Spiro Diazine Patents (Class 544/231)
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Patent number: 11884629Abstract: Provided are embodiments of para-substituted 1,1-dialkyl-4-phenylpiperazin-1-ium iodides advantageous for modulating inflammation that have been synthesized and their electrophysiology activities for ?9, ?9?10, and ?7 nAChRs compared. The para position contained alkyl or aryl amides, or heterocyclic isosteres for the amide, and the alkyl groups were varied at the ammonium piperazine nitrogen to see if compensatory changes in size at this position of the molecule impacted function. The compounds were characterized with two-electrode voltage-clamp measurements on Xenopus oocytes expressing nAChRs. General, the compounds were more potent for ?9-containing receptors than for ?7, and the majority were either full or strong partial agonists for ?9-containing nAChR.Type: GrantFiled: September 6, 2022Date of Patent: January 30, 2024Assignee: University of Florida Research Foundation, Inc.Inventors: Nicole Alana Horenstein, Roger Lee Papke, Hina Andleeb
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Patent number: 11767614Abstract: A chitin-modified polypropylene spunbond non-woven fabric and a preparation method of the chitin-modified polypropylene spunbond non-woven fabric are provided. The chitin-modified polypropylene spunbond non-woven fabric contains a modified chitin in a weight percentage range of approximately 0.2%-1.5%. The modified chitin includes chitin modified by a modifier including 2-hydroxybenzimidazole, cellulose acetate butyrate, and adipic acid dihydrazide. The chitin-modified polypropylene spunbond non-woven fabric has an anti-mold grade less than 1, and an antibacterial rate greater than 9.5%.Type: GrantFiled: December 9, 2020Date of Patent: September 26, 2023Assignees: SINOTECH ACADEMY OF TEXTILE (QINGDAO) CO., LTD., BESTEE MATERIAL (TSINGTAO) CO., LTD.Inventors: Xiaohua Huang, Yanming Liu, Xiaoqian Huang
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Patent number: 11512156Abstract: Poly(aryl piperidinium) polymers with pendant cationic groups are provided which have an alkaline-stable cation, piperidinium, introduced into a rigid aromatic polymer backbone free of ether bonds. Hydroxide exchange membranes or hydroxide exchange ionomers formed from these polymers exhibit superior chemical stability, hydroxide conductivity, decreased water uptake, good solubility in selected solvents, and improved mechanical properties in an ambient dry state as compared to conventional hydroxide exchange membranes or ionomers. Hydroxide exchange membrane fuel cells comprising the poly(aryl piperidinium) polymers with pendant cationic groups exhibit enhanced performance and durability at relatively high temperatures.Type: GrantFiled: September 28, 2018Date of Patent: November 29, 2022Assignee: University of DelawareInventors: Yushan Yan, Keda Hu, Junhua Wang, Lan Wang, Bingjun Xu, Yun Zhao
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Patent number: 9708321Abstract: The present invention relates to novel spiro-quinazolinone derivatives as positive allosteric modulators for modulating metabotropic glutamate receptor subtype 4 (mGluR4) and/or altering glutamate level or glutamatergic signalling.Type: GrantFiled: January 23, 2014Date of Patent: July 18, 2017Assignee: MERCK PATENT GMBHInventors: Nadia Brugger, Brian L. Hodous, Amanda E. Sutton, Justin Potnick, Theresa L. Johnson, Thomas E. Richardson, Thomas Francis Nelson Haxell, James M. Dorsey, Robert James Foglesong
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Patent number: 9434737Abstract: Provided is a process for producing (3R)-2?-(4-bromo-2-fluorobenzyl)spiro{pyrrolidine-3,4?(1?H)-pyrrolo[1,2-a]pyrazine}-1?,2,3?,5(2?H)-tetraone (compound A). The method includes converting an optically active succinimide derivative of formula (I) to compound A, in which the compound of formula (I) has been prepared by reacting a base with an optically active amide derivative of formula (VI).Type: GrantFiled: December 12, 2013Date of Patent: September 6, 2016Assignees: Sumitomo Dainippon Pharma Co., Ltd., Kyowa Hakko Bio Co., Ltd.Inventors: Masaji Kasai, Shinji Kita, Tadashi Ogawa, Hideaki Tokai
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Patent number: 9409899Abstract: The present invention discloses process for preparing benzisothiazol-3-yl-piperazin-1-yl-methyl-cyclohexylmethanisoindol-1,3-dione and intermediates thereof.Type: GrantFiled: February 12, 2013Date of Patent: August 9, 2016Assignee: Cadila Healthcare LimitedInventors: Shri Prakash Dhar Dwivedi, Ramesh Chandra Singh, Rajendra Gokalbhai Chavda
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Publication number: 20150133428Abstract: The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: November 14, 2014Publication date: May 14, 2015Inventors: Upender Velaparthi, Chetan Padmakar Darne, Peiying Liu, Mark D. Wittman, Bradley C. Pearce, Erika M. V. Araujo, Bireshwar Dasgupta, Jalathi Surendran Nair, Sakthi Kumaran Janakiraman, Chandrasekhar Reddy Rachamreddy, Mettu Mallikarjuna Rao, Arul Mozhi Selvan Subbiah Karuppiah, Bandreddy Subba Reddy, Pulicharla Nagalakshmi, Rajesh Onkardas Bora, Shilpa Holehatti Maheshwarappa, Selvakumar Kumaravel, Dibakar Mullick, Ramesh Sistla
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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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Publication number: 20150126502Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: January 14, 2015Publication date: May 7, 2015Inventors: Robert A. GALEMMO, Dean R. ARTIS, Xiaocong Michael YE, Danielle Aubele, Anh TRUONG, Simeon BOWERS, Roy K. Hom, Yong-Liang ZHU, R. Jeffrey NEITZ, Jennifer SEALY, Marc ADLER, Paul BEROZA, John P. ANDERSON
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Patent number: 9006265Abstract: The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.Type: GrantFiled: September 2, 2011Date of Patent: April 14, 2015Assignee: Bayer Intellectual Property GmbHInventors: Jens Frackenpohl, Hans-Joachim Zeiβ, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döring, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills, Monika H. Schmitt
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Publication number: 20150099743Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: ApplicationFiled: October 3, 2014Publication date: April 9, 2015Inventors: Hui LI, Seiji NUKUI, Stephanie Anne SCALES, Min TENG, Chunfeng YIN
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Patent number: 8999981Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: GrantFiled: January 6, 2012Date of Patent: April 7, 2015Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Iriny Botrous, Yufeng Hong, Hui Li, Kevin Kun-Chin Liu, Seiji Nukui, Min Teng, Eileen Valenzuela Tompkins, Chunfeng Yin
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Patent number: 8993753Abstract: The present invention relates to a process for the stereoselective preparation of compounds of formulae (1A) and (1B) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.Type: GrantFiled: January 14, 2014Date of Patent: March 31, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Markus Ostermeier, Juergen Daeubler, Guenther Huchler, Stephan Kling, Marco Santagostino
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Publication number: 20150087830Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.Type: ApplicationFiled: November 7, 2014Publication date: March 26, 2015Inventors: Nobuyuki AE, Yuji FUJIWARA
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Patent number: 8957083Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A1, A3, A4, A5, A6, A8, L, R2, R7, R9, W and Y of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, sub-Formula embodiments of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulae I-III.Type: GrantFiled: November 18, 2011Date of Patent: February 17, 2015Assignee: Amgen Inc.Inventors: Ana Elena Minatti, Oleg Epstein, Ryan White, Matthew Weiss, Wenge Zhong, Jonathan D. Low
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Publication number: 20150031691Abstract: The present invention relates to compounds represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.Type: ApplicationFiled: October 8, 2014Publication date: January 29, 2015Inventors: Lawrence Wayne Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh B. Singh, Yajun Zheng
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Publication number: 20150031880Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: ApplicationFiled: August 5, 2014Publication date: January 29, 2015Inventors: Francis X. Tavares, Jay C. Strum
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Publication number: 20150018368Abstract: The present invention discloses process for preparing benzisothiazol-3-yl-piperazin-1-yl-methyl-cyclo hexyl-methan-isoindol-1,3-dione and intermediates thereof.Type: ApplicationFiled: February 12, 2013Publication date: January 15, 2015Inventors: Shri Prakash Dhar Dwivedi, Ramesh Chandra Singh, Rajendra Gokalbhai Chavda
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Publication number: 20150018347Abstract: The present application describes modulators of chemokine receptor activity of formula I or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.Type: ApplicationFiled: October 1, 2014Publication date: January 15, 2015Inventors: T. G. Murali Dhar, John V. Duncia, Daniel S. Gardner, Weiwei Guo, John Hynes
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Publication number: 20150018348Abstract: Compounds useful as kinase inhibitors are provided herein, as well as salts, pharmaceutical compositions, methods of medical treatment and methods of synthesis thereof.Type: ApplicationFiled: September 26, 2014Publication date: January 15, 2015Inventor: Francis Xavier Tavares
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Publication number: 20150005295Abstract: Inhibitors of HBV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1-R5, B and Z have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.Type: ApplicationFiled: January 4, 2013Publication date: January 1, 2015Inventors: Koen Vandyck, Geerwin Yvonne Paul Haché, Geert Rombouts, Wim Gaston Verschueren, Pierre Jean-Marie Raboisson
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Publication number: 20140364411Abstract: Compounds of formula (I) described herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.Type: ApplicationFiled: June 5, 2014Publication date: December 11, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Chi-Kit WOO, Lilian ALCARAZ, Carmelida CAPALDI
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Publication number: 20140357626Abstract: Inhibitors of HCV replication of formula I, including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: ApplicationFiled: December 27, 2012Publication date: December 4, 2014Inventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20140350244Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.Type: ApplicationFiled: August 7, 2014Publication date: November 27, 2014Inventors: Richard V. Connors, Kang DAI, John EKSTEROWICZ, Pingchen FAN, Benjamin FISHER, Jiasheng FU, Kexue LI, Zhihong LI, Lawrence R. MCGEE, Rajiv SHARMA, Xiaodong WANG, Dustin L. MCMINN, Jeffrey T. MIHALIC, Jeffrey DEIGNAN
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Publication number: 20140336208Abstract: This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.Type: ApplicationFiled: July 9, 2014Publication date: November 13, 2014Inventors: David Banner, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Benoit Hornsperger, Roland Humm, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Emmanuel Pinard, Mark Rogers-Evans, Thomas Woltering, Wolfgang Wostl
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Patent number: 8883789Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. R1, R2, R3, R4, Q have meanings given in the description.Type: GrantFiled: December 10, 2012Date of Patent: November 11, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Annekatrin Heimann, Georg Dahmann, Marc Grundl, Stephan Georg Mueller, Bernd Wellenzohn
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Patent number: 8877749Abstract: The present application describes modulators of chemokine receptor activity of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.Type: GrantFiled: October 6, 2010Date of Patent: November 4, 2014Assignee: Bristol-Myers Squibbs CompanyInventors: T. G. Murali Dhar, John V. Duncia, Daniel S. Gardner, Weiwei Guo, John Hynes
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Publication number: 20140316132Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 1, 2014Publication date: October 23, 2014Inventors: Manoj C. Desai, Randal L. Halcomb, Paul Hrvatin, Hon Chung Hui, Ryan McFadden, Paul A. Roethle, Hong Yang
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Publication number: 20140309213Abstract: This invention relates to compounds of Formula I-VI having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R is a 6-8 membered saturated heterocyclic ring having 2 Nitrogen atoms connected with —(CH2)n1— and —(CH2)n2—, respectively, and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 25, 2012Publication date: October 16, 2014Inventors: Shawn P. Walsh, Alexander Pasternak, Reynalda K. DeJesus, Haifeng Tang, Barbara Pio, Aurash Shahripour, Kevin M. Belyk, Harry R. Chobanian, Yan Guo, Jessica L. Frie, Zhi-Cai Shi, Helen Chen, Timothy A. Blizzard, Brian Cato
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Patent number: 8853395Abstract: Disclosed is a new and efficient process for the synthesis with high yields and purity of lurasidone hydrochloride, a medicament which is useful as a psychotropic substance. The process involves the preparation of lurasidone base in a reaction system not containing inorganic salts, followed by conversion of the latter to an addition salt with an organic carboxylic acid, which is finally converted to lurasidone hydrochloride.Type: GrantFiled: February 20, 2014Date of Patent: October 7, 2014Assignee: Edmond Pharma S.R.L.Inventors: Matteo Zacche', Fulvio Gerli, Pierandrea Gatti
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Publication number: 20140288100Abstract: Disclosed are inhibitors of human galactokinase of formula (1) that are useful in treating or preventing a galactokinase mediated disease or disorder, e.g., galactosemia. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal.Type: ApplicationFiled: September 23, 2011Publication date: September 25, 2014Applicants: University of Utah Research Foundation, The United States of American, as Represented by the Decretary, Department of Health and HumanInventors: Matthew B. Boxer, Martin J. Walsh, Li Liu, Cordelle D. Tanega, Min Shen, Kent Lai, Manshu Tang, Douglas S. Auld
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Publication number: 20140275017Abstract: Compounds of Formula I: (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.Type: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
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Publication number: 20140275066Abstract: This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: G1 THERAPEUTICS, INC.Inventors: Norman E. Sharpless, Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
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Publication number: 20140275067Abstract: This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: G1 Therapeutics, Inc.Inventors: Norman E. Sharpless, Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
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Publication number: 20140256939Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.Type: ApplicationFiled: March 7, 2014Publication date: September 11, 2014Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Nobuyuki AE, Yuji FUJIWARA
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Publication number: 20140249129Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: February 20, 2014Publication date: September 4, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Christian GNAMM, Thorsten OOST, Stefan PETERS, Klaus RUDOLF
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Publication number: 20140221378Abstract: Provided is a substituted spiropyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, which is useful as an anti-HIV agent. The present invention relates to a compound represented by the following formula [I] or [II] or a pharmaceutically acceptable salt thereof: wherein each symbol is as defined in the specification.Type: ApplicationFiled: December 27, 2013Publication date: August 7, 2014Applicant: JAPAN TOBACCO INC.Inventors: Susumu MIYAZAKI, Hirotaka ISOSHIMA, Kengo OSHITA, Seiji KAWASHITA, Noboru NAGAHASHI, Masakazu TERASHITA
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Publication number: 20140221380Abstract: [Summary] [Problem] Provided is a substituted spiropyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, which is useful as an anti-HIV agent. [Solving Means] The present invention relates to a compound represented by the following formula [I] or [II] or a pharmaceutically acceptable salt thereof: wherein each symbol is as defined in the specification.Type: ApplicationFiled: December 27, 2013Publication date: August 7, 2014Applicant: JAPAN TOBACCO INC.Inventors: Susumu MIYAZAKI, Hirotaka ISOSHIMA, Kengo OSHITA, Seiji KAWASHITA, Noboru NAGAHASHI, Masakazu TERASHITA
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Patent number: 8785451Abstract: Disclosed are compounds of formula (IA), formula (IV) or formula (V), wherein the variables are as defined herein, and pharmaceutical compositions containing them which are useful for treating a subject with a proliferative disorder, such as cancer. The disclosed compounds and pharmaceutical compositions are also useful for treating disorders responsive to Hsp70 induction and/or natural killer induction.Type: GrantFiled: August 20, 2007Date of Patent: July 22, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Jun Jiang
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Publication number: 20140200223Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.Type: ApplicationFiled: December 18, 2013Publication date: July 17, 2014Inventors: Salvacion Cacatian, David A. Claremon, Lawrence Wayne Dillard, Klaus Fuchs, Niklas Heine, Lanqi Jia, Katerina Leftheris, Brian Mckeever, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Guosheng Wu, Zhongren Wu, Zhenrong Xu, Jing Yuan, Yajun Zheng
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Patent number: 8765763Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein R1, R2, R3, Ra, Rb, Rc, X, Y and Z are defined as mentioned hereinafter, the individual diastereomers, the individual enantiomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, the use thereof and processes for the preparation thereof.Type: GrantFiled: June 2, 2010Date of Patent: July 1, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Alexander Dreyer, Henri Doods, Kai Gerlach, Dirk Gottschling, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Schaenzle
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Patent number: 8765744Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, R7, A, Z and m are as defined herein. The compounds of formula (I) are inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 (11beta-HSD1) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.Type: GrantFiled: June 23, 2011Date of Patent: July 1, 2014Assignee: Boehringer Ingelheim International GmbHInventor: Frank Himmelsbach
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Patent number: 8754073Abstract: Piperidinodihydrothienopyrimidines of formula 1 wherein X is SO or SO2 (preferably SO), and R1, R2, R3, and R4 may have the meanings given in the disclosure and claims, pharmacologically acceptable salts thereof, and pharmaceutical compositions containing these compounds. These piperidinodihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system, or cancers.Type: GrantFiled: October 16, 2008Date of Patent: June 17, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Pascale Pouzet, Ralf Anderskewitz, Horst Dollinger, Dennis Fiegen, Thomas Fox, Rolf Goeggel, Christoph Hoenke, Domnic Martyres, Peter Nickolaus, Klaus Klinder
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Publication number: 20140142306Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: ApplicationFiled: January 23, 2014Publication date: May 22, 2014Applicant: G1 Therapeutics, Inc.Inventors: Francis X. Tavares, Jay C. Strum
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Publication number: 20140135495Abstract: The present invention relates to a process for the stereoselective preparation of compounds of formulae (1A) and (1B) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.Type: ApplicationFiled: January 14, 2014Publication date: May 15, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Markus OSTERMEIER, Juergen DAEUBLER, Guenther HUCHLER, Stephan KLING, Marco SANTAGOSTINO
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Publication number: 20140128371Abstract: The present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.Type: ApplicationFiled: January 13, 2014Publication date: May 8, 2014Applicant: ASTRAZENECA ABInventors: Kevin BARVIAN, Gregory Steven BASARAB, Madhusudhan Reddy GOWRAVARAM, Sheila Irene HAUCK, Fei ZHOU
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Publication number: 20140113895Abstract: A compound or its pharmaceutically acceptable salt, optionally including both individual enantiomeric forms, a racemate, diastereomers and mixtures thereof, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.Type: ApplicationFiled: December 20, 2013Publication date: April 24, 2014Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Publication number: 20140099681Abstract: A process for producing optically active succinimide derivatives as key intermediates of (3R)-2?-(4-bromo-2-fluorobenzyl)spiro{pyrrolidine-3,4?(1?H)-pyrrolo[1,2-a]pyrazine}-1?,2,3?,5(2?H)-tetraone, which comprises the following reaction steps.Type: ApplicationFiled: December 12, 2013Publication date: April 10, 2014Applicants: Kyowa Hakko Bio Co., Ltd., Dainippon Sumitomo Pharma Co., Ltd.Inventors: Masaji KASAI, Shinji KITA, Tadashi OGAWA, Hideaki TOKAI
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Publication number: 20140080823Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C?R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.Type: ApplicationFiled: November 22, 2013Publication date: March 20, 2014Applicant: DAC S.R.L.Inventors: Mario Varasi, Florian Thaler, Agnese Abate, Giacomo Carenzi, Ciro Mercurio, Saverio Minucci
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Publication number: 20140066369Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.Type: ApplicationFiled: April 18, 2012Publication date: March 6, 2014Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Dawei Yue, Xiuwen Zhu