The Nitrogens Are In The 1,4-positions Of The Hetero Ring Patents (Class 540/575)
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Patent number: 11834432Abstract: Provided in the present invention are a substituted amino six-membered nitric heterocyclic ring compound and a preparation and use thereof. In particular, provided in the present invention is a compound as shown by general formula (I) below, wherein the definition of each group is as described in the description. The compound of the present invention has an excellent tyrosine kinase inhibitory activity, and can thus be used to prepare a series of medicines for treating diseases related to tyrosine kinase inhibitory activity.Type: GrantFiled: February 17, 2017Date of Patent: December 5, 2023Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCESInventors: Ao Zhang, Meiyu Geng, Li Xing, Jing Ai, Zilan Song, Xia Peng, Wangting Gu, Jian Ding
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Patent number: 11229654Abstract: The present invention provides methods, compositions, and combinations for treating cancer via combined use of a compound of formula I or a pharmaceutically acceptable salt, ester, solvate and/or prodrug thereof, wherein A, Q, n, m, R7, R8, V, X1, X2, X3, X4, X5, X6, and X7 are as defined herein, and at least one therapeutically active agents selected from immunotherapeutics, anticancer agents, and anti-angiogenics.Type: GrantFiled: January 18, 2019Date of Patent: January 25, 2022Assignee: SENHWA BIOSCIENCES, INC.Inventor: John Soong
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Patent number: 11191770Abstract: The present invention provides methods, compositions, and combinations for treating cancer via combined use of a compound of formula I or a pharmaceutically acceptable salt, ester, solvate and/or prodrug thereof, wherein A, Q, n, m, R7, R8, V, X1, X2, X3, X4, X5, X6, and X7 are as defined herein, and at least one therapeutically active agents selected from immunotherapeutics, anticancer agents, and anti-angiogenics.Type: GrantFiled: January 18, 2019Date of Patent: December 7, 2021Assignee: SENHWA BIOSCIENCES, INC.Inventor: John Soong
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Patent number: 11174237Abstract: Disclosed are a 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride polymorph, a preparation method therefor and an application thereof. Specifically, disclosed are three crystalline forms, i.e., crystalline forms A, B, and C, of 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride (formula I), preparation methods for the three crystalline forms, and use of the three crystalline forms in preparation of drugs.Type: GrantFiled: May 31, 2018Date of Patent: November 16, 2021Assignees: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, FUKANG (SHANGHAI) HEALTH TECHNOLOGY CO., LTD.Inventors: Chunhao Yang, Zehong Miao, Cun Tan, Xiajuan Huan, Jian Ding, Yi Chen
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Patent number: 10793569Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, R3, R4, Ar and X1 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.Type: GrantFiled: May 1, 2020Date of Patent: October 6, 2020Assignee: BRISTOL-MYERS SQUIBB COMPANYInventors: Liqi He, Sanjeev Gangwar, Yam B. Poudel, Prasanna Sivaprakasam
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Patent number: 10723736Abstract: Compounds having a structure according to formula (I) where R1 and Ar are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.Type: GrantFiled: October 22, 2019Date of Patent: July 28, 2020Assignee: Bristol-Myers Squibb CompanyInventors: Yam B. Poudel, Liqi He, Sanjeev Gangwar, Shoshana L. Posy, Prasanna Sivaprakasam
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Patent number: 10508115Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, R3, R4, Ar and X1 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.Type: GrantFiled: August 14, 2018Date of Patent: December 17, 2019Assignee: Bristol-Myers Squibb CompanyInventors: Liqi He, Sanjeev Gangwar, Yam B. Poudel, Prasanna Sivaprakasam
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Patent number: 10494370Abstract: Compounds having a structure according to formula (I) where R1 and Ar are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.Type: GrantFiled: August 14, 2018Date of Patent: December 3, 2019Assignee: Bristol-Myers Squibb CompanyInventors: Yam B. Poudel, Liqi He, Sanjeev Gangwar, Shoshana L. Posy, Prasanna Sivaprakasam
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Patent number: 10195196Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: November 29, 2016Date of Patent: February 5, 2019Assignee: Novartis AGInventors: Atwood Kim Cheung, Donovan Noel Chin, Natalie Dales, Aleem Fazal, Timothy Hurley, John Kerrigan, Gary O'Brien, Lei Shu, Robert Sun, Moo Je Sung
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Patent number: 9969719Abstract: Disclosed is a substituted 2H-pyrazole derivative serving as a selective CDK4/6 inhibitor. Specifically, disclosed is a compound of formula (I) or a pharmaceutically acceptable salt thereof which serves as a selective CDK4/6 inhibitor.Type: GrantFiled: March 10, 2016Date of Patent: May 15, 2018Assignees: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., MEDSHINE DISCOVERY INC.Inventors: Charles Z. Ding, Shuhui Chen, Baoping Zhao, Zhaobing Xu, Yingchun Liu, Ruibin Lin, Fei Wang, Jian Li
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Patent number: 9809547Abstract: The present invention is directed to novel processes for the preparation of histamine H3 receptor modulators, in the treatment of for example, cognitive disorders, sleep disorders and/or psychiatric disorders.Type: GrantFiled: November 11, 2016Date of Patent: November 7, 2017Assignee: Janssen Pharmaceutica NVInventors: Diego Fernando Domenico Broggini, Vit Lellek, Susanne Lochner, Neelakandha S. Mani, Adrian Maurer, Daniel J. Pippel, Lana K. Young
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Patent number: 9586951Abstract: There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof (In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z2 represents CH or the like; Z1 represents CR6 or the like; R6 represents a hydrogen atom or the like; X1 represents CHR7 or the like; R7 represents a hydrogen atom or the like; X2 represents CH2 or the like; R1 and R2 are the same as or different from each other, and each of R1 and R2 represents a hydrogen atom or the like; R3, R4, and R5 are the same as or different from each other, and each of R3, R4, and R5 represents a hydrogen atom, NRaRb, or the like; and each of Ra and Rb represents a hydrogen atom, a C1-8 alkyl group which may have a substituent, or the like).Type: GrantFiled: February 24, 2016Date of Patent: March 7, 2017Assignee: FUJIFILM CorporationInventors: Yohei Kubo, Makoto Ando, Hidehiko Tanaka, Shuhei Osaka, Takuya Matsumoto, Hiyoku Nakata, Daisuke Terada, Tatsuya Nitabaru
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Patent number: 9545404Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: April 1, 2014Date of Patent: January 17, 2017Assignee: NOVARTIS AGInventors: Atwood Kim Cheung, Donovan Noel Chin, Natalie Dales, Aleem Fazal, Timothy Hurley, John Kerrigan, Gary O'Brien, Lei Shu, Robert Sun, Moo Je Sung
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Patent number: 9540344Abstract: The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.Type: GrantFiled: December 5, 2014Date of Patent: January 10, 2017Assignee: KOWA CO., LTD.Inventors: Noriaki Gomi, Tadaaki Ohgiya, Kimiyuki Shibuya
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Patent number: 9388148Abstract: The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor.Type: GrantFiled: March 14, 2014Date of Patent: July 12, 2016Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KGInventors: Andreas Haupt, Jürgen Dinges, Liliane Unger, Karsten Wicke, Robert Van Waterschoot, Karla Drescher, Ana Relo
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Patent number: 9357782Abstract: The invention relates to compounds of the general formula (I), wherein the variable have the meanings as indicated in the claims, or a physiologically acceptable salt thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling endoparasites in warm-blooded animals.Type: GrantFiled: August 6, 2013Date of Patent: June 7, 2016Assignee: NOVARTIS TIERGESUNDHEIT AGInventors: Noelle Gauvry, Francois Pautrat
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Patent number: 9045460Abstract: The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.Type: GrantFiled: August 25, 2011Date of Patent: June 2, 2015Assignee: KOWA CO., LTD.Inventors: Noriaki Gomi, Tadaaki Ohgiya, Kimiyuki Shibuya
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Publication number: 20150148327Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: June 17, 2013Publication date: May 28, 2015Applicant: Merck Canada Inc.Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
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Patent number: 9040522Abstract: The present invention provides compounds of the formula: which are useful as inhibitors of PHD and pharmaceutical compositions thereof.Type: GrantFiled: March 26, 2014Date of Patent: May 26, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Jason W. Brown, Melinda Davis, Anthony Ivetac, Benjamin Jones, Andre A. Kiryanov, Jon Kuehler, Marion Lanier, Joanne Miura, Sean Murphy, Xiaolun Wang
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Publication number: 20150133425Abstract: 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: ApplicationFiled: May 17, 2013Publication date: May 14, 2015Inventors: 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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Publication number: 20150132258Abstract: 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.Type: ApplicationFiled: November 14, 2014Publication date: May 14, 2015Inventor: George D. Hartman
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Publication number: 20150133432Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4, R5 and R6 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: November 10, 2014Publication date: May 14, 2015Inventors: Stephanie HACHTEL, Christian SCHOENAU, Matthias LOEHN, Oliver PLETTENBURG, Stefania PFEIFFER-MAREK, Alexander SCHIFFER, Holger GAUL, Aimo KANNT, Juergen DEDIO, Angela DUDDA
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Patent number: 9029356Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: GrantFiled: March 14, 2014Date of Patent: May 12, 2015Assignee: Nerviano Medical Sciences S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Publication number: 20150119380Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.Type: ApplicationFiled: December 28, 2012Publication date: April 30, 2015Inventors: Matthew G. Woll, Guangming Chen, Soongyu Choi, Amal Dakka, Song Huang, Gary Mitchell Karp, Chang-Sun Lee, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Sergey Paushkin, Hongyan Qi, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Emmanuel Pinard, Hasane Ratni
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Publication number: 20150111879Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.Type: ApplicationFiled: December 24, 2014Publication date: April 23, 2015Applicants: CURIS, INC., GENENTECH, INC.Inventors: Janet L. GUNZNER, Daniel P. SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
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Publication number: 20150104384Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.Type: ApplicationFiled: March 1, 2013Publication date: April 16, 2015Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
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Publication number: 20150105550Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Applicants: CURIS, INC., GENENTECH, INC.Inventors: Janet L. GUNZNER, Daniel SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
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Publication number: 20150105370Abstract: Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.Type: ApplicationFiled: October 14, 2014Publication date: April 16, 2015Inventors: ERIC CARLSON, HANS HANSEN, LYNN HAWKINS, SALLY ISHIZAKA, MATTHEW MACKEY, SHAWN SCHILLER, CHIKAKO OGAWA, HEATHER DAVIS
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Patent number: 9006276Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.Type: GrantFiled: September 23, 2011Date of Patent: April 14, 2015Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
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Publication number: 20150099732Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.Type: ApplicationFiled: March 7, 2013Publication date: April 9, 2015Inventors: Alan Ashworth, Christopher James Lord, Richard James Rowland Elliot, Dan Niculescu-Duvaz, Roderick Porter, Raymond John Boffey, Melanie Jayne Bayford, Stuart Firth-Clark, Ashley Nicholas Jarvis, Trevor Robert Perrior, Rebekah Elisabeth Key
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Patent number: 8999973Abstract: The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.Type: GrantFiled: January 31, 2011Date of Patent: April 7, 2015Assignees: Hanmi Science Co., Ltd, Korea Institute of Science and Technology, Catholic University Industry Academic Cooperation FoundationInventors: Jung Beom Son, Seung Hyun Jung, Wha II Choi, Young Hee Jung, Jae Yul Choi, Ji Yeon Song, Kyu Hang Lee, Jae Chul Lee, Eun Young Kim, Young Gil Ahn, Maeng Sup Kim, Hwan Geun Choi, Tae Bo Sim, Young Jin Ham, Dong-sik Park, Hwan Kim, Dong-Wook Kim
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Patent number: 8999974Abstract: The present invention relates to acyl piperazine derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: GrantFiled: August 9, 2011Date of Patent: April 7, 2015Assignee: Raqualia Pharma Inc.Inventors: Mikiko Morita, Shuzo Watanabe
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Publication number: 20150094298Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: December 5, 2014Publication date: April 2, 2015Inventors: Shawn M. Bauer, Zhaozhong J. Jia, Mukund Mehrotra, Yonghong Song, Qing Xu, Wolin Huang, Chandrasekar Venkataramani, Jack W. Rose, Anjali Pandey
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Transamination of nitrogen-containing compounds to make cyclic and cyclic/acyclic polyamine mixtures
Patent number: 8993759Abstract: A transamination process is described to prepare polyamine product mixtures from reactants comprising mixed nitrogen-containing compounds with binary carbon spacing between nitrogen-containing groups (a binary component). A second nitrogen-containing component with a second carbon atom spacing between nitrogen-containing groups may also be employed. The molar ratio between the binary and second components can be adjusted to customize the product composition for desired end uses.Type: GrantFiled: October 20, 2011Date of Patent: March 31, 2015Assignee: DOW Global Technologies LLCInventor: Stephen W. King -
Publication number: 20150087823Abstract: The present invention relates to a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical agent containing the compound as an active ingredient. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt, which is the compound of the present invention, is specifically represented by the general formula (I): wherein X is a substituent such as a 1-pyrrolidyl, a 3-thiazolizyl, or a piperidino, and the compound is highly useful as a pharmaceutical agent, such as a prophylactic or therapeutic agent for a peripheral nerve disorder induced by administration of an anticancer agent, a prophylactic or therapeutic agent for neurodegenerative diseases or mental diseases such as dementia, Alzheimer's disease, Parkinson's disease, diabetic neuropathy, depression, glaucoma, or autistic disorder spectrum, a therapeutic or repairing agent for spinal cord injury, analgesics against various pain diseases, or the like.Type: ApplicationFiled: April 26, 2013Publication date: March 26, 2015Inventors: Munekazu Iinuma, Shoei Furukawa, Mitsuru Naiki, Tomonori Matsumoto, Kunihiko Higashiura
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Publication number: 20150087635Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.Type: ApplicationFiled: December 4, 2014Publication date: March 26, 2015Inventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
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Publication number: 20150087824Abstract: The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.Type: ApplicationFiled: December 5, 2014Publication date: March 26, 2015Applicant: KOWA CO., LTD.Inventors: Noriaki GOMI, Tadaaki OHGIYA, Kimiyuki SHIBUYA
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Patent number: 8987250Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: GrantFiled: April 19, 2013Date of Patent: March 24, 2015Assignee: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20150080383Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.Type: ApplicationFiled: March 14, 2013Publication date: March 19, 2015Inventors: Tianle Yang, Gary Mitchell Karp, Hongyan Qi
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Publication number: 20150080371Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-fJ[1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.Type: ApplicationFiled: December 11, 2012Publication date: March 19, 2015Inventors: Marie-Pierre Collin, Dirk Brohm, Melanie Heroult, Mario Lobell, Walter Hübsch, Klemens Lustig, Sylvia Grünewald, Ulf Bömer, Verena Vöhringer, Niels Lindner
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Publication number: 20150080382Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.Type: ApplicationFiled: June 24, 2014Publication date: March 19, 2015Inventors: Damian O. Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J. Kochanny, Amy Liang, David Light, John Parkinson, Guo Ping Wei, Bin Ye
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Patent number: 8981084Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, Y, Q, X, B and L are as defined herein, and methods of making and using the same.Type: GrantFiled: January 13, 2011Date of Patent: March 17, 2015Assignee: Tempero Pharmaceuticals, Inc.Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
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Publication number: 20150073136Abstract: The present invention relates to pyrazinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: November 17, 2014Publication date: March 12, 2015Inventors: Stephen Brough, Richard Evans, Timothy Jon Luker, Piotr Raubo
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Patent number: 8975249Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: October 31, 2011Date of Patent: March 10, 2015Assignee: Celgene Avilomics Research, Inc.Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Matthew F. Baevsky, Juswinder Singh
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Patent number: 8975250Abstract: The present invention relates to 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives having Formula (I) as defined herein, their preparation and their therapeutic use.Type: GrantFiled: July 9, 2012Date of Patent: March 10, 2015Assignee: SANOFIInventors: Philippe Beauverger, Guillaume Begis, Sandrine Biscarrat, Olivier Duclos, Gary McCort
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Publication number: 20150065465Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: November 4, 2014Publication date: March 5, 2015Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
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Patent number: 8969336Abstract: Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.Type: GrantFiled: May 6, 2010Date of Patent: March 3, 2015Assignees: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.Inventors: Itsuro Shimada, Kazuo Kurosawa, Takahiro Matsuya, Kazuhiko Iikubo, Yutaka Kondoh, Akio Kamikawa, Hiroshi Tomiyama, Yoshinori Iwai
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Publication number: 20150057263Abstract: This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.Type: ApplicationFiled: March 19, 2013Publication date: February 26, 2015Inventors: Robert Brown, Matthew John Fuchter, Nadine Chapman-Rothe, Nitipol Srimongkolpithak, Joachim Caron, James Synder, Thota Ganesh, Jin Liu, Aiming Sun
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Publication number: 20150057265Abstract: The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.Type: ApplicationFiled: August 22, 2014Publication date: February 26, 2015Applicant: INCYTE CORPORATIONInventors: Yun-Long Li, David M. Burns, Hao Feng, Taisheng Huang, Song Mei, Jun Pan, Oleg Vechorkin, Hai-Fen Ye, Wenyu Zhu, Maria Rafalski, Anlai Wang, Chu-Biao Xue
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Publication number: 20150051185Abstract: The invention relates to chemical compounds of formula I, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.Type: ApplicationFiled: July 24, 2014Publication date: February 19, 2015Applicant: AstraZeneca ABInventors: Leslie DAKIN, James Edward DOWLING, Michelle Laurae LAMB, Jon READ, Qibin SU, XiaoLan ZHENG