Patents Issued in June 27, 2019
  • DUAL NAV1.2/5HT2a INHIBITORS FOR TREATING CNS DISORDERS
    Publication number: 20190194163
    Abstract: Compounds of formula I: are disclosed, as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disorders in a patient in need are also disclosed. Such disorders include depression, bipolar disorder, pain, schizophrenia, obsessive compulsive disorder, addiction, social disorder, attention deficit hyperactivity disorder, an anxiety disorder, autism, a cognitive impairment, or a neuropsychiatric symptom such as apathy, depression, anxiety, psychosis, aggression, agitation, impulse control disorders, and sleep disorders in neurological disorders such as Alzheimer's and Parkinson's diseases.
    Type: Application
    Filed: August 4, 2016
    Publication date: June 27, 2019
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Michele L.R. HEFFERNAN, Larry Wendell HARDY, Scott P. BROWN, Lee W. HERMAN
  • COMPOUNDS WITH SPIROBIFLUORENE-STRUCTURES
    Publication number: 20190194164
    Abstract: The invention relates to spirobifluorene derivatives which are substituted with electron transport groups, in particular for use in electronic devices. The invention further relates to a method for producing the compounds according to the invention, and to electronic devices comprising the same.
    Type: Application
    Filed: September 11, 2017
    Publication date: June 27, 2019
    Inventors: Amir PARHAM, Tobias GROSSMANN, Aurélie LUDEMANN, Dominik JOOSTEN, Jonas KROEBER
  • SPIRO THREE-MEMBERED RING, SPIRO FIVE-MEMBERED RING PEPTIDE DEFORMYLASE INHIBITOR AND USE THEREOF IN ANTIBACTERIA AND ANTI-TUMOR
    Publication number: 20190194165
    Abstract: Disclosed are the anti-bacterial activity and the anti-tumor activity of a class of new spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, are effective against many antibiotic-resistant Gram-positive strains by inhibiting the activity of the peptide deformylase required in the synthesis of bacterial proteins, and do not affect the synthetic process of the main proteins of the human body, thus selectively killing bacteria.
    Type: Application
    Filed: May 10, 2017
    Publication date: June 27, 2019
    Applicant: Rudong Ruien Pharmaceutical Technology Co. Ltd
    Inventors: Wenhao HU, Fengping LV, Yang TANG, Ziyan LI, Chen CHEN, Jianhai WEI, Suzhen DONG, Yu QIAN
  • SUBSTITUTED PYRIDINES AS INHIBITORS OF DNMT1
    Publication number: 20190194166
    Abstract: The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: June 13, 2017
    Publication date: June 27, 2019
    Inventors: Nicholas David ADAMS, Andrew B. BENOWITZ, María Lourdes Rueda BENEDE, Karen Anderson EVANS, David T. FOSBENNER, Bryan Wayne KING, Mei LI, Juan Ignacio LUENGO, William Henry MILLER, Alexander Joseph REIF, Stuart Paul ROMERIL, Stanley J. SCHMIDT, Roger J. BUTLIN, Kristen M. GOLDBERG, Allan M. JORDAN, Christopher S. KERSHAW, Ali RAOOF, Bohdan WASZKOWYCS
  • DI-SUBSTITUTED PYRAZOLE COMPOUNDS FOR THE TREATMENT OF DISEASES
    Publication number: 20190194167
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds and compositions in treating a condition, disease, or disorder associated with abnormal activation of the SREBP pathway, including metabolic disorders such as obesity, cancer, cardiovascular disease, and nonalcoholic fatty liver disease (NAFLD) wherein the compound is according to Formula (I).
    Type: Application
    Filed: September 7, 2017
    Publication date: June 27, 2019
    Inventors: Motonari UESUGI, John KINCAID, Joel HUFF
  • CRYSTAL FORM, SALT TYPE OF SUBSTITUTED 2-HYDRO-PYRAZOLE DERIVATIVE AND PREPARATION METHOD THEREFOR
    Publication number: 20190194168
    Abstract: A crystal form and a salt type of a substituted 2-hydro-pyrazole derivative, preparation method therefor, and use of the crystal form and the salt type in preparation of a medicament for treating cancers such as breast cancer, lung cancer and the like.
    Type: Application
    Filed: September 8, 2017
    Publication date: June 27, 2019
    Inventors: Charles Z. Ding, Shuhui Chen, Lihong Hu, Zhaobing Xu, Yingchun Liu, Bingjie Ren, Weidong Li, Zongbin Li, Rui Zhao, Xiquan Zhang
  • NOVEL PYRIMIDINES AS EGFR INHIBITORS AND METHODS OF TREATING DISORDERS
    Publication number: 20190194169
    Abstract: The application relates to a compound having Formula (I): which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.
    Type: Application
    Filed: March 1, 2019
    Publication date: June 27, 2019
    Inventors: Nathanael S. GRAY, Pasi JANNE, Hwan Geun CHOI, Jaebong JANG
  • POLYMORPHS AND SOLID FORMS OF A PYRIMIDINYLAMINO-PYRAZOLE COMPOUND, AND METHODS OF PRODUCTION
    Publication number: 20190194170
    Abstract: The present disclosure relates to crystalline polymorph and amorphous forms of 2-methyl-2-(3-methyl-4-(4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-1H-pyrazol-1-yl)propanenitrile or solvates, tautomers, and pharmaceutically acceptable salts or cocrystals thereof, and processes for their preparation.
    Type: Application
    Filed: November 20, 2018
    Publication date: June 27, 2019
    Applicant: Denali Therapeutics Inc.
    Inventors: Travis Remarchuk, Anantha Sudhakar
  • ORGANIC MOLECULES FOR USE IN ORGANIC OPTOELECTRONIC DEVICES
    Publication number: 20190194171
    Abstract: An organic molecule is disclosed having: a first chemical unit according to Formula I and two second chemical units D, which are respectively the same or different in each occurrence, according to Formula II, wherein, in each case, the first chemical unit is connected to the two second chemical units D via a single bond.
    Type: Application
    Filed: August 31, 2017
    Publication date: June 27, 2019
    Inventors: Larissa Bergmann, Daniel Zink, Stefan Seifermann
  • PYRAZINE DERIVATIVES WITH EXTENDED CONJUGATION AND METHODS OF USING THE SAME IN OPTICAL APPLICATIONS
    Publication number: 20190194172
    Abstract: The present invention relates to pyrazine derivatives capable of absorbing and emanating spectral energy in the visible and/or near infrared spectrum. Pyrazine derivatives of the invention may be administered to a patient in the form of a pharmaceutically acceptable composition and utilized in medical (e.g., diagnostic imaging) procedures.
    Type: Application
    Filed: February 28, 2019
    Publication date: June 27, 2019
    Inventors: William L. Neumann, Raghavan Rajagopalan, Richard B. Dorshow
  • 6-HYDROXY-5-(PHENYL/HETEROARYLSULFONYL)PYRIMIDIN-4(1H)-ONE AS APJ AGONISTS
    Publication number: 20190194173
    Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.
    Type: Application
    Filed: June 14, 2017
    Publication date: June 27, 2019
    Inventors: George O. Tora, Heather Finlay, Wen Jiang, Wei Meng, Xiaojun Zhang
  • QUINAZOLINONES AS PARP14 INHIBITORS
    Publication number: 20190194174
    Abstract: The present invention relates to quinazolinones and related compounds which are inhibitors of PARP14 and are useful, for example, in the treatment of cancer and inflammatory diseases.
    Type: Application
    Filed: December 20, 2018
    Publication date: June 27, 2019
    Inventors: Laurie B. Schenkel, Melissa Marie Vasbinder, Kevin Wayne Kuntz, Kerren Kalai Swinger
  • SALT FORMS OF 4-CYANO-N-(4,4-DIMETHYLCYCLOHEX-1-EN-1-YL)-6-(2,2,6,6-TETRAMETHYLTETRAHYDRO-2H-PYRAN-4-YL)PYRIDIN-3-YL)-1H-IMIDAZOLE-2-CARBOXAMIDE
    Publication number: 20190194175
    Abstract: The present disclosure discusses salt forms of 4-cyano-N-[2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl]-1H-imidazole-2-carboxamide.
    Type: Application
    Filed: February 28, 2019
    Publication date: June 27, 2019
    Inventors: Nagy E. Fawzy, David Breslin
  • INHIBITORS OF JUN N-TERMINAL KINASE
    Publication number: 20190194176
    Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
    Type: Application
    Filed: February 28, 2019
    Publication date: June 27, 2019
    Applicant: IMAGO PHARMACEUTICALS, INC.
    Inventors: Hing L. SHAM, Roy K. HOM, Andrei W. KONRADI, Gary D. PROBST, Simeon BOWERS, Anh TRUONG, R. Jeffrey NEITZ, Jennifer SEALY, Gergely TOTH
  • PROCESS FOR THE PREPARATION OF COMPOUNDS USEFUL AS INHIBITORS OF SGLT2
    Publication number: 20190194177
    Abstract: The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.
    Type: Application
    Filed: April 12, 2012
    Publication date: June 27, 2019
    Applicant: JANSSEN PHARAMCEUTICA NV
    Inventors: Ioannis Nicolaos Houpis, Sebastien Francois Emmanuel Lemaire
  • SUBSTITUTED UREAS AND METHODS OF MAKING AND USING SAME
    Publication number: 20190194178
    Abstract: The invention relates to substituted ureas, and compositions comprising the same, which in certain embodiments are useful for treating and/or preventing pain in a subject in need thereof.
    Type: Application
    Filed: August 31, 2017
    Publication date: June 27, 2019
    Inventors: BRETT A. TOUNGE, SHARIFF BAYOUMY, LAWRENCE C. KUO, SCOTT DAX
  • ANTIBIOTIC COMPOUNDS
    Publication number: 20190194179
    Abstract: The present invention relates to antibiotic compounds of formula (I), to compositions containing these compounds and to methods of treating bacterial diseases and infections using the compounds. The compounds find application in the treatment of infection with, and diseases caused by, Gram-positive and/or Gram-negative bacteria, and in particular in the treatment of infection with, and diseases caused by, Neisseria gonorrhoeae.
    Type: Application
    Filed: August 22, 2017
    Publication date: June 27, 2019
    Applicant: DISCUVA LTD.
    Inventors: Paul MEO, Nawaz KHAN
  • SUBSTITUTED N-[2-(4-PHENOXYPIPERIDIN-1-YL)-2-(1,3-THIAZOL-5-YL)ETHYL]BENZAMIDE AND N-[2-(4-BENZYLOXYPIPERIDIN-1-YL)-2-(1,3-THIAZOL-5-YL)ETHYL]BENZAMIDE DERIVATIVES P2X7 RECEPTOR ANTAGONISTS
    Publication number: 20190194180
    Abstract: The present invention relates to novel substituted phenoxy- and benzyloxy-piperidine compounds of formula (I) having P2X7 receptor (P2X7) antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.
    Type: Application
    Filed: August 9, 2017
    Publication date: June 27, 2019
    Applicant: Axxam S.P.A.
    Inventors: Paolo Pevarello, Adolfo Prandi
  • Substituted Fused Imidazole Derivatives, Pharmaceutical Compositions, and Methods of Use Thereof
    Publication number: 20190194181
    Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating conditions or diseases of the eye are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.
    Type: Application
    Filed: March 5, 2019
    Publication date: June 27, 2019
    Inventors: Adnan M.M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
  • RAD51 INHIBITORS
    Publication number: 20190194182
    Abstract: This application is directed to inhibitors of RAD51 represented by the following structural formula, and methods for their use, such as to treat cancer, autoimmune diseases, immune deficiencies, or neurodegenerative diseases.
    Type: Application
    Filed: December 31, 2018
    Publication date: June 27, 2019
    Inventors: Alfredo C. CASTRO, Casey Cameron MCCOMAS, Joseph VACCA, Tyler MACLAY
  • TRIAZOLOPYRIDINES
    Publication number: 20190194183
    Abstract: The present invention relates to compounds of formula wherein HetAr is a five or six membered hetaryl group, containing one, two or three heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R2 is lower alkyl substituted by halogen; R3 is hydrogen, lower alkyl substituted by halogen, lower alkyl or lower alkyl substituted by hydroxy; Y is R4 is lower alkoxy, lower alkoxy substituted by halogen or CN; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
    Type: Application
    Filed: December 18, 2018
    Publication date: June 27, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Bjoern BARTELS, Roland JAKOB-ROETNE, Anja LIMBERG, Werner NEIDHART, Hasane RATNI, Rosa Maria RODRIGUEZ SARMIENTO
  • BENZENESULFONAMIDE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS
    Publication number: 20190194184
    Abstract: This invention is directed to methods of preparing benzenesulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy.
    Type: Application
    Filed: February 28, 2019
    Publication date: June 27, 2019
    Inventors: Jean-Christophe Andrez, Kristen Nicole Burford, Sultan Chowdhury, Charles Jay Cohen, Christoph Martin Dehnhardt, Robert Joseph Devita, James Roy Empfield, Thilo Focken, Michael Edward Grimwood, Syed Abid Hasan, James Philip Johnson, JR., Alla Yurevna Zenova
  • PHENYL [A]INDOLE[2,3-G]QUINOLIZINE COMPOUNDS, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND APPLICATIONS THEREOF
    Publication number: 20190194185
    Abstract: The present invention relates to phenyl [a]indole[2,3-g]quinolizine compounds represented by formula (I), a preparation method therefor, a pharmaceutical composition, and applications thereof. Specific applications are applications in the preparation of drugs for treating diseases related to a proprotein convertase subtilisin Kexin-9 (PCSK9), comprising the applications in the preparation of drugs for treating hyperlipemia, hypercholesterolemia, hypertriglyceridemia, fatty liver deformation, atherosclerosis, obesity and other metabolic diseases.
    Type: Application
    Filed: March 29, 2017
    Publication date: June 27, 2019
    Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Hong Liu, Yiping Wang, Fei Zhao, Jing Zhao, Jiang Wang, Cong Xi, Chenglin Wu, Hao Shen, Xu Han, Hualiang Jiang, Kaixian Chen
  • HETEROARYL SUBSTITUTED BENZOIC ACIDS AS RORgammaT INHIBITORS AND USES THEREOF
    Publication number: 20190194186
    Abstract: The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
    Type: Application
    Filed: October 27, 2016
    Publication date: June 27, 2019
    Inventors: Hongjun Zhang, Kenneth Jay Barr, Blair T. Lapointe, Hakan Gunaydin, Kun Liu, B. Wesley Trotter
  • PROCESS FOR PREPARING N-(5-(3-(7-(3-FLUOROPHENYL)-3H-IMIDAZO[4,5-C]PYRIDIN-2-YL)-1H-INDAZOL-5-YL)PYRIDIN-3-YL)-3-METHYLBUTANAMIDE
    Publication number: 20190194187
    Abstract: Provided herein is a synthetic process for preparing a compound of Formula (1). The disclosure also provides useful intermediates and salts, amorphous and polymorph forms of the compound of Formula (1). These compounds are useful for various disease including cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, and osteoarthritis as well as Wnt-related diseases.
    Type: Application
    Filed: August 28, 2018
    Publication date: June 27, 2019
    Inventor: Sunil Kumar KC
  • METHODS FOR TREATING CANCER AND NON-NEOPLASTIC CONDITIONS
    Publication number: 20190194188
    Abstract: Compounds that selectively inhibit pathological production of human vascular endothelial growth factor (VEGF) and compositions comprising such Compounds are described. Compounds that inhibit viral replication or the production of viral RNA or DNA or viral protein and compositions comprising such Compounds are described. Also described are methods of reducing VEGF using such Compounds and methods for treating cancer and non-neoplastic conditions involving the administration of such Compounds. Further described are methods of inhibiting viral replication or the production of viral RNA or DNA or viral protein using such Compounds and methods for treating viral infections involving the administration of such Compounds. The Compounds may be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatments.
    Type: Application
    Filed: September 5, 2018
    Publication date: June 27, 2019
    Inventors: THOMAS W. DAVIS, MARLA L. WEETALL
  • 1H-PYRAZOLO[4,3-B]PYRIDINES AS PDE1 INHIBITORS
    Publication number: 20190194189
    Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
    Type: Application
    Filed: December 12, 2018
    Publication date: June 27, 2019
    Inventors: Karsten Juhl, Mikkel Jessing, Morten Langgård, Paulo Jorge Vieira Vital, Jan Kehler, Lars Kyhn Rasmussen, Carl Martin Sebastian Clementson, Mauro Marigo
  • Compounds and Their Use in Treating Cancer
    Publication number: 20190194190
    Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts and prodrugs thereof, where R1, R4, R5, R6, R7, Linker, X, Y, A, G, D and E have any of the meanings defined herein. This specification also relates to the use of such compounds and pharmaceutically acceptable salts and prodrugs thereof in methods of treatment of the human or animal body, for example in prevention or treatment of cancer. This specification also relates to processes and intermediate compounds involved in the preparation of such compounds and to pharmaceutical compositions containing them.
    Type: Application
    Filed: December 18, 2018
    Publication date: June 27, 2019
    Inventors: Bin YANG, Jason Grant KETTLE, Thomas George Christopher HAYHOW, Timothy Gordon RASMUSSON, Johannes Wilhelmus Maria NISSINK, Charlene FALLAN, Gillian McGregor Lamont
  • DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
    Publication number: 20190194191
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Application
    Filed: December 20, 2018
    Publication date: June 27, 2019
    Inventors: George D. Hartman, Scott Kuduk
  • NOVEL BENZYLAMINO SUBSTITUTED PYRIDOPYRIMIDINONES AND DERIVATIVES AS SOS1 INHIBITORS
    Publication number: 20190194192
    Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R4, A and p have the meanings given in the claims and specification, their use as inhibitors of SOS1, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Application
    Filed: December 20, 2018
    Publication date: June 27, 2019
    Inventors: Juergen RAMHARTER, Christiane KOFINK, Heinz STADTMUELLER, Tobias WUNBERG, Marco Hans HOFMANN, Anke BAUM, Michael GMACHL, Dorothea Ingrid RUDOLPH, Fabio SAVARESE, Markus OSTERMEIER, Markus FRANK, Annika GILLE, Stefan GOEPPER, Marco SANTAGOSTINO, Julian WIPPICH
  • AMINOQUINAZOLINE COMPOUNDS HAVING ANTI-INFLAMMATORY, ANTIFUNGAL, ANTIPARASITIC, AND ANTICANCER ACTIVITY
    Publication number: 20190194193
    Abstract: Amine compounds having activity against inflammation, fungi, unicellular parasitic microorganisms, and cancer are described. The compounds contain a monocyclic, bicyclic, or tricyclic aromatic ring having one, two, or three ring nitrogen atoms.
    Type: Application
    Filed: February 26, 2019
    Publication date: June 27, 2019
    Inventors: David M. SIMPSON, Dennis Bryan ZERBY, Ming LU, Reid W. VON BORSTEL, Rui LI, Julian READING, Stephen WOLPE
  • ANTIBACTERIAL CYCLOPENTA[C]PYRROLE SUBSTITUTED 3,4-DIHYDRO-1H-[1,8]NAPHTHYRIDINONES
    Publication number: 20190194194
    Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
    Type: Application
    Filed: February 26, 2019
    Publication date: June 27, 2019
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
  • METHOD OF MAKING TETRAHYDRONAPHTHYRIDINYL NONANOIC ACID COMPOUNDS
    Publication number: 20190194195
    Abstract: The present application relates to methods of preparing a compound of formula I: or a pharmaceutically acceptable salt or solvate thereof.
    Type: Application
    Filed: February 28, 2019
    Publication date: June 27, 2019
    Inventor: Takeru FURUYA
  • SALTS AND CRYSTALLINE FORMS OF AN APOPTOSIS-INDUCING AGENT
    Publication number: 20190194196
    Abstract: Salts and crystalline forms of 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}-sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
    Type: Application
    Filed: February 28, 2019
    Publication date: June 27, 2019
    Inventors: Nathaniel Catron, Shuang Chen, Yuchuan Gong, Geoff G. Zhang
  • NEW PROCESSES FOR THE PREPARATION OF VEMURAFENIB
    Publication number: 20190194197
    Abstract: Novel processes are disclosed for manufacture of N-(3-(5-(4-chlorophenyl)-1 H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide (I), wherein no protection-deprotection sequences or halogenation steps are required and use of palladium catalysts is minimized.
    Type: Application
    Filed: June 30, 2017
    Publication date: June 27, 2019
    Applicant: Fermion Oy
    Inventor: Antti KATAJA
  • NOVEL PYRAZOLE DERIVATIVE AS ALK5 INHIBITOR AND USES THEREOF
    Publication number: 20190194198
    Abstract: The present disclosure relates to a novel substituted pyrazole derivative having an effect of inhibiting serine/threonine kinase activity targeting receptor ALK5 of TGF-?, and a pharmaceutical composition including the compound of the present disclosure as an active ingredient may be useful in preventing and/or treating cancers, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, pulmonary diseases, cardiovascular diseases or metabolic diseases, or other diseases associated with a decrease in TGF family signaling activity.
    Type: Application
    Filed: June 30, 2017
    Publication date: June 27, 2019
    Applicant: HANMI PHARMACEUTICAL CO., LTD.
    Inventors: Kyung Ik LEE, Young Hee JUNG, Ji Young SONG, Seung Ah JUN
  • Pharmaceutically Acceptable Salt of EGFR Inhibitor, Crystal Form Thereof, Preparation Method Therefor and Application Thereof
    Publication number: 20190194199
    Abstract: Provided in the present disclosure are a pharmaceutically acceptable salt of an epidermal growth factor receptor (EGFR) inhibitor, a crystal form thereof, a preparation method therefor and an application thereof. The structural formula of the EGFR inhibitor is as shown in formula I, and the pharmaceutically acceptable salt is a mesylate, p-toluenesulfonate, phosphate, hydrochloride or citrate salt of the EGFR inhibitor. The pharmaceutically acceptable salt of EGFR inhibitor of the present disclosure has a specific crystal form, has a higher solubility and stability than a corresponding free base, is more suitable for preparing drugs for use in treating cancer (especially non-small cell lung cancer), and satisfies the requirements for bioavailability and drug efficacy.
    Type: Application
    Filed: January 2, 2018
    Publication date: June 27, 2019
    Inventors: Ping Zhou, Jiaquan Wu, Shenshuang Jin, Li Li
  • SPIRO-LACTAM NMDA MODULATORS AND METHODS OF USING SAME
    Publication number: 20190194200
    Abstract: Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Application
    Filed: August 1, 2017
    Publication date: June 27, 2019
    Applicant: Aptinyx Inc.
    Inventor: M. Amin KHAN
  • 7-BENZYL-4-(2-METHYLBENZYL)-2,4,6,7,8,9-HEXAHYDROIMIDAZO [1,2-A]PYRIDO[3,4-E]PYRIMIDIN-5(1H)-ONE, ANALOGS THEREOF, AND SALTS THEREOF AND METHODS FOR THEIR USE IN THERAPY
    Publication number: 20190194201
    Abstract: This disclosure relates to methods of treatment using compound (1) or analogs thereof, and pharmaceutically acceptable salts thereof. Also disclosed are compounds of formula (10): as defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising the same. Methods of treatment, such as for cancer, are provided that comprise administering the compounds and their salts to a subject in need of such treatment.
    Type: Application
    Filed: February 27, 2019
    Publication date: June 27, 2019
    Applicant: ONCOCEUTICS, INC.
    Inventors: Joshua E. ALLEN, Martin STOGNIEW, Richard S. POTTORF, Bhaskara Rao NALLAGANCHU, Gary OLSON, Yanjun SUN
  • COMPOUNDS AND COMPOSITIONS FOR TREATING CHEMICAL WARFARE AGENT-INDUCED INJURIES
    Publication number: 20190194202
    Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.
    Type: Application
    Filed: January 24, 2019
    Publication date: June 27, 2019
    Inventor: Jayhong A. Chong
  • HETEROARYL PYRIDONE AND AZA-PYRODINE COMPOUNDS
    Publication number: 20190194203
    Abstract: Heteroaryl pyridone and aza-pyridone compounds are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: June 27, 2018
    Publication date: June 27, 2019
    Applicant: Genentech, Inc.
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
  • 1,5-DIHYDRO-4H-PYRAZOLO[3,4-D]PYRIMIDIN-4-ONES AND 1,5-DIHYDRO-4H-PYRAZOLO[4,3-C]PYRIDIN-4-ONES AS PDE1 INHIBITORS
    Publication number: 20190194204
    Abstract: The present invention provides 1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-ones of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
    Type: Application
    Filed: August 1, 2018
    Publication date: June 27, 2019
    Inventors: Karsten Juhl, Mikkel Jessing, Morten Langgård, Paulo Jorge Vieira Vital, Mauro Marigo, Jan Kehler, Lars Kyhn Rasmussen
  • ANTIMICROBIALS AND METHODS OF MAKING AND USING SAME
    Publication number: 20190194205
    Abstract: The present disclosure relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, reducing the risk of, and delaying the onset of microbial infections in humans and animals. In some embodiments, the present disclosure provides a compound of Formula (I) or a tautomer thereof or a pharmaceutically acceptable salt of the compound or tautomer.
    Type: Application
    Filed: May 5, 2017
    Publication date: June 27, 2019
    Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Zoltan F. Kanyo, Joseph A. Ippolito
  • NOVEL SELECTIVE PI3K DELTA INHIBITORS
    Publication number: 20190194206
    Abstract: The present invention relates to selective inhibitors of PI3K delta protein kinases, methods of preparing them, pharmaceutical compositions containing them and methods of treatment and/or prevention of kinase mediated diseases or disorders with them.
    Type: Application
    Filed: August 22, 2018
    Publication date: June 27, 2019
    Inventors: Swaroop K. Vakkalanka, Meyyappan Muthuppalaniappan, Dhanapalan Nagarathnam
  • COMPOSITIONS AND METHODS OF USING THE SAME FOR TREATMENT OF NEURODEGENERATIVE AND MITOCHONDRIAL DISEASE
    Publication number: 20190194207
    Abstract: The present disclosure is directed, in part, to compounds, or pharmaceutically acceptable salts thereof, for the treatment and/or prevention of neurodegenerative disease, mitochondrial disease, fibrosis, and/or cardiomyopathy.
    Type: Application
    Filed: November 15, 2018
    Publication date: June 27, 2019
    Inventors: Daniel de Roulet, Robert Devita
  • DIARYL SUBSTITUTED 5,5-FUSED RING COMPOUNDS AS C5aR INHIBITORS
    Publication number: 20190194208
    Abstract: The present disclosure provides, inter alia, Compounds of Formula (I) or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathologic activation from C5a and non-pharmaceutical applications.
    Type: Application
    Filed: December 20, 2018
    Publication date: June 27, 2019
    Inventors: Pingchen FAN, Christopher W. LANGE, Rebecca M. LUI, Viengkham MALATHONG, Venkat Reddy MALI, Sreenivas PUNNA, Rajinder SINGH, Yibin ZENG, Penglie ZHANG
  • PYRAZOLE CARBOXAMIDE COMPOUNDS AND METHODS OF USE
    Publication number: 20190194209
    Abstract: Pyrazole carboxamide compounds of Formula I are provided, with various substituents, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: February 28, 2019
    Publication date: June 27, 2019
    Applicant: Genentech, Inc.
    Inventors: Roland J. BILLEDEAU, James J. CRAWFORD, Saul JAIME-FIGUEROA, Wendy LEE, Francisco Javier LOPEZ-TAPIA, Sung-Sau SO
  • SYNTHESIS OF TRANS-8-CHLORO-5-METHYL-1 -[4-(PYRIDIN-2-YLOXY)-CYCLOHEXYL]-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENE AND CRYTALLINE FORMS THEREOF
    Publication number: 20190194210
    Abstract: The invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.
    Type: Application
    Filed: March 4, 2019
    Publication date: June 27, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Benno Rothenhaeusler, Rene Trussardi, Fabienne Hoffmann-Emery, Urs Schwitter, Jean-Michel Adam, Olaf Grassmann, Thomas Hartung, Frederic Ran, Ralph Diodone, Christophe Pfleger, Bjorn Bartels
  • PROCESS FOR PREPARING BETA 3 AGONISTS AND INTERMEDIATES
    Publication number: 20190194211
    Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.
    Type: Application
    Filed: March 11, 2019
    Publication date: June 27, 2019
    Inventors: Feng Xu, Zhuqing Liu, Richard Desmond, Jeonghan Park, Alexei Kalinin, Birgit Kosjek, Hallena Strotman, Hongmei Li, Johannah Moncecchi
  • Compounds For Reducing c-Myc In c-Myc Overexpressing Cancers Background
    Publication number: 20190194212
    Abstract: The invention relates to new compounds that reduce c-Myc expression and useful for cancer treatment, particularly hematological cancers such as aggressive B- and T-cell lymphomas. The new compounds may be combined with adjunct c-Myc inhibor agents such as a PI3K inhibitor, CK-1 inhibitor, Akt-inhibitor, proteasome inhibitor and/or mTor inhibitor. The c-Myc reducing agent may be provided as a lead-in treatment to reduce or initiate reduction of c-Myc prior to adminstration of the adjunct cancer therapeutic agent. Treatment with a c-Myc reducing agent modulates the disease state of the c-Myc overexpressing cancer making it less malignant and more susceptible to adjunctive cancer therapies.
    Type: Application
    Filed: May 15, 2017
    Publication date: June 27, 2019
    Inventors: Changchun Deng, Mark Lipstein, Owen O'Connor, Donald W. Landry, Xiaoming Xu, Shi-Xian Deng, Xavier O. Jirau Serrano