Quinoline Or Isoquinoline (including Hydrogenated) Patents (Class 544/363)
  • QUINOLINE DERIVATIVE AND QUINAZOLINE DERIVATIVE INHIBITING SELF-PHOSPHORYLATION OF HEPATOCYTUS PROLIFERATOR RECEPTOR, AND MEDICINAL COMPOSITION CONTAINING THE SAME
    Publication number: 20110105747
    Abstract: An objective of the present invention is to provide compounds having potent antitumor activity. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X=CH or N; Z=O or S; L=O or S; M=CR10R11, wherein R10 and R11=H, alkyl, or alkoxy, NR12 wherein R12=H or alkyl; R1, R2, and R3=H or optionally substituted alkoxy; R4=H; R5-8=H, halogen, alkoxy or the like; and R9=alkyl optionally substituted by -T-R15, or —NR16R17 wherein T=O, S, or NH; R14=an optionally substituted carbocyclic or heterocyclic ring; and R15-17=alkyl or an optionally substituted carbocyclic or heterocyclic ring, or —NR18R19 wherein R18 and R19=H, optionally substituted alkyl, or an optionally substituted carbocylic or heterocyclic ring, or optionally substituted carbocyclic or heterocyclic ring.
    Type: Application
    Filed: January 10, 2011
    Publication date: May 5, 2011
    Applicant: KIRIN BEER KABUSHIKI KAISHA
    Inventors: Yasunari FUJIWARA, Terufumi Senga, Tsuyoshi Nishitoba, Tatsushi Osawa, Atsushi Niwa, Kazuhide Nakamura
  • QUINOLINE OR ISOQUINOLINE SUBSTITUTED P2X7 ANTAGONISTS
    Publication number: 20110092481
    Abstract: The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.
    Type: Application
    Filed: April 21, 2009
    Publication date: April 21, 2011
    Inventors: Christopher John Love, Joseph Elisabeth Leenaerts, Ludwig Paul Cooymans, Donald Alec Labsack, Bryan James Branstetter, Jason Christopher Rech, Elizabeth Ann Gleason, Jennifer Diane Venable, Danielle Wiener, Deborah Margaret Smith, James Guy Breitenbucher
  • Pyridinone derivative for the treatment of premature ejaculation
    Patent number: 7928108
    Abstract: The invention provides 3-(methyloxy)-1-{4-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]butyl}-2(1H)-pyridinone of formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 3, 2008
    Date of Patent: April 19, 2011
    Assignee: Glaxo Group Limited
    Inventors: Gabriella Gentile, Valeria Zucchelli
  • NOVEL QUINOLINYLAMIDE DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE AND SEROTONIN RECEPTORS
    Publication number: 20110085978
    Abstract: This invention provides novel quinolinylamide derivatives having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, 5HT1A and 5-HT2A receptor subtypes, and in particular useful for the treatment of neuropsychiatric disorders, incl. schizophrenia.
    Type: Application
    Filed: March 13, 2009
    Publication date: April 14, 2011
    Applicant: NeuroSearch A/S
    Inventors: Dan Peters, Lars Christian Rønn, Karin Sandager Nielsen, Jørgen Scheel-Krüger
  • PIPERAZINYL OXOALKYL TETRAHYDROISOQUINOLINES AND RELATED ANALOGUES
    Publication number: 20110082130
    Abstract: Piperazinyl oxoalkyl tetrahydroisoquinolines and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
    Type: Application
    Filed: August 23, 2010
    Publication date: April 7, 2011
    Applicant: LIGAND PHARMACEUTICALS, INC.
    Inventors: Yang Gao, Bingsong Han, Yuelian Xu, Timothy M Caldwell, Linghong Xie
  • Pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound
    Patent number: 7919494
    Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.
    Type: Grant
    Filed: August 19, 2009
    Date of Patent: April 5, 2011
    Assignee: Astellas Pharma, Inc.
    Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
  • Pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound
    Patent number: 7919495
    Abstract: To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: April 5, 2011
    Assignee: Astellas Pharma, Inc.
    Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
  • KINASE INHIBITORS
    Publication number: 20110077237
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: April 1, 2010
    Publication date: March 31, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Juan-Miguel Jimenez, Guy W. Bemis, Francois Maltais, Tiansheng Wang, Ronald Knegtel, Chris Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Mortimore
  • Urotensin II receptor antagonists
    Patent number: 7915260
    Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.
    Type: Grant
    Filed: January 10, 2007
    Date of Patent: March 29, 2011
    Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
  • HETEROARYL-SUBSTITUTED 1,3-DIHYDROINDOL-2-ONE DERIVATIVES AND MEDICAMENTS CONTAINING THEM
    Publication number: 20110071156
    Abstract: The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6, and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.
    Type: Application
    Filed: July 20, 2010
    Publication date: March 24, 2011
    Applicant: Abbott GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Hornberger, Herve Geneste, Daryl Richard Sauer, Wolfgang Wernet, Andrea Hager-Wernet, Liliane Unger, Wilfried Lubisch
  • Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
    Patent number: 7910589
    Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous aripiprazole crystals is stored for an extended period.
    Type: Grant
    Filed: April 26, 2007
    Date of Patent: March 22, 2011
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Takuji Bando, Satoshi Aoki, Junichi Kawasaki, Makoto Ishigami, Youichi Taniguchi, Tsuyoshi Yabuuchi, Kiyoshi Fujimoto, Yoshihiro Nishioka, Noriyuki Kobayashi, Tsutomu Fujimura, Masanori Takahashi, Kaoru Abe, Tomonori Nakagawa, Koichi Shinhama, Naoto Utsumi, Michiaki Tominaga, Yoshihiro Ooi, Shohei Yamada, Kenji Tomikawa
  • THERAPEUTIC PIPERAZINES
    Publication number: 20110065691
    Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.
    Type: Application
    Filed: September 22, 2010
    Publication date: March 17, 2011
    Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
  • NOVEL AGENTS OF CALCIUM ION CHANNEL MODULATORS
    Publication number: 20110065703
    Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.
    Type: Application
    Filed: March 12, 2008
    Publication date: March 17, 2011
    Inventor: Jay Jie-Qiang Wu
  • Inhibitors of bruton's tyrosine kinase
    Patent number: 7906509
    Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: wherein, variables R, X, Y1, Y2, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: March 15, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Joshua Kennedy-Smith, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth, Zachary Kevin Sweeney, Joshua Paul Gergely Taygerly
  • NOVEL ARYL PIPERAZINE DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE AND SEROTONIN RECEPTORS
    Publication number: 20110059019
    Abstract: This invention provides novel aryl piperazine derivatives having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, 5HT1A and 5-HT2A receptor subtypes, and in particular useful for the treatment of neuropsychiatric disorders, incl. schizophrenia.
    Type: Application
    Filed: January 29, 2009
    Publication date: March 10, 2011
    Applicant: NeuroSearch A/S
    Inventors: Dan Peters, Lars Christian Rønn, Karin Sandager Nielsen, Jørgen Scheel-Krüger
  • DUAL ACTION ANTIBIOTICS
    Publication number: 20110059946
    Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:
    Type: Application
    Filed: September 10, 2010
    Publication date: March 10, 2011
    Applicant: Morphochem Aktiengesellschaft fuer Kombinatorische Chemie
    Inventors: Christian Hubschwerlen, Jean-Luc Specklin
  • Crystalline aripiprazole solvates
    Patent number: 7902198
    Abstract: Alcoholates of aripiprazole are useful as pharmaceuticals and/or as intermediates in making aripiprazole Form A or Form B.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: March 8, 2011
    Assignee: Synthon BV
    Inventors: Gerrit Jan Ettema, Raymond Westheim, Faysal Kalmoua
  • FUSED PYRIDINES ACTIVE AS INHIBITORS OF C-MET
    Publication number: 20110053935
    Abstract: Fused pyridines of formula (I) and the pharmaceutically acceptable salts thereof have activity as inhibitors of c-Met and may thus be used to treat various diseases and disorders including cancer. Processes for synthesizing the compounds are also described.
    Type: Application
    Filed: January 26, 2009
    Publication date: March 3, 2011
    Inventors: Adrian John Folkes, Paul Goldsmith, Neil Anthony Pegg
  • INHIBITORS OF THE BMP SIGNALING PATHWAY
    Publication number: 20110053930
    Abstract: The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.
    Type: Application
    Filed: March 13, 2009
    Publication date: March 3, 2011
    Applicants: The Brigham and Women's Hospital, Inc., The General Hospital Corporation
    Inventors: Paul B. Yu, Gregory D. Cuny, Kenneth D. Bloch, Randall T. Peterson, Charles C. Hong
  • METHODS FOR SYNTHESIZING HETEROCYCLIC COMPOUNDS.
    Publication number: 20110046376
    Abstract: A method for synthesizing a heterocyclic compound includes: reacting 1-methylpiperazine with 5-chloro-2-nitroaniline at an internal temperature sufficient to provide a compound of Formula VIH The 1-methylpiperazine and the 5-chloro-2-nitroaniline are reacted in a solvent that comprises water in an amount greater than 50 percent by volume based on the amount of the solvent and/or are reacted in a solvent that comprises an organic solvent component that has a boiling point of greater than 100° C. at atmospheric pressure.
    Type: Application
    Filed: May 17, 2006
    Publication date: February 24, 2011
    Applicant: NOVARTIS AG
    Inventors: Gabriel Galvin, Eric Harwood, David Ryckman, Shuguang Zhu
  • 1-[(2?-substituted)-piperazin-1? -yl]-isoquinolines as norepinephrine transporter inhibitor therapeutics and positron emission tomography imaging agents
    Patent number: 7887784
    Abstract: Racemic mixtures and enantiomerically pure forms of novel 1-[(2?-substituted)-piperazin-1?-yl]-isoquinolines are norepinephrine (NE) transporter (NET) inhibitor compounds. Compounds of the invention are considered therapeutic agents for central nervous system (CNS) diseases and disorders, without limitation, including neurodegeneration, anxiety, depression, attention deficit disorders, drug dependency, and post traumatic stress disorder. Examples of the chemical syntheses of the compounds of the invention are provided. The isoquinoline compounds of the invention competitively bind at NET at nanomolar concentrations. The isoquinoline agents of the invention bind selectively to NET over other competitive transporter targets and receptor binding sites, including those of serotonin and dopamine, amongst others. The chemical syntheses of the invention are suitable for labeling with radionuclide atoms.
    Type: Grant
    Filed: March 21, 2008
    Date of Patent: February 15, 2011
    Assignee: University of Montana
    Inventors: John M. Gerdes, David B. Bolstad, Michael R. Braden, August W. Barany
  • Piperazine-substituted benzothiophenes for treatment of mental disorders
    Patent number: 7888362
    Abstract: The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Grant
    Filed: April 12, 2006
    Date of Patent: February 15, 2011
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Yamashita, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Hideaki Kuroda, Haruka Takahashi, Satoshi Shimizu, Tatsuyoshi Tanaka
  • Salts of aripiprazole
    Patent number: 7884205
    Abstract: The present invention relates to acid addition salts of aripiprazole, a process for preparing said acid addition salts and their use to prepare or purify aripiprazole in the form of a free base or in the form of a pharmaceutically acceptable salt.
    Type: Grant
    Filed: January 27, 2006
    Date of Patent: February 8, 2011
    Assignee: Sandoz AG
    Inventors: Johannes Ludescher, Hubert Sturm
  • INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
    Publication number: 20110028464
    Abstract: Compounds of formula I: wherein c, R2, R3, R4, R5, R6, R7 and R8 are defined herein, are useful as inhibitors of HIV replication.
    Type: Application
    Filed: November 3, 2008
    Publication date: February 3, 2011
    Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBH
    Inventors: Youla S. Tsantrizos, Murray D. Bailey, François Bilodeau, Rebekah J. Carson, Lee Fader, Teddy Halmos, Stephen Kawai, Serge R. Landry, Steven Laplante, Bruno Simoneau
  • Crystalline Forms and Two Solvated Forms of 4-Amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one Lactic Acid Salts
    Publication number: 20110021536
    Abstract: Crystalline forms or polymorphs of 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one lactic acid salts, as well as to methods of making the same, pharmaceutical compositions comprising the same and methods of treatment using the same.
    Type: Application
    Filed: March 18, 2009
    Publication date: January 27, 2011
    Applicant: NORVARTIS AG
    Inventors: Danielle Giron, Walter Hammerschmidt, Philippe Piechon, Johanne Polasek, Andreas Schreiner, Frank Stowasser
  • HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF NEUROLOGICAL AND PSYCHOLOGICAL DISORDERS
    Publication number: 20110015156
    Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.
    Type: Application
    Filed: June 24, 2010
    Publication date: January 20, 2011
    Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
  • AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS
    Publication number: 20110015171
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Application
    Filed: April 22, 2010
    Publication date: January 20, 2011
    Inventors: Haiyan BIAN, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Intermediates useful for the preparation of aripiprazole and methods for the preparation of the novel intermediates and aripiprazole
    Patent number: 7872132
    Abstract: An improved process for the preparation of aripiprazole (1) which comprises (i) reacting 6-hydroxy-l-indanone (11) with 1,4-dihalobutane (12) in the presence of a base and a solvent at a temperature in the range of 90 to 110 deg C to form the novel intermediate 6-(4-halo butoxy)-indan-1-one (3), (ii) reacting the novel intermediate with 1-(2,3-clichlorophenyl)-piperazine (9) to get another novel intermediate 6-[4-[4-(2,3-dichlorophenyl)-l-piperazinyl]butoxy]-indan-l-one (2) and (iii) reacting the resulting novel compound with sodium azide. The invention also relates to the novel intermediates of the formulae (2) & (3) and processes for their preparation. The invention also includes intermediate compounds useful for the preparation of aripiprazole.
    Type: Grant
    Filed: October 8, 2004
    Date of Patent: January 18, 2011
    Assignee: Suven Life Sciences Limited
    Inventors: Rajendiran Chinnapillai, Veera Reddy Arava, Venkata Subba Rao Athukuru, Venkateswarlu Jasti
  • Enantiomers of 2'-Fluoralkyl-6-nitroquipazine as Serotonin Transporter Positron Emission Tomography Imaging Agents and Antidepressant Therapeutics
    Publication number: 20110009419
    Abstract: Racemic mixtures and individual enantiomers of fluorine-18 or carbon-11 radiolabelled 2?-alkyl-6-nitroquipazine ligands are serotonin transporter (SERT) tracers for positron emission tomography (PET) imaging. The non-radioactive ligand forms possess therapeutic antidepressant in vitro and in vivo pharmacological binding profiles in rodent brain and cells expressing human serotonin transporter (hSERT). Twelve 2?-alkyl-6-nitroquipazine ligands potently bind in sub-nanomolar concentrations to the pre-synaptic SERT binding site where established antidepressant drugs bind and inhibit the re-uptake of the neurotransmitter serotonin (5-HT). In vivo tracer studies in rats as well as monkey PET scan trial have demonstrated the fluorine-18 and carbon-11 positron radionuclide labeled tracers perform as quantitative tracers of specific binding the SERT protein in live brain.
    Type: Application
    Filed: September 22, 2010
    Publication date: January 13, 2011
    Inventors: John M. Gerdes, David B. Bolstad, Brian R. Kusche
  • PRODRUGS OF NH-ACIDIC COMPOUNDS
    Publication number: 20110003828
    Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.
    Type: Application
    Filed: June 24, 2010
    Publication date: January 6, 2011
    Inventors: Laura Cook Blumberg, Julius F. Remenar, Örn Almarsson, Tarek A. Zeidan
  • ENROFLOXACIN HEXAHYDRATE
    Publication number: 20110003829
    Abstract: The present invention relates to a novel hexahydrate of enrofloxacin, to processes for its preparation, to pharmaceuticals containing it, and to its use in combating diseases.
    Type: Application
    Filed: January 18, 2008
    Publication date: January 6, 2011
    Applicant: BAYER ANIMAL HEALTH GMBH
    Inventors: Alfons Grunenberg, Clemens Bothe, Birgit Keil
  • Human Adam-10 Inhibitors
    Publication number: 20110003812
    Abstract: Magnesium salts/complexes of compounds useful for inhibiting the ADAM-IO protein and methods of making and purifying them are provided. Further provided are compositions comprising magnesium salts/complexes of the compounds in combination with a pharmaceutically acceptable carrier. The compounds well as such compositions comprising them are useful for the treatment of cancer, arthritis, diseases related to angiogenesis, such as renal diseases, heart diseases, such as heart failure, atherosclerosis, and stroke, inflammation, ulcer, infertility, scleroderma, endometriosis, mesothelioma, and diabetes. In addition, methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role are provided.
    Type: Application
    Filed: October 15, 2008
    Publication date: January 6, 2011
    Applicant: SYMPHONY EVOLUTION, INC.
    Inventors: Sriram Naganathan, JoAnn Wilson, Daniel Dickman
  • THERAPEUTIC COMPOUNDS AND COMPOSITIONS
    Publication number: 20100331307
    Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Application
    Filed: June 29, 2010
    Publication date: December 30, 2010
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders, Shunqi Yan
  • Cyanoisoquinoline
    Patent number: 7858620
    Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides a process for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.
    Type: Grant
    Filed: September 11, 2008
    Date of Patent: December 28, 2010
    Assignee: H. Lundbeck A/S
    Inventors: Jan Kehler, Jacob Nielsen, Morten Langgaard
  • Substituted imidazole 4-carboxamides as cholecystokinin-1 receptor modulators
    Patent number: 7858629
    Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.
    Type: Grant
    Filed: April 10, 2007
    Date of Patent: December 28, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Scott Edmondson, Alexa Hansen, Cheng Zhu
  • Substituted tetrahydroisochinolines as MMP inhibitors, related production method and use as medicine
    Patent number: 7858619
    Abstract: The present invention is directed to a compound of formula (I), wherein R1, R2, R3, R4, A, L and n are as defined herein, its pharmaceutical composition, preparation and uses as a MMP inhibitor.
    Type: Grant
    Filed: September 27, 2007
    Date of Patent: December 28, 2010
    Assignee: sanofi-aventis
    Inventors: Armin Hofmeister, Manfred Schudok, Hans Matter, Kristin Breitschopf, Antonio Ugolini
  • CRYSTALLINE FORMS OF 4-[(2,4-DICHLORO-5-METHOXYPHENYL)AMINO]-6-METHOXY-7-[3-(4-METHYL-1-PIPERAZINYL)PROPOXY]-3-QUINOLINECARBONITRILE AND METHODS OF PREPARING THE SAME
    Publication number: 20100324066
    Abstract: This invention is directed to a crystalline 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile monohydrate having an x-ray diffraction pattern wherein 2? angles (°) of significant peaks are at about: 9.19, 11.48, 14.32, 19.16, 19.45, 20.46, 21.29, 22.33, 23.96, 24.95, 25.29, 25.84, 26.55, 27.61, and 29.51, and a transition temperature of about 109° C. to about 115° C.
    Type: Application
    Filed: June 22, 2010
    Publication date: December 23, 2010
    Applicant: Wyeth LLC
    Inventors: Marc Sadler Tesconi, Gregg Feigelson, Henry Strong, Hong Wen
  • AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS
    Publication number: 20100324012
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Application
    Filed: April 22, 2010
    Publication date: December 23, 2010
    Inventors: Haiyan BIAN, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS
    Publication number: 20100324011
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Application
    Filed: April 22, 2010
    Publication date: December 23, 2010
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • 5-Quinoline derivatives having an anti-bacterial activity
    Publication number: 20100324030
    Abstract: The present invention describes novel anti-bacterial compounds of the formula (I). These compounds are, amongst others, of interest as inhibitors of DNA gyrase and topoisomerases, for example of topoisomerase II and IV.
    Type: Application
    Filed: April 11, 2008
    Publication date: December 23, 2010
    Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische Chemie
    Inventors: Glenn Dale, Sabine Pierau, Michael W. Cappi, Christopher Gray, Christian Hubschwerlen, Jean P. Surivet, Cornelia Zumbrunn
  • AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS
    Publication number: 20100324013
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Application
    Filed: April 22, 2010
    Publication date: December 23, 2010
    Inventors: Haiyan BIAN, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Monomaleate Monohydrate Salt of a 5HT1A Receptor Antagonist
    Publication number: 20100317672
    Abstract: The present invention relates to a monomaleate monohydrate salt of 7-methyl-6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4,5-dihydroimidazo[1,5-a]quinoline-3-carboxamide, uses of the salt as a medicament in the treatment of sexual dysfunction and pharmaceutical compositions and dosage forms comprising the salt.
    Type: Application
    Filed: January 15, 2009
    Publication date: December 16, 2010
    Applicant: GLAXO GROUP LIMITED
    Inventors: Clare Louise Anderton, Grahame Robert Woollam
  • HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20100317624
    Abstract: Compounds of formula (IA) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
    Type: Application
    Filed: June 7, 2010
    Publication date: December 16, 2010
    Inventors: Allison Laura CHOY, Ann EAKIN, Olga QUIROGA, Brian SHERER
  • PROCESS FOR PREPARING ANHYDROUS ARIPIRAZOLE TYPE I
    Publication number: 20100317857
    Abstract: Type I anhydrous aripiprazole is prepared by dissolving aripiprazole (or an acid salt thereof) in an alcoholic solvent, optionally containing water, at elevated temperature, adding seed crystals of Type 1 anhydrous aripiprazole to the solution, cooling the mixture, and isolating crystals aripiprazole and drying the isolated crystals to obtain low moisture Type 1 anhydrous aripiprazole.
    Type: Application
    Filed: October 24, 2007
    Publication date: December 16, 2010
    Applicant: CAMBREX CHARLES CITY, INC.
    Inventor: Brian T. Becicka
  • MONTELUKAST BENZHYDRYL PIPERAZINE SALTS AND PROCESS FOR PREPARATION THEREOF
    Publication number: 20100292251
    Abstract: The invention relates to Benzhydryl piperazine salts of [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid represented by the formula (III). Furthermore, the invention relates to the use of Benzhydryl piperazine salts of [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid represented by the formula (III) for the preparation of substantially pure [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropane acetic acid or its alkali salts and pharmaceutical composition comprising the same.
    Type: Application
    Filed: January 5, 2009
    Publication date: November 18, 2010
    Applicant: Torrent Pharmaceuticals Limited
    Inventors: Nitin Ashok Shimpi, Mahendra Gordhanbhai Lakkad, Sunil Sadanand Nadkarni, Srinivasa Rao A.v.v.
  • Tetrahydroisoquinoline sulfonamide derivatives, the preparation thereof, and the use of the same in therapeutics
    Patent number: 7833999
    Abstract: The invention relates to tetrahydroisoquinoline sulfonamide compounds (of formula (1) as defined in the specification), their preparation and their use in therapies for the treatment of central nervous system diseases such as vigilance and sleep disorders, narcolepsy, Alzheimer's disease and other dementias, Parkinson's disease, attention disorders in hyperkinetic children, memory and learning disorders, epilepsy, schizophrenia, moderate cognitive disorders, depression, anxiety, sexual dysfunction, dizziness and travel sickness.
    Type: Grant
    Filed: November 15, 2006
    Date of Patent: November 16, 2010
    Assignee: sanofi-aventis
    Inventors: Juan Antonio Diaz Martin, Maria Dolores Jimenez Bargueno
  • SUBSTITUTED ARYL ALKYLAMINO-OXY-ANALOGS AND USES THEREOF
    Publication number: 20100286164
    Abstract: Aspects of the invention relate to substituted aryl propylamino-oxy-analogs and uses thereof. Aspects of the invention relate to compositions that are inhibitors of ?-secretase and uses thereof for treating subjects having, or at risk of developing, Alzheimer's disease.
    Type: Application
    Filed: October 10, 2008
    Publication date: November 11, 2010
    Applicant: The Brigham and Women's Hospital, Inc
    Inventors: Corinne Elizabeth Augelli-Szafran, Michael S. Wolfe, Han-Xun Wei
  • CXCR3 RECEPTOR ANTAGONISTS
    Publication number: 20100280028
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R5, A, B, D and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: April 27, 2010
    Publication date: November 4, 2010
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Jennifer A. KOWALSKI, Daniel Richard MARSHALL, Anthony S. PROKOPOWICZ, III, Sabine SCHLYER, Robert SIBLEY, Ronald John SORCEK, Di WU, Frank WU, Erick Richard Roush YOUNG
  • CHEMICAL COMPOUNDS
    Publication number: 20100280010
    Abstract: The present invention provides compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 of a target cell.
    Type: Application
    Filed: January 24, 2007
    Publication date: November 4, 2010
    Inventors: Kristjan Gudmundsson, Sharon Davis Boggs, John Franklin Miller, Angilique Christina Svolto
  • DUAL MECHANISM INHIBITORS FOR THE TREATMENT OF DISEASE
    Publication number: 20100280011
    Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
    Type: Application
    Filed: January 27, 2010
    Publication date: November 4, 2010
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty