Nitrogen Bonded Directly To Ring Carbon Of The Thiazole Ring Patents (Class 514/370)
  • Patent number: 11173149
    Abstract: 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: Grant
    Filed: April 17, 2018
    Date of Patent: November 16, 2021
    Assignee: Romark Laboratories L.C.
    Inventors: Jean-Francois Rossignol, Maria Gabriella Santoro
  • Patent number: 11071793
    Abstract: Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: July 27, 2021
    Assignee: CHDI Foundation, Inc.
    Inventors: Celia Dominguez, John Wityak, Jonathan Bard, Christopher John Brown, Thomas Martin Krülle, Daniel Clark-Frew, Sarah Hayes
  • Patent number: 11064695
    Abstract: 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: Grant
    Filed: February 15, 2019
    Date of Patent: July 20, 2021
    Assignee: VALENT U.S.A., LLC
    Inventors: Toshiya Ogawa, Ke Zhou, Jessica Tanuwidjaja
  • Patent number: 10925861
    Abstract: 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: Grant
    Filed: February 28, 2018
    Date of Patent: February 23, 2021
    Assignee: SAWAI PHARMACEUTICAL CO., LTD.
    Inventors: Toshihiro Yanagi, Kenji Nozawa, Kaori Umemura, Masatoshi Arimura, Akiko Takada
  • Patent number: 10912768
    Abstract: 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: Grant
    Filed: June 21, 2019
    Date of Patent: February 9, 2021
    Assignee: Romark Laboratories L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Patent number: 10865196
    Abstract: 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: Grant
    Filed: January 16, 2018
    Date of Patent: December 15, 2020
    Assignees: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION, ONCTERNAL THERAPEUTICS, INC.
    Inventors: Duane D. Miller, Jianjun Chen, James T. Dalton, Chien-Ming Li, Sunjoo Ahn, Wei Li
  • Patent number: 10568927
    Abstract: 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: Grant
    Filed: November 13, 2017
    Date of Patent: February 25, 2020
    Assignee: Serenity Pharmaceuticals LLC
    Inventors: Seymour H. Fein, Samuel Herschkowitz
  • Patent number: 10501453
    Abstract: 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: Grant
    Filed: November 29, 2017
    Date of Patent: December 10, 2019
    Assignee: Icahn School of Medicine at Mount Sinai
    Inventors: Russell Dahl, Ah Young Lee, Changwon Kho, Roger J. Hajjar
  • Patent number: 10478399
    Abstract: 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: Grant
    Filed: October 12, 2017
    Date of Patent: November 19, 2019
    Assignee: Synthon B.V.
    Inventors: Agnes Fernandez Pena, Onne Peter Hilbert Backers, Jose Velada Calzada
  • Patent number: 10363243
    Abstract: 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: Grant
    Filed: November 16, 2017
    Date of Patent: July 30, 2019
    Assignee: Romark Laboratories L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Patent number: 10351609
    Abstract: 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: Grant
    Filed: February 10, 2017
    Date of Patent: July 16, 2019
    Assignee: Medical Diagnostic Laboratories, LLC
    Inventors: Elisa A Waxman, Thais Acquafreda
  • Patent number: 10336738
    Abstract: 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: Grant
    Filed: June 3, 2015
    Date of Patent: July 2, 2019
    Assignee: CALCIMEDICA, INC.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Patent number: 10301285
    Abstract: 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: Grant
    Filed: April 21, 2015
    Date of Patent: May 28, 2019
    Assignees: GTX, INC., UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
    Inventors: Duane D. Miller, Jianjun Chen, James T. Dalton, Chien-Ming Li, Sunjoo Ahn, Wei Li
  • Patent number: 10253005
    Abstract: The present invention provides a process for the preparation of ?-Form crystals of Mirabegron using a solvent selected from water.
    Type: Grant
    Filed: May 9, 2016
    Date of Patent: April 9, 2019
    Assignee: Aurobindo Pharma Ltd.
    Inventors: Sukumar Nandi, Shantan Kumar Reddy, Gona Bala Narashimha Reddy, Sivakumaran Meenakshisundaram
  • Patent number: 10137211
    Abstract: Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use
    Type: Grant
    Filed: August 26, 2016
    Date of Patent: November 27, 2018
    Assignee: 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
  • Patent number: 10045978
    Abstract: 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: Grant
    Filed: December 2, 2015
    Date of Patent: August 14, 2018
    Assignee: AB SCIENCE
    Inventors: Alain Moussy, Jean-Pierre Kinet
  • Patent number: 10022356
    Abstract: 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: Grant
    Filed: March 5, 2014
    Date of Patent: July 17, 2018
    Assignee: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
    Inventors: Jin Wang, Jianjun Chen, Duane D. Miller, Wei Li
  • Patent number: 9957229
    Abstract: 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: Grant
    Filed: May 23, 2017
    Date of Patent: May 1, 2018
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Colin Zhang, Brian W. Metcalf, Chunhong He, Ding-Quan Qian
  • Patent number: 9845320
    Abstract: 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: Grant
    Filed: August 29, 2013
    Date of Patent: December 19, 2017
    Assignee: Icahn School of Medicine at Mount Sinai
    Inventors: Russell Dahl, Ah Young Lee, Changwon Kho, Roger J. Hajjar
  • Patent number: 9820975
    Abstract: 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: Grant
    Filed: April 20, 2016
    Date of Patent: November 21, 2017
    Assignee: Romark Laboratories L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Patent number: 9814753
    Abstract: 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: Grant
    Filed: July 23, 2014
    Date of Patent: November 14, 2017
    Assignee: Serenity Pharmaceuticals LLC
    Inventors: Seymour H. Fein, Samuel Herschkowitz
  • Patent number: 9802904
    Abstract: 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: Grant
    Filed: December 26, 2013
    Date of Patent: October 31, 2017
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, University of Delaware
    Inventors: David J. Maloney, Andrew S. Rosenthal, Ajit Jadhav, Thomas S. Dexheimer, Anton Simeonov, Zhihao Zhuang, Qin Liang, Diane K. Luci
  • Patent number: 9770021
    Abstract: 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: Grant
    Filed: May 25, 2009
    Date of Patent: September 26, 2017
    Assignee: Syngenta Participations AG
    Inventors: Jason Keiper, Joshua Koon, Sarah Beth Cush, Michael James Hopkinson, Johnny D. Reynolds, Jorge Cisneros, Jennifer Peterson, Roy Boykin
  • Patent number: 9650369
    Abstract: 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: Grant
    Filed: September 27, 2013
    Date of Patent: May 16, 2017
    Assignee: XAVIER UNIVERSITY OF LOUISIANA
    Inventors: Guangdi Wang, Quan Jiang, Qiu Zhong, Qiang Zhang, Shilong Zheng
  • Patent number: 9458118
    Abstract: 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: Grant
    Filed: January 13, 2016
    Date of Patent: October 4, 2016
    Assignee: Chromocell Corporation
    Inventors: Olga Babich, Tina Garyantes, Robert Z. Luo, David J. Palling, Srinivasan P. Venkatachalan, Yanlin Wang-Fischer
  • Patent number: 9382219
    Abstract: 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: Grant
    Filed: February 12, 2015
    Date of Patent: July 5, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
  • Patent number: 9365526
    Abstract: The present invention relates to processes for the preparation of dasatinib and its intermediates.
    Type: Grant
    Filed: December 31, 2013
    Date of Patent: June 14, 2016
    Assignee: SUN PHARMACEUTICAL INDUSTRIES LIMITED
    Inventors: Jagdev Singh Jaryal, Munish Kapoor, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
  • Patent number: 9345690
    Abstract: 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: Grant
    Filed: March 16, 2015
    Date of Patent: May 24, 2016
    Assignee: Romark Laboratories L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Patent number: 9126927
    Abstract: 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: Grant
    Filed: September 23, 2011
    Date of Patent: September 8, 2015
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
  • Patent number: 9102636
    Abstract: 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: Grant
    Filed: March 8, 2011
    Date of Patent: August 11, 2015
    Assignee: Galleon Pharmaceuticals, Inc.
    Inventors: James C. Mannion, Scott L. Dax
  • Patent number: 9102602
    Abstract: 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: Grant
    Filed: November 29, 2010
    Date of Patent: August 11, 2015
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Junko Takada, Shunsuke Iwamoto, Satoshi Nakano
  • Patent number: 9040456
    Abstract: 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: Grant
    Filed: June 5, 2013
    Date of Patent: May 26, 2015
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Hajime Ikeda
  • Patent number: 9040530
    Abstract: 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: Grant
    Filed: March 15, 2013
    Date of Patent: May 26, 2015
    Assignee: PORTOLA PHARMACEUTICALS, INC.
    Inventors: Zhaozhong J. Jia, Brian Kane, Jack Rose, Shawn M. Bauer, Yonghong Song, Qing Xu, Anjali Pandey
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Patent number: 9029407
    Abstract: The present invention relates to new aminothiazole modulators of beta-3-adrenoreceptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: June 19, 2013
    Date of Patent: May 12, 2015
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Tadimeti Rao, Chengzhi Zhang
  • Patent number: 9029408
    Abstract: 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: Grant
    Filed: October 9, 2013
    Date of Patent: May 12, 2015
    Assignees: GTx, Inc., University of Tennessee Research Foundation
    Inventors: Duane D. Miller, Wei Li, Jianjun Chen, James T. Dalton, Chien-Ming Li, Sunjoo Ahn
  • Publication number: 20150126565
    Abstract: 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: Application
    Filed: December 29, 2014
    Publication date: May 7, 2015
    Inventors: YUUKI TAKAISHI, SOICHIRO NAKAMURA, YUTAKA TAKAHASHI
  • Publication number: 20150126564
    Abstract: 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: Application
    Filed: May 31, 2012
    Publication date: May 7, 2015
    Applicant: The Curators of the University of Missouri
    Inventors: Bumsuk Hahm, Young-Jin Seo, Stephen Alexander, Vijayan Madhuvanthi
  • Patent number: 9023877
    Abstract: 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: Grant
    Filed: June 23, 2010
    Date of Patent: May 5, 2015
    Assignee: Romark Laboratories L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Publication number: 20150119430
    Abstract: 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: Application
    Filed: May 10, 2013
    Publication date: April 30, 2015
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Song Li, Wu Zhong, Juan Liu, Kunlun He, Junhai Xiao, Xinbo Zhou
  • Publication number: 20150119376
    Abstract: 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: Application
    Filed: April 12, 2012
    Publication date: April 30, 2015
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: SeoHee LEE, JungTaek OH, JaeKwang LEE, JaeWon LEE, Suyeal BAE, Nina HA, Sera LEE
  • Patent number: 9018209
    Abstract: 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: Grant
    Filed: September 25, 2006
    Date of Patent: April 28, 2015
    Assignee: Yale University
    Inventors: William L. Jorgensen, Juliana Ruiz-Caro, Andrew D. Hamilton
  • Publication number: 20150111897
    Abstract: 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: Application
    Filed: December 30, 2014
    Publication date: April 23, 2015
    Inventors: Hong Hu, Sunghan Yim, Uma Santhanam, John W. Lyga
  • Publication number: 20150111934
    Abstract: 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: Application
    Filed: October 3, 2014
    Publication date: April 23, 2015
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Alessio BOVE, Pietro ALLEGRINI, Emanuele ATTOLINO
  • Patent number: 8999889
    Abstract: 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: Grant
    Filed: January 28, 2011
    Date of Patent: April 7, 2015
    Assignee: BASF SE
    Inventors: 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
  • Publication number: 20150094307
    Abstract: 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: Application
    Filed: October 1, 2014
    Publication date: April 2, 2015
    Inventors: Ann Marie Schmidt, Ravichandran Ramasamy, Alexander Shekhtman, Vivek Rai, Michaele B. Manigrasso
  • Publication number: 20150094310
    Abstract: The present invention relates to a corticotropin releasing hormone receptor type 1 (CRHR1) antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in a novel group of patients, i.e. patients having corticotropin releasing hormone (CRH) overactivity.
    Type: Application
    Filed: April 23, 2013
    Publication date: April 2, 2015
    Inventor: Florian Holsboer
  • Patent number: 8993567
    Abstract: 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: Grant
    Filed: March 27, 2014
    Date of Patent: March 31, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
  • Patent number: 8980837
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: March 17, 2015
    Assignee: Genentech, Inc.
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Publication number: 20150072970
    Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.
    Type: Application
    Filed: May 19, 2014
    Publication date: March 12, 2015
    Applicant: MELINTA THERAPEUTICS, INC.
    Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu