Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/210.21)
  • Patent number: 11180501
    Abstract: Disclosed in the present disclosure are a crystal form of a ?-lactamase inhibitor and a preparation method therefor, as well as an application of the crystal form in preparing a ?-lactamase inhibitor drug.
    Type: Grant
    Filed: December 3, 2018
    Date of Patent: November 23, 2021
    Assignee: QILU PHARMACEUTICAL CO., LTD.
    Inventors: Cheng Li, Zhigang Huang, Charles Z. Ding, Weidong Li
  • Patent number: 11174232
    Abstract: The present invention provides substituted heterocyclylderivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors. These compounds are useful in the treatment and prevention of diseases and/or disorders associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted heterocyclyl derivatives of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.
    Type: Grant
    Filed: May 6, 2020
    Date of Patent: November 16, 2021
    Assignee: Aurigene Discovery Technologies Limited
    Inventors: Susanta Samajdar, Ramulu Poddutoori, Chetan Pandit, Subhendu Mukherjee, Rajeev Goswami
  • Patent number: 11174251
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.
    Type: Grant
    Filed: October 17, 2019
    Date of Patent: November 16, 2021
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
  • Patent number: 11161852
    Abstract: Compounds having activity as inhibitors of NEK7 are provided. The compounds have Structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein, A, X, Y, R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of the NLRP3 inflammasome are also provided.
    Type: Grant
    Filed: May 7, 2021
    Date of Patent: November 2, 2021
    Assignee: HALIA THERAPEUTICS, INC.
    Inventors: David James Bearss, John Sai Keong Kauwe, III, Alexis Henri Abel Mollard
  • Patent number: 11154539
    Abstract: The invention provides a compound for use in the treatment of T-Cell Acute Lymphoblastic Leukaemia (T-ALL), the compound having the formula (1): or being a pharmaceutically acceptable salt thereof; wherein: n is 0, 1 or 2; Ar1 is selected from an optionally substituted phenyl, pyridyl, thienyl and furanyl; Q1 is selected from C(?O), S(?O) and SO2; A is absent or is NR2; R1 is selected from: hydrogen; an optionally substituted C1-6 non-aromatic hydrocarbon group; and optionally substituted 3- to 7-membered non-aromatic carbocyclic and heterocyclic rings containing one or two heteroatom ring members selected from O, N and S, and bridged bicyclic heterocyclic rings of seven to nine ring members of which one or two are nitrogen atoms, the carbocyclic and heterocyclic rings and bridged bicyclic heterocyclic rings; R2 is selected from hydrogen and C1-4 alkyl; or NR1R2 forms an optionally substituted 4- to 7-membered non-aromatic nitrogen-containing heterocyclic ring optionally containing a second hete
    Type: Grant
    Filed: October 20, 2017
    Date of Patent: October 26, 2021
    Assignee: Sareum Limited
    Inventor: John Charles Reader
  • Patent number: 11155879
    Abstract: The present invention relates to a method of predicting the likelihood that a patient will respond therapeutically to a pancreatic cancer treatment comprising the administration of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one (Compound 1) and/or tautomers thereof or a pharmaceutically acceptable salt or hydrate thereof, comprising the steps of: STEP (1): determining a KRAS gene mutation status of a sample from a patient, and STEP (2): predicting an increased likelihood that the patient will respond therapeutically to the pancreatic cancer treatment if the patient has the presence of KRAS gene mutation(s), and to methods of treating pancreatic cancer.
    Type: Grant
    Filed: March 1, 2017
    Date of Patent: October 26, 2021
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Akihiro Ohashi, Kenichi Iwai, Tadahiro Nambu, Ryo Dairiki, Yuko Ishii
  • Patent number: 11149025
    Abstract: This invention provides, among other things, compounds useful for treating diseases such as cancer, pharmaceutical formulations containing such compounds, as well as combinations of these compounds with at least one additional therapeutic agent.
    Type: Grant
    Filed: February 13, 2020
    Date of Patent: October 19, 2021
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Csaba J. Peto, David Jablons, Hassan Lemjabbar-Alaoui
  • Patent number: 11117896
    Abstract: A process for preparing a diazabicyclooctane compound represented by the following formula (I): wherein A represents RcO—; B represents NH or NC1-6 alkyl; C represents a benzyl group; Rc represents a C1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c): wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.
    Type: Grant
    Filed: October 22, 2019
    Date of Patent: September 14, 2021
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Takao Abe, Takeshi Furuuchi, Yoshiaki Sakamaki, Seiichi Inamura, Akihiro Morinaka
  • Patent number: 11091489
    Abstract: Provided herein are crystalline forms of a triazolopyrimidine compound, which is useful for treating a PRC2-mediated disease or disorder.
    Type: Grant
    Filed: June 19, 2017
    Date of Patent: August 17, 2021
    Assignee: Novartis AG
    Inventors: Ying Huang, Bo Liu, Liang Mao, Long Wang, Liladhar Murlidhar Waykole, Lijun Zhang
  • Patent number: 11077128
    Abstract: Provided herein are alpha2-selective Na,K-ATPase inhibitors and prodrugs thereof, characterized by having a cyclic moiety attached to a digoxin or digitoxin derivative, as well as uses thereof in lowering intraocular pressure and in treating glaucoma and heart conditions.
    Type: Grant
    Filed: April 14, 2020
    Date of Patent: August 3, 2021
    Assignee: Yeda Research and Development Co. Ltd.
    Inventors: Steven J. D. Karlish, Adriana Katz, Daniel M. Tal, Arie Marcovich
  • Patent number: 11053239
    Abstract: Bcl-2 inhibitors, pharmaceutical compositions thereof, and methods of use thereof are provided. In particular, Bcl-2 inhibitors of formula (I) are provided, wherein the variable groups are as defined in the specification. The Bcl-2 inhibitors can be used to treat cell proliferative disorders.
    Type: Grant
    Filed: January 5, 2018
    Date of Patent: July 6, 2021
    Assignee: Fochon Pharmaceuticals, Ltd.
    Inventors: Xingdong Zhao, Zuwen Zhou, Chengxi He, Zhifu Li, Yue Rong, Rui Tan, Huajie Zhang, Hongbin Liu, Weipeng Zhang, Haohan Tan, Zhifang Chen, Lihua Jiang, Yanxin Liu, Min Lin, Jing Sun, Weibo Wang
  • Patent number: 11028085
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.
    Type: Grant
    Filed: September 14, 2020
    Date of Patent: June 8, 2021
    Assignee: Nimbus Saturn, Inc.
    Inventors: Neelu Kaila, Ian Linney, Stuart Ward, Grant Wishart, Ben Whittaker, Alexandre Cote, Jeremy Robert Greenwood, Abba Leffler, Steven K. Albanese, Daniel L. Severance
  • Patent number: 11028081
    Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
    Type: Grant
    Filed: December 30, 2019
    Date of Patent: June 8, 2021
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
  • Patent number: 10988482
    Abstract: The present invention relates to a compound inhibiting the activity of an IRAK4 kinase, a pharmaceutical composition thereof, a use thereof in preparing drugs, a method in which same is used for inhibiting the activity of the IRAK4 kinase and a method in which same is used for treating and/or preventing IRAK4 kinase mediated diseases or conditions in mammals (particularly humans). The compound has a structural formula I.
    Type: Grant
    Filed: August 13, 2015
    Date of Patent: April 27, 2021
    Assignee: BEIJING HANMI PHARMACEUTICAL CO., LTD.
    Inventors: Baoyu Xue, Runa Zheng, Mi Young Cha, Maengsup Kim
  • Patent number: 10981909
    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: Grant
    Filed: March 9, 2020
    Date of Patent: April 20, 2021
    Assignee: Samumed, LLC
    Inventor: Sunil Kumar Kc
  • Patent number: 10966980
    Abstract: Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing them, and therapeutic uses thereof.
    Type: Grant
    Filed: August 10, 2015
    Date of Patent: April 6, 2021
    Assignee: Pfizer Inc.
    Inventors: Michael L. Vazquez, Neelu Kaila, Jamison B. Tuttle, Patrick Robert Verhoest, Matthew R. Reese, Karen J. Coffman, Tarek Samad, James M. Duerr, Simone Sciabola, Mihir D. Parikh
  • Patent number: 10954253
    Abstract: The present invention provides a 1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one compound having an inhibitory effect on Wee1, and includes an application of the compound in treating various types of tumors.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: March 23, 2021
    Assignee: SHIJIAZHUANG SAGACITY NEW DRUG DEVELOPMENT CO., LTD.
    Inventors: Wenyuan Qian, Chundao Yang, Zhengwei Li, Jie Li, Jian Li, Shuhui Chen
  • Patent number: 10934295
    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: Grant
    Filed: May 5, 2017
    Date of Patent: March 2, 2021
    Assignee: BIOVERSYS AG
    Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Zoltan F. Kanyo, Joseph A. Ippolito
  • Patent number: 10927126
    Abstract: Disclosed herein are thieno[2,3-b:5,4-c?]dipyridin-8-amine and pyrido[4?,3?:4,5]thieno[2,3-c]pyridazin-8-amine compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: February 23, 2021
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Darren W. Engers, Alison R. Gregro, Kayla Temple, Paul K. Spearing, Madeline F. Long, Julie L. Engers
  • Patent number: 10894793
    Abstract: The present invention relates to bicyclic pyridine, pyrazine, and pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3K? inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: June 15, 2017
    Date of Patent: January 19, 2021
    Assignee: Janssen Pharmaceutica NV
    Inventors: Didier Jean-Claude Berthelot, Laurence Anne Mevellec, Patrick Rene Angibaud, Sophie Coupa, Christophe Gabriel Marcel Demestre, Lieven Meerpoel, Guillaume Jean Maurice Mercey, Christophe Meyer, Elisabeth Therese Jeanne Pasquter, Isabelle Noelle Constance Pilatte, Virginie Sophie Poncelet, Olivier Alexis Georges Querolle
  • Patent number: 10875829
    Abstract: The disclosure provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula (I): (I) or an isotope labelled analog thereof, or a pharmaceutically acceptable salt thereof, wherein: each of R1, R2, R3, R6 and R7 represents H or F, R4 represents H or CH3 R5 represents H or C1-C4alkyl, wherein at least two of R1, R2, R3, R6 and R7 represent F, together with at least one pharmaceutically acceptable carrier, excipient and/or diluent.
    Type: Grant
    Filed: November 17, 2017
    Date of Patent: December 29, 2020
    Assignee: INTEGRATIVE RESEARCH LABORATORIES SWEDEN AB
    Inventors: Clas Sonesson, Fredrik Pettersson
  • Patent number: 10857138
    Abstract: Pharmaceutical compositions comprising aztreonam or a pharmaceutically acceptable derivative, and a compound of Formula (I) or a stereoisomer or a pharmaceutically acceptable derivative thereof are disclosed.
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: December 8, 2020
    Assignee: WOCKHARDT LIMITED
    Inventors: Sachin Bhagwat, Snehal Rameshwar Palwe, Prashant Ratnakar Joshi, Hemant Narendra Khande, Kushal Umarkar, Mahesh Vithalbhai Patel
  • Patent number: 10844049
    Abstract: The invention described herein provides compounds of Formula (I) and pharmaceutical compositions thereof, for use in, e.g. treating type 2 diabetes mellitus, pre-diabetes, obesity, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and cardiovascular disease.
    Type: Grant
    Filed: May 15, 2020
    Date of Patent: November 24, 2020
    Assignee: QILU REGOR THERAPEUTICS INC.
    Inventor: Wenge Zhong
  • Patent number: 10844051
    Abstract: There are provided compounds, their preparation and their use in the treatment of medical conditions including cancers and immune disorders.
    Type: Grant
    Filed: July 22, 2016
    Date of Patent: November 24, 2020
    Inventors: Jian Hui Wu, Xiaohong Tian, Qianhui Yi
  • Patent number: 10806726
    Abstract: This disclosure features the use of one or more indazole-3-carboxamide compounds or salts or analogs thereof, in the treatment of one or more diseases or conditions independently selected from the group consisting of a tendinopathy, dermatitis, psoriasis, morphea, ichthyosis, Raynaud's syndrome, and Darier's disease; and/or for promoting wound healing. The methods include administering to a subject (e.g., a subject in need thereof) a therapeutically effective amount of one or more indazole-3-carboxamide compounds or salts or analogs thereof as described anywhere herein.
    Type: Grant
    Filed: October 23, 2017
    Date of Patent: October 20, 2020
    Assignee: Samumed, LLC
    Inventors: Vishal Deshmukh, Eric Anthony Murphy, John Hood
  • Patent number: 10807966
    Abstract: The present invention is directed to certain amides and heterocyclic compounds. The present invention also relates to uses of these compounds to treat several diseases including autoimmune disorders, cardiovascular disorders, inflammation, central nervous system disorders, arterial thrombotic disorders, fibrotic disorders, glaucoma, and neoplastic disorders.
    Type: Grant
    Filed: November 20, 2017
    Date of Patent: October 20, 2020
    Assignee: Translational Drug Development, LLC
    Inventors: Tong Wang, Stephen Gately
  • Patent number: 10758523
    Abstract: Provided are single-dose, ready-to-use formulations and methods for preparing the formulations that include a compound of Formula (I) including pharmaceutically acceptable salts and amorphous and polymorph forms thereof.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: September 1, 2020
    Assignee: Samumed, LLC
    Inventor: Luis A. Dellamary
  • Patent number: 10738041
    Abstract: The invention relates to novel ferroportin inhibitors of the general formula (I) pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for the prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, such as particularly iron overload states such as in particular thalassemia and hemochromatosis.
    Type: Grant
    Filed: October 21, 2016
    Date of Patent: August 11, 2020
    Assignee: Vifor (International) AG
    Inventors: Franz Dürrenberger, Wilm Buhr, Susanna Burckhardt, Michael Burgert, Aris Kalogerakis, Stefan Reim, Vania Manolova, Susan Boyce, Christopher John Yarnold, Paula Pena, Jon Shepherd, Cristina Lecci, Richard Jarjes-Pike, John Scott
  • Patent number: 10702526
    Abstract: The present disclosure relates to the use MNK-specific inhibitors to inhibit immunosuppression components, such as immune checkpoint proteins PD-1, PD-L1, LAG3, and/or immunosuppressive cytokines, such as IL-10, in order to inhibit or release immune suppression in certain diseases, such as cancer and infectious disease.
    Type: Grant
    Filed: April 15, 2016
    Date of Patent: July 7, 2020
    Assignee: eFFECTOR Therapeutics Inc.
    Inventors: Kevin R. Webster, Vikas Goel
  • Patent number: 10689377
    Abstract: The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
    Type: Grant
    Filed: November 14, 2018
    Date of Patent: June 23, 2020
    Assignees: Mirati Therapeutics, Inc., Array Biopharma Inc.
    Inventors: James F. Blake, Laurence E. Burgess, Mark Joseph Chicarelli, James Gail Christensen, Adam Cook, Jay Bradford Fell, John P. Fischer, Matthew Arnold Marx, Macedonio J. Mejia, Pavel Savechenkov, Guy P. A. Vigers, Christopher Ronald Smith, Martha E. Rodriguez
  • Patent number: 10682413
    Abstract: The present invention relates to a pharmaceutical composition and a lyophilisate of a diazabicyclooctane derivative represented by Compound I, a process for producing the same and methods for using the same.
    Type: Grant
    Filed: September 25, 2018
    Date of Patent: June 16, 2020
    Assignees: FEDORA PHARMACEUTICALS INC., MEIJI SEIKA PHARMA CO., LTD.
    Inventor: Kewei Yang
  • Patent number: 10668077
    Abstract: The invention relates to a pharmaceutical composition comprising a combination of a compound of formula (I) or a pharmaceutically acceptable salt thereof, and at least one second agent selected from the group consisting of signal transduction pathway inhibitors, tumour immunotherapeutics, agents inhibiting the BCL2 family of proteins, agents inhibiting Mcl-1, proteasome Inhibitors, poly (ADP-ribose) polymerase (PARP) Inhibitors, aromatase inhibitors, conventional cytotoxic agents or a miscellaneous agent selected from abiraterone, ARN-509 and MYC inhibitors.
    Type: Grant
    Filed: August 19, 2016
    Date of Patent: June 2, 2020
    Assignee: Karus Therapeutics Limited
    Inventors: Stephen Joseph Shuttleworth, Andrew David Whale
  • Patent number: 10647715
    Abstract: The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
    Type: Grant
    Filed: May 14, 2019
    Date of Patent: May 12, 2020
    Assignees: MIRATI THERAPEUTICS, INC., ARRAY BIOPHARMA INC.
    Inventors: Matthew Arnold Marx, Thomas P. Bobinski, Aaron Craig Burns, John Gaudino, Julia Haas, John Michael Ketcham, John David Lawson, Brad Newhouse, Spencer Pajk, Christopher Ronald Smith, Tony P. Tang
  • Patent number: 10633380
    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: Grant
    Filed: August 28, 2018
    Date of Patent: April 28, 2020
    Assignee: Samumed, LLC
    Inventor: Sunil Kumar KC
  • Patent number: 10633386
    Abstract: The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein B, R1, R5, Q1, Q?, L, X, Y, and Z are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains such as cancer.
    Type: Grant
    Filed: April 6, 2017
    Date of Patent: April 28, 2020
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Bing Zhou, Fuming Xu, Jiantao Hu, Longchuan Bai, Chao-Yie Yang
  • Patent number: 10610520
    Abstract: The present invention provides a compound having an MAGL inhibitory action, and useful as an agent for the prophylaxis or treatment of neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, traumatic brain injury, glaucoma, multiple sclerosis etc.), anxiety disorder, pains (e.g., inflammatory pain, cancerous pain, neurogenic pain etc.), epilepsy, depression and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: March 30, 2017
    Date of Patent: April 7, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shuhei Ikeda, Hideyuki Sugiyama, Jumpei Aida, Hidekazu Tokuhara, Tomohiro Okawa, Yuya Oguro, Minoru Nakamura, Masataka Murakami
  • Patent number: 10603322
    Abstract: The invention provides a method of inhibiting casein kinase 1? (CK1?), comprising contacting the CK1? with a compound of formula (I), as defined herein; such as compound SR-3029. We demonstrate that CSNK1D is amplified and/or overexpressed in human breast tumors and that CK1? can be medically targeted in human breast cancer subtypes overexpressing this kinase. The invention further provides a method of treating cancer, such as a breast cancer, melanoma, glioblastoma, medulloblastoma, renal, bladder or colon cancer, or a cancer that metastasizes to the brain, lung, or bone provided that both elevated CK1? and ?-catenin dependence are involved in those metastatic diseases. The cancer can be a breast cancer of the triple negative subclass of breast cancers (TNBC), or can be an HER+ breast cancer.
    Type: Grant
    Filed: October 5, 2016
    Date of Patent: March 31, 2020
    Assignee: The Scripps Research Institute
    Inventors: William R. Roush, Derek R. Duckett, John L. Cleveland, Laura H. Rosenberg
  • Patent number: 10604522
    Abstract: A process for producing a compound of the following Formula (VII-CR): The process involving providing a compound represented by the following Formula (VI): in a case where the R3ONHC(?O) side chain in the compound of the Formula (VI) has a protecting group, removing the protecting group from the compound of the Formula (VI) with an acid, and adding an ester-based poor solvent to the resultant reaction solution to precipitate the compound of Formula (VII-CR), wherein in the compounds of the Formulas (VII-CR) and (VI), R3 is a C1-6 alkyl or a heterocycle.
    Type: Grant
    Filed: October 1, 2018
    Date of Patent: March 31, 2020
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Takao Abe, Takeshi Furuuchi, Yoshiaki Sakamaki, Nakako Mitsuhashi, Yumiko Saito
  • Patent number: 10604502
    Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for the treatment of lysine (K)-specific demethylase 1A (LSD1)-mediated diseases or disorders: wherein R1, R2, R3, R4, and R5 are as defined herein.
    Type: Grant
    Filed: June 19, 2018
    Date of Patent: March 31, 2020
    Assignee: Novartis AG
    Inventors: Lei Du-Cuny, Qitao Xiao, Guoliang Xun, Qiangang Zheng
  • Patent number: 10584123
    Abstract: The present invention relates to a process for producing crystalline and amorphous forms of a diazabicyclooctane derivative represented by Compound (I) and methods for producing the same.
    Type: Grant
    Filed: September 25, 2018
    Date of Patent: March 10, 2020
    Assignees: FEDORA PHARMACEUTICALS INC., MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Michael Kammerer, Frédéric Ran
  • Patent number: 10561651
    Abstract: Methods of treating neuroblastoma associated with a deregulated protein kinase activity are disclosed. The treatment may include administration of substituted indazole derivatives of formula (I) or formula 2.(I) and pharmaceutically acceptable salts therefor, as degined in the specification.
    Type: Grant
    Filed: July 31, 2018
    Date of Patent: February 18, 2020
    Assignees: IGNYTA, INC., NERVIANO MEDICAL SCIENCES, S.R.L.
    Inventors: Jonathan Lim, Elena Ardini, Maria Menichincheri
  • Patent number: 10561616
    Abstract: This invention relates to sustained release dosage forms comprising {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof, and doses and methods related thereto.
    Type: Grant
    Filed: May 18, 2017
    Date of Patent: February 18, 2020
    Assignee: Incyte Corporation
    Inventors: Krishnaswamy Yeleswaram, Bhavnish Parikh, Dilip P. Modi, Trupti Sheth
  • Patent number: 10562908
    Abstract: The present invention relates to ortho substituted phenylpyrazolo- and pyrrolo-pyridazine derivatives having dual pharmacological activity towards both the ?2? subunit, in particular the ?2?-1 subunit, of the voltage-gated calcium channel and the ?-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Grant
    Filed: November 30, 2017
    Date of Patent: February 18, 2020
    Assignee: ESTEVE PHARMACEUTICALS, S.A.
    Inventors: Marina Virgili-Bernado, Monica Alonso-Xalma, Carmen Almansa-Rosales
  • Patent number: 10562886
    Abstract: This invention provides, among other things, compounds useful for treating diseases such as cancer, pharmaceutical formulations containing such compounds, as well as combinations of these compounds with at least one additional therapeutic agent.
    Type: Grant
    Filed: May 23, 2016
    Date of Patent: February 18, 2020
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Csaba J. Peto, David Jablons, Hassan Lemjabbar-Alaoui
  • Patent number: 10556891
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Grant
    Filed: May 24, 2018
    Date of Patent: February 11, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
  • Patent number: 10544146
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1 ,R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Grant
    Filed: June 28, 2018
    Date of Patent: January 28, 2020
    Assignee: FEDORA PHARMACEUTICALS INC.
    Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
  • Patent number: 10526346
    Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Grant
    Filed: January 3, 2018
    Date of Patent: January 7, 2020
    Assignee: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
  • Patent number: 10519155
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Grant
    Filed: February 17, 2018
    Date of Patent: December 31, 2019
    Assignee: WOCKHARDT LIMITED
    Inventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Bharat Dond, Amol Kale, Loganathan Velupillai, Deepak Dekhane, Satish Shrimant Birajdar, Mohammad Usman Shaikh, Sushilkumar Maurya, Piyush Ambalal Patel, Prasad Dixit, Mangesh Pawar, Mahesh Vithalbhai Patel, Sachin Bhagwat
  • Patent number: 10493078
    Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions associated with a PTEN deficiency that are ameliorated by the inhibition of PARP activity.
    Type: Grant
    Filed: August 3, 2018
    Date of Patent: December 3, 2019
    Assignee: Medivation Technologies LLC
    Inventors: Daniel Chu, Bing Wang, Ying Feng, Yuqiao Shen, Leonard E. Post
  • Patent number: 10494364
    Abstract: The invention relates to capthepsin K inhibitors and uses thereof, specifically relates to a class of compounds having the formula (I) which are used for treating or preventing cathepsin dependent diseases or conditions, specifically, wherein the cathepsin is capthepsin K. The compounds and compositions thereof can be used as bone resorption inhibitors for the treatment of associated diseases.
    Type: Grant
    Filed: August 26, 2016
    Date of Patent: December 3, 2019
    Assignees: SUNSHIN LAKE PHARMA CO., LTD, NORTH & SOUTH BROTHER PHARMACY INVESTMENT COMPANY LIMITED
    Inventors: Xiaojun Wang, Pingjian Zhou, Chuanwen Yang, Changwei Huang, Shaohui Xiong, Yingjun Zhang, Jiancun Zhang