Isoquinolines (including Hydrogenated) Patents (Class 514/307)
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Publication number: 20150148329Abstract: Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1A2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent.Type: ApplicationFiled: June 24, 2013Publication date: May 28, 2015Inventors: Allen B. Reitz, Garry Robert Smith
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Publication number: 20150148318Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.Type: ApplicationFiled: September 26, 2014Publication date: May 28, 2015Inventors: Hoau-Yan Wang, Lindsay Burns Barbier
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Publication number: 20150141456Abstract: The present invention relates to tertiary amines of formula (I) for use in therapy, particularly for use in treating cardiovascular disorders. The compounds have been found to regulate phospholamban phosphorylation by interfering with the A-kinase anchor protein 18delta (AKAP18?) binding to the PKA substrate phospholamban. The compounds share a tri(alkylaryl/alkylheteroaryl) amine structure.Type: ApplicationFiled: November 20, 2014Publication date: May 21, 2015Inventors: Jo Klaveness, Kjetil Tasken
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Publication number: 20150140082Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.Type: ApplicationFiled: January 30, 2015Publication date: May 21, 2015Applicant: SARCODE BIOSCIENCE INC.Inventors: Thomas Gadek, John Burnier
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Publication number: 20150141424Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.Type: ApplicationFiled: January 12, 2015Publication date: May 21, 2015Inventors: Qingping ZENG, Andras TORO, John Bruce PATTERSON, Warren Stanfield WADE, Zoltan ZUBOVICS, Yun YANG, Zhipeng WU
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Publication number: 20150140076Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.Type: ApplicationFiled: January 30, 2015Publication date: May 21, 2015Applicant: SARCODE BIOSCIENCE INC.Inventors: Thomas Gadek, John Burnier
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Patent number: 9034899Abstract: Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.Type: GrantFiled: May 11, 2010Date of Patent: May 19, 2015Assignee: Albany Molecular Research, Inc.Inventors: Shuang Liu, Bruce F. Molino, Kassoum Nacro
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Publication number: 20150133427Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.Type: ApplicationFiled: October 15, 2014Publication date: May 14, 2015Applicant: Epizyme, Inc.Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
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Publication number: 20150133414Abstract: It was determined whether SNPs in SLC4A5 are associated with salt sensitivity of blood pressure (BP). Subjects consumed an isocaloric constant diet with a randomized order of 7 days low Na+ (10 mmol/d) and 7 days high Na+ (300 mmol/d) intake. Salt sensitivity was defined as a ?7 mm Hg increase in mean arterial pressure (MAP). 35 polymorphisms in 17 candidate genes were assayed. Association analyses with salt sensitivity revealed three variants that associated with salt sensitivity, two in SLC4A5 (rs7571842, rs10177833; P<0.001), and one in GRK4 (rs1801058; P=0.020). Paradoxical changes in blood pressure in response to changes in salt intake were also found associated with a SNP for DRD2 (rs6276). In conclusion, SLC4A5 variants are strongly associated with salt sensitivity of BP in Caucasian and a DRD2 SNP is a marker for paradoxical response to salt intake.Type: ApplicationFiled: April 22, 2013Publication date: May 14, 2015Applicant: University of Virginia Patent FoundationInventors: Robin A. Felder, Robert M. Carey, John E. Jones, Pedro A. Jose, Scott M. Williams
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Patent number: 9029391Abstract: 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: January 23, 2012Date of Patent: May 12, 2015Assignee: ViiV Healthcare UK LimitedInventors: Martha Alicia De La Rosa, Simon Haydar, Brian Alvin Johns, Emile Johann Velthuisen
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Publication number: 20150126529Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: January 16, 2015Publication date: May 7, 2015Inventors: Upender Velaparthi, Peiying Liu
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Publication number: 20150126517Abstract: Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: January 9, 2015Publication date: May 7, 2015Inventors: Shuang Liu, Bruce F. Molino, Kassoum Nacro
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Publication number: 20150126548Abstract: There is provided compounds for treating bone loss diseases and for preventing bone loss. Specifically the present invention relates to compounds, preferable isoquinolene derivatives.Type: ApplicationFiled: May 3, 2013Publication date: May 7, 2015Inventors: Abbas Jafari, Li Chen, Moustapha Kassem, Basem Abdallah
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Patent number: 9018207Abstract: The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.Type: GrantFiled: March 28, 2014Date of Patent: April 28, 2015Assignee: Spinifex Pharmaceuticals Pty LtdInventors: Maree Therese Smith, Bruce Douglas Wyse
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Publication number: 20150111886Abstract: The invention relates to a compound of formula (I) wherein A1, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: December 22, 2014Publication date: April 23, 2015Applicant: Hoffmann-La Roche Inc.Inventors: Atsushi Kimbara, Uwe Grether, Matthias Nettekoven, Bernd Puellmann, Mark Rogers-Evans, Tanja Schulz-Gasch
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Publication number: 20150111921Abstract: The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: I and salts thereof, wherein R1, R2, R3, R4, n, and m are as defined herein; processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; methods for treating a proliferative disease; methods for treating a disease associated with aberrant angiogenesis; methods for inhibiting angiogenesis; and processes for preparing cortistatin A, J, K, and L, and analogs thereof.Type: ApplicationFiled: June 2, 2014Publication date: April 23, 2015Applicant: President and Fellows of Harvard CollegeInventors: Alec Nathanson Flyer, Hong Myung Lee, Andrew G. Myers, Cristina Montserrat Nieto-Oberhuber, Matthew D. Shair, Chong Si
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Patent number: 9012443Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: GrantFiled: December 6, 2012Date of Patent: April 21, 2015Assignee: Amgen Inc.Inventors: Christiane Boezio, Howard Bregman, James R. Coats, Erin F. Dimauro, Thomas Dineen, Bingfan Du, Russell Graceffa, Charles Kreiman, Daniel La, Isaac E. Marx, Nagasree Chakka, Hanh Nho Nguyen, Emily Anne Peterson, Matthew Weiss, Katrina W. Copeland, Holly L. Deak, Alessandro Boezio
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Publication number: 20150105422Abstract: (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described.Type: ApplicationFiled: December 17, 2014Publication date: April 16, 2015Applicant: SPINIFEX PHARMACEUTICALS PTY LTDInventors: Thomas David McCarthy, Craig James Stewart Boyle, Alexander Redvers Eberlin, Peter Michael Kelly
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Publication number: 20150105354Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Applicants: MERCK SHARP & DOHME CORP., PHARMACOPEIA, LLCInventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, JR., John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
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Publication number: 20150098928Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A is a 6-membered aromatic ring containing carbon atoms and 0-3 nitrogen atoms as ring members, said ring optionally substituted with 1-5 substituents independently selected from R2; R1 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl or C4-C7 cycloalkylalkyl, each optionally substituted with one or more substituents independently selected from R21; R21 is independently H, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, CN or NO2; and Q is as defined in the disclosure.Type: ApplicationFiled: January 6, 2014Publication date: April 9, 2015Applicant: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Ty Wagerle, Ming Xu
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Publication number: 20150099733Abstract: Compounds represented by the following formula (I); wherein each symbol is as defined in the specification, are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.Type: ApplicationFiled: December 11, 2014Publication date: April 9, 2015Applicant: AJINOMOTO CO., INC.Inventors: Takahiro KOSHIBA, Munetaka TOKUMASU, Taisuke ICHIMARU, Koji OHSUMI, Tadakiyo NAKAGAWA, Tatsuhiro YAMADA, Kayo MATSUMOTO, Tamotsu SUZUKI
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Patent number: 9000010Abstract: The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.Type: GrantFiled: January 19, 2011Date of Patent: April 7, 2015Assignee: SanofiInventors: Ahmed Abouabdellah, Antoine Ravet
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Patent number: 8993567Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.Type: GrantFiled: March 27, 2014Date of Patent: March 31, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
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Patent number: 8993593Abstract: This invention provides a compound of formula A The compound provided herein can affect the opening of, or otherwise modulate, voltage-gated potassium channels. The compound provided herein is useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.Type: GrantFiled: February 1, 2010Date of Patent: March 31, 2015Assignee: Valeant Pharmaceuticals InternationalInventors: Jean-Michel Vernier, Martha Alicia De La Rosa, Huanming Chen, Jim Zhen Wu, Gary Lee Larson, Ian Wayne Cheney
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Patent number: 8993561Abstract: The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.Type: GrantFiled: November 18, 2011Date of Patent: March 31, 2015Assignee: SanofiInventor: Alain Pellet
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Publication number: 20150080428Abstract: The present invention relates to compounds of formula (I) in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.Type: ApplicationFiled: December 12, 2012Publication date: March 19, 2015Applicant: Novartis AGInventors: Michael Scott Visser, Naeem Yusuff
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Publication number: 20150072978Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: ApplicationFiled: November 17, 2014Publication date: March 12, 2015Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew J. Souers
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Publication number: 20150072971Abstract: The present application relates methods for treating a depressive symptom comprising administering an effective amount of a ? opioid receptor agonist or a pharmaceutically acceptable salt thereof to a subject in need thereof. Non-limiting examples of such agonist include the compounds of Formulas I, II, III, and IV, as well as the compounds of Table A.Type: ApplicationFiled: May 23, 2014Publication date: March 12, 2015Applicant: Alkermes Pharma Ireland LimitedInventors: Laura Cook Blumberg, Dan Deaver, David Eyerman, Thomas Wynn
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Patent number: 8975411Abstract: An object of the present invention is to provide a pharmaceutical agent useful for treating and preventing neurological disease, having satisfactory solubility and oxidative stress-mediated cell death suppressive activity as well as capable of exhibiting excellent blood-brain barrier permeability. The present invention is directed to an acylaminoimidazole derivative represented by general formula (I) or a salt thereof, and a pharmaceutical and a therapeutic or preventive agent for neurological disease containing the same, as an active ingredient.Type: GrantFiled: July 15, 2011Date of Patent: March 10, 2015Assignees: Neugen Pharma Inc., Wakunaga Pharmaceutical Co., Ltd.Inventors: Joh-E Ikeda, Noriaki Hirayama, Satoshi Inoue, Kazunori Tanaka, Takuya Kanno
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Patent number: 8975263Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent glucose lowering effect. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof: wherein R1 represents a C1-C3 alkyl group, each substituent R2 may be the same or different and may each represent a C1-C3 alkyl group, R3 represents an optionally substituted pyridyl group or the like, R4 and R5, which are the same or different, each represent a C1-C3 alkyl group, R6 and R7, which are the same or different, each represent a C1-C3 alkyl group, and n represents 0 to 3.Type: GrantFiled: May 30, 2014Date of Patent: March 10, 2015Assignee: Daiichi Sankyo Company, LimitedInventors: Shigeo Yamanoi, Katsuji Kagechika, Tsuyoshi Soneda, Yuichi Ochiai, Hidenori Namiki, Fuminao Doi, Madoka Hoshino, Shoko Yoshida
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Publication number: 20150065538Abstract: Compounds of formula (I) wherein R1, R2, R3, and Y are defined in the description are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: November 4, 2014Publication date: March 5, 2015Inventors: Richard J. Perner, Michael E. Kort, Stanley DiDomenico, Jun Chen, Anil Vasudevan
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Publication number: 20150065471Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.Type: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventors: Carlos Puig Duran, Francesc Carrera Carrera, Juan Bautista Pérez Garcia, Enrique Moyes Valles, Iolanda Marchueta Hereu
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Publication number: 20150065477Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.Type: ApplicationFiled: March 14, 2013Publication date: March 5, 2015Inventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Möller, Wilfried Hornberger, Gisela Backfisch, Yanbin Lao, Marjoleen Nijsen
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Patent number: 8969377Abstract: The present disclosure is directed to compounds of the structure (X): wherein: n is 2 or 3; NHE has the structure wherein: R1 is H or —SO2—NR7R8—; R2 is selected from H, —NR7(CO)R8, —SO2—NR7R8— and —NR7R8; R3 is hydrogen; R7 is hydrogen; R8 is a bond linking to L; L is a polyalkylene glycol linker; and Core has the following structure: wherein: X is selected from the group consisting of a bond, —O—, —NH—, NHC(?O)—, —NHC(?O)NH— and —NHSO2—; and Y is selected from the group consisting of a bond, optionally substituted C1-6 alkylene, optionally substituted benzene, pyridinyl, a polyethylene glycol linker and —(CH2)1-6O(CH2)1-6—, and methods of using such compounds for the treatment of irritable bowel syndrome, chronic kidney disease and end-stage renal disease.Type: GrantFiled: March 14, 2013Date of Patent: March 3, 2015Assignee: Ardelyx, Inc.Inventors: Noah Bell, Christopher Carreras, Dominique Charmot, Jeffrey W Jacobs, Michael Robert Leadbetter, Marc Navre
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Publication number: 20150057218Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: November 3, 2014Publication date: February 26, 2015Inventors: Min ZHONG, Leping LI
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Publication number: 20150057307Abstract: Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.Type: ApplicationFiled: June 23, 2014Publication date: February 26, 2015Inventors: Edward Roberts, Hugh Rosen, Steven Brown, Miguel A. Guerrero, Xuemei Peng, Ramulu Poddutoori
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Patent number: 8962654Abstract: The invention provides certain 3,4-dihydroisoquinolin-2(1H)-yl compounds, particularly compounds of formula I, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat cognitive impairment associated with Parkinson's disease or schizophrenia.Type: GrantFiled: May 27, 2014Date of Patent: February 24, 2015Assignee: Eli Lilly and CompanyInventors: Christopher David Beadle, David Andrew Coates, Junliang Hao, Joseph Herman Krushinski, Jr., Matthew Robert Reinhard, John Mehnert Schaus, Craig Daniel Wolfangel
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Publication number: 20150051194Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: ApplicationFiled: October 31, 2014Publication date: February 19, 2015Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. WENTLAND
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Publication number: 20150051226Abstract: The invention, in a first aspect relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is a 6-membered aromatic ring, or a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N, or a 6-membered benzocondensed heteroaromatic ring containing N as heteroatom, optionally each of said rings being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl, cyano, trifluoromethyl, dimethylamino, or phenyl which optionally is substituted with one or more halogen atoms, or a 5- or 6-membered heterocycle containing from one to three nitrogen atoms; X is O or N; P is pyridyl, pyrimidyl, pyrazyl, or pyridazyl, each being optionally substituted with one or more substituents selected from the group consisting of (C1-C3)alkyl, halogen, trifluoromethyl, and cyano, and use thereof as pharmaceuticals.Type: ApplicationFiled: February 28, 2013Publication date: February 19, 2015Inventors: Luigi Piero Stasi, Lucio Rovati, Roberto Artusi, Clara Bovino, Fabrizio Colace, Stefano Mandelli
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Patent number: 8957089Abstract: The present invention relates to tetrahydroisoquinoline of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are GlyT1 inhibitors.Type: GrantFiled: March 10, 2013Date of Patent: February 17, 2015Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Wilfried Braje, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles Hutchins
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Publication number: 20150045387Abstract: Bi- and tri-aromatic compounds of the formula (I) wherein R1 to RIO and X are as defined, are Nox2 inhibitors that are useful as medicaments for the treatment of a disease or condition selected from: cardiovascular diseases, respiratory diseases, inflammatory diseases, cancers, ageing and age related disorders, kidney diseases, neurodegenerative diseases, diabetes and conditions associated with diabetes. The compounds, their preparation and pharmaceutical compositions comprising them are disclosed.Type: ApplicationFiled: September 17, 2012Publication date: February 12, 2015Inventors: Jian-Mei Li, Brendan Howlin, Daniel Nathan Meijles
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Patent number: 8951536Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as pharmaceutical compositions thereof and methods of use thereof relating to the treatment of cancer and other diseases.Type: GrantFiled: February 28, 2013Date of Patent: February 10, 2015Assignee: Incyte CorporationInventors: Andrew P. Combs, Amy Takvorian, Wenyu Zhu, Richard B. Sparks
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Publication number: 20150038416Abstract: The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.Type: ApplicationFiled: June 5, 2014Publication date: February 5, 2015Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
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Patent number: 8946259Abstract: The present invention is directed to benzazole compounds that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which BACE is involved.Type: GrantFiled: October 28, 2013Date of Patent: February 3, 2015Assignee: High Point Pharmaceuticals, LLCInventors: Adnan M. M. Mjalli, David Robert Jones, Devi Reddy Gohimukkula, Guoxiang Huang, Jeff Jiqun Zhu, Mohan Rao, Robert Carl Andrews, Tan Ren
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Publication number: 20150031673Abstract: Compounds of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, R5 and T are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.Type: ApplicationFiled: July 21, 2014Publication date: January 29, 2015Inventors: Arnaud LE TIRAN, Thierry LE DIGUARHER, Jérôme-Benoît STARCK, Jean-Michel HENLIN, Anne-Françoise GUILLOUZIC, Guillaume DE NANTEUIL, Olivier GENESTE, Imre FEJES, Janos TATAI, Miklos NYERGES, James Edward Paul DAVIDSON, James Brooke MURRAY, I-Jen CHEN, Didier DURAND
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Patent number: 8940898Abstract: The present invention is directed to piperidinyl alkyne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the piperidinyl alkyne compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: GrantFiled: October 19, 2012Date of Patent: January 27, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Jason W. Skudlarek
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Patent number: 8940732Abstract: The invention relates to methods for diagnosis and treatment of autism spectrum disorders, particularly for autism spectrum disorders characterized by increased head size (circumference) and deficits in social behavior.Type: GrantFiled: January 15, 2010Date of Patent: January 27, 2015Assignee: Massachusetts Institute of TechnologyInventors: Damon Theron Page, Mriganka Sur
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Patent number: 8940737Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: GrantFiled: October 11, 2012Date of Patent: January 27, 2015Assignee: AbbVie Inc.Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew Souers
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Publication number: 20150023913Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.Type: ApplicationFiled: July 2, 2013Publication date: January 22, 2015Inventors: Piyasena Hewawasam, Omar D. Lopez, Yong Tu, Alan Xiangdong Wang, Ningning Xu, John F. Kadow, Nicholas A. Meanwell, Samayamuthula Venkata Satya Arun Kumar Gupta, Indasi J. Gopi Kumar, Suresh Kumar Ponugupati, Makonen Belema
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Publication number: 20150025044Abstract: A screening method for identifying compounds that alter the fidelity with which the initiation codon in mRNAs is recognized by the translational apparatus in eukaryotes is disclosed. This screening method was used to identify compounds having such activity. Methods of altering the fidelity of initiation codon selection are also disclosed. Methods of treating disorders characterized by single nucleotide mutations in initiation codons using compounds identified by the screening method, as well as methods of treating fungal and parasitic infections and hyperproliferative disorders using compounds identified by the screening method are also disclosed.Type: ApplicationFiled: June 30, 2014Publication date: January 22, 2015Inventors: Jon R. Lorsch, Julie Ellen Takacs, Timothy Brian Neary