The Additional Hetero Ring Is A 1,3-diazine Ring (including Hydrogenated) Patents (Class 514/263.21)
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Patent number: 8846695Abstract: 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: GrantFiled: January 7, 2010Date of Patent: September 30, 2014Assignee: Boehringer Ingelheim International GmbHInventor: Klaus Dugi
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Publication number: 20140274889Abstract: 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: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Odd-Erik JOHANSEN, Maximilian VON EYNATTEN, Thomas KLEIN, Hans-Juergen WOERLE
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Publication number: 20140274890Abstract: 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: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Klaus DUGI, Eva Ulrike GRAEFE-MODY, Ruth HARPER, Hans-Juergen WOERLE
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SUBSTITUTED QUINAZOLINES, THE PREPARATION THEREOF AND THE USE THEREOF IN PHARMACEUTICAL COMPOSITIONS
Publication number: 20140228283Abstract: 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: ApplicationFiled: July 13, 2012Publication date: August 14, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Waldemar Pfrengle, Markus Frank, Thomas Klein -
Publication number: 20140221400Abstract: 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: ApplicationFiled: November 8, 2013Publication date: August 7, 2014Applicant: ASTRAZENECA ABInventors: Hakan Eriksson, Werner Poewe
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Publication number: 20140213630Abstract: 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: ApplicationFiled: February 29, 2012Publication date: July 31, 2014Inventor: Thomas Diacovo
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Publication number: 20140206650Abstract: 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: ApplicationFiled: January 21, 2014Publication date: July 24, 2014Inventors: Blaise S. Lippa, Qingyi Li, Lily Cheng, Christopher M. Liu, Iwona E. Wrona, Chester A. Metcalf, III, Andrew J. Jackson
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Patent number: 8785455Abstract: The present invention relates to a novel polymorph of Linagliptin benzoate and to methods for its preparation. Furthermore the present invention relates to the use of the novel polymorph for the preparation of a medicament. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel polymorph of Linagliptin benzoate.Type: GrantFiled: May 9, 2012Date of Patent: July 22, 2014Assignee: Sandoz AGInventors: Andreas Hotter, Arthur Pichler
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Patent number: 8785454Abstract: 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: GrantFiled: November 4, 2011Date of Patent: July 22, 2014Assignee: Intellikine LLCInventors: Pingda Ren, Yi Liu, Liansheng Li, Troy Edward Wilson
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Publication number: 20140179718Abstract: 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: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: GILEAD CALISTOGA LLCInventors: Jerry EVARTS, Leena PATEL, Joshua KAPLAN, Jennifer A. TREIBERG, Stephane PERRAULT, Gary PHILLIPS
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Publication number: 20140163048Abstract: This disclosure describes solid forms of the compound of Formula (I) and pharmaceutical compositions for inhibiting the TRPA1 ion channel and/or medical conditions related to TRPA1, such as pain.Type: ApplicationFiled: August 9, 2013Publication date: June 12, 2014Applicant: Cubist Pharmaceuticals, Inc.Inventors: Nicholas Barker, Jian-Qiao Gu, Gaauri NAIK, Jan-Ji LAI, Stephen MACHATHA, You Seok Hwang, Pradip M. Pathare
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Publication number: 20140158116Abstract: This disclosure describes novel compounds and pharmaceutical compositions for inhibiting the TRPA1 ion channel and/or medical conditions related to TRPA1, such as asthma.Type: ApplicationFiled: August 9, 2013Publication date: June 12, 2014Applicant: Cubist Pharmaceuticals, Inc.Inventors: Jayhong A. Chong, Scott C. Coleman, Rory Curtis, Donato del Camino, Yu Gui Gu, Qingyi Li, Blaise S. Lippa, Chester A. Metcalf, III, Magdalene M. Moran, Michael D. Ryan, Dong Zou
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Publication number: 20140155394Abstract: 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: ApplicationFiled: June 21, 2013Publication date: June 5, 2014Applicant: Astrazeneca ABInventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
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Publication number: 20140135348Abstract: 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: ApplicationFiled: January 22, 2014Publication date: May 15, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Klaus DUGI, Frank HIMMELSBACH, Michael MARK
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Publication number: 20140128402Abstract: The present invention discloses a pharmaceutical combination comprising Hydroxychloroquine and a DPP-IV inhibitor or their pharmaceutically acceptable salts, solvates or prodrugs thereof, for preventing, slowing the progression of, delaying, improving, restoring, or treating a condition or a disease resulting from metabolic disorders.Type: ApplicationFiled: January 10, 2014Publication date: May 8, 2014Applicant: IPCA Laboratories LimitedInventors: Anil PAREEK, Gopakumar G. NAIR
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Publication number: 20140121224Abstract: 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: ApplicationFiled: October 8, 2013Publication date: May 1, 2014Applicant: ICOS CORPORATIONInventors: Kerry W. FOWLER, Danwen HUANG, Edward A. KESICKI, Hua Chee OOI, Amy OLIVER, Fuqiang RUAN, Jennifer TREIBERG, Kamal Deep PURI
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Publication number: 20140121223Abstract: 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: ApplicationFiled: October 8, 2013Publication date: May 1, 2014Applicant: ICOS CORPORATIONInventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg, Kamal Deep Puri
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Publication number: 20140121225Abstract: The present invention relates to a novel polymorph of Linagliptin benzoate and to methods for its preparation. Furthermore the present invention relates to the use of the novel polymorph for the preparation of a medicament. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel polymorph of Linagliptin benzoate.Type: ApplicationFiled: May 9, 2012Publication date: May 1, 2014Applicant: SANDOZ AGInventors: Andreas Hotter, Arthur Pichler
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Publication number: 20140100236Abstract: The present invention relates inter alia to the use of selectively moisture-adjusted tabletting material in the preparation of mechanically stable oral tablets which contain at least one hydrate-forming active substance and/or adjuvant relevant to the mechanical stability of the tablets, particularly arginine-containing oral tablets.Type: ApplicationFiled: October 8, 2013Publication date: April 10, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Maria BUSL, Eduard BALTHES
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Patent number: 8691829Abstract: The invention provides methods to treat certain liver disorders by administering a compound that inhibits PD K isoforms, particularly the delta isoform. It further provides specific compounds useful for these methods and ways to identify subjects who are particularly suitable for receiving these treatments.Type: GrantFiled: July 21, 2010Date of Patent: April 8, 2014Assignee: Gilead Calistoga LLCInventor: Roger G. Ulrich
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Publication number: 20140079781Abstract: The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and pioglitazone, processes for the preparation thereof, and their use to treat certain diseases.Type: ApplicationFiled: November 22, 2013Publication date: March 20, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Peter SCHNEIDER, Thorsten NEUHAUS
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Publication number: 20140080799Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.Type: ApplicationFiled: September 20, 2013Publication date: March 20, 2014Applicant: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
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Patent number: 8673927Abstract: 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: GrantFiled: November 15, 2010Date of Patent: March 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Klaus Dugi, Frank Himmelsbach, Michael Mark
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Patent number: 8664232Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: April 17, 2012Date of Patent: March 4, 2014Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz, Mohammad Tadayyon
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Publication number: 20140057901Abstract: 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: ApplicationFiled: February 21, 2013Publication date: February 27, 2014Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
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Patent number: 8653089Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: February 8, 2012Date of Patent: February 18, 2014Assignee: F. Hoffmann-La Roche AGInventors: Robert Heald, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Bohdan Waszkowycz
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Patent number: 8629102Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: GrantFiled: March 15, 2013Date of Patent: January 14, 2014Assignee: Mochida Pharmaceutical Co., Ltd.Inventor: Munetaka Ohkouchi
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Publication number: 20140005198Abstract: The present invention comprises a new class of compounds capable of modulating the activity of Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein each of A1, A2, A3, A4, A5, A6, A7, A8, A9, bond B, X, rings Z1 and Z2, R1 and R3 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: August 28, 2013Publication date: January 2, 2014Applicant: AMGEN INC.Inventors: Adrian L. SMITH, Elizabeth M. DOHERTY, Qi HUANG, Gang LIU
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Publication number: 20130344138Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administration of a compound of formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such compound admixed with at least one pharmaceutically acceptable excipient.Type: ApplicationFiled: August 28, 2013Publication date: December 26, 2013Applicant: GILEAD CALISTOGA LLCInventors: Kamal D. PURI, Jerry B. EVARTS, Brian LANNUTTI, Neill GIESE
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Publication number: 20130324463Abstract: The present invention relates to the use of a certain DPP-4 inhibitor for modifying food intake and regulating food preference.Type: ApplicationFiled: May 21, 2013Publication date: December 5, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thomas KLEIN, Michael MARK
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Publication number: 20130317046Abstract: The present invention relates to methods for treating and/or preventing autoimmune diabetes, particularly LADA, as well as diseases related or associated therewith, comprising the administration of an effective amount of a certain DPP-4 inhibitor, as well as to the use of a certain DPP-4 inhibitor for modifying disease trajectory of autoimmune diabetes (particularly LADA).Type: ApplicationFiled: May 21, 2013Publication date: November 28, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Odd-Erik JOHANSEN
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Publication number: 20130310398Abstract: Combinations of DPP-4 inhibitors with GPR119 agonists, as well as to the use of these combinations for treating and/or preventing metabolic diseases, particularly diabetes (especially type 2 diabetes mellitus) and conditions related thereto.Type: ApplicationFiled: July 24, 2013Publication date: November 21, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Michael MARK, Peter EICKELMANN, Gerd LUIPPOLD, Leo THOMAS
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Publication number: 20130303554Abstract: The present invention relates to methods for treating and/or preventing SIRS and/or sepsis comprising the administration of an effective amount of a certain DPP-4 inhibitor, as well as to the use of a certain DPP-4 inhibitor for treating and/or preventing a metabolic disease in a patient with or at risk of SIRS and/or sepsis.Type: ApplicationFiled: May 13, 2013Publication date: November 14, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thomas KLEIN, Andreas DAIBER, Klaus DUGI, Michael MARK, Thomas MUENZEL
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Publication number: 20130303462Abstract: The present invention relates to methods for treating and/or preventing podocytes related disorders and/or nephrotic syndrome comprising the administration of an effective amount of a certain DPP-4 inhibitor, as well as to the use of a certain DPP-4 inhibitor for treating and/or preventing a metabolic disease in a patient with or at risk of podocytes related disorders and/or nephrotic syndrome.Type: ApplicationFiled: May 13, 2013Publication date: November 14, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thomas KLEIN, Maximilian von EYNATTEN, Berthold HOCHER, Michael MARK, Yuliya SHARKOVSKA
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Publication number: 20130281373Abstract: The present invention relates to methods for treating and/or preventing metabolic diseases comprising the combined administration of a GLP-1 receptor agonist and a DPP-4 inhibitor.Type: ApplicationFiled: May 5, 2011Publication date: October 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thomas Klein, Rolf Grempler, Michael Mark
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Publication number: 20130274273Abstract: This disclosure describes a novel compounds and pharmaceutical compositions for inhibiting the TRPA1 ion channel and/or medical conditions related to TRPA1, such as pain.Type: ApplicationFiled: March 15, 2013Publication date: October 17, 2013Applicant: Cubist Pharmaceuticals, Inc.Inventors: Chester A. Metcalf, III, Yu Gui Gu, Spencer D. Kimball, Qingy Li, Blaise S. Lippa, Dominic Ryan, Xinyuan Wu, Dong Zou
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Publication number: 20130252976Abstract: 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: ApplicationFiled: March 5, 2013Publication date: September 26, 2013Applicant: GILEAD CALISTOGA LLCInventors: Ernest CARRA, Michael GERBER, Bing SHI, Keiko SUJINO, Duong TRAN, Fang WANG
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Publication number: 20130225552Abstract: Heterobicyclic compounds of Formula (I): or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.Type: ApplicationFiled: February 28, 2013Publication date: August 29, 2013Applicant: AMGEN INC.Inventor: Amgen Inc.
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Publication number: 20130210721Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: MOCHIDA PHARMACEUTICAL CO., LTD.
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Publication number: 20130196898Abstract: The present invention relates to methods for preventing or treating of metabolic disorders and related conditions, such as in certain patient groups.Type: ApplicationFiled: November 26, 2010Publication date: August 1, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Michael Mark, Hans-Juergen Woerle, Heike Zimdahl-Gelling
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Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions
Publication number: 20130184204Abstract: 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: ApplicationFiled: July 13, 2012Publication date: July 18, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Waldemar PFRENGLE, Markus FRANK, Thomas KLEIN -
Publication number: 20130178485Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.Type: ApplicationFiled: March 1, 2013Publication date: July 11, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Waldemar PFRENGLE, Thorsten PACHUR, Thomas NICOLA, Adil DURAN
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Publication number: 20130172244Abstract: The present invention relates to methods for treating and/or preventing metabolic diseases comprising the subcutaneous or transdermal administration of a therapeutically effective amount of a certain DPP-4 inhibitor. The invention further relates to a subcutaneous combination of a certain DPP-4 inhibitor and GLP-1 having a short half life, particularly for reducing weight.Type: ApplicationFiled: December 27, 2012Publication date: July 4, 2013Inventors: Thomas KLEIN, Michael MARK
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Patent number: 8476285Abstract: The invention relates to compounds of Formulae I-III: and therapeutic uses thereof, wherein A is chosen from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carbocyclic group; B is chosen from a substituted or unsubstituted piperidine, homopiperidine, piperazine, pyrrolidine or azetidine group; R1 is chosen from hydro, alkyl, aryl, heteroaryl, amino, or halo; and L1, L2, are as defined herein.Type: GrantFiled: June 30, 2009Date of Patent: July 2, 2013Assignee: Myrexis, Inc.Inventors: Ashok C. Bajji, Se-Ho Kim, Benjamin Markovitz, Richard Trovato, Rajendra Tangallapally, Mark B. Anderson, Daniel Wettstein, Mark Shenderovich, John A. Vanecko
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Publication number: 20130165427Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: ApplicationFiled: August 24, 2012Publication date: June 27, 2013Applicant: HYDRA BIOSCIENCES, INC.Inventor: Jayhong A. Chong
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Publication number: 20130143902Abstract: Provided are methods that relate to a novel therapeutic strategy for the treatment of cancers. In particular, the method comprises administration of Compound A, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such compound admixed with at least one pharmaceutically acceptable excipient.Type: ApplicationFiled: November 30, 2012Publication date: June 6, 2013Applicant: GILEAD CALISTOGA LLCInventor: Gilead Calistoga LLC
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Publication number: 20130137629Abstract: Various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis can be treated with a compound selected from an incretin mimetic and a dipeptidyl peptidase IV inhibitor in combination with a Compound of Formula I or a pharmaceutically acceptable salt thereof Three of R1, R2, R3, R4 and R5 are hydrogen and the remainder are independently selected from the group consisting of hydrogen, halo, hydroxy, methyl, ethyl, perfluoromethyl, methoxy, ethoxy, and perfluoromethoxy; and m is 0, 2 or 4. R6 is hydrogen, O or hydroxy, and X is —OR7, wherein R7 is hydrogen or alkyl having from 1 to 3 carbon atoms; or R6 is hydrogen, and X is —NR8R9, wherein R8 is hydrogen or hydroxy and R9 is hydrogen, methyl or ethyl. When X is —NR8R9, hydroxy none of R1, R2, R3, R4 and R5 is hydroxy.Type: ApplicationFiled: January 24, 2013Publication date: May 30, 2013Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventor: WELLSTAT THERAPEUTICS CORPORATION
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Publication number: 20130122089Abstract: The present invention relates to pharmaceutical compositions of DPP IV inhibitors with an amino group, their preparation and their use to treat diabetes mellitus.Type: ApplicationFiled: January 7, 2013Publication date: May 16, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Anja Kohlrausch, Patrick Romer, Gerd Seiffert
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Publication number: 20130123282Abstract: The present invention provides solid state forms of Linagliptin, processes for preparing the solid state forms, and pharmaceutical compositions thereof.Type: ApplicationFiled: November 15, 2012Publication date: May 16, 2013Inventors: Leonid Metsger, Revital Burstein, Ariel Mitteman, Motti Erlich, Slavik Yurkovsky
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Patent number: 8440677Abstract: The invention provides compounds, compositions and methods to treat certain inflammatory conditions and/or oncology by administering a compound that inhibits PI3K isoforms, particularly the delta isoform. It further provides specific stereoisomers of a compound useful for these methods. In particular, the compound is an optically active atropisomer of 2-((6-amino-9H-purin-9-yl)methyl)-5-methyl-3-o-tolylquinazolin-4(3H)-one.Type: GrantFiled: March 24, 2010Date of Patent: May 14, 2013Assignee: Gilead Calistoga LLCInventors: Jerry B. Evarts, Roger G. Ulrich