1,4-diazine As One Of The Cyclos Patents (Class 514/249)
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Patent number: 9921230Abstract: This invention relates to compositions and methods for diagnosing and treating concussion/mTBI.Type: GrantFiled: October 8, 2015Date of Patent: March 20, 2018Assignee: Rhode Island HospitalInventors: Adam Chodobski, Joanna Szmydynger-Chodobska
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Patent number: 9907783Abstract: The present invention includes compositions and methods for the treatment of skin conditions by administration of a cyclolignan such as picropodophyllin and/or a derivative, metabolite, analog, prodrug, pharmaceutically acceptable salt, or hydrate thereof.Type: GrantFiled: May 9, 2014Date of Patent: March 6, 2018Assignee: m.Alphabet 2, LLCInventors: Howard Fein, Joshua M. Berlin
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Patent number: 9868741Abstract: The present invention provides a compound of Formula I: useful for treating chronic kidney disease and diabetic kidney disease.Type: GrantFiled: February 3, 2017Date of Patent: January 16, 2018Assignee: Eli Lilly and CompanyInventor: Cynthia Darshini Jesudason
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Patent number: 9868708Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: GrantFiled: October 19, 2015Date of Patent: January 16, 2018Assignee: BioEnergenix LLCInventors: John M. McCall, Donna L. Romero, John McKearn, Michael Clare
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Patent number: 9855215Abstract: A Methotrexate composition for oral administration is provided comprising a pharmaceutically acceptable salt of Methotrexate and an aqueous carrier agent. The Methotrexate salt is substantially or completely soluble in the aqueous carrier agent, forming an aqueous solution. There is also provided a method of manufacturing a Methotrexate composition for oral administration, comprising mixing a pharmaceutically acceptable salt of Methotrexate with an aqueous carrier agent until the Methotrexate salt is substantially or completely soluble in the carrier agent to form an aqueous solution.Type: GrantFiled: February 9, 2016Date of Patent: January 2, 2018Assignee: Rosemont Pharmaceuticals Ltd.Inventors: Carl Tierney, Stacey Powell, Peter Braybrooke, Geraint Jones
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Patent number: 9845326Abstract: The present invention relates to novel 3,4-dihydro-pyrrolo[1,2-a]pyrazin-1-ylamine derivatives of formula (I) wherein R1, R2, R3, R4, X1, X2, X3, X4, L, and Ar are defined in the specification, as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.Type: GrantFiled: March 7, 2012Date of Patent: December 19, 2017Assignee: Janssen Pharmaceutica NVInventors: Andrés Avelino Trabanco-Suárez, Francisca Delgado-Jiménez
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Patent number: 9840507Abstract: The present invention relates to novel 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine inhibitors of beta-secretase, having the structure shown in Formula (I) wherein R1, R2, R3, R4, X1, X2, X3, X4, L and Ar are defined in the specification. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebrovascular amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.Type: GrantFiled: December 21, 2011Date of Patent: December 12, 2017Assignee: Janssen Pharmaceutica, NVInventors: Andrés Avelino Trabanco-Suárez, Francisca Delgado-Jiménez, Juan Antonio Vega Ramiro, Gary John Tresadern, Henricus Jacobus Maria Gijsen, Daniel Oehlrich
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Patent number: 9834551Abstract: The present invention relates to compounds described by Formula I: salts thereof, their synthesis, and their use as ITK and JAK3 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and or disorders such disease associated with abnormal cell growth such as autoimmune, inflammation, rheumatoid arthritis, systemic lupus erythematosus, atherosclerosis, ulcerative colitis, psoriatic arthritis, psoriasis, Crohn's, metabolic and cancer diseases. The present invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions and processes for preparing the compounds of the invention.Type: GrantFiled: October 27, 2015Date of Patent: December 5, 2017Assignee: ARRIEN PHARMACEUTICALS LLCInventors: Hariprasad Vankayalapati, Venkatakrishnareddy Yerramreddy, Paramareddy Gangireddy, Rajendra P. Appalaneni
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Patent number: 9822130Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 19, 2015Date of Patent: November 21, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Raphaelle Berger, Guizhen Dong, Subharekha Raghavan, Zhiqiang Yang
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Patent number: 9815768Abstract: Position-1 halogen can be selectively reduced by reacting a compound represented by formula (3): [wherein X represents a chlorine atom, a bromine atom, or an iodine atom] with halogen in the presence of a heterogeneous transition metal catalyst to produce 2-(halogenomethyl)-1-methyl-3-nitrobenzene represented by formula (1): [wherein the symbol is as defined above].Type: GrantFiled: February 16, 2015Date of Patent: November 14, 2017Assignee: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Satoru Ujita, Takashi Miyamoto
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Patent number: 9808445Abstract: In its many embodiments, the present invention provides a novel class of benzamide compounds represented by Formula (I) or pharmaceutically acceptable salts or solvates thereof, or pharmaceutical compositions comprising one or more said compounds or pharmaceutically acceptable salts or solvates thereof, and methods for using said compounds or pharmaceutically acceptable salts or solvates thereof for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.Type: GrantFiled: April 10, 2015Date of Patent: November 7, 2017Assignees: Merck Sharp & Dohme Corp., Mochida Pharmaceutical Co., Ltd.Inventors: Isao Sakurada, Tomokazu Hirabayashi, Yoshitaka Maeda, Hiroshi Nagasue, Takashi Mizuno, Jiayi Xu, Ting Zhang, Cameron Smith, Dann Parker
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Patent number: 9801878Abstract: The present invention provides quinoline derivatives of formula I that are PDE10A enzyme inhibitors, and as such are useful to treat neurodegenerative and psychiatric disorders. Especially, the invention provides compounds that are highly selective for PDE10A over other PDE subtypes. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.Type: GrantFiled: November 13, 2015Date of Patent: October 31, 2017Assignee: H. Lundbeck A/SInventors: Jan Kehler, Jacob Nielsen, Ask Püschl, John Paul Kilburn, Morten Langgård
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Patent number: 9796721Abstract: In some embodiments, the invention relates to crystalline solid forms, including hydrates, polymorphs, and salt forms, of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention relates to amorphous solid forms of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention also relates to pharmaceutical compositions containing the solid forms, and methods for treating conditions or disorders by administering to a subject a pharmaceutical composition that includes the forms, including pharmaceutical compositions and methods for overcoming the effects of acid reducing agents.Type: GrantFiled: July 1, 2016Date of Patent: October 24, 2017Assignee: Acerta Pharma B.V.Inventors: Fritz Blatter, Tim Ingallinera, Tjeerd Barf, Edwin Aret, Cecile Krejsa, Jerry Evarts
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Patent number: 9783542Abstract: The present invention provides a novel process for the purification of alpha-propargylhomoterephthalic acid dimethyl ester substantially free of homoterephthalic acid dimethyl ester. The present invention also provides a novel process for the purification of pralatrexate.Type: GrantFiled: November 1, 2013Date of Patent: October 10, 2017Assignee: Hetero Research FoundationInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Katham Srinivasa Reddy, Bandi Vamsi Krishna
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Patent number: 9783536Abstract: A compound represented by Formula [1](in the formula, Z1 represents N, CH, or the like; X1 represents NH or the like; R1 represents a heteroaryl group or the like; each of R2, R3, and R4 represents a hydrogen atom, a halogen atom, an alkoxy group, or the like; and R5 represents a heteroaryl group or the like) or salt thereof.Type: GrantFiled: July 9, 2015Date of Patent: October 10, 2017Assignee: FUJIFILM CorporationInventors: Hidetomo Furuyama, Hideki Kurihara, Takahiro Terao, Daisuke Nakagawa, Shintaro Tanabe, Takayuki Kato, Masahiko Yamamoto, Shinichiro Sekine, Tomoyuki Mashiko, Shinsuke Inuki, Satoshi Ueda
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Patent number: 9782399Abstract: Pharmaceutical compositions that bind to a predicted FK506 Binding Protein 52 (FKBP52) interaction surface on the androgen receptor hormone binding domain, otherwise known as FKBP52 Targeting Agents (FTAs) are provided. These compositions of the present invention are found to specifically recognize the FKBP52 regulatory surface on the androgen receptor and inhibit FKBP52 from functionally interacting with the androgen receptor. Compositions comprising the pharmaceutical composition, as well as methods of use, treatment and screening are also provided.Type: GrantFiled: December 1, 2015Date of Patent: October 10, 2017Assignees: The United States of America, as represented by The Secretary, Department of Health and Human Services, The Regents of the University of California, The Board of Regents of The University of Texas SystemInventors: Leonard M. Neckers, Marc B. Cox, Jane B. Neckers, Yeong Sang Kim, Aki Iwai, Yangmin Ning, Johanny Kugelman-Tonos, Heather A. Balsiger, Robert Fletterick
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Patent number: 9776997Abstract: The present application relates to novel 3-aryl-substituted imidazo[1,2-a]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.Type: GrantFiled: June 4, 2014Date of Patent: October 3, 2017Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Alexandros Vakalopoulos, Markus Follmann, Ingo Hartung, Philipp Buchgraber, Alexey Gromov, Niels Lindner, Frank Wunder, Johannes-Peter Stasch, Gorden Redlich, Volkhart Min-Jian Li
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Patent number: 9770464Abstract: The present invention relates to methods for treating optic disorders or for reducing or alleviating the signs, symptoms, or pathological conditions related to such optic disorders. In particular, methods are provided for treating optic disorders, or reducing the symptoms thereof, the methods involving the administration of one or more downstream folate compounds and/or methyl-B12. In one particular embodiment, the method comprises administration of L-methylfolate. In other embodiments, the method involves administering both L-methylfolate and methyl-B12. In still further embodiments, the method further involves reducing dietary intake of folic acid. In certain embodiments, the method further involves identifying a subject organism with a malfunction in one or more of the folate or B4 cycles. In certain embodiments, such a malfunction is one or more of the C677T and A1298C mutations.Type: GrantFiled: August 14, 2014Date of Patent: September 26, 2017Inventor: Brian W Buell
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Patent number: 9765073Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I wherein X, R1, R2a, R2b, R4a, R4b, R5a, R5b, R6, R7, R10, R11, and y are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: December 19, 2016Date of Patent: September 19, 2017Assignee: PFIZER INC.Inventors: Martin Youngjin Pettersson, Christopher William am Ende, Douglas Scott Johnson, Gregory Wayne Kauffman, Antonia Friederike Stepan, Patrick Robert Verhoest
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Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders
Patent number: 9751877Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: October 7, 2015Date of Patent: September 5, 2017Assignee: PFIZER INC.Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William am Ende, Michael Eric Green, Nandini Chaturbhai Patel, Cory Michael Stiff, Tuan Phong Tran, Gregory Wayne Kauffman, Antonia Friederike Stepan, Patrick Robert Verhoest -
Patent number: 9750881Abstract: Injection systems comprising a powered injector and one or more hazardous agents are disclosed.Type: GrantFiled: August 22, 2016Date of Patent: September 5, 2017Assignee: Antares Pharma, Inc.Inventors: Paul K. Wotton, Peter L. Sadowski, John W. Hayes
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Patent number: 9746477Abstract: Improved methods are provided for treating cancer patients, particularly patients suffering from lung cancer. Methods are provided for identifying whether a lung tumor will be responsive to treatment with a therapeutic regimen that includes pemetrexed and optionally includes cisplatin. A specific FR-? fragment peptide and a specific GART fragment peptide are precisely detected and quantitated by SRM-mass spectrometry directly in lung tumor cells collected from lung tumor tissue that was obtained from a cancer patient and compared to reference levels in order to determine if the lung cancer patient will positively respond to treatment with the c therapeutic regimen.Type: GrantFiled: August 1, 2016Date of Patent: August 29, 2017Assignees: Expression Pathology, Inc., West Virginia UniversityInventors: Todd Hembrough, Fabiola Cecchi, Eunkyung An, Manish Monga
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Patent number: 9737535Abstract: Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a TOR kinase inhibitor and an effective amount a second active agent to a patient having a cancer, wherein the TOR kinase inhibitor is a compound of formula (I): and pharmaceutically acceptable salts, clathrates, solvates, stereoisomers, tautomers, metabolites, isotopologues and prodrugs thereof.Type: GrantFiled: April 15, 2015Date of Patent: August 22, 2017Assignee: Signal Pharmaceuticals, LLCInventors: Kimberly Elizabeth Fultz, Tam Minh Tran, Shuichan Xu, Weiming Xu
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Patent number: 9725421Abstract: Described herein are kinase inhibitors represented by Formula I: and pharmaceutical compositions thereof, for use in the treatment of cancer.Type: GrantFiled: November 12, 2013Date of Patent: August 8, 2017Assignee: NEUPHARMA, INC.Inventors: Xiangping Qian, Yong-liang Zhu
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Patent number: 9718824Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.Type: GrantFiled: April 15, 2015Date of Patent: August 1, 2017Assignee: Signal Pharmaceuticals, LLCInventor: Kevin Klopfer
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Patent number: 9713616Abstract: Compositions comprising a calcium salt of L-leucovorin may be prepared that have a higher concentration of L-leucovorin than may be prepared using racemic leucovorin under similar conditions. Thus, some pharmaceutical compositions described herein may comprise a calcium salt of L-leucovorin at a relatively high concentration, such as at least about 15 mg/mL. Such a composition may be a stable aqueous solution, and may have near physiological pH, such as about 6 to about 8. Some pharmaceutical compositions may be substantially free of D-leucovorin, and may contain either: a) no EDTA, or b) less than about 1 mg/ml of EDTA. These compositions may be prepared, for example, by sonicating a mixture comprising the solid calcium salt of L-leucovorin and water. In some compositions, a calcium salt of L-leucovorin may be sufficiently soluble that it does not precipitate when it is injected.Type: GrantFiled: August 6, 2013Date of Patent: July 25, 2017Assignee: Spectrum Pharmaceuticals, Inc.Inventors: Pramod Kumar Gupta, Bahman Shimiaei, Shaofeng Xie
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Patent number: 9695176Abstract: The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).Type: GrantFiled: October 14, 2013Date of Patent: July 4, 2017Assignee: Bristol-Myers Squibb CompanyInventor: Andrew P. Degnan
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Patent number: 9695168Abstract: The present invention is directed to imidazo[1,5-a]pyridine and imidazo[1,5-a]pyrazine derivatives of Formula I, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.Type: GrantFiled: July 9, 2015Date of Patent: July 4, 2017Assignee: Incyte CorporationInventors: Liangxing Wu, Leah C. Konkol, Neil Lajkiewicz, Liang Lu, Meizhong Xu, Wenqing Yao, Zhiyong Yu, Colin Zhang, Chunhong He
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Patent number: 9695180Abstract: The present invention is directed to imidazo[1,2-a]pyrazine derivatives of Formula I, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.Type: GrantFiled: July 9, 2015Date of Patent: July 4, 2017Assignee: Incyte CorporationInventors: Liangxing Wu, Joel R. Courter, Chunhong He, Jingwei Li, Liang Lu, Yaping Sun, Xiaozhao Wang, Wenqing Yao, Colin Zhang, Jincong Zhuo
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Patent number: 9688669Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.Type: GrantFiled: October 6, 2014Date of Patent: June 27, 2017Assignee: Bristol-Myers Squibb CompanyInventors: Andrew P. Degnan, Darrell Maxwell, Matthew D. Hill, Haiquan Fang, Michael F. Parker, Fukang Yang, Joanne J. Bronson, John E. Macor
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Patent number: 9687492Abstract: Disclosed are methods for treating a cancer in a subject (e.g., a human) in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of formula I: or a pharmaceutically acceptable salt thereof. The subject may be very high risk or high risk for the cancer. The subject who has the cancer may also be refractory to at least one chemotherapy treatment, or is in relapse after treatment with chemotherapy, or both. The cancer may be a hematologic malignancy, such as leukemia or lymphoma.Type: GrantFiled: December 3, 2014Date of Patent: June 27, 2017Assignee: Gilead Sciences, Inc.Inventors: Julie Di Paolo, Michael J. Hawkins, Jing Hu, Feng Jin, Flordeliza Melchor-Khan, Anita Reddy
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Patent number: 9688684Abstract: The present invention relates to tetrahydro-tetrazolo[1,5-a]pyrazine compounds of formula (I), wherein R1 denotes —R3, —CH2—R3 or —CO—R3; R2 denotes Ar2, Hetar2 or C3-7-cycloalkyl; and R3 denotes Ar3, Hetar3 or C3-7-cycloalkyl. These compounds are useful for inhibiting the retinoid-related orphan receptor ? (ROR ?, ROR-gamma) and for the prevention and/or treatment of medical conditions affected by ROR ? activity such as rheumatoid arthritis, multiple sclerosis, psoriasis, ulcerative colitis, asthma, autoimmune hepatitis or type 1 and type 2 diabetes.Type: GrantFiled: November 26, 2014Date of Patent: June 27, 2017Assignee: Merck Patent GmbHInventors: Dirk Finsinger, Margarita Wucherer-Plietker, Beatrix Blume
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Patent number: 9682996Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.Type: GrantFiled: September 2, 2015Date of Patent: June 20, 2017Assignee: PRISM BioLab Co., Ltd.Inventors: Hiroyuki Kouji, Yuji Kogami, Takenao Odagami
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Patent number: 9676778Abstract: The present disclosure provides compounds of formula (I) wherein the variables are as defined herein that are JAK3 inhibitors and therefore useful for the treatment of diseases treatable by inhibition of JAK3 such as cancer and inflammatory diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: GrantFiled: November 19, 2013Date of Patent: June 13, 2017Assignee: PRINCIPIA BIOPHARMA INC.Inventors: David Michael Goldstein, Kenneth Albert Brameld, Tim Owens
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Patent number: 9676782Abstract: Described are negative allosteric modulators of metabotropic glutamate receptor 3 (mGlu3), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating depression, cognitive disorders, schizophrenia, Alzheimer's disease, or cancer in a subject.Type: GrantFiled: June 12, 2015Date of Patent: June 13, 2017Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Julie L. Engers, Leah C. Konkol
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Patent number: 9655898Abstract: Long term storage stable pemetrexed-containing liquid pharmaceutical compositions are disclosed. The compositions can include pemetrexed or pharmaceutically acceptable salts thereof; an antioxidant selected from lipoic acid, dihydrolipoic acid, methionine and mixtures thereof; a chelating agent selected from lactobionic acid, sodium citrate, tribasic and mixtures thereof; and a pharmaceutically acceptable fluid. The pH of the compositions is in a range of about 8 to about 9.5. The pemetrexed-containing compositions have less than about 5% total impurities, on a normalized peak area response (“PAR”) basis as determined by high performance liquid chromatography (“HPLC”) at a wavelength of 227 nm, after at least about 18 months of storage at a temperature of from about 5° C. to about 25° C. Methods of preparing the formulation as well as methods of treatment of pemetrexed-susceptible diseases using the same are also disclosed.Type: GrantFiled: July 26, 2011Date of Patent: May 23, 2017Assignee: EAGLE PHARMACEUTICALS, INC.Inventors: Nagesh R. Palepu, Philip Christopher Buxton
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Patent number: 9642853Abstract: The administration of leucovorin as well as other active, reduced folates is useful as an antidote to drugs which act as folic acid antagonists and in combination chemotherapy with 5-FU. The most often used calcium salts of the folates have a low solubility in water and form almost insoluble degradation products. Therefore, aqueous solutions are unstable and precipitates result. Precipitates in injectable products present an unacceptable safety risk to patients. Stable high strength pharmaceutical aqueous compositions are formed containing calcium salts, magnesium or zinc salts of the reduced folates leucovorin, (6R,S)-tetrahydrofolic acid, (6S)-tetrahydrofolic acid, 5,10-methylene-(6R,S)-tetrahydrofolate, 5,10-methylene-(6R)-tetrahydrofolate, 5-methyl-(6R,S)-tetrahydrofolate or 5-methyl-(6S)-tetrahydrofolate and one or more of the compounds sodium gluconate, potassium gluconate, glycerophosphate disodium salt or glycerophosphate dipotassium salt.Type: GrantFiled: April 30, 2014Date of Patent: May 9, 2017Assignee: APROFOL AGInventor: Martin Ulmann
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Patent number: 9643970Abstract: This invention is directed to compounds, which are PDE9 enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I) The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).Type: GrantFiled: October 9, 2012Date of Patent: May 9, 2017Assignee: H. Lundbeck A/SInventors: Niels Svenstrup, Klaus Baek Simonsen, Lars Kyhn Rasmussen, Karsten Juhl, Morten Langgard, Kate Wen, Yazhou Wang
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Patent number: 9624206Abstract: The invention relates to antibacterial compounds of formula I wherein X is N or CH; R1 is H or halogen; R2 is alkynyloxy or the group M; R3 is H or halogen; M is one of the groups MA and MB represented below wherein A is a bond, CH2CH2, CH?CH or C?C; R1A is H or halogen; R2A is H, alkoxy or halogen; R3A is H, alkoxy, hydroxyalkoxy, alkoxyalkoxy, thioalkoxy, trifluoromethoxy, amino, hydroxyalkyl, 2-hydroxyacetamido, 1-aminocyclopropyl, 1-hydroxymethyl-cycloprop-1-yl, 1-((phosphonooxy)methyl)cyclopropyl, 1-(((dimethylglycyl)oxy)methyl)cyclopropyl, trans-2-hydroxymethyl-cycloprop-1-yl, 1,2-dihydroxyethyl, 3-hydroxyoxetan-3-yl, 3-(hydroxyalkyl)oxetan-3-yl, 3-aminooxetan-3-yl, 3-hydroxythietan-3-yl, morpholin-4-ylalkoxy, morpholin-4-yl-alkyl, oxazol-2-yl or [1,2,3]triazol-2-yl; and R1B is hydroxyalkyl, dihydroxyalkyl, aminoalkyl, 1-hydroxymethyl-cycloprop-1-yl, 1-aminomethyl-cycloprop-1-yl, trans-2-hydroxymethyl-cycloprop-1-yl, 3-hydroxyoxetan-3-yl, 3-hydroxythietan-3-yl, 1-(2-hydroxyacetyl)azetidin-3-yl,Type: GrantFiled: December 18, 2014Date of Patent: April 18, 2017Assignee: ACTELION PHARMACEUTICALS LTDInventors: Gaelle Chapoux, Jean-Christophe Gauvin, Christian Hubschwerlen, Azely Mirre, Etienne Ochala, Jean-Luc Specklin, Jean-Philippe Surivet
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Patent number: 9624188Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or autoimmune diseases utilizing the compounds of the invention. Formula (I).Type: GrantFiled: March 12, 2014Date of Patent: April 18, 2017Assignee: Bristol-Myers Squibb CompanyInventors: James Aaron Balog, Audris Huang, Bin Chen, Libing Chen, Weifang Shan
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Patent number: 9598423Abstract: 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: GrantFiled: November 14, 2014Date of Patent: March 21, 2017Assignee: Bristol-Myers Squibb CompanyInventors: 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, Mallikarjuna Rao Mettu, 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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Patent number: 9540691Abstract: Disclosed herein are novel assays, systems and kits for selecting a treatment regimen for a subject with depression by identifying at least one nucleic acid polymorphism, e.g., but not limited to, at the MTHFR, MTR, or MTRR locus, and/or determining expression levels of peripheral biomarkers (e.g., SAM, SAH, and 4-HNE) in a test sample from a human subject. These biomarkers can be used to determine the effectiveness of treating a depressed subject with a folate-containing compound (alone or as an adjunct to an antidepressant). Additionally, these biomarkers can be used to select an appropriate treatment regimen for subjects with treatment-resistant depression (e.g., resistant to at least one selective serotonin reuptake inhibitor). Methods and compositions for treating a subject with depression and/or determining or improving the effectiveness of an antidepressant drug taken by a subject are also provided herein.Type: GrantFiled: March 7, 2013Date of Patent: January 10, 2017Assignee: NESTEC S.A.Inventors: Maurizio Fava, George Papakostas, Harold O. Koch, Jr., David Kronlage
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Patent number: 9527834Abstract: The invention relates to substituted 1-benzylquinoxalin-2(1H)-one analogs, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); methods for making the compounds; pharmaceutical compositions; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction.Type: GrantFiled: April 28, 2014Date of Patent: December 27, 2016Assignee: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Shaun R. Stauffer, Joseph David Panarese
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Patent number: 9522140Abstract: The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blocker such as NaV1.3 and NaV1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.Type: GrantFiled: July 2, 2015Date of Patent: December 20, 2016Assignee: RAQUALIA PHARMA INC.Inventors: Tadashi Inoue, Shuzo Watanabe, Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Kaoru Shimada
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Patent number: 9512129Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.Type: GrantFiled: April 15, 2015Date of Patent: December 6, 2016Assignee: Signal Pharmaceuticals, LLCInventor: Jeffrey Eckert
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Patent number: 9505751Abstract: Provided herein are substituted triazolopyrazine phosphodiesterase inhibitors, and pharmaceutical compositions thereof, useful for the treatment of, for example, central nervous system and metabolic diseases and disorder.Type: GrantFiled: June 19, 2013Date of Patent: November 29, 2016Assignee: Sunovion Pharmaceuticals Inc.Inventors: John Emmerson Campbell, Phillip G. Jones, Scott Malcolm
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Patent number: 9499533Abstract: The present invention is related to a compound represented by formula (I) wherein R1 is a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted aromatic carbocyclyl, or the like; X is —N(R3)—, —O—, or —S—; Y is ?C(R4)—, or ?N—; Z is —N(R7)—, —O—, or —S—; R2 is substituted or unsubstituted alkyloxy, or the like, or a group represented by the following formula: —(CR2aR2b)n—R2c, wherein R2a is each independently a hydrogen atom, halogen, or the like; R2b is each independently a hydrogen atom, halogen, or the like; R2a and R2b which are attached to the same carbon atom may be taken together to form oxo, a substituted or unsubstituted non-aromatic carbocycle, or the like; two of R2a which are attached to the adjacent carbon atoms and/or two of R2b which are attached to the adjacent carbon atoms may be taken together to form a bond; R2c is substituted or unsubstituted aromatic carbocyclyl, or the like; n is an integer from 1 to 3; R3 and R7 are each independently a hydrogen atom, subsType: GrantFiled: March 26, 2013Date of Patent: November 22, 2016Assignee: SHIONOGI & CO., LTD.Inventors: Akira Yukimasa, Naotake Kobayashi, Kenji Takaya, Yoshio Hato
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Patent number: 9492451Abstract: The present invention relates to stable pharmaceutical compositions of tetrahydrobiopterin and processes for producing such compositions. Particularly the present invention relates to stable pharmaceutical compositions comprising tetrahydrobiopterin and at least one stabilizing agent.Type: GrantFiled: March 1, 2012Date of Patent: November 15, 2016Assignee: DiPharma S.A.Inventors: Maharukh Tehmasp Rustomjee, Anilkumar Surendrakumar Gandhi
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Patent number: 9493479Abstract: The present invention relates to 4-Pyridone Compounds of Formula (I); and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R1, R2, and R3 are as defined herein. The present invention also relates to compositions comprising at least one 4-Pyridone Compound, and methods of using the 4-Pyridone Compounds for treating or preventing HIV infection in a subject or the clinical manifestations thereof.Type: GrantFiled: April 11, 2014Date of Patent: November 15, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Thomas H. Graham, John S. Wai, Andrew Stamford, Wensheng Liu
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Patent number: 9486453Abstract: Compositions and methods for the treatment of depression and psychoses in humans are disclosed. More particularly, the invention is directed to formulations containing antipsychotic and/or antidepressant medications and also containing an NMDAR antagonist. The present Invention Is also directed to methods tor the treatment of humans suffering from depression and other psychoses, including, schizophrenia, by administration of the inventive compositions in antidepressant and/or antipsychotic effective amounts.Type: GrantFiled: September 3, 2015Date of Patent: November 8, 2016Assignee: Glytech LLCInventor: Daniel C. Javitt