公开(公告)号：US20250011333A1

公开(公告)日：2025-01-09

申请号：US18394122

申请日：2023-12-22

Applicant: Nerviano Medical Sciences S. R. L.

Inventor： Gabriella TRAQUANDI ,  Maria Gabriella Brasca ,  Roberto D'Alessio ,  Paolo Polucci ,  Fulvia Roletto ,  Anna Vulpetti ,  Palolo Pevarello ,  Achille Panzeri ,  Francesca Quartieri ,  Ron Ferguson ,  Paola Vianello ,  Daniele Fancelli

IPC: C07D487/14 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  C07D231/56 ,  C07D239/72 ,  C07D401/10 ,  C07D403/14 ,  C07D413/14 ,  C07D487/04

Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

公开(公告)号：US12049461B2

公开(公告)日：2024-07-30

申请号：US16950654

申请日：2020-11-17

Applicant: Gilead Sciences, Inc.

Inventor： Ling-Jie Gao ,  Piet Andre Maurits Maria Herdewijn ,  Steven Cesar Alfons De Jonghe ,  William John Watkins ,  Lee Shun Chong

IPC: A61K31/517 ,  A61K31/5375 ,  A61K31/5377 ,  A61P31/14 ,  C07D239/72 ,  C07D239/78 ,  C07D239/86 ,  C07D239/88 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04

CPC classification number: C07D413/04 ,  A61K31/517 ,  A61K31/5375 ,  A61K31/5377 ,  A61P31/14 ,  C07D239/72 ,  C07D239/78 ,  C07D239/86 ,  C07D239/88 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04

Abstract: This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R2 is hydrogen, NR′R″, C1-7alkyl, arylC1-7 alkyl or C3-10 cycloalkyl; R4 is amino, C1-7alkyl, C2-7 alkenyl, C3-10 cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C1-7alkyl or C3-10 cycloalkyl-C1-7 alkyl; R5 is hydrogen or C1-7 alkyl, or R5 and R4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C1-7alkylene, C2-7 alkenylene or C2-7 alkynylene; R6 is halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, C1-7 alkyl-carbonyl or C1-7 alkyl; provided that R4 is not phenyl substituted with morpholino when R2 is H and R5 is H, and provided that when NR4R5 is piperazinyl, said NR4R5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

公开(公告)号：US11008339B2

公开(公告)日：2021-05-18

申请号：US15568561

申请日：2016-05-17

Applicant: Shenyang Sinochem Agrochemicals R&D Co., Ltd.

Inventor： Changling Liu ,  Aiying Guan ,  Junfeng Wang ,  Xufeng Sun ,  Zhinian Li ,  Jinbo Zhang ,  Lanfeng Ban ,  Sen Ma ,  Jie Lan ,  Xiaoli Xia ,  Jinlong Yang

IPC: C07D513/04 ,  C07D403/12 ,  A01N43/54 ,  C07D495/04 ,  C07D417/14 ,  C07D401/14 ,  A01N43/56 ,  C07D239/72 ,  C07D403/14 ,  C07D409/14 ,  C07D487/04 ,  C07D498/04

Abstract: Disclosed are substituted pyrazole compounds containing pyrimidinyl as shown in Formula I: The definitions of each of the substituents can be seen in the description. The compounds of present invention have a good spectrum of bactericidal, insecticidal and acaricidal activity, and have good control effect on downy mildew of cucumber, powdery mildew of wheat, corn rust, rice blast, cucumber anthracnosis and the like. The compounds of present invention also show good insecticidal activity.

公开(公告)号：US10167296B2

公开(公告)日：2019-01-01

申请号：US15308712

申请日：2015-04-30

Applicant: EVOTEC INTERNATIONAL GMBH

Inventor： Andreas Blum

IPC: C07D493/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D239/72 ,  C07D413/12 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D239/94

Abstract: The application relates to novel sulfoximine substituted quinazoline derivatives of formula wherein Ar, R1, R2 and R3 are as defined in the description and claims, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.

公开(公告)号：US20180141961A1

公开(公告)日：2018-05-24

申请号：US15568561

申请日：2016-05-17

Applicant: Shenyang Sinochem Agrochemicals R&D Co., Ltd.

Inventor： Changling Liu ,  Aiying Guan ,  Junfeng Wang ,  Xufeng Sun ,  Zhinian Li ,  Jinbo Zhang ,  Lanfeng Ban ,  Sen Ma ,  Jie Lan ,  Xiaoli Xia ,  Jinlong Yang

IPC: C07D513/04 ,  C07D498/04 ,  C07D495/04 ,  C07D487/04 ,  C07D409/14 ,  C07D403/14 ,  C07D403/12 ,  C07D239/72 ,  A01N43/56 ,  A01N43/54

CPC classification number: C07D513/04 ,  A01N43/54 ,  A01N43/56 ,  C07D239/72 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04

Abstract: Disclosed are substituted pyrazole compounds containing pyrimidinyl as shown in Formula I: The definitions of each of the substituents can be seen in the description. The compounds of present invention have a good spectrum of bactericidal, insecticidal and acaricidal activity,and have good control effect on downy mildew of cucumber, powdery mildew of wheat, corn rust, rice blast, cucumber anthracnosis and the like. The compounds of present invention also show good insecticidal activity.

公开(公告)号：US09878992B2

公开(公告)日：2018-01-30

申请号：US15366981

申请日：2017-07-13

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Somasekhar Bhamidipati ,  Marina Gelman ,  Pingyu Ding ,  Rajinder Singh ,  Jeffrey Clough ,  Todd Kinsella ,  Donald Payan

IPC: C07D239/72 ,  C07D401/04 ,  C07D498/04 ,  C07D213/26 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D417/04 ,  C07D405/04 ,  C07F9/6503 ,  C07D487/04 ,  C07D453/02 ,  C07D417/14 ,  C07D413/04 ,  C07D513/04

CPC classification number: C07D401/04 ,  C07D213/26 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D453/02 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07F9/65038

Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.

公开(公告)号：US09676755B2

公开(公告)日：2017-06-13

申请号：US14402560

申请日：2013-05-13

Applicant: BASF SE ,  EMPA—EIDGENOESSISCHE MATERIALPRUEFUNGS- UND FORSCHUNGSANSTALT ,  MAX-PLANCK-GESELLSCHAFT ZUR FOERDERUNG DER WISSENSCHAFTEN E.V.

Inventor： Roman Fasel ,  Pascal Ruffieux ,  Klaus Muellen ,  Jinming Cai ,  Xinliang Feng ,  Reinhard Berger

IPC: C07D403/10 ,  C01B31/04 ,  C07D215/18 ,  C07D237/26 ,  C07D239/72 ,  C07D209/56 ,  B82Y30/00 ,  B82Y40/00

CPC classification number: C07D403/10 ,  B82Y30/00 ,  B82Y40/00 ,  C01B32/182 ,  C01B32/184 ,  C01B2204/06 ,  C01B2204/065 ,  C07D209/56 ,  C07D215/18 ,  C07D237/26 ,  C07D239/72

Abstract: The present invention relates to a graphene nanoribbon, comprising a repeating unit which comprises at least one modification, wherein the modification is selected from a heteroatomic substitution, a vacancy, a sp3 hybridization, a Stone-Wales defect, an inverse Stone-Wales defect, a hexagonal sp2 hybridized carbon network ring size modification, and any combination thereof.

公开(公告)号：US09381198B2

公开(公告)日：2016-07-05

申请号：US14670782

申请日：2015-03-27

Applicant: BioVascular, Inc.

Inventor： Paul F. Glidden ,  Alison J. Pilgrim ,  Stephen R. Hanson

IPC: A61K31/519 ,  C07D239/72 ,  A61K9/48 ,  A61K9/50 ,  A61K31/00 ,  A61L27/02 ,  A61L27/20 ,  A61L27/22 ,  A61L27/34 ,  A61L27/54 ,  A61L27/56 ,  C07D487/04

CPC classification number: A61K9/1676 ,  A61K9/0053 ,  A61K9/1617 ,  A61K9/1652 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/2081 ,  A61K9/4808 ,  A61K9/4858 ,  A61K9/4866 ,  A61K9/5078 ,  A61K31/00 ,  A61K31/519 ,  A61L27/025 ,  A61L27/20 ,  A61L27/227 ,  A61L27/34 ,  A61L27/54 ,  A61L27/56 ,  A61L2300/42 ,  A61L2300/602 ,  A61L2300/608 ,  A61L2300/622 ,  A61L2300/63 ,  A61L2420/08 ,  C07D239/72 ,  C07D487/04 ,  C08L3/04 ,  C08L1/02

Abstract: Provided are prophylactic and therapeutic methods of treatment of subjects for the purpose of inhibiting vaso-occlusive events, including embolism, by administering agents, including anagrelide and anagrelide derivatives, which reduce the number of circulating platelets to low normal or to below normal levels. Methods and pharmaceutical preparations comprising such agents are provided.

公开(公告)号：US09365516B2

公开(公告)日：2016-06-14

申请号：US14353251

申请日：2012-10-22

Applicant: Exelixis, Inc.

Inventor： Jo Ann Wilson ,  Sriram Naganathan ,  Neil G. Andersen ,  Matthew Pfeiffer

IPC: C07D239/72 ,  C07D215/00 ,  C07D215/233 ,  C07D239/90 ,  C07C231/02

CPC classification number: C07D215/233 ,  C07C231/02 ,  C07C233/58 ,  C07C233/59 ,  C07D215/00 ,  C07D239/90

Abstract: A process for preparing a compound of Formula I is disclosed: wherein: R1 is halo; R2 is halo; R3 is (C1-C6)alkyl or (C1-C6)alkyl optionally substituted with heterocycloalkyl; R4 is (C1-C6)alkyl; and Q is CH or N; comprising: (a) contacting 1,1-cyclopropane dicarboxylic acid with thionyl chloride in a polar aprotic solvent; (b) adding and a tertiary amine base to the mixture of step (a) to form a compound of Formula A; and (c) coupling a compound of Formula A with an amine of Formula B to form a compound of Formula I.

Abstract translation: 公开了制备式I化合物的方法：其中：R1为卤素; R2是卤素; R 3是（C 1 -C 6）烷基或任选被杂环烷基取代的（C 1 -C 6）烷基; R4是（C1-C6）烷基; Q为CH或N; 包括：（a）在极性非质子溶剂中将1,1-环丙烷二羧酸与亚硫酰氯接触; （b）向步骤（a）的混合物中加入叔胺碱，形成式A的化合物; 和（c）将式A的化合物与式B的胺偶联以形成式I的化合物。

公开(公告)号：US09187459B2

公开(公告)日：2015-11-17

申请号：US14118200

申请日：2012-05-17

Applicant: Wang Shen ,  Wei Xiao ,  Jack Maung ,  Aimin Zhang ,  Xiaoling Zheng ,  Zhenzhong Wang ,  Qingming Guo ,  Yingguang Li

Inventor： Wang Shen ,  Wei Xiao ,  Jack Maung ,  Aimin Zhang ,  Xiaoling Zheng ,  Zhenzhong Wang ,  Qingming Guo ,  Yingguang Li

IPC: A01N43/54 ,  A61K31/517 ,  C07D401/00 ,  C07D239/72 ,  C07D405/12 ,  C07D493/04

CPC classification number: C07D405/12 ,  C07D493/04

Abstract: The invention provides quinazoline-7-ether derivatives, particularly 4-anilinyl-6-butenamido-quinazoline-7-ether derivatives that are inhibitors of the receptor protein tyrosine kinases (RTK). The compounds are useful in the treatment of diseases and disorders where RTK activity is implicated such as a hyperproliferative diseases (e.g., cancer). Also provided are methods of preparation of the quinazoline derivatives and methods of use as therapeutic agents alone or in a drug combination.

Abstract translation: 本发明提供了喹唑啉-7-醚衍生物，特别是作为受体蛋白酪氨酸激酶（RTK）抑制剂的4-苯乙烯基-6-丁烯酰氨基 - 喹唑啉-7-醚衍生物。 所述化合物可用于治疗涉及RTK活性的疾病和病症，例如过度增殖性疾病（例如癌症）。 还提供了制备喹唑啉衍生物的方法和单独使用或作为药物组合用作治疗剂的方法。