The Additional Hetero Ring Is 1,3-diazine (including Hydrogenated) Patents (Class 540/600)
  • Patent number: 11155534
    Abstract: Disclosed are an EGFR inhibitor free base or acid salt polycrystalline form, a preparation method therefor, and an application thereof. The present invention specifically relates to an N-(5-((4-(1-cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide free base or acid salt polycrystalline form, a preparation method therefor, and an application of the polycrystalline form in preparing a drug for treating an EGFR mutant activity-mediated disease. The present invention is used for inhibiting the activity of an L858R EGFR mutant, a T790M EGFR mutant and an exon 19 deletion activating mutant etc., may be widely applied in preventing and treating cancer, especially non-small cell lung cancer and other related diseases, and is expected to develop into a new generation of EGFR inhibitors.
    Type: Grant
    Filed: August 6, 2020
    Date of Patent: October 26, 2021
    Assignees: Jiangsu Hansoh Pharmaceutical Group Co., Ltd., Shanghai Hansoh Biomedical Co., Ltd.
    Inventors: Zhongke Chen, Fuping Liu, Lei Liu, Rudi Bao
  • Patent number: 10865216
    Abstract: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. In addition, species of tricyclic gyrase inhibitors compounds are also disclosed herein. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
    Type: Grant
    Filed: September 11, 2013
    Date of Patent: December 15, 2020
    Assignees: MERCK SHARP & DOHME CORP., LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
    Inventors: Daniel Bensen, Allen Borchardt, Zhiyong Chen, John M. Finn, Thanh To Lam, Suk Joong Lee, Xiaoming Li, Leslie William Tari, Min Teng, Michael Trzoss, Junhu Zhang, Michael E. Jung, Felice C. Lightstone, Sergio E. Wong, Toan B. Nguyen
  • Patent number: 10053452
    Abstract: The present invention relates to crystalline forms and co-crystal forms of pharmaceutically acceptable salts of the compound, N-(4-((3-(2-amino-4-pyrimidinyl)-2-pyridinyl)oxy)phenyl)-4-(4-methyl-2-thienyl)-1-phthalazinamine (AMG 900, and pharmaceutical compositions comprising said crystalline and co-crystal forms thereof. The invention further provides uses of the crystalline forms and compositions, to treat cancer, including various types of solid tumors and hematologic cancer including myeloma and leukemia.
    Type: Grant
    Filed: November 25, 2014
    Date of Patent: August 21, 2018
    Assignee: AMGEN INC.
    Inventors: Mary Chaves, Matthew Bio, Matthew Peterson
  • Patent number: 9708300
    Abstract: The present invention relates to an amorphous form of vilazodone hydrochloride and process for the preparation of amorphous form of vilazodone hydrochloride. The invention also relates to pharmaceutical compositions that include a therapeutically effective amount of the amorphous form of vilazodone hydrochloride and use of said compositions for the treatment of major depressive disorder (MDD).
    Type: Grant
    Filed: March 16, 2012
    Date of Patent: July 18, 2017
    Assignee: Cadila Healthcare Limited
    Inventors: Shirprakash Dhar Dwivedi, Ramesh Chandra Singh, Jigar Mukundbhai Raval
  • Patent number: 9643971
    Abstract: The present invention includes pyrimido[5,4-d]pyrimidines that are useful in the prevention and/or treatment of breathing control diseases or disorders in a subject in need thereof. The present invention also includes a method of preventing and/or treating a respiratory disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of at least one compound of the invention. The present invention further includes a method of preventing destabilization or stabilizing breathing rhythm in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of at least one compound of the invention.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: May 9, 2017
    Assignee: Galleon Pharmaceuticals, Inc.
    Inventors: Scott Dax, James Joseph Mencel, Vita Ozola, Kirill Shubin, Marina Martjuga, Edgars Suna
  • Patent number: 9381197
    Abstract: The present invention relates to the active pharmaceutical ingredient dipyridamole. In particular, it relates to efficient processes for the preparation of dipyridamole which are amenable to large scale commercial production and provide the required product with improved yield and purity. The present invention also relates to a novel crystallization method for the purification of dipyridamole.
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: July 5, 2016
    Assignee: Generics [UK] Limited
    Inventors: Dattatrey Kokane, Bindu Manojkumar, Vinayak Govind Gore
  • Patent number: 9133165
    Abstract: The invention relates to sulfonic acid salts of heterocyclylamide-substituted imidazoles, and to solvates and hydrates thereof, to the use thereof for treating and/or preventing diseases, and to use thereof for producing drugs for treating and/or preventing diseases, in particular for use as antiviral agents, in particular against cytomegaloviruses.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: September 15, 2015
    Assignee: AICURIS GMBH & CO. KG
    Inventors: Wilfried Schwab, Guido Schiffer, Kurt Voegtli, Andreas Kyas, Gerd Osswald
  • Patent number: 9056839
    Abstract: The present invention provides a solid form and compositions thereof, which are useful as an inhibitor of EGFR kinases and which exhibit desirable characteristics for the same.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 16, 2015
    Assignee: Celgene Avilomics Research, Inc.
    Inventor: Mei Lai
  • Publication number: 20150141408
    Abstract: The present invention relates to tricyclic pyrrolo derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Mauro Angiolini, Italo Beria, Maria Gabriella Brasca, Francesco Casuscelli, Roberto D'Alessio, Andrea Lombardi Borgia
  • Publication number: 20150057263
    Abstract: This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.
    Type: Application
    Filed: March 19, 2013
    Publication date: February 26, 2015
    Inventors: Robert Brown, Matthew John Fuchter, Nadine Chapman-Rothe, Nitipol Srimongkolpithak, Joachim Caron, James Synder, Thota Ganesh, Jin Liu, Aiming Sun
  • Patent number: 8916554
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Patrick René´ Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
  • Patent number: 8906906
    Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: December 9, 2014
    Assignee: Katholieke Universiteit Leuven
    Inventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
  • Publication number: 20140323466
    Abstract: Disclosed are new thienyl[3,2-d]pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.
    Type: Application
    Filed: October 23, 2012
    Publication date: October 30, 2014
    Inventors: Hong Liu, Jia Li, Jian Li, Jingya Li, Jiang Wang, Mingbo Su, Jie Lian, Hualiang Jiang, Kaixian Chen
  • Publication number: 20140309215
    Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
    Type: Application
    Filed: June 24, 2014
    Publication date: October 16, 2014
    Inventors: Michael H. RABINOWITZ, Mark D. ROSEN, Kyle T. TARANTINO, Hariharan VENKATESAN
  • Publication number: 20140303149
    Abstract: Compounds of the formula I or II: wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.
    Type: Application
    Filed: April 2, 2014
    Publication date: October 9, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Nidhi Arora, Shaoqing Chen, Johannes Cornelius Hermann, Andreas Kuglstatter, Sharada Shenvi Labadie, Clara Jeou Jen Lin, Matthew C. Lucas, Amy Geraldine Moore, Eva Papp, Francisco Xavier Talamas, Jutta Wanner, Yansheng Zhai
  • Publication number: 20140294764
    Abstract: This disclosure relates to compounds, compositions and methods of epigenetically transforming cells. In certain embodiments, the disclosure relates to methods of generating epigenetically altered cells comprising mixing isolated cells with compositions disclosed herein under conditions such that epigenetically altered cells are formed. In certain embodiments, the disclosure contemplates inducing cells, such as adult somatic cells or cells that are not naturally pluripotent, into cells with chemically induce pluripotency. In certain embodiments, the disclosure contemplates certain compounds disclosed herein, compounds disclosed herein optionally substituted with one or more substituents, derivatives, or salts thereof, for these purposes.
    Type: Application
    Filed: November 8, 2012
    Publication date: October 2, 2014
    Applicants: ISTITUTO PASTEUR - FONDAZIONE CENCI BOLOGNETTI, EMORY UNIVERSITY
    Inventors: Young-Sup Yoon, Xiaodong Cheng, Ji Woong Han, Antonello Mai
  • Patent number: 8829011
    Abstract: Certain 2-aminopyrimidine compounds of formula (I) are serotonin receptor modulators useful in the treatment of diseases mediated by serotonin receptors.
    Type: Grant
    Filed: October 29, 2009
    Date of Patent: September 9, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Nicholas I. Carruthers, Gregor J. MacDonald, Brock T. Shireman, Vi T. Tran
  • Publication number: 20140235615
    Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: March 24, 2014
    Publication date: August 21, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Misaki HOMMA, Toru MIYAZAKI, Yuya OGURO, Osamu KURASAWA
  • Publication number: 20140228352
    Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: March 24, 2014
    Publication date: August 14, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Misaki HOMMA, Toru MIYAZAKI, Yuya OGURO, Osamu KURASAWA
  • Patent number: 8796263
    Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
    Type: Grant
    Filed: August 12, 2011
    Date of Patent: August 5, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
  • Publication number: 20140179673
    Abstract: The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which R1, R2, n, R3, R4, R5 and R6 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3K?. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3K?.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: GILEAD CALISTOGA LLC
    Inventors: Jerry EVARTS, Leena PATEL, Jennifer A. TREIBERG, Stephane PERREAULT, Arthur YEUNG, Lafe J. PURVIS, II, Musong KIM
  • Patent number: 8759338
    Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: June 24, 2014
    Assignee: Novartis AG
    Inventors: Matthew Burger, Jiong Lan
  • Publication number: 20140163010
    Abstract: New pyrazolo[3,4-d]pyrimidine compounds having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for preparing these compounds, to compositions comprising them and to their use as medicaments.
    Type: Application
    Filed: July 13, 2012
    Publication date: June 12, 2014
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Maria Rosa Cuberes-Altisent, Jordi Corbera-Arjona, Jose Luis Diaz-Fernanadez, Carmen Almansa-Rosales
  • Publication number: 20140163000
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as defined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 12, 2014
    Inventors: Nadia Ahmad, Dean Boyall, Jean-Damien Charrier, Chris Davis, Rebecca Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Donald Middleton, Michael O'Donnell, Maninder Panesar, Francoise Pierard, Joanne Pinder, David Shaw, Pierre-Henri Storck, John Studley, Heather Twin
  • Publication number: 20140155386
    Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: December 2, 2013
    Publication date: June 5, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak
  • Publication number: 20140154240
    Abstract: The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
    Type: Application
    Filed: May 30, 2013
    Publication date: June 5, 2014
    Inventors: Kerim Babaoglu, Constantine G. Boojamra, Eugene J. Eisenberg, Hon Chung Hui, Richard L. Mackman, Jay P. Parrish, Michael Sangi, Oliver L. Saunders, Dustin Siegel, David Sperandio, Hai Yang
  • Patent number: 8729079
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: May 20, 2014
    Assignee: Endo Pharmaceuticals Inc.
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • Publication number: 20140135492
    Abstract: The present application includes a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.
    Type: Application
    Filed: January 17, 2014
    Publication date: May 15, 2014
    Inventors: Michael Graupe, Randall L. Halcomb
  • Publication number: 20140135315
    Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
    Type: Application
    Filed: April 9, 2013
    Publication date: May 15, 2014
    Applicant: KuDOS Pharmaceuticals Limited
    Inventor: KuDOS Pharmaceuticals Limited
  • Publication number: 20140113882
    Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R7, R8, R9, G, and X are as defined herein. This application further describes compositions comprising the same. Compounds of formula (I) and their salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.
    Type: Application
    Filed: September 27, 2013
    Publication date: April 24, 2014
    Applicants: Cancer Research Technology Limited, Cephalon, Inc.
    Inventors: Henry J. Breslin, Bruce D. Dorsey, Benjamin J. Dugan, Katherine M. Fowler, Robert L. Hudkins, Eugen F. Mesaros, Nathaniel J.T. Monck, Emma L. Morris, Ikeoluwa Olowoye, Gregory R. Ott, Gregoire A. Pave, Jonathan R. Roffey, Christelle N. Soudy, Ming Tao, Craig A. Zificsak, Allison L. Zulli
  • Publication number: 20140057901
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: February 21, 2013
    Publication date: February 27, 2014
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
  • Patent number: 8648068
    Abstract: The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: February 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thorsten Lehmann-Lintz, Joerg Kley, Norbert Redemann, Achim Sauer, Leo Thomas, Dieter Wiedenmayer, Matthias Austen, John Danilewicz, Martin Schneider, Kay Schreiter, Phillip Black, Wesley Blackaby, Ian Linney
  • Patent number: 8633183
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: January 24, 2011
    Date of Patent: January 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Siegfried Schneider, Dirk Kessler, Lars van der Veen, Tobias Wunberg
  • Publication number: 20130345192
    Abstract: The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.
    Type: Application
    Filed: October 28, 2011
    Publication date: December 26, 2013
    Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.
    Inventors: Brian T. Hopkins, Daniel Scott, Patrick Conlon, Tracy J. Jenkins, Noel Powell, Bing Guan, Julio H. Cuervo, Deping Wang, Art Taveras
  • Publication number: 20130303521
    Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.
    Type: Application
    Filed: October 26, 2012
    Publication date: November 14, 2013
    Applicant: HYDRA BIOSCIENCES, INC
    Inventor: HYDRA BIOSCIENCES, INC
  • Publication number: 20130296305
    Abstract: The present invention relates to tricyclic pyrrolo derivatives of Formula (I), which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: January 19, 2012
    Publication date: November 7, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Mauro Angiolini, Italo Beria, Maria Gabriella Brasca, Francesco Casuscelli, Roberto D'Alessio, Andrea Lombardi Borgia
  • Patent number: 8551981
    Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
    Type: Grant
    Filed: October 7, 2011
    Date of Patent: October 8, 2013
    Assignee: AbbVie Inc.
    Inventors: David J. Calderwood, Noel S. Wilson, Philip Cox, Michael Z. Hoemann, Bruce Clapham, Anil Vasudevan, Clara I. Villamil, Bin Li, Gagandeep Somal, Kelly D. Mullen
  • Publication number: 20130231331
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 5, 2013
    Inventors: Annapurna Pendri, David R. Langley, Samuel Gerritz, Guo Li, Weixu Zhai, Stanley D'Andrea, Manoj Patel, B. Narasimhulu Naidu, Kevin Peese, Zhongyu Wang
  • Publication number: 20130165428
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: February 21, 2013
    Publication date: June 27, 2013
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
  • Publication number: 20130143871
    Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
    Type: Application
    Filed: August 12, 2011
    Publication date: June 6, 2013
    Inventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
  • Publication number: 20130116236
    Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: November 6, 2012
    Publication date: May 9, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130053346
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Application
    Filed: August 23, 2012
    Publication date: February 28, 2013
    Applicant: Endo Pharmaceuticals Inc
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • Publication number: 20130029969
    Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: February 16, 2011
    Publication date: January 31, 2013
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Misaki Homma, Toru Miyazaki, Yuya Oguro, Osamu Kurasawa
  • Publication number: 20130012489
    Abstract: The invention relates to compounds of the formulae (I), (II) and (III) in which R1, R2, R3, R4, Y, W1, W2, L, A, Alk, Cyc, Ar, Het1, Het2, Hal and n have the meaning indicated in claim 1, and/or physiologically acceptable salts, tautomers and stereo-isomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of their salts.
    Type: Application
    Filed: February 17, 2011
    Publication date: January 10, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Werner Mederski, Thomas Fuchss, Frank Zenke
  • Publication number: 20120270858
    Abstract: The invention provides isoquinoline, quinoline, and quinazoline derivatives to treat a variety of disorders, diseases and pathologic conditions, and more specifically to the use of isoquinoline, quinoline, and quinazoline derivatives to inhibit the hedgehog signaling pathway and to the use of those compounds to the treatment of hyperproliferative diseases and pathologic angiogenesis.
    Type: Application
    Filed: June 9, 2010
    Publication date: October 25, 2012
    Applicant: CALIFORNIA CAPITAL EQUITY, LLC
    Inventors: Chunlin Tao, Xiaowen Sun, Hongna Han, Lukasz Koroniak, Neil Desai
  • Publication number: 20120270856
    Abstract: Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).
    Type: Application
    Filed: July 2, 2012
    Publication date: October 25, 2012
    Inventors: Tomoharu IINO, Akio OHNO, Norikazu OTAKE, Takuya SUGA, Masanori ASAI
  • Publication number: 20120252783
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: June 15, 2012
    Publication date: October 4, 2012
    Applicant: BOEHRINGER INGELHEIM PHARMA & CO. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
  • Publication number: 20120252782
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: June 15, 2012
    Publication date: October 4, 2012
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH AND CO. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
  • Publication number: 20120252791
    Abstract: The present invention relates to the field of small molecule heterocyclic inhibitors of GTP cyclohydrolase (GCH-I), or a tautomer, prodrug, or pharmaceutically acceptable salt thereof. The invention also features pharmaceutical compositions of the compounds and the medical use of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, or neuropathic pain).
    Type: Application
    Filed: September 16, 2010
    Publication date: October 4, 2012
    Inventor: Julian Blagg
  • Publication number: 20120238751
    Abstract: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
    Type: Application
    Filed: March 14, 2012
    Publication date: September 20, 2012
    Applicant: TRIUS THERAPEUTICS, INC.
    Inventors: Daniel Bensen, Zhiyong Chen, John Finn, Thanh To Lam, Suk Joong Lee, Xiaoming Li, Douglas W. Phillipson, Leslie William Tari, Michael Trzoss, Junhu Zhang, Felice C. Lightstone, Toan B. Nguyen, Sergio E. Wong, Paul Aristoff, Michael Jung