The Shared Ring Nitrogen Is Bonded Directly To A Ring Nitrogen Of The Second Ring Of The Bicyclo Ring System (e.g., Pyrazolo[1,5-a]pyrimidine, Etc.) Patents (Class 514/259.3)
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Patent number: 12116369Abstract: The invention provides substituted pyrazolo[1,5-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrazolo[1,5-a]pyrimidinyl carboxamide compounds described herein include 2-heterocyclyl-4-alkyl-pyrazolo[1,5-a]pyrimidine-3-carboxamide compounds and variants thereof. The invention provides, in part, a compound of Formula (IV): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined herein.Type: GrantFiled: October 25, 2021Date of Patent: October 15, 2024Assignee: Bial—R&D Investments, S.A.Inventors: Renato T. Skerlj, Elyse Marie Josee Bourque, Peter T. Lansbury, Andrew C. Good
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Patent number: 12060356Abstract: The present invention provides a compound of Formula (I) wherein R is (II) or (III); or a pharmaceutically acceptable salt thereof, useful for treating psoriasis or systemic lupus erythematosus.Type: GrantFiled: December 4, 2019Date of Patent: August 13, 2024Assignee: Eli Lilly and CompanyInventors: Zhaogen Chen, Theodore Curtis Jessop
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Patent number: 12006321Abstract: Provided herein are agonists of the apelin receptor of Formula (I): for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions.Type: GrantFiled: May 12, 2022Date of Patent: June 11, 2024Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTEInventors: Layton H. Smith, Anthony B. Pinkerton, Paul Hershberger, Patrick Maloney, Danielle McAnally
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Patent number: 11891400Abstract: The present invention provides a compound of Formula I: wherein R is methyl or ethyl; or a pharmaceutically acceptable salt thereof useful for treating psoriasis or systemic lupus erythematosus.Type: GrantFiled: September 4, 2019Date of Patent: February 6, 2024Assignee: Eli Lilly and CompanyInventors: Zhaogen Chen, Jon Andre Erickson, Gaiying Zhao
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Patent number: 11884676Abstract: Disclosed herein are analogues of 6-(4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)oxy)piperidin-1 -yl)-[1,2,4]triazolo[4,3-b]pyridazine of formula (Ib), 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: GrantFiled: March 22, 2023Date of Patent: January 30, 2024Assignee: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Darren W. Engers, Alison R. Gregro, Kayla J. Temple, Madeline F. Long, Anna E. Ringuette, Logan A. Baker, Thomas Jensen
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Patent number: 11845754Abstract: Inhibitors of CDK9 that are pyrazolo[1,5-a]pyrimidine derivatives and salts thereof, corresponding to formula (I):Type: GrantFiled: September 15, 2021Date of Patent: December 19, 2023Assignee: Kronos Bio, Inc.Inventors: Peter Mikochik, Joseph Vacca, David Freeman, Andrew S. Tasker
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Patent number: 11753411Abstract: Described herein are TYK2 pseudokinase ligands of Formula (I?), methods of utilizing these TYK2 pseudokinase ligands in the treatment of diseases, disorders or conditions, and pharmaceutical compositions containing such compounds: wherein X, Y, L1, R1, R2, R3, R4, R5, R6, and R8 are defined in the specification.Type: GrantFiled: November 5, 2020Date of Patent: September 12, 2023Assignee: VENTYX BIOSCIENCES, INC.Inventors: Raju Mohan, John Nuss, Jason Harris, Shendong Yuan
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Patent number: 11708369Abstract: The invention concerns compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment of respiratory syncytial virus infection.Type: GrantFiled: April 19, 2019Date of Patent: July 25, 2023Assignee: Janssen Sciences Ireland Unlimited CompanyInventors: David Francis Alain Lançois, Jérome Émile Georges Guillemont, Pierre Jean-Marie Bernard Raboisson, Peter Rigaux, Antoine Benjamin Michaut, Sabrina Dany France Quatrevaux, Sovy Chao, Dirk André Emmy Roymans
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Patent number: 11691977Abstract: The invention relates to Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide of general formula (I) which are inhibitors of phosphodiesterase 2, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.Type: GrantFiled: October 20, 2020Date of Patent: July 4, 2023Assignee: Boehringer Ingelheim International GmbHInventors: Christoph Hoenke, Barbara Bertani, Marco Ferrara, Giacomo Fossati, Sara Frattini, Riccardo Giovannini, Scott Hobson
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Patent number: 11649238Abstract: The invention relates to compounds of formula (I) which are inhibitors of kinase activity, pharmaceutical formulations containing the compounds and their uses in treating and preventing viral infections and disorders caused or exacerbated by the viral infection wherein R1, R2, R3, R4a, R4b, R4c, R5, W, X, Y and Z are defined herein.Type: GrantFiled: January 15, 2019Date of Patent: May 16, 2023Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITEDInventors: Nicholas Paul Barton, Sophie Marie Bertrand, Kenneth David Down, Matthew Gray
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Patent number: 11634423Abstract: The present invention provides a compound of Formula I: wherein R is or a pharmaceutically acceptable salt thereof, useful for treating psoriasis, systemic lupus erythematosus, or type 1 diabetes.Type: GrantFiled: February 5, 2021Date of Patent: April 25, 2023Assignee: Eli Lilly and CompanyInventors: Thomas John Bleisch, Zhaogen Chen, Theodore Curtis Jessop
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Patent number: 11453671Abstract: 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: GrantFiled: June 16, 2020Date of Patent: September 27, 2022Assignee: Genentech, Inc.Inventors: Mark Edward Zak, Naomi S. Rajapaksa, Yun-Xing Cheng, Jessica Grandner, Daniel G. M. Shore, Marian C. Bryan
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Patent number: 11414431Abstract: The present invention provides compounds of Formula I?: compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.Type: GrantFiled: October 15, 2019Date of Patent: August 16, 2022Assignee: Nimbus Lakshmi, Inc.Inventors: Craig E. Masse, Jeremy Robert Greenwood, Sayan Mondal
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Patent number: 11369612Abstract: The present invention is directed to the combination of the RSV inhibiting Compound A, i.e. 3-({5-chloro-1-[3-(methylsulfonyl)propyl]-1H-indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-imidazo[4,5-c]pyridin-2-one, and the RSV inhibiting Compound B, i.e. (1S,2S)-2-[4-[7-cyclopropyl-5-[(1R)-1-methyl-3,4-dihydro-1H-isoquinoline-2-carbonyl]pyrazolo[1,5-a]pyrimidin-2-yl]-3-fluoro-phenyl]cyclopropanecarboxylic acid for treating or ameliorating RSV infection. The invention further relates to the combination product of Compound A and Compound B, a pharmaceutical product comprising Compound A and Compound B, the use of the combination of Compound A and Compound B—or the pharmaceutical product comprising Compound A and Compound B—for the treatment of RSV infection, and a method of treating or ameliorating RSV infection in a subject in need thereof comprising administering the combination of Compound A and Compound B in an effective amount to said subject.Type: GrantFiled: December 4, 2018Date of Patent: June 28, 2022Assignee: Janssen Sciences Ireland Unlimited CompanyInventors: Nina Ysebaert, Nele Isa E. Goeyvaerts, Dirk André Emmy Roymans, Anil Koul
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Patent number: 11345705Abstract: Provided herein are agonists of the apelin receptor of Formula (I): for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions.Type: GrantFiled: August 8, 2018Date of Patent: May 31, 2022Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTEInventors: Layton H. Smith, Anthony B. Pinkerton, Paul Hershberger, Patrick Maloney, Danielle McAnally
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Patent number: 11339164Abstract: Salts and solid state forms of Larotrectinib, processes for preparation thereof, pharmaceutical compositions thereof, and uses thereof are disclosed.Type: GrantFiled: October 31, 2018Date of Patent: May 24, 2022Assignee: ASSIA CHEMICAL INDUSTRIES LTD.Inventors: Sharona Shachan-Tov, Doron Rudik, Oshrat Frenkel, Rotem Sella-Erez, Maytal Piran, Ido Fuchs
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Patent number: 11312720Abstract: A salt of the compound represented by formula (1) and crystals thereof having the potential to be used as drug substances for pharmaceutical products.Type: GrantFiled: February 22, 2019Date of Patent: April 26, 2022Assignee: Eisai R&D Management Co., Ltd.Inventor: Taro Yamashita
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Patent number: 11306066Abstract: The present disclosure relates generally, but not exclusively, to compounds and their use in therapy, to compositions and agents comprising said compounds, to methods of treatment using said compounds, and their use in the manufacture of medicaments. The disclosure further relates to inhibitors of IRAP and their use in the treatment or prevention of Alzheimer's disease and the treatment and prevention of memory and cognitive disorders.Type: GrantFiled: May 6, 2016Date of Patent: April 19, 2022Assignee: Monash UniversityInventors: Siew Yeen Chai, Philip Thompson, Simon Mountford, Michael W. Parker
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Patent number: 11192892Abstract: The invention provides substituted pyrazolo[1,5-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrazolo[1,5-a]pyrimidinyl carboxamide compounds described herein include 2-heterocyclyl-4-alkyl-pyrazolo[1,5-a]pyrimidine-3-carboxamide compounds and variants thereof. The invention provides, in part, a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined herein.Type: GrantFiled: April 6, 2017Date of Patent: December 7, 2021Assignee: Bial—R&D Investments, S.A.Inventors: Renato T. Skerlj, Elyse Marie Josee Bourque, Peter T. Lansbury, Andrew C. Good
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Patent number: 11155560Abstract: Inhibitors of CDK9 that are pyrazolo[1,5-a]pyrimidine derivatives and salts thereof, corresponding to formula (I):Type: GrantFiled: October 29, 2019Date of Patent: October 26, 2021Assignee: kronos bio, inc.Inventors: Peter Mikochik, Joseph Vacca, David Freeman, Andrew S. Tasker
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Patent number: 11142528Abstract: The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.Type: GrantFiled: January 10, 2020Date of Patent: October 12, 2021Assignee: BEIGENE SWITZERLAND GMBHInventors: Zhiwei Wang, Yunhang Guo
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Patent number: 11046698Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.Type: GrantFiled: July 26, 2018Date of Patent: June 29, 2021Assignee: Nimbus Lakshmi, Inc.Inventors: Craig E. Masse, Jeremy Robert Greenwood, Sayan Mondal, Scott D. Cowen, Thomas H. McLean
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Patent number: 10960007Abstract: The present invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention also relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention also provides a method for manufacture of medicaments useful in the treatment of such disorders.Type: GrantFiled: March 12, 2018Date of Patent: March 30, 2021Assignee: RICHTER GEDEON NYRT.Inventors: István Borza, Viktor Román, János Éles, Zsuzsa Hadady, József Huszár
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Patent number: 10953012Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: GrantFiled: April 26, 2012Date of Patent: March 23, 2021Assignee: BioEnergenix LLCInventors: John M. McCall, Robert C. Kelly, Donna L. Romero
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Patent number: 10941162Abstract: Trisubstituted bicyclic heterocyclic compounds (e.g., pyridopyrimidinones) and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: GrantFiled: March 1, 2019Date of Patent: March 9, 2021Assignee: Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. Castro, Catherine A. Evans, Martin R. Tremblay
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Patent number: 10934298Abstract: The invention provides substituted pyrazolo[1,5-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrazolo[1,5-a]pyrimidinyl carboxamide compounds described herein include 2-heterocyclyl-4-alkyl-pyrazolo[1,5-a]pyrimidine-3-carboxamide compounds and variants thereof. The invention provides, in part, a compound of formula (I-A): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined herein.Type: GrantFiled: March 18, 2019Date of Patent: March 2, 2021Assignee: Bial—Biotech Investments, Inc.Inventors: Renato T. Skerlj, Elyse Marie Josee Bourque, Peter T. Lansbury
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Patent number: 10875867Abstract: The invention relates to Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide of general formula (I) which are inhibitors of phosphodiesterase 2, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.Type: GrantFiled: October 14, 2019Date of Patent: December 29, 2020Assignee: Boehringer Ingelheim International GmbHInventors: Christoph Hoenke, Barbara Bertani, Marco Ferrara, Giacomo Fossati, Sara Frattini, Riccardo Giovannini, Scott Hobson
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Patent number: 10849902Abstract: The present invention provides a medicament for preventing or treating heart failure. More specifically, the present invention provides a medicament for preventing or treating heart failure, comprising a compound selected from the group consisting of (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-methoxyphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-5-(2-fluorophenyl)-2,7,7-trimethyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and salts thereof.Type: GrantFiled: December 21, 2016Date of Patent: December 1, 2020Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Takahisa Matsuda, Takashi Motoyaji, Shuji Kitamura, Masato Yoshida
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Patent number: 10813936Abstract: A novel crystalline form of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.Type: GrantFiled: March 27, 2019Date of Patent: October 27, 2020Assignee: Array BioPharma, Inc.Inventors: Alisha B. Arrigo, Derrick Juengst, Khalid Shah
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Patent number: 10799505Abstract: A novel crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.Type: GrantFiled: November 16, 2015Date of Patent: October 13, 2020Assignee: Array BioPharma, Inc.Inventors: Alisha B. Arrigo, Derrick Juengst, Khalid Shah
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Patent number: 10786506Abstract: The present invention provides a medicament for preventing or treating heart failure. More specifically, the present invention provides a medicament for preventing or treating heart failure, comprising a compound selected from the group consisting of (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-methoxyphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-5-(2-fluorophenyl)-2,7,7-trimethyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and salts thereof.Type: GrantFiled: December 21, 2016Date of Patent: September 29, 2020Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Takahisa Matsuda, Takashi Motoyaji, Shuji Kitamura, Masato Yoshida
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Patent number: 10781218Abstract: The present disclosure provides compounds of Formula (II-A), which inhibit the interaction of menin with one or more of MLL1, MLL2 and MLL-fusion oncoproteins. Also disclosed are methods for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.Type: GrantFiled: March 15, 2017Date of Patent: September 22, 2020Assignees: KURA ONCOLOGY, INC., THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Tao Wu, Liansheng Li, Yi Wang, Pingda Ren, Jolanta Grembecka, Tomasz Cierpicki, Szymon Klossowski, Jonathan Pollock, Dmitry Borkin
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Patent number: 10774085Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.Type: GrantFiled: July 25, 2018Date of Patent: September 15, 2020Assignee: ARRAY BIOPHARMA INC.Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
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Patent number: 10758542Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.Type: GrantFiled: April 8, 2019Date of Patent: September 1, 2020Assignee: Array BioPharma Inc.Inventors: Shelley Allen, Steven W. Andrews, Kevin Ronald Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Kercher, Jeongbeob Seo
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Patent number: 10759806Abstract: Provided are isotopologues of isoquinolinone and quinazolinone compounds of formula (AB?) that modulate PI3 kinase activity, processes for the preparation of the compounds, pharmaceutical compositions comprising the compounds, and methods of treatment of diseases and disorders using the compounds or pharmaceutical compositions.Type: GrantFiled: March 16, 2017Date of Patent: September 1, 2020Assignee: Infinity Pharmaceuticals, Inc.Inventor: Catherine A. Evans
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Patent number: 10584128Abstract: Bicyclic dihydropyrimidine-carboxamide compounds of formula I described herein inhibit Rho Kinase and may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF), and pulmonary arterial hypertension (PAH).Type: GrantFiled: December 21, 2017Date of Patent: March 10, 2020Assignee: CHIESI FARMACEUTICI S.p.A.Inventors: Alessandro Accetta, Fabio Rancati, Anna Maria Capelli, David Edward Clark, Patrizia Tisselli, Christine Edwards, Gurdip Bhalay
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Patent number: 10479794Abstract: The invention relates to Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide of general formula (I) which are inhibitors of phosphodiesterase 2, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.Type: GrantFiled: January 9, 2018Date of Patent: November 19, 2019Assignee: Boehringer Ingelheim International GmbHInventors: Christoph Hoenke, Barbara Bertani, Marco Ferrara, Giacomo Fossati, Sara Frattini, Riccardo Giovannini, Scott Hobson
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Patent number: 10329294Abstract: The present invention relates to pyrazolopyrimidine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.Type: GrantFiled: March 7, 2016Date of Patent: June 25, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Jongwon Lim, Michael D. Altman, Jason D. Brubaker, Craig R. Gibeau
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Patent number: 10285993Abstract: A novel crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.Type: GrantFiled: September 15, 2017Date of Patent: May 14, 2019Assignee: Array BioPharma Inc.Inventors: Alisha B. Arrigo, Derrick Juengst, Khalid Shah
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Patent number: 10251889Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.Type: GrantFiled: October 4, 2017Date of Patent: April 9, 2019Assignee: Array BioPharm Inc.Inventors: Shelley Allen, Steven W. Andrews, Kevin Ronald Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Kercher, Jeongbeob Seo
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Patent number: 10239882Abstract: The invention provides a chemical entity of Formula (I): (I), wherein R1, R2, R3, and R4, have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by PDE2 activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including hematological, cardiovascular, gastroenterological, and dermatological disorders.Type: GrantFiled: November 3, 2015Date of Patent: March 26, 2019Assignee: DART NEUROSCIENCE (CAYMAN) LTD.Inventors: Amy Lynn Allan, James Breitenbucher, Laurent Gomez, Terence Patrick Keenan, Robert Lemus, Kiev Ly, Tami Jo Marrone
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Patent number: 10172861Abstract: A novel crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.Type: GrantFiled: January 16, 2018Date of Patent: January 8, 2019Assignee: Array BioPharma Inc.Inventors: Alisha B. Arrigo, Derrick Juengst, Khalid Shah
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Patent number: 10118930Abstract: The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.Type: GrantFiled: October 30, 2015Date of Patent: November 6, 2018Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Manuel Ellermann, Gaelle Valot, Yolanda Cancho Grande, Jorma Haßfeld, Tom Kinzel, Johannes Köbberling, Kristin Beyer, Susanne Röhrig, Michael Sperzel, Jan Stampfuß, Imke Meyer, Maria Köllnberger, Nils Burkhardt, Karl-Heinz Schlemmer, Christian Stegmann, Joachim Schuhmacher, Matthias Werner, Jörg Heiermann, Willem Jan Hengeveld
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Patent number: 10072000Abstract: The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R1, X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.Type: GrantFiled: August 13, 2013Date of Patent: September 11, 2018Assignee: FERRER INTERNACIONAL, S.A.Inventors: Luis Anglada, Albert Palomer, Antonio Guglietta
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Patent number: 10005783Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.Type: GrantFiled: January 5, 2017Date of Patent: June 26, 2018Assignee: Array BioPharma Inc.Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
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Patent number: 9963455Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof, useful in therapy, in particular in the treatment of a viral infection.Type: GrantFiled: January 21, 2015Date of Patent: May 8, 2018Assignee: Curovir ABInventor: Jacob Westman
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Patent number: 9862707Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.Type: GrantFiled: March 23, 2015Date of Patent: January 9, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Helen Mitchell, Harold B. Wood, Chun Sing Li, Qinghua Mao, Zhiqi Qi
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Patent number: 9845327Abstract: The present disclosure provides technologies relating to lysosomal activation. The disclosure provides several strategies for increasing level and/or activity of lysosomal enzyme, and furthermore demonstrates the surprising applicability of such strategies in the treatment and/or prophylaxis of certain proteinopathies. Among other things, the present invention provides methods and compositions for the treatment and/or prophylaxis of proteinopathies other than lysosomal storage diseases through lysosomal activation. In particular, the present disclosure provides methods and compositions for the treatment and/or prophylaxis of neurodegenerative proteinopathies, and in particular those associated with accumulation of ?-synuclein. The present disclosure specifically provides methods and compositions for the treatment and/or prophylaxis of Parkinson's disease.Type: GrantFiled: June 22, 2012Date of Patent: December 19, 2017Assignee: THE GENERAL HOSPITAL CORPORATIONInventors: Dmitri Krainc, Joseph R. Mazzulli
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Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
Patent number: 9840510Abstract: The invention provides substituted pyrazolo[1,5-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrazolo[1,5-a]pyrimidinyl carboxamide compounds described herein include 2-heterocyclyl-4-alkyl-pyrazolo[1,5-a]pyrimidine-3-carboxamide compounds and variants thereof.Type: GrantFiled: August 16, 2017Date of Patent: December 12, 2017Assignee: LYSOSOMAL THERAPEUTICS INC.Inventors: Renato T. Skerlj, Elyse Marie Josee Bourque, Peter T. Lansbury -
Patent number: 9796724Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.Type: GrantFiled: January 9, 2017Date of Patent: October 24, 2017Assignee: Array BioPharma, Inc.Inventors: Shelley Allen, Steven W. Andrews, Kevin Ronald Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Kercher, Jeongbeob Seo