The Additional Hetero Ring Is A 1,3-diazine Ring (including Hydrogenated) Patents (Class 514/263.21)
  • Patent number: 10358449
    Abstract: The present invention relates to a Xanthine derivative as shown in formula (I), wherein, R is selected from: R1 is selected from cyano or methoxycarbonyl; R2 is selected from hydrogen and halogen atoms, a linear or branched C1-6 alkyl group which is substituted or unsubstituted by 1 to 5 halogen atoms, a linear or branched C1-6 alkoxy group which is substituted or unsubstituted by 1 to 5 halogen atoms; X and Y are each independently selected from C or N; and n is 0, 1, 2, 3 or 4.
    Type: Grant
    Filed: May 26, 2016
    Date of Patent: July 23, 2019
    Assignee: Jiangsu Tasly Diyi Pharmaceutical Co, LTD.
    Inventors: Yuzhe Gao, Guocheng Wang
  • Patent number: 10214519
    Abstract: The present application provides the compounds of formula I or IA or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein s, t, m, n, R1, R2, R3, R4, R5, R6 and R7 are as described herein.
    Type: Grant
    Filed: September 21, 2017
    Date of Patent: February 26, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Jayaraman Chandrasekhar, Julian Andrew Codelli, Devan Naduthambi, Leena Patel, Stephane Perreault, Gary Phillips, Kassandra F. Sedillo, Jennifer Anne Treiberg, Joshua Van Veldhuizen, William J. Watkins
  • Patent number: 10154972
    Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Grant
    Filed: October 31, 2016
    Date of Patent: December 18, 2018
    Assignee: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain D. Baron, Mark S. Fineman, Nigel R. A. Beeley
  • Patent number: 10034877
    Abstract: 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: Grant
    Filed: October 6, 2016
    Date of Patent: July 31, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Ruth Harper, Hans-Juergen Woerle
  • Patent number: 10028923
    Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Grant
    Filed: October 31, 2016
    Date of Patent: July 24, 2018
    Assignee: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain D. Baron, Mark S. Fineman, Nigel R. A. Beeley
  • Patent number: 9879011
    Abstract: The present invention relates to an amorphous form of linagliptin and processes for the preparation thereof. The invention also relates to a pharmaceutical composition comprising a therapeutically effective amount of an amorphous form of linagliptin and use of the composition for treatment of diabetes especially type-I or type-II, prediabetes or reduction of glucose tolerance.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: January 30, 2018
    Assignee: Cadila Healthcare Limited
    Inventors: Shriprakash Dhar Dwivedi, Ashok Prasad, Kuldeep Natwarlal Jain, Kumar Kamlesh Singh, Jitendra Maganbhai Gajera
  • Patent number: 9765060
    Abstract: The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (J), or pharmaceutically acceptable salts thereof, in which A, n, m, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms. The present disclosure further provides pharmaceutical compositions that include a compound of formula (J), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms.
    Type: Grant
    Filed: June 23, 2015
    Date of Patent: September 19, 2017
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Jerry Evarts, Joshua Kaplan, Musong Kim, Devan Naduthambi, Leena Patel, Stephane Perreault, Gary Phillips, Lafe J. Purvis, II, Kirk L. Stevens, Jennifer A. Treiberg
  • Patent number: 9708327
    Abstract: Polymorphs of a hydrochloride salt of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are disclosed. Solvent forms of a hydrochloride salt of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are also disclosed.
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: July 18, 2017
    Assignee: GILEAD CALISTOGA LLC
    Inventors: Suzanne Buttar, Ernest Carra, Tracy Ehiwe, Duong Tran, Fang Wang, Christopher Worrall, Jerry Evarts
  • Patent number: 9556180
    Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: January 31, 2017
    Assignee: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Robert Mah, Keiichi Masuya, Achim Schlapbach, Andrea Vaupel
  • Patent number: 9545367
    Abstract: Cosmetic and dermatological compositions comprising N-heteroarylbisamide analogs and methods of using such compositions to impart anti-aging benefits to the skin and/or improve skin conditions resulting from reduced collagen and hyaluronic acid production are disclosed. The N-heteroarylbisamides are believed to stimulate collagen and hyaluronic acid production and restore or maintain homeostasis for these compounds.
    Type: Grant
    Filed: April 30, 2015
    Date of Patent: January 17, 2017
    Assignee: AVON PRODUCTS, INC.
    Inventors: Satish Parimoo, Nancy T. Ilaya, John W. Lyga
  • Patent number: 9518059
    Abstract: The present invention relates to new crystalline forms of the inhibitor, 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazoline-4-one; the present invention also relates to methods for preparing the new crystalline forms of 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one, pharmaceutical compositions containing the new crystalline forms thereof, and uses thereof for the treatment and/or prevention of diseases such as chronic lymphocytic leukemia and indolent non-Hodgkin's lymphoma.
    Type: Grant
    Filed: December 2, 2015
    Date of Patent: December 13, 2016
    Assignee: HANGZHOU PUSHAI PHARMACEUTICAL TECHNOLOGY
    Inventors: Zhonghua Zhang, Xiaoxia Sheng, Xiaohong Sheng
  • Patent number: 9499479
    Abstract: This invention provides a compound having the structure: wherein R1 is H, halogen, —NR5R6, —NR5—C(?O)—R6, —NH—C(?O)—OR7, —OR7, —NO2, —CN, —SR7, —SO2R7, —CO2R7, CF3, —SOR7, —POR7, —C(?S)R7, —C(?O)—NR5R6, —CH2—C(?O)—NR5R6, —C(?NR5)R6, —P(?O)(OR5)(OR6), —P(OR5)(OR6), —C(?S)R7, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, aryl, heteroaryl, or heterocyclyl, wherein R5, R6, and R7 and are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; m is an integer from 0 to 2; R2 and R3 are each, independently, H, halogen, —NH2, —CX3, —C(?O)OR8, C(?O)R8, —C(?O)NR9R10, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, heteroalkyl, aryl, heteroaryl, or heterocyclyl; wherein X is Cl, Br, or F; R8, R9 and R10 are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; Q is —Ar1—Z— or —Z—Ar1—Z—, wherein Ar1 is aryl or heteroaryl; and each occurrence of Z is independently present or
    Type: Grant
    Filed: October 3, 2012
    Date of Patent: November 22, 2016
    Assignees: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK, SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Ronald Breslow, Paul A. Marks
  • Patent number: 9481642
    Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Grant
    Filed: August 4, 2014
    Date of Patent: November 1, 2016
    Assignee: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain D. Baron, Mark S. Fineman, Nigel R. A. Beeley
  • Patent number: 9394308
    Abstract: This disclosure describes novel compounds and pharmaceutical compositions for inhibiting the TRPA1 ion channel and/or medical conditions related to TRPA1, such as pain and respiratory conditions.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: July 19, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Qingyi Li, Lily Cheng, Christopher M. Liu, Iwona E. Wrona, Blaise S. Lippa, Chester A. Metcalf, III, Andrew J. Jackson, Lauren M. Chapman
  • Patent number: 9388183
    Abstract: 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: Grant
    Filed: October 10, 2014
    Date of Patent: July 12, 2016
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • Patent number: 9381199
    Abstract: The present invention provides a novel amorphous solid dispersion of linagliptin in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: July 5, 2016
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy, Bandi Vamsi Krishna
  • Patent number: 9212183
    Abstract: The present invention relates to novel salt forms of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, processes for making these novel salts, and pharmaceutical compositions comprising such novel salts. The invention also relates to the use of these novel salts in the treatment of type 2 diabetes.
    Type: Grant
    Filed: May 9, 2014
    Date of Patent: December 15, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Peter Sieger, Waldemar Pfrengle
  • Patent number: 9199998
    Abstract: The present invention relates to substituted quinazolines of formula (I) wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: December 1, 2015
    Assignee: Boehringer Ingelheim Internatioal GmbH
    Inventors: Waldemar Pfrengle, Markus Frank, Thomas Klein
  • Patent number: 9173859
    Abstract: The specification describes the use of selected DPP IV inhibitors for the treatment of physiological functional disorders and for reducing the risk of the occurrence of such functional disorders in at-risk patient groups. In addition, the use of the above-mentioned DPP IV inhibitors in conjunction with other active substances is described, by means of which improved treatment outcomes can be achieved. These applications may be used to prepare corresponding medicaments.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: November 3, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Dugi, Frank Himmelsbach, Michael Mark
  • Publication number: 20150148345
    Abstract: Provided herein are methods, compositions, and kits for treating myeloproliferative disorders or neoplasms, including polycythemia vera, primary myelofibrosis, thrombocythemia, and essential thrombocythemia.
    Type: Application
    Filed: November 25, 2014
    Publication date: May 28, 2015
    Inventors: Brian Lannutti, Sarah Meadows, Christophe Queva, Matthew Robert Warr, James Andrew Whitney
  • Patent number: 9029384
    Abstract: The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which n, m, R1, R2, and R3 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: Grant
    Filed: December 20, 2013
    Date of Patent: May 12, 2015
    Assignee: Gilead Calistoga, LLC.
    Inventors: Jerry Evarts, Leena Patel, Joshua Kaplan, Jennifer A. Treiberg, Stephane Perreault, Gary Phillips
  • Publication number: 20150105318
    Abstract: Methods of using antidiabetic medications which are suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance, and hyperglycemia, among others.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 16, 2015
    Inventors: Eva GRAEFE-MODY, Hans-Juergen WOERLE
  • Publication number: 20150105383
    Abstract: 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: Application
    Filed: October 8, 2014
    Publication date: April 16, 2015
    Applicant: Acetylon Pharmaceuticals, Inc.
    Inventors: Steven Norman Quayle, Simon Stewart Jones
  • Publication number: 20150099768
    Abstract: There is provided inter alia a dry powder pharmaceutical formulation for inhalation comprising: (i) 6-(2-((4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl) methyl)-3-(2-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-5-yl)-N,N-bis(2-methoxyethyl)hex-5-ynamide or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof and solvates thereof in particulate form as active ingredient; (ii) particulate lactose as carrier; and (iii) a particulate stabilizing agent selected from metal salts of stearic acid such as magnesium stearate and metal salts of stearyl fumarate.
    Type: Application
    Filed: March 13, 2013
    Publication date: April 9, 2015
    Inventors: Rudy Laurent Maria Broeckx, Walter Ferdinand Maria Filliers, Patrick Hubert J. Nieste, Alex Herman Copmans, Filip Marcel C. Vanhoutte, Carina Leys
  • Publication number: 20150093391
    Abstract: A method of treating cancer or metastasis is provided involving administering at least one oncostatin M (OSM) antagonist to a subject, wherein the subject has been diagnosed with cancer. Administration of an OSM antagonist such as a small molecule pharmaceutical is provided as well as an anti-OSM antibody, an anti-OSM aptamer, and an OSM mRNA antagonist. The OSM antagonists were found to inhibit or prevent tumor cell detachment, proliferation and metastasis in several cancer types.
    Type: Application
    Filed: September 5, 2014
    Publication date: April 2, 2015
    Applicant: BOISE STATE UNIVERSITY
    Inventors: Cheryl Jorcyk, Dong Xu
  • Publication number: 20150087585
    Abstract: Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H-imidazo[4,5-d]pyrazine of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
    Type: Application
    Filed: March 26, 2013
    Publication date: March 26, 2015
    Applicant: PFIZER INC.
    Inventors: Kay Ahn, Markus Boehm, Shawn Cabral, Philip A. Carpino, Kentaro Futatsugi, David Hepworth, Daniel W. Kung, Suvi Orr, Jian Wang
  • Publication number: 20150065431
    Abstract: The present invention provides methods of reducing cutaneous scar formation by treating a cutaneous wound with a composition comprising a therapeutic agent that is a sodium channel blocker and/or an inhibitor of the Nax/SCN7A pathway. The present invention also provides wound cover components impregnated with such compositions, kits composed of such compositions with a wound dressing or sterile wipe, and mixtures of such compositions with a topical component (e.g., cream, ointment, or gel) suitable for application to a cutaneous wound. The present invention also provides compositions, kits, devices, and methods for treating skin conditions (e.g., dermatitis, psoriasis, or other skin conditions) with such compositions and devices. Examples of such therapeutic agents include, but are not limited to, an inhibitor of a gene or protein selected from: ENac, COX-2, PGE2, PI3K, PKB, Nax Prss8, IL-1?, IL-8, SAPK, Erk gene, p38 gene, PAR2, S100A8, S100A9, S100A12.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 5, 2015
    Inventors: Wei Xu, Seok Jong Hong, Robert D. Galiano, Thomas A. Mustoe
  • Patent number: 8962636
    Abstract: The present invention relates to substituted quinazolines of formula (I) wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV(DPP-IV).
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: February 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Markus Frank, Thomas Klein
  • Publication number: 20150051228
    Abstract: The present invention relates to an amorphous form of linagliptin and processes for the preparation thereof. The invention also relates to a pharmaceutical composition comprising therapeutically effective amount of an amorphous form of linagliptin and use of said composition for treatment of diabetes especially type-I or type-II, prediabetes or reduction of glucose tolerance.
    Type: Application
    Filed: March 12, 2013
    Publication date: February 19, 2015
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Shriprakash Dhar Dwivedi, Ashok Prasad, Kuldeep Natwarlal Jain, Kumar Kamlesh Singh, Jitendra Maganbhai Gajera
  • Publication number: 20150025089
    Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.
    Type: Application
    Filed: October 6, 2014
    Publication date: January 22, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Waldemar PFRENGLE, Thorsten PACHUR, Thomas NICOLA, Adil DURAN
  • Publication number: 20150011545
    Abstract: The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.
    Type: Application
    Filed: July 15, 2014
    Publication date: January 8, 2015
    Applicant: AstraZeneca AB
    Inventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle Laurae LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
  • Publication number: 20140378398
    Abstract: The invention relates to a pharmaceutical combination comprising the compound of formula I or pharmaceutically acceptable salts thereof in combination with at least one second therapeutic agent 2. The pharmaceutical combination of the invention is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Bradford S. HAMILTON, Thomas RAUCH, Manami TSUTSUMI
  • Publication number: 20140378479
    Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.
    Type: Application
    Filed: May 21, 2014
    Publication date: December 25, 2014
    Applicant: ICOS CORPORATION
    Inventors: Edward A. KESICKI, Kerry W. FOWLER, Danwen HUANG, Hua Chee OOI, Amy OLIVER, Kamal Deep PURI, Fuqiang RUAN, Jennifer TREIBERG
  • Publication number: 20140371243
    Abstract: The present invention relates to the use of a certain DPP-4 inhibitor along with angioplasty or stenting, and/or to its use for treating and/or preventing restenosis from angioplasty or stenting.
    Type: Application
    Filed: June 13, 2014
    Publication date: December 18, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Thomas KLEIN, Takashi NOMIYAMA, Yuichi TERAWAKI, Toshihiko YANASE
  • Publication number: 20140343014
    Abstract: The present invention relates to the use of a combination of a certain DPP-4 inhibitor and an alpha-glucosidase inhibitor for use in therapy, e.g. for use in treating and/or preventing a metabolic disease such as type 2 diabetes mellitus and/or conditions related thereto. The invention also relates to the use of such combination for improving body weight control, reducing body weight, inducing satiety, inhibiting gastric emptying and/or reducing food intake, in a patient in need thereof.
    Type: Application
    Filed: May 16, 2014
    Publication date: November 20, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thomas KLEIN, Michael MARK
  • Patent number: 8883805
    Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: November 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Thorsten Pachur, Thomas Nicola, Adil Duran
  • Publication number: 20140323441
    Abstract: The present invention relates to purine derivatives of formula (I), processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Application
    Filed: November 8, 2012
    Publication date: October 30, 2014
    Inventors: Jean-François Bonfanti, Frédéric Marc Maurice Doublet, Werner Embrechts, Jérôme Michel Claude Fortin, David Craig Mc Gowan, Philippe Muller, Piere Jean-Marie Bernand Raboisson
  • Patent number: 8865730
    Abstract: Polymorphs of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are disclosed.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: October 21, 2014
    Assignee: Gilead Calistoga LLC
    Inventors: Ernest Carra, Michael Gerber, Bing Shi, Keiko Sujino, Duong Tran, Fang Wang, Jerry B. Evarts
  • Patent number: 8865729
    Abstract: The present invention relates to novel salt forms of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, a DPP-4 inhibitor and their use in pharmaceutical compositions useful in the treatment of type 2, diabetes, as well as their production.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: October 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Peter Sieger, Waldemar Pfrengle
  • Publication number: 20140303194
    Abstract: The present invention relates to novel salt forms of a certain DPP-4 inhibitor and their use in pharmaceutical compositions useful in the treatment of type 2 diabetes, as well as their production.
    Type: Application
    Filed: May 9, 2014
    Publication date: October 9, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Peter SIEGER, Waldemar PFRENGLE
  • Patent number: 8853156
    Abstract: 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: Grant
    Filed: August 5, 2009
    Date of Patent: October 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Ruth Harper, Hans-Juergen Woerle
  • Publication number: 20140296260
    Abstract: The invention relates to novel quinazolinone compounds and their use as inhibitors of PI3 kinases, for example, PI3K?, for treating and/or preventing diseases, disorder, and conditions associated with modulating PI3 kinase activity. Novel 3-aryl-2-((arylamino)methyl)quinazolin-4(3H)-one derivatives and pharmaceutically acceptable salts or solvates thereof and their use for the treatment or prevention of diseases, disorders, and conditions associated with the activity of one or more PI3 kinase, such as PI3K?, are disclosed.
    Type: Application
    Filed: March 28, 2014
    Publication date: October 2, 2014
    Inventors: Ben C. Askew, Takeru Furuya
  • Patent number: 8846695
    Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for improving glycemic control in type 2 diabetes patients with inadequate glycemic control despite metformin therapy.
    Type: Grant
    Filed: January 7, 2010
    Date of Patent: September 30, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Klaus Dugi
  • Publication number: 20140274890
    Abstract: 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: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Klaus DUGI, Eva Ulrike GRAEFE-MODY, Ruth HARPER, Hans-Juergen WOERLE
  • Publication number: 20140274889
    Abstract: The present invention relates to a certain DPP-4 inhibitor for use in cardio- and/or renoprotective therapy, including in patients at high vascular risk.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Odd-Erik JOHANSEN, Maximilian VON EYNATTEN, Thomas KLEIN, Hans-Juergen WOERLE
  • Publication number: 20140228283
    Abstract: The present invention relates to substituted quinazolines of formula (I) wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-W (DPP-IV).
    Type: Application
    Filed: July 13, 2012
    Publication date: August 14, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Waldemar Pfrengle, Markus Frank, Thomas Klein
  • Publication number: 20140221400
    Abstract: The present invention relates to the use of MPO inhibitors for the treatment of multiple system atrophy. The present invention also relates to the use of MPO inhibitors for the treatment of Huntington's disease. The present invention also relates to the use of MPO inhibitors for neuroprotection.
    Type: Application
    Filed: November 8, 2013
    Publication date: August 7, 2014
    Applicant: ASTRAZENECA AB
    Inventors: Hakan Eriksson, Werner Poewe
  • Publication number: 20140213630
    Abstract: The present invention provides, inter alia, methods for treating, preventing, or ameliorating the effects of a lymphoid malignancy, such as those associated with a mutated phosphatase and tensin homolog (PTEN) gene, or T-cell acute lymphoblastic leukemia (T-ALL). These methods include administering to a subject an effective amount of a phosphoinositide 3-kinase-delta (PI3K?) inhibitor and a phosphoinositide 3-kinase-gamma (PI3K?) inhibitor. The present invention also provides pharmaceutical compositions for treating the effects of a lymphoid malignancy. This invention further provides a method for identifying a subject who may benefit from co-treatment with a PI3K? inhibitor and a PI3K? inhibitor. This method includes determining from a sample of the subject whether the subject has a mutated PTEN gene. Additionally, this invention provides methods for identifying a compound that has both PI3K? and PI3K? inhibitory activity.
    Type: Application
    Filed: February 29, 2012
    Publication date: July 31, 2014
    Inventor: Thomas Diacovo
  • Publication number: 20140206650
    Abstract: This disclosure describes novel compounds and pharmaceutical compositions for inhibiting the TRPA1 ion channel and/or medical conditions related to TRPA1, such as pain and respiratory conditions.
    Type: Application
    Filed: January 21, 2014
    Publication date: July 24, 2014
    Inventors: Blaise S. Lippa, Qingyi Li, Lily Cheng, Christopher M. Liu, Iwona E. Wrona, Chester A. Metcalf, III, Andrew J. Jackson
  • Patent number: 8785454
    Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.
    Type: Grant
    Filed: November 4, 2011
    Date of Patent: July 22, 2014
    Assignee: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Troy Edward Wilson