Bicyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos (e.g., 1,4-benzoxazines, Etc.) Patents (Class 514/230.5)
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Patent number: 9539259Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.Type: GrantFiled: May 23, 2013Date of Patent: January 10, 2017Assignee: THE JOHNS HOPKINS UNIVERSITYInventors: Donald J. Zack, Derek Stuart Welsbie, Zhiyong Yang
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Patent number: 9532998Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.Type: GrantFiled: January 13, 2016Date of Patent: January 3, 2017Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda, Thomas Sun, Valentino J. Stella
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Patent number: 9522906Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.Type: GrantFiled: February 5, 2014Date of Patent: December 20, 2016Assignee: ACADIA PHARMACEUTICALS, INC.Inventors: Niels Skjaerbaek, Kristian Norup Koch, Bo Lennart Mikael Friberg, Bo-Ragnar Tolf
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Patent number: 9522176Abstract: The present invention provides, among other things, methods of treating phenylketonuria (PKU), including administering to a subject in need of treatment a composition comprising an mRNA encoding phenylalanine hydroxylase (PAH) at an effective dose and an administration interval such that at least one symptom or feature of PKU is reduced in intensity, severity, or frequency or has delayed in onset. In some embodiments, the mRNA is encapsulated in a liposome comprising one or more cationic lipids, one or more non-cationic lipids, one or more cholesterol-based lipids and one or more PEG-modified lipids.Type: GrantFiled: October 22, 2014Date of Patent: December 20, 2016Assignee: Shire Human Genetic Therapies, Inc.Inventors: Frank DeRosa, Michael Heartlein, Anusha Dias
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Patent number: 9518052Abstract: A compound having the structure: or a pharmaceutically acceptable salt or solvate thereof, wherein A and A? are C or N, where C may be substituted by halo or C1-C6 alkyl; R and R0 are selected from the group consisting of H, C1-C6 alkyl, —(CH2)n—W, etc., where W is 5- or 6-membered heteroaryl or heterocyclic containing N, S and/or O atoms, —NR?SO2—R?, etc., where R? and R? are C1-C6 alkyl, etc.; wherein each alkyl, etc., may be substituted; or, R and R0 and the N atom to which they are bonded together to form a monocyclic or bicyclic heterocyclic ring, etc.; R1 is H, halo or cyano; R2 and R2? are H, C1-C6 alkyl, etc.; X is a bond, etc.; R3 is H, C1-C4 alkyl, etc.; Y is a bond, —(CH2)m—, etc. The invention also relates to compositions and uses in the treatment of various diseases.Type: GrantFiled: May 13, 2015Date of Patent: December 13, 2016Assignee: Pfizer Inc.Inventors: Jotham Wadsworth Coe, Christoph Martin Dehnhardt, Peter Jones, Yogesh Anil Sabnis, Joseph Walter Strohbach, Florian Michel Wakenhut, Gavin Alistair Whitlock
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Patent number: 9505780Abstract: The invention relates to methods of treating diseases including but not limited to, cancer, non-cancer proliferative disease, sepsis, autoimmune disease, viral infaction, atheroscleosis, Type 1 or 2 diabetes, obesity, inflammatory disease, or Myc-depenent disorder including by modulating biological processes by the inhibition of PI3 kinase and/or bromodomain protein binding to substrates composing the administration of a compound(s) of Formula I-IX (or pharmaceutically acceptable salts thereof) as defined herein.Type: GrantFiled: May 4, 2015Date of Patent: November 29, 2016Assignee: SignalRx Pharmaceuticals, Inc.Inventors: Donald L. Durden, Guillermo A. Morales, Joseph R. Garlich
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Patent number: 9499537Abstract: The present invention relates to a pyrrolopyridine derivative represented by the Chemical Formula I, and a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and relates to an antiviral composition including the same as an active ingredient. The compound of the Chemical Formula I has excellent antiviral activity and selectivity for wild type and resistant HIV-1, and thereby is useful as a therapeutic agent for acquired immune deficiency syndrome (AIDS).Type: GrantFiled: May 15, 2014Date of Patent: November 22, 2016Assignee: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Jong Chan Son, Bong Jin Kim, Jae Hak Kim, Ill Young Lee, Chang Soo Yun, Sang Ho Lee, Chong Kgo Lee
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Patent number: 9481673Abstract: 6-Alkynyl-pyridine of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer.Type: GrantFiled: August 10, 2015Date of Patent: November 1, 2016Assignee: Boehringer ingelheim International GmbHInventor: Ulrich Reiser
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Patent number: 9481682Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.Type: GrantFiled: January 22, 2014Date of Patent: November 1, 2016Assignee: MERCK SHARP & DOHME CORP.Inventors: Ronald M. Kim, Jian Liu, Xiaolei Gao, Sobhana Babu Boga, Deodialsingh Guiadeen, Joseph A. Kozlowski, Wensheng Yu, Rajan Anand, Younong Yu, Oleg B. Selyutin, Ying-Duo Gao, Hao Wu, Shilan Liu, Chundao Yang, Hongjian Wang
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Patent number: 9394291Abstract: Disclosed are certain derivatives of benzoxazinone amides of formula (I), or pharmaceutically acceptable salts thereof, that act as mineralocorticoid (MR) receptor modulators that may reduce oxidative stress in endothelium and hence improve vascular function, to methods for their potential therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds.Type: GrantFiled: June 29, 2015Date of Patent: July 19, 2016Assignee: AstraZeneca ABInventors: Gavin O'Mahony, Michael Kossenjans, Karl Edman, Johan Kajanus, Karl Anders Hogner, Philip Cornwall, Andrew Turner
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Patent number: 9351948Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: GrantFiled: January 29, 2015Date of Patent: May 31, 2016Assignee: Allergan, Inc.Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
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Patent number: 9346829Abstract: The present invention provides a method of treating nicotine addiction comprising administering a 5-HT3 receptor antagonists of Formula (I):Type: GrantFiled: March 12, 2015Date of Patent: May 24, 2016Assignee: Takeda Phamaceutical Company LimitedInventors: Stephen Hitchcock, Holger Monenschein, Holly Reichard, Huikai Sun, Shota Kikuchi, Todd Macklin, Maria Hopkins
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Patent number: 9346804Abstract: The present invention relates to antibacterial compounds of formula (I) wherein “----” is a bond or is absent, V is CH, CR6 or N; R0 is H or, if “----” is a bond, may also be alkoxy; R1 is cyano, alkyl, or ethynyl; U is CH or N when “----” is a bond, or, if “----” is absent, U is CH2, NH or NH9; R2 is H, alkylcarbonyl or CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2, wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sType: GrantFiled: December 4, 2013Date of Patent: May 24, 2016Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Daniel Ritz, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 9334264Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.Type: GrantFiled: May 10, 2013Date of Patent: May 10, 2016Assignee: AbbVie Inc.Inventors: Ramzi F. Sweis, Michael L. Curtin, Marina A. Pliushchev, Todd M. Hansen, Kenton Longenecker
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Patent number: 9296723Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.Type: GrantFiled: May 10, 2013Date of Patent: March 29, 2016Assignee: AbbVie Inc.Inventors: Michael L. Curtin, Kenton Longenecker, Todd M. Hansen, Richard F. Clark, Bryan Sorensen, Howard R. Heyman, Zhiqin Ji
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Patent number: 9290487Abstract: Provided is a compound represented by the following general formula (I), or a pharmaceutically acceptable salt thereof. This novel compound has a glycogen-synthase activation ability, but activates a receptor PPAR to a low degree and is highly safe. In the formula, Ar is an aromatic carbocyclic ring or a heterocyclic ring; and Ar2 is represented by any one of the following rings and the like.Type: GrantFiled: May 2, 2014Date of Patent: March 22, 2016Assignee: AJINOMOTO CO., INC.Inventors: Tadakiyo Nakagawa, Kayo Matsumoto, Sen Takeshita, Tomomi Yoshida, Munetaka Tokumasu, Hiroki Inoue, Kaori Kobayashi
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Patent number: 9278944Abstract: The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.Type: GrantFiled: March 15, 2012Date of Patent: March 8, 2016Assignees: MITSUBISHI TANABE PHARMA CORPORATION, SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.Inventors: Toru Iijima, Hiroshi Sugama, Takayuki Kawaguchi, Jingkang Shen, Guangxin Xia, Jianshu Xie, Miki Hirai
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Patent number: 9266912Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.Type: GrantFiled: June 20, 2014Date of Patent: February 23, 2016Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda, Thomas Sun, Valentino J. Stella
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Patent number: 9249101Abstract: An object of the present invention is to provide a probe for imaging a ?-sheet structure protein which can be used for the diagnosis of conformational diseases, particularly disease (tauopathy) having a cardinal symptom such as intracerebral accumulation of tau protein, for example, Alzheimer's disease. Another object of the present invention is to provide a compound which is highly specific to tau and can image tau with satisfactory sensitivity, and also has high brain transition, low or non-recognized bone-seeking properties and low or non-recognized toxicity. According to the present invention, the above problems are solved by providing a compound of a formula I (wherein A, R1, R2, R3, R4, R5, R6, Ra and Rb are as defined in the present description) or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: October 28, 2011Date of Patent: February 2, 2016Assignee: CLINO LTD.Inventors: Yukitsuka Kudo, Shozo Furumoto, Nobuyuki Okamura
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Patent number: 9227952Abstract: The disclosure provides crystalline Sovaprevir forms. The crystalline forms of Sovaprevir comprise a Form A polymorph, a Form B polymorph, a Form C polymorph, a Form D polymorph, and a Form E polymorph. The Form A, B, C, D, and E polymorphs exhibit X-ray powder diffraction patterns having peak locations in accordance with FIGS. 1, 4, 7, 10, and 13, respectively.Type: GrantFiled: March 14, 2014Date of Patent: January 5, 2016Assignee: Achillion Pharmaceuticals, Inc.Inventor: Avinash Phadke
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Patent number: 9216983Abstract: Compounds according to Formula I, Formula II, Formula III, Formula V, Formula VI, or to Formula VII, and pharmaceutical compositions of compounds that conform to Formula IV or Formula VIII: where R1 through R33 are prescribed, selectively inhibit P. falciparum dihydroorotate dehydrogenase. Accordingly, a method for preventing and treating malaria attaches to such compounds, as well as to pharmaceutically acceptable salts, solvates, stereoisomers, tautomers, and prodrugs thereof.Type: GrantFiled: December 19, 2008Date of Patent: December 22, 2015Assignees: BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM, UNIVERSITY OF WASHINGTON, MONASH UNIVERSITYInventors: Margaret Phillips, Pradipsinh K. Rathod, Ramesh Gujjar, Alka Marwaha, Susan A. Charman
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Patent number: 9199988Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4 and A1 to A5 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.Type: GrantFiled: March 26, 2014Date of Patent: December 1, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Christian Smethurst, Harald Engelhardt, Davide Gianni, Ulrich Reiser
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Patent number: 9187476Abstract: The invention relates to a new process suitable for manufacturing the compounds of formula I (I) wherein W is H, Br, Cl or methyl, which are synthetic intermediates useful in the preparation of antibiotic compounds.Type: GrantFiled: April 26, 2013Date of Patent: November 17, 2015Assignee: Actelion Pharmaceuticals Ltd.Inventors: Stefan Abele, Hans Meier, Gunther Schmidt, Heinz Steiner
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Patent number: 9187470Abstract: Disclosed are methods of identifying, generating and synthesizing compounds that inhibit MAPK13 activity. In various embodiments, compounds, salts thereof and prodrugs thereof of the present teachings can be useful for the treatment of diseases and disorders that involve excess mucus production.Type: GrantFiled: January 16, 2015Date of Patent: November 17, 2015Assignee: Washington UniversityInventors: Michael Holtzman, Arthur Romero, Yael Alevy, Anand Patel, Thomas Brett, Dhara Patel
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Patent number: 9181232Abstract: Provided herein is a compound of formula I: as wells as a pharmaceutical composition, a process of making and a method of using a compound of formula I. The compounds of formula I are BACE1 inhibitors useful for the treatment of, for example, Alzheimer's Disease.Type: GrantFiled: June 24, 2013Date of Patent: November 10, 2015Assignee: HOFFMANN-LA ROCHE INC.Inventor: Hans Hilpert
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Patent number: 9180100Abstract: An oral methylphenidate extended release tablet is described, which can be scored and still retain its extended release profile. The tablet contains a combination of an uncoated methylphenidate-ion exchange resin complex, a barrier coated methylphenidate-ion exchange resin complex-matrix, and an uncomplexed methylphenidate active component. Following administration of a single dose of the extended release methylphenidate chewable tablet, a therapeutically effective amount of methylphenidate is reached in less than about 20 minutes and the composition provides a twelve-hour extended release profile.Type: GrantFiled: February 18, 2015Date of Patent: November 10, 2015Assignee: Tris Pharma, Inc.Inventors: Yu-Hsing Tu, Ashok Perumal, Kalyan Kathala
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Patent number: 9163023Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).Type: GrantFiled: July 10, 2013Date of Patent: October 20, 2015Assignee: ViiV Healthcare UK LimitedInventors: Martha Alicia De La Rosa, Brian Alvin Johns, Wieslaw Mieczyslaw Kazmierski, Vicente Samano, Lita Suwandi, David Temelkoff, Emile Velthuisen, Jason Gordon Weatherhead
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Patent number: 9155743Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2, R3, A, W, U and V are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: April 20, 2012Date of Patent: October 13, 2015Assignee: ASTEX THERAPEUTICS LIMITEDInventors: Ildiko Maria Buck, Gianni Chessari, Steven Howard, David Charles Rees, Alison Jo-Anne Woolford
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Patent number: 9150532Abstract: The present invention comprises processes for preparing compounds of Formula (I). wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification.Type: GrantFiled: July 24, 2014Date of Patent: October 6, 2015Assignee: JANSSEN PHARMACEUTICA NVInventors: Shawn Branum, Michael Reuman, Ronald K Russell, Christopher A. Teleha
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Patent number: 9126997Abstract: Disclosed are methods and pharmaceutical compositions for treating diseases, disorders, and conditions associated with glucocorticoid receptor (GR) expression and activity. The disclosed methods typically include administering to a patient in need thereof a proteasome inhibitor and administering to the patient in need thereof a glucocorticoid receptor (GR) agonist, either before, concurrently with, or after the proteasome inhibitor is administered.Type: GrantFiled: September 7, 2011Date of Patent: September 8, 2015Assignee: Northwestern UniversityInventors: Irina Budunova, Alexander Yemelyanov
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Patent number: 9119859Abstract: The present invention relates to methods for treating an ophthalmic, otic, or nasal infection comprising treating the infected tissue with a composition comprising finafloxacin or a finafloxacin derivative. The present invention also relates to antimicrobial compositions comprising finafloxacin or a finafloxacin derivative. The compositions are suitable for the treatment of ophthalmic, otic, or nasal infections.Type: GrantFiled: August 15, 2013Date of Patent: September 1, 2015Assignee: Alcon Research, Ltd.Inventors: David W. Stroman, Masood A. Chowhan, Kenneth C. Appell
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Patent number: 9115096Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: May 8, 2012Date of Patent: August 25, 2015Assignee: Gilead Sciences, Inc.Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Gregory Notte, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
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Patent number: 9108958Abstract: The present invention relates to novel and selective antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD as well as pain.Type: GrantFiled: July 13, 2012Date of Patent: August 18, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Stefan Scheuerer
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Patent number: 9073830Abstract: Disclosed are a novel compound or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition including the same for inhibiting human 11-?-hydroxy steroid dehydrogenase type 1 (11?-HSD1). The disclosed compound and the pharmaceutical composition including the same for inhibiting human 11-?-hydroxy steroid dehydrogenase type 1 (11?-HSD1) are excellent in activity and solubility, and is more efficient in formulation and transfer.Type: GrantFiled: August 6, 2012Date of Patent: July 7, 2015Assignee: Hyundai Pharm Co., Ltd.Inventors: Inhee Lee, Doohyeok Pyeon, Myounghyeon Shin, Jeongun Hwang, Changmin Park, Sehoan Kim, Heeil Chae, Soonyoung Moon, Soyoun Kim, Jaekeol Rhee
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Publication number: 20150148328Abstract: The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH2)m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO2 —Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)?N—ORc, —CO 2 Rd, —CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.Type: ApplicationFiled: June 21, 2013Publication date: May 28, 2015Inventors: Youssef El-Ahmad, Bruno Filoche-Romme, Jean-Philippe Letallec, Gilbert Marciniak, Baptiste Ronan, Bertrand Vivet, Maurice Brollo
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Publication number: 20150148341Abstract: The present invention provides octahydro fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: November 21, 2014Publication date: May 28, 2015Inventors: Hazel Hunt, Iain Walters, Benoit Gourdet
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Publication number: 20150148340Abstract: The present application relates to novel bicyclically substituted uracil derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases.Type: ApplicationFiled: May 3, 2013Publication date: May 28, 2015Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Chantal Fürstner, Jens Ackerstaff, Alexander Straub, Heinrich Meier, Hanna Tinel, Katja Zimmermann, Adrian Tersteegen, Dmitry Zubov, Raimund Kast, Jens Schamberger, Martina Schäfer, Kirsten Börngen
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Publication number: 20150148327Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: June 17, 2013Publication date: May 28, 2015Applicant: Merck Canada Inc.Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
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Publication number: 20150148342Abstract: The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: ApplicationFiled: November 26, 2014Publication date: May 28, 2015Applicant: INCYTE CORPORATIONInventors: Eddy W. Yue, Andrew P. Combs, Brent Douty
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Patent number: 9040527Abstract: Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.Type: GrantFiled: July 23, 2013Date of Patent: May 26, 2015Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Andy Atuegbu, John Ramphal, Hui Li, Marina Gelman, Jeffrey Clough, Carlos Valdez, Somasekhar Bhamidipati, Sambaiah Thota, Darren McMurtrie
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Patent number: 9040532Abstract: Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor. The compounds can include a naphthalene, a quinoline, a benzoimidazole or an isoquinoline as a core structure. Methods of making, using and formulating these compounds are described.Type: GrantFiled: October 6, 2010Date of Patent: May 26, 2015Assignee: Allergan, Inc.Inventors: Ken Chow, Liming Wang, Wenkui K. Fang, Evelyn G. Corpuz, Santosh C. Sinha, Daniel W. Gil, Mohammad I. Dibas, John E. Donello
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Publication number: 20150141396Abstract: The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases.Type: ApplicationFiled: July 3, 2013Publication date: May 21, 2015Applicant: Ares Trading S.A.Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Patrick Gerber, Mathilde Muzerelle
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Publication number: 20150141407Abstract: The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.Type: ApplicationFiled: May 30, 2013Publication date: May 21, 2015Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Lan Xie, Xiaofeng Wang, Kuo-Hsiung Lee
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Publication number: 20150133437Abstract: The invention provides tetrahydro[1,8]naphthyridine and related compounds, methods of promoting RORy activity and/or increasing the amount of iL-17 in a subject, and therapeutic uses of the tetrahydro[1,8]naphthyridine and related compounds. In particular, the invention provides sulfonamide-tetrahydro[1,8]naphthyridine and related compounds, methods of using such compounds to promote RORy activity and/or increase the amount of iL-17 in a subject, and treat medical conditions in which activation of immune response would be beneficial such as in cancer and infections.Type: ApplicationFiled: May 8, 2013Publication date: May 14, 2015Inventors: Thomas D. Aicher, Peter L. Toogood, Xiao Hu
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Publication number: 20150132258Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.Type: ApplicationFiled: November 14, 2014Publication date: May 14, 2015Inventor: George D. Hartman
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Publication number: 20150133429Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.Type: ApplicationFiled: January 14, 2015Publication date: May 14, 2015Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
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Publication number: 20150133426Abstract: The present invention relates to substituted pyrrolopyrimidine compounds general formula I: in which A, X, R1, R2, m and n are as described and defined herein, 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: ApplicationFiled: May 17, 2013Publication date: May 14, 2015Inventors: Ulrich Klar, Georg Kettschau, Detlev Sülzle, Florian Puehler, Dirk Kosemund, Philip Lienau, Ulf Bömer, Lars Wortmann
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Publication number: 20150133440Abstract: The present invention provides difluoro-cyclopentaoxazinyls and difluoroenzooxazinyls of formula (I) having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.Type: ApplicationFiled: June 24, 2013Publication date: May 14, 2015Applicant: Hoffmann-La Roche Inc.Inventor: Hans Hilpert
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Patent number: 9029366Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: June 19, 2013Date of Patent: May 12, 2015Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Miguel Angel Pena-Piñón, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
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Patent number: 9029367Abstract: The present invention provides a compound of Formula III: Formula III wherein A is: and Z, R1, R2, R3, and R4 are as defined herein, or a pharmaceutically acceptable salt thereof, which is useful for treating Alzheimer's disease.Type: GrantFiled: June 11, 2014Date of Patent: May 12, 2015Assignee: Eli Lilly and CompanyInventors: Steven James Green, Erik James Hembre, Dustin James Mergott, Yuan Shi, Brian Morgan Watson, Leonard Larry Winneroski, Jr.