Chalcogen Bonded Directly To Ring Carbon Of The Bicyclo Ring System Patents (Class 546/183)
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Patent number: 11957726Abstract: A pharmaceutical composition or a health food composition for controlling blood sugar, raw materials of which include dioscoreae rhizome, medlar, and coconut oil. A preparation method for the composition includes: mixing dioscoreae rhizome and a decoction thereof with medlar for homogenization, pulverization and drying, and mixing the resultant product with coconut oil and water, followed by baking and drying. Further disclosed are a pharmaceutical preparation or a health food including the composition and an excipient, and a use of the composition in the preparation of a pharmaceutical preparation or a health food for reducing or eliminating diabetic conditions.Type: GrantFiled: September 8, 2017Date of Patent: April 16, 2024Assignee: BEIJING HEBABIZ BIOTECHNOLOGY CO., INC.Inventor: James Zhou
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Patent number: 11608347Abstract: The invention provides new heterocyclic compounds having the general formula (Ie) wherein R1, R1a and R7 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.Type: GrantFiled: July 7, 2020Date of Patent: March 21, 2023Assignee: Hoffmann-La Roche Inc.Inventors: Ann Petersen, Joerg Benz, Uwe Grether, Benoit Hornsperger, Buelent Kocer, Bernd Kuhn, Hans Richter, Satoshi Tsuchiya, Yangcheng Qiu, Rui Chen
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Patent number: 11573488Abstract: A holographic recording medium composition comprising component (e): a compound having an isocyanate group or an isocyanate-reactive functional group and further having a nitroxyl radical group, wherein component (e) contains component (e-1) below: component (e-1): a compound having a heterobicyclic ring structure or a heterotricyclic ring structure, the heterobicyclic ring structure or the heterotricyclic ring structure being obtained by replacing a carbon atom in a bicyclic ring structure or a tricyclic ring structure by the nitroxyl radical group.Type: GrantFiled: December 28, 2020Date of Patent: February 7, 2023Assignee: MITSUBISHI CHEMICAL CORPORATIONInventor: Takanori Shimizu
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Patent number: 11518762Abstract: The invention concerns a scalable, large-scale castanospermine preparation method that yields levels of purity greater than 98% from castanospermine-containing plant sources, such as Castanospermum australe seed material.Type: GrantFiled: June 4, 2021Date of Patent: December 6, 2022Assignee: Florida State University Research Foundation, Inc.Inventors: Eric Holmes, Gary Ostrander
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Patent number: 9562045Abstract: The present invention provides compounds of general formula 1 useful as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula 1 can be employed as therapeutics in human and veterinary medicine, where they can be used, for example, for the treatment and prophylaxis of the following diseases: heart failure, dilated cardiomyopathy, platelet inhibitors, cancer and obstructive pulmonary diseases.Type: GrantFiled: January 19, 2016Date of Patent: February 7, 2017Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Budde Mahendar, Saidulu Mattapally, Mettu Ravinder, Sanjay Kumar Banerjee, Vaidya Jayathirtha Rao
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Patent number: 9249139Abstract: The present invention provides compounds of general formula A useful as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula A can be employed as therapeutics in human and veterinary medicine, where they can be used, for example, for the treatment and prophylaxis of the following diseases: heart failure, dilated cardiomyopathy, platelet inhibitors, cancer and obstructive pulmonary diseases.Type: GrantFiled: January 30, 2014Date of Patent: February 2, 2016Assignee: Council of Scientific & Industrial ResearchInventors: Budde Mahendar, Saidulu Mattapally, Mettu Ravinder, Sanjay Kumar Banerjee, Vaidya Jayathirtha Rao
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Patent number: 9040508Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.Type: GrantFiled: December 8, 2009Date of Patent: May 26, 2015Assignee: VM Pharma LLCInventors: Jay Jie-Qiang Wu, Ling Wang
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Publication number: 20150105378Abstract: The present invention provides compounds of Formula (I) or Formula (III): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Publication number: 20150099887Abstract: The disclosure generally relates to a process for the preparation of compounds of formula I, including synthetic intermediates which are useful in the process.Type: ApplicationFiled: December 12, 2014Publication date: April 9, 2015Inventors: David K. Leahy, Yu Fan, Collin Chan, Lopa V. Desai, Sunil S. Patel, Masano Sugiyama
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Publication number: 20150065501Abstract: The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.Type: ApplicationFiled: March 27, 2013Publication date: March 5, 2015Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
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Patent number: 8969570Abstract: Aryl substituted diazabicyclooctanes (DBO) compounds that inhibit ?-lactamases of class A, class C or class D and potentiate ?-lactam antibiotics are disclosed. In particular, this disclosure provides DBO compounds that, when used in the disclosed Synergy MIC Assay with a ?-lactam antibiotic at a fixed concentration have an MIC of 8 ?g/mL or less against one or more isogenic ?-lactamase expressing bacterial strains.Type: GrantFiled: March 29, 2013Date of Patent: March 3, 2015Assignee: Cubist Pharmaceuticals, Inc.Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Robert Busch, Roland E. Dolle, Chester A. Metcalf, III
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Publication number: 20150056699Abstract: This invention provides a compound having the structure wherein A is a ring structure, with or without substitution; Z is present or absent and when present is wherein n is 0, 1, 2, 3, or 4; Y is —(CR11R12)—, —NH(CR11R12)—, or —O(CR11R12)—, wherein R11 and R12 are each hydrogen or combine to form a carbonyl; R1, R2, R3, R4, R5 and R6 are independently H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroaryl, hydroxyl, amino, ester or amide; ? represents a bond, which is present or absent and when ? is present, then R7 and R8 are absent; R7 and R8 are present when ? is absent and are independently H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroaryl, hydroxyl, amino, ester, amide or R5 and R7 combine to form a carbonyl or R6 and R8 combine to form a carbonyl; R9 and R10 are each hydrogen oType: ApplicationFiled: August 24, 2012Publication date: February 26, 2015Applicant: The Trustees of Columbia University in the City of New YorkInventors: Dalibor Sames, Xiaoguang Li, Shu Li, Andrew Kruegel, Richard Karpowicz, Ignacio Carrera, Souvik Rakshit
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Patent number: 8962844Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.Type: GrantFiled: March 29, 2013Date of Patent: February 24, 2015Assignee: Cubist Pharmaceuticals, Inc.Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Dongpeng Wan
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Patent number: 8962843Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.Type: GrantFiled: March 29, 2013Date of Patent: February 24, 2015Assignee: Cubist Pharmaceuticals, Inc.Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
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Patent number: 8940897Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.Type: GrantFiled: March 29, 2013Date of Patent: January 27, 2015Assignee: Cubist Pharmaceuticals, Inc.Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
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Patent number: 8933233Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.Type: GrantFiled: March 29, 2013Date of Patent: January 13, 2015Assignee: Cubist Pharmaceuticals, Inc.Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
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Patent number: 8933232Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.Type: GrantFiled: March 29, 2013Date of Patent: January 13, 2015Assignee: Cubist Pharmaceuticals, Inc.Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
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Patent number: 8927724Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.Type: GrantFiled: March 29, 2013Date of Patent: January 6, 2015Assignee: Cubist Pharmaceuticals, Inc.Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch, Dongpeng Wan, Jon Christian Baber
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Patent number: 8921560Abstract: Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: December 16, 2011Date of Patent: December 30, 2014Assignee: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Patent number: 8916709Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.Type: GrantFiled: March 29, 2013Date of Patent: December 23, 2014Assignee: Cubist Pharmaceuticals, Inc.Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Jon Christian Baber
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Patent number: 8907095Abstract: The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.Type: GrantFiled: October 20, 2008Date of Patent: December 9, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Yan Xia, Craig D. Boyle, William J. Greenlee, Samuel Chackalamannil, Charles Lee Jayne
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Publication number: 20140350246Abstract: The present invention relates to 7-membered nitrogen-containing heterocyclic compounds and methods of making the same. Using a novel aza-[4+3] cycloaddition reaction, the 7-membered heterocyclic compounds are synthesized by reacting a first reactant and a second reactant. Exemplary first reactants and second reactants include ?-halohydroxamates and dienes, respectively.Type: ApplicationFiled: August 13, 2014Publication date: November 27, 2014Applicant: Board of Regents of the Nevada System of Higher Education, on behalf of the University of NevadaInventor: Christopher S. Jeffrey
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Publication number: 20140349987Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: December 3, 2012Publication date: November 27, 2014Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
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Patent number: 8853406Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I).Type: GrantFiled: August 5, 2008Date of Patent: October 7, 2014Assignee: Janssen Pharmaceutica NVInventors: Alain Philippe Poncelet, Bruno Schoentjes, Pierre-Henri Storck, Virginie Sophie Poncelet, Carina Leys
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Publication number: 20140296530Abstract: The present invention provides compounds of general formula A useful as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula A can be employed as therapeutics in human and veterinary medicine, where they can be used, for example, for the treatment and prophylaxis of the following diseases: heart failure, dilated cardiomyopathy, platelet inhibitors, cancer and obstructive pulmonary diseases.Type: ApplicationFiled: January 30, 2014Publication date: October 2, 2014Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Budde MAHENDAR, Saidulu MATTAPALLY, Mettu RAVINDER, Sanjay Kumar BANERJEE, Vaidya Jayathirtha RAO
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Publication number: 20140275034Abstract: A method for repelling blood-sucking and biting insects, ticks and mites involving treating an object or area with a blood-sucking and biting insects, ticks and mites repelling effective amount of camphor lactams, verbenone lactams, dolicholactams, dolicholactone, and their precursors, and mixtures thereof, and optionally a carrier.Type: ApplicationFiled: March 14, 2013Publication date: September 18, 2014Inventors: Kamlesh R. Chauhan, Bheema R. Paraselli
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Publication number: 20140275006Abstract: The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia, and so forth.Type: ApplicationFiled: October 25, 2012Publication date: September 18, 2014Applicant: TAISHO PHARMACEUTICAL CO., LTDInventors: Mitsukane Yoshinaga, Takeshi Kuwada, Naoki Miyakoshi, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Youichi Shimazaki
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Publication number: 20140235665Abstract: An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in a ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): where X1 and X2 are preferably both fluorine atoms. The composition can be used to treat constipation without substantive side-effects, such as stomachache.Type: ApplicationFiled: April 30, 2014Publication date: August 21, 2014Applicant: SUCAMPO AGInventor: Ryuji UENO
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Publication number: 20140228321Abstract: The present invention provides compounds of Formula (I): (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 24, 2012Publication date: August 14, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Jennifer X. Qiao, Heather Finlay, Ji Jiang, John Lloyd, Carol Hui Hu, Zulan Pi, George O. Tora, James Neels, Jon J. Hangeland, Todd J. Friends
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Publication number: 20140221357Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 25, 2012Publication date: August 7, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Publication number: 20140200227Abstract: The present disclosure describes thiazole and pyridine carboxamide derivatives, 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: January 14, 2014Publication date: July 17, 2014Applicant: INCYTE CORPORATIONInventors: Chu-Biao Xue, Yun-Long Li, Hao Geng, Jun Pan, Anlai Wang, Ke Zhang, Wenqing Yao, Fenglei Zhang, Jincong Zhuo
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Patent number: 8759341Abstract: This invention relates to novel bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.Type: GrantFiled: February 5, 2010Date of Patent: June 24, 2014Assignee: Bayer Intellectual Property GmbHInventors: Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Mario Lobell, Nicole Teusch, Shendong Yuan
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Publication number: 20140148477Abstract: The present invention provides an animal ectoparasite-controlling agent and a method for preventing or treating infection in animals caused by parasites by using the controlling agent. An animal ectoparasite-controlling agent exhibiting excellent insecticidal activity, and a method for preventing or treating infection in animals caused by parasites by using the controlling agent are obtained by using a compound having a pyrazole ring at the 4-position of the piperidine ring as an active ingredient.Type: ApplicationFiled: July 19, 2012Publication date: May 29, 2014Applicant: OTSUKA AGRITECHNO CO., LTD.Inventors: Yasuhiro Endo, Yuichi Shirai
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Publication number: 20140135500Abstract: The disclosure generally relates to a process for the preparation of compounds of formula I, including synthetic intermediates which are useful in the process.Type: ApplicationFiled: January 16, 2014Publication date: May 15, 2014Inventors: David K. Leahy, Yu Fan, Collin Chan, Lopa V. Desai, Sunil S. Patel, Masano Sugiyama
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Publication number: 20140128365Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, salts, tautomers or prodrugs thereof wherein, A, W, X, Y and R1 are defined herein.Type: ApplicationFiled: November 2, 2012Publication date: May 8, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Jeffrey A. Robl, Shung C. Wu, David S. Yoon
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Publication number: 20140113908Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.Type: ApplicationFiled: December 23, 2013Publication date: April 24, 2014Applicant: NOVARTIS AGInventors: Dominik FEUERBACH, Mathias FREDERIKSEN, Konstanze HURTH, Bernard Lucien ROY, Beatrix WAGNER
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Publication number: 20140107110Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.Type: ApplicationFiled: October 1, 2013Publication date: April 17, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
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Patent number: 8680276Abstract: The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%.Type: GrantFiled: March 4, 2010Date of Patent: March 25, 2014Inventors: Riccardo Motterle, Giancarlo Arvotti, Elisabetta Bergantino, Andrea Castellin, Stefano Fogal, Marco Galvagni
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Publication number: 20140051719Abstract: The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: August 15, 2013Publication date: February 20, 2014Applicant: Simon Fraser UniversityInventors: David Jaro Vocadlo, Ernest John McEachern, Keith Stubbs
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Patent number: 8609686Abstract: The present application relates to novel substituted pyrrolopyridine, pyrazolopyridine and isoxazolopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: December 9, 2008Date of Patent: December 17, 2013Assignee: Bayer Intellectual Property GmbHInventors: Peter Nell, Alexandros Vakalopoulos, Frank Süβmeier, Barbara Albrecht-Küpper, Katja Zimmerman, Joerg Keldenich, Daniel Meibom
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Patent number: 8586570Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.Type: GrantFiled: April 27, 2011Date of Patent: November 19, 2013Assignee: Massachusetts Institute of TechnologyInventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
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Patent number: 8563580Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivurs infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.Type: GrantFiled: September 23, 2009Date of Patent: October 22, 2013Assignee: Georgetown UniversityInventors: Radhakrishnan Padmanabhan, Nagarajan Pattabiraman, Niklaus Mueller, Kuppuswamy Nagarajan
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Publication number: 20130274287Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A and n are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: April 17, 2013Publication date: October 17, 2013Applicant: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Rainer E. Martin, Alexander V. Mayweg, Peter Mohr, Xuefei Tan
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Publication number: 20130267710Abstract: This invention provides novel (1R,4R) 7-oxo-2-azabicyclo[2.2.2]oct-5-ene and derivatives thereof, preferably in substantially enantiomerically enriched forms, intermediates thereto, and processes of their synthesis.Type: ApplicationFiled: January 24, 2013Publication date: October 10, 2013Inventor: Robert M. Moriarty
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Patent number: 8541441Abstract: The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: GrantFiled: July 31, 2009Date of Patent: September 24, 2013Assignee: Simon Fraser UniversityInventors: David Jaro Vocadlo, Ernest John McEachern, Keith Stubbs
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Patent number: 8536164Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, A, R4, n, and R7 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: December 13, 2011Date of Patent: September 17, 2013Assignee: Pfizer Inc.Inventors: Todd W. Butler, Ramalakshmi Y. Chandrasekaran, Scot R. Mente, Chakrapani Subramanyam, Travis T. Wager
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Publication number: 20130237515Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, L1, L2, U and B are as defined in the application, which have valuable pharmacological properties, and in particular modulate the activity of the MCH receptor.Type: ApplicationFiled: February 28, 2013Publication date: September 12, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Thorsten OOST, Ralf LOTZ, Dirk STENKAMP
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Patent number: 8461340Abstract: There are provided, according to the present invention, a method for producing a cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative, the method characterized in that a trans-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative or a mixture of the trans- and cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivatives is isomerized in the presence of an aluminum compound represented by a formula Al(OR1)3 (wherein R1 represents a hydrocarbon group in which a carbon atom having an oxygen atom bonded thereto is a secondary carbon atom). In the process, a ketone compound may be further added, in addition to the aluminum compound.Type: GrantFiled: August 27, 2008Date of Patent: June 11, 2013Assignee: Nippon Soda Co., Ltd.Inventors: Hiroshi Hakuta, Tsutomu Imagawa, Hirohito Oooka, Shinya Fukuhara
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Patent number: 8431707Abstract: The object is to produce an azabicycloalkanol derivative, particularly a cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative which is a useful intermediate for agricultural chemicals or pharmaceutical agents, with a good yield and at an industrially low cost. A diastereomer of an azabicyclo-C6-10-alkanol derivative having a methyne substituted a hydroxyl group as an asymmetric carbon (e.g., a trans-3-substituted-3-azabicyclo[3.2.1]-8-ol derivative) is isomerized in the presence of a transition metal complex, thereby producing an excess amount of a thermodynamically more stable one of diastereomers (e.g., a cis-3-substituted-3-azabicyclo[3.2.1]-8-ol derivative). In this manner, a thermodynamically more stable one of diastereomers of the azabicyclo-C6-10-alkanol derivatives can be produced.Type: GrantFiled: April 24, 2012Date of Patent: April 30, 2013Assignee: Nippon Soda Co., Ltd.Inventors: Hirohito Oooka, Shinya Fukuhara
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Patent number: RE45364Abstract: A chemical compound represented by the formula [I]: (wherein R1 represents a hydroxyl group or the like, m represents 0 or an integer of 1 to 5, R2 represents a halogen atom or the like, k represents 0 or an integer of 1 to 4, R3, R31, R4, R41, R5, R51, R6, R61, and R7 each independently represents a hydrogen atom or the like, X represents an oxygen atom or the like, and n represents 1), a salt, an N-oxide of the chemical compound represented by formula [I], and a pest control agent containing the formula [I] as its active constituent.Type: GrantFiled: January 21, 2014Date of Patent: February 3, 2015Assignee: Nippon Soda Co., Ltd.Inventors: Isami Hamamoto, Jun Takahashi, Makio Yano, Daisuke Hanai, Takao Iwasa