公开(公告)号：US11964949B2

公开(公告)日：2024-04-23

申请号：US16740660

申请日：2020-01-13

Applicant: The Global Alliance for TB Drug Development, Inc.

Inventor： Christopher B. Cooper ,  Haihong Huang ,  Dongfeng Zhang ,  Nader Fotouhi ,  Takushi Kaneko

IPC: C07D417/14 ,  A61K31/422 ,  A61K31/5386 ,  A61K31/554 ,  A61K45/06 ,  A61P31/06 ,  C07D263/20 ,  C07D263/24 ,  C07D413/06 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12 ,  C07D491/08 ,  C07D491/107 ,  C07D495/08 ,  C07D495/10 ,  C07D498/08 ,  C07D513/08

CPC classification number: C07D263/20 ,  A61K31/422 ,  A61K31/5386 ,  A61K31/554 ,  A61K45/06 ,  A61P31/06 ,  C07D263/24 ,  C07D413/06 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D491/08 ,  C07D491/107 ,  C07D495/08 ,  C07D495/10 ,  C07D498/08 ,  C07D513/08 ,  A61K31/554 ,  A61K2300/00 ,  A61K31/422 ,  A61K2300/00

Abstract: The present invention relates to novel oxazolidinones (Formula I): or a pharmaceutically acceptable salt having ring A characterized by N-containing monocyclic, bicyclic or spirocyclic substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.

公开(公告)号：US20240124388A1

公开(公告)日：2024-04-18

申请号：US18467190

申请日：2023-09-14

Applicant: ModernaTX, Inc.

Inventor： Kerry E. BENENATO ,  Mark CORNEBISE

IPC: C07C229/12 ,  A61K9/00 ,  A61K9/127 ,  A61K9/16 ,  A61K9/51 ,  A61K31/7105 ,  A61K38/17 ,  A61K38/18 ,  A61K47/54 ,  A61K47/69 ,  A61K48/00 ,  C07C227/16 ,  C07C227/18 ,  C07C229/16 ,  C07C233/36 ,  C07C233/72 ,  C07C235/10 ,  C07C255/24 ,  C07C263/20 ,  C07C271/20 ,  C07C275/14 ,  C07C279/12 ,  C07C279/24 ,  C07C279/28 ,  C07C279/32 ,  C07C311/05 ,  C07C335/08 ,  C07D207/27 ,  C07D233/72 ,  C07D249/04 ,  C07D263/20 ,  C07D265/33 ,  C07D271/06 ,  C07D271/10 ,  C07D277/38 ,  C07F9/09 ,  C07K14/505

CPC classification number: C07C229/12 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0073 ,  A61K9/127 ,  A61K9/1272 ,  A61K9/1617 ,  A61K9/1641 ,  A61K9/5123 ,  A61K9/5146 ,  A61K31/7105 ,  A61K38/1725 ,  A61K38/1816 ,  A61K47/543 ,  A61K47/6911 ,  A61K48/0033 ,  A61K48/005 ,  C07C227/16 ,  C07C227/18 ,  C07C229/16 ,  C07C233/36 ,  C07C233/72 ,  C07C235/10 ,  C07C255/24 ,  C07C263/20 ,  C07C271/20 ,  C07C275/14 ,  C07C279/12 ,  C07C279/24 ,  C07C279/28 ,  C07C279/32 ,  C07C311/05 ,  C07C335/08 ,  C07D207/27 ,  C07D233/72 ,  C07D249/04 ,  C07D263/20 ,  C07D265/33 ,  C07D271/06 ,  C07D271/10 ,  C07D277/38 ,  C07F9/091 ,  C07K14/505 ,  A61K9/1271 ,  A61K48/00 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2601/18

Abstract: The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

公开(公告)号：US20190248753A1

公开(公告)日：2019-08-15

申请号：US16397172

申请日：2019-04-29

Applicant: Merck Sharp & Dohme Corp.

Inventor： Mihir B. Mandal ,  David B. Olsen ,  Jing Su ,  Lihu Yang ,  Katherine Young ,  Takao Suzuki ,  Lanying You

IPC: C07D263/20 ,  C07D487/04 ,  A61K45/06 ,  C07D417/10 ,  C07D413/06 ,  A61K31/541 ,  A61K31/4439 ,  A61K31/5377 ,  A61K31/553 ,  C07D413/04 ,  C07D417/14 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/506 ,  C07D413/10 ,  A61K31/422 ,  A61K31/421 ,  C07D413/14 ,  A61K31/427 ,  C07D471/04

CPC classification number: C07D263/20 ,  A61K31/421 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/553 ,  A61K45/06 ,  C07D413/04 ,  C07D413/06 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  A61K2300/00

Abstract: The present invention relates to oxazolidinone compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, E, and R1 are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.

公开(公告)号：US20180127368A1

公开(公告)日：2018-05-10

申请号：US15806554

申请日：2017-11-08

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： David Marcoux ,  Myra Beaudoin Bertrand ,  T.G. Murali Dhar ,  Michael G. Yang ,  Zili Xiao ,  Hai-Yun Xiao ,  Yeheng Zhu ,  Carolyn A. Weigelt ,  Douglas G Batt

IPC: C07D211/48 ,  C07D213/40 ,  C07D295/195 ,  C07D213/75 ,  C07D333/48 ,  C07C317/44 ,  C07D335/02 ,  C07D471/04 ,  C07D307/22 ,  C07D241/08 ,  C07D207/10 ,  C07D207/16 ,  C07D231/08 ,  C07D309/10 ,  C07D211/96 ,  C07D471/10 ,  C07D205/04 ,  C07D207/277 ,  C07D257/04 ,  C07D205/08 ,  A61P37/00

CPC classification number: C07D211/48 ,  A61P37/00 ,  C07B2200/05 ,  C07B2200/07 ,  C07C317/20 ,  C07C317/24 ,  C07C317/30 ,  C07C317/44 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/38 ,  C07C2602/44 ,  C07C2602/50 ,  C07C2603/08 ,  C07C2603/12 ,  C07C2603/16 ,  C07C2603/90 ,  C07D205/04 ,  C07D205/08 ,  C07D207/09 ,  C07D207/10 ,  C07D207/16 ,  C07D207/277 ,  C07D207/28 ,  C07D211/62 ,  C07D211/78 ,  C07D211/96 ,  C07D213/40 ,  C07D213/56 ,  C07D213/75 ,  C07D213/81 ,  C07D215/36 ,  C07D231/06 ,  C07D231/08 ,  C07D231/18 ,  C07D233/64 ,  C07D233/76 ,  C07D233/78 ,  C07D233/90 ,  C07D241/08 ,  C07D249/12 ,  C07D257/04 ,  C07D261/18 ,  C07D263/20 ,  C07D285/06 ,  C07D295/16 ,  C07D295/195 ,  C07D305/08 ,  C07D307/22 ,  C07D309/10 ,  C07D333/48 ,  C07D335/02 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D471/04 ,  C07D471/10 ,  C07F9/091

Abstract: There are described RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

公开(公告)号：US09771345B2

公开(公告)日：2017-09-26

申请号：US13500857

申请日：2010-10-07

Applicant: Francis Barany ,  Maneesh Pingle ,  Sarah Filippa Giardina ,  Donald Bergstrom ,  Lee Daniel Arnold

Inventor： Francis Barany ,  Maneesh Pingle ,  Sarah Filippa Giardina ,  Donald Bergstrom ,  Lee Daniel Arnold

IPC: A61K31/69 ,  C07D319/14 ,  C07D207/12 ,  C07D207/24 ,  C07D209/52 ,  C07D239/42 ,  C07D239/54 ,  C07D241/36 ,  C07D263/20 ,  C07D295/18 ,  C07D307/80 ,  C07D317/10 ,  C07D317/44 ,  C07D319/12 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D413/06 ,  C07D471/14 ,  C07D491/04 ,  C07D491/10 ,  C07D491/14 ,  C07F5/02 ,  C40B30/04

CPC classification number: C07D319/14 ,  C07D207/12 ,  C07D207/24 ,  C07D209/52 ,  C07D239/42 ,  C07D239/54 ,  C07D241/36 ,  C07D263/20 ,  C07D295/18 ,  C07D307/80 ,  C07D317/10 ,  C07D317/44 ,  C07D319/12 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D413/06 ,  C07D471/14 ,  C07D491/04 ,  C07D491/10 ,  C07D491/14 ,  C07F5/025 ,  C40B30/04

Abstract: The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 μM and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.

公开(公告)号：US20170210698A1

公开(公告)日：2017-07-27

申请号：US15476263

申请日：2017-03-31

Applicant: MODERNATX, Inc.

Inventor： Kerry E. Benenato ,  Ellalahewage Sathyajith Kumarasinghe ,  Mark Cornebise

IPC: C07C229/12 ,  A61K38/18 ,  A61K9/00 ,  A61K9/16

CPC classification number: C07C229/12 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0073 ,  A61K9/127 ,  A61K9/1271 ,  A61K9/1272 ,  A61K9/1617 ,  A61K9/1641 ,  A61K9/5123 ,  A61K9/5146 ,  A61K31/7105 ,  A61K38/1725 ,  A61K38/1816 ,  A61K47/543 ,  A61K47/6911 ,  A61K48/00 ,  A61K48/0033 ,  A61K48/005 ,  C07C227/16 ,  C07C227/18 ,  C07C229/16 ,  C07C233/36 ,  C07C235/10 ,  C07C255/24 ,  C07C271/20 ,  C07C275/14 ,  C07C279/12 ,  C07C279/24 ,  C07C279/28 ,  C07C279/32 ,  C07C311/05 ,  C07C335/08 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2601/18 ,  C07D207/27 ,  C07D233/72 ,  C07D249/04 ,  C07D263/20 ,  C07D265/33 ,  C07D271/06 ,  C07D271/10 ,  C07D277/38 ,  C07F9/091 ,  C07K14/505

Abstract: The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

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：US09512112B2

公开(公告)日：2016-12-06

申请号：US14328959

申请日：2014-07-11

Applicant: Roche Palo Alto LLC

Inventor： Li Chen ,  Michael Patrick Dillon ,  Lichun Feng ,  Minmin Yang

IPC: C07D401/02 ,  C07D413/12 ,  C07D207/27 ,  C07D233/32 ,  C07D263/20 ,  C07D407/14 ,  C07D413/10 ,  C07D413/14 ,  C07D473/00 ,  C07D403/12

CPC classification number: A61K31/497 ,  C07D207/27 ,  C07D233/32 ,  C07D263/20 ,  C07D401/14 ,  C07D403/12 ,  C07D407/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D473/00

Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.

Abstract translation: 式I：或其药学上可接受的盐，其中X，Y，R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所定义。

公开(公告)号：US20160318859A1

公开(公告)日：2016-11-03

申请号：US15206553

申请日：2016-07-11

Applicant: MASTEAM BIO-TECH CO. LTD.

Inventor： Yaowu Peng ,  Wenjing Tian ,  Qing Ye ,  Zhicheng Fang

IPC: C07C315/04 ,  C07D263/10

CPC classification number: C07C315/04 ,  C07D263/10 ,  C07D263/20 ,  C07C317/32

Abstract: The present invention discloses a new florfenicol synthesizing method. The method synthesizes florfenicol products meeting requirements of the Drug Administration by a series of combinations of cyclization, selective reduction, fluorinated open ring, deprotection and acylation, hydroxyl sulfoacid esterified configuration converting reaction, hydrolysis reaction and the like. The synthesizing method of the present invention utilizing chiral amine closed-ring aziridine three-membered ring uses a physical separation method to repeatedly purify chiral aminoketone of high yield obtaining single R configuration, and uses selective reduction and converts the configuration to obtain florfenicol, greatly improving atom economy, while avoiding waste water pollution caused by the existing process, and greatly reducing costs for treating waste water and reducing pollution to the environment, thus lowering costs and simplifying the process. In addition, the present invention uses triethylamine hydrofluoride as a fluorinated open-ring reagent, to improve safety of a liquid reaction compared to a gas reaction and reduce corrosion of equipment, facilitating industrial production.

Abstract translation: 本发明公开了一种新的氟苯尼考合成方法。 该方法通过环化，选择性还原，氟化开环，去保护和酰化，羟基磺酸酯化配置转化反应，水解反应等一系列组合合成符合药物管理要求的氟苯尼考产品。 利用手性胺封闭环氮丙啶三元环的本发明合成方法采用物理分离方法，以高产率反复纯化手性氨基酮获得单一R构型，并采用选择性还原法转化构型，得到氟苯尼考，大大提高 原子经济，同时避免现有工艺造成的废水污染，大大降低处理废水的成本，减少对环境的污染，降低成本，简化工艺。 此外，本发明使用三乙基氢氟酸作为氟化开环试剂，以提高与气体反应相比的液体反应的安全性，并减少设备的腐蚀，促进工业生产。

公开(公告)号：US09434702B2

公开(公告)日：2016-09-06

申请号：US14378825

申请日：2013-02-08

Applicant: Zhejiang Hisun Pharmaceutical Co., Ltd. ,  Shanghai Institute of Pharmaceutical Industry

Inventor： Fuli Zhang ,  Chunbo Yang ,  Bin Liang ,  Pengcheng Qiu ,  Hairong Luo ,  Jiang Li ,  Jian Chai ,  Qingfeng Cai

IPC: C07D413/06 ,  C07D263/20

CPC classification number: C07D263/20 ,  C07D413/06

Abstract: Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-(3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazoline) (I), wherein the intermediate (I) is obtained by the cyclization of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III). This process has a short process route, low cost, easy operation, and high yield, so is suitable for a large-scale industrial production.