At Least Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/236)
  • Patent number: 10392392
    Abstract: The present invention provides substituted imidazo[1,2-b]pyridazines that are useful as protein kinase inhibitors and have one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. For example, a compound having the following structure: Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.
    Type: Grant
    Filed: July 11, 2018
    Date of Patent: August 27, 2019
    Assignee: Tolero Pharmaceuticals, Inc.
    Inventors: Yong Xu, Benjamin Gary Brenning, Steven G. Kultgen, Xiaohui Liu, Michael David Saunders, Koc-Kan Ho
  • Patent number: 10214545
    Abstract: The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I): in which A, E, R2, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: January 6, 2015
    Date of Patent: February 26, 2019
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Volker Schulze, Knut Eis, Florian Puehler, Ludwig Zorn, Detlev Sülzle, Philip Lienau, Antje Margret Wengner, Kirstin Petersen, Ulf Bömer
  • Patent number: 10150733
    Abstract: The present invention relates to novel amidoheteroaryl aroyl hydrazide ethynes as tyrosine kinase inhibitors, process of preparation thereof, and use of the compounds for preparation of pharmaceutical compositions in the therapeutic treatment of disorders related to tyrosine kinases in humans.
    Type: Grant
    Filed: May 18, 2016
    Date of Patent: December 11, 2018
    Assignee: SUN PHARMA ADVANCED RESEARCH COMPANY LTD.
    Inventors: Hemant Ashvinbhai Chokshi, Sabbirhusen Yusufbhai Chimanwala, Varun Anilkumar Mehta, Prabal Sengupta, Chitturi Trinadha Rao
  • Patent number: 10047093
    Abstract: The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.
    Type: Grant
    Filed: July 11, 2016
    Date of Patent: August 14, 2018
    Assignee: TOLERO PHARMACEUTICALS, INC.
    Inventors: Yong Xu, Benjamin Gary Brenning, Steven G. Kultgen, Xiaohui Liu, Michael David Saunders, Koc-Kan Ho
  • Patent number: 9988389
    Abstract: Methods are disclosed for making 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide, intermediates and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: June 5, 2018
    Assignee: Apicore US LLC
    Inventors: Ravishanker Kovi, Jayaraman Kannapan, Sanjay F. Thakor, Ashish Naik, Dhakhada Chetana Bharatbhai, Khichi Kuldip Fatehlal, Shivnath Sahebrao Patil
  • Patent number: 9981951
    Abstract: Disclosed are a novel crystalline form and an amorphous form of Olaparib, and the process for their preparation.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: May 29, 2018
    Assignee: OLON S.P.A.
    Inventors: Barbara Novo, Jacopo Bonanomi, Stella Defiore, Francesco Calogero
  • Patent number: 9868732
    Abstract: A process of synthesizing 2-bromo-LSD or a salt or hydrate thereof comprising the steps of reacting methylergometrine with a brominating agent to produce [(1S)-1-(Hydroxymethyl)propylamino][(6aR,9R)-5-bromo-7-methyl-4,7-diaza-4,6,6a,7,8,9-hexahydroacephenanthrylen-9-yl]formaldehyde as a first intermediate, and then hydrolyzing [(1S)-1-(Hydroxymethyl)propylamino][(6aR,9R)-5-bromo-7-methyl-4,7-diaza-4,6,6a,7,8,9-hexahydroacephenanthrylen-9-yl]formaldehyde to yield bromo-lysergic acid as a second intermediate, wherein bromo-lysergic acid is then amidated to yield 2-bromo-LSD or a salt or hydrate thereof.
    Type: Grant
    Filed: January 7, 2016
    Date of Patent: January 16, 2018
    Inventor: Justin Kirkland
  • Patent number: 9745310
    Abstract: The present disclosure provides a compound of Chemical Formula (1) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same: wherein X, Z, R1 and R2 are as defined in the specification. The compound of Chemical Formula (1) or pharmaceutically acceptable salt thereof acts as a positive allosteric modulator of metabotropic glutamate receptor subtype 5 (mGluR5), thereby being useful in the prevention or treatment of disorder mediated by glutamate dysfunction and mGluR5.
    Type: Grant
    Filed: February 25, 2016
    Date of Patent: August 29, 2017
    Assignee: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Chun Eung Park, Young Koo Jang, Yong Je Shin, Ji Yeon Kim, Seung Mo Ham, Yong Gil Kim, Hye Kyung Min, Soo Bong Cha, Hyo Jun Jung, Ju Young Lee, Seung Nam Han, Jin Yong Chung, Eun Ju Choi, Chan Mi Joung, Jong Sil Park, Ji Won Lee, Nahm Ryune Cho, Eun Ju Ryu, Cheol Young Maeng
  • Patent number: 9617271
    Abstract: The present invention relates to compounds of formula (I) and its use for the treatment of neurological disorders.
    Type: Grant
    Filed: May 6, 2015
    Date of Patent: April 11, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Christian Lerner
  • Patent number: 9604989
    Abstract: The present invention relates to a method for the treatment of a cancer that is sensitive to Pi3K/Akt pathway inhibition by administering a therapeutically effective amount of a compound of formula (I)
    Type: Grant
    Filed: July 6, 2015
    Date of Patent: March 28, 2017
    Assignees: BAYER INTELLECTUAL PROPERTY GMBH, BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Lars Bärfacker, William Scott, Andrea Hägebarth, Stuart Ince, Hartmut Rehwinkel, Oliver Politz, Roland Neuhaus, Hans Briem, Ulf Bömer
  • Patent number: 9255100
    Abstract: The present invention relates to substituted imidazopyridazine compounds of general formula (I), which are Mps-1 (Monopolar Spindle 1) Kinase inhibitors (also known as Tyrosine Threonine Kinase, TTK) in which R3, R5, and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: September 6, 2011
    Date of Patent: February 9, 2016
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ulrich Klar, Marcus Koppitz, Rolf Jautelat, Dirk Kosemund, Rolf Bohlmann, Philip Lienau, Gerhard Siemeister, Antje Margret Wengner
  • Patent number: 9206185
    Abstract: The application relates to imidazopyridazines of formula (I) which are useful as Akt inhibitors suitable for the treatment of cancer, and processes for their production and the use thereof.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: December 8, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Lars Bärfacker, William Scott, Andrea Hägebarth, Stuart Ince, Hartmut Rehwinkel, Oliver Politz, Roland Neuhaus, Hans Briem, Ulf Bömer
  • Patent number: 9193725
    Abstract: Compounds of Formula I are provided, including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: wherein Z is selected from the group consisting of: which are useful as HIV attachment inhibitors.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: November 24, 2015
    Assignee: Bristol-Meyers Squibb Company
    Inventors: Tao Wang, John F. Kadow, Nicholas A. Meanwell, Lawrence G. Hamann
  • Publication number: 20150148349
    Abstract: The present invention provides a compound of formula (I): a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 27, 2013
    Publication date: May 28, 2015
    Applicant: NOVARTIS AG
    Inventors: Eva Altmann, Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Jean Quancard, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
  • Patent number: 9029377
    Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
  • Patent number: 9029533
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: May 12, 2015
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
  • Publication number: 20150126506
    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: Application
    Filed: January 8, 2015
    Publication date: May 7, 2015
    Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
  • Patent number: 9024021
    Abstract: The present invention relates to novel diarylacetylene hydrazide compounds of formula (I) or pharmaceutically acceptable salt thereof, as tyrosine kinase inhibitors, the process for their preparation, and to the use of the compounds of formula (I) in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders related to tyrosine kinases, in warm-blooded animals.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: May 5, 2015
    Assignee: Sun Pharma Advanced Research Company Ltd.
    Inventors: Prabal Sengupta, Hemant Ashvinbhai Chokshi, Chetan Surjitsingh Puri, Sabbirhusen Yusufbhai Chimanwala, Varun Anilkumar Mehta, Dipali Manubhai Desai, Trinadha Rao Chitturi, Rajamannar Thennati
  • Patent number: 9023850
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: May 5, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
  • Publication number: 20150119398
    Abstract: The present invention provides the Form 2 crystalline polymorph of 7-(ieri-Butyl-d9)-3-(2,5-difluorophenyl)-6((1-methyl-1H-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine. The polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data (“XRPD”); (b) differential scanning calorimetry (“DSC”); (c) FT-Raman spectrum; (d) FT-IT spectrum; and (e) thermogravimetric analysis (TGA).
    Type: Application
    Filed: May 11, 2013
    Publication date: April 30, 2015
    Inventors: Steve Weissman, Joanna Bis, David Turnquist, David Igo
  • Patent number: 9018208
    Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-10 related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: April 28, 2015
    Assignee: Icagen Inc.
    Inventors: Thomas Eugene Christos, George S. Amato, Robert N. Atkinson, Maria Graciela Barolli, Lilli Ann Wolf-Gouveia, Mark J. Suto
  • Publication number: 20150111895
    Abstract: This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?1-GABA-A receptor antagonist and/or a ?2, ?3 and ?5 GABA-A receptor agonist.
    Type: Application
    Filed: December 23, 2014
    Publication date: April 23, 2015
    Inventor: Scott L. Harbeson
  • Publication number: 20150112061
    Abstract: Hydrazinopyridazines, fused hydrazinopyridazines, phenylethylhydrazines, or combinations thereof, compositions comprising hydrazinopyridazines, fused hydrazinopyridazines, phenyl ethylhydrazines, or combinations thereof, and methods for using them for the treatment of pain are described.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventor: Riyi Shi
  • Publication number: 20150105394
    Abstract: Compounds of Formula I are provided, including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: wherein Z is selected from the group consisting of: which are useful as HIV attachment inhibitors.
    Type: Application
    Filed: March 13, 2013
    Publication date: April 16, 2015
    Inventors: Tao Wang, John F. Kadow, Nicholas A. Meanwell, Lawrence G. Hamann
  • Publication number: 20150104526
    Abstract: The present invention relates to substituted imidazopyridazine compounds of general formula I in which R3, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: March 11, 2013
    Publication date: April 16, 2015
    Inventors: Marcus Koppitz, Ulrich Klar, Antje Margret Wengner, Roland Neuhaus, Gerhard Siemeister
  • Publication number: 20150105396
    Abstract: The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.
    Type: Application
    Filed: December 19, 2014
    Publication date: April 16, 2015
    Inventors: Kiyoyuki Omoto, Robert McKenzie Owen, David Cameron Pryde, Christine Ann Louise Watson, Mifune Takeuchi
  • Publication number: 20150104384
    Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 16, 2015
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
  • Publication number: 20150105385
    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: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: Alfredo C. CASTRO, Katrina CHAN, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Liansheng LI, Tao LIU, Yi LIU, Pingda REN, Daniel A. SNYDER, Martin R. TREMBLAY
  • Publication number: 20150099753
    Abstract: The present invention provides individual crystalline polymorphs of 7-(tert-Butyl-d9)-3-(2,5-difluorophenyl)-6-((1-methyl-1H-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine designated Form 5. The Form 5 polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data (“XRPD”); (b) differential scanning calorimetry (“DSC”); (c) FT-Raman spectroscopy; (d) FT-IR spectroscopy; and (e) thermogravimetric analysis (TGA).
    Type: Application
    Filed: May 11, 2013
    Publication date: April 9, 2015
    Inventors: David Igo, Joanna Bis, Steve Weissman, David Turnquist
  • Publication number: 20150094297
    Abstract: The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R5, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Application
    Filed: April 24, 2013
    Publication date: April 2, 2015
    Inventors: Jacques Banville, Roger Rèmillard, Edward H. Ruediger, Daniel H. Deon, Marc Gagnon, Laurence Dubé, Julia Guy, Eldon Scott Priestley, Shoshana L. Posy, Brad D. Maxwell, Pancras C. Wong, R. Michael Lawrence, Michael M. Miller
  • Publication number: 20150094300
    Abstract: The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I); in which A, R1, R2, R3, R4, R5 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: March 27, 2013
    Publication date: April 2, 2015
    Inventors: Knut Eis, Florian Puehler, Ludwig Zorn, Volker Schulze, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Kirstin Petersen, Ulf Bömer
  • Publication number: 20150094311
    Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: December 1, 2014
    Publication date: April 2, 2015
    Inventors: HENRICUS JACOBUS MARIA GIJSEN, ADRIANA INGRID VELTER, GREGOR JAMES MACDONALD, FRANCOIS PAUL BISCHOFF, TONGFEI WU, SVEN FRANCISCUS ANNA VAN BRANDT, MICHEL SURKYN, MIRKO ZAJA, SERGE MARIA ALOYSIUS PIETERS, DIDIER JEAN-CLAUDE BERTHELOT, MICHEL ANNA JOZEF DE CLEYN, DANIEL OEHLRICH
  • Patent number: 8993570
    Abstract: This invention relates to novel substituted triazolo-pyridazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?1-GABAA receptor antagonist or an ?2- and/or an ?3-GABAA receptor partial agonist.
    Type: Grant
    Filed: August 5, 2013
    Date of Patent: March 31, 2015
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Scott L. Harbeson, Roger Tung, Julie F. Liu
  • Patent number: 8993562
    Abstract: The invention provides novel imidazo[1,2-b]pyridazines of formula (I) and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoisomers thereof. Compounds of formula (I) are useful for treating or preventing diseases associated with GABAA receptors modulation, anxiety, epilepsy, sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.
    Type: Grant
    Filed: October 27, 2011
    Date of Patent: March 31, 2015
    Assignee: Ferrer Internacional, S.A.
    Inventors: José Luís Falcó, Albert Palomer, Antonio Guglietta
  • Publication number: 20150087631
    Abstract: The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I), in which A, R1, R2, R3, R4, R5 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 26, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Knut Eis, Florian Puehler, Ludwig Zorn, Volker Schulze, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Kirstin Petersen, Ulf Bömer
  • Publication number: 20150087644
    Abstract: The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 26, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Christian Lerner
  • Publication number: 20150072982
    Abstract: Disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection, with an aza-pyridone compounds. Examples of an orthomyxovirus viral infection include an influenza infection.
    Type: Application
    Filed: September 10, 2014
    Publication date: March 12, 2015
    Inventors: Robert Than Hendricks, Leonid Beigelman, David Bernard Smith, Antitsa Dimitrova Stoycheva
  • Publication number: 20150065510
    Abstract: The present application discloses Rilyazine analogs, methods for their preparation, and the treatment of cancer by the administration of an effective amount of the Rilyazine analogs to a patient in need thereof.
    Type: Application
    Filed: August 29, 2014
    Publication date: March 5, 2015
    Applicant: Warner Babcock Institute For Green Chemistry, LLC
    Inventors: John C. Warner, Jeffery A. Gladding, Thomas W. Gero, Srinivasa R. Cheruku
  • Publication number: 20150065482
    Abstract: The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Application
    Filed: August 22, 2014
    Publication date: March 5, 2015
    Applicant: GENENTECH, INC.
    Inventors: Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Jason Burch
  • Patent number: 8969345
    Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: March 3, 2015
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
  • Publication number: 20150057279
    Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Publication number: 20150051190
    Abstract: The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R1, G, T, Y1, Y2, Y3, and Y4 are as defined herein.
    Type: Application
    Filed: June 3, 2013
    Publication date: February 19, 2015
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Yasuyuki Takeda, Kenji Yoshikawa, Yoshiko Kagoshima, Yuko Yamamoto, Ryoichi Tanaka, Yuichi Tominaga, Masaki Kiga, Yoshito Hamada
  • Publication number: 20150045368
    Abstract: Compounds of Formula (I) and Formula (II) are useful inhibitors of tankyrase. Compounds of Formula (I) and Formula (II) have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: March 1, 2013
    Publication date: February 12, 2015
    Inventors: Howard Bregman, John L. Buchanan, Nagasree Chakka, Erin F. Dimauro, Hakan Gunaydin, Angel Guzman-Perez, Zihao Hua, Hongbing Huang, Xin Huang, Matthew W. Martin, Vinod F. Patel
  • Patent number: 8952058
    Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: February 10, 2015
    Assignee: Ambit Biosciences Corporation
    Inventors: Michael J. Hadd, Michael D. Hocker, Mark W. Holladay, Gang Liu, Martin W. Rowbottom, Shimin Xu
  • Patent number: 8952008
    Abstract: The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: February 10, 2015
    Assignee: Pfizer Limited
    Inventors: Kiyoyuki Omoto, Robert McKenzie Owen, David Cameron Pryde, Christine Ann Louise Watson, Mifune Takeuchi
  • Publication number: 20150038503
    Abstract: The present invention provides novel 6-substituted [1,2,4]triazolo[4,3-b]pyridazines that are agonists of Rev-Erb. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the activation of Rev-Erb has therapeutic effects, for instance in inflammatory and circadian rhythm-related disorders or cardiometabolic diseases.
    Type: Application
    Filed: September 27, 2012
    Publication date: February 5, 2015
    Applicant: GENFIT
    Inventors: Maryline Bourotte, Jean-Francois Delhomel, Mathieu Dubernet, Marie-Helene Gouy
  • Publication number: 20150038485
    Abstract: The present invention relates to heterocyclyl aminoimidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: June 21, 2012
    Publication date: February 5, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Knut Eis, Florian Pühler, Ludwig Zorn, Arne Scholz, Philip Lienau, Mark Jean Gnoth, Ulf Bömer, Judith Günther, Jörg Fanghänel, Daniel Korr
  • Publication number: 20150038506
    Abstract: The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), neurodegenerative diseases (e.g., Alzheimer's disease), metabolic diseases (e.g. diabetes), neurodevelopmental disorders (e.g. autism), or psychiatric disorders (e.g. schizophrenia or anxiety)) as well as methods of treating these diseases.
    Type: Application
    Filed: October 17, 2014
    Publication date: February 5, 2015
    Applicants: Agency for Science, Technology and Research, University of Basel
    Inventors: Kassoum Nacro, Stephane Baudouin, Peter Scheiffele
  • Publication number: 20150031672
    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: Application
    Filed: October 10, 2014
    Publication date: January 29, 2015
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • Publication number: 20150031668
    Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: July 15, 2014
    Publication date: January 29, 2015
    Inventors: Kaustav Biswas, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Vu Van Ma, Kelvin Sham, James Brown, Wenge Zhong, Thomas T. Nguyen