Patents Issued in June 20, 2019
  • Publication number: 20190185429
    Abstract: The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
    Type: Application
    Filed: February 20, 2019
    Publication date: June 20, 2019
    Inventors: William J. Hoekstra, Christopher M. Yates, Mark Behnke, Asaf Alimardanov, Scott A. David, Douglas Franklin Fry
  • Publication number: 20190185430
    Abstract: The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
    Type: Application
    Filed: February 20, 2019
    Publication date: June 20, 2019
    Inventors: William J. Hoekstra, Christopher M. Yates, Mark Behnke, Asaf Alimardanov, Scott A. David, Douglas Franklin Fry
  • Publication number: 20190185431
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: November 14, 2018
    Publication date: June 20, 2019
    Inventors: Samedy Ouk, Esmir Gunic, Jean-Michel Vernier, Chixu Chen
  • Publication number: 20190185432
    Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.
    Type: Application
    Filed: December 21, 2018
    Publication date: June 20, 2019
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Taiju Nakamura, Taichi Abe, Yusuke Miyashita, Hirofumi Kuroda, Yusuke Ayata, Atsushi Akao
  • Publication number: 20190185433
    Abstract: Provision of a stabilized crystal of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound A). A crystal of compound A, which shows a particular X-ray powder diffraction pattern of a characteristic diffraction peaks at diffraction angles 2?(°) as measured by X-ray powder diffractmetry.
    Type: Application
    Filed: July 20, 2018
    Publication date: June 20, 2019
    Applicant: Japan Tobacco Inc.
    Inventors: Motohide SATOH, Takahisa MOTOMURA, Takashi MATSUDA, Kentaro KONDO, Koji ANDO, Koji MATSUDA, Shuji MIYAKE, Hideto UEHARA
  • Publication number: 20190185434
    Abstract: The present invention relates to novel fluorophores and their use in combination with novel nucleic acid molecules, called aptamers, that bind specifically to the fluorophore and thereby enhance the fluorescence signal of the fluorophore upon exposure to radiation of suitable wavelength. Molecular complexes formed between the novel fluorophores, novel nucleic acid molecules, and their target molecules are described, and the use of multivalent aptamer constructs as fluorescent sensors for target molecules of interest are also described.
    Type: Application
    Filed: February 26, 2019
    Publication date: June 20, 2019
    Inventors: Samie R. JAFFREY, Jeremy S. PAIGE
  • Publication number: 20190185435
    Abstract: Provided, in part, is a composition comprising one or more chemical entities of formula I, each of which is a compound of formula I: a pharmaceutically acceptable salt thereof, a solvate thereof, or a solvate of a pharmaceutically acceptable salt thereof, the composition characterized in that greater than a first threshold amount of the total amount of chemical entities of formula I in the composition: are chemical entities of formula I.a, wherein the first threshold amount is 50%; or are chemical entities of formula I.b.1, wherein the first threshold amount is 25%; or are chemical entities of formula I.b.2, wherein the first threshold amount is 25%, wherein the chemical entities of formula I.a, I.b.1, and I.b.2, are described herein, and methods of using such compositions, for example, for the delivery of a polynucleotide in vivo.
    Type: Application
    Filed: November 1, 2018
    Publication date: June 20, 2019
    Inventors: Frank DeRosa, Shrirang Karve, Michael Heartlein
  • Publication number: 20190185436
    Abstract: The invention relates to triazole compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as modulators of demyelinating diseases: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention, methods of using the compositions and kits thereof in the treatment of various demyelinating and neurodegenerative diseases, including multiple sclerosis.
    Type: Application
    Filed: October 17, 2018
    Publication date: June 20, 2019
    Inventors: Robert J. Davies, Jingrong Cao, Meghan Elise Cockerill, Philip Noel Collier, Elisabeth Doyle, James Daniel Frantz, Huai Gao, Brian Anthony Goldman, Ronald Lee Grey, JR., Anne-Laure Grillot, Wenxin Gu, James A. Henderson, Raul Eduardo Krauss, Adrianne Lynn Kolpak, Yusheng Liao, Sanjay Shivayogi Magavi, David Messersmith, Albert Charles Pierce, Emanuele Perola, Elizabeth Jin-Sun Ryu, Joshua Syken, Jian Wang, Michael Paul DeNinno, Francois Maltais
  • Publication number: 20190185437
    Abstract: The present invention relates to compounds suitable for treating, ameliorating and/or preventing neuromuscular disorders, including the reversal of drug-induced neuromuscular blockade. The compounds as defined herein preferably inhibit the ClC-1 ion channel.
    Type: Application
    Filed: December 14, 2017
    Publication date: June 20, 2019
    Applicant: NMD Pharma ApS
    Inventors: Lars J.S. Knutsen, Martin E. Cooper, Andrew W. Brown
  • Publication number: 20190185438
    Abstract: Disclosed herein are salts and polylmoprhs of (2S)-2-[(S)-(ethoxyphenoxy)phenylmethyl]morpholine (esreboxetine) as shown in Formula I: wherein an acid is selected from adipic, L-ascorbic, L-aspartic, fumaric, glycolic, hydrochloric, maleic, mucic, phosphoric, sulfuric, and thiocyanic acid.
    Type: Application
    Filed: December 6, 2017
    Publication date: June 20, 2019
    Inventors: Seth Lederman, Bruce Daughtery
  • Publication number: 20190185439
    Abstract: Radiofluorinated carboximidamides are disclosed as selective IDO enzyme radioligands and generate specific binding in accordance with IDO expression in vitro. MicroPET experiments indicate [18F]IDO49 specifically accumulate in IDO-expressing tumors which confirmed by Western blot and IHC analysis supported. Using Hela tumor bearing models with IFN-? treatment confirmed that [18F]IDO49 accumulation in the IFN-? treatment tumor mouse. These results can have implications that [18F]IDO49 has substantial potential as an imaging agent that targets IDO in tumors.
    Type: Application
    Filed: August 24, 2017
    Publication date: June 20, 2019
    Inventors: Haibin TIAN, Robert GILLIES
  • Publication number: 20190185440
    Abstract: A process for the preparation of diaminophenothiazinium compounds is described, which allows achieving quickly and effectively a high degree of purity of the same.
    Type: Application
    Filed: May 16, 2017
    Publication date: June 20, 2019
    Inventors: Matteo COLOMBO, Paola DAVERIO, Stella BORRELLI
  • Publication number: 20190185441
    Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables R1, R2, R3, R4, subscipt m and n, have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Application
    Filed: August 24, 2017
    Publication date: June 20, 2019
    Applicant: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY
    Inventors: Sidney HECHT, Omar KHDOUR, Sandipan Roy CHOWDHURY, Nishant P VISAVADIYA
  • Publication number: 20190185442
    Abstract: The present invention provides dehydroleucodine derivatives. In particular, the present invention provides amine derivatives of dehydroleucodine and methods of using dehydroleucodine and the amine derivatives of dehydroleucodine to inhibit the growth of cancer cells.
    Type: Application
    Filed: February 22, 2019
    Publication date: June 20, 2019
    Inventors: Cesar M. Compadre, Paola E. Ordonez, Monica L. Guzman, Darin E. Jones, Omar Malagon, Giovanni Vidari, Peter Crooks
  • Publication number: 20190185443
    Abstract: Disclosed are compounds and compositions that modulate cannabinoid receptors, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors. This disclosure is directed to methods of treating cannabinoid dependence, neuropathy, inflammation, glaucoma, a neurodegenerative disorder, a motor function disorder, a gastrointestinal disorder, hypothermia, emesis, loss of appetite, or anorexia associated with AIDS.
    Type: Application
    Filed: January 7, 2019
    Publication date: June 20, 2019
    Inventors: Alexandros Makriyannis, Ganeshsingh A. Thakur, Rishi Sharma
  • Publication number: 20190185444
    Abstract: The present invention provides novel compounds having the general formula: wherein R1 to R6, X, Y, A1 and A2 are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: November 26, 2018
    Publication date: June 20, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Dongdong Chen, Wenming Chen, Song Feng, Lu Gao, Hong Shen, Xuefei Tan, Li Wang
  • Publication number: 20190185445
    Abstract: An electrolyte solution containing a compound represented by the following formula (1): wherein Rf is a C1-C8 fluorinated alkyl group, and vinylene carbonate. Also disclosed is an electrochemical device including the electrolyte solution, a lithium ion secondary battery including the electrolyte solution and a module including the lithium ion secondary battery.
    Type: Application
    Filed: February 25, 2019
    Publication date: June 20, 2019
    Applicant: DAIKIN INDUSTRIES, LTD.
    Inventors: Shinya TANAKO, Mayuko TAKANO, Akinori TANI, Michiaki OKADA, Hideo SAKATA, Tomo SHIMADA, Shinichi KINOSHITA
  • Publication number: 20190185446
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
    Type: Application
    Filed: December 18, 2018
    Publication date: June 20, 2019
    Inventors: YAN SHI, Peter Tai Wah Cheng, Ying Wang, Jun Shi, Shiwei Tao, Jun Li, Lawrence J. Kennedy, Robert F. Kaltenbach, III, Hao Zhang, James R. Corte
  • Publication number: 20190185447
    Abstract: Disclosed herein is a process of making a compound of formula I The compound of formula I is an inhibitor of MEK and thus can be used to treat cancer.
    Type: Application
    Filed: February 8, 2019
    Publication date: June 20, 2019
    Inventors: Sriram Naganathan, Nathan Guz, Matthew Pfeiffer, C. Gregory Sowell, Tracy Bostick, Jason Yang, Amit Srivastava, Neel Kumar Anand
  • Publication number: 20190185448
    Abstract: The present invention is directed to methods of inhibiting or modulating p97 and compounds and compositions useful in such methods. Diseases and conditions that can be treated with the compounds and compositions of the invention include, but are not limited to, cancer and neurodegenerative disorders susceptible to treatment by modulation or inhibition of p97.
    Type: Application
    Filed: May 11, 2017
    Publication date: June 20, 2019
    Inventors: Donna M. HURYN, Peter WIPF, Matthew G. LAPORTE
  • Publication number: 20190185449
    Abstract: The present invention relates to novel compounds of formula (I) or formula (Ia) pharmaceutically-acceptable salts, hydrates, solvates, or stereoisomers thereof, and pharmaceutical compositions of these compounds which are useful for preventive and therapeutic use in human and veterinary medicine.
    Type: Application
    Filed: December 17, 2018
    Publication date: June 20, 2019
    Inventors: Marc LABELLE, Ulrich KESSLER, Valentino CATTORI, Cyril COOK, Ramkrishna Reddy VAKITI, Kevin R. D. JOHNSON, Matinder KAUR, Jean-d'Amour K. TWIBANIRE, Farman ULLAH
  • Publication number: 20190185450
    Abstract: The present disclosure generally relates to compounds of formula (I), wherein R2 is a phenyl or pyridinyl moiety, useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.
    Type: Application
    Filed: July 5, 2017
    Publication date: June 20, 2019
    Inventors: Kap-Sun YEUNG, Katharine A. Grant-Young, Juliang Zhu, Mark G. Saulnier, David B. Frennesson, Zhaoxing Meng, Paul Michael Scola
  • Publication number: 20190185451
    Abstract: Compounds and compositions for modulating fibroblast activation protein (FAP) are described. The compounds and compositions may find use as therapeutic agents for the treatment of diseases, including hyperproliferative diseases.
    Type: Application
    Filed: December 14, 2018
    Publication date: June 20, 2019
    Inventors: Jennifer ALFARO, Sebastian BELMAR, Sebastian BERNALES, Brahmam PUJALA, Dayanand PANPATIL, Bhawana BHATT
  • Publication number: 20190185452
    Abstract: The present invention relates to novel piperidine derivatives having better cell growth inhibitory activities toward cancer cell cultures and, more particularly, PANC-1 cancer cell cultures than FK866. Accordingly, the present invention relates to compounds of formula I, wherein Ar1 is aryl or heteroaryl, which are optionally substituted by one, two or three substituents selected from lower alkyl; lower alkoxy; formyl; hydroxyl; lower alkyl substituted by lower alkoxy or hydroxyl; A is CnH2n, CnH2n?2 or CnH2n?4, wherein n=4, 5, 6, 7; B is ?N—CN, oxo (?O), thio (?S); D is NH, —CH?CH—; Ar2 is aryl or heteroaryl which are optionally substituted by one, two or three halogen substituents; wherein, if B is oxo (?O), Ar1 and Ar2 are not simultaneously phenyl and pyridine-3-yl; B and D are not simultaneously ?N—CN and —CH?CH—, or a pharmaceutically acceptable salt, a racemic mixture or its corresponding enantiomers and/or optical isomers.
    Type: Application
    Filed: August 4, 2017
    Publication date: June 20, 2019
    Inventors: Pierre VOGEL, Michel DUCHOSAL, Nahimana AIMABLE, Robina INMACULADA, Faustino MOLLINEDO, Alessio NENCIONI
  • Publication number: 20190185453
    Abstract: Disclosed are a crystal of a maleate of a compound of formula (I), a preparation method for the crystal, a crystallization composition of same, a pharmaceutical composition of same, and uses thereof in preventing and treating a tumor.
    Type: Application
    Filed: August 24, 2017
    Publication date: June 20, 2019
    Inventors: Song TANG, Yizhong ZHU, Fei LIU, Jie ZHOU, Zhilin CHEN, Hongjiang XU, Xin TIAN
  • Publication number: 20190185454
    Abstract: Described herein are compounds that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
    Type: Application
    Filed: July 20, 2018
    Publication date: June 20, 2019
    Inventors: Jason D. BRUBAKER, Joseph L. KIM, Kevin J. WILSON, Douglas WILSON, Lucian V. DIPIETRO
  • Publication number: 20190185455
    Abstract: The invention relates to compounds according to general formula (I), which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
    Type: Application
    Filed: December 18, 2018
    Publication date: June 20, 2019
    Inventors: Florian JAKOB, Jo ALEN, Sebastian KRÜGER, Markus SCHADE, Daniela FRIEBE, Stephanie HENNEN
  • Publication number: 20190185456
    Abstract: The invention provides a novel class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the treatment of influenza.
    Type: Application
    Filed: August 15, 2017
    Publication date: June 20, 2019
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Qingyun REN, Changhua TANG, Junjun YIN, Kai YI, Yingjun ZHANG
  • Publication number: 20190185457
    Abstract: A heterocyclic compound represented by Formula 1: (A)n-L, ??Formula 1 wherein, in Formula 1, A, L, and n are the same as described in the specification.
    Type: Application
    Filed: December 14, 2018
    Publication date: June 20, 2019
    Inventors: Shiro IRISA, Keisuke KORAI, Mitsunori ITO
  • Publication number: 20190185458
    Abstract: There is provided a compound of formula (I) which is an inhibitor of the family of p38 mitogen-activated protein kinase enzymes, and to its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.
    Type: Application
    Filed: February 26, 2019
    Publication date: June 20, 2019
    Inventors: Kazuhiro ITO, Catherine Elisabeth Charron, John King-Underwood, Stuart Thomas Onions, Alistair Ian Longshaw, Rudy Broeckx, Walter Filliers, Alex Copmans
  • Publication number: 20190185459
    Abstract: A compound represented by Formula (I), or a salt thereof: wherein, R1 represents an unsubstituted or substituted C1-6 alkylthio group, or the like; A1 represents a nitrogen atom or CH; A2 represents a nitrogen atom or CR2; R2 and R3 each independently represents a hydrogen atom, an unsubstituted or substituted C6-10 aryl group, an unsubstituted or substituted 3- to 6-membered heterocyclyl group, or the like; B1 and B2 each independently represents a nitrogen atom or CR5, with the proviso that B1 and B2 do not represent CR5 at the same time, wherein R5 represents a hydrogen atom, an unsubstituted or substituted C1-6 alkyl group, or the like; R4 represents an unsubstituted or substituted C1-6 alkyl group, or the like, and R4 binds to any one of nitrogen atoms forming an imidazole ring or a triazole ring; and Ar represents an unsubstituted or substituted C6-10 aryl group or the like.
    Type: Application
    Filed: September 13, 2017
    Publication date: June 20, 2019
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Keita SAKANISHI, Takao IWASA, Hikaru AOYAMA, Norifumi SAKIYAMA, Daisuke USHIJIMA, Maki MATSUI, Tomomi KOBAYASHI
  • Publication number: 20190185460
    Abstract: An amine-based compound and an organic light-emitting device including the same are provided.
    Type: Application
    Filed: December 19, 2018
    Publication date: June 20, 2019
    Inventors: Jongwoo KIM, Jangyeol BAEK, Eunjae JEONG, Sanghyun HAN, Youngkook KIM, Seokhwan HWANG
  • Publication number: 20190185461
    Abstract: A compound represented by general formula (I), or a stereoisomer, a hydrate, a metabolite, a solvate, a pharmaceutically acceptable salt, a cocrystal, or a prodrug thereof, the preparation method thereof, and use thereof in the manufacture of a medicament for treatment of an airway obstructive disease, wherein the substituents are defined as in the specification.
    Type: Application
    Filed: July 12, 2016
    Publication date: June 20, 2019
    Applicant: Sichuan Haisco Pharmaceutical Co., Ltd.
    Inventors: Yonggang WEI, Guanpeng QUI, Bolin LEI, Yonghua LU, Suxin ZHENG
  • Publication number: 20190185462
    Abstract: The present invention is directed to substituted 5-trifluoromethyl oxadiazole compounds of generic formula (I) or a pharmaceutically acceptable salt thereof. In particular, the invention is directed to a class of aryl and heteroaryl substituted 5-trifluoromethyl oxadiazole compounds of formula I which may be useful as HDAC6 inhibitors for treating cellular proliferative diseases, including cancer, neurodegenerative diseases, such as schizophrenia and stroke, as well as other diseases.
    Type: Application
    Filed: June 19, 2017
    Publication date: June 20, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Abbas Walji, Richard Berger, Craig A. Stump, Kelly Ann S. Schlegel, James J. Mulhearn, Thomas J. Greshock, Deping Wang, Mark E. Fraley, Kristen G. Jones
  • Publication number: 20190185463
    Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.
    Type: Application
    Filed: July 26, 2018
    Publication date: June 20, 2019
    Inventors: Michel C. Maillard, Perla Breccia, Celia Dominguez, Alan F. Haughan, Rebecca E. Jarvis, Christopher A. Luckhurst, Elizabeth A. Saville-Stones, Andrew J. Stott, Amanda Van de Poël, Michael Wall, Grant Wishart
  • Publication number: 20190185464
    Abstract: The present invention relates to an oxopicolinamide derivative, a preparation method therefor and the pharmaceutical use thereof. In particular, the present invention relates to an oxopicolinamide derivative as shown in the general formula (AI), a preparation method therefor and a pharmaceutical composition comprising the derivative, and to the use thereof as a therapeutic agent, in particular as an inhibitor of blood coagulation factor XIa (Factor XIa, FXIa for short) and the use thereof in the preparation of a drug for treating diseases such as thromboembolism, wherein the definition of each substituent in the general formula (AI) is the same as defined in the description.
    Type: Application
    Filed: August 30, 2017
    Publication date: June 20, 2019
    Inventors: Fanglong YANG, Weimin WANG, Xiaodong LI, Gang CHEN, Feng HE, Weikang TAO
  • Publication number: 20190185465
    Abstract: A 2-substituted benzothiazolyl-3-substituted phenyl-5-substituted sulfonated phenyl-2H-tetrazolium salt represented by the following Formula (1): wherein, R1 can be a hydrogen atom, a hydroxyl group, a methoxy group, and an ethoxy group; R2 can be a nitro group, —OR4, and a carboxyl group; R3 is a hydrogen atom, a methyl group, or an ethyl group, while at least one is a methyl group or an ethyl group; R4 is a methyl group or an ethyl group; m is 1 or 2; n is an integer from 0 to 2; p is 0 or 1; n+p is 1 or greater; q is 1 or 2; when q is 2, the OR3's are disposed adjacently to each other and may form a ring; and X is a hydrogen atom or an alkali metal atom.
    Type: Application
    Filed: January 23, 2019
    Publication date: June 20, 2019
    Applicant: TERUMO KABUSHIKI KAISHA
    Inventor: Hiroya SATO
  • Publication number: 20190185466
    Abstract: The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: November 15, 2018
    Publication date: June 20, 2019
    Applicant: Bayer Aktiengesellschaft
    Inventors: Adam James DAVENPORT, Nico BRÄUER, Oliver Martin FISCHER, Andrea ROTGERI, Antje ROTTMANN, Ioana NEAGOE, Jens NAGEL, Anne-Marie GODINHO-COELHO, Jürgen KLAR
  • Publication number: 20190185467
    Abstract: {4-[3-(Dimethylamino)propoxy]phenyl}methyl(4S)-4-(propan-2-yl)-3H,4H,5H,6H,7H-imidazo[4,5-c]pyridine-5-carboxylate, and pharmaceutically or veterinarily acceptable salts thereof.
    Type: Application
    Filed: July 21, 2016
    Publication date: June 20, 2019
    Applicant: PROXIMAGEN LIMITED
    Inventor: Lee PATIENT
  • Publication number: 20190185468
    Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent ATM kinase mediated disease, including cancer. The specification further relates to crystalline forms of compounds of imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating ATM kinase mediated disease, including cancer, using such compounds and salts.
    Type: Application
    Filed: December 12, 2018
    Publication date: June 20, 2019
    Inventors: Bernard Christophe BARLAAM, Kurt Gordon PIKE
  • Publication number: 20190185469
    Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, R5, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Application
    Filed: December 17, 2018
    Publication date: June 20, 2019
    Inventors: Alaric J. Dyckman, Dharmpal S. Dodd, Christopher P. Mussari, Trevor C. Sherwood, Brian K. Whiteley, John L. Gilmore, Sreekantha Ratna Kumar, Laxman Pasunoori, Pitani Veera Venkata Srinivas, Srinivasan Kunchithapatham Duraisamy, Subramanya Hegde, Rushith Kumar Anumula
  • Publication number: 20190185470
    Abstract: The invention relates to compounds according to general formula (I), which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
    Type: Application
    Filed: December 18, 2018
    Publication date: June 20, 2019
    Inventors: Florian JAKOB, Jo ALEN, Sebastian KRÜGER, Markus SCHADE, Daniela FRIEBE, Stephanie HENNEN
  • Publication number: 20190185471
    Abstract: Aspects of the present application relate to solid forms of Venetoclax and preparative processes thereof. Specific aspects relate to an amorphous form of Venetoclax, its solid dispersion and crystalline forms of Venetoclax or salts thereof. Further aspects of the present application relate to processes for the preparation of Venetoclax.
    Type: Application
    Filed: June 8, 2017
    Publication date: June 20, 2019
    Applicant: Dr. Reddy's Laboratories Limited
    Inventors: Subba Reddy PEDDI REDDY, Mohan Kumar KOTTUR, Ramprasad JURUPULA, Mohammed Azeezulla BAIG, Ramesh CHAKKA, Rajesh THI PPARABOINA, Vishweshwar PEDDY, Pallavi RAO, Srinivas ORUGANTI, Vilas Hareshwar DAHANUKAR
  • Publication number: 20190185472
    Abstract: The present invention relates to fused heterocyclic derivatives, processes for their preparation and their use in medicine. Specifically, the present invention relates to a novel derivative represented by the formula (I?), or its pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the derivative or its pharmaceutically acceptable salt thereof, and the method for preparing the derivative and its pharmaceutically acceptable salt thereof. The present invention also relates to the use of the derivative and its pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing the derivative and its pharmaceutically acceptable salt thereof in the preparation of medicines, in particularly as IDO inhibitor medicines, for treating and/or preventing cancers. Wherein each substituent of the formula (I?) is the same as defined in the specification.
    Type: Application
    Filed: August 16, 2017
    Publication date: June 20, 2019
    Inventors: Xiangyang CHEN, Yingxiang GAO
  • Publication number: 20190185473
    Abstract: The present invention relates to avibactam free acid, a method for preparing avibactam free acid and a method for preparing avibactam sodium by further reacting avibactam free acid. The invention further refers to a pharmaceutical composition comprising avibactam free acid, one or more alkaline sodium salt(s) and one or more beta-lactam antibiotic(s). The pharmaceutical composition of the present invention can be used as medicament, in particular for treatment and/or prevention of bacterial infections.
    Type: Application
    Filed: August 25, 2017
    Publication date: June 20, 2019
    Applicant: Sandoz AG
    Inventors: Michael Fischer, Andreas Lechner, Brigitte Staggl
  • Publication number: 20190185474
    Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.
    Type: Application
    Filed: January 9, 2019
    Publication date: June 20, 2019
    Inventors: Tatiana Koudriakova, Kevin D. Kreutter, Kristi Leonard, Michele C. Rizzolio, Russell C. Smith, Mark S. Tichenor, Aihua Wang
  • Publication number: 20190185475
    Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, Y3, Y4 R1, R2, R4a, R4b, R5a, R5b, R6a and R6b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.
    Type: Application
    Filed: June 15, 2016
    Publication date: June 20, 2019
    Inventors: Jeffrey T. Bagdanoff, Zhuoliang Chen, Michael Dore, Jorge Garcia Fortanet, Mitsunori Kato, Matthew J. LaMarche, Patrick James Sarver, Michael Shultz, Troy Douglas Smith, Sarah Williams
  • Publication number: 20190185476
    Abstract: The present invention relates to compounds of the formula (I), or pharmaceutically acceptable salts, enantiomer or diastereomer thereof, wherein R1 to R3 are as described above. The compounds may be useful for the treatment or prophylaxis of hepatitis B virus infection.
    Type: Application
    Filed: November 20, 2018
    Publication date: June 20, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Taishan Hu, Haixia Liu
  • Publication number: 20190185477
    Abstract: Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphic forms, cocrystals, and amorphous forms thereof, and pharmaceutical compositions thereof.
    Type: Application
    Filed: November 20, 2018
    Publication date: June 20, 2019
    Inventors: Louis Grenier, Andre Lescarbeau, Praveen Sharma, Daniel G. Genov
  • Publication number: 20190185478
    Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents H; optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy, NH2, —NHC1-3alkyl and —N(C1-3alkyl)2); —C(O)Oalkyl; haloalkyl; haloalkoxy; or -alkylaryl; each R2 independently represents H; optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy, NH2, —NHC1-3alkyl and —N(C1-3alkyl)2); -alkylaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independentl
    Type: Application
    Filed: December 19, 2018
    Publication date: June 20, 2019
    Applicant: Agency for Science, Technology and Research
    Inventors: Jenefer Alam, Soo Yei Ho, Wei Ling Wang, Athisayamani Jeyaraj Duraiswamy