The Additional Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbons Patents (Class 514/263.22)
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Patent number: 11802120Abstract: The present invention relates to fused cyclic urea derivatives which have antagonistic activities against CRHR1 and/or CRHR2, and which are useful in the treatment or prevention of disorders and diseases in which CRHR1 and/or CRHR2 is involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CRHR1 and/or CRHR2 is involved.Type: GrantFiled: April 9, 2019Date of Patent: October 31, 2023Assignee: RaQualia Pharma Inc.Inventors: Masashi Ohmi, Takeshi Matsushita, Kazuo Ando, Ryuichi Yamaguchi, Yutaka Fukumoto, Ryohei Magara, Tatsuya Yamagishi, Mikito Takefuji
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Patent number: 11746118Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where R1 and R2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.Type: GrantFiled: August 27, 2021Date of Patent: September 5, 2023Inventors: Maurice Raymond Verschoyle Finlay, Frederick Woolf Goldberg, Attilla Kuan Tsuei Ting
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Patent number: 11590139Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.Type: GrantFiled: January 12, 2021Date of Patent: February 28, 2023Assignee: Signal Pharmaceuticals, LLCInventors: Matthew Alexander, Sogole Bahmanyar, John Frederick Boylan, Joshua Hansen, Dehua Huang, Robert Hubbard, Brandon Jeffy, Jim Leisten, Mehran Moghaddam, Raj K. Raheja, Heather Raymon, Kimberly Schwarz, Marianne Sloss, Eduardo Torres, Tam Minh Tran, Shuichan Xu, JingJing Zhao
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Patent number: 11530216Abstract: Disclosed herein are deuterated compounds of the formula which are useful as colony stimulating factor-1 receptor inhibitors (“CSF-1R inhibitors”).Type: GrantFiled: February 11, 2022Date of Patent: December 20, 2022Assignee: GENZYME CORPORATIONInventors: John L. Kane, Jr., Nellwyn A. Hagan, Maria A. Fitzgerald
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Patent number: 11312718Abstract: Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.Type: GrantFiled: January 3, 2020Date of Patent: April 26, 2022Assignee: Infinity Pharmaceuticals, Inc.Inventors: Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
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Patent number: 11247995Abstract: Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphic forms, cocrystals, and amorphous forms thereof, and pharmaceutical compositions thereof.Type: GrantFiled: November 20, 2018Date of Patent: February 15, 2022Assignee: Infinity Pharmaceuticals, Inc.Inventors: Louis Grenier, Andre Lescarbeau, Praveen Sharma, Daniel G. Genov
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Patent number: 11208414Abstract: The invention relates to novel heterocyclic compounds having CD73 inhibitory activity and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.Type: GrantFiled: September 27, 2019Date of Patent: December 28, 2021Assignee: CALITHERA BIOSCIENCES, INC.Inventors: Lijing Chen, Jim Li, Eric B. Sjogren, Roland J. Billedeau
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Patent number: 11174261Abstract: The invention relates to novel heterocyclic compounds having CD73 inhibitory activity and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.Type: GrantFiled: September 27, 2019Date of Patent: November 16, 2021Assignee: CALITHERA BIOSCIENCES, INC.Inventors: Lijing Chen, Jim Li, Eric B. Sjogren, Roland J. Billedeau
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Patent number: 11136340Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where R1 and R2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.Type: GrantFiled: July 30, 2019Date of Patent: October 5, 2021Assignee: AstraZeneca ABInventors: Maurice Raymond Verschoyle Finlay, Frederick Woolf Goldberg, Attilla Kuan Tsuei Ting
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Patent number: 10940152Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.Type: GrantFiled: April 13, 2020Date of Patent: March 9, 2021Assignee: SIGNAL PHARMACEUTICALS, LLCInventors: Matthew Alexander, Sogole Bahmanyar, John Frederick Boylan, Joshua Hansen, Dehua Huang, Robert Hubbard, Brandon Jeffy, Jim Leisten, Mehran Moghaddam, Raj K. Raheja, Heather Raymon, Kimberly Schwarz, Marianne Sloss, Eduardo Torres, Tam Minh Tran, Shuichan Xu, JingJing Zhao
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Patent number: 10933063Abstract: Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I):Type: GrantFiled: May 22, 2019Date of Patent: March 2, 2021Assignees: Suzhou Baijibugong Pharmaceutical Technology Co., Ltd.Inventors: Xibin Liao, Jia Li, Zhijian Lu, Yubo Zhou, Anhui Gao
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Patent number: 10899765Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the identification of CCR2 antagonists.Type: GrantFiled: January 11, 2019Date of Patent: January 26, 2021Assignee: ChemoCentryx, Inc.Inventors: Antoni Krasinski, Sreenivas Punna, Solomon Ungashe, Qiang Wang, Yibin Zeng
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Patent number: 10844062Abstract: The present invention provides a novel pyridine derivative, a pharmaceutically acceptable salt thereof, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient. The pyridine derivative according to the present invention inhibits Raf kinase (B-Raf, Raf-1, or B-RafV600E) and a vascular endothelial growth factor receptor (VEGFR2) involved in angiogenesis, and thus, can be favorably used for the prevention or treatment of melanoma, colorectal cancer, prostate cancer, thyroid cancer, lung cancer, pancreatic cancer, ovarian cancer, or the like, which is induced by RAS mutation.Type: GrantFiled: January 11, 2017Date of Patent: November 24, 2020Assignees: Incheon University Industry Academic Cooperation Foundation, Samjin Pharmaceutical Co., Ltd., Bamichem Co., Ltd.Inventors: Eui Hwan Cho, Hee Jong Shin, Min Hyo Ki, Ho Seok Kwon, Jae Woong Lee, Jeong Ho Joo, Keun Kuk Lee, Jong Min Kim, Yong Bin Park, Sung Hyun Kang, Hyoung Min Cho, Hyun Tae Kim, Soon Kil Ahn, Sung Pyo Hong, Sung Hye Kim
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Patent number: 10723737Abstract: Disclosed herein inter alia are compositions and methods useful in the treatment neurodegenerative diseases and cardiomyopathy, and for modulating the activity of PINK1.Type: GrantFiled: February 21, 2017Date of Patent: July 28, 2020Assignees: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, MITOKININ LLCInventors: Nicholas T. Hertz, Kevan M. Shokat, Robert DeVita
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Patent number: 10646493Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.Type: GrantFiled: July 17, 2019Date of Patent: May 12, 2020Assignee: Signal Pharmaceuticals, LLCInventors: Matthew Alexander, Sogole Bahmanyar, John Frederick Boylan, Joshua Hansen, Dehua Huang, Robert Hubbard, Brandon Jeffy, Jim Leisten, Mehran Moghaddam, Raj K. Raheja, Heather Raymon, Kimberly Schwarz, Marianne Sloss, Eduardo Torres, Tam Minh Tran, Shuichan Xu, JingJing Zhao
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Patent number: 10584125Abstract: Compounds of formula (I): wherein: R1 is butoxy or methylbutoxy; R2 is a group having the structure: where n is an integer having a value of five; Het is a six-membered saturated heterocycle containing five carbon atoms and one nitrogen atom, wherein Het is attached to the —(CH2)n— moiety at the carbon 4 position of the heterocycle; and R3 is hydrogen; or pharmaceutically acceptable salts thereof; and their use as vaccine adjuvants and in the treatment of various disorders.Type: GrantFiled: November 13, 2015Date of Patent: March 10, 2020Assignee: GLAXOSMITHKLINE BIOLOGICALS SAInventors: Helene G. Bazin-Lee, Yufeng Li
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Patent number: 10577368Abstract: Disclosed are compounds of the formula (I) and (II): which are A3 adenosine receptor agonists, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein X, Y, Z, R2-R6, and R103-R106 are as defined in the specification. These compounds are selective to the A3 receptor, and are contemplated for use in the treatment or prevention of a number of diseases or conditions, for example, neuropathic pain.Type: GrantFiled: April 10, 2018Date of Patent: March 3, 2020Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, Saint Louis UniversityInventors: Kenneth A. Jacobson, Dilip K. Tosh, Daniela Salvemini
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Patent number: 10550122Abstract: Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including Pl3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.Type: GrantFiled: October 31, 2017Date of Patent: February 4, 2020Assignee: Infinity Pharmaceuticals, Inc.Inventors: Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
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Patent number: 10398700Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.Type: GrantFiled: October 24, 2018Date of Patent: September 3, 2019Assignee: Signal Pharmaceuticals, LLCInventors: Matthew Alexander, Joshua Hansen, Dehua Huang, Robert Hubbard, Raj K. Raheja, Kimberly Schwarz, Marianne Sloss, Eduardo Torres, JingJing Zhao
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Patent number: 10328731Abstract: A printer for printing objects for marking electrical components, having a housing, a printing space formed inside of the housing, a printing device, a receiving device for a replaceable magazine for receiving the object to be printed, a control and evaluation unit, and an input and display device, wherein the receiving device can move between a loading and unloading position outside of the printing space and a printing position inside of the printing space. The printer has lower and upper housing parts, wherein the printing space, the printing device, the receiving device, and the control and evaluation unit are arranged in the lower housing part. A tablet computer is pivotably attached on the top side of the upper housing part, whereby the tablet computer can be locked in an upwardly pivoted position, and the upper housing part is mounted to pivot about a rotational axis on the lower housing part.Type: GrantFiled: January 19, 2017Date of Patent: June 25, 2019Assignee: PHOENIX CONTACT GMBH & CO. KGInventors: Sandra Klocke, Peter Isaak, Albrecht Schierholz
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Patent number: 10208050Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the identification of CCR2 antagonists.Type: GrantFiled: August 4, 2017Date of Patent: February 19, 2019Assignee: ChemoCentryx, Inc.Inventors: Antoni Krasinski, Sreenivas Punna, Solomon Ungashe, Qiang Wang, Yibin Zeng
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Patent number: 10196395Abstract: The present disclosure relates to crystalline Form ? of a compound of formula (I) used for preparing a blood-cancer drug and preparation method thereof. The crystalline Form ? in the present disclosure has better stability, and its solubility and hygroscopicity meet the requirements of medical use. Form ? has simple preparation method and low manufacturing cost, and provides great value to future optimization and development of this drug.Type: GrantFiled: February 1, 2016Date of Patent: February 5, 2019Assignee: Crystal Pharmatech Co., LtdInventors: Minhua Chen, Yanfeng Zhang, Xiaojuan Diao, Nan Xia, Xiaoyu Zhang
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Patent number: 10149849Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.Type: GrantFiled: July 5, 2017Date of Patent: December 11, 2018Assignee: Signal Pharmaceuticals, LLCInventors: Matthew Alexander, Joshua Hansen, Dehua Huang, Robert Hubbard, Raj K. Raheja, Kimberly Schwarz, Marianne Sloss, Eduardo Torres, JingJing Zhao
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Patent number: 10010507Abstract: Described herein are pharmaceutical formulations of Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one. Also disclosed are methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: GrantFiled: March 1, 2018Date of Patent: July 3, 2018Assignee: Pharmacyclics LLCInventors: Ching W. Chong, Robert Kuehl, Heow Tan, Harisha Atluri
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Patent number: 9877968Abstract: Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.Type: GrantFiled: April 21, 2016Date of Patent: January 30, 2018Assignee: GLAXOSMITHKLINE LLCInventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
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Patent number: 9840505Abstract: Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.Type: GrantFiled: February 4, 2016Date of Patent: December 12, 2017Assignee: Infinity Pharmaceuticals, Inc.Inventors: Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
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Patent number: 9737541Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.Type: GrantFiled: October 27, 2016Date of Patent: August 22, 2017Assignee: Signal Pharmaceuticals, LLCInventors: Matthew Alexander, Sogole Bahmanyar, Joshua Hansen, Dehua Huang, Robert Hubbard, Brandon Jeffy, Jim Leisten, Mehran Moghaddam, Raj K. Raheja, Heather Raymon, Kimberly Schwarz, Marianne Sloss, Eduardo Torres, Tam Minh Tran, Shuichan Xu, JingJing Zhao, John Frederick Boylan
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Patent number: 9738644Abstract: Substituted isoquinolinone compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: GrantFiled: September 29, 2015Date of Patent: August 22, 2017Assignee: Infinity Pharmaceuticals, Inc.Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
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Patent number: 9512124Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.Type: GrantFiled: October 5, 2015Date of Patent: December 6, 2016Assignee: Signal Pharmaceuticals, LLCInventors: Matthew Alexander, Sogole Bahmanyar, Joshua Hansen, Dehua Huang, Robert Hubbard, Brandon Jeffy, Jim Leisten, Mehran Moghaddam, Raj K. Raheja, Heather Raymon, Kimberly Schwarz, Marianne Sloss, Eduardo Torres, Tam Minh Tran, Shuichan Xu, JingJing Zhao, John Frederick Boylan
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Patent number: 9486526Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in patients for whom metformin therapy is inappropriate due to intolerability or contraindication against metformin.Type: GrantFiled: June 3, 2014Date of Patent: November 8, 2016Assignee: Boehringer Ingelheim International GmbHInventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Ruth Harper, Hans-Juergen Woerle
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Patent number: 9388140Abstract: The present invention relates to substituted benzimidazole compounds of general formula (I) in which R3, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: GrantFiled: March 28, 2012Date of Patent: July 12, 2016Assignee: Bayer Intellectual Property GmbHInventors: Ulrich Klar, Marcus Koppitz, Duy Nguyen, Dirk Kosemund, Roland Neuhaus, Gerhard Siemeister
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Patent number: 9346806Abstract: Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.Type: GrantFiled: October 13, 2011Date of Patent: May 24, 2016Assignee: GlaxoSmithKline LLCInventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
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Patent number: 9290497Abstract: Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.Type: GrantFiled: July 9, 2014Date of Patent: March 22, 2016Assignee: Infinity Pharmaceuticals, Inc.Inventors: Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
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Patent number: 9266893Abstract: Disclosed herein is a solid oral dosage form comprising at least one coating chosen from enteric coatings and delayed release coatings, at least one pharmaceutically acceptable excipient, and a compound, or a pharmaceutically acceptable salt thereof, having the structure:Type: GrantFiled: January 10, 2014Date of Patent: February 23, 2016Assignee: Pharmacyclics LLCInventors: Lee Honigberg, Erik Verner, Zhengying Pan
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Patent number: 9216982Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.Type: GrantFiled: June 5, 2014Date of Patent: December 22, 2015Assignee: Intellikine LLCInventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
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Patent number: 9212381Abstract: Synthesis of many proteins is tightly controlled at the level of translation and plays an essential role in fundamental processes such as cell growth and proliferation, signaling, differentiation or death. Methods that allow imaging and identification of nascent proteins allow for dissecting regulation of translation, both spatially and temporally, including in whole organisms. Described herein are robust chemical methods for imaging and affinity-purifying nascent polypeptides in cells and in animals, based on puromycin analogs. Puromycin analogs of the present invention form covalent conjugates with nascent polypeptide chains, which are rapidly turned over by the proteasome and can be visualized and specifically captured by a bioorthogonal reaction (e.g., [3+2] cycloaddition). The methods of the present invention have broad applicability for imaging protein synthesis and for identifying proteins synthesized under various physiological and pathological conditions in vivo.Type: GrantFiled: November 9, 2012Date of Patent: December 15, 2015Assignee: President and Fellows of Harvard CollegeInventors: Adrian Salic, Jing Liu
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Patent number: 9212185Abstract: Disclosed herein are compounds of Formula (D) that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: GrantFiled: November 14, 2013Date of Patent: December 15, 2015Assignee: PHARMACYCLICS LLCInventors: Lee Honigberg, Erik Verner, Zhengying Pan
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Patent number: 9193735Abstract: Disclosed herein is a solid oral formulation comprising a therapeutically effective amount of a compound of Formula (A) formulated for release of the compound in the intestine, wherein the compound of Formula (A) has the structure:Type: GrantFiled: January 15, 2014Date of Patent: November 24, 2015Assignee: PHARMACYCLICS LLCInventors: Lee Honigberg, Erik Verner, Zhengying Pan
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Patent number: 9181257Abstract: Disclosed herein are pyrazolo[3,4-d]pyrimidines that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: GrantFiled: November 14, 2013Date of Patent: November 10, 2015Assignee: PHARMACYCLICS LLCInventors: Lee Honigberg, Erik Verner, Zhengying Pan
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Patent number: 9163026Abstract: Disclosed herein are compounds of Formula (D) that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: GrantFiled: November 14, 2013Date of Patent: October 20, 2015Assignee: PHARMACYCLICS LLCInventors: Lee Honigberg, Erik Verner, Zhengying Pan
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Patent number: 9156846Abstract: Disclosed herein is a solid oral formulation comprising a therapeutically effective amount of a compound of Formula (A) formulated for release of the compound in the intestine, wherein the compound of Formula (A) has the structure:Type: GrantFiled: January 15, 2014Date of Patent: October 13, 2015Assignee: PHARMACYCLICS LLCInventors: Lee Honigberg, Erik Verner, Zhengying Pan
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Patent number: 9156847Abstract: Disclosed is a process for the preparation of the following compounds: where R1, R1a and R2a have the definitions in the description, as well as a process to prepare other intermediates that may be useful to synthesize downstream products, especially compounds that are useful as medicaments, for instance Bruton's tyrosine kinase (Btk) inhibitors such as ibrutinib. Also disclosed are other processes, other intermediates and compounds per se.Type: GrantFiled: March 11, 2014Date of Patent: October 13, 2015Assignee: Janssen Pharmaceutica NVInventors: Philip Pye, Cyril Ben Haim, Matteo Conza, Ioannis Nicolaos Houpis
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Patent number: 9073879Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.Type: GrantFiled: April 18, 2011Date of Patent: July 7, 2015Assignee: MERCK SHARP & DOHME CORP.Inventors: Philippe G. Nantermet, Zhi-Qiang Yang, Constantine Kreatsoulas, Abbas M. Walji, Hong Zhu
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Publication number: 20150148354Abstract: The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms.Type: ApplicationFiled: October 27, 2014Publication date: May 28, 2015Inventors: Benjamin Mark SKEAD, Christopher Peter WORRALL, Jonathan Charles Christian ATHERTON, Julian Scott NORTHEN, Philippe FERNANDES
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Publication number: 20150141407Abstract: The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.Type: ApplicationFiled: May 30, 2013Publication date: May 21, 2015Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Lan Xie, Xiaofeng Wang, Kuo-Hsiung Lee
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Publication number: 20150141402Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, G, ring A, ring B, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, and m are defined herein. The novel purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.Type: ApplicationFiled: November 20, 2014Publication date: May 21, 2015Applicant: PFIZER INC.Inventors: Douglas Carl Behenna, Hengmiao Cheng, Sujin Cho-Schultz, Theodore Otto Johnson, JR., John Charles Kath, Asako Nagata, Sajiv Krishnan Nair, Simon Paul Planken
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Publication number: 20150126506Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: January 8, 2015Publication date: May 7, 2015Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
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Publication number: 20150126488Abstract: [Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. [Means for Solution] It was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.Type: ApplicationFiled: April 17, 2013Publication date: May 7, 2015Applicant: ASTELLAS PHARMA INCInventors: Yutaka Nakajima, Sunao Imada, Yuji Takasuna, Naohiro Aoyama, Takahiro Nigawara, Shohei Shirakami, Fumiyuki Shirai, Junji Sato, Keita Nakanishi, Kaori Kubo
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Publication number: 20150126509Abstract: The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: January 12, 2015Publication date: May 7, 2015Inventors: Randall L. Halcomb, Paul A. Roethle
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Publication number: 20150105383Abstract: The invention relates to HDAC inhibitors, or combinations comprising an HDAC inhibitor and a PI3K inhibitor for the treatment of non-hodgkin's lymphoma in a subject in need thereof. Also provided herein are methods for treating non-hodgkin's lymphoma in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor, or a combination comprising an HDAC inhibitor and a PI3K inhibitor.Type: ApplicationFiled: October 8, 2014Publication date: April 16, 2015Applicant: Acetylon Pharmaceuticals, Inc.Inventors: Steven Norman Quayle, Simon Stewart Jones