by dehydrocondensating, in the presence of a catalytic metal compound, a benzene compound having at least two alkyl groups (two of the alkyl groups being at the first and fourth position) in order to form the composite on the substrate surface.

公开(公告)号：US20190040048A1

公开(公告)日：2019-02-07

申请号：US15764616

申请日：2016-09-30

Applicant: CRYSTAL PHARMA, S.A.U.

Inventor： Alfonso PÉREZ ENCABO ,  José Ángel TURIEL HERNANDEZ ,  Yolanda FERNÁNDEZ SAINZ ,  Antonio LORENTE BONDE-LARSEN

IPC: C07D409/04 ,  C07D215/227 ,  C07D295/15 ,  C07D295/033 ,  C07D409/12

Abstract: A process for preparing compounds of formula (I), or a salt or solvate thereof, including Brexpiprazole, which process comprises cyclization of a compound of formula (II) or (III), or a salt or solvate thereof. The invention also refers to intermediates of said process.

公开(公告)号：US20180127389A1

公开(公告)日：2018-05-10

申请号：US15624417

申请日：2017-06-15

Applicant: H. Lundbeck A/S

Inventor： Thomas Ruhland ,  Garrick Paul Smith ,  Benny Bang-Andersen ,  Ask Puschl ,  Ejner Knud Moltzen ,  Kim Andersen

IPC: C07D295/145 ,  C07D295/033 ,  C07D211/20 ,  C07D243/08 ,  C07D211/70 ,  C07D295/096

CPC classification number: C07D295/145 ,  C07D211/20 ,  C07D211/70 ,  C07D243/08 ,  C07D295/033 ,  C07D295/096

Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.

公开(公告)号：US09567307B2

公开(公告)日：2017-02-14

申请号：US13978384

申请日：2012-01-06

Applicant: Neil K. Garg ,  Stephen D. Ramgren ,  Amanda L. Silberstein ,  Kyle W. Quasdorf

Inventor： Neil K. Garg ,  Stephen D. Ramgren ,  Amanda L. Silberstein ,  Kyle W. Quasdorf

IPC: C07D263/38 ,  C07D295/033 ,  C07D295/073 ,  C07D295/096 ,  C07D209/08 ,  C07D211/06 ,  C07F7/10 ,  C07B37/04 ,  C07C209/66 ,  C07C269/06 ,  C07C303/34 ,  C07D209/88 ,  C07D213/74 ,  C07D263/20

CPC classification number: C07D263/38 ,  C07B37/04 ,  C07C209/66 ,  C07C269/06 ,  C07C303/34 ,  C07D209/08 ,  C07D209/88 ,  C07D211/06 ,  C07D213/74 ,  C07D263/20 ,  C07D295/033 ,  C07D295/073 ,  C07D295/096 ,  C07F7/10 ,  C07C211/52 ,  C07C211/55 ,  C07C307/02 ,  C07C271/44

Abstract: Embodiments of the invention provide methods and materials for chemical cross-coupling reactions that utilize aryl alcohol derivatives as cross-coupling partners. Embodiments of the invention include methods for the amination of aryl sulfamates and carbamates, which are attractive cross-coupling partners, particularly for use in multistep synthesis. Illustrative embodiments include versatile means to use simple derivatives of phenol as precursors to polysubstituted aryl amines, as exemplified by a concise synthesis of the antibacterial drug linezolid.

Abstract translation: 本发明的实施方案提供了利用芳基醇衍生物作为交联偶联物的化学交叉偶联反应的方法和材料。 本发明的实施方案包括氨基磺酸芳基酯和氨基甲酸酯的胺化方法，其是有吸引力的交联剂，特别是用于多步合成。 说明性实施方案包括使用苯酚的简单衍生物作为多取代芳基胺的前体的通用方法，例如通过抗菌药物利奈唑胺的简明合成。

公开(公告)号：US09453009B2

公开(公告)日：2016-09-27

申请号：US14566244

申请日：2014-12-10

Applicant: Concert Pharmaceuticals, Inc.

Inventor： Julie F. Liu ,  Xuejun Tang ,  Scott L. Harbeson ,  Craig E. Masse

IPC: C07D413/10 ,  C07D295/135 ,  C07D295/033 ,  C07C215/12 ,  C07D295/02 ,  C07D295/06 ,  C07D295/12 ,  C07D413/14 ,  C07D263/06 ,  A61K31/5377 ,  A61K45/06

CPC classification number: C07D413/10 ,  A61K31/5377 ,  A61K45/06 ,  C07B2200/05 ,  C07C215/12 ,  C07D263/06 ,  C07D295/02 ,  C07D295/033 ,  C07D295/06 ,  C07D295/12 ,  C07D295/135 ,  C07D413/14

Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.

公开(公告)号：US20160137620A1

公开(公告)日：2016-05-19

申请号：US14744197

申请日：2015-06-19

Applicant: H. Lundbeck A/S

Inventor： Thomas Ruhland ,  Garrick Paul Smith ,  Benny Bang-Andersen ,  Ask Puschl ,  Ejner Knud Moltzen ,  Kim Andersen

IPC: C07D295/145 ,  C07D295/033

CPC classification number: C07D295/145 ,  C07D211/20 ,  C07D211/70 ,  C07D243/08 ,  C07D295/033 ,  C07D295/096

Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.

Abstract translation: 本发明提供由通式I表示的化合物，其中取代基在本申请中定义。 这些化合物可用于治疗情感障碍，包括抑郁症，焦虑症，包括一般焦虑症，惊恐障碍和强迫症。

公开(公告)号：US09061963B2

公开(公告)日：2015-06-23

申请号：US14111217

申请日：2012-04-03

Applicant: Manfred Reetz ,  Gerlinde Mehler

Inventor： Manfred Reetz ,  Gerlinde Mehler

IPC: C07D215/38 ,  C07D217/22 ,  C07D295/033 ,  C07D213/74 ,  C07C209/10 ,  C07B43/04

CPC classification number: C07C209/10 ,  C07B43/04 ,  C07D213/74 ,  C07D215/38 ,  C07D217/22 ,  C07D295/033

Abstract: A process is described for preparing aromatic and heteroaromatic amines of the general formula (I) Ar—NR1R2, in which an aromatic compound with the general formula (II) Ar—X is reacted in the presence of a catalyst with an amine of the general formula (III) H—NR1R2 and a base, wherein the catalyst is selected from transition metal complexes having one or more ligands with the general formula (IV).

Abstract translation: 描述了用于制备通式（I）Ar-NR1R2的芳族和杂芳族胺的方法，其中通式（II）Ar-X的芳族化合物在催化剂存在下与一般的胺反应 式（III）H-NR1R2和碱，其中催化剂选自具有一个或多个具有通式（IV）的配体的过渡金属配合物。