Patents Issued in August 15, 2019
  • CYCLOPROPYL UNSATURATED QUINOLINE COMPOUND USED AS LEUKOTRIENE RECEPTOR ANTAGONIST AND APPLICATIONS THEREOF
    Publication number: 20190248746
    Abstract: A cyclopropyl unsaturated quinoline compound used as leukotriene receptor antagonist and applications thereof, wherein the structural formula of the compound is as follows: An application of the compound or its pharmaceutically acceptable salts, hydrates, solvates, or prodrugs in preparing a drug for treating and/or preventing and/or delaying and/or providing adjuvant therapy for asthma and/or allergic rhinitis and asthma syndromes is provided. A drug composition includes the cyclopropyl unsaturated quinoline compound or the pharmaceutically acceptable salts, hydrates, solvates, or prodrugs thereof. The compound series has favorable foreground in preparing drugs for treating and/or preventing and/or delaying and/or providing adjuvant therapy for asthma and/or allergic rhinitis and asthma syndromes.
    Type: Application
    Filed: April 23, 2019
    Publication date: August 15, 2019
    Inventor: Yingjie LAI
  • ASYMMETRIC BISAMINOQUINOLINES AND BISAMINOQUINOLINES WITH VARIED LINKERS AS AUTOPHAGY INHIBITORS FOR CANCER AND OTHER THERAPY
    Publication number: 20190248747
    Abstract: The invention provides novel asymmetric and symmetric bisaminoquinolmes and related compounds, methods of treatment and syntheses. The novel compounds exhibit effective anticancer activity and are useful in the treatment of a variety of autophagy-related disorders.
    Type: Application
    Filed: November 27, 2018
    Publication date: August 15, 2019
    Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: Ravi K. Amaravadi, Jeffrey Winkler
  • PROCESSES FOR THE PREPARATION OF ELUXADOLINE
    Publication number: 20190248748
    Abstract: The present invention relates to processes for the preparation of eluxadoline. The present invention also provides a compound of Formula V, a process for its preparation, and its use for the preparation of eluxadoline.
    Type: Application
    Filed: September 20, 2017
    Publication date: August 15, 2019
    Inventors: Murad Ismail INAMDAR, Sriram Hari MOHAN, Ketan Vithalbhai HIRPARA
  • MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    Publication number: 20190248749
    Abstract: Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Application
    Filed: October 15, 2018
    Publication date: August 15, 2019
    Inventors: Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou
  • METHOD FOR PRODUCING (4S)-4-[4-CYANO-2-(METHYLSULFONYL)PHENYL]-3,6-DIMETHYL-2-OXO-1-[3-(TRIFLUOROMETHYL)PHENYL]-1,2,3,4-TETRAHYDRO PYRIMIDINE-5-CARBONITRILE
    Publication number: 20190248750
    Abstract: The invention relates to a new and improved method for preparation of (4S)-4-[4-cyano-2-(methyl sulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I), as well as the preparation and use of the crystal form (A) of (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I).
    Type: Application
    Filed: April 25, 2019
    Publication date: August 15, 2019
    Applicant: pH Pharma Co., Ltd.
    Inventors: Heiko Schirmer, Philipp Rubenbauer, Birgit Keil, Britta Olenik
  • Pyrimidone Compounds Used as Lp-PLA2 Inhibitors and Pharmaceutical Compositions Thereof
    Publication number: 20190248751
    Abstract: The present invention relates to pyrimidone compounds used as Lp-PLA2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R1, R2, R3, X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA2 enzyme.
    Type: Application
    Filed: March 12, 2019
    Publication date: August 15, 2019
    Inventors: Jianhua Shen, Yiping Wang, Xinde Chen, Wenwei Xu, Kai Wang
  • HETEROCYCLIC FXR MODULATORS
    Publication number: 20190248752
    Abstract: The present technology is directed to compounds of formula (I), compositions, and methods related to modulation of FXR. In particular, the present compounds and compositions may be used to treat FXR-mediated disorders and conditions, including, e.g., liver disease, hyperlipidemia, hypercholesteremia, obesity, metabolic w syndrome, cardiovascular disease, gastrointestinal disease, and atherosclerosis, and renal disease.
    Type: Application
    Filed: September 27, 2017
    Publication date: August 15, 2019
    Inventor: Xiaodong XU
  • OXAZOLIDINONE COMPOUNDS AND METHODS OF USE THEREOF AS ANTIBACTERIAL AGENTS
    Publication number: 20190248753
    Abstract: The present invention relates to oxazolidinone compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, E, and R1 are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.
    Type: Application
    Filed: April 29, 2019
    Publication date: August 15, 2019
    Inventors: Mihir B. Mandal, David B. Olsen, Jing Su, Lihu Yang, Katherine Young, Takao Suzuki, Lanying You
  • GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
    Publication number: 20190248754
    Abstract: Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
    Type: Application
    Filed: January 18, 2019
    Publication date: August 15, 2019
    Inventor: Bing Wang
  • CRYSTAL FORM OF OZANIMOD HYDROCHLORIDE, AND PREPARATION METHOD THEREFOR
    Publication number: 20190248755
    Abstract: The present disclosure relates to crystalline form CS3 of ozanimod hydrochloride which can be used for treating autoimmune diseases, particularly used for preparing drugs for treating multiple sclerosis and ulcerative colitis and preparation method thereof.
    Type: Application
    Filed: September 14, 2017
    Publication date: August 15, 2019
    Applicant: Crystal Pharmaceutical (Suzhou) Co., Ltd.
    Inventors: Minhua CHEN, Yanfeng ZHANG, Xiaoting ZHAI, Kaiqiang YAN, Chaohui YANG, Xiaoyu ZHANG
  • BCL-3 INHIBITORS
    Publication number: 20190248756
    Abstract: The present application relates to compounds of any one of Formulae I, Ia, Ib, Ic, Id, Ie, and If. Compounds of Formula I have the structure: wherein A, B, Y, Z, R2, R4, R5, R6, Rq and q are as defined herein. The compounds can be used as inhibitors of Bcl-3 and can be used for the treatment of cancer, particularly metastatic cancer.
    Type: Application
    Filed: April 29, 2019
    Publication date: August 15, 2019
    Inventors: Andrew David Westwell, Andrea Brancale, Richard William Ernest Clarkson
  • PHOTOINITIATORS WITH PROTECTED CARBONYL GROUP
    Publication number: 20190248757
    Abstract: Disclosed are of the protected photoinitiators of the formula: wherein Aryl1 is an aromatic or heteroaromatic ring; Aryl2 is an aromatic ring; each R1 is an alkyl, an aryl, an electron donating group or an electron withdrawing group, and subscript a is 0 to 3; each R2 is an alkyl, an aryl, an electron donating group or an electron withdrawing group, and subscript b is 0 to 3; Prot is a protected carbonyl group.
    Type: Application
    Filed: October 9, 2017
    Publication date: August 15, 2019
    Inventors: Kelly A. Volp, Shih-Hung Chou, Paul J. Homnick, Ahmed S. Abuelyaman, Tao Gong, Joel D. Oxman, Wayne S. Mahoney
  • Novel Process for Preparation of Rotigotine and Intermediates Thereof
    Publication number: 20190248758
    Abstract: The present invention relates to a novel process for the preparation of Rotigotine of formula (I) and intermediates thereof.
    Type: Application
    Filed: February 14, 2019
    Publication date: August 15, 2019
    Inventors: Victor Paul Raj Irudayaraj, Senthilkumar Subramani, Vedhachalam Govindaraj, Jeyakanthan Jayavelu, Boopathy Jayaraman, Uttam Kumar Ray, Tangirala Vittal
  • METHOD FOR PRODUCING 3-METHYL-2-THIOPHENECARBOXYLIC ACID
    Publication number: 20190248759
    Abstract: To provide a method for producing 3-methyl-2-thiophenecarboxylic acid. A method for producing 3-methyl-2-thiophenecarboxylic acid, which comprises reacting 3-methylthiophene with chlorosulfonyl isocyanate, and hydrolyzing the obtained reaction product.
    Type: Application
    Filed: October 24, 2017
    Publication date: August 15, 2019
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventor: Tatsunori YOSHIDA
  • INDOLE CARBOXAMIDE COMPOUNDS
    Publication number: 20190248760
    Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR4 or N; R1, R2, R3, R4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Application
    Filed: April 29, 2019
    Publication date: August 15, 2019
    Inventors: Qingjie LIU, Scott Hunter Watterson, John E. Macor, Khehyong Ngu, Saleem Ahmad
  • NON-SELECTIVE KINASE INHIBITORS
    Publication number: 20190248761
    Abstract: Disclosed herein are compounds, compositions, and methods for preventing and treating proliferative diseases associated with aberrant receptor tyrosine kinase (RTK) activity. The therapeutic indications described herein more specifically relate to the non-selective inhibition of RTKs associated with vascular and pulmonary disorders.
    Type: Application
    Filed: February 12, 2019
    Publication date: August 15, 2019
    Inventor: Lawrence S. Zisman
  • APOPTOSIS SIGNAL-REGULATING KINASE INHIBITOR
    Publication number: 20190248762
    Abstract: The present invention relates to a compound of formula (I): The compound has apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis.
    Type: Application
    Filed: January 11, 2019
    Publication date: August 15, 2019
    Inventor: Gregory Notte
  • PYRIDONE COMPOUND AS C-MET INHIBITOR
    Publication number: 20190248763
    Abstract: Disclosed in the present invention is a type of pyridone compounds as c-met inhibitors, and specifically disclosed is a compound as shown in formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 23, 2017
    Publication date: August 15, 2019
    Applicant: FUJIAN COSUNTER PHARMACEUTICAL CO., LTD.
    Inventors: Xiongbin XU, Gang LI, Charles Z. DING, Lihong HU, Guoping HU, Jian LI, Shuhui CHEN, Zhigang CHI, Kun WANG
  • PIPERAZINE DERIVATIVES AS TRPML MODULATORS
    Publication number: 20190248764
    Abstract: The new piperazine derivatives are modulators of TRPML and are useful in treating disorders related to TRPML activities such as lysosome storage diseases, muscular dystrophy, age-related common neurodegenerative diseases, oxidative stress or reactive oxygen species (ROS) related diseases, and ageing.
    Type: Application
    Filed: June 29, 2017
    Publication date: August 15, 2019
    Applicant: CalyGene Biotechnolgy, Inc.
    Inventor: Congxin Liang
  • COMPOUNDS, COMPOSITIONS, AND METHODS FOR INCREASING CFTR ACTIVITY
    Publication number: 20190248765
    Abstract: The present disclosure is directed to disclosed compounds that modulate, e.g., address underlying defects in cellular processing of CFTR activity.
    Type: Application
    Filed: October 26, 2017
    Publication date: August 15, 2019
    Inventors: Daniel Parks, Benito Munoz
  • ADDITIVE FOR IMPARTING ULTRAVIOLET ABSORBENCY AND/OR HIGH REFRACTIVE INDEX TO MATRIX, AND RESIN MEMBER USING SAME
    Publication number: 20190248766
    Abstract: Provided is an additive for imparting ultraviolet absorbency, or an additive for imparting a high refractive index, which has satisfactory compatibility with a resin serving as a matrix and can maintain high transparency even if added in high concentrations. Also provided is an additive with which the function of imparting both ultraviolet absorbency and a high refractive index can be realized by means of one kind of additive. This additive is represented by the following Formula (I): wherein at least one of R1a to R9a is a monovalent sulfur-containing group represented by the following Formula (i-1) or Formula (i-2): ?R10a?mSH??(i-1) ?R11a?nS?R12a—S?pR13a??(i-2) wherein R10a to R12a each represent a divalent hydrocarbon group or the like; and R13a represents a monovalent hydrocarbon group or the like.
    Type: Application
    Filed: April 25, 2019
    Publication date: August 15, 2019
    Applicants: Miyoshi Oil & Fat Co., Ltd., Tokai Optical Co., Ltd.
    Inventors: Koji KAWAI, Kotaro KANEKO, Nobuhiro KANEKO, Yuichi SHISHINO, Kuniyoshi OKAMOTO
  • Tetrahydroquinazoline Derivatives Useful as Anticancer Agents
    Publication number: 20190248767
    Abstract: Compounds of the general formula: processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
    Type: Application
    Filed: February 1, 2019
    Publication date: August 15, 2019
    Applicant: PFIZER INC.
    Inventors: Simon PLANKEN, Hengmiao CHENG, Michael Raymond COLLINS, Jillian Elyse SPANGLER, Alexei BROOUN, Andreas MADERNA, Cynthia PALMER, Maria Angelica LINTON, Asako NAGATA, Ping CHEN
  • METHOD FOR PURIFYING BENZOPYRAN DERIVATIVE, CRYSTAL FORM THEREOF, AND METHOD FOR PREPARING CRYSTAL FORM
    Publication number: 20190248768
    Abstract: The present invention provides a process for purifying (2R,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(1H-imidazol-2-ylmethyl)amino]-3-hydroxy-2-methyl-2-dimethoxymethyl-3,4-dihydro-2H-1-benzopyran, comprising converting an amorphous (2R,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(1H-imidazol-2-ylmethyl)amino]-3-hydroxy-2-methyl-2-dimethoxymethyl-3,4-dihydro-2H-1-benzopyran to a crystalline form thereof. And also, the present invention provides a novel crystalline form of (2R,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(1H-imidazol-2-ylmethyl)amino]-3-hydroxy-2-methyl-2-dimethoxymethyl-3,4-dihydro-2H-1-benzopyran and processes for preparing the same.
    Type: Application
    Filed: November 24, 2016
    Publication date: August 15, 2019
    Applicant: HANLIM PHARMACEUTICAL CO., LTD.
    Inventors: Jae-Chun RYU, Yong-Kyun PARK, Hyun-Kyu KIM, Dong-Yeop SHIN
  • SUBSTITUTED BICYCLE HETEROCYCLIC DERIVATIVES USEFUL AS ROMK CHANNEL INHIBITORS
    Publication number: 20190248769
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein R1 is (II) or (III); each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3, L1, L2, R1a, R1b, R1c, and n are define herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.
    Type: Application
    Filed: November 2, 2017
    Publication date: August 15, 2019
    Inventors: Prashantha Gunaga, Rajeev S. Bhide, Rajesh Onkardas Bora, Manoranjan Panda, Navnath Dnyanoba Yadav, Eldon Scott Priestley, Jeremy Richter
  • INDOLE DERIVATIVE USED AS CRTH2 INHIBITOR
    Publication number: 20190248770
    Abstract: The present application discloses an indole as represented by formula (I) used as a CRTH2 inhibitor, and a pharmaceutically acceptable salt or tautomer of the indole, and an application of same in treating a disease related to a CRTH2 receptor.
    Type: Application
    Filed: July 21, 2017
    Publication date: August 15, 2019
    Inventors: Yuanshan YAO, Bin CHEN, Yuan CHEN, Ao LI, Ran XU, Zhensheng HUANG, Dongdong TIAN, Hongwei LI, Chengshuai YANG, Jian LI, Shuhui Chen
  • MONOCYCLIC HETEROARYL SUBSTITUTED COMPOUNDS
    Publication number: 20190248771
    Abstract: Disclosed are compounds of Formulas (I), (II), (III), (IV), (V), (VI), (VII), or (VIII): (I) (II) (III) (IV) (V) (VI) (VII) (VIII) or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a monocyclic heteroaryl group substituted with zero to 3 R3a; and R1, R2, R3a, R4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.
    Type: Application
    Filed: July 13, 2017
    Publication date: August 15, 2019
    Inventors: Jeremy M. Richter, Xiaojun Zhang, Eldon Scott Priestley
  • TYROSINE KINASE INHIBITOR AND APPLICATION THEREOF
    Publication number: 20190248772
    Abstract: The invention discloses a compound with the general formula of (I), wherein, K is selected from: naphthene alkyl and haloalkane alkyl or N—R6. The invention also discloses a tyrosine kinase inhibitor containing the above compound and the application of the compound in preparing drugs for treating cancers. The tyrosine kinase inhibitor of the invention inhibits the bioactivity of multiple signal conduction kinases such as C-MET, VEGF, KDR, etc., it can effectively inhibit cell proliferation and has favorable therapeutic effects on various diseases such as cancer, it has significant therapeutic effects especially on lung cancer, gastric cancer, ovarian cancer, malignant glioma, etc., and it has a very broad application prospect.
    Type: Application
    Filed: June 22, 2017
    Publication date: August 15, 2019
    Inventors: Fang SUN, Youni ZHAN
  • PROCESS FOR THE PREPARATION OF PURE AND STABLE CRYSTALLINE RALTEGRAVIR POTASSIUM FORM 3
    Publication number: 20190248773
    Abstract: The present invention provides improved, commercially viable and consistently reproducible processes for the preparation of pure and stable crystalline Raltegravir potassium Form 3 and pharmaceutical composition thereof.
    Type: Application
    Filed: September 13, 2017
    Publication date: August 15, 2019
    Inventors: Purna Chandra Ray, Samir Shanteshwar Shabade, Surinder Kumar Arora, D. Rajput Lalitkumar, B. Shivdavkar Radhakrishna, G. Varade Shantanu, D. Ausekar Govind, Girij Pal Singh, Shreyas Pandurang Deshmukh, Gaurav Amrut Patil
  • HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS
    Publication number: 20190248774
    Abstract: Heterocyclic compounds as CDK4 or CDK6 or other CDK inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
    Type: Application
    Filed: February 15, 2019
    Publication date: August 15, 2019
    Inventors: Son Minh PHAM, Sarvajit CHAKRAVARTY, Jayakanth KANKANALA, Brahmam PUJALA, Amit SHETE, Bhawana BHATT, Anil Kumar AGARWAL, Sanjeev SONI, Jiyun CHEN
  • SALT AND CRYSTAL FORMS OF PLK-4 INHIBITOR
    Publication number: 20190248775
    Abstract: A fumarate salt and a maleate salt of compound (I) represented by the following structural formula, as well as their corresponding pharmaceutical compositions, are disclosed. Particular single crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are characterized by a variety of properties and physical measurements. Methods of preparing specific crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are also disclosed. The present invention also provides methods of treating a subject with a cancer.
    Type: Application
    Filed: April 19, 2019
    Publication date: August 15, 2019
    Inventors: Peter Brent Sampson, Miklos Feher, Heinz W. Pauls
  • 2,3-DIHYDRO-4H-1,3-BENZOXAZIN-4-ONE DERIVATIVES AS MODULATORS OF CHOLINERGIC MUSCARINIC M1 RECEPTOR
    Publication number: 20190248776
    Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, which may be useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof: wherein each symbol is as defined in the attached DESCRIPTION.
    Type: Application
    Filed: April 25, 2019
    Publication date: August 15, 2019
    Inventors: Takahiro SUGIMOTO, Shinkichi SUZUKI, Hiroki SAKAMOTO, Masami YAMADA, Minoru NAKAMURA, Makoto KAMATA, Kenichiro SHIMOKAWA, Masaki OGINO, Eiji KIMURA, Masataka MURAKAMI, Jinichi YONEMORI, Takuto KOJIMA
  • ISOXAZOLE DERIVATIVES AS FXR AGONISTS AND METHODS OF USE THEREOF
    Publication number: 20190248777
    Abstract: The present invention provides compounds of Formula (I): pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR. Specifically, the present invention relates to isoxazole derivatives useful as agonists for FXR, and methods for their preparation and use.
    Type: Application
    Filed: February 11, 2019
    Publication date: August 15, 2019
    Inventors: Ruichao Shen, Jun Ma, Guoqiang Wang, Xuechao Xing, Yat Sun Or
  • INHIBITORS OF C-JUN-N-TERMINAL KINASE (JNK)
    Publication number: 20190248778
    Abstract: The present invention provides novel compounds according to Formula (I): where Ring A, Ring B, X, L1, L2, RA, RC, RD, RE, m, n, and p are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of human diseases associated with kinase activity, for example, proliferative diseases, neurodegenerative diseases, metabolic disorders, inflammatory diseases, and cardiovascular diseases.
    Type: Application
    Filed: November 28, 2018
    Publication date: August 15, 2019
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Tinghu Zhang
  • COMPOUNDS, COMPOSITIONS, AND METHODS FOR INCREASING CFTR ACTIVITY
    Publication number: 20190248779
    Abstract: The present disclosure is directed to disclosed compounds that modulate, e.g., address underlying defects in cellular processing of CFTR activity.
    Type: Application
    Filed: October 26, 2017
    Publication date: August 15, 2019
    Inventors: Daniel Parks, Benito Munoz
  • BENZOTHIOPHENE-BASED SELECTIVE MIXED ESTROGEN RECEPTOR DOWNREGULATORS
    Publication number: 20190248780
    Abstract: This invention is benzothiophene-based selective mixed estrogen receptor downregulators and their compositions and uses to treat estrogen-related disorders.
    Type: Application
    Filed: April 24, 2019
    Publication date: August 15, 2019
    Applicant: The Board of Trustees of the University of Illnois
    Inventors: Gregory R. Thatcher, Rui Xiong, Yunlong Lu, Jiong Zhao, Debra A. Tonetti
  • COMPOSITIONS OF KINASE INHIBITORS AND THEIR USE FOR TREATMENT OF CANCER AND OTHER DISEASES RELATED TO KINASES
    Publication number: 20190248781
    Abstract: The present invention relates to novel thiazole-substituted indolin-2-ones as inhibitors of CSCPK and related kinases; to methods of inhibiting cancer stem cells by using a kinase inhibitor; to pharmaceutical compositions containing such compounds; and to methods of using such compounds in the treatment of a protein kinase related disorder in a mammal; and to processes of making such compounds and intermediates thereof.
    Type: Application
    Filed: November 14, 2018
    Publication date: August 15, 2019
    Inventors: Chiang Jia Li, Ji-Feng Liu, Youzhi Li, Wei Li, Harry Rogoff
  • METHOD FOR PREPARING MARAVIROC
    Publication number: 20190248782
    Abstract: Provided is a method for preparing a tropane derivative, maraviroc, including reacting a compound of formula (II) with a compound of formula (I), wherein the compound of formula (II) is prepared by the steps of acetylation of a compound of formula (III), activation and substitution of a compound of formula (IV) by a chlorination agent, cyclization of a compound of formula (V), and debenzylation of a compound of formula (VI) by hydrogenation. Hence, the present disclosure provides a method for preparing maraviroc with good yield and simple operation.
    Type: Application
    Filed: January 25, 2019
    Publication date: August 15, 2019
    Inventors: Heng-Yen Wang, Chen-Yi Kao
  • AMINO-SUBSTITUTED IMIDAZO[1,2-A] PYRIDINECARBOXAMIDES AND THEIR USE
    Publication number: 20190248783
    Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: July 2, 2018
    Publication date: August 15, 2019
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Alexandros VAKALOPOULOS, Markus FOLLMAN, Ingo HARTUNG, Philipp BUCHGRABER, Rolf JAUTELAT, Jorma HAßFELD, Niels LINDNER, Alexey GROMOV, Frank WUNDER, Johannes-Peter STASCH, Gorden REDLICH, Volkhart Min-Jian LI, Eva Maria BECKER-PELSTER, Andreas KNORR
  • Naphthyridinedione derivatives
    Publication number: 20190248784
    Abstract: The invention relates to compound of the formula (I?) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: October 10, 2018
    Publication date: August 15, 2019
    Inventors: Juergen REINHARDT, Niko SCHMIEDEBERG, Carsten SPANKA
  • SUBSTITUTED POLYCYCLIC CARBAMOYL PYRIDONE DERIVATIVE PRODRUG
    Publication number: 20190248785
    Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: November 19, 2018
    Publication date: August 15, 2019
    Applicant: Shionogi & Co., Ltd.
    Inventors: Chika TAKAHASHI, Hidenori MIKAMIYAMA, Toshiyuki AKIYAMA, Kenji TOMITA, Yoshiyuki TAODA, Makoto KAWAI, Kosuke ANAN, Masayoshi MIYAGAWA, Naoyuki SUZUKI
  • NOVEL TETRAHYDROPYRAZOLOPYRIDINE COMPOUNDS FOR THE TREATMENT OF INFECTIOUS DISEASES
    Publication number: 20190248786
    Abstract: The present invention relates to compounds of the formula (I), or pharmaceutically acceptable salts, enantiomer or diastereomer thereof, wherein R1 to R5 are as described above. The compounds may be useful for the treatment or prophylaxis of hepatitis B virus infection.
    Type: Application
    Filed: January 14, 2019
    Publication date: August 15, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Taishan Hu, Hong Shen, Xingchun Han
  • IRAK4 INHIBITING AGENTS
    Publication number: 20190248787
    Abstract: Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production.
    Type: Application
    Filed: February 8, 2019
    Publication date: August 15, 2019
    Inventors: Timothy Chan, Kevin Guckian, Tracy Jenkins, Jermaine Thomas, Jeffery Vessels, Gnanasambandam Kumaravel, Robert Meissner, Joseph Lyssikatos, Brian Lucas, Irina Leaf, Jeremy Duffield
  • ABT-199 ADDITION SALT AND CRYSTAL FORM THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION THEREOF
    Publication number: 20190248788
    Abstract: Crystalline forms, preparation methods and pharmaceutical compositions of ABT-199 monohydrochloride and ABT-199 dihydrochloride are disclosed. Compared with known ABT-199, they have one or more improved properties. They can be used to prepare drugs for the treatment and/or prevention of one or more diseases which are overexpressed by an anti-apoptotic BCL-2 family protein.
    Type: Application
    Filed: September 14, 2016
    Publication date: August 15, 2019
    Applicant: SOLIPHARMA LLC
    Inventors: XIAOHONG SHENG, XIAOXIA SHENG, JIANFENG ZHENG
  • P2X3 AND/OR P2X2/3 COMPOUNDS AND METHODS
    Publication number: 20190248789
    Abstract: The present application provides novel compounds and methods for preparing and using these compounds. In one embodiment, the compounds are of the structure of formula (I), wherein R1-R4 are defined herein. In a further embodiment, these compounds are useful in method for regulating one or both of the P2X3 or P2X2/3 receptors. In another embodiment, these compounds are useful for treating pain in patients by administering one or more of the compounds to a patient.
    Type: Application
    Filed: April 24, 2019
    Publication date: August 15, 2019
    Inventors: Scott K. Thompson, Aranapakam Venkatesan, Tony Priestley, Mrinal Kundu, Ashis Saha
  • DEUTERATED COMPOUNDS FOR TREATING FABRY, GAUCHER, PARKINSON'S AND RELATED DISEASES AND CONDITIONS, AND COMPOSITIONS AND METHODS THEREOF
    Publication number: 20190248790
    Abstract: Novel deuterium-containing chemical compounds are provided. They are glucosylceramide (GSC) synthase inhibitors and are useful for treating various types of lysosomal storage diseases including Fabry's disease, Gaucher's disease and Parkinson's disease, or related diseases and conditions. Also described are pharmaceutical compositions, and methods of preparation and use thereof.
    Type: Application
    Filed: February 8, 2019
    Publication date: August 15, 2019
    Applicant: X-Cutag Therapeutics, Inc.
    Inventors: Hui Joyce LI, Shuhao WEN, Changfu CHENG, Xiao CHEN, Gao SHANG
  • NOVEL MODULATORS OF CALCIUM RELEASE-ACTIVATED CALCIUM CHANNEL AND METHODS FOR TREATMENT OF NON-SMALL CELL LUNG CANCER
    Publication number: 20190248791
    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: October 23, 2018
    Publication date: August 15, 2019
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Kanthikiran V.S. Varanasi, Gayatri Swaroop Merikapudi, Swaroop Kumar V.S. Vakkalanka
  • NOVEL PYRAZOLOPYRAZINE AND TRIAZOLOPYRAZINE COMPOUNDS FOR THE TREATMENT OF INFECTIOUS DISEASES
    Publication number: 20190248792
    Abstract: The present invention relates to compounds of the formula (I), or pharmaceutically acceptable salts, enantiomer or diastereomer thereof, wherein R1 to R4 and Q are as described above. The compounds may be useful for the treatment or prophylaxis of hepatitis B virus infection.
    Type: Application
    Filed: January 14, 2019
    Publication date: August 15, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Xingchun Han, Xianfeng Lin, Hong Shen, Taishan Hu, Zhisen Zhang
  • RSV ANTIVIRAL PYRAZOLO- AND TRIAZOLO-PYRIMIDINE COMPOUNDS
    Publication number: 20190248793
    Abstract: The invention concerns novel substituted pyrazolo- and triazolo-pyrimidine compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment of respiratory syncytial virus infection.
    Type: Application
    Filed: February 11, 2019
    Publication date: August 15, 2019
    Inventors: David Francis Alain LANÇOIS, Jérôme Émile Georges GUILLEMONT, Pierre Jean-Marie Bernard RABOISSON, Dirk André Emmy ROYMANS, Boris ROGOVOY, Vadim BICHKO, Delphine Yvonne Raymonde LARDEAU, Antoine Benjamin MICHAUT, Anil KOUL
  • sGC STIMULATORS
    Publication number: 20190248794
    Abstract: The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP), or both, or an upregulation of the NO pathway is desirable.
    Type: Application
    Filed: February 12, 2019
    Publication date: August 15, 2019
    Inventors: Glen Robert Rennie, Rajesh R. Iyengar, Thomas Wai-Ho Lee, Takashi Nakai, Ara Mermerian, Lei Jia, G-Yoon Jamie Im, Paul Allan Renhowe, Joon Jung, Peter Germano, Karthik Iyer, Timothy Claude Barden, Kim Tang
  • WEE-1 INHIBITING PYRAZOLOPYRIMIDINONE COMPOUNDS
    Publication number: 20190248795
    Abstract: The present invention relates to compounds that are useful as inhibitors of the activity of Wee-1 kinase. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.
    Type: Application
    Filed: July 12, 2017
    Publication date: August 15, 2019
    Inventors: Frank BURKAMP, James Samuel Shane ROUNTREE, Adam Piotr TREDER