Patents Examined by Douglas M Willis
  • Patent number: 10377776
    Abstract: A process can prepare an isocyanurate compound by hydrosilylation. The compound is a tris[3-(trialkoxysilyl)propyl] isocyanurate, a tris[3-(alkyldialkoxysilyl)propyl] isocyanurate, and/or a tris[3-(dialkylalkoxysilyl)propyl] isocyanurate. The process includes (A) preparing a mixture of at least one carboxylic acid, a platinum catalyst, and 1,3,5-triallyl-1,3,5-triazine-2,4,6(1H,3H,5H)-trione; (B) heating the mixture to a temperature in the range of 40 to 140° C.; (C) adding at least one H-silane among a hydrotrialkoxysilane, a hydroalkyldialkoxysilane, and a hydrodialkylalkoxysilane to the mixture; (D) adding at least one alcohol to the mixture prepared in step (C); and (E) isolating the isocyanurate compound.
    Type: Grant
    Filed: October 15, 2018
    Date of Patent: August 13, 2019
    Assignee: Evonik Degussa GmbH
    Inventors: Philipp Albert, Eckhard Just
  • Patent number: 10376509
    Abstract: Methods for inhibiting the activity of Clostridium difficile in a subject comprise administering to the subject in need thereof a pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and a clofazimine analog selected from B746 clofazimine analog or B826 clofazimine analog.
    Type: Grant
    Filed: August 22, 2018
    Date of Patent: August 13, 2019
    Assignee: KamTek, Inc.
    Inventors: Venkata M. Reddy, Wolf Prensky, Sharanjit VedBrat
  • Patent number: 10376504
    Abstract: The present invention is directed to azacyanoquinolinone compounds of the general structural formula: (wherein R5 and R6 are defined herein) which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: August 13, 2019
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Antonella Converso, Kevin Rodzinak
  • Patent number: 10370364
    Abstract: A compound represented by the following Formula 1 or a pharmaceutically acceptable salt thereof: wherein R1 is a substituted or unsubstituted C1-5 linear or branched alkyl, a C5-6 cycloalkyl, a C5-6 cycloalkyl containing at least one heteroatom selected from among O and N, a substituted or unsubstituted C6-12 aryl, or a C5-6 heteroaryl containing at least one heteroatom selected from among O and N; R2 is hydrogen, ethyl, acetyl, acetoxy, carboxy, benzoyloxy or 3,4,5-trihydroxybenzoyloxy; and R3 to R5 are each independently hydrogen, hydroxyl, methyl, methoxy, acetoxy, carboxy or benzoyloxy.
    Type: Grant
    Filed: July 17, 2018
    Date of Patent: August 6, 2019
    Assignee: OSTEONEUROGEN INC.
    Inventors: Byung Soo Youn, Jun Hwan Kim, Han Soo Kim, Ho Sup Yoon, Ik Hwan Kim
  • Patent number: 10370386
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: August 6, 2019
    Assignee: Araxes Pharma LLC
    Inventors: Liansheng Li, Jun Feng, Tao Wu, Pingda Ren, Yi Liu, Yuan Liu, Yun Oliver Long
  • Patent number: 10364248
    Abstract: The present invention is related to processes for preparing 4-chloro-7H-pyrollo[2,3,-d]pyrimidine, and related synthetic intermediate compounds. 4-Chloro-7H-pyrrolo[2,3,-d]pyrimidine is an intermediate for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines, which are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.
    Type: Grant
    Filed: January 12, 2018
    Date of Patent: July 30, 2019
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: Jiacheng Zhou, James D. Rodgers, Haisheng Wang
  • Patent number: 10358416
    Abstract: The present invention is directed to a process for the preparation of aryl-carbonyl-pyrrolidine carboxylic acid derivative compounds which are useful in treating metabolic diseases, said process consisting of coupling a pyrrolidine ester compound with an aryl carboxylic acid derivative, followed by alkaline or acidic treatment, hydrogenolysis or treatment with a fluoride of the obtained intermediate, to afford novel aryl-carbonyl-pyrrolidine carboxylic acid derivative compounds.
    Type: Grant
    Filed: June 20, 2018
    Date of Patent: July 23, 2019
    Assignee: Epics Therapeutics
    Inventors: Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq
  • Patent number: 10357440
    Abstract: The present invention relates to the cosmetic use, in a composition containing a physiologically acceptable medium, of at least one compound of formula (I) in which: —R3 means a hydrogen atom or a hydroxyl radical, —R1 and R2 mean, independently of each other, a hydrogen atom, a linear or branched C1-C6 alkyl radical; a benzyl radical; a linear or branched C1-C6 alkylcarbonyl radical not conjugated with the carbonyl; or a linear or branched C1-C6 alkoxycarbonyl radical, and/or of an isomer and/or of a salt and/or of a solvate of said compound of formula (1), for preventing and/or treating the signs of ageing of the skin and its appendages.
    Type: Grant
    Filed: December 21, 2015
    Date of Patent: July 23, 2019
    Assignee: L'OREAL
    Inventors: Julien Hitce, Maria Dalko, Marie-Céline Frantz
  • Patent number: 10342794
    Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.
    Type: Grant
    Filed: April 4, 2018
    Date of Patent: July 9, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Jennifer R. Lo, Scott A. Mitchell, Aaron C. Schmitt, Sundaramoorthi Swaminathan, Jin-Ming Xiong, Jianjun Xu, Zhongdong Zhao
  • Patent number: 10344049
    Abstract: A compound and pharmaceutically acceptable salts thereof for treating cancer, having a structure represented by the following formula (I) or formula (II): in which X and Y each individually represent: R1, R2, R3, R4, and R5 individually represents hydrogen atom, acyl having 20 or less carbon atoms, alkyl having 20 or less carbon atoms, alkanoyl having 20 or less carbon atoms, aroyl having 20 or less carbon atoms, aryl having 20 or less carbon atoms, aralkyl having 20 or less carbon atoms, sulfonyl having 20 or less carbon atoms, phosphonyl having 20 or less carbon atoms, or haloacyl having 20 or less carbon atoms.
    Type: Grant
    Filed: December 14, 2017
    Date of Patent: July 9, 2019
    Assignee: AQUAVAN TECHNOLOGY CO., LTD
    Inventors: Shi-Yie Cheng, Yao-Ting Wang, Kuo-Tang Tseng, Wen-Hung Chen, Hsin Ju Wang
  • Patent number: 10336756
    Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of preparing such compounds are also disclosed, including the use of (S)-2-(1-aminopropyl)-5-fluoro-3-phenylquinazolin-4(3H)-one as a precursor to synthesize an exemplary compound disclosed in this application, (S)-2-(1-((9H-purin-6-yl)amino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.
    Type: Grant
    Filed: August 13, 2015
    Date of Patent: July 2, 2019
    Assignee: ICOS CORPORATION
    Inventors: Edward A. Kesicki, Kerry W. Fowler, Danwen Huang, Hua Chee Ooi, Amy Oliver, Kamal Deep Puri, Fuqiang Ruan, Jennifer Treiberg
  • Patent number: 10336763
    Abstract: The present invention relates to crystal forms B, C and D of Ribociclib succinate salt and derivatives thereof, and their preparation method and composition. The crystal forms B, C and D of Ribociclib succinate salts are obtained by adding 7-cyclopentyl-N,N-dimethyl-2-(5-(piperain-1-yl)pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide solution into succinic acid solution for reaction, stirring the solution under high temperature, filtering the solution after cooling off.
    Type: Grant
    Filed: August 3, 2018
    Date of Patent: July 2, 2019
    Assignee: CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO. LTD.
    Inventors: Satyanarayana Kamani, Tzu-Chiang Lu, Hsin-Yun Chang, Chin-Cheng Mai
  • Patent number: 10329277
    Abstract: The present disclosure relates to aniline pyrimidine derivatives or pharmaceutically acceptable salts thereof as EGFR inhibitors, specifically relates to compounds represented by formula (I) or pharmaceutically acceptable salts, pharmaceutical compositions, the method and uses thereof for treating EGFR mediated diseases.
    Type: Grant
    Filed: July 15, 2016
    Date of Patent: June 25, 2019
    Assignees: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD., CENTAURUS BIOPHARMA CO., LTD.
    Inventors: Yan Zhu, Na Zhao, Xianxing Shang, Yuandong Hu, Yong Peng, Hui Zhang, Bo Liu, Hong Luo, Yongxin Han, Ling Yang, Hongjiang Xu
  • Patent number: 10328074
    Abstract: Method for treating AML and MM by administration of a compound of the formula (I) wherein the groups R1 to R3 have the meanings given in the specification.
    Type: Grant
    Filed: January 14, 2016
    Date of Patent: June 25, 2019
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Harald Engelhardt, Davide Gianni, Christian Smethurst
  • Patent number: 10328054
    Abstract: Provided herein are compounds of the formula (I), as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment or prevention of mGluR5 mediated disorders, such as acute and/or chronic neurological disorders, cognitive disorders and memory deficits, as well as acute and chronic pain.
    Type: Grant
    Filed: October 21, 2016
    Date of Patent: June 25, 2019
    Assignee: Hua Medicine (Shanghai) Ltd.
    Inventors: Li Chen, Yuejiao Duan, Jin She, Chengde Wu
  • Patent number: 10329290
    Abstract: Disclosed is a preparation method for a Palbociclib free base crystal form A as shown in Formula I, comprising the following steps: treating a Palbociclib free base and/or a Palbociclib salt compound by using an inorganic base in a water solvent at the temperature of 35 to 100° C. to obtain a Palbociclib free base crystal form A, the water solvent being water or mixed solvent obtained by water and an organic solvent capable of being mixed and disclosed in the water. Also disclosed is a preparation method for a Palbociclib free base crystal form B, comprising the following steps: treating a Palbociclib salt compound by using an inorganic base in a water solvent at the temperature of 0 to 20° C. to obtain a Palbociclib free crystal form B, the water solvent being water or a mixed solvent obtained by water and an organic solvent capable of being mixed and dissolved in the water. The method is safe and convenient in operation and low in pollution, and facilitates industrial production.
    Type: Grant
    Filed: November 2, 2016
    Date of Patent: June 25, 2019
    Assignees: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD, SHANGHAI SYNCORES TECHNOLOGIES INC. LTD.
    Inventors: Haisheng Fan, Xiaowen Guo, Luning Huang, Hong Gu
  • Patent number: 10322130
    Abstract: The present invention provides PI3K protein kinase modulators of formula wherein R, Cy1, R1, R2, L1 and Cy2 are as defined herein. The present invention also relates to methods of preparing compounds of formula (I) to pharmaceutical compositions containing them and to methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: August 15, 2017
    Date of Patent: June 18, 2019
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventors: Dhanapalan Nagarathnam, Swaroop K. Vakkalanka, Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Prashant K. Bhavar
  • Patent number: 10314841
    Abstract: The present invention provides compounds of Formula (II) for the treatment of cancer, rheumatoid arthritis and other diseases.
    Type: Grant
    Filed: January 9, 2015
    Date of Patent: June 11, 2019
    Assignee: Merck Patent GmbH
    Inventors: Catherine Jorand-Lebrun, Reinaldo Jones
  • Patent number: 10316044
    Abstract: The present disclosure relates to certain chiral diaryl macrocyclic derivatives of the formula I pharmaceutical compositions containing them, and methods of using them to treat cancer, pain, neurological diseases, autoimmune diseases, and inflammation.
    Type: Grant
    Filed: June 30, 2016
    Date of Patent: June 11, 2019
    Assignee: TP Therapeutics, Inc.
    Inventors: Jingrong J. Cui, Yishan Li, Evan W. Rogers, Dayong Zhai, Wei Deng, Jane Ung
  • Patent number: 10316045
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disase pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: June 11, 2019
    Assignee: PFIZER INC.
    Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin