At 2-position And At 4- Or 6-position Patents (Class 544/323)
  • Patent number: 10988463
    Abstract: Provided herein are substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
    Type: Grant
    Filed: August 21, 2020
    Date of Patent: April 27, 2021
    Assignee: Pfizer Inc.
    Inventors: Matthew Dowling, Dilinie Fernando, Kentaro Futatsugi, Kim Huard, Thomas Victor Magee, Brian Raymer, Andre Shavnya, Aaron Smith, Benjamin Thuma, Andy Tsai, Meihua Tu
  • Patent number: 10975039
    Abstract: Provided herein are isotopologues of Compound A, which are enriched with isotopes such as, for example, deuterium. Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided.
    Type: Grant
    Filed: May 11, 2020
    Date of Patent: April 13, 2021
    Assignee: SIGNAL PHARMACEUTICALS, LLC
    Inventors: Hon-Wah Man, Mohit Atul Kothare
  • Patent number: 10919865
    Abstract: Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: February 16, 2021
    Assignee: SIGNAL PHARMACEUTICALS, LLC
    Inventors: Mercedes Delgado, Jan Elsner, Paul Erdman, Robert Hilgraf, Mark A. Nagy, Stephen Norris, David A. Paisner, Yoshitaka Satoh, Marianne Sloss, Jayashree Tikhe, Won Hyung Yoon
  • Patent number: 10828300
    Abstract: The present invention provides 2,4-diaminopyrimidines, and/or pharmaceutically acceptable compositions thereof, as kinase inhibitors.
    Type: Grant
    Filed: June 1, 2018
    Date of Patent: November 10, 2020
    Assignee: Celgene CAR LLC
    Inventors: Juswinder Singh, Russell C. Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
  • Patent number: 10787438
    Abstract: Provided herein are substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
    Type: Grant
    Filed: January 16, 2020
    Date of Patent: September 29, 2020
    Assignee: Pfizer Inc.
    Inventors: Matthew Dowling, Dilinie Fernando, Kentaro Futatsugi, Kim Huard, Thomas Victor Magee, Brian Raymer, Andre Shavnya, Aaron Smith, Benjamin Thuma, Andy Tsai, Meihua Tu
  • Patent number: 10696665
    Abstract: The present application provides compounds of Formula I: Formula (I) that are useful as inhibitors of mutant IDH1, pharmaceutical compositions, and uses for the treatment of cancer.
    Type: Grant
    Filed: May 30, 2017
    Date of Patent: June 30, 2020
    Assignee: Eli Lilly and Company
    Inventors: Wenceslao Lumeras Amador, Serge Louis Boulet, Timothy Paul Burkholder, Santiago Carballares Martin, Raymond Gilmour, Patric James Hahn, Renato Alejandro Bauer, Zoran Rankovic
  • Patent number: 10676445
    Abstract: A new azido compound, 5-amino-6-chloro-2,4-diazido-pyrimidine, and a process for synthesizing. The synthesis may include reacting 5-amino-2,4,6-trichloropyrimidine and sodium azide. There is an excess molar amount of sodium azide for each chloro fractional molar amount on the 5-amino-2,4,6-trichloropyrimidine. The synthesis is a two phase reaction that is a dispersion. The 5-amino-2,4,6-trichloropyrimidine dissolved in acetone is a liquid phase, and the sodium azide is insoluble in acetone and is a solid phase, that is present in excess of chemical equivalents. The reaction product is soluble in acetone, and the reaction by-product, sodium chloride is also insoluble in acetone, and the crude yield is about 92%. Unreacted sodium azide and formed sodium chloride are removed by filtration.
    Type: Grant
    Filed: June 6, 2019
    Date of Patent: June 9, 2020
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: Christopher Wilhelm, Farhad Forohar, Denisse Soto
  • Patent number: 10596172
    Abstract: The present invention provides 2,4-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: June 29, 2018
    Date of Patent: March 24, 2020
    Assignee: Celgene CAR LLC
    Inventors: Juswinder Singh, Russell C. Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
  • Patent number: 10266500
    Abstract: Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
    Type: Grant
    Filed: June 28, 2018
    Date of Patent: April 23, 2019
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Brydon L. Bennett, Mercedes Delgado, Jan Elsner, Paul Erdman, Robert Hilgraf, Laurie Ann LeBrun, Meg McCarrick, Mark A. Nagy, Stephen Norris, David A. Paisner, Yoshitaka Satoh, Marianne Sloss, Jayashree Tikhe, Won Hyung Yoon
  • Patent number: 10206922
    Abstract: Methods for treating cough, chronic cough and urges to cough associated with respiratory diseases with a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are as defined herein.
    Type: Grant
    Filed: August 1, 2017
    Date of Patent: February 19, 2019
    Assignee: Afferent Pharmaceuticals, Inc.
    Inventors: Anthony P. Ford, Bruce G. McCarthy
  • Patent number: 10174007
    Abstract: Provided herein are substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
    Type: Grant
    Filed: October 11, 2017
    Date of Patent: January 8, 2019
    Assignee: Pfizer Inc.
    Inventors: Matthew Dowling, Dilinie Fernando, Kentaro Futatsugi, Kim Huard, Thomas Victor Magee, Brian Raymer, Andre Shavnya, Aaron Smith, Benjamin Thuma, Andy Tsai, Meihua Tu
  • Patent number: 10040770
    Abstract: Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
    Type: Grant
    Filed: June 7, 2017
    Date of Patent: August 7, 2018
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Mercedes Delgado, Jan Elsner, Paul Erdman, Robert Hilgraf, Laurie Ann LeBrun, Meg McCarrick, Mark A. Nagy, Stephen Norris, David A. Paisner, Yoshitaka Satoh, Marianne Sloss, Jayashree Tikhe, Won Hyung Yoon
  • Patent number: 10039775
    Abstract: Disclosed is a preparation method for an antitumor drug AP26113 (I). The method comprises the following preparation steps: cyclizing N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and N,N-dimethylamino acrylate, condensing N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and 4-(dimethyl phosphitylate)aniline, and chlorinating N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and a chlorinating agent, sequentially, so as to prepare AP26113 (I). The preparation method adopts easily-obtained raw materials, causes few side reactions, and is economical, environmentally friendly, and suitable for industrial production.
    Type: Grant
    Filed: November 24, 2017
    Date of Patent: August 7, 2018
    Assignee: SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
    Inventor: Xuenong Xu
  • Patent number: 10010548
    Abstract: The present invention provides 2,4-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: July 3, 2018
    Assignee: Celgene CAR LLC
    Inventors: Juswinder Singh, Russell C. Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
  • Patent number: 10004726
    Abstract: Polymorphs, Forms II and III, of cocrystals of p-coumaric acid and nicotinamide in a 1:1 molar ratio. Pharmaceutical compositions containing Forms II or III, processes for making such forms, and methods of treatment with such Forms.
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: June 26, 2018
    Assignee: AMRI SSCI, LLC
    Inventors: Melanie Janelle Bevill, Nate Schultheiss
  • Patent number: 9809579
    Abstract: Provided herein are substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: November 7, 2017
    Assignee: Pfizer Inc.
    Inventors: Matthew Dowling, Dilinie Fernando, Kentaro Futatsugi, Kim Huard, Thomas Victor Magee, Brian Raymer, Andre Shavnya, Aaron Smith, Benjamin Thuma, Andy Tsai, Meihua Tu
  • Patent number: 9751893
    Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
    Type: Grant
    Filed: June 18, 2009
    Date of Patent: September 5, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
  • Patent number: 9732070
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: September 9, 2016
    Date of Patent: August 15, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Kin Tso, Jing Zhang, Matthew Duncton, Salvador Alvarez, Rao Kolluri, John Ramphal, Sacha Holland
  • Patent number: 9724346
    Abstract: Methods for treating cough, chronic cough and urges to cough associated with respiratory diseases with a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are as defined herein.
    Type: Grant
    Filed: February 2, 2016
    Date of Patent: August 8, 2017
    Assignee: Afferent Pharmaceuticals Inc.
    Inventors: Anthony P. Ford, Bruce G. McCarthy
  • Patent number: 9701644
    Abstract: An object of the present invention is to provide a compound and pharmaceutical composition showing superior stability and/or solubility, etc. and having superior FLT3 inhibitory activity. The present invention provides a salt of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide, or a crystal thereof. Since the salt or a crystal thereof has superior FLT3 inhibitory activity and shows superior physicochemical properties as drugs, such as storage stability, solubility, and so forth, it is useful for treatments of diseases or conditions relating to FLT3. The present invention also provides a pharmaceutical composition and FLT3 inhibitor containing the salt or a crystal thereof.
    Type: Grant
    Filed: April 15, 2016
    Date of Patent: July 11, 2017
    Assignee: FUJIFILM Corporation
    Inventors: Shinsuke Mizumoto, Takuya Matsumoto
  • Patent number: 9701643
    Abstract: Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
    Type: Grant
    Filed: July 31, 2015
    Date of Patent: July 11, 2017
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Brydon L. Bennett, Mercedes Delgado, Jan Elsner, Paul Erdman, Robert Hilgraf, Laurie Ann LeBrun, Meg McCarrick, Mehran F. Moghaddam, Mark A. Nagy, Stephen Norris, David A. Paisner, William J. Romanow, Yoshitaka Satoh, Marianne Sloss, Jayashree Tikhe, Won Hyung Yoon
  • Patent number: 9573942
    Abstract: This invention concerns pyrimidine derivatives of formula having HIV (Human Immunodeficiency Virus) replication inhibiting properties, the preparation thereof and pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: February 21, 2017
    Assignee: Janssen Sciences Ireland UC
    Inventors: Jerôme Emile Georges Guillemont, Mikaël Paugam, Bruno François Marie Delest
  • Patent number: 9567342
    Abstract: Disclosed herein are protein kinase inhibitors, more particularly novel pyrimidine derivatives and pharmaceutical compositions thereof, and method of use thereof.
    Type: Grant
    Filed: October 29, 2015
    Date of Patent: February 14, 2017
    Assignees: SHANGHAI FOCHON PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES
    Inventors: Weibo Wang, Meiyu Geng, Jian Ding, Xingdong Zhao, Jing Ai, Qiang Tian, Xia Peng, Weipeng Zhang, Hongbin Liu, Haohan Tan, Ling Chen
  • Patent number: 9549927
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: September 2, 2015
    Date of Patent: January 24, 2017
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Richland Tester, Prasoon Chaturvedi, Zhendong Zhu, Sekhar S. Surapaneni, Lisa Beebe
  • Patent number: 9314459
    Abstract: Polymorphs, Forms II and III, of cocrystals of p-coumaric acid and nicotinamide in a 1:1 molar ratio. Pharmaceutical compositions containing Forms II or III, processes for making such forms, and methods of treatment with such Forms.
    Type: Grant
    Filed: January 28, 2015
    Date of Patent: April 19, 2016
    Assignee: AMRI SSCI, LLC
    Inventors: Melanie Janelle Bevill, Nate Schultheiss
  • Patent number: 9284279
    Abstract: Methods for treating cough, chronic cough and urges to cough associated with respiratory diseases with a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are as defined herein.
    Type: Grant
    Filed: August 22, 2014
    Date of Patent: March 15, 2016
    Assignee: Afferent Pharmaceuticals, Inc.
    Inventors: Anthony P. Ford, Bruce G. McCarthy
  • Patent number: 9206166
    Abstract: Disclosed herein are protein kinase inhibitors, more particularly novel pyrimidine derivatives and pharmaceutical compositions thereof, and method of use thereof.
    Type: Grant
    Filed: November 5, 2013
    Date of Patent: December 8, 2015
    Assignees: Shanghai Institute of Materia Medica Academy of Sciences, Shanghai Fochon Pharmaceutical Co., LTD
    Inventors: Weibo Wang, Meiyu Geng, Jian Ding, Xingdong Zhao, Jing Ai, Qiang Tian, Xia Peng, Weipeng Zhang, Hongbin Liu, Haohan Tan, Ling Chen
  • Patent number: 9181222
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: November 10, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Sacha Holland, Rao Kolluri, Salvador Alvarez, Matthew Duncton, Rajinder Singh, Jing Zhang, Esteban Masuda
  • Patent number: 9133134
    Abstract: Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein, including a kinase.
    Type: Grant
    Filed: May 15, 2013
    Date of Patent: September 15, 2015
    Assignee: PHARMACYCLICS LLC
    Inventors: Wei Chen, David J. Loury, Tarak D. Mody
  • Patent number: 9126950
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: September 8, 2015
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Richland Tester, Prasoon Chaturvedi, Zhendong Zhu, Sekhar S. Surapaneni, Lisa Beebe
  • Patent number: 9126949
    Abstract: The present invention provides a novel process for the preparation of 4-(4-hydroxypyrimidin-2-ylamino)benzonitrile. The present invention also provides a novel process for the preparation of 4-iodo-2,6-dimethyl benzenamine. The present invention further provides an improved process for the preparation of rilpivirine. The present invention further provides a tosylate salt of rilpivirine, process for its preparation and pharmaceutical compositions comprising it.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: September 8, 2015
    Assignee: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Adulla Venkat Narsimha Reddy, Bandi Vamsi Krishna
  • Patent number: 9120766
    Abstract: Disclosed are processes for preparing cocrystals, including processes for scaling up of cocrystal formation, as well as scalable processes for preparing cocrystals. Also disclosed are processes for scaled-up preparation of pterostilbene, progesterone, p-coumaric, and minoxidil cocrystals. Minoxidil cocrystals, such as minoxidil:benzoic acid 1:1 monohydrate cocrystals are also disclosed herein.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: September 1, 2015
    Assignee: AMRI SSCI, LLC
    Inventors: Melanie Janelle Bevill, Christopher Scott Seadeek, Ekaterina V. Albert, Petinka I. Vlahova, Richard James Ely, Patricia Andres
  • Patent number: 9062068
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: December 3, 2013
    Date of Patent: June 23, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rao Kolluri, Esteban Masuda, Kin Tso, Salvador Alvarez, Thilo Heckrodt, Sacha Holland, Ryan Kelley, Matthew Duncton, Rajinder Singh, Darren McMurtrie
  • Patent number: 9040543
    Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases are therapeutically useful.
    Type: Grant
    Filed: April 8, 2014
    Date of Patent: May 26, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Ankush Argade, Sambaiah Thota, David Carroll, Arvinder Sran, Robin Cooper, Rajinder Singh, Kin Tso, Somasekhar Bhamidipati
  • Publication number: 20150126504
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Application
    Filed: January 12, 2015
    Publication date: May 7, 2015
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
  • Publication number: 20150111912
    Abstract: Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein, including a kinase.
    Type: Application
    Filed: May 15, 2013
    Publication date: April 23, 2015
    Applicant: Pharmacyclics, Inc.
    Inventors: Wei Chen, David J. Loury, Tarak D. Mody
  • Patent number: 9012462
    Abstract: The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: May 21, 2009
    Date of Patent: April 21, 2015
    Assignee: Ariad Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Wei-Sheng Huang, Shuangying Liu, William C. Shakespeare, R. Mathew Thomas, Jiwei Qi, Feng Li, Xiaotian Zhu, Anna Kohlman, David C. Dalgarno, Jan Antoinette C. Romero, Dong Zou
  • Patent number: 9006243
    Abstract: HIV replication inhibitors of formula R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2, R3, R6 and R7 are hydrogen; hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(?O)R9; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 and R5 are hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; formyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(?O)R9; cyano; —S(?O)rR9; —NH—S(?O)2R9; —NHC(?O)H; —C(?O)NHNH2; —NHC(?O)R9; Het; —Y-Het; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R5 is pyridyl, —C(?O)NR5aR5b; —CH(OR5c)R5d; —CH2—NR5eR5f; —CH?NOR5a; —CH2—O—C2-6alkenyl; —CH2—O—P(?O)(OR5g)2; —CH2—O—C(?O)—NH2; —C(?O)—R5d; X is —NR1—, —O—, —CH2—, —S—; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compou
    Type: Grant
    Filed: December 28, 2007
    Date of Patent: April 14, 2015
    Assignee: Janssen R&D Ireland
    Inventors: Jerôme Emile Georges Guillemont, Céline Isabelle Mordant
  • Publication number: 20150099875
    Abstract: The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventors: Jean-Damien Charrier, Michael Edward O'Donnell
  • Publication number: 20150099749
    Abstract: This invention concerns pyrimidine derivatives of formula having HIV (Human Immunodeficiency Virus) replication inhibiting properties, the preparation thereof and pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 9, 2015
    Inventors: Jerôme Emile Georges Guillemont, Mikaël Paugam, Bruno François Marie Delest
  • Publication number: 20150094298
    Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
    Type: Application
    Filed: December 5, 2014
    Publication date: April 2, 2015
    Inventors: Shawn M. Bauer, Zhaozhong J. Jia, Mukund Mehrotra, Yonghong Song, Qing Xu, Wolin Huang, Chandrasekar Venkataramani, Jack W. Rose, Anjali Pandey
  • Publication number: 20150094296
    Abstract: The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: March 27, 2013
    Publication date: April 2, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Tetsuya Tsukamoto, Yusuke Ohba, Takafumi Yukawa, Hiroyuki Nagamiya, Taku Kamei, Norihito Tokunaga, Morihisa Saitoh, Atsutoshi Okabe
  • Publication number: 20150080368
    Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Applicant: VERASTEM, INC.
    Inventors: Michael Joseph Luzzio, Kevin Daniel Freeman-Cook, Samit Kumar Bhattacharya, Matthew Merrill Hayward, Catherine Angela Hulford, Christopher Lowell Autry, Xumiao Zhao, Jun Xiao, Kendra Louise Nelson
  • Patent number: 8969510
    Abstract: Fluorinated supramolecular polymers containing at least 5% by weight of covalently bonded fluorine atoms, based on total weight of the polymers are disclosed. The polymers comprise a fluorinated polymer chain and a (self-)complementary unit capable of forming at least three hydrogen bonds being covalently bonded to the fluorinated polymer chain. Also disclosed are materials comprising (a) a fluorinated supramolecular polymer and (b) a non-fluorinated polymer and/or (c) a fluorinated compound, the non-fluorinated polymer being a polymer containing less than 5% by weight of covalently bonded fluorine atoms, based on the total weight of the non-fluorinated polymer, and the fluorinated compound being either a low molecular weight fluorinated compound comprising at least one fluorine atom and having a molecular weight of 34 to 600 amu, or a fluoropolymer containing at least 5% by weight of covalently bonded fluorine atoms and a Mn from about 600 to about 5000.
    Type: Grant
    Filed: November 22, 2011
    Date of Patent: March 3, 2015
    Assignee: SupraPolix B.V.
    Inventor: Anton Willem Bosman
  • Patent number: 8962641
    Abstract: The invention relates to new pyrrolidine derivatives of the formula wherein R1 to R3, Ar, L T and n are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: April 7, 2014
    Date of Patent: February 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Annekatrin Heimann, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Patent number: 8962643
    Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.
    Type: Grant
    Filed: February 23, 2007
    Date of Patent: February 24, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Ankush Argade, Kin Tso, Sambaiah Thota, David Carroll, Arvinder Sran, Robin Cooper, Rajinder Singh, Somasekhar Bhamidipati, Vanessa Taylor, Esteban Masuda
  • Patent number: 8957068
    Abstract: The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: February 17, 2015
    Assignee: Novartis AG
    Inventors: Thomas Raymond Caferro, Young Shin Cho, Abran Q. Costales, Huangshu Lei, Francois Lenoir, Julian Roy Levell, Gang Liu, Mark G. Palermo, Keith Bruce Pfister, Martin Sendzik, Cynthia Shafer, Michael David Shultz, Troy Smith, James Clifford Sutton, Bakary-Barry Toure, Fan Yang, Qian Zhao
  • Patent number: 8957081
    Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: February 17, 2015
    Assignee: IRM LLC
    Inventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, III, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
  • Publication number: 20150045339
    Abstract: The object is to provide an Fms-like tyrosine kinase 3 (FLT3) inhibitor useful as a therapeutic agent for acute myeloid leukemia (AML). A novel nitrogen-containing heterocyclic compound represented by the general formula [1] or a salt thereof is provided. The compound or a salt thereof of the present invention can be used as an active ingredient of a pharmaceutical composition for a treatment of a disease or condition relating to FLT3, such as acute myeloid leukemia (AML) and acute promyelocytic leukemia (APL).
    Type: Application
    Filed: October 16, 2014
    Publication date: February 12, 2015
    Applicant: FUJIFILM CORPORATION
    Inventors: Masaru TAKASAKI, Toshiaki TSUJINO, Shintarou TANABE, Megumi OOKUBO, Kimihiko SATO, Atsushi HIRAI, Daisuke TERADA, Shinsuke INUKI, Shinsuke MIZUMOTO
  • Patent number: 8952155
    Abstract: Disclosed is process for the preparation of a key Rilpivirine intermediate namely, (E)-4-(2-cyanoethenyl)-2,6-dimethylphenylamine hydrochloride (II) by a process comprising reaction of the tetrafluoroborate salt of the diazonium ion of 2,6-dimethyl-4-amino-1-carboxybenzyl phenylamine (VI) with acrylonitrile in presence of palladium acetate, followed by treatment with an acid and its subsequent conversion to the hydrochloride salt (II), wherein the undesired Z isomer is less than 0.5% and provides Rilpivirine hydrochloride having Z isomer less than 0.1%.
    Type: Grant
    Filed: April 9, 2012
    Date of Patent: February 10, 2015
    Assignee: Emcure Pharmaceuticals Limited
    Inventors: Mukund Keshav Gurjar, Golakchandra Sudarshan Maikap, Shashikant Gangaram Joshi, Sachin Aravind Badhe, Samit Satish Mehta