Three Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/278)
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Patent number: 12075770Abstract: Method for pest treatment of a plantation field, controlling device for controlling a pest treatment of a plantation field and a treatment device having said controlling device, wherein the treatment considers a pest insect population and a beneficial insect population.Type: GrantFiled: March 25, 2020Date of Patent: September 3, 2024Assignee: BASF Agro Trademarks GmbHInventors: Ole Janssen, Bjoern Kiepe, Mirwaes Wahabzada, Andreas Johnen
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Patent number: 11980621Abstract: The invention provides methods of treating endometriosis in a patient by administration of a gonadotropin-releasing hormone (GnRH) antagonist, for instance, according to dosing regimens predicated on the patient's level of anti-Müllerian hormone (AMH) or ?17-estradiol (E2).Type: GrantFiled: June 5, 2018Date of Patent: May 14, 2024Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Ernest Loumaye, Jean-Pierre Gotteland
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Patent number: 11730742Abstract: Disclosed is use of a thieno[3,2-d]pyrimidin-4-one compound represented by general formula (I). Definition of each substituent is as stated in the description and claims, and the compound is used for preparing medicines for treating and/or preventing liver fibrosis and related diseases or preparing a DPP-4 inhibitor, or is used as a DPP-4 inhibitor.Type: GrantFiled: March 8, 2019Date of Patent: August 22, 2023Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCESInventors: Hong Liu, Jia Li, Jiang Wang, Yi Zang, Jian Li, Jingya Li, Dandan Sun, Hualiang Jiang, Kaixian Chen
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Patent number: 11673898Abstract: The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins with compositions of Formula (II-A). The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions of Formula (II-A) for use in these methods are also provided.Type: GrantFiled: July 30, 2020Date of Patent: June 13, 2023Assignees: KURA ONCOLOGY, INC., THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Tao Wu, Liansheng Li, Yi Wang, Pingda Ren, Jolanta Grembecka, Tomasz Cierpicki, Szymon Klossowski, Jonathan Pollock, Dmitry Borkin
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Patent number: 11649251Abstract: The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions for use in these methods are also provided.Type: GrantFiled: September 19, 2018Date of Patent: May 16, 2023Assignee: KURA ONCOLOGY, INC.Inventors: Tao Wu, Liansheng Li, Pingda Ren
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Patent number: 11571431Abstract: The present invention relates to salts of arachidyl amido cholanoic acid (Aramchol), pharmaceutical compositions comprising Aramchol salts, methods for their preparation, and methods of use thereof in medical treatment.Type: GrantFiled: October 24, 2021Date of Patent: February 7, 2023Assignee: Galmed Research and Development LtdInventors: Allen Baharaff, Idit Eshkar-Oren
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Patent number: 11560389Abstract: The invention provides compounds of formulae A, B, and C as described herein that inhibit monocarboxylate transporters, such as MCT1 and MCT4. Compounds of the invention can be used for treatment of a condition in a patient, wherein the condition is characterized by the heightened activity or by the high prevalence of MCT1 and/or MCT4, such as cancer or type II diabetes.Type: GrantFiled: November 23, 2020Date of Patent: January 24, 2023Assignee: University of Florida Research Foundation, IncorporatedInventors: Thomas D. Bannister, William R. Roush, John L. Cleveland, Jun Yong Choi, Reji N. Nair, Andy S. Tsai, Jitendra K. Mishra
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Patent number: 11555041Abstract: The present disclosure provides compounds of Formula (I-A) for inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The compounds are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.Type: GrantFiled: July 13, 2020Date of Patent: January 17, 2023Assignees: KURA ONCOLOGY, INC., THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Tao Wu, Liansheng Li, Yi Wang, Pingda Ren, Jolanta Grembecka, Tomasz Cierpicki, Szymon Klossowski, Jonathan Pollock, Dmitry Borkin
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Patent number: 11492357Abstract: The present invention relates to a compound, 4-amino-N-(1-((3-chloro-2-fluoro-4-hydroxyphenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide, and pharmaceutically acceptable salts thereof having inhibitory activity for protein kinases.Type: GrantFiled: November 29, 2018Date of Patent: November 8, 2022Assignee: Hanmi Pharm. Co., Ltd.Inventors: In Hwan Bae, Seung Hyun Jung, Young Gil Ahn, Kwee Hyun Suh
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Patent number: 11254686Abstract: Disclosed herein, inter alia, are certain substituted thieno[3,2-b]pyrimidine compositions and methods for modulating Adenosine Receptors, for example, having the formula:Type: GrantFiled: August 31, 2018Date of Patent: February 22, 2022Assignee: Corvus Pharmaceuticals, Inc.Inventors: Zhihong Li, Lubov Konstantinovna Filonova, Erin Kathleen Bradley, Erik Verner
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Patent number: 11078213Abstract: The present invention relates to thienopyrimidine compound, preparation method thereof, pharmaceutical composition and use thereof, and in particular to a type of compounds having ALK and/or c-Met selective inhibitory activity, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for preventing or treating a disease associated with anaplastic lymphoma kinase in vivo, and in the manufacture of a medicament for preventing or treating a disease associated with angiogenesis or cancer metastasis, in particular in the manufacture of a medicament for preventing or treating tumor growth and metastasis.Type: GrantFiled: September 28, 2017Date of Patent: August 3, 2021Assignee: HONGYUN BIOTECH CO., LTD.Inventors: Xianming Deng, Baoding Zhang, Shuang Liu, Chao Dong, Xihuan Sun, Xiaoxing Huang, Zhou Deng, Yunzhan Li, Yue Lu, Li Li, Zhiyu Hu
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Patent number: 11053256Abstract: This invention relates to dihydropyranopynmidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.Type: GrantFiled: June 30, 2017Date of Patent: July 6, 2021Assignee: Janssen Sciences Ireland Unlimited CompanyInventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Jérôme Émile Georges Guillemont, David Craig McGowan, Werner Constant Johan Embrechts, Ludwig Paul Cooymans, Laurent Calmus
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Patent number: 10995099Abstract: The present invention provides compounds of Formula (I) which can be used as ACC inhibitors and potently as therapeutic agents against diseases mediated by ACC.Type: GrantFiled: July 17, 2018Date of Patent: May 4, 2021Assignee: Nanjing Ruijie Pharmatech Co., Ltd.Inventors: Junbo Zhang, Hong Liao, Peipei Wang, Peng Wang
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Patent number: 10975100Abstract: The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to fused bicyclic compounds, pharmaceutical composition comprising such compounds, and their use as menin/MLL protein/protein interaction inhibitors, useful for treating diseases such as cancer, myelodysplastic syndrome (MDS) and diabetes.Type: GrantFiled: February 13, 2020Date of Patent: April 13, 2021Assignee: Janssen Pharmaceutica NVInventors: Patrick Rene Angibaud, Vineet Pande, Barbara Herkert, Daniel Jason Krosky, Olivier Alexis Georges Querolle, Aaron Nathaniel Patrick
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Patent number: 10646491Abstract: An object of the present invention is to provide pharmaceutical agents that reduce risk for decrease in bone mineral density due to their effect of reducing estrogen levels and exert excellent therapeutic effects on endometriosis. The present invention relates to pharmaceutical compositions for treating endometriosis comprising 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid or a pharmaceutically acceptable salt thereof, which are administered orally once a day at a daily dose of between 50 mg and 75 mg calculated as a free form.Type: GrantFiled: August 7, 2017Date of Patent: May 12, 2020Assignee: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Takuro Dan, Hideomi Takahashi, Yu Kuramochi
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Patent number: 10611767Abstract: Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula I: These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.Type: GrantFiled: June 6, 2018Date of Patent: April 7, 2020Assignees: Duquesne University of the Holy Spirit, Wayne State UniversityInventors: Aleem Gangjee, Larry H. Matherly
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Patent number: 10611778Abstract: The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to fused bicyclic compounds, pharmaceutical composition comprising such compounds, and their use as menin/MLL protein/protein interaction inhibitors, useful for treating diseases such as cancer, myelodysplastic syndrome (MDS) and diabetes.Type: GrantFiled: September 13, 2017Date of Patent: April 7, 2020Assignee: Janssen Pharmaceutica NVInventors: Patrick Rene Angibaud, Vineet Pande, Barbara Herkert, Daniel Jason Krosky, Olivier Alexis Georges Querolle, Aaron Nathaniel Patrick
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Patent number: 10576084Abstract: The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt having excellent solubility and storage stability.Type: GrantFiled: June 27, 2018Date of Patent: March 3, 2020Assignee: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazumichi Jo, Hideki Takeuchi
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Patent number: 10561658Abstract: The present invention provides for the design and synthesis of halogenated thieno- and pyrrolopyrimidine compounds that exhibit cancer proliferation inhibitory activity and the use thereof for cancer treatment.Type: GrantFiled: February 12, 2018Date of Patent: February 18, 2020Assignee: UNIVERSITY OF MARYLAND, BALTIMORE COUNTYInventors: Katherine L. Radtke, Kartik Temburnikar
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Patent number: 10500212Abstract: The present invention relates to compounds of formula (I): wherein R6 is —CONH2 or a —C(R?)(R?)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.Type: GrantFiled: January 10, 2019Date of Patent: December 10, 2019Assignee: SANOFIInventors: Jean-Christophe Carry, Fabienne Chatreaux, Stephanie Deprets, Olivier Duclos, Vincent Leroy, Sergio Mallart, Dominique Melon-Manguer, Maria Mendez-Perez, Fabrice Vergne
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Patent number: 10464946Abstract: The present invention relates to crystalline forms of N-(3-(2-(4-(4-methylpiperazin-1-yl)phenylamino)thieno[3,2-d]pyrimidin-4-yloxy)phenyl)acrylamide, and pharmaceutical compositions containing the same. The crystalline forms can be easily used for the preparation of a pharmaceutical composition containing the same as an active ingredient.Type: GrantFiled: December 30, 2016Date of Patent: November 5, 2019Assignee: HANMI PHARM. CO., LTD.Inventors: Jae Hyuk Jung, Jong Ouk Baek, Sun Young Jung, Eun Joo Kwak, Hee Cheol Kim, Tae Hee Ha
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Patent number: 10336765Abstract: The present invention relates to a novel dihydropyranopyrimidinone derivative, a tautomer thereof, a stereoisomer thereof and their mixture, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating a tankyrase-related disease, which contains the same as an active ingredient.Type: GrantFiled: December 1, 2016Date of Patent: July 2, 2019Assignee: ST. PHARM CO., LTD.Inventors: Kyungjin Kim, Uk-Il Kim, Ji Hye Yoon
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Patent number: 10183950Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.Type: GrantFiled: January 26, 2017Date of Patent: January 22, 2019Assignee: Cancer Research Technology LimitedInventors: Bruce D. Dorsey, Keith S. Learn, Emma L. Morris, Gregory R. Ott, Jonathan R. A. Roffey, Christelle N. Soudy, Jason C. Wagner
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Patent number: 10087195Abstract: Provided are compound of formula (I) as certain CDK4/6 inhibitors, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: May 27, 2015Date of Patent: October 2, 2018Assignees: SHANGHAI FOCHON PHARMACEUTICAL CO., LTD., CHONGQING FOCHON PHARMACEUTICAL CO., LTD.Inventors: Weibo Wang, Xingdong Zhao, Tongshuang Li, Qiang Tian, Huajie Zhang, Haohan Tan, Xianlong Wang, Qihong Liu, Zhifu Li, Weipeng Zhang, Zhifang Chen, Lihua Jiang, Yanxin Liu, Li Linghu, Min Lin, Jing Sun
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Patent number: 10016433Abstract: The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt having excellent solubility and storage stability.Type: GrantFiled: July 12, 2017Date of Patent: July 10, 2018Assignee: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazumichi Jo, Hideki Takeuchi
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Patent number: 10000498Abstract: Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula I: These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.Type: GrantFiled: November 3, 2016Date of Patent: June 19, 2018Assignee: Duquesne University of the Holy SpiritInventors: Aleem Gangjee, Larry H. Matherly
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Patent number: 9988399Abstract: The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.Type: GrantFiled: May 8, 2014Date of Patent: June 5, 2018Assignee: Gilead Apollo, LLCInventors: Jeremy Robert Greenwood, Geraldine C. Harriman, George Borg, Craig E. Masse
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Patent number: 9890168Abstract: The present invention relates to a 2,4-disubstituted 7H-pyrrolo[2,3-d]pyrimidine derivative, a preparation method and a medicinal use thereof. In particular, the present invention discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. For the definition of each group in formula (I), see the description tbr details.Type: GrantFiled: July 24, 2015Date of Patent: February 13, 2018Assignees: Shanghai Haiyan Pharmaceutical Technology Co., Ltd., Yangtze River Pharmaceutical Group Co., Ltd.Inventors: Jiong Lan, Yunzhou Jin, Fusheng Zhou, Jing Lei, Chong Wen, Zhiyuan Zhang, Xiangyu He
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Patent number: 9737539Abstract: The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt having excellent solubility and storage stability.Type: GrantFiled: September 28, 2015Date of Patent: August 22, 2017Assignee: KISSEI PHARMACEUTICALS CO., LTD.Inventors: Kazumichi Jo, Hideki Takeuchi
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Patent number: 9732090Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.Type: GrantFiled: September 21, 2015Date of Patent: August 15, 2017Assignee: Duquesne University of the Holy GhostInventor: Aleem Gangjee
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Patent number: 9642852Abstract: A sulfur-containing bicyclic compound of the present invention has a PAM action of GABAB. A composition containing the sulfur-containing bicyclic compound. And, a method for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease by administering the sulfur-containing bicyclic compound.Type: GrantFiled: April 17, 2015Date of Patent: May 9, 2017Assignee: Astellas Pharma Inc.Inventors: Nobuyuki Shiraishi, Hiroaki Hoshii, Wataru Hamaguchi, Eriko Honjo, Tomofumi Takuwa, Yuji Kondo, Takayuki Goto
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Patent number: 9586928Abstract: The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as ROR?, ROR?, or ROR?, of formula with the variable atoms as defined herein and R1 comprising a hydroxyl- or alkoxyl-substituted fluoroalkyl group. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.Type: GrantFiled: May 16, 2012Date of Patent: March 7, 2017Assignee: The Scripps Research InstituteInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Youseung Shin, Yuanjun He, Anne-Laure Blayo, Brent R. Lyda, Marcel Koenig, Naresh Kumar, Thomas Burris
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Patent number: 9540392Abstract: The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: GrantFiled: May 17, 2013Date of Patent: January 10, 2017Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Georg Kettschau, Florian Puehler, Knut Eis, Ulrich Klar, Dirk Kosemund, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Ulf Bömer, Lars Wortmann, Keith Graham, Antje Margret Wengner
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Patent number: 9422307Abstract: A substituted thieno pyrimidine compound of Formula 1, pharmaceutically acceptable salts and a pharmaceutical composition thereof is provided. The compound of Formula 1 exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction. The compound of Formula 1 and its compositions are useful for the prevention and treatment of diseases caused by abnormal cell growth including cancer.Type: GrantFiled: October 22, 2010Date of Patent: August 23, 2016Assignee: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Tae Bo Sim, Jung Mi Hah, Hwan Geun Choi, Young Jin Ham, Jung Hun Lee, Dong Sik Park, Hwan Kim
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Patent number: 9271979Abstract: The present invention is concerned with deuterium-enriched pyrimidine compounds of formula 1, their derivatives and pharmaceutically acceptable salts and methods of use thereof for the prevention and treatment of neuroendocrine neoplasia including metastasis and fibrosis, fibrotic processes associated with neuroendocrine cell dysregulation for example Crohn's disease, pulmonary arterial hypertension, pulmonary hypertension associated with chronic obstructive pulmonary disease (COPD), right ventricular hypertrophy, pulmonary vascular remodeling, asthma, cystic fibrosis, hypertension, ischemic stroke, angina pectoris, congestive heart failure, arrhythmia, arterial fibrillation, neurodenerative diseases, gastrointestinal disorders , stress disorders, obsessive compulsive disorders, demyelinating diseases, cereberal vascular disorders, bronchoconstriction, vasodilation, smooth muscle contraction, brain disorders, vascular disorders, neuropathological diseases and cardiovascular system regulation.Type: GrantFiled: September 14, 2011Date of Patent: March 1, 2016Inventor: Daljit Singh Dhanoa
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Patent number: 9169266Abstract: An objective of the present invention is to improve the solubility of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid. The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt has excellent solubility and storage stability.Type: GrantFiled: February 9, 2011Date of Patent: October 27, 2015Assignee: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazumichi Jo, Hideki Takeuchi
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Patent number: 9156852Abstract: Provided are a thieno[3,2-d]pyrimidine derivative of formula (I) or a pharmaceutically acceptable salt thereof having inhibitory activity for protein kinase, and a pharmaceutical composition comprising same for prevention and treatment of abnormal cell growth diseases.Type: GrantFiled: December 27, 2012Date of Patent: October 13, 2015Assignee: HANMI PHARM. CO., LTDInventors: In Hwan Bae, Jung Beom Son, Sang Mi Han, Eun Joo Kwak, Ho Seok Kim, Ji Young Song, Eun Young Byun, Seung Ah Jun, Young Gil Ahn, Kwee Hyun Suh
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Patent number: 9139590Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.Type: GrantFiled: February 2, 2012Date of Patent: September 22, 2015Assignee: Duquesne University of the Holy SpiritInventor: Aleem Gangjee
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Patent number: 9133209Abstract: The compounds of general formula I, wherein X, R1, R2, R3 and A are defined as in the description, are of the class of 4-amino-thieno[2,3-d]-pyrimidine compounds useful to control pests that damage plants and crops, and parasites that harm animals:Type: GrantFiled: July 29, 2010Date of Patent: September 15, 2015Assignee: MERIAL, INC.Inventors: Mark David Soll, Charles Meng, Matthias Pohlman, Ernst Baumann, Ralph Paulini
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Patent number: 9051339Abstract: A sulfur-containing bicyclic compound having a PAM action of GABAB, and it use for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease. A pharmaceutical composition for preventing and/or treating schizophrenia, cognitive impairment associated with schizophrenia (CIAS), cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, Charcot-Marie-Tooth disease, or the like, which has a positive allosteric modulator (PAM action) of GABAB.Type: GrantFiled: October 17, 2014Date of Patent: June 9, 2015Assignee: Astellas Pharma Inc.Inventors: Nobuyuki Shiraishi, Hiroaki Hoshii, Wataru Hamaguchi, Eriko Honjo, Tomofumi Takuwa, Yuji Kondo, Takayuki Goto
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Patent number: 9045491Abstract: Disclosed are new thienyl [3,2-d] pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.Type: GrantFiled: October 23, 2012Date of Patent: June 2, 2015Assignees: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Cisen Pharmaceutical Co., Ltd.Inventors: Hong Liu, Jia Li, Jian Li, Jingya Li, Jiang Wang, Mingbo Su, Jie Lian, Hualiang Jiang, Kaixian Chen
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Publication number: 20150148322Abstract: The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is Cl and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.Type: ApplicationFiled: March 15, 2012Publication date: May 28, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pascale A.J. Pouzet, Peter Nickolaus, Ulrike Werthmann, Rogelio P. Frutos, Bing-Shiou Yang, Soojin Kim, Jason Alan Mulder, Nitinchandra Patel, Chris H. Senanayake, Thomas G. Tampone, Xudong Wei
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Patent number: 9040693Abstract: The present invention provides a compound useful as an agent for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides a fused heterocyclic derivative represented by the following general formula (I), a pharmaceutical composition containing the same, a medicinal use thereof and the like. In the formula (I), ring A represents 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA represents halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like ; ring B represents aryl or heteroaryl; RB represents halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; E1 and E2 represent an oxygen atom or the like; U represents a single bond or alkylene; X represents a group represented by Y, —SO2—Y, —O—(alkylene)—Y, —O—Z in which Y represents Z, amino or the like; Z represents cycloalkyl, heterocycloalkyl, aryl, heteroaryl or the like; or the like.Type: GrantFiled: October 17, 2006Date of Patent: May 26, 2015Assignee: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kohsuke Ohno, Takashi Miyagi, Tomonaga Ozawa, Nobuhiko Fushimi
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Publication number: 20150126513Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.Type: ApplicationFiled: July 13, 2012Publication date: May 7, 2015Applicant: Novartis AGInventors: Christine Hiu-Tung Chen, Donovan Noel Chin, Lucian V. DiPietro, Jianmei Fan, Mark G. Palermo, Michael David Shultz, Bakary-Barry Toure
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Patent number: 9023858Abstract: The present invention provides a compound useful for the prophylaxis or treatment of eicosanoid-associated diseases such as atherosclerosis, atherothrombosis, diabetes, obesity, asthma, fever, pain, cancer, rheumatism, osteoarthritis, atopic dermatitis and the like, and having superior pharmacological action, physicochemical properties and the like. The present invention relates to a compound represented by the following formula: wherein each symbol is as defined in the specification, or a salt thereof.Type: GrantFiled: July 22, 2011Date of Patent: May 5, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Nobuyuki Matsunaga, Hideo Suzuki, Kouhei Asano, Hidekazu Tokuhara, Takeshi Yamamoto, Rei Okamoto
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Patent number: 9018209Abstract: The present invention relates to compounds according to the formula I: Where Ra is H or an optionally OH-substituted C1-C3 alkyl; R1 is OR1, an optionally substituted C4-12 carbocyclic group which may be saturated or unsaturated (including aromatic) or an optionally substituted heterocyclic group; R1 is an optionally substituted C1-C14 hydrocarbyl group or an optionally substituted heterocyclic group; R2, R3 and R4 are each independently H, an optionally substituted C1-C4 alkyl group (preferably CH3, CH2CH3 or CF3), halogen (preferably F, Cl, Br), OR, CN, NO2, a C1-C6 thioether, a C1-C6 thioester group, an optionally substituted CO2R group, an optionally substituted COR group or an optionally substituted OCOR group (preferably R4 is H); R is H or an optionally substituted C1-C6 alkyl group; RHET is an optionally substituted heterocyclic group; and pharmaceutically acceptable salts, solvates or polymorphs thereof.Type: GrantFiled: September 25, 2006Date of Patent: April 28, 2015Assignee: Yale UniversityInventors: William L. Jorgensen, Juliana Ruiz-Caro, Andrew D. Hamilton
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Patent number: 9018175Abstract: The compounds of Formula (1), in which A, R1, R2, R3 and R5 have the meanings as given in the description, are novel effective inhibitors of type 4 and 5 phosphodiesterase.Type: GrantFiled: December 15, 2010Date of Patent: April 28, 2015Assignee: Takeda GmbHInventors: Dieter Flockerzi, Thomas Stengel, Alexander Mann, Harald Ohmer, Ulrich Kautz, Steffen Weinbrenner, Stefan Fischer, Christof Zitt, Armin Hatzelmann, Torsten Dunkern, Christian Hesslinger, Thomas Maier, Hermann Tenor, Clemens Braun, Raimund Külzer, Degenhard Marx
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Publication number: 20150111876Abstract: A sulfur-containing bicyclic compound having a PAM action of GABAB, and it use for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease. A pharmaceutical composition for preventing and/or treating schizophrenia, cognitive impairment associated with schizophrenia (CIAS), cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, Charcot-Marie-Tooth disease, or the like, which has a positive allosteric modulator (PAM action) of GABAB.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Applicant: Astellas Pharma Inc.Inventors: Nobuyuki Shiraishi, Hiroaki Hoshii, Wataru Hamaguchi, Eriko Honjo, Tomofumi Takuwa, Yuji Kondo, Takayuki Goto
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Publication number: 20150111038Abstract: The present disclosure is directed to salts of N-{4-[2,4-difluoro-3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl}dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetamide and process for the preparation thereof (formula II).Type: ApplicationFiled: June 8, 2013Publication date: April 23, 2015Applicant: GLENMARK PHARMACEUTICALS S.A.Inventors: Suresh Mahadev Kadam, Abraham Thomas, Sukumar Sinha, Sukeerthi Kumar, Bipin Parsottam Kansagra, Sachin Gavhane, Sandeep Bandu Khandagale, Shailesh Pawase, Jayant Prakashrao Patil, Shailendra Bhadane, Bhavna Mishra, Rajesh Dwivedi
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Patent number: RE47451Abstract: Provided are a thieno[3,2-d]pyrimidine derivative of formula (I) or a pharmaceutically acceptable salt thereof having inhibitory activity for protein kinase, and a pharmaceutical composition comprising same for prevention and treatment of abnormal cell growth diseases.Type: GrantFiled: October 13, 2017Date of Patent: June 25, 2019Assignee: Hanmi Pharm. Co. Ltd.Inventors: In Hwan Bae, Jung Beom Son, Sang Mi Han, Eun Joo Kwak, Ho Seok Kim, Ji Young Song, Eun Young Byun, Seung Ah Jun, Young Gil Ahn, Kwee Hyun Suh