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公开(公告)号：US20230020507A1
公开(公告)日：2023-01-19
申请号：US17766135
申请日：2020-09-29
Applicant: PARENCHYMA BIOTECH INC.
Inventor： Su Kil SEO , Won Hee JANG , Soung Min LEE , Eun Hye YOON , Ha Young PARK , Chae Eun KIM
IPC: C07D403/00 , C07D417/12 , C07D209/14 , A61P1/00 , A61P37/06 , A61P35/00
Abstract: A compound according to an embodiment is represented by Formula 1. The compound may be used for treatment of autoimmune diseases. A composition for treatment or prevention of autoimmune diseases includes the compound and is expected to not only control inflammation but also recover immune balance as well as damaged tissues, thereby restoring bowel tissue homeostasis.
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公开(公告)号：US09790210B2
公开(公告)日：2017-10-17
申请号：US14442604
申请日：2013-11-12
Applicant: Array BioPharma Inc.
Inventor： Steven Wade Andrews , James F. Blake , Barbara J. Brandhuber , Timothy Kercher , Shannon L. Winski
IPC: C07D231/00 , C07D403/00 , C07D401/00 , C07D211/72 , C07D413/00 , C07D405/12 , C07D403/12 , C07D401/14 , C07D231/40 , C07D231/44 , C07D401/04 , C07D413/12 , C07D231/52 , C07D401/12 , C07D405/04 , A61K31/4155
CPC classification number: C07D405/12 , A61K31/4155 , C07D231/40 , C07D231/44 , C07D231/52 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D413/12
Abstract: Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
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公开(公告)号：US09730936B2
公开(公告)日：2017-08-15
申请号：US14998042
申请日：2015-12-23
Applicant: Gilead Sciences, Inc. , Institute of Organic Chemistry and Biochemistry of the AS CR, v.v.i.
Inventor： Ond{hacek over (r)}ej Baszczy{hacek over (n)}ski , Milan Dejmek , Yunfeng Eric Hu , Petr Jansa , Eric Lansdon , Richard L. Mackman , Petr {hacek over (S)}imon
IPC: A01N43/54 , A61K31/517 , C07D401/00 , C07D403/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D401/12 , C07D239/94 , A61K45/06 , C07D239/84 , C07D239/95 , C07D403/12
CPC classification number: A61K31/517 , A61K45/06 , C07D239/84 , C07D239/94 , C07D239/95 , C07D401/12 , C07D403/12
Abstract: Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds.
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公开(公告)号：US09650374B2
公开(公告)日：2017-05-16
申请号：US14400656
申请日：2014-10-29
Applicant: UMM AL-QURA UNIVERSITY
Inventor： Saleh Abdel-Mgeed Ahmed Saleh , Mohamed Mokhtar Mohamed Abdalla , Khalid Soliman Khalil Khairou
IPC: G02B5/23 , C07D471/04 , C07D217/04 , C07D401/04 , G02F1/01 , C07D471/10 , C09B57/00 , G03C1/685 , G02F1/03 , G02F1/07 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00
CPC classification number: C07D471/04 , C07D217/04 , C07D401/04 , C07D471/10 , C09B23/0091 , C09B57/00 , C09B69/105 , C09B69/109 , G02F1/0126 , G03C1/685
Abstract: Photochromic tetrahydroindolizines (THIs) bearing dihydroisoquinoline derivatives as heterocyclic bases and central fluorene groups have been synthesized via different chemical and photochemical pathways. Three alternative pathways for the synthesis of the target photochromic THI-based pyridazinopyrrolo[1,2-b]isoquinolines via in situ trapping with hydrazine hydrate are also provided. High product yields are obtained using different Sonogashira-mediated coupling reactions provided herein. Low temperature multichannel UV-vis and flash photolysis techniques were used to detect the photochromic and kinetic properties of the synthesized system.
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公开(公告)号：US09630947B2
公开(公告)日：2017-04-25
申请号：US14692434
申请日：2015-04-21
Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
Inventor： Masaki Suzuki , Kazumi Kondo , Muneaki Kurimura , Krishna Reddy Valluru , Akira Takahashi , Takeshi Kuroda , Haruka Takahashi , Tae Fukushima , Shin Miyamura , Indranath Ghosh , Abhishek Dogra , Geraldine Harriman , Amy Elder , Satoshi Shimizu , Kevin J. Hodgetts , Jason S. Newcom
IPC: A01N43/54 , A61K31/517 , C07D401/00 , C07D403/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D401/14 , C07D401/04 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D495/04 , A61K45/06
CPC classification number: C07D401/04 , A61K31/517 , A61K45/06 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D495/04
Abstract: Methods of treating disorders using compounds that modulate striatal-enriched tyrosine phosphatase (STEP), such as those of formula (III), and composition thereof are described herein. Exemplary disorders include schizophrenia and cognitive deficit.
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公开(公告)号：US09624174B2
公开(公告)日：2017-04-18
申请号：US14943091
申请日：2015-11-17
Applicant: GlaxoSmithKline LLC
Inventor： Mui Cheung , Raghuram S. Tangirala
IPC: A61K31/50 , A61K31/501 , A61K31/4965 , A01N43/40 , A61K31/44 , A01N43/78 , A61K31/425 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D213/04 , C07D277/00 , C07D213/72 , A61K31/122 , C07D237/20 , C07D213/74 , C07D277/42 , C07D401/12 , C07D405/12 , C07D417/12
CPC classification number: C07D213/72 , A61K31/122 , A61K31/50 , C07D213/74 , C07D237/20 , C07D277/42 , C07D401/12 , C07D405/12 , C07D417/12
Abstract: Compounds of Formula (I) are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), useful in the treatment of obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as mycocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.
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公开(公告)号：US09434693B2
公开(公告)日：2016-09-06
申请号：US13968465
申请日：2013-08-16
Applicant: Janssen Pharmaceutica NV
Inventor： Mark Wall , Nalin Subasinghe , Zhihua Sui , Christopher Flores
IPC: A61K31/00 , A61K31/415 , A61K31/445 , A61K31/42 , C07D401/00 , C07D231/00 , C07D403/00 , C07D403/02 , C07D261/00 , C07D413/00 , C07D231/22 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/14
CPC classification number: C07D231/22 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/14
Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, ring A, and G are defined herein.
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公开(公告)号：US09376402B2
公开(公告)日：2016-06-28
申请号：US14493972
申请日：2014-09-23
Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
Inventor： Dhiman Sarkar , Sunita Ranjan Deshpande , Shailaja Pramod Maybhate , Anjali Prabhakar Likhite , Sampa Sarkar , Arshad Khan , Preeti Madhukar Chaudhary , Sayalee Ramchandra Chavan
IPC: C07D403/00 , C07D249/12 , C07D249/08 , C07D403/14 , C07D249/06
CPC classification number: C07D249/12 , C07D249/06 , C07D249/08 , C07D403/14
Abstract: Triazole derivatives useful as anti-tubercular compounds; process for preparation of the triazoles and a method for inhibiting growth of Mycobacterium bovis BCG and Mycobacterium tuberculosis H37Ra using the triazoles.
Abstract translation: 用作抗结核化合物的三唑衍生物; 制备三唑的方法和使用三唑抑制牛分枝杆菌BCG和结核分枝杆菌H37Ra生长的方法。
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公开(公告)号：US09315498B2
公开(公告)日：2016-04-19
申请号：US14085064
申请日：2013-11-20
Applicant: Hoffmann-La Roche Inc.
Inventor： Luke Green , Wolfgang Guba , Georg Jaeschke , Synese Jolidon , Lothar Lindemann , Antonio Ricci , Daniel Rueher , Heinz Stadler , Eric Vieira
IPC: A61K31/50 , A61K31/501 , A61K31/4965 , A61K31/505 , A61K31/44 , C07D401/04 , C07D401/14 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D239/02 , C07D471/04 , C07D403/04 , C07D413/04 , C07D413/14 , C07D498/04 , C07D491/107 , C07D241/02 , C07D241/00
CPC classification number: C07D471/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/14 , C07D491/107 , C07D498/04
Abstract: The present invention relates to ethynyl compounds of formula I-C1 wherein R1, R2, R2′, R3, R3′, R6, U, V and W are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof, which are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
Abstract translation: 本发明涉及式I-C1的炔基化合物，其中R 1，R 2，R 2'，R 3，R 3'，R 6，U，V和W如本文所定义，并且涉及药学上可接受的酸加成盐， 或其相应的对映异构体和/或光学异构体和/或立体异构体，其是代谢型谷氨酸受体亚型5（mGluR5）的变构调节剂。
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公开(公告)号：US09309273B2
公开(公告)日：2016-04-12
申请号：US14364276
申请日：2012-12-10
Applicant: Viamet Pharmaceuticals, Inc.
Inventor： William J. Hoekstra , Christopher M. Yates
IPC: A61K31/675 , A61K31/535 , A61K31/50 , A61K31/501 , A61K31/4965 , A61K31/445 , A61K31/44 , A61K31/41 , C07D413/00 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D417/00 , C07D419/00 , C07F9/06 , C07F9/28 , C07D211/68 , C07D211/80 , C07D213/02 , C07D421/00 , C07D257/00 , A61K31/4439 , C07D401/06 , C07D409/14 , C07D401/14 , C07D405/14 , C07D413/14 , C07D403/06 , C07D403/14 , C07D409/06 , C07D417/14 , A01N43/713 , A01N43/84 , A01N57/16
CPC classification number: C07D401/06 , A01N43/713 , A01N43/84 , A01N57/16 , A61K31/4439 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07F9/06 , C07F9/65583 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/415
Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
