公开(公告)号：US20240343692A1

公开(公告)日：2024-10-17

申请号：US18682031

申请日：2022-06-21

Applicant: University of Pittsburgh - Of the Commonwealth System of Higher Education

Inventor： Peter Wipf ,  Nikhil R. Tasker ,  Ethan J. Pazur

IPC: C07D221/22 ,  A61K31/4045 ,  A61K31/437 ,  A61K31/439 ,  C07D221/18

CPC classification number: C07D221/22 ,  A61K31/4045 ,  A61K31/437 ,  A61K31/439 ,  C07D221/18

Abstract: A compound, or a pharmaceutically acceptable salt thereof, of formula I:






wherein R1, R8, R9, R31, R32, R33, and R34 are each independently H, C1-C6 alkyl, or substituted C1-C6 alkyl; and
R2, R4, R5, R6, and R7 are each independently H, F, Cl, Br, —OR1—NR8R9, C1-C6 alkyl, or substituted C1-C6 alkyl.

公开(公告)号：US20180127369A1

公开(公告)日：2018-05-10

申请号：US15725949

申请日：2017-10-05

Applicant: Mirati Therapeutics, Inc.

Inventor： Matthew Arnold Marx ,  Arkadii Vaisburg ,  James Gail Christensen ,  Robert Anthony Galemmo, JR.

IPC: C07D211/58 ,  C07D213/64 ,  C07D413/14 ,  C07D413/12 ,  C07D401/12 ,  C07D417/12 ,  C07D205/04 ,  C07D211/76 ,  C07D221/22 ,  C07D265/10 ,  C07D211/88

CPC classification number: C07D211/58 ,  C07D205/04 ,  C07D211/76 ,  C07D211/88 ,  C07D213/64 ,  C07D221/22 ,  C07D265/10 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: The present invention relates to compounds that inhibit LSD1 activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.

公开(公告)号：US20180009762A1

公开(公告)日：2018-01-11

申请号：US15708341

申请日：2017-09-19

Applicant: University of Pittsburgh - Of the Commonwealth System of Higher Education

Inventor： Patrick J. Pagano ,  Peter Wipf ,  Maria E. Cifuentes-Pagano ,  Erin M. Skoda

IPC: C07D221/22 ,  C07D413/06 ,  C07D405/10 ,  A61K31/4748 ,  C07D401/06 ,  A61K45/06 ,  C07D453/06 ,  C07D409/06

CPC classification number: C07D221/22 ,  A61K31/4748 ,  A61K45/06 ,  C07D401/06 ,  C07D405/10 ,  C07D409/06 ,  C07D413/06 ,  C07D453/06

Abstract: Embodiments of bridged tetrahydroisoquinolines and methods for their use in selectively inhibiting nicotinamide adenine dinucleotide phosphate (NADPH) oxidase 2 are disclosed. The disclosed compounds have a structure according to general formula I or a pharmaceutically acceptable salt thereof: wherein “” represents a single or double bond, R1 is hydrogen, halogen, lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Ra is hydrogen, —CH2R2, R3, or —SO2R4; R2 is lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R3 is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R4 is lower aliphatic, or substituted or unsubstituted aryl; and R5 is hydrogen, halogen, or lower aliphatic.

公开(公告)号：US09796681B2

公开(公告)日：2017-10-24

申请号：US14888390

申请日：2014-05-01

Applicant: University of Pittsburgh—Of the Commonwealth System of Higher Education

Inventor： Patrick J. Pagano ,  Peter Wipf ,  Maria E. Cifuentes-Pagano ,  Erin M. Skoda

IPC: C07D221/22 ,  A61K31/4748 ,  C07D453/06 ,  A61K45/06 ,  C07D401/06 ,  C07D405/10 ,  C07D409/06 ,  C07D413/06

CPC classification number: C07D221/22 ,  A61K31/4748 ,  A61K45/06 ,  C07D401/06 ,  C07D405/10 ,  C07D409/06 ,  C07D413/06 ,  C07D453/06

Abstract: Embodiments of bridged tetrahydroisoquinolines and methods for their use in selectively inhibiting nicotinamide adenine dinucleotide phosphate (NADPH) oxidase 2 are disclosed. The disclosed compounds have a structure according to general formula I or a pharmaceutically acceptable salt thereof: wherein “” represents a single or double bond, R1 is hydrogen, halogen, lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Ra is hydrogen, —CH2R2, R3, or —SO2R4; R2 is lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R3 is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R4 is lower aliphatic, or substituted or unsubstituted aryl; and R5 is hydrogen, halogen, or lower aliphatic.

公开(公告)号：US20170260201A1

公开(公告)日：2017-09-14

申请号：US15599239

申请日：2017-05-18

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Stephen Hitchcock ,  Holger Monenschein ,  Holly Reichard ,  Huikai Sun ,  Shota Kikuchi ,  Todd Macklin ,  Maria Hopkins

IPC: C07D498/08 ,  C07C53/40 ,  C07C53/18 ,  A61K31/5386 ,  A61K31/19 ,  C07D221/22 ,  C07D519/00 ,  C07D471/04 ,  C07D451/12 ,  C07D453/02 ,  C07D471/08

CPC classification number: C07D498/08 ,  A61K31/19 ,  A61K31/5386 ,  C07C53/18 ,  C07C53/40 ,  C07D221/22 ,  C07D451/12 ,  C07D453/02 ,  C07D471/04 ,  C07D471/08 ,  C07D519/00

Abstract: The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

公开(公告)号：US20170158687A1

公开(公告)日：2017-06-08

申请号：US15296601

申请日：2016-10-18

Applicant: BIOGEN MA INC.

Inventor： Kevin M. Guckian ,  Gnanasambandam Kumaravel ,  Bin Ma ,  Sha Mi ,  Hairuo Peng ,  Zhaohui Shao ,  Lihong Sun ,  Arthur G. Taveras ,  Deping Wang ,  Zhili Xin ,  Lei Zhang

IPC: C07D451/02 ,  C07D401/06 ,  A61K45/06 ,  A61K31/4725 ,  C07D217/22 ,  A61K31/472

CPC classification number: C07D451/02 ,  A61K31/136 ,  A61K31/196 ,  A61K31/439 ,  A61K31/445 ,  A61K31/46 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/5375 ,  A61K31/55 ,  A61K45/06 ,  C07B2200/07 ,  C07C217/22 ,  C07C229/46 ,  C07C229/48 ,  C07C255/59 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/42 ,  C07D209/52 ,  C07D211/34 ,  C07D211/62 ,  C07D217/22 ,  C07D221/22 ,  C07D223/06 ,  C07D295/096 ,  C07D401/06 ,  C07D471/08 ,  Y02A50/401

Abstract: Disclosed are bicyclic aryl compounds of formula (I), that can modulate the activity of the autotaxin (ATX) enzyme. This invention further relates to compounds that are ATX inhibitors, and methods of making and using such compounds in the treatment of demyelination due to injury or disease, as well as for treating proliferative disorders such as cancer.

公开(公告)号：US20170015629A1

公开(公告)日：2017-01-19

申请号：US15277421

申请日：2016-09-27

Applicant: Novira Therapeutics, Inc.

Inventor： George D. Hartman ,  Scott Kuduk

IPC: C07D223/08 ,  A61K31/55 ,  C07D221/22 ,  A61K31/439 ,  C07D267/10 ,  A61K31/554 ,  C07D243/08 ,  A61K31/551 ,  C07D295/26 ,  C07D403/12 ,  C07D223/32 ,  C07D283/00 ,  A61K45/06 ,  A61K31/553

CPC classification number: C07D223/08 ,  A61K31/439 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/554 ,  A61K38/21 ,  A61K45/06 ,  A61K47/60 ,  C07D221/22 ,  C07D223/06 ,  C07D223/32 ,  C07D243/08 ,  C07D267/10 ,  C07D283/00 ,  C07D295/26 ,  C07D403/12 ,  A61K2300/00

Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.

Abstract translation: 本文提供了可用于治疗有需要的受试者的HBV感染的化合物，其药物组合物，以及抑制，抑制或预防受试者中HBV感染的方法。

公开(公告)号：US20160204358A1

公开(公告)日：2016-07-14

申请号：US14902093

申请日：2014-06-06

Applicant: Merck Patent GmbH

Inventor： Mr. Philipp Stoessel ,  Mr. Dominik Joosten ,  Mr. Nils Koenen

IPC: H01L51/00 ,  C07D405/04 ,  C07D401/04 ,  C09K11/02 ,  C07D491/18 ,  C07D491/08 ,  C07D495/08 ,  C07D221/22 ,  C07D471/08

CPC classification number: H01L51/0072 ,  C07D221/22 ,  C07D401/04 ,  C07D405/04 ,  C07D413/04 ,  C07D471/04 ,  C07D471/08 ,  C07D491/08 ,  C07D491/18 ,  C07D495/04 ,  C07D495/08 ,  C09K11/025 ,  H01L51/0052 ,  H01L51/0058 ,  H01L51/0067 ,  H01L51/0071 ,  H01L51/0073 ,  H01L51/5012 ,  H01L51/5056 ,  H01L51/5096

Abstract: The present invention relates to compounds having polycyclic structural units and to electronic devices, in particular organic electroluminescent devices, containing said compounds.

Abstract translation: 本发明涉及具有多环结构单元的化合物和包含所述化合物的电子器件，特别是有机电致发光器件。

公开(公告)号：US09365499B2

公开(公告)日：2016-06-14

申请号：US14234420

申请日：2012-07-26

Applicant: Hui Zhang ,  Yanyan Dong

Inventor： Hui Zhang ,  Yanyan Dong

IPC: C07C237/26 ,  C07D221/20 ,  C07D205/04 ,  C07D205/12 ,  C07D209/52 ,  C07D209/54 ,  A61K31/65 ,  C07C231/12 ,  C07D221/22 ,  C07D305/06 ,  C07D491/107

CPC classification number: C07C237/26 ,  A61K31/65 ,  C07C231/12 ,  C07C2601/04 ,  C07C2602/40 ,  C07C2603/46 ,  C07C2603/94 ,  C07D205/04 ,  C07D205/12 ,  C07D209/52 ,  C07D209/54 ,  C07D221/20 ,  C07D221/22 ,  C07D305/06 ,  C07D491/107

Abstract: The present invention relates to 9-aminomethyl substituted tetracycline compounds represented by formula (I), or pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as well as a method for preparing these compounds and a pharmaceutical composition comprising the same. The present invention relates also to a use of these compounds in the preparation of a medicament for the treatment and/or prophylaxis of tetracycline drug-sensitive disease. wherein, R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, R10, R11, R12, R13a and R13b are each independently as defined in the description.

Abstract translation: 本发明涉及由式（I）表示的9-氨基甲基取代的四环素化合物或其药学上可接受的盐，前药，溶剂化物或异构体，以及制备这些化合物的方法和包含其的药物组合物。 本发明还涉及这些化合物在制备用于治疗和/或预防四环素药物敏感性疾病的药物中的用途。 其中，R2a，R2b，R3，R4a，R4b，R5，R6a，R6b，R7，R8，R9a，R9b，R10，R11，R12，R13a和R13b各自独立地如说明书中所定义。

公开(公告)号：US20160159745A1

公开(公告)日：2016-06-09

申请号：US14905331

申请日：2014-06-17

Applicant: ZHEJIANG WANBANG PHARMACEUTICAL PLC.

Inventor： Shouming ZHAO ,  Ping CHEN ,  Shaoping PENG ,  Yinqiang ZHUANG ,  Rongzhen SHI ,  Jinsheng XIE ,  Weihua XIE

IPC: C07D221/22

CPC classification number: C07D221/22

Abstract: The present invention relates to a method for preparing (−)-huperzine A. The method involves: allowing a mixture of (±)-huperzine A obtained from chemical synthesis and a chiral acid to form (±)-huperzine A chiral acid salt under suitable conditions; recrystallizing the chiral acid salt from an organic solvent and basifying with an alkali to obtain optically pure (−)-huperzine A. The method is convenient to operate and suitable for industrial production. The chemical purity and optical purity of (−)-huperzine A obtained by the method are each greater than 99.5%, satisfying the requirement for raw pharmaceutical purity in the pharmaceutical industry.

Abstract translation: 本发明涉及一种制备（ - ） - 石杉碱甲酯的方法。该方法包括：使从化学合成获得的（±） - 海星嗪A与手性酸的混合物形成（±） - 胡比嗪A手性酸盐 适合条件; 将手性酸盐从有机溶剂中重结晶，并用碱碱化，得到光学纯的（ - ） - 石杉碱A。该方法操作方便，适合工业生产。 通过该方法获得的（ - ） - 石杉碱甲的化学纯度和光学纯度均大于99.5％，满足制药行业原始药物纯度的要求。