Spiro Ring System Patents (Class 514/278)
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Patent number: 10174050Abstract: The present invention concerns a spiroisoxazoline compound of general formula (I): in which m and n are 0 or 1, R1 represents, inter alia, an optionally substituted alkyl chain, in particular substituted with fluorine or with a cyclic group, and R2 is chosen from phenyl and optionally substituted benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and the heterocycles having 5 or 6 vertices comprising at least one atom chosen from S, N and O. The present invention also concerns the use of this compound as a drug, in particular in the treatment of bacterial and mycobacterial infections such as tuberculosis in combination with an antibiotic that is active against bacteria and/or mycobacteria, said compound potentiating the activity of said antibiotic.Type: GrantFiled: December 20, 2013Date of Patent: January 8, 2019Assignee: Universite de Droit et de la Sante de Lille 2Inventors: Nicolas Willand, Benoit Deprez, Alain Baulard, Priscille Brodin, Matthieu Frederik Desroses, Laurence Agouridas-Dutot
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Patent number: 10150769Abstract: Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.Type: GrantFiled: June 12, 2018Date of Patent: December 11, 2018Assignee: Aptinyx Inc.Inventor: M. Amin Khan
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Patent number: 10072017Abstract: The invention relates to a compound of Formula I or IA compositions comprising compounds of Formula I or IA, and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:Type: GrantFiled: December 28, 2016Date of Patent: September 11, 2018Assignee: Flatley Discovery Lab, LLCInventors: Michael P. Zawistoski, Asmita Deshpande, Bridget M. Cole
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Patent number: 10035816Abstract: The present invention declares a kind of compound to treat respiratory syncytial virus infection and its preparation method and application. The compound stated is cyclopamine's chemical analogs, has the property of inhibiting respiratory syncytial virus replication, and does not have the property of inhibiting Hedgehog signaling pathways. The preparation method stated is to get the cyclopamine's chemical analogs through drug chemical synthesis, then to screen the analogs with two parallel in vitro experiment. The compound described can be used to treat respiratory virus infection, paramyxovirus, respiratory syncytial virus infection, capillary bronchitis/pneumonia/tympanitis caused by respiratory syncytial virus. Furthermore, the compound described never cause the side effects of fetal malformation, and it overcame the teratogenicity of cyclopamine, and filled the gap of anti-human respiratory syncytial virus drug, especially of the field of pediatric drug.Type: GrantFiled: December 7, 2017Date of Patent: July 31, 2018Assignee: SHANDONG UNIVERSITYInventors: Ralf Altmeyer, Jingjing Cao
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Patent number: 10030021Abstract: In one aspect, the invention provides compounds of Formula I: (I) and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, Y, Za are defined as set forth in the disclosure. The invention also provides compounds of any one of Formulae II to VII, IA to IC, and IIA to IIC, and pharmaceutically acceptable salts and solvates thereof. Other aspects of the invention include the use of compounds of Formulae I to VII, IA to IC, and IIA to IIC, and pharmaceutically acceptable salts and solvates thereof for the treatment of disorders responsive to modulation of one or more opioid receptors. In certain embodiments, the Compounds of the Invention are useful for treating pain.Type: GrantFiled: May 26, 2015Date of Patent: July 24, 2018Assignee: Purdue Pharma L.P.Inventors: Mark A. Youngman, Laykea Tafesse, R. Richard Goehring, Jianming Yu
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Patent number: 10011601Abstract: The present invention relates to compounds according to Formula 1 and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancer, lymphocyte homing, chronic inflammation, neuropathic pain, fibrotic diseases, thrombosis, and cholestatic pruritus, mediated at least in part by ATX.Type: GrantFiled: April 3, 2015Date of Patent: July 3, 2018Assignee: X-Rx, Inc.Inventors: Lee Babiss, Matthew Clark, Anthony D. Keefe, Mark J. Mulvihill, Haihong Ni, Louis Renzetti, Frank Ruebsam, Ce Wang, Zhifeng Xie, Ying Zhang
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Patent number: 10000502Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the antagonism of one or more androgen receptor types. Such compounds are represented by Formula (I) as follows: wherein R1 and G are defined herein.Type: GrantFiled: January 11, 2017Date of Patent: June 19, 2018Assignee: Janssen Pharmaceutica NVInventors: Gilles Bignan, Peter J Connolly, Ian Hickson, Lieven Meerpoel, Vineet Pande, Zhuming Zhang, Jonathan Branch, Christian Rocaboy, Luis B Trabalón Escolar
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Patent number: 9957238Abstract: The present invention relates to the compound of the formula: or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.Type: GrantFiled: March 1, 2017Date of Patent: May 1, 2018Assignee: Parion Sciences, Inc.Inventor: Michael R. Johnson
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Patent number: 9956193Abstract: Sustained release compositions of sotalol, or a pharmaceutically acceptable salt thereof, are provided. In certain examples, sotalol, or a pharmaceutically acceptable salt thereof, may be administered in an effective amount to provide a therapeutic effect to a patient, such as, for example, a patient suffering from a cardiac disorder. In some examples, sotalol combined with a sustained release system may be administered to provide a sustained release of sotalol for a desired period, e.g., at least about 24 hours.Type: GrantFiled: March 2, 2017Date of Patent: May 1, 2018Assignee: The Roshni Singh 2015 TrustInventor: Bramah N. Singh
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Patent number: 9943508Abstract: There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of Alzheimer type dementia in combination with an acetyl choline esterase inhibitor (AChEI) and pharmaceutical compositions comprising (a) a 5HT3 receptor antagonist, a dopamine antagonist, a H1-receptor antagonist, a cannabinoid agonist, aprepitant or casopitant as an antiemetic agent and (b) an acetylcholine esterase inhibitor are also described.Type: GrantFiled: July 17, 2017Date of Patent: April 17, 2018Assignee: Chase Pharmaceuticals CorporationInventors: Thomas N. Chase, Kathleen E. Clarence-Smith
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Patent number: 9908883Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: GrantFiled: August 15, 2016Date of Patent: March 6, 2018Assignee: Pfizer Inc.Inventors: Mary Didiuk, Robert Lee Dow, David Andrew Griffith
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Patent number: 9873699Abstract: An anti-cancer agent having the formula: wherein Ph is a phenyl group and Ar is an aromatic group independently selected from the group consisting of phenyl, 2-bromophenyl, 4-bromophenyl, 2-chlorophenyl, 2,4, dichlorophenyl, 4-chlorophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2 methoxyphenyl, 3-methoxyphenyl, 4-methoxyphenyl, and 3-nitrophenyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 17, 2017Date of Patent: January 23, 2018Assignee: KING SAUD UNIVERSITYInventors: Abdulrahman I. Almansour, Natarajan Arumugam, Raju Suresh Kumar, Periasamy Vaiyapuri Subbarayan, Ali Abdullah Alshatwi, Jegan Athinarayanan
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Patent number: 9868754Abstract: The present invention relates to methods of treating immune disorders and/or inflammation using certain modulator compounds. In one embodiment, the present invention provides a method of treating an immune and inflammatory disorders disorder by administering a composition comprising a therapeutically effective dosage of an ascaroside compound, or a mixture of ascaroside compounds, or a mixture containing at least one ascaroside.Type: GrantFiled: August 8, 2012Date of Patent: January 16, 2018Assignees: California Institute of Technology, Boyce Thompson Institute for Plant ResearchInventors: Andrea Choe, Paul W. Sternberg, Frank C. Schroeder, Stephan H. Von Reuss
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Patent number: 9845330Abstract: The present invention relates to newer generation of triazoles, tetrazoles, isoxazoles, urea and sulphonamide functionalities containing 6-nitro-2,3-dihydronitroimidazooxazoles agents of formula 1, their method of preparation, and their use as drugs for treating Mycobacterium tuberculosis, MDR-TB and XDR-TB either alone or in combination with other anti-tubercular agents. In the present invention, new generation 6-nitro-2,3-dihydronitroimidazooxazoles agents also show acceptable pharmacokinetic properties and synergistic or additive effects with known anti-tubercular drugs.Type: GrantFiled: March 31, 2014Date of Patent: December 19, 2017Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Parvinder Pal Singh, Gurunadham Munagala, Reddy Yempalla Kushalava, Inshad Ali Khan, Nitin Pal Kalia, Vikrant Singh Rajput, Amit Nargotra, Sanghapal Damodhar Sawant, Ram Asray Vishwakarma
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Patent number: 9828357Abstract: The present invention provides compounds having a Toll-like receptor 4 (TLR4) signaling inhibitory action useful as preventive and therapeutic drugs of inflammatory disease and/or central nervous system disease or diseases such as chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver injury, ischemia-reperfusion injury (IRI) and the like. The present invention relates to a compound represented by formula (I) and a salt thereof: wherein, each symbol is explained in greater detail in the specification.Type: GrantFiled: November 21, 2016Date of Patent: November 28, 2017Assignee: Takeda Pharmaceutical Company LimitedInventors: Toshitake Kobayashi, Morihisa Saitoh, Yasufumi Wada, Hiroshi Nara, Nobuyuki Negoro, Taisuke Katoh, Masashi Yamasaki, Takahiro Tanaka, Naomi Kitamoto
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Patent number: 9809593Abstract: Use of a tetramic acid compound according to formula (I) or (I?) with a second nematicide as a treatment for crop plants to combat and control nematodes in the soil of said crop plants.Type: GrantFiled: May 21, 2014Date of Patent: November 7, 2017Assignee: Syngenta Participations AGInventors: Fabienne Hatt, Anke Buchholz
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Patent number: 9771365Abstract: A compound of the formula I wherein the substituents are as defined in claim 1, are useful as a pesticides.Type: GrantFiled: May 28, 2015Date of Patent: September 26, 2017Assignee: Syngenta Participations AGInventors: Michel Muehlebach, Thomas Pitterna, Jerome Yves Cassayre, Andrew Edmunds, Camilla Corsi, Myriem El Qacemi, Roger Graham Hall, Andre Jeanguenat, Andre Stoller, Christopher Richard Godfrey, Jurgen Harry Schaetzer, Olivier Loiseleur, Peter Maienfisch, Neil Brian Carter
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Patent number: 9718845Abstract: 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: GrantFiled: August 1, 2016Date of Patent: August 1, 2017Assignee: Bristol-Myers Squibb CompanyInventors: David K. Leahy, Yu Fan, Collin Chan, Lopa V. Desai, Sunil S. Patel, Masano Sugiyama
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Patent number: 9708289Abstract: Provided are imidazolidinedione compounds of formula (I), processes for preparation, uses and pharmaceutically compositions thereof. Said imidazolidinedione compounds possess androgen receptor antagonist activity and can be used for preventing and treating diseases and disorders related to androgen receptor, such as prostate cancer, alopecia, hair regeneration, acne and adolescent acne.Type: GrantFiled: May 27, 2014Date of Patent: July 18, 2017Assignee: Hinova Pharmaceuticals Inc.Inventors: Yuanwei Chen, Yu Gong
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Patent number: 9708297Abstract: The present invention provides a compound of Formula II: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 5, 2016Date of Patent: July 18, 2017Assignee: Eli Lilly and CompanyInventors: David Andrew Coates, Kevin Charles Fortner, Steven Marc Massey, Jason Kenneth Myers, Antonio Navarro, Miles Goodman Siegel, Russell Dean Stucky
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Patent number: 9686992Abstract: A pesticidal mixture comprising as active ingredient a mixture of component A and component B, wherein component A is a compound of formula (I) in which Q is i or ii wherein X, Y and Z, m and n, A, G, and R, are as defined as in claim 1, and component B is a compound selected from the insecticides as defined in claim 1. The present invention also relates to methods of using said mixtures for the control of plant pests.Type: GrantFiled: January 17, 2013Date of Patent: June 27, 2017Assignee: Syngenta Participations AGInventors: Anke Buchholz, Fabienne Hatt, Alfred Rindlisbacher, Michel Muehlebach
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Patent number: 9670183Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula (1), or a salt thereof, wherein Q, R1, R2, R3 and R4 are as defined herein.Type: GrantFiled: February 6, 2015Date of Patent: June 6, 2017Assignee: Heptares Therapeutics LimitedInventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Michael Alistair O'Brien, Mark Pickworth, Mark David Rackham, Benjamin Gerald Tehan, Barry John Teobald
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Patent number: 9670154Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: GrantFiled: July 24, 2015Date of Patent: June 6, 2017Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Colin Zhang, Brian W. Metcalf, Chunhong He, Ding-Quan Qian
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Patent number: 9656993Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.Type: GrantFiled: December 18, 2015Date of Patent: May 23, 2017Assignee: Theravance Biopharma R&D IP, LLCInventors: Sabine Axt, Timothy J. Church
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Patent number: 9656967Abstract: A production method of the present invention is a method for producing a halohydantoin compound in which method a composition including a halohydantoin compound and an impurity is treated, the method including the step of adding the composition to a mixed solvent of water and an organic solvent and washing the composition.Type: GrantFiled: November 15, 2013Date of Patent: May 23, 2017Assignee: NIPPOH CHEMICALS CO., LTD.Inventors: Naoki Fujiwara, Keisuke Takahashi
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Patent number: 9637495Abstract: The present invention provides a compound of Formula II: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 5, 2016Date of Patent: May 2, 2017Assignee: Eli Lilly and CompanyInventors: David Andrew Coates, Kevin Charles Fortner, Richard Duane Johnston, Steven Marc Massey, Jason Kenneth Myers, Qing Shi, Miles Goodman Siegel
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Patent number: 9629828Abstract: Treatment of traveler's diarrhea using in subjects having hepatic encephalopathy using gastrointestinal specific antibiotics is disclosed. One example of a gastrointestinal specific antibiotic is rifaximin.Type: GrantFiled: January 26, 2015Date of Patent: April 25, 2017Assignee: Salix Pharmaceuticals, Ltd.Inventors: William Forbes, Enoch Bortey
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Patent number: 9625475Abstract: The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: GrantFiled: March 19, 2010Date of Patent: April 18, 2017Assignee: AbbVie Inc.Inventors: Michael R. Schrimpf, Chih-Hung Lee, Tao Li, Gregory A. Gfesser, Kathleen H. Mortell, Ramin Faghih, Diana L. Nersesian, Kevin B. Sippy, William H. Bunnelle, Marc Scanio, Lei Shi, Murali Gopalakrishnan, Diana L. Donnelly-Roberts, Min Hu
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Patent number: 9603367Abstract: A pesticidal mixture comprising as active ingredient a mixture of component A and component B, wherein component A is a compound of formula (I), in which Q is i or ii wherein X, Y and Z, m and n, A, G, and R, are as defined as in claim 1, and component B is a compound selected from the insecticides as defined in claim 1. The present invention also relates to methods of using said mixtures for the control of plant pests.Type: GrantFiled: January 17, 2013Date of Patent: March 28, 2017Assignee: Syngenta Participations AGInventors: Anke Buchholz, Fabienne Hatt, Alfred Rindlisbacher, Michel Muehlebach
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Patent number: 9598412Abstract: This invention relates to spiroindoline compounds for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: GrantFiled: October 14, 2014Date of Patent: March 21, 2017Assignee: Intervet Inc.Inventors: Jürgen Lutz, Sandra Koch, Manfred Uphoff, Anja Regina Heckeroth, Britta von Oepen, Ulrich Sondern, Christophe Pierre Alain Chassaing
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Patent number: 9592228Abstract: Methods of inhibiting release of a proinflammatory cytokine from a macrophage are provided. The methods comprise treating the macrophage with a cholinergic agonist in an amount sufficient to decrease the amount of the proinflammatory cytokine that is released from the macrophage, wherein the cholinergic agonist is selective for an ?7 nicotinic receptor. Methods for inhibiting an inflammatory cytokine cascade in a patient are also provided. The methods comprise treating the patient with a cholinergic agonist in an amount sufficient to inhibit the inflammatory cytokine cascade, wherein the cholinergic agonist is selective for an ?7 nicotinic receptor. Methods for determining whether a compound is a cholinergic agonist reactive with an ?7 nicotinic receptor are also provided. The methods comprise determining whether the compound inhibits release of a proinflammatory cytokine from a mammalian cell.Type: GrantFiled: September 3, 2015Date of Patent: March 14, 2017Assignee: The Feinstein Institute for Medical ResearchInventors: Kevin J. Tracey, Hong Wang
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Patent number: 9585880Abstract: The present invention relates to tertiary amines of formula (I) for use in therapy, particularly for use in treating cardiovascular disorders. The compounds have been found to regulate phospholamban phosphorylation by interfering with the A-kinase anchor protein 18delta (AKAP18?) binding to the PKA substrate phospholamban. The compounds share a tri(alkylaryl/alkylheteroaryl) amine structure.Type: GrantFiled: November 20, 2014Date of Patent: March 7, 2017Assignee: Universitetet I OsloInventors: Jo Klaveness, Kjetil Tasken
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Patent number: 9499545Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: September 12, 2014Date of Patent: November 22, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman
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Patent number: 9453023Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.Type: GrantFiled: May 5, 2014Date of Patent: September 27, 2016Assignee: SanofiInventor: Zhongli Gao
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Patent number: 9409916Abstract: The present invention is directed to piperidinone carboxamide spirohydantoin derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: March 14, 2012Date of Patent: August 9, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Justin Belardi
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Patent number: 9345692Abstract: Pharmaceutical formulations containing salts of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl]-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.Type: GrantFiled: March 19, 2013Date of Patent: May 24, 2016Assignee: OPKO Health, Inc.Inventors: Zhihui Qiu, Larisa Reyderman
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Patent number: 9320729Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient, which is selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient, which is a propionic acid derivative selected from the group consisting of ibuprofen, naproxen, ketoprofen, flurbiprofen, fenoprofen, fenbufen, suprofen, pirprofen, indoprofen, tiaprofenic acid, oxaprozin, ibuproxam, flunoxaprofen, alminoprofen, naproxcinod, and the physiologically acceptable salts thereof.Type: GrantFiled: May 13, 2013Date of Patent: April 26, 2016Assignee: Gruenenthal GmbHInventors: Stefanie Frosch, Klaus Linz, Klaus Schiene
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Patent number: 9289416Abstract: A pharmaceutical dosage form for administration twice daily, once daily or less frequently, which contains 6?-fluoro-(N-methyl- or N,N-dimethyl)-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine or a physiologically acceptable salt thereof.Type: GrantFiled: December 22, 2014Date of Patent: March 22, 2016Assignee: Gruenenthal GmbHInventors: Nadja Gruening, Marc Schiller, Ashish Hemani, Chris Kirby, Ingo Friedrich, John Bothmer, Andreas Scholz
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Patent number: 9278092Abstract: There is described a method for increasing the maximal tolerated close and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of Alzheimer type dementia in combination with an acetyl choline esterase inhibitor (AChEI) and pharmaceutical compositions comprising (a) a 5HT3 receptor antagonist, a dopamine antagonist, a H1-receptor antagonist, a cannabinoid agonist, aprepitant or casopitant as an antiemetic agent and (b) an acetylcholine esterase inhibitor are also described.Type: GrantFiled: September 18, 2014Date of Patent: March 8, 2016Assignee: Chase Pharmaceuticals CorporationInventors: Thomas N. Chase, Kathleen E. Clarence-Smith
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Patent number: 9273048Abstract: The application is directed to compounds of Formula I?-A and especially to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein R1a-R5a, Y, Za are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I?-A, and especially compounds of Formula I-A, to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.Type: GrantFiled: January 28, 2015Date of Patent: March 1, 2016Assignee: Purdue Pharma L.P.Inventors: R. Richard Goehring, Laykea Tafesse, Mark A. Youngman
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Patent number: 9273064Abstract: Compounds of the general formula I wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—; R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3; X is a bond, —CH2—, or —NH—; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; and R4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.Type: GrantFiled: December 30, 2014Date of Patent: March 1, 2016Assignee: LEO PHARMA A/SInventor: Simon Feldbaek Nielsen
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Patent number: 9227973Abstract: The present invention is directed to pyridine derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: May 3, 2013Date of Patent: January 5, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair
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Patent number: 9221838Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: GrantFiled: December 23, 2010Date of Patent: December 29, 2015Assignee: ALMAC DISCOVERY LIMITEDInventors: Lixin Zhang, Graham Peter Trevitt, Hugues Miel, Frank Burkamp, Timothy Harrison, Andrew John Wilkinson, Charles-Henry Fabritius
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Patent number: 9206198Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.Type: GrantFiled: December 15, 2014Date of Patent: December 8, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Fa-Xiang Ding, Shuzhi Dong, Jessica Frie, Xin Gu, Jinlong Jiang, Alexander Pasternak, Haifeng Tang, Zhicai Wu, Yang Yu, Takao Suzuki
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Patent number: 9181214Abstract: The present invention relates to novel compounds of formula (A) and (B) as modulators of GPR-119, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of GPR-119 mediated diseases or disorders with them.Type: GrantFiled: June 8, 2012Date of Patent: November 10, 2015Assignee: RHIZEN PHARMACEUTICALS SAInventors: Dhanapalan Nagarathnam, Swaroop Kumar V. S. Vakkalanka, Srikant Viswanadha, Gayatri S. Merikapudi
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Patent number: 9168248Abstract: Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.Type: GrantFiled: February 16, 2010Date of Patent: October 27, 2015Assignee: Merck Canada Inc.Inventors: Nicolas Lachance, Jean-Philippe Leclerc, Chun Sing Li, Oscar Miguel Moradei
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Patent number: 9145416Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: GrantFiled: September 19, 2014Date of Patent: September 29, 2015Assignee: Pfizer Inc.Inventors: Mary Theresa Didiuk, Robert Lee Dow, David Andrew Griffith
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Patent number: 9139587Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: GrantFiled: May 9, 2014Date of Patent: September 22, 2015Assignee: Pfizer Inc.Inventors: Scott William Bagley, David Andrew Griffith, Daniel Wei-Shung Kung
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Patent number: 9126941Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.Type: GrantFiled: April 17, 2012Date of Patent: September 8, 2015Assignee: The Regents of the University of CaliforniaInventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Chris Tran, John Wongvipat
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Patent number: 9115148Abstract: 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: GrantFiled: November 22, 2013Date of Patent: August 25, 2015Assignee: DAC S.R.L.Inventors: Mario Varasi, Florian Thaler, Agnese Abate, Giacomo Carenzi, Ciro Mercurio, Saverio Minucci