公开(公告)号：US11851443B2

公开(公告)日：2023-12-26

申请号：US17579457

申请日：2022-01-19

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Roland Gendron ,  Melissa Fleury ,  Adam D. Hughes

IPC: C07D498/08 ,  C07D213/81 ,  C07D231/14 ,  C07D233/26 ,  C07D233/90 ,  C07D237/24 ,  C07D239/34 ,  C07D241/24 ,  C07D249/04 ,  C07D249/10 ,  C07D249/18 ,  C07D257/04 ,  C07D261/20 ,  C07D263/34 ,  C07D271/06 ,  C07D277/56 ,  C07D307/68 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/12 ,  C07D409/06 ,  C07D471/04 ,  C07D498/04 ,  C07D261/18 ,  C07D207/34 ,  C07D239/36 ,  C07D413/06 ,  A61K31/42 ,  A61K31/422 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D413/12 ,  C07D213/79 ,  C07D213/80 ,  C07D237/04 ,  C07D249/08 ,  C07D249/12 ,  C07D261/12 ,  C07D263/56 ,  C07D277/46 ,  C07D333/40

CPC classification number: C07D498/08 ,  A61K31/42 ,  A61K31/422 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D231/14 ,  C07D233/26 ,  C07D233/90 ,  C07D237/04 ,  C07D237/24 ,  C07D239/34 ,  C07D239/36 ,  C07D241/24 ,  C07D249/04 ,  C07D249/08 ,  C07D249/10 ,  C07D249/12 ,  C07D249/18 ,  C07D257/04 ,  C07D261/12 ,  C07D261/18 ,  C07D261/20 ,  C07D263/34 ,  C07D263/56 ,  C07D271/06 ,  C07D277/46 ,  C07D277/56 ,  C07D307/68 ,  C07D333/40 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/12 ,  C07D409/06 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04 ,  C07D498/04

Abstract: In one aspect, the invention relates to compounds having the formula:




where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

公开(公告)号：US11021456B2

公开(公告)日：2021-06-01

申请号：US16730085

申请日：2019-12-30

Applicant: Aerie Pharmaceuticals, Inc.

Inventor： Mitchell A. deLong ,  Jill Marie Sturdivant ,  Susan M. Royalty

IPC: C07D333/24 ,  C07D213/56 ,  C07D237/04 ,  C07D417/12 ,  C07D413/12 ,  C07D409/12 ,  C07D405/12 ,  C07D401/12 ,  C07D217/24 ,  A61K31/4709 ,  A61K31/16 ,  A61K31/47 ,  A61K31/381 ,  C07C237/48 ,  C07D217/02 ,  C07C237/04

Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.

公开(公告)号：US20210079017A1

公开(公告)日：2021-03-18

申请号：US16947214

申请日：2020-07-23

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Roland Gendron ,  Melissa Fleury ,  Adam D. Hughes

IPC: C07D498/08 ,  C07D213/81 ,  C07D231/14 ,  C07D233/26 ,  C07D233/90 ,  C07D237/24 ,  C07D239/34 ,  C07D241/24 ,  C07D249/04 ,  C07D249/10 ,  C07D249/18 ,  C07D257/04 ,  C07D261/20 ,  C07D263/34 ,  C07D271/06 ,  C07D277/56 ,  C07D307/68 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/12 ,  C07D409/06 ,  C07D471/04 ,  C07D498/04 ,  C07D261/18 ,  C07D207/34 ,  C07D239/36 ,  C07D413/06 ,  A61K31/42 ,  A61K31/422 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D413/12 ,  C07D213/79 ,  C07D213/80 ,  C07D237/04 ,  C07D249/08 ,  C07D249/12 ,  C07D261/12 ,  C07D263/56 ,  C07D277/46 ,  C07D333/40

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

公开(公告)号：US10927096B2

公开(公告)日：2021-02-23

申请号：US16815962

申请日：2020-03-11

Applicant: Nocion Therapeutics, Inc.

Inventor： Bridget McCarthy Cole ,  James Lamond Ellis

IPC: A61K31/55 ,  A61K31/4425 ,  A61K31/452 ,  A61K31/40 ,  A61K31/444 ,  A61K31/4439 ,  A61K31/4025 ,  A61K31/415 ,  C07D207/08 ,  C07D207/16 ,  C07D211/14 ,  C07D211/34 ,  C07D237/04 ,  C07D295/037 ,  C07D207/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D225/02 ,  C07D223/04 ,  C07D211/00 ,  C07D231/12 ,  C07D213/02 ,  C07D401/06 ,  C07D401/12 ,  C07D211/60 ,  C07D213/56 ,  A61K45/06

Abstract: The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.

公开(公告)号：US20170313717A1

公开(公告)日：2017-11-02

申请号：US15416758

申请日：2017-01-26

Applicant: Celgene International II SÀRL

Inventor： Marcus F. Boehm ,  Esther Martinborough ,  Manisha Moorjani ,  Junko Tamiya ,  Liming Huang ,  Adam R. Yeager ,  Enugurthi Brahmachary ,  Thomas Fowler ,  Andrew Novak ,  Premji Meghani ,  Michael Knaggs

IPC: C07D495/04 ,  A61K31/155 ,  C07D417/04 ,  C07D413/14 ,  C07D413/12 ,  C07D413/10 ,  C07D413/04 ,  C07D409/14 ,  C07D409/12 ,  C07D405/12 ,  C07D403/14 ,  C07D403/12 ,  C07D403/10 ,  C07D403/04 ,  C07D401/12 ,  C07D401/04 ,  C07D271/06 ,  C07D243/08 ,  C07D239/26 ,  C07D237/04 ,  C07D233/64 ,  C07D231/12 ,  A61K31/551 ,  A61K31/506 ,  A61K31/505 ,  A61K31/4985 ,  A61K31/4453 ,  A61K31/4245 ,  A61K31/4164 ,  A61K31/415 ,  C07D417/12 ,  C07D471/04

CPC classification number: C07D495/04 ,  A61K31/155 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4245 ,  A61K31/4453 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/506 ,  A61K31/551 ,  C07D231/12 ,  C07D233/64 ,  C07D237/04 ,  C07D239/26 ,  C07D243/08 ,  C07D271/06 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04

Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.

公开(公告)号：US20170037014A1

公开(公告)日：2017-02-09

申请号：US15305257

申请日：2015-04-29

Applicant: E. I. DU PONT DE NEMOURS AND COMPANY

Inventor： Andrew Edmund Taggi ,  Jeffrey Keith Long

IPC: C07D237/04 ,  A01N43/56

CPC classification number: C07D237/04 ,  A01N43/56 ,  C07D237/08 ,  C07D237/14

Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein Q1, X, R1, R1a, R2 and R3, are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

Abstract translation: 公开了式1的化合物，包括所有几何和立体异构体，N-氧化物及其盐，其中Q1，X，R1，R1a，R2和R3如本公开所定义。 还公开了含有式1化合物的组合物和用于控制由真菌病原体引起的植物病害的方法，包括施用有效量的本发明化合物或组合物。

公开(公告)号：US09562019B2

公开(公告)日：2017-02-07

申请号：US12520256

申请日：2007-12-21

Applicant: Hakim Djaballah ,  Harold E. Varmus ,  David Shum ,  Romel Somwar ,  Alexander Chucholowski ,  Mohan Santhanam Thiruvazhi

Inventor： Hakim Djaballah ,  Harold E. Varmus ,  David Shum ,  Romel Somwar ,  Alexander Chucholowski ,  Mohan Santhanam Thiruvazhi

IPC: C07D237/10 ,  C07D237/04 ,  C07D307/68 ,  C07D307/71 ,  C07D307/85 ,  C07D307/92 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  C07D495/04 ,  C07D401/14 ,  C07D405/10 ,  C07D413/04 ,  C07D417/10

CPC classification number: C07D237/04 ,  C07D307/68 ,  C07D307/71 ,  C07D307/85 ,  C07D307/92 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D417/10 ,  C07D471/04 ,  C07D495/04

Abstract: The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.

Abstract translation: 本发明涉及式（I）的哒嗪酮化合物和式（II）的呋喃化合物，式（I）和（II）化合物的药物组合物，包含这些化合物的试剂盒，合成方法和治疗方法 通过施用治疗有效量的式（I）或（II）化合物来治疗受试者的增殖性疾病。 通过筛选小分子文库的集合来鉴定两类化合物。

公开(公告)号：US20130225596A1

公开(公告)日：2013-08-29

申请号：US13816085

申请日：2011-08-09

Applicant: Hiroyuki Kai ,  Takeshi Endoh ,  Sae Jikihara ,  Kentaro Asahi ,  Tohru Horiguchi

Inventor： Hiroyuki Kai ,  Takeshi Endoh ,  Sae Jikihara ,  Kentaro Asahi ,  Tohru Horiguchi

IPC: C07C233/75 ,  C07D239/84 ,  C07D213/74 ,  C07C217/84 ,  C07D211/72 ,  C07D405/06 ,  C07C217/80 ,  C07D413/12 ,  C07D409/12 ,  C07D409/06 ,  C07D277/28 ,  C07D401/14 ,  C07D237/04

CPC classification number: C07D239/545 ,  C07C217/80 ,  C07C217/84 ,  C07C217/92 ,  C07C233/25 ,  C07C233/75 ,  C07C2601/14 ,  C07D211/72 ,  C07D213/64 ,  C07D213/69 ,  C07D213/74 ,  C07D213/79 ,  C07D213/80 ,  C07D213/82 ,  C07D215/22 ,  C07D215/56 ,  C07D217/22 ,  C07D217/24 ,  C07D231/38 ,  C07D233/88 ,  C07D233/96 ,  C07D235/30 ,  C07D237/04 ,  C07D237/20 ,  C07D237/32 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/54 ,  C07D239/557 ,  C07D239/78 ,  C07D239/84 ,  C07D239/95 ,  C07D239/96 ,  C07D241/20 ,  C07D255/02 ,  C07D261/12 ,  C07D263/32 ,  C07D263/34 ,  C07D263/48 ,  C07D265/06 ,  C07D265/10 ,  C07D265/26 ,  C07D265/36 ,  C07D277/20 ,  C07D277/28 ,  C07D277/34 ,  C07D277/38 ,  C07D277/42 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D407/06 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect.A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.

Abstract translation: 本发明提供具有P2X3和/或P2X2 / 3受体拮抗作用的新化合物。 一种具有P2X3和/或P2X2 / 3受体拮抗作用的药物组合物，其包含式（I）化合物：其中环A是取代或未取代的5至7元环烷烃，取代或未取代的5至7元环烯烃或 喜欢; C是碳原子; -X-是-N（R 16） - 等; R 16是氢，取代或未取代的烷基等; R 7是取代或未取代的5元或6元杂芳基，取代或未取代的6至10元芳基; Q1和Q2各自独立地为碳原子或氮原子; -L-是-O-，-S-等; R6是取代或未取代的环烷基，取代或未取代的环烯基等; R2是氢，羟基等，或其药学上可接受的盐或其溶剂合物。

公开(公告)号：US08501731B2

公开(公告)日：2013-08-06

申请号：US12933104

申请日：2009-03-18

Applicant: Youhong Hu ,  Liguang Lou ,  Shijun Lin ,  Hongbing Zhao ,  Zhende Liu ,  Yongping Xu ,  Bo Chao

Inventor： Youhong Hu ,  Liguang Lou ,  Shijun Lin ,  Hongbing Zhao ,  Zhende Liu ,  Yongping Xu ,  Bo Chao

IPC: C07D403/10 ,  C07D401/10 ,  C07D277/04 ,  C07D237/04 ,  C07D413/10 ,  A61K31/55 ,  A61K31/501 ,  A61P35/00

CPC classification number: C07D237/14 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D413/10 ,  C07D417/10 ,  Y02P20/582

Abstract: The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.

Abstract translation: 本发明涉及一类式I的哒嗪酮，其包含作为母核的6- [3-（三氟甲基）苯基]哒嗪-3（2H） - 酮，其制备方法及其在制备药物中的用途 肿瘤，特别是肝癌。

公开(公告)号：USRE43748E1

公开(公告)日：2012-10-16

申请号：US12869074

申请日：2010-08-26

Applicant: Yousuke Furuta ,  Hiroyuki Egawa ,  Nobuhiko Nomura

Inventor： Yousuke Furuta ,  Hiroyuki Egawa ,  Nobuhiko Nomura

IPC: C07D241/28 ,  A61K31/495 ,  A61K31/50 ,  A61K31/505 ,  A61K31/53 ,  C07D237/04 ,  C07D237/06 ,  C07D239/20 ,  C07D239/24 ,  C07D253/06 ,  C07D253/065

CPC classification number: C07D239/36 ,  C07D237/24 ,  C07D241/24 ,  C07D253/07 ,  C07D253/075

Abstract: Nitrogen-containing heterocyclic carboxamide derivatives represented by the following general formula: wherein ring A is a substituted or unsubstituted pyrazine, pyrimidine, pyridazine or triazine ring; R1 is O or OH; R2 is a hydrogen atom, an acyl group or a substituted or unsubstituted carbamoylalkyl or carboxyalkyl group; and the broken line represents a single bond or a double bond; or salts thereof are useful for preventing and treating virus infections and especially influenza virus infections.

Abstract translation: 由以下通式表示的含氮杂环甲酰胺衍生物：其中环A为取代或未取代的吡嗪，嘧啶，哒嗪或三嗪环; R1是O或OH; R2是氢原子，酰基或取代或未取代的氨基甲酰基烷基或羧基烷基; 虚线表示单键或双键; 或其盐可用于预防和治疗病毒感染，特别是流感病毒感染。