Nitrogen Bonded Directly To Ring Carbon Of The Thiazole Ring Patents (Class 514/370)
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Patent number: 12128033Abstract: The present disclosure relates to the fields of chemistry and medicine, more particularly to processes for making 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-prop-2-ynyl-1,3-thi-azol-2-amine (Compound 1), pharmaceutically acceptable salts, and crystalline forms thereof, for the treatment of congenital adrenal hyperplasia (CAH).Type: GrantFiled: March 14, 2024Date of Patent: October 29, 2024Assignees: Neurocrine Biosciences, Inc., SanofiInventors: Andrew Becker, Joel Radisson
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Patent number: 11850237Abstract: This invention is directed to methods for treating and preventing influenza infection by inhibiting influenza virus HA maturation processes employing compounds of formula I. It is also directed to combinations for treating and preventing influenza infection comprising compounds of formula I and other agents.Type: GrantFiled: February 8, 2021Date of Patent: December 26, 2023Assignee: Romark Laboratories L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
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Patent number: 11528516Abstract: A distributed transcoding method includes splitting image content into segments of a fixed interval; allocating the split segments to a plurality of workers and performing parallel transcoding; and concatenating the transcoded segments and merging same into one encoded file.Type: GrantFiled: May 27, 2020Date of Patent: December 13, 2022Assignee: NAVER CORPORATIONInventors: Kuenbaek Park, Bong Sub Kim, Jae Hoon Kim, Seongcheol Jo, Seungjin Kim, Seung Ha Yang
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Patent number: 11433054Abstract: The present invention relates to a pharmaceutical preparation containing an active ingredient and a release-controlling agent for adjusting the release of the active ingredient, in which the active ingredient is at least one selected from among mirabegron and a pharmaceutically acceptable salt thereof, and the release-controlling agent is a hydrogel-forming polymer, the hydrogel-forming polymer being at least one selected from among polyethylene oxide, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, sodium carboxymethylcellulose, and hydroxyethyl cellulose and having an average molecular weight ranging from 100,000 to 8,000,000. The present invention is capable of suppressing the generation of impurities therein and of effectively controlling the release of at least one selected from among mirabegron and a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 13, 2018Date of Patent: September 6, 2022Assignee: DAEWOONG PHARMACEUTICAL CO., LTD.Inventors: Jae Hee Yoon, Han Kang
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Patent number: 11173149Abstract: Provided are methods of treating a disease or condition associated with an increased level of expression of a protein disulfide-isomerase A3 (PDIA3) by administering to a subject with an increased level of expression of PDIA3 a PDIA3-inhibiting effective amount of a thiazolide compound, such as nitazoxanide or tizoxanide. Also provided are methods of screening for therapeutic agents based on PDIA3 inhibition.Type: GrantFiled: April 17, 2018Date of Patent: November 16, 2021Assignee: Romark Laboratories L.C.Inventors: Jean-Francois Rossignol, Maria Gabriella Santoro
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Patent number: 11071793Abstract: Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.Type: GrantFiled: August 28, 2015Date of Patent: July 27, 2021Assignee: CHDI Foundation, Inc.Inventors: Celia Dominguez, John Wityak, Jonathan Bard, Christopher John Brown, Thomas Martin Krülle, Daniel Clark-Frew, Sarah Hayes
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Patent number: 11064695Abstract: The present invention is generally directed to an agricultural formulation comprising, ethaboxam, metalaxyl and a compound selected from the group consisting of 3-(difluoromethyl)-1-methyl-N-[(3R)-1,1,3-trimethyl-2,3-dihydroinden-4-yl]pyrazole-4-carboxamide and mandestrobin, a process for preparing the agricultural formulation and methods of use thereof.Type: GrantFiled: February 15, 2019Date of Patent: July 20, 2021Assignee: VALENT U.S.A., LLCInventors: Toshiya Ogawa, Ke Zhou, Jessica Tanuwidjaja
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Patent number: 10925861Abstract: To provide a mirabegron-containing tablet that maintains the amorphous form of mirabegron even after long-term storage. Also, to provide a mirabegron-containing pharmaceutical preparation that can maintain the purity of mirabegron while preventing the generation of related substances at the time of storage, a method for producing a mirabegron-containing pharmaceutical preparation, and a method for producing a mirabegron-containing granulated product. According to an embodiment of the present invention, there is provided a mirabegron-containing pharmaceutical preparation containing mirabegron, hypromellose, and polyvinylpyrrolidone. The mirabegron-containing pharmaceutical preparation may contain a spray-dried granulated product containing the mirabegron, the hypromellose, and the polyvinylpyrrolidone.Type: GrantFiled: February 28, 2018Date of Patent: February 23, 2021Assignee: SAWAI PHARMACEUTICAL CO., LTD.Inventors: Toshihiro Yanagi, Kenji Nozawa, Kaori Umemura, Masatoshi Arimura, Akiko Takada
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Patent number: 10912768Abstract: This invention is directed to methods for treating and preventing influenza infection by inhibiting influenza virus HA maturation processes employing compounds of formula I. It is also directed to combinations for treating and preventing influenza infection comprising compounds of formula I and other agents.Type: GrantFiled: June 21, 2019Date of Patent: February 9, 2021Assignee: Romark Laboratories L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
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Patent number: 10865196Abstract: The present invention relates to a compound of formula XXII and a compound of formula 17ya, which are defined as anywhere in the specification, to a composition comprising the same, and to a method of using thereof in the treatment of various forms of cancer.Type: GrantFiled: January 16, 2018Date of Patent: December 15, 2020Assignees: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION, ONCTERNAL THERAPEUTICS, INC.Inventors: Duane D. Miller, Jianjun Chen, James T. Dalton, Chien-Ming Li, Sunjoo Ahn, Wei Li
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Patent number: 10568927Abstract: The invention provides methods and compositions for use of desmopressin in combination with a beta-3-adrenergic receptor agonist. The methods and compositions are useful in the treatment of nocturia and other urinary frequency disorders.Type: GrantFiled: November 13, 2017Date of Patent: February 25, 2020Assignee: Serenity Pharmaceuticals LLCInventors: Seymour H. Fein, Samuel Herschkowitz
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Patent number: 10501453Abstract: Provided are SUMO activators, which can enhance SUMOylation of SERCA2a, which are useful in the treatment of heart failure, cardiovascular diseases, cancer, neurodegenerative disorders, viral infection, bacterial infection, liver disease, inflammation, and other diseases.Type: GrantFiled: November 29, 2017Date of Patent: December 10, 2019Assignee: Icahn School of Medicine at Mount SinaiInventors: Russell Dahl, Ah Young Lee, Changwon Kho, Roger J. Hajjar
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Patent number: 10478399Abstract: The present invention relates to a pharmaceutical composition, particularly a modified release tablet composition comprising mirabegron or a pharmaceutically acceptable salt thereof and to a process for preparing such a composition.Type: GrantFiled: October 12, 2017Date of Patent: November 19, 2019Assignee: Synthon B.V.Inventors: Agnes Fernandez Pena, Onne Peter Hilbert Backers, Jose Velada Calzada
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Patent number: 10363243Abstract: This invention is directed to methods for treating and preventing influenza infection by inhibiting influenza virus HA maturation processes employing compounds of formula I. It is also directed to combinations for treating and preventing influenza infection comprising compounds of formula I and other agents.Type: GrantFiled: November 16, 2017Date of Patent: July 30, 2019Assignee: Romark Laboratories L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
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Patent number: 10351609Abstract: Disclosed are methods of determining activity of mTOR variants upon exposure to mTOR inhibitors, such a rapamycin or rapalogs thereof, methods for determining kinase activity of a mTOR variant, and methods for determining tumor cell response to treatment with rapamycin or rapalogs thereof. A method for determining whether a compound inhibits mTOR activity in a cell is also disclosed.Type: GrantFiled: February 10, 2017Date of Patent: July 16, 2019Assignee: Medical Diagnostic Laboratories, LLCInventors: Elisa A Waxman, Thais Acquafreda
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Patent number: 10336738Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: June 3, 2015Date of Patent: July 2, 2019Assignee: CALCIMEDICA, INC.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Patent number: 10301285Abstract: The present invention relates to a compound of formula XXII and a compound of formula 17ya, which are defined as anywhere in the specification, to a composition comprising the same, and to a method of using thereof in the treatment of various forms of cancer.Type: GrantFiled: April 21, 2015Date of Patent: May 28, 2019Assignees: GTX, INC., UNIVERSITY OF TENNESSEE RESEARCH FOUNDATIONInventors: Duane D. Miller, Jianjun Chen, James T. Dalton, Chien-Ming Li, Sunjoo Ahn, Wei Li
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Patent number: 10253005Abstract: The present invention provides a process for the preparation of ?-Form crystals of Mirabegron using a solvent selected from water.Type: GrantFiled: May 9, 2016Date of Patent: April 9, 2019Assignee: Aurobindo Pharma Ltd.Inventors: Sukumar Nandi, Shantan Kumar Reddy, Gona Bala Narashimha Reddy, Sivakumaran Meenakshisundaram
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Patent number: 10137211Abstract: Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their useType: GrantFiled: August 26, 2016Date of Patent: November 27, 2018Assignee: CHDI Foundation, Inc.Inventors: Celia Dominguez, John Wityak, Jonathan Bard, Christopher John Brown, Michael Edward Prime, Peter David Johnson, Thomas Martin Krulle, Daniel Clark-Frew, Duane Higgins, Matthew Robert Mills, Richard Waldron Marston, Samuel Coe, Samantha Brown, Sarah Hayes
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Patent number: 10045978Abstract: The treatment of mastocytosis, and in particular indolent forms of mastocytosis (including smoldering systemic, indolent systemic and cutaneous mastocytosis), including the administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt or solvate thereof, in particular in an appropriate dosage regimen.Type: GrantFiled: December 2, 2015Date of Patent: August 14, 2018Assignee: AB SCIENCEInventors: Alain Moussy, Jean-Pierre Kinet
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Patent number: 10022356Abstract: The present invention relates to pharmaceutical compositions for treating cancer comprising BRAF inhibitors, (e.g. vemurafenib) and/or MEK inhibitor, (e.g. trametinib, RO5068760), in combination with anti-tubulin compounds of the invention or other known tubulin inhibitors, and using such compositions for treating cancer such as melanoma, drug-resistant cancer, and cancer metastasis.Type: GrantFiled: March 5, 2014Date of Patent: July 17, 2018Assignee: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATIONInventors: Jin Wang, Jianjun Chen, Duane D. Miller, Wei Li
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Patent number: 9957229Abstract: 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: May 23, 2017Date of Patent: May 1, 2018Assignees: 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: 9845320Abstract: Provided are SUMO activators, which can enhance SUMOylation of SERCA2a, which are useful in the treatment of heart failure, cardiovascular diseases, cancer, neurodegenerative disorders, viral infection, bacterial infection, liver disease, inflammation, and other diseases.Type: GrantFiled: August 29, 2013Date of Patent: December 19, 2017Assignee: Icahn School of Medicine at Mount SinaiInventors: Russell Dahl, Ah Young Lee, Changwon Kho, Roger J. Hajjar
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Patent number: 9820975Abstract: This invention is directed to methods for treating and preventing influenza infection by inhibiting influenza virus HA maturation processes employing compounds of formula I. It is also directed to combinations for treating and preventing influenza infection comprising compounds of formula I and other agents.Type: GrantFiled: April 20, 2016Date of Patent: November 21, 2017Assignee: Romark Laboratories L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
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Patent number: 9814753Abstract: The invention provides methods and compositions for use of desmopressin in combination with a beta-3-adrenergic receptor agonist. The methods and compositions are useful in the treatment of nocturia and other urinary frequency disorders.Type: GrantFiled: July 23, 2014Date of Patent: November 14, 2017Assignee: Serenity Pharmaceuticals LLCInventors: Seymour H. Fein, Samuel Herschkowitz
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Patent number: 9802904Abstract: Disclosed are inhibitors of the USP1/UAF1 deubiquitinase complex, for example. of formula (I), wherein R1, R2, and Q are as defined herein, which are useful in treating diseases such as cancer, and improving the efficacy of DNA damaging agents in cancer treatment. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, a method of method of inhibiting a heterodimeric deubiquitinase complex in a cell, and a method of enhancing the chemotherapeutic treatment of cancer in a mammal undergoing treatment with an anti cancer agent. Further disclosed is a method of preparing compounds of the invention.Type: GrantFiled: December 26, 2013Date of Patent: October 31, 2017Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, University of DelawareInventors: David J. Maloney, Andrew S. Rosenthal, Ajit Jadhav, Thomas S. Dexheimer, Anton Simeonov, Zhihao Zhuang, Qin Liang, Diane K. Luci
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Patent number: 9770021Abstract: A formulated composition suitable for controlling or preventing pathogenic damage in a plant comprising (A) at least one solid active ingredient having a water solubility of at most 100 ?g/liter at 25° C. at neutral pH, in an amount of at least 1 weight %, based on the total weight of the formulated composition, (B) at least one non-ionic surface active compound having a hydrophile-lipophile balance (HLB) of between 10 and 18, one or more customary formulation auxiliaries, and water; wherein active ingredient (A) is suspended or dispersed in the water, the weight ratio of surface active compound (B) to active ingredient (A) is in the range of from 1.5 to 15.0, provided the minimum amount of surface active compound (B) is at least 6 weight %, based on the total weight of the formulated composition. Also a method of improving pesticide residue levels in agriculture.Type: GrantFiled: May 25, 2009Date of Patent: September 26, 2017Assignee: Syngenta Participations AGInventors: Jason Keiper, Joshua Koon, Sarah Beth Cush, Michael James Hopkinson, Johnny D. Reynolds, Jorge Cisneros, Jennifer Peterson, Roy Boykin
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Patent number: 9650369Abstract: Thiazole analog compounds and their pharmaceutically acceptable salts are disclosed, including pharmaceutical compositions comprising the thiazole analog compounds, either alone or in combination with at least one additional therapeutic agent, and/or with a pharmaceutically acceptable carrier. Methods of using the thiazole analog compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative diseases, such as cancer, are also disclosed.Type: GrantFiled: September 27, 2013Date of Patent: May 16, 2017Assignee: XAVIER UNIVERSITY OF LOUISIANAInventors: Guangdi Wang, Quan Jiang, Qiu Zhong, Qiang Zhang, Shilong Zheng
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Patent number: 9458118Abstract: Provided herein are sodium channel modulating Compounds, in particular NaV1.7 modulating compounds of Formula I or compounds of Formula I?: In particular, provided herein are processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions comprising, and therapeutic methods comprising administering such compounds. In particular, provided herein are compounds for the treatment of pain and diabetes.Type: GrantFiled: January 13, 2016Date of Patent: October 4, 2016Assignee: Chromocell CorporationInventors: Olga Babich, Tina Garyantes, Robert Z. Luo, David J. Palling, Srinivasan P. Venkatachalan, Yanlin Wang-Fischer
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Patent number: 9382219Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.Type: GrantFiled: February 12, 2015Date of Patent: July 5, 2016Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
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Patent number: 9365526Abstract: The present invention relates to processes for the preparation of dasatinib and its intermediates.Type: GrantFiled: December 31, 2013Date of Patent: June 14, 2016Assignee: SUN PHARMACEUTICAL INDUSTRIES LIMITEDInventors: Jagdev Singh Jaryal, Munish Kapoor, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
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Patent number: 9345690Abstract: This invention is directed to methods for treating and preventing influenza infection by inhibiting influenza virus HA maturation processes employing compounds of formula I. It is also directed to combinations for treating and preventing influenza infection comprising compounds of formula I and other agents.Type: GrantFiled: March 16, 2015Date of Patent: May 24, 2016Assignee: Romark Laboratories L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
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Patent number: 9126927Abstract: 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: September 23, 2011Date of Patent: September 8, 2015Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
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Patent number: 9102636Abstract: The invention relates to compounds, compositions, and methods for diminishing pain in a subject in need thereof comprising administering the compounds and compositions herein described.Type: GrantFiled: March 8, 2011Date of Patent: August 11, 2015Assignee: Galleon Pharmaceuticals, Inc.Inventors: James C. Mannion, Scott L. Dax
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Patent number: 9102602Abstract: The object of the present invention is to provide a novel method for producing an isothiocyanate compound having a carboxyl group(s) by a reaction of the corresponding amino compound having a carboxyl group(s), thiocarbonyldiimidazole and a base, in one step with high purity. An amino compound having a carboxyl group(s) is reacted with thiocarbonyldiimidazole in a solvent in the presence of a base to obtain an isothiocyanate compound having a carboxyl group(s).Type: GrantFiled: November 29, 2010Date of Patent: August 11, 2015Assignee: Nissan Chemical Industries, Ltd.Inventors: Junko Takada, Shunsuke Iwamoto, Satoshi Nakano
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Patent number: 9040530Abstract: Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.Type: GrantFiled: March 15, 2013Date of Patent: May 26, 2015Assignee: PORTOLA PHARMACEUTICALS, INC.Inventors: Zhaozhong J. Jia, Brian Kane, Jack Rose, Shawn M. Bauer, Yonghong Song, Qing Xu, Anjali Pandey
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Patent number: 9040456Abstract: To provide a method which exerts excellent controlling effects on noxious organisms in a field of soybean, corn or cotton. A method for controlling noxious organisms in a field of soybean, corn or cotton, wherein at least one PPO inhibitor compound selected from the group consisting of flumioxazin, sulfentrazone, saflufenacil, oxyfluorfen, fomesafen-sodium, and a compound represented by formula (I): is applied to the field before, at or after sowing a soybean, corn or cotton seed treated with ethaboxam.Type: GrantFiled: June 5, 2013Date of Patent: May 26, 2015Assignee: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Hajime Ikeda
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Publication number: 20150133442Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.Type: ApplicationFiled: June 7, 2013Publication date: May 14, 2015Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
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Patent number: 9029407Abstract: The present invention relates to new aminothiazole modulators of beta-3-adrenoreceptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: June 19, 2013Date of Patent: May 12, 2015Assignee: Auspex Pharmaceuticals, Inc.Inventors: Tadimeti Rao, Chengzhi Zhang
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Patent number: 9029408Abstract: The present invention relates to a compound of formula XXII and a compound of formula 17ya, which are defined as anywhere in the specification, to a composition comprising the same, and to a method of using thereof in the treatment of various forms of cancer.Type: GrantFiled: October 9, 2013Date of Patent: May 12, 2015Assignees: GTx, Inc., University of Tennessee Research FoundationInventors: Duane D. Miller, Wei Li, Jianjun Chen, James T. Dalton, Chien-Ming Li, Sunjoo Ahn
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Publication number: 20150126565Abstract: A pharmaceutical composition for modified release comprising (R)-2-(2-aminothiazol-4-yl)-4?-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or a pharmaceutically acceptable salt thereof, and a carrier for a sustained release pharmaceutical composition, wherein a maximum blood drug concentration (Cmax) when administered in a fasted state is 400 ng/mL or less, is disclosed.Type: ApplicationFiled: December 29, 2014Publication date: May 7, 2015Inventors: YUUKI TAKAISHI, SOICHIRO NAKAMURA, YUTAKA TAKAHASHI
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Publication number: 20150126564Abstract: The present invention relates to compounds and methods for the prevention or treatment of infections by negative strand RNA viruses, such as influenza virus and measles virus, wherein said compounds delay or inhibit viral replication by modulating the level or activity of a polypeptide involved in the synthesis or degradation of sphingosine-1-phosphate (S1P) in a cell, tissue, or subject. The methods involve administration of one or more compounds which modulate the level of gene expression, where the gene encodes a polypeptide involved in regulating the metabolic level of S1P, or modulate the level or activity of a polypeptide involved in regulating the metabolic level of S1P, such as sphingosine kinase (SK) and S1P lyase (SPL). Exemplary methods are directed towards reducing the level of SW by reducing the level or activity of one or more SKs, increasing the level or activity of one or more SPLs, or a combination of both steps.Type: ApplicationFiled: May 31, 2012Publication date: May 7, 2015Applicant: The Curators of the University of MissouriInventors: Bumsuk Hahm, Young-Jin Seo, Stephen Alexander, Vijayan Madhuvanthi
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Patent number: 9023877Abstract: This invention is directed to methods for treating and preventing influenza infection by inhibiting influenza virus HA maturation processes employing compounds of formula I. It is also directed to combinations for treating and preventing influenza infection comprising compounds of formula I and other agents.Type: GrantFiled: June 23, 2010Date of Patent: May 5, 2015Assignee: Romark Laboratories L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
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Publication number: 20150119430Abstract: The present invention relates to a compound of Formula (I), or an isomer, pharmaceutically acceptable salt and solvate thereof; the present invention further relates to a pharmaceutical composition, which comprises the compound of Formula (I), or isomer, pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents; the present invention further relates to the use of the compound of Formula (I), or isomer, pharmaceutically acceptable salt or solvate thereof, for anti-apoptosis, prophylaxis or treatment of a disease or symptom associated with apoptosis, especially for protecting myocardial cells, and prophylaxis or treatment of a disease or symptom associated with cardiomyocyte apoptosis.Type: ApplicationFiled: May 10, 2013Publication date: April 30, 2015Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Song Li, Wu Zhong, Juan Liu, Kunlun He, Junhai Xiao, Xinbo Zhou
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Publication number: 20150119376Abstract: The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.Type: ApplicationFiled: April 12, 2012Publication date: April 30, 2015Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: SeoHee LEE, JungTaek OH, JaeKwang LEE, JaeWon LEE, Suyeal BAE, Nina HA, Sera LEE
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Patent number: 9018209Abstract: The present invention relates to compounds according to the formula I: Where Ra is H or an optionally OH-substituted C1-C3 alkyl; R1 is OR1, an optionally substituted C4-12 carbocyclic group which may be saturated or unsaturated (including aromatic) or an optionally substituted heterocyclic group; R1 is an optionally substituted C1-C14 hydrocarbyl group or an optionally substituted heterocyclic group; R2, R3 and R4 are each independently H, an optionally substituted C1-C4 alkyl group (preferably CH3, CH2CH3 or CF3), halogen (preferably F, Cl, Br), OR, CN, NO2, a C1-C6 thioether, a C1-C6 thioester group, an optionally substituted CO2R group, an optionally substituted COR group or an optionally substituted OCOR group (preferably R4 is H); R is H or an optionally substituted C1-C6 alkyl group; RHET is an optionally substituted heterocyclic group; and pharmaceutically acceptable salts, solvates or polymorphs thereof.Type: GrantFiled: September 25, 2006Date of Patent: April 28, 2015Assignee: Yale UniversityInventors: William L. Jorgensen, Juliana Ruiz-Caro, Andrew D. Hamilton
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Publication number: 20150111934Abstract: The present invention relates to the acetate salt of Mirabegron, in particular in two novel crystalline forms, a process for their preparation and the use of said salt and its crystalline forms in the synthesis of Mirabegron with high yields and chemical purity.Type: ApplicationFiled: October 3, 2014Publication date: April 23, 2015Applicant: DIPHARMA FRANCIS S.R.L.Inventors: Alessio BOVE, Pietro ALLEGRINI, Emanuele ATTOLINO
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Publication number: 20150111897Abstract: The compositions and methods of described herein comprise novel ingredients effective to reduce unwanted pigmentation, such as skin discoloration, freckles, age spots, liver spots, sun damage, tans, pigmented acne marks, scars, pigmented birthmarks, hyperpigmentation, post-inflammatory hyperpigmentation, post-injury hyperpigmentation, melasma, cholasma, after-burn scar, nail stain, yellowing of skin, dark circles under eyes, and the like. The composition may include additional ingredients accordingly for a colored cosmetic, moisturizer, cleanser, toner, and the like.Type: ApplicationFiled: December 30, 2014Publication date: April 23, 2015Inventors: Hong Hu, Sunghan Yim, Uma Santhanam, John W. Lyga
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Patent number: 8999889Abstract: The invention relates to substituted ketonic isoxazoline compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the substituted ketonic isoxazoline compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such substituted ketonic isoxazoline compounds. The substituted ketonic isoxazoline compounds of the present invention are defined by the following formula I: wherein A1 to A4, R1 to R3, (R4)p, (R5)q, X and (G)m are defined as in the description.Type: GrantFiled: January 28, 2011Date of Patent: April 7, 2015Assignee: BASF SEInventors: Karsten Koerber, Florian Kaiser, Wolfgang von Deyn, Steffen Gross, Joachim Dickhaut, Prashant Deshmukh, Nina Gertrud Bandur, Arun Narine, Deborah L. Culbertson, Douglas D. Anspaugh, Franz Josef Braun
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Publication number: 20150094307Abstract: Amino, amido, and heterocyclic compounds are disclosed. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diabetes complications, inflammation, and neurodegeneration, obesity, cancer, ischemia/reperfusion injury, cardiovascular disease and other diseases related to RAGE activity.Type: ApplicationFiled: October 1, 2014Publication date: April 2, 2015Inventors: Ann Marie Schmidt, Ravichandran Ramasamy, Alexander Shekhtman, Vivek Rai, Michaele B. Manigrasso