Patents Assigned to PRINCIPIA BIOPHARMA, INC.
  • Patent number: 10899760
    Abstract: Disclosed herein are processes for preparing 8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one and FGFR inhibitor, as well as polymorphs and/or salt forms thereof.
    Type: Grant
    Filed: January 17, 2020
    Date of Patent: January 26, 2021
    Assignee: PRINCIPIA BIOPHARMA, INC.
    Inventors: Jiang Zhu, Mohammad Masjedizadeh
  • Publication number: 20210015821
    Abstract: Disclosed herein are processes for preparing 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile free base (compound (I)), salts of compound (I) and solid state form of said salts. Also disclosed herein are pharmaceutical compositions comprising such salts and solid state form thereof and methods of treating cancer, autoimmune, and inflammatory diseases using compound (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 5, 2020
    Publication date: January 21, 2021
    Applicant: PRINCIPIA BIOPHARMA INC.
    Inventors: Mohammad Reza MASJEDIZADEH, Steven Gourlay
  • Patent number: 10828307
    Abstract: Disclosed herein are processes for preparing 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile free base (compound (I)), salts of compound (I) and solid state form of said salts. Also disclosed herein are pharmaceutical compositions comprising such salts and solid state form thereof and methods of treating cancer, autoimmune, and inflammatory diseases using compound (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 8, 2019
    Date of Patent: November 10, 2020
    Assignee: Principia Biopharma Inc.
    Inventors: Mohammad Reza Masjedizadeh, Steven Gourlay
  • Publication number: 20200190092
    Abstract: The present disclosure provides compounds of Formula (IA) and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: December 9, 2019
    Publication date: June 18, 2020
    Applicant: PRINCIPIA BIOPHARMA INC.
    Inventors: Tim OWENS, Erik VERNER
  • Patent number: 10654843
    Abstract: The present disclosure provides compounds that are Large Multifunctional Protease 7 (LMP7) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of LMP7. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: June 18, 2015
    Date of Patent: May 19, 2020
    Assignee: Principia Biopharma Inc.
    Inventors: Timothy Owens, Kenneth Albert Brameld
  • Publication number: 20200101059
    Abstract: The present disclosure provides provides methods of treating with a BTK inhibitor a blistering disease, in particular pemphigus vulgaris or pemphigus folliaceous in a mammal, use of a BTK inhibitor as a replacement therapy for corticosteroid therapy for diseases treatable with a corticosteroid, such as autoimmune or inflammatory disease and in particular where corticosteroids are used as first or second line therapy, and pharmaceutical formulations comprising the same.
    Type: Application
    Filed: October 4, 2019
    Publication date: April 2, 2020
    Applicant: Principia Biopharma Inc.
    Inventor: Steven GOURLAY
  • Publication number: 20200038405
    Abstract: Disclosed herein are processes for preparing 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile free base (compound (I)), salts of compound (I) and solid state form of said salts. Also disclosed herein are pharmaceutical compositions comprising such salts and solid state form thereof and methods of treating cancer, autoimmune, and inflammatory diseases using compound (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 8, 2019
    Publication date: February 6, 2020
    Applicant: PRINCIPIA BIOPHARMA INC.
    Inventors: Mohammad Reza MASJEDIZADEH, Steven GOURLAY
  • Patent number: 10538518
    Abstract: To an appropriate reactor equipped with mechanical stirrer was charged acetic acid (12 L), tert-butyl 4-(3-(6-(3,5-dimethoxyphenyl)-2-(methylthio)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl)propyl)piperazine-1-carboxylate (2000 g) and triethylamine (639 g, 2.3 eq.). Internal temperature was adjusted to approximately 20° C. and N-chlorosuccinimide (1651 g, 4.5 eq.) was added at 20-30° C. Reaction was stirred for 2 hours. Ethyl acetate (30 L) was added. 5% aqueous NaCl solution (20 L) was added. The organic layer was separated and the aqueous layer was extracted with EtOAc. The combined organic layers were washed with 30% aqueous potassium carbonate solution (14 L). The organic layer was concentrated to ˜12 L and used for next step directly.
    Type: Grant
    Filed: August 10, 2016
    Date of Patent: January 21, 2020
    Assignee: Principia Biopharma, Inc.
    Inventors: Jiang Zhu, Mohammad Masjedizadeh
  • Patent number: 10538517
    Abstract: Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: May 18, 2016
    Date of Patent: January 21, 2020
    Assignee: Principia Biopharma, Inc.
    Inventors: Kenneth Albert Brameld, Erik Verner
  • Patent number: 10533013
    Abstract: The present disclosure provides compounds of Formula (IA), such as, e.g., (R)-2-(3-(4-amino-3-(2-fluoro-4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carbonyl)-4-methyl-4-(4-(oxetan-3-yl)piperazin-1-yl)pent-2-enenitrile having the chemical structure ?and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK inhibitors, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 11, 2018
    Date of Patent: January 14, 2020
    Assignee: Principia Biopharma Inc.
    Inventors: Tim Owens, Erik Verner
  • Patent number: 10485797
    Abstract: The present disclosure provides methods of treating with a BTK inhibitor a blistering disease, in particular pemphigus vulgaris or pemphigus folliaceous in a mammal, use of a BTK inhibitor as a replacement therapy for corticosteroid therapy for diseases treatable with a corticosteroid, such as autoimmune or inflammatory disease and in particular where corticosteroids are used as first or second line therapy, and pharmaceutical formulations comprising the same.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: November 26, 2019
    Assignee: PRINCIPIA BIOPHARMA INC.
    Inventor: Steven Gourlay
  • Publication number: 20190345159
    Abstract: The present disclosure provides compounds of formula (I) that are tyrosine kinase inhibitors, in particular Bruton tyrosine kinase (“BTK”) inhibitors, and are therefore useful for the treatment of diseases treatable by inhibition of BTK such as cancer, autoimmune, inflammatory, and thromboembolic diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Application
    Filed: July 26, 2019
    Publication date: November 14, 2019
    Applicant: Principia Biopharma Inc.
    Inventors: David M. GOLDSTEIN, Timothy D. OWENS
  • Patent number: 10456403
    Abstract: Disclosed herein are processes for preparing 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile free base (compound (I)), salts of compound (I) and solid state form of said salts. Also disclosed herein are pharmaceutical compositions comprising such salts and solid state form thereof and methods of treating cancer, autoimmune, and inflammatory diseases using compound (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 29, 2018
    Date of Patent: October 29, 2019
    Assignee: PRINCIPIA BIOPHARMA INC.
    Inventors: Mohammad Reza Masjedizadeh, Steven Gourlay
  • Publication number: 20190231784
    Abstract: Modified release formulations, such as solid oral dosage forms comprising a core composition comprising Compound (I) and/or a pharmaceutically acceptable salt thereof; a sub-coating layer coating the core composition, said sub-coating layer comprising a polyvinyl alcohol and/or a hydroxypropyl methyl cellulose; and an enteric coating layer encapsulating the sub-coating layer and the core composition, said enteric coating layer comprising at least one polymer selected from an acrylic/methacrylic/ethacrylic acid homopolymer and copolymers thereof, a cellulose derivative, and a polyvinylpyrrolidone, and methods of administration of a Bruton's tyrosine kinase (BTK) inhibitor using said formulations.
    Type: Application
    Filed: June 29, 2017
    Publication date: August 1, 2019
    Applicant: Principia Biopharma Inc.
    Inventors: Abu J. FERDOUS, Mohammad R. MASJEDIZADEH, Wu LIN
  • Patent number: 10294223
    Abstract: Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: November 8, 2017
    Date of Patent: May 21, 2019
    Assignee: PRINCIPIA BIOPHARMA, INC.
    Inventors: Erik Verner, Kenneth Albert Brameld
  • Publication number: 20190076435
    Abstract: Disclosed herein are processes for preparing 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]pyiperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile free base (compound (I)), salts of compound (I) and solid state form of said salts. Also disclosed herein are pharmaceutical compositions comprising such salts and solid state form thereof and methods of treating cancer, autoimmune, and inflammatory diseases using compound (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 29, 2018
    Publication date: March 14, 2019
    Applicant: PRINCIPIA BIOPHARMA INC.
    Inventors: Mohammad Reza MASJEDIZADEH, Steven GOURLAY
  • Publication number: 20180327413
    Abstract: The present disclosure provides compounds of Formula (IA) and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: May 11, 2018
    Publication date: November 15, 2018
    Applicant: PRINCIPIA BIOPHARMA INC.
    Inventors: Tim OWENS, Erik VERNER
  • Publication number: 20180305350
    Abstract: The present disclosure provides compounds of formula (I) that are tyrosine kinase inhibitors, in particular Bruton tyrosine kinase (“BTK”) inhibitors, and are therefore useful for the treatment of diseases treatable by inhibition of BTK such as cancer, autoimmune, inflammatory, and thromboembolic diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Application
    Filed: June 23, 2016
    Publication date: October 25, 2018
    Applicant: Principia Biopharma Inc.
    Inventors: David M. GOLDSTEIN, Timothy D. OWENS
  • Patent number: 10092569
    Abstract: Disclosed herein are processes for preparing 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile free base (compound (I)), salts of compound (I) and solid state form of said salts. Also disclosed herein are pharmaceutical compositions comprising such salts and solid state form thereof and methods of treating cancer, autoimmune, and inflammatory diseases using compound (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 20, 2015
    Date of Patent: October 9, 2018
    Assignee: PRINCIPIA BIOPHARMA INC.
    Inventors: Mohammad Reza Masjedizadeh, Steven Gourlay
  • Publication number: 20180215756
    Abstract: Disclosed herein are processes for preparing 8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one and FGFR inhibitor, as well as polymorphs and/or salt forms thereof.
    Type: Application
    Filed: August 10, 2016
    Publication date: August 2, 2018
    Applicant: Principia Biopharma, Inc.
    Inventors: Jiang ZHU, Mohammad MASJEDIZADEH