Patents Issued in December 24, 2020
  • Publication number: 20200399236
    Abstract: Disclosed herein is a process for preparation of 1-chloro-2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)propan-2-ol (compound of formula (I)) 5 and 2-(1-chlorocyclopropyl)-2-[(2-chlorophenyl)methyl]oxirane (compound of formula (II)).
    Type: Application
    Filed: June 4, 2018
    Publication date: December 24, 2020
    Inventors: Santosh Ganpat Shelke, Talati Paresh Vithaldas, Jaidev Rajnikant Shroff, Vikram Rajnikant Shroff
  • Publication number: 20200399237
    Abstract: An object of the present invention is to provide a method for producing 5-hydroxymethyl-2-furfural (5-HMF) with suppressed production of byproducts. The present invention provides a method for producing 5-HMF, comprising the step of performing a dehydration reaction of a carbohydrate comprising a hexose as a constituent sugar or a derivative thereof to produce 5-hydroxymethyl-2-furfural, wherein the dehydration reaction is performed in the presence of activated carbon. The present invention also provides a method for producing a carbohydrate composition comprising 5-hydroxymethyl-2-furfural, comprising the step of heating a carbohydrate composition comprising one or more selected from the group consisting of a carbohydrate comprising a hexose as a constituent sugar and a derivative thereof, in the presence of an acid catalyst and activated carbon at a temperature of 90 to 400° C.
    Type: Application
    Filed: December 7, 2018
    Publication date: December 24, 2020
    Inventors: Yuichi Nishimura, Hitoshi Takaguchi, Norihisa Hamaguchi
  • Publication number: 20200399238
    Abstract: Substituted aurones were found to have antitrypanosomal, antifungal and immunomodulatory activity. The invention provides novel aurone compounds, pharmaceutical compositions, and methods encompassing medical and veterinary applications.
    Type: Application
    Filed: September 3, 2020
    Publication date: December 24, 2020
    Applicant: MIDDLE TENNESSEE STATE UNIVERSITY
    Inventors: Jeannie Stubblefield, Zachary E. Taylor, Scott Handy, Mary Farone, Erin McClelland, Caleb Sutton, Anthony Farone, Hyo Park, Danielle Araujo, Anthony Newsome
  • Publication number: 20200399239
    Abstract: Process to continuously prepare a cyclic carbonate product by reacting an epoxide compound with carbon dioxide in the presence of a supported dimeric aluminium salen complex which complex is activated by a halide compound comprising the following steps, (a) contacting carbon dioxide with the epoxide compound in a suspension of liquid cyclic carbonate and the supported dimeric aluminium salen complex which complex is activated by a halide compound, (b) separating part of the cyclic carbonate product from the supported dimeric aluminium salen complex, (c) separating the halide compound from the cyclic carbonate product to obtain purified cyclic carbonate product, (d) use all or part of the halide compound as obtained in step (c) to activate deactivated supported dimeric salen complex.
    Type: Application
    Filed: December 18, 2018
    Publication date: December 24, 2020
    Applicant: NEW GREEN WORLD B.V.
    Inventors: Frank VERGUNST, Sander LAURENTIUS
  • Publication number: 20200399240
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor.
    Type: Application
    Filed: June 8, 2020
    Publication date: December 24, 2020
    Inventors: Luca Fadini, Peter Manini, Claudio Pietra, Claudio Giuliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J. Stella
  • Publication number: 20200399241
    Abstract: Disclosed are indazole compounds and derivatives thereof for use as modulators of the activity of mitogen-activated protein kinase 4 (MEK4). The disclosed compounds include 3-Arylindazoles which may be formulated in pharmaceutical composition for treating cell proliferative diseases and disorders associated with MEK4 activity, including cancer.
    Type: Application
    Filed: June 24, 2020
    Publication date: December 24, 2020
    Applicant: NORTHWESTERN UNIVERSITY
    Inventors: Karl A. Scheidt, Gary E. Schiltz, Matthew R. Clutter, Ada J. Kwong
  • Publication number: 20200399242
    Abstract: The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R1 may optionally be substituted; R2 is an ?,??-substituted cyclic group which may optionally be further substituted; R3 and R4 are each independently hydrogen, halogen, —OH, —NH2, —CN, —R5, —OR5, —NHRs or —N(R5)2; or R3 and R4 together with the carbon atom to which they are attached may form a 3- to 7-membered saturated or unsaturated, optionally substituted cyclic group; and R5 is independently optionally substituted C1-C4 alkyl. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
    Type: Application
    Filed: March 1, 2019
    Publication date: December 24, 2020
    Inventors: David MILLER, Jimmy VAN WILTENBURG, Matthew COOPER
  • Publication number: 20200399243
    Abstract: The present invention relates to compounds of formula (1): wherein Q is selected from O or S; R1 is a 5-membered nitrogen-containing heteroaryl group substituted with R6 and optionally further substituted; R2 is an alpha, alpha?-substituted cyclic group which may optionally be further substituted; R3 and R4 are each independently hydrogen, halogen, —OH, —NH2, —CN, —R5, —OR5, —NHR5 or —N(R5)2; or R3 and R4 together with the carbon atom to which they are attached may form a 3 to 7 membered saturated or unsaturated, optionally substituted cyclic group; R5 is independently an optionally substituted C1-C4 alkyl group; and R6 is any group comprising a nitrogen atom. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
    Type: Application
    Filed: March 1, 2019
    Publication date: December 24, 2020
    Inventors: David MILLER, Jimmy VAN WILTENBURG, Matthew COOPER
  • Publication number: 20200399244
    Abstract: The present invention relates to compounds of formula (I) and formula (II): and to salts thereof, wherein R—R4 of formula (I) and R5-R6 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II), or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
    Type: Application
    Filed: May 28, 2020
    Publication date: December 24, 2020
    Applicants: GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Patrick Cyr, Sarah Bronner, F. Anthony Romero, Steven Magnuson, Vickie Hsiao-Wei Tsui, John Wai, Kwong Wah Lai, Fei Wang
  • Publication number: 20200399245
    Abstract: The present invention provides a novel pyrimidine compound represented by Formula [I] and a salt thereof: [in the formula, the symbols are as defined in the specification], which is useful for treating, preventing and/or diagnosing seizure and the like in disease involving epileptic seizure or convulsive seizure (including multiple drug resistant seizure, refractory seizure, acute symptomatic seizure, febrile seizure and status epilepticus), as well as a medical use therefor.
    Type: Application
    Filed: September 2, 2020
    Publication date: December 24, 2020
    Applicant: OTSUKA PHARMACEUTICAL CO, LTD.
    Inventors: Tomoichi SHINOHARA, Shin IWATA, Kenta ARAI, Nobuaki ITO, Masaki SUZUKI
  • Publication number: 20200399246
    Abstract: A charge transport material containing a compound represented by the following formula (1). R1 and R2 each are a fluoroalkyl group, Ar1 and Ar2 each are an aromatic ring, A1 and A2 each are an aryl group substituted with a group having a positive Hammett ?p value or with a phenyl group, or are a substituted or unsubstituted heteroaryl group bonding to Ar1 or Ar2 via a carbon atom, n1 and n2 each are a natural number.
    Type: Application
    Filed: March 13, 2019
    Publication date: December 24, 2020
    Inventors: Linsong CUI, Chihaya ADACHI, Keiro NASU, Ayataka ENDO, Shuo-Hsien CHENG, YuSeok YANG, Hiroko NOMURA
  • Publication number: 20200399247
    Abstract: Novel compounds inhibiting ATR protein kinase include compounds of formula (I) disclosed herein, as well as liposome formulations comprising ATR protein kinase inhibitor compounds. The compositions are useful for the treatment of cancer.
    Type: Application
    Filed: January 17, 2020
    Publication date: December 24, 2020
    Inventors: Daryl C. Drummond, Bolin Geng, Dmitri B. Kirpotin, Suresh K. Tipparaju, Alexander Koshkaryev, Ozan Alkan
  • Publication number: 20200399248
    Abstract: Disclosed is a pyrimidinone-containing compound represented by formula I, a preparation method thereof, a pharmaceutical composition, and an application thereof. The pyrimidinone-containing compound of the present disclosure can be used as HIV-1 inhibitor and can be also used in the treatment of human immunodeficiency virus infection.
    Type: Application
    Filed: March 4, 2019
    Publication date: December 24, 2020
    Inventors: Yanping HE, Hongbin ZHANG, Yongtang ZHENG, Yumeng WU, Chengrun TANG, Ruomei RUI, Liumeng YANG, Jiangyuan WANG
  • Publication number: 20200399249
    Abstract: The present invention discloses a compound represented by the following Formula (I) and a pharmaceutically acceptable salt thereof. The compound improves the THR? selectivity while maintaining good THR? agonistic activity, thereby improving properties of the finished drug.
    Type: Application
    Filed: September 4, 2020
    Publication date: December 24, 2020
    Inventors: Shanghai YU, Ben LI
  • Publication number: 20200399250
    Abstract: The present invention relates to novel TrkA inhibitors of formula (1) which are useful in the treatment or prevention of acute and chronic pain but also for other abnormal activities of TrkA beyond pain therapy, such as inflammation and cancer.
    Type: Application
    Filed: November 22, 2018
    Publication date: December 24, 2020
    Inventors: Eid Sameh, Simone Fulle, Benjamin Merget, Samo Turk
  • Publication number: 20200399251
    Abstract: The present application relates to an amine compound according to formula (I), (II) or (III) which is suitable for use in electronic devices.
    Type: Application
    Filed: March 6, 2019
    Publication date: December 24, 2020
    Inventors: Ilona STENGEL, Florian MAIER-FLAIG, Philipp HARBACH, Elvira MONTENEGRO, Aurélie LUDEMANN
  • Publication number: 20200399252
    Abstract: The invention relates to 3-((hetero-)aryl)-alkyl-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
    Type: Application
    Filed: August 31, 2020
    Publication date: December 24, 2020
    Applicant: Grünenthal GmbH
    Inventors: Sven KUEHNERT, Rene Michael KOENIGS, Achim KLESS, Anita WEGERT, Paul RATCLIFFE, Ruth JOSTOCK, Thomas KOCH, Klaus LINZ, Wolfgang SCHROEDER, Klaus SCHIENE, lngo KONETZKI
  • Publication number: 20200399253
    Abstract: This invention relates to compounds which are used in the preparation of the compound of formula (I).
    Type: Application
    Filed: September 4, 2020
    Publication date: December 24, 2020
    Applicant: PULMOCIDE LIMITED
    Inventors: MIHIRO SUNOSE, THOMAS CHRISTOPHER COLLEY, KAZUHIRO ITO, GARTH RAPEPORT, PETER STRONG
  • Publication number: 20200399254
    Abstract: The present invention is directed to substituted pyridine derivatives, pharmaceutical compositions containing said derivatives and the use of said derivatives in the treatment of disorders mediated by c-fms kinase. The present invention is further directed to a process for the preparation of said substituted pyridine derivatives.
    Type: Application
    Filed: September 2, 2020
    Publication date: December 24, 2020
    Inventors: Jie Chen, Matthew Donahue, Heng-Keang Lim, Ronghui Lin, Rhys Salter, Jiejun Wu, Yong Gong
  • Publication number: 20200399255
    Abstract: The invention relates to 8-amino-2-oxo-1,3-diaza-spiro[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
    Type: Application
    Filed: August 31, 2020
    Publication date: December 24, 2020
    Applicant: Grünenthal GmbH
    Inventors: Sven KUEHNERT, Rene Michael KOENIGS, Achim KLESS, Anita WEGERT, Paul RATCLIFFE, Ruth JOSTOCK, Thomas KOCH, Klaus LINZ, Wolfgang SCHROEDER
  • Publication number: 20200399256
    Abstract: The invention relates to an organic molecule, in particular for use in organic optoelectronic devices.
    Type: Application
    Filed: May 16, 2018
    Publication date: December 24, 2020
    Inventor: Stefan Seifermann
  • Publication number: 20200399257
    Abstract: Compounds of formula (I) as defined herein, to processes for preparing them, to pesticidal, in particular insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control pests such as insect, acarine, mollusc and nematode pests.
    Type: Application
    Filed: October 4, 2018
    Publication date: December 24, 2020
    Applicant: Syngenta Participations AG
    Inventors: Aurelien BIGOT, Myriem EL QACEMI, Denis GRIBKOV, André STOLLER
  • Publication number: 20200399258
    Abstract: The present invention relates to compounds of formula (1) or pharmaceutically acceptable salts thereof, wherein Ring A, R1-R8, and n are defined herein. The novel benzisoxazole sulfonamide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in patients. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in patients.
    Type: Application
    Filed: June 16, 2020
    Publication date: December 24, 2020
    Inventors: Ylva Elisabet Bergman Bozikis, Oleg Brodsky, Michelle Ang Camerino, Samantha Elizabeth Greasley, Robert Louis Hoffman, Robert Arnold Kumpf, Pei-Pei Kung, Paul Francis Richardson, Paul Anthony Stupple, Scott Channing Sutton
  • Publication number: 20200399259
    Abstract: This disclosure provides compounds with Bcl inhibitory activity based on a new chemical scaffold. Phosphonamidate compounds typically include a P-phenyl phosphonamidate moiety which is substituted with an N-aryl or N-heteroaryl group. The P-phenyl phosphonamidate moiety may be optionally substituted at phosphorus with thio (?S) instead of oxo (?O), and/or with a thioxy group or a second amino group instead of an oxy group. One of the heteroatoms attached to phosphorus may be cyclically linked to the N-substituted nitrogen atom that is attached to the phosphorus to provide a heterocyclic ring. By incorporating such a cyclic constraint between two phosphorus substituents of the core linking moiety, a favorable binding conformation may be promoted in the compounds. Selected compounds promote apoptosis in senescent cells, and can be developed for treating senescent-related conditions, such as osteoarthritis, ophthalmic disease, pulmonary disease, and atherosclerosis.
    Type: Application
    Filed: July 2, 2020
    Publication date: December 24, 2020
    Inventors: Anne-Marie Beausoleil, Ryan Hudson
  • Publication number: 20200399260
    Abstract: Disclosed are a compound as an ATR inhibitor and an application in preparing a drug as an ATR inhibitor. In particular, disclosed is a compound represented by formula (I) or an isomer or pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 2, 2019
    Publication date: December 24, 2020
    Inventors: Wenyuan QIAN, Jian WANG, Jie LI, Jian LI, Shuhui CHEN
  • Publication number: 20200399261
    Abstract: The present invention provides PRMT5 inhibitors of Formula (I), wherein R1 is a non-hydrogen monovalent group; W is a direct bond or —NH—; T, U, and V are independently of each other selected from C and N; R2 is H or a halo; m is 1 or 2; X is a carbon, a nitrogen, or an oxygen; Y is C or N; Z is a direct bond or a carbon; R3 is H, a non-hydrogen monovalent group, an oxo group, a bivalent spiro ring-forming group, or a bivalent bridge-forming group; n is 1 or 2; and Formula (II) stands for a single bond or a double bond. Pharmaceutical products comprising the PRMT5 inhibitors and use thereof in treating proliferative disorders such as cancer, metabolic disorders, blood disorders, autoimmune diseases, and inflammatory diseases are also provided.
    Type: Application
    Filed: March 8, 2019
    Publication date: December 24, 2020
    Inventors: Liu LIU, Jin LI, Minmin YANG
  • Publication number: 20200399262
    Abstract: The present invention relates to compounds for inhibiting protein degradation and/or the ubiquitin-proteasome system and/or for modulating autophagy, pharmaceutical composition and methods of use thereof in the treatment of cancer.
    Type: Application
    Filed: March 7, 2019
    Publication date: December 24, 2020
    Applicant: PI Therapeutics Ltd
    Inventors: Ori KALID, Irina GOTLIV, Einat LEVY-APTER, Danit FINKELSHTEIN BEKER, Parkash JAGTAP
  • Publication number: 20200399263
    Abstract: A process for preparing a compound represented by Formula [1], the process comprising a step of hydrolyzing a compound represented by Formula [2] under an acidic or basic condition, and a step of reacting a compound represented by Formula [3] with a metal acetate salt, and a step of halogenating a compound represented by Formula [4]; a process for preparing a compound represented by Formula [1] comprising a step of reacting a compound represented by Formula [3] with a metal acetate salt, and then, adding alcohol, water, or base to the reaction solution to perform reaction; a process for preparing a compound represented by Formula [1] comprising a step of reacting a compound represented by Formula [3] under a presence or absence of a base, an ionic liquid and a metal sulfate salt, in water or a mixed solvent of water and an organic solvent; a compound represented by Formula [2] or a salt of the same; and a compound represented by Formula [3] or a salt of the same.
    Type: Application
    Filed: February 8, 2016
    Publication date: December 24, 2020
    Inventors: Tsuyoshi Kawano, Makota Bamba, Diasuke Horikoshi
  • Publication number: 20200399264
    Abstract: The present disclosure is concerned with benzoannulene compounds that are capable of inhibiting a viral infection and methods of treating viral infections such as, for example, chikungunya, Venezuelan equine encephalitis, Eastern equine encephalitis, Western equine encephalitis, dengue, West Nile, influenza, and zika, using these compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 15, 2020
    Publication date: December 24, 2020
    Inventors: Ashish Kumar Pathak, Corinne E. Augelli-Szafran, Syed Kaleem Ahmed, Atefeh Garzan, Daniel Streblow, Nicole Haese
  • Publication number: 20200399265
    Abstract: The present invention relates to a CSF1R inhibitor, and in particular to a highly active CSF1R inhibitor compound having the structure of formula (I). Said compound of the present invention has high inhibitory activity on CSF1R.
    Type: Application
    Filed: May 24, 2019
    Publication date: December 24, 2020
    Applicant: ADLAI NORTYE BIOPHARMA CO., LTD.
    Inventors: Shifeng LIU, Zhiyong YU, Wei PANG, Ji WANG, Peng CHEN
  • Publication number: 20200399266
    Abstract: Disclosed herein are serine threonine kinase (AKT) degradation/disruption compounds including an AKT ligand, a degradation/disruption tag, and a linker, and methods of using such compounds in the treatment of AKT-mediated diseases.
    Type: Application
    Filed: March 6, 2019
    Publication date: December 24, 2020
    Inventors: Jian Jin, Jing Liu, Ramon E. Parsons, Jia Xu, Xufen Yu
  • Publication number: 20200399267
    Abstract: The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR4 enzyme and are useful in the treatment of FGFR4-associated diseases such as cancer.
    Type: Application
    Filed: July 9, 2020
    Publication date: December 24, 2020
    Inventors: Liang Lu, Liangxing Wu, Ding-Quan Qian, Wenqing Yao
  • Publication number: 20200399268
    Abstract: The invention relates to 6,5 heterobicyclic ring derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use for the treatment of inflammatory conditions driven by STING activation, such as, but not confined to, SLE and geographic atrophy.
    Type: Application
    Filed: February 15, 2019
    Publication date: December 24, 2020
    Inventors: Jag Paul Heer, Michal Sarah Hallside, Adam Peter Smalley, Josep Llaveria Cros, Benedicte Lallemand, Martin Alexander Lowe, Xianfu Li, Anthony John Richardson, Robert James Townsend
  • Publication number: 20200399269
    Abstract: The present disclosure provides compounds of formula (I) or (II) or a pharmaceutically acceptable salt or stereoisomer thereof, wherein Rx-R8 are defined herein. Also provided are compositions comprising a compound described herein and a pharmaceutically effective excipient, methods of stabilizing microtubules in a patient comprising administering to the patient a microtubule-stabilizing amount of a compound described herein, methods of treating cancer in a patient comprising administering to the patient a therapeutically effective amount of a compound described herein, and methods of treating a neurodegenerative disease in a patient comprising administering to the patient a therapeutically effective amount of a compound described herein.
    Type: Application
    Filed: February 28, 2019
    Publication date: December 24, 2020
    Inventors: Kurt R. BRUNDEN, Virginia M.Y. LEE, John Q. TROJANOWSKI, Carlo BALLATORE, Killian OUKOLOFF, Amos B. SMITH, III
  • Publication number: 20200399270
    Abstract: The invention provides an indolizine compound represented by formula I or a pharmaceutically acceptable salt thereof, a preparation method and a use thereof. The indolizine compound has an inhibitory effect on wild-type and/or mutant EZH2 or EZH1, and is expected to be developed into a novel drug for anti-tumor or for the treatment of autoimmune diseases.
    Type: Application
    Filed: March 5, 2019
    Publication date: December 24, 2020
    Inventors: Xuxing Chen, Yi Chen, Ying Huang, Meiyu Geng, Qiong Zhang, Jian Ding, Yucai Yao, Qianqian Shen, Yanyan Shen
  • Publication number: 20200399271
    Abstract: The present disclosure is concerned with xanthine analogs, methods of making xanthine analogs, and methods of treating West Nile virus using these analogs. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 18, 2020
    Publication date: December 24, 2020
    Inventors: Ashish Kumar Pathak, Theresa Ha Nguyen, Corinne E. Augelli-Szafran, Alec Jay Hirsch, Jessica Lee Smith
  • Publication number: 20200399272
    Abstract: The present invention relates to a crystal form of 2-(6-methyl-pyridin-2-yl)-3-(6-amido-quinolin-4-yl)-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazole (Galunisertib or LY2157299), represented by formula (I). Compared with the known solid form of Galunisertib, the crystal form of the present invention has advantages in terms of solubility, hygroscopicity, crystal stability, morphology and the like. The present invention also relates to a process of preparing the crystal forms of Galunisertib, a pharmaceutical composition thereof and a use thereof in the preparation of a medicament for the prevention and/or treatment of diseases associated with TGF-beta.
    Type: Application
    Filed: March 17, 2017
    Publication date: December 24, 2020
    Applicant: Hangzhou SoliPharma Co., Ltd.
    Inventors: Xiaohong SHENG, Xiaoxia SHENG, Jing WANG
  • Publication number: 20200399273
    Abstract: The present application provides sulfonyl amide compounds, which are inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.
    Type: Application
    Filed: March 27, 2020
    Publication date: December 24, 2020
    Inventors: Alexander Sokolsky, Sarah Winterton, Liangxing Wu, Wenqing Yao, Min Ye, Yingnan Chen, Margaret Favata, Yvonne Lo
  • Publication number: 20200399274
    Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined herein, and salts thereof, that are useful as JAK kinase inhibitors are described herein. Also provided are pharmaceutical compositions that include such a JAK inhibitor and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.
    Type: Application
    Filed: June 16, 2020
    Publication date: December 24, 2020
    Applicant: Genentech, Inc.
    Inventors: Mark Edward Zak, Naomi S. Rajapaksa, Yun-Xing Cheng, Jessica Grandner, Daniel G.M. Shore, F. Anthony Romero, Marian C. Bryan
  • Publication number: 20200399275
    Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined herein, and salts thereof that are useful as JAK kinse inhibitors are described herein. Also provided are pharmaceutical compositions that include such a JAK inhibitor and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.
    Type: Application
    Filed: June 16, 2020
    Publication date: December 24, 2020
    Applicant: Genentech, Inc.
    Inventors: Mark Edward Zak, Naomi S. Rajapaksa, Yun-Xing Cheng, Jessica Grandner, Daniel G.M. Shore, Marian C. Bryan
  • Publication number: 20200399276
    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 malaria.
    Type: Application
    Filed: June 29, 2020
    Publication date: December 24, 2020
    Applicant: THE BROAD INSTITUTE, INC.
    Inventors: EAMON COMER, NOBUTAKA KATO, CHRISTINA SCHERER, JESSICA BASTIEN, JEREMY DUVALL, TIMOTHY LEWIS, MORGANE SAYES, MATTHEW LEIGHTY, JUN PU, JENNIFER BEAUDOIN, BERTRAND BRAIBANT, BENITO MUNOZ
  • Publication number: 20200399277
    Abstract: The present invention provides a compound of Formula I: wherein R1 is methyl, ethyl or cyclopropyl; R2 is hydrogen, methyl, or ethyl; R3 is methyl or AA; and R4 is C2-C4 alkyl, BB; or a pharmaceutically acceptable salt thereof; for use as a PDE1 inhibitor.
    Type: Application
    Filed: January 13, 2019
    Publication date: December 24, 2020
    Inventors: Nicholas Paul CAMP, Chafiq HAMDOUCHI, Jayana Pankaj LINESWALA, John Richard MORPHY, Qing SHI
  • Publication number: 20200399278
    Abstract: The present invention provides a compound having an excellent control effect on a harmful arthropod.
    Type: Application
    Filed: December 25, 2018
    Publication date: December 24, 2020
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Ayaka TANAKA, Naoya SUGIMOTO, Risa KONO, Yoshihiko NOKURA
  • Publication number: 20200399279
    Abstract: Provided herein are compounds of the Formula I: and tautomers and pharmaceutically acceptable salts and solvates thereof, wherein R1 and R2 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
    Type: Application
    Filed: January 18, 2019
    Publication date: December 24, 2020
    Inventors: James F. BLAKE, Donghua DAI, Julia HAAS, Yutong JIANG, Gabrielle R. KOLAKOWSKI, Andrew T. METCALF, David A. MORENO, Brett PRIGARO, Li REN
  • Publication number: 20200399280
    Abstract: The invention relates to 3-(carboxymethyl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
    Type: Application
    Filed: August 31, 2020
    Publication date: December 24, 2020
    Applicant: Grünenthal GmbH
    Inventors: Sven KUEHNERT, Rene Michael KOENIGS, Florian JAKOB, Achim KLESS, Paul RATCLIFFE, Ruth JOSTOCK, Thomas KOCH, Klaus LINZ, Wolfgang SCHROEDER, Klaus SCHIENE, Anita WEGERT
  • Publication number: 20200399281
    Abstract: A compound having the structure: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A, A? and A? are independently O, C?O, C—R? or N—R?, where R? and R? may independently be H, amino, —NR7COR6, COR6, —CONR7R8, C1-C6 alkyl, or hydroxy(C1-C6 alkyl), and R? may be present or absent, and is present where the rules of valency permit, and where not more than one of A, A? and A? is O or C?O; R0 and R are independently H, Br, Cl, F, or C1-C6 alkyl; R1 is H, C1-C6 alkyl, or hydroxy(C1-C6 alkyl); R2 is selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, hydroxy(C1-C6 alkyl), phenyl(C1-C6 alkyl), formyl, heteroaryl, heterocyclic, —COR6, —OCOR6, —COOR6, —NR7COR6, —CONR7R8, and —(CH2)n—W, where W is cyano, hydroxy, C3-C8 cycloalkyl, —SO2NR7R8, and —SO2—R9, where R9 is C1-C6 alkyl, C3-C8 cycloalkyl, heteroaryl, or heterocyclic; wherein each of said alkyl, cycloalkyl, heterocyclic, or heteroaryl may be unsu
    Type: Application
    Filed: September 8, 2020
    Publication date: December 24, 2020
    Applicant: Pfizer Inc.
    Inventors: Matthew Frank BROWN, Alpay DERMENCI, Andrew FENSOME, Brian Stephen GERSTENBERGER, Matthew Merrill HAYWARD, Dafydd Rhys OWEN, Stephen Wayne WRIGHT, Li Huang XING, Xiaojing YANG
  • Publication number: 20200399282
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts therefore, wherein R1 to R6, A, U, V, W, X, Y, and Z are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: February 13, 2019
    Publication date: December 24, 2020
    Inventors: Steven Brunette, Jianwen Cui, Michael D. Lowe, Christopher Ronald Sarko, Simon Surprenant, Michael Robert Turner, Xinyuan Wu, Lana Louise Smith Keenan, Thierry Bouyssou, Paul Nicklin
  • Publication number: 20200399283
    Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
    Type: Application
    Filed: January 21, 2020
    Publication date: December 24, 2020
    Inventors: Minna BUI, Patrick CONLON, Julio H. CUERVO, Daniel A. ERLANSON, Junfa FAN, Bing GUAN, Brian T. HOPKINS, Tracy J. JENKINS, Gnanasambandam KUMARAVEL, Alexey A. LUGOVSKOY, Doug MARCOTTE, Noel POWELL, Daniel SCOTT, Laura SILVIAN, Art TAVERAS, Deping WANG, Min ZHONG
  • Publication number: 20200399284
    Abstract: The present invention relates to an urea-substituted aromatic ring-linked dioxinoquinoline compound of formula (I), or a pharmaceutically acceptable salt or a hydrate thereof. The invention also provides a preparation method of the compound of formula (I) and a pharmaceutically acceptable salt thereof, as well as uses thereof as a drug, wherein the drug acting as a tyrosine kinase (i.e. VEGFR-2, C-RAF, B-RAF, and RET) inhibitor is used for treating disorders related to tyrosine kinase.
    Type: Application
    Filed: January 25, 2019
    Publication date: December 24, 2020
    Inventors: Qiang Zhang, Shannan Yu, Zhongxiang Wang, Shouye Feng, Yansheng Liu, Xingfu Li, Hongbo Zhang, Leifu Yang, Hailong Yang, Likai Zhou, Nanqiao Zheng, Chenming Hu, Zhanqiang Xu
  • Publication number: 20200399285
    Abstract: The present invention relates to a dioxinoquinoline compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention also provides a preparation method of the compound of formula (I) and a pharmaceutically acceptable salt thereof, as well as uses thereof as a drug, wherein the drug acting as a tyrosine kinase (i.e. VEGFR-2 and c-MET) inhibitor is used for treating disorders related to tyrosine kinase.
    Type: Application
    Filed: January 25, 2019
    Publication date: December 24, 2020
    Inventors: Qiang Zhang, Shannan Yu, Zhongxiang Wang, Shouye Feng, Yueming Sun, Yansheng Liu, Hongbo Zhang, Leifu Yang, Hailong Yang, Likai Zhou, Nanqiao Zheng, Chenming Hu, Zhanqiang Xu