Patents Issued in November 2, 2017
  • ISOQUINOLIN-3-YL CARBOXAMIDES AND PREPARATION AND USE THEREOF
    Publication number: 20170313681
    Abstract: Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.
    Type: Application
    Filed: April 27, 2017
    Publication date: November 2, 2017
    Inventors: Sunil Kumar KC, Gopi Kumar Mittapalli, Brian Joseph Hofilena, Joseph Timothy Marakovits, Chandramouli Chiruta, Chi Ching Mak, Jianguo Cao
  • ISOQUINOLIN-3-YL CARBOXAMIDES AND PREPARATION AND USE THEREOF
    Publication number: 20170313682
    Abstract: Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Application
    Filed: April 27, 2017
    Publication date: November 2, 2017
    Inventors: Sunil Kumar KC, Chi Ching Mak, Brian Walter Eastman, Jianguo Cao, Venkataiah Bollu, Gopi Kumar Mittapalli, Chandramouli Chiruta
  • BTK INHIBITOR
    Publication number: 20170313683
    Abstract: Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV).
    Type: Application
    Filed: July 14, 2017
    Publication date: November 2, 2017
    Inventors: Xuehai Wang, Chengde Wu, Yong Xu, Chunli Shen, Li'e Li, Guoping Hu, Yang Yue, Jian Li, Diliang Guo, Nengyang Shi, Lu Huang, Shuhui Chen, Ronghua Tu, Zhongwen Yang, Xuwen Zhang, Qiang Xiao, Hua Tian, Yanping Yu, Hailiang Chen, Wenjie Sun, Zhenyu He, Jie Shen, Jing Yang, Jing Tang, Wen Zhou, Jing Yu, Yi Zhang, Quan Liu
  • PYRAZOLE OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20170313684
    Abstract: The present invention is directed to pyrazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the pyrazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: October 27, 2015
    Publication date: November 2, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: NIGEL LIVERTON, SCOTT D. KUDUK, YUNFU LUO
  • BROAD-SPECTRUM NON-COVALENT CORONAVIRUS PROTEASE INHIBITORS
    Publication number: 20170313685
    Abstract: This invention pertains to materials and methods for the treatment of patients with coronavirus infection and the control of zoonotic disease outbreaks using broad-spectrum non-covalent coronavirus protease inhibitors.
    Type: Application
    Filed: April 28, 2017
    Publication date: November 2, 2017
    Applicant: Purdue Research Foundation
    Inventors: Sarah Emma St. John, Andrew D. Mesecar
  • COMPOUNDS AND THEIR USE AS BACE INHIBITORS
    Publication number: 20170313686
    Abstract: The present application relates to compounds of formula (I), (Ia), or (Ib) and their pharmaceutical compositions/preparations. This application further relates to methods of treating or preventing A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia, including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease.
    Type: Application
    Filed: October 7, 2015
    Publication date: November 2, 2017
    Applicants: AstraZeneca AB, AstraZeneca AB
    Inventors: Roland Bürli, Mark E. Duggan, Jörg Holenz, Patrik Johansson, Karin Kolmodin, Philip Vellacott Thorne, Michael John McKenzie
  • Compounds and Compositions for Cognition-Enhancement, Methods of Making, and Methods of Treating
    Publication number: 20170313687
    Abstract: Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.
    Type: Application
    Filed: July 18, 2017
    Publication date: November 2, 2017
    Inventors: Michael L. Hendrickson, Jeffrey C. Ockuly, Trevor M. Twose, Melinda L. Verdone, Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson
  • HISTONE DEACETYLASE INHIBITORS AND USES THEREOF
    Publication number: 20170313688
    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 of cancer. Additionally, provided is a method for treating cancer, comprising the step of administering a therapeutically effective amount of a compound according to formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier to a patient in need thereof.
    Type: Application
    Filed: November 6, 2015
    Publication date: November 2, 2017
    Inventors: Patrick M. Woster, Youxuan Li
  • PROCESS FOR PREPARING A POLYMORPH OF RIVAROXABAN
    Publication number: 20170313689
    Abstract: This invention describes a process for the preparation of rivaroxaban modification I comprising: (i) dissolving rivaroxaban in a mixture of a solvent (e.g. THF) and an antisolvent (e.g. water and/or toluene), wherein the antisolvent has a higher boiling point than the solvent; (ii) removing the solvent by distillation; and (iii) collecting the resultant rivaroxaban modification I.
    Type: Application
    Filed: October 22, 2015
    Publication date: November 2, 2017
    Applicant: Zaklady Fammaceutyczne Polpharma SA
    Inventors: Karol Sagol, Magdalena Kozien-Sajnog
  • NOVEL MODULATORS OF CALCIUM RELEASE-ACTIVATED CALCIUM CHANNEL
    Publication number: 20170313690
    Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
    Type: Application
    Filed: June 28, 2017
    Publication date: November 2, 2017
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri S. Merikapudi, Swaroop K. Vakkalanka
  • 6-AMINOPYRIDIN-3-YL THIAZOLES AS MODULATORS OF RORyT
    Publication number: 20170313691
    Abstract: The present invention comprises compounds of Formula I. wherein: A1, A2, A3, A4, A5, R1, and R2 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
    Type: Application
    Filed: April 26, 2017
    Publication date: November 2, 2017
    Applicant: Janssen Pharmaceutica NV
    Inventors: Steven Goldberg, Kelly McClure, Virginia M. Tanis, Elizabeth G. Fennema, Alec D. Lebsack, Connor L. Martin, Hariharan Venkatesan, Xiaohua Xue, Craig R. Woods
  • AGONISTS OF THE MU OPIOID RECEPTOR
    Publication number: 20170313692
    Abstract: The present technology is directed to compounds, compositions, and methods related to non-morphinan-like mu opioid receptor agonists. Compounds of the present technology demonstrate remarkable potency and selectivity for the mu opioid receptor over the kappa opioid receptor, while also exhibiting a significant reduction (or, essentially, absence) of the negative side effects of many morphine-derived compounds.
    Type: Application
    Filed: April 27, 2017
    Publication date: November 2, 2017
    Inventors: Thomas E. Prisinzano, Andrew P. Riley, Chad E. Groer
  • PIPERIDINE OXADIAZOLE AND THIADIAZOLE OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20170313693
    Abstract: The present invention is directed to piperidine oxadiazole and thiadiazole orexin compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: September 27, 2015
    Publication date: November 2, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: NIGEL LIVERTON, SCOTT D. KUDUK, YUNFU LUO, NA MENG, TINGTING YU
  • Crystalline Form of (R)-7-Chloro-N-(Quinuclidin-3-YL)benzo[B]thiophene-2-Carboxamide Hydrochloride Monohydrate
    Publication number: 20170313694
    Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.
    Type: Application
    Filed: December 12, 2016
    Publication date: November 2, 2017
    Inventors: Patricia Oliver-Shaffer, Gideon Shapiro, Richard Chesworth, Muneki Kishida, Takayuki Ishige
  • PROCESS FOR THE PREPARATION OF APIXABAN
    Publication number: 20170313695
    Abstract: The present invention relates to an improved process for the preparation of Apixaban and its intermediates.
    Type: Application
    Filed: July 28, 2016
    Publication date: November 2, 2017
    Inventors: Srinivas Reddy DESI REDDY, Dnyandev Ragho RANE, Venkata Srinivaso Rao VELIVELA
  • ISOXAZOLE DERIVATIVE AS MUTANT ISOCITRATE DEHYDROGENASE 1 INHIBITOR
    Publication number: 20170313696
    Abstract: It has been found that a compound of the general formula (I) having an isoxazole skeleton has excellent inhibitory activity against mutant IDH1 protein and inhibits the production of 2-HG by this protein, while the compound is also capable of effectively inhibiting the growth of various tumors expressing the protein. In the formula, R1, R2, R3, Y, and Z are as defined in claim 1.
    Type: Application
    Filed: October 1, 2015
    Publication date: November 2, 2017
    Applicants: Daiichi Sankyo Company, Limited, National Cancer Center
    Inventors: Shoichi Saito, Masao Itoh, Tetsunori Fujisawa, Hironao Saito, Yohei Kiyotsuka, Hideaki Watanabe, Hironori Matsunaga, Yoshiko Kagoshima, Tetsuya Suzuki, Yoko Ogawara, Kazuo Kitabayashi
  • PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AND USE THEREOF
    Publication number: 20170313697
    Abstract: Disclosed in the disclosure are a pyrazolo[1,5-a]pyrideine compound with structural features as shown in formula (I) or a pharmaceutically acceptable salt, stereoisomer or prodrug molecule thereof and a use thereof. Such compounds have a good in vitro antituberculosis activity, and the minimal inhibitory concentration (MIC) of the compounds is lower than 0.1 ?g/mL and partially achieves 0.01 ?g/mL, and have a very strong inhibiting effect on clinically selected multi-drug resistant tuberculosis (MDR-TB) strains. In an in vivo experiment, the pyrazolo[1,5-a]pyrideine compounds of the present disclosure can effectively scavenge the infectious dose of H37Ra in a mouse body at 20 mg/kg/d does, thereby being a new type of antituberculosis compound.
    Type: Application
    Filed: August 13, 2015
    Publication date: November 2, 2017
    Inventors: Xiaoyun Lu, Jian Tang, Ke Ding, Tianyu Zhang, Xiantao Zhang, Zhengchao Tu, Tian Wu, Junting Wan, Yuanyuan Cao, Shengjiang He
  • POLYHETEROARL HISTONE DEACETYLASE INHIBITORS AND THEIR USE IN THERAPY
    Publication number: 20170313698
    Abstract: The present invention is a compound having the following formula: or a pharmaceutically acceptable salt thereof, wherein e.g. L and Y are each independently an optionally substituted 6-membered nitrogen-containing heteroaryl; M is an optionallysubstituted 5- to 10-membered heteroaryl; W is a zinc-binding group; each R2 is independently hydrogen or C1-C6 alkyl; and R3 is an aryl or heteroaryl. The compounds are useful as histone deacetylase (HDAC) inhibitors.
    Type: Application
    Filed: October 29, 2015
    Publication date: November 2, 2017
    Inventors: Stephen Joseph Shuttleworth, Alexander Richard Liam Cecil, Somhairle MacCormick, William John Nodes, Cyrille Davy Tomassi, Franck Alexandre Silva
  • PROCESS FOR THE PREPARATION OF APIXABAN AND INTERMEDIATES THEREOF
    Publication number: 20170313699
    Abstract: The present invention relates to an improved process for the preparation of Apixaban and intermediates thereof. Further the present invention also relates to novel intermediate of Formula V and its process for the preparation.
    Type: Application
    Filed: October 20, 2015
    Publication date: November 2, 2017
    Applicant: JUBILANT GENERICS LIMITED
    Inventors: Khushwant SINGH, Amit Kumar SRIVASTAVA, Ratnakar TRIPATHI, Jai Prakash VERMA, Dharam VIR, Lalit KUMAR, Mukesh MASAND, Rajendra Singh SHEKHAWAT, Rakesh TIWARI, Sujay BISWAS
  • SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINES AND IMIDAZO[1,2-A]PYRAZINES AND THEIR USE
    Publication number: 20170313700
    Abstract: The present application relates to novel substituted pyrazolo[1,5-a]pyridines and imidazo[1,2-a]pyrazines, 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: Application
    Filed: November 30, 2015
    Publication date: November 2, 2017
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Alexandros VAKALOPOULOS, Damian BROCKSCHNIEDER, Frank WUNDER, Johannes-Peter STASCH, Tobias MARQUARDT, Lisa DIETZ, Volkhart Min-Jian LI
  • Fused Heterocyclic Compounds as Selective BMP Inhibitors
    Publication number: 20170313701
    Abstract: The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.
    Type: Application
    Filed: July 17, 2017
    Publication date: November 2, 2017
    Inventors: Corey R. Hopkins, Charles C. Hong, Craig W. Lindsley, Darren W. Engers
  • HISTONE DEMETHYLASE INHIBITORS
    Publication number: 20170313702
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrrolopyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: July 17, 2017
    Publication date: November 2, 2017
    Applicant: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Young K. Chen, Michael Brennan Wallace
  • Cis-tetrahydro-spiro(cyclohexane-1,1?-pyrido[3,4-b]indole)-4-amine Compounds
    Publication number: 20170313703
    Abstract: Cis-tetrahydro-spiro(cyclohexane-1,1?-pyrido[3,4-b]indole)-4-amine compounds which act on the nociceptin/ORL-1 receptor system as well as on the ?-opioid receptor system and which are distinguished in particular by selective effectiveness in the treatment of chronic pain, such as inflammatory pain, visceral pain, tumour pain, and neuropathic pain, without at the same time developing pronounced effectiveness against acute, nociceptive pain.
    Type: Application
    Filed: July 19, 2017
    Publication date: November 2, 2017
    Inventors: Klaus LINZ, Saskia ZEMOLKA, Bert NOLTE, Stefan SCHUNK, Hans SCHICK
  • PROCESS FOR MAKING TRICYCLIC LACTAM COMPOUNDS
    Publication number: 20170313704
    Abstract: Processes are described for the preparation of tricyclic lactam compound of Formula (I), having the structure and intermediates useful for the preparation of (I).
    Type: Application
    Filed: July 18, 2017
    Publication date: November 2, 2017
    Applicant: Genentech, Inc.
    Inventors: Ngiap-Kie Lim, Haiming Zhang, Chong Han
  • PURINONE DERIVATIVE
    Publication number: 20170313705
    Abstract: Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.
    Type: Application
    Filed: July 13, 2017
    Publication date: November 2, 2017
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shingo YAMAMOTO, Toshio YOSHIZAWA
  • PURINONE DERIVATIVE HYDROCHLORIDE
    Publication number: 20170313706
    Abstract: The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.
    Type: Application
    Filed: July 19, 2017
    Publication date: November 2, 2017
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shingo YAMAMOTO, Toshio YOSHIZAWA
  • SOLID FORMS OF A TOLL-LIKE RECEPTOR MODULATOR
    Publication number: 20170313707
    Abstract: The present invention provides crystalline forms, solvates and hydrates of 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one, and methods of making.
    Type: Application
    Filed: May 10, 2017
    Publication date: November 2, 2017
    Inventors: Patricia Andres, Brandon Heath Brown, Krista Marie Diaz, Yoo Joong Kim, Paul A. Roethle, Valeriya Smolenskaya, Fang Wang
  • NONANOIC AND DECANOIC ACID DERIVATIVES AND USES THEREOF
    Publication number: 20170313708
    Abstract: The present disclosure relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present disclosure also relates to pharmaceutical compositions containing the fluorinated compounds of the disclosure, and methods of treating fibrosis, macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: April 27, 2017
    Publication date: November 2, 2017
    Inventors: Takeru Furuya, Ben C. Askew
  • CRYSTALLINE FORM OF JAK KINASE INHIBITOR BISULFATE AND A PREPARATION METHOD THEREOF
    Publication number: 20170313709
    Abstract: A crystal form of JAK kinase inhibitor bisulfate and a preparation method thereof are provided. In particular, a type II crystal of (3aR,5s,6aS)-N-(3-methoxyl-1,2,4-thiadiazole-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-formamide bisulfate and a preparation method thereof are described. The preparation method includes steps of crystallizing any solid crystal form or amorphous compound of formula (I) in a single organic solvent or a mixed organic solvent to obtain a type II crystal form of the compound of formula (I). The type II crystal form of the compound of formula (I) obtained by the described methods has good crystal stability and chemical stability. In addition, the solvent used for crystallization has low toxicity and residue, which is better suited for use in clinical treatment.
    Type: Application
    Filed: October 9, 2015
    Publication date: November 2, 2017
    Inventors: Piaoyang SUN, Guaili WU, Quanliang ZHANG, Yongjiang CHEN, Lingjia SHEN
  • TRICYCLIC TRIAZOLIC COMPOUNDS
    Publication number: 20170313710
    Abstract: The present invention relates to new tricyclic triazolic compounds having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
    Type: Application
    Filed: July 2, 2015
    Publication date: November 2, 2017
    Applicant: Laboratorios del Dr. Esteve, S.A.
    Inventors: Félix CUEVAS-CORDOBÉS, Miguel Angel PERICÁS-BRONDO
  • 1,5-DISUBSTITUTED 1,2,3-TRIAZOLES ARE INHIBITORS OF RAC/CDC42 GTPASES
    Publication number: 20170313711
    Abstract: Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.
    Type: Application
    Filed: April 27, 2017
    Publication date: November 2, 2017
    Inventors: Cornelis P. VLAAR, Suranganie DHARMAWARDHANE FLANAGAN, Eliud HERNANDEZ-O'FARRILL, Linette CASTILLO-PICHARDO
  • DIHETEROARYL HISTONE DEACETYLASE INHIBITORS AND THEIR USE IN THERAPY
    Publication number: 20170313712
    Abstract: The present invention is a compound having the following formula: (Formula (I)) or a pharmaceutically acceptable salt thereof, wherein e.g. X is C or N; n is 1 to 10; each L is independently a 5- to 12-membered heteroaryl containing at least two nitrogen atoms; and W is a zinc-binding group. The compounds are useful as histone deacetylase (HDAC) inhibitors.
    Type: Application
    Filed: October 29, 2015
    Publication date: November 2, 2017
    Inventors: Stephen Joseph Shuttleworth, Alexander Richard Liam Cecil, Somhairle MacCormick, William John Nodes, Cyrille Davy Tomassi
  • AMINOINDANE-, AMINOTETRAHYDRONAPHTHALENE- AND AMINOBENZOCYCLOBUTANE-DERIVED PRMT5-INHIBITORS
    Publication number: 20170313713
    Abstract: A compound of formula (1a), (1b) or (1c) wherein: n is 1 or 2; RN is H or Me; R1 is optionally one or more halo or methyl groups; R1 and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4a is selected from OH, —NH2, —C(?O)NH2, and —CH2OH; R4b is either H or Me; R5 is either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl.
    Type: Application
    Filed: September 3, 2015
    Publication date: November 2, 2017
    Inventors: Ylva Elisabet Bergman, Romina Lessene, Danny Ganame, Richard Charles Foitzik, Benjamin Joseph Morrow, Michelle Ang Camerino, Scott Raymond Walker, H. Rachel Lagiakos, John Feutrill, Paul Anthony Stupple
  • EGFR INHIBITOR, PREPARATION METHOD AND USE THEREOF
    Publication number: 20170313714
    Abstract: Epidermal growth factor receptor (EGFR) inhibitors are provided. In particular, 4-substituted-2-(N-(5-substituted allyl amide)phenyl)amino)pyrimidine derivatives of formula (I), a preparation method and use thereof as an EGFR inhibitor are provided. The 4-substituted-2-(N-(5-substituted allyl amide)phenyl)amino)pyrimidine derivatives of formula (I) have inhibitory activity against the L858R EGFR mutant, the T790M EGFR mutant and the exon 19 deletion activating mutant, and can be used to treat diseases mediated alone or in part by EGFR mutant activity. The derivatives of formula (I) can be used to treat and/or prevent cancers, particularly non-small cell lung cancer.
    Type: Application
    Filed: September 30, 2015
    Publication date: November 2, 2017
    Applicants: Shanghai Hansoh Biomedical Co., Ltd., Jiangsu Hansoh Pharmaceutical Group Co., Ltd.
    Inventors: Mingsong WEI, Guangjun SUN, Songliang TAN, Peng GAO, Shaobao WANG, Wenhua XIU, Fujun ZHANG, Rudi BAO
  • SIX-MEMBERED RING BENZO DERIVATIVES AS DPP-4 INHIBITOR AND USE THEREOF
    Publication number: 20170313715
    Abstract: The present invention relates to six-membered ring benzo derivatives as a DPP-4 inhibitor and a use thereof. In particular, the present invention relates to a compound as shown in formula I, a pharmaceutical composition containing the compound as shown in formula I and a use of the compound in the preparation of drugs for treating DPP-4 related diseases or inhibiting DPP-4.
    Type: Application
    Filed: October 30, 2015
    Publication date: November 2, 2017
    Inventors: Honglin LI, Hualiang JIANG, Yufang XU, Jia LI, Zhenjiang ZHAO, Jingya LI, Hongling XU, Shiliang LI
  • ORIDONIN ANALOGS, COMPOSITIONS, AND METHODS RELATED THERETO
    Publication number: 20170313716
    Abstract: Certain embodiments are directed to oridonin analogs or derivatives. In certain aspects, the derivatives are used as anticancer or anti-inflammatory agents.
    Type: Application
    Filed: June 28, 2017
    Publication date: November 2, 2017
    Inventors: Jia ZHOU, Chunyong DING, Qiang SHEN
  • NOVEL GLP-1 RECEPTOR MODULATORS
    Publication number: 20170313717
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
    Type: Application
    Filed: January 26, 2017
    Publication date: November 2, 2017
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
  • INHIBITORS OF HIF PROLYL HYDROXYLASE
    Publication number: 20170313718
    Abstract: The present invention concerns compounds of formula I or a pharmaceutically acceptable salt thereof which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
    Type: Application
    Filed: September 23, 2015
    Publication date: November 2, 2017
    Applicants: MERCK SHARP & DOHME CORP., MSD R&D (CHINA) CO., LTD.
    Inventors: JIAQIANG CAI, ALEJANDRO CRESPO, JOHN DEBENHAM, XIAOXING DU, PING LIU, RONGQIANG LIU, CHRISTINA B. MADSEN-DUGGAN, WEIGUO QUAN, CHRISTOPHER SINZ, LIPING WANG
  • Thieno[2,3-D]pyrimidin-4-one Derivatives as NMDAR Modulators and Uses Related Thereto
    Publication number: 20170313719
    Abstract: The disclosure relates thieno[2,3-d]pyrimidin-4-one derivatives as modulators of NMDA receptors and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising compounds disclosed herein or pharmaceutically acceptable salts or prodrugs thereof. In certain embodiments, the compositions disclosed herein are used for managing conditions related to cognition, typically prevention or treatment of neurological conditions related to the NMDA receptor.
    Type: Application
    Filed: November 18, 2015
    Publication date: November 2, 2017
    Inventors: Stephen F. Traynelis, Lanny S. Liebeskind, Dennis C. Liotta, Ethel C. Garnier-Amblard, PavanKumar Reddy Gangireddy
  • METHODS FOR TREATMENT OF RESISTANT CANCER
    Publication number: 20170313720
    Abstract: The present disclosure describes a method to treat conditions, including cancer, using compounds that can target resistant cancer cells. The compounds of the invention can decrease the rate of proliferation of drug-resistant cancer cells, such as glioma, lung cancer, and uterine sarcoma.
    Type: Application
    Filed: April 27, 2017
    Publication date: November 2, 2017
    Inventors: Snezna ROGELJ, Liliya FROLOVA, Alexander KORNIENKO, Sean HENRY
  • SUBSTITUTED 1,2,3-TRIAZOL-1-YL-METHYL-2,3-DIHYDRO-2-METHYL-6-NITROIMIDAZO[2,1-B]OXAZOLES AS ANTI-MYCOBACTERIAL AGENTS AND A PROCESS FOR THE PREPARATION THEREOF
    Publication number: 20170313721
    Abstract: The present invention relates to new generation of triazole functionality containing 6-nitro-2,3-dihydroimidazooxazole agents for general formula I, their method of preparation and their use as drugs for treatment of tuberculosis, MDR-TB and XDR-TB either alone or in combination with other anti-tubercular agents.
    Type: Application
    Filed: September 9, 2015
    Publication date: November 2, 2017
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Kushalava Reddy YEMPALLA, Gurunadham MUNAGALA, Samsher SINGH, Sumit SHARMA, Inshad Ali KHAN, Ram Asrey VISHWAKARMA, Parvinder Pal SINGH
  • TETRAHYDRONAPHTHYRIDINE AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
    Publication number: 20170313722
    Abstract: The invention provides tetrahydronaphthyridine and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydronaphthyridine and related compounds.
    Type: Application
    Filed: May 5, 2017
    Publication date: November 2, 2017
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Blair T. Lapointe, Vladimir Simov, Karin A. Stein, William D. Thomas, Peter L. Toogood, Chad A. VanHuis, Catherine M. White
  • Alkyl derivatives of 1-oxa-4,9-diazaspiro undecane compounds having multimodal activity against pain
    Publication number: 20170313723
    Abstract: The present invention relates to compounds having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opiod receptor and more particularly to diazaspiro undecane compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Application
    Filed: June 2, 2015
    Publication date: November 2, 2017
    Applicant: Laboratorios del Dr. Esteve, S.A.
    Inventors: Marina VIRGILI-BERNADO, Monica ALONSO-XALMA, Carlos ALEGRET-MOLINA, Carmen ALMANSA-ROSALES, Monica GARCIA LOPEZ
  • CRYSTALLINE FORMS OF A THERAPEUTIC COMPOUND AND USES THEREOF
    Publication number: 20170313724
    Abstract: Disclosed herein are certain crystalline forms of Compound 5, N-(5-((2-(4-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butanamido)imidazo[1,2-0]pyridazin-6-yl)oxy)-2-methylphenyl)-1,3-dimethyl-1/-/-pyrazole-5-carboxamide, as well as pharmaceutical compositions comprising the crystalline forms. The present disclosure further relates to methods for treating or preventing diseases or disorders using the crystalline forms or pharmaceutical compositions thereof in a subject in need thereof, including diseases or disorders associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor signaling pathway (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases and ocular diseases.
    Type: Application
    Filed: November 24, 2015
    Publication date: November 2, 2017
    Inventors: Tadeas Liska, Elizabeth Enlow, Jinsoo Kim, Winston Ong
  • Process For Producing Tetrakis(F aryl)Borate Salts
    Publication number: 20170313725
    Abstract: This invention provides processes for forming halomagnesium tetrakis(Faryl)borates, which processes comprise bringing together, in an anhydrous liquid organic medium, at least one boron trihalide; at least one Faryl Grignard reagent; and at least one copper compound. Also provided are processes for forming halomagnesium tetrakis(Faryl)borates, which processes comprise bringing together, in an anhydrous liquid organic medium, at least one boron trihalide; at least one copper compound; magnesium metal; and at least one polyhaloaromatic compound.
    Type: Application
    Filed: July 17, 2017
    Publication date: November 2, 2017
    Inventors: Rajeev S. Mathur, Jamie R. Strickler
  • BIODEGRADABLE HYBRID POLYMERS USABLE IN MEDICAL TECHNOLOGY OR IN BIOLOGY, STARTING SILANES THEREFOR, AND PREPARATION PROCESS THEREFOR AND USES THEREOF
    Publication number: 20170313726
    Abstract: The invention relates to a silane or silane mixture obtainable by reacting a hydrolysable silane of the formula (A): SiR4 in which R is a hydrolytically condensable group or hydroxyl with a compound R*(OH)x where x is 1, 2, 3 or greater 3, where R* has a straight-chain or branched hydrocarbon skeleton which, according to the number x, is monovalent, divalent, trivalent or multivalent, and has a hydrocarbonaceous chain interrupted by at least two —C(O)O— groups, wherein there are a maximum of 8 successive carbon atoms in the individual hydrocarbon units formed by interruptions within this chain and the, or in the case of branched structures at least one, end of the hydrocarbonaceous chain at the opposite end to the sole hydroxyl group or one of the hydroxyl groups bears an organically polymerizable group, wherein the alcohol is otherwise unsubstituted or has further substituents.
    Type: Application
    Filed: August 28, 2015
    Publication date: November 2, 2017
    Applicant: Fraunhofer-Gesellschaft Zur Forderung der Angewandten Forschung E.V.
    Inventors: Herbert WOLTER, Somchith NIQUE, Kerstin OBEL
  • SUBSTITUTED DIHYDROPYRROLOPYRAZOLE COMPOUND
    Publication number: 20170313727
    Abstract: Provided is a compound represented by formula (I) or a pharmacologically acceptable salt thereof: wherein L1 is an optionally substituted C1-6 alkylene group or the like, L2 is a single bond or the like, L3 is a single bond or the like, R1, R2, and R3 are each independently an optionally substituted C1-4 alkyl group or the like, R4 is a hydrogen atom or the like, and R5 is a hydrogen atom or the like.
    Type: Application
    Filed: October 30, 2015
    Publication date: November 2, 2017
    Applicant: UBE INDUSTRIES, LTD.
    Inventors: Yasuhiro AGA, Shigeru USHIYAMA, Noriaki IWASE, Shigeyuki KONO, Hidetoshi SUNAMOTO, Takashi MATSUSHITA, Sayaka OGI, Masayuki TANAKA, Masaaki MATOYAMA, Satoshi UMEZAKI, Yusuke SHIRAISHI, Kazuhiro ONUMA, Masahiro KOJIMA, Hayato NISHIYAMA, Tomio KIMURA
  • TRANSPARENT FILM
    Publication number: 20170313728
    Abstract: The object of the present invention is to attain water repellency as well as the heat resistance and the light resistance. the transparent film of the present invention comprises: a polysiloxane backbone; and a trialkylsilyl containing molecular chain bonded to a part of silicon atoms forming the polysiloxane backbone, wherein alkyl groups in the trialkylsilyl containing molecular chain may be replaced by fluoroalkyl groups, and the transparent film satisfies at least one of the relationships of: (BH?A0)/A0×100(%)??27(%); and (BL?A0)/A0×100(%)??15(%), provided that A0 is an initial contact angle of a liquid droplet on the transparent film, BH is a contact angle of a liquid droplet on the transparent film incubated at 200° C. for 24 hours, and BL is a contact angle of a liquid droplet on the transparent film irradiated by a xenon lamp with an intensity of 250 W for 100 hours.
    Type: Application
    Filed: October 27, 2015
    Publication date: November 2, 2017
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Sayaka SAKURAI, Tomonori MIYAMOTO, Ryu TAKEKO
  • METHOD OF HYDROSILYLATION IMPLEMENTING AN ORGANIC CATALYST DERIVED FROM GERMYLENE
    Publication number: 20170313729
    Abstract: The present invention concerns a method for the hydrosilylation of an unsaturated compound comprising at least one ketone function, one aldehyde function, one alkene function and/or one alkyne function, with a compound comprising at least one hydrogen-silyl function implementing an organic catalyst of tri-coordinated germanium.
    Type: Application
    Filed: November 12, 2015
    Publication date: November 2, 2017
    Inventors: ANTOINE BACEIREDO, TSUYOSHI KATO, YANLI MAO, JULIETTE BERTHE, MAGALI BOUSQUIÉ
  • PROCESS FOR PREPARING PHOSPHORUS CONTAINING CYANOHYDRINS
    Publication number: 20170313730
    Abstract: The present invention relates primarily to a process for preparing certain phosphorus-containing cyanohydrins of the formula (I), and also to certain phosphorus-containing cyanohydrins per se and to their use for the preparation of glufosinate and/or glufosinate salts. The present invention further relates to certain mixtures particularly suitable for preparing the phosphorus-containing cyanohydrins of the formula (I).
    Type: Application
    Filed: July 20, 2017
    Publication date: November 2, 2017
    Inventors: Hans-Joachim RESSEL, Kilian TELLMAN, Mark James FORD, Martin LITTMANN, Friedrich August MUEHLTHAU, Guenter SCHLEGEL