Six-membered Ring Consisting Of One Nitrogen And Five Carbons (e.g., Pyridine, Etc.) Patents (Class 544/360)
  • Patent number: 10208073
    Abstract: Disclosed is a solution comprising the chloride hydrochloride salt of 4-(5-(2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethylpropanamido)-4-(o-tolyl)pyridin-2-yl)-1-methyl-1-((phosphonooxy)methyl)piperazin-1-ium (fosnetupitant) and palonosetron hydrochloride in combination with dexamethasone and its application in methods for preventing acute and delayed nausea and vomiting in a human patient receiving highly emetogenic cancer chemotherapy.
    Type: Grant
    Filed: January 18, 2018
    Date of Patent: February 19, 2019
    Assignee: Helsinn Healthcare SA
    Inventors: Luca Fadini, Peter Manini, Claudio Pietra, Claudio Giuliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J Stella
  • Patent number: 10023556
    Abstract: Described herein are compounds that are androgen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon androgen receptors.
    Type: Grant
    Filed: September 9, 2016
    Date of Patent: July 17, 2018
    Assignee: Aragon Pharmaceuticals, Inc.
    Inventors: Nicholas D. Smith, Celine Bonnefous, Jackaline D. Julien
  • Patent number: 9725436
    Abstract: Embodiments of the present invention relate to novel cytochrome P450 inhibitors and pharmaceutical compositions thereof having a disease-modifying action in the treatment of diseases associated with the production of cortisol that include metabolic syndrome, obesity, headache, depression, hypertension, diabetes mellitus, Cushing's Syndrome, pseudo-Cushing syndrome, cognitive impairment, dementia, heart failure, renal failure, psoriasis, glaucoma, cardiovascular disease, cancer, stroke or incidentalomas.
    Type: Grant
    Filed: September 15, 2014
    Date of Patent: August 8, 2017
    Assignee: CORTENDO AB (PUBL)
    Inventors: Benjamin Eric Blass, Magid A Abou-Gharbia, Wayne E. Childers, Pravin Iyer, Joshodeep Boruwa
  • Patent number: 9403772
    Abstract: Compounds and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor, based on 4-(5-(2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethylpropanamido)-4-(o-tolyl)3yridine-2-yl)-1-methyl-1-((phosphonooxy)methyl)piperazin-1-ium and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: August 2, 2016
    Assignee: HELSINN HEALTHCARE SA
    Inventors: Luca Fadini, Peter Manini, Claudio Pietra, Claudio Giuliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J Stella
  • Patent number: 9365553
    Abstract: A heterocyclic compound useful as an antiallergic agent is provided. A compound represented by the following formula (1) or a salt thereof: wherein the ring A is a homocyclic or heterocyclic ring; the ring B is a heterocyclic ring which contains G and nitrogen atom N as constituent atoms thereof, wherein G is CH or N; R1 is a carbonyl group or an alkylene group; R2a and R2b are an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; X is an oxygen atom or a sulfur atom; Z is a hydroxyl group, an alkoxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, an amino group, or an N-substituted amino group; and n is 0 or 1; with the proviso that when the ring A is a benzene ring or when the ring B is a piperazine ring, R1 is an alkylene group which may have a substituent.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: June 14, 2016
    Assignee: Aska Pharmaceutical Co., Ltd.
    Inventors: Makoto Okada, Koichi Hasumi, Takahiro Nishimoto, Miwa Yoshida, Kouki Ishitani, Tomoji Aotsuka, Hashime Kanazawa
  • Patent number: 9034850
    Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: May 19, 2015
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
  • Publication number: 20150133663
    Abstract: The present invention relates to a method of making compounds having affinity for the 1 A subtype of the serotonin receptor, i.e. 5HT1A. The method of the present invention provides advantages over the known methods of synthesis. The compounds obtained by the method of the invention have use in therapeutic methods. The compounds of the invention may also optionally compose a moiety suitable for detection by an in vivo imaging procedure and as such these compounds have use in in vivo imaging methods. The compounds have particular use in the treatment and diagnosis of various neurological and/or psychiatric disorders.
    Type: Application
    Filed: September 21, 2012
    Publication date: May 14, 2015
    Inventors: Radha Achanath, Jinto Jose, Chitralekha Rangaswamy, Subrata Mandal, Afsal Mohammed Kadivilpparampu Mohamed, Ian Martin Newington, Srinath Balaji
  • Patent number: 9029381
    Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.
    Type: Grant
    Filed: November 21, 2011
    Date of Patent: May 12, 2015
    Assignee: Astrazeneca AB
    Inventors: James Arnold, Todd Andrew Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
  • Patent number: 9024033
    Abstract: The present invention is related to a use of aminopyridine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyridine derivatives useful for the preparation of a pharmaceutical foimulation for the inhibition of malaria parasite proliferation.
    Type: Grant
    Filed: January 17, 2011
    Date of Patent: May 5, 2015
    Assignee: MMV Medicines for Malaria Venture
    Inventors: Michael John Witty, David Hardick
  • Publication number: 20150119373
    Abstract: The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
    Type: Application
    Filed: April 19, 2013
    Publication date: April 30, 2015
    Inventors: Bandi Parthasaradhi Reddy, Vedula Manohar Sharma, Kura Rathnakar Reddy, Mamnoor Prem Kumar, Kasireddy Bhaskar Reddy, Mogili Narsingam, Mukkera Venkati, Lanka VL Subrahmanyam, Ravi Mallikarjun Reddy
  • Publication number: 20150105386
    Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).
    Type: Application
    Filed: October 24, 2014
    Publication date: April 16, 2015
    Inventors: Helmut Mack, Nicole Teusch, Bernhard K. Muller, Wilfried Hornberger, Michael F. Jarvis, Daryl Sauer, Steven L. Swann, Jr., Dominique Bonafoux, Ryan Keddy, Adrian Donald Hobson, Anil Vasudevan
  • Publication number: 20150099762
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Application
    Filed: December 9, 2014
    Publication date: April 9, 2015
    Inventors: Hilary Schenck EIDAM, Kaushik RAHA, Zhen GONG, Huiping Amy GUAN, Chengde WU, Haiying YANG, Haiyu YU, Zhiliu ZHANG, Mui CHEUNG
  • Publication number: 20150099760
    Abstract: This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.
    Type: Application
    Filed: June 18, 2014
    Publication date: April 9, 2015
    Applicant: Novartis AG
    Inventors: John Vincent Calienni, Guang-Pei Chen, Baoqing Gong, Prasad Koteswara Kapa, Vishal Saxena
  • Patent number: 8999989
    Abstract: The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: April 7, 2015
    Assignee: R-Tech Ueno, Ltd.
    Inventors: Tatsuya Matsukawa, Kazuhiro Masuzaki, Akiko Kawasaki, Akiko Akasaka, Yosuke Kawai
  • Patent number: 8993760
    Abstract: The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are compounds that inhibit Rho-protein associated kinase function. Compounds of the invention include piperazinyl pyridines, piperazinylmethyl pyridines, piperazinyl ureas and carbamates, piperazinyl pyridines and quinoilines (including isoquinliones) as well as piperazinyl (including piperazinylmethyl) pyridines and quinolines (including isoquinolines). Compounds of the invention disrupt Rho-kinase activation and function and significantly inhibit tumor cell growth and induce tumor cell death.
    Type: Grant
    Filed: June 22, 2009
    Date of Patent: March 31, 2015
    Assignees: University of South Florida, Yale University
    Inventors: Said M. Sebti, Andrew D. Hamilton
  • Publication number: 20150087639
    Abstract: The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.
    Type: Application
    Filed: July 18, 2013
    Publication date: March 26, 2015
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Yingjun Zhang, Jiancun Zhang, Xiaojun Wang, Runfeng Lin, Shengtian Cao, Zhaohe Wang, Jing Li
  • Publication number: 20150080365
    Abstract: This invention relates to certain heteroaryl compounds for use as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of helminth infections and the treatment of parasitosis caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 19, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Patent number: 8981094
    Abstract: The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —C(?O)—; —O—C(?O)—; C(?O)—C(?O)—; —NRx—C(?O)—; —Z1—C(O)—; —Z1—NRx—C(?O)—; —C(?O)—Z1—; —NRx—C(?O)—Z1—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z1—C(?S)—; —Z1—NRx—C(?S)—; —C(?S)—Z1-; —NRx—C(?S)—Z—; Y represents NRx—C(=0)-Z2—; —NRx—C(=0)-Z2—NRy—; —NRx—C(=0)-Z2—NRy—C(=0)-; —NRx—C(=0)-Z2—NRy—C(=0)-O—; —NRx—C(=0)-Z2-0-; —NRx—C(=0)-Z2-0-C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-0-; —NRx—C(?O)—O—Z2—O—C(?O)—; —NRx—C(?O)—Z2—C(?O)—NRy—; —NRx—C(?O)—Z2—NRy—C(=0)-NRy—; —C(?O)—Z2—; —C(?O)—Z2—O—; —C(=0)-NRx—Z2—; —C(=0)-NRx—Z2-0-; —C(=0)-NRx—Z2—C(=0)-0-; —C(=0)-NRx—Z2-0-C(=0)-; —C(=0)-NRx—Z2—NRy—; —C(=0)-NRx—Z2—NRy—C(=0)-; —C(=0)-NRx—Z2—NRy—C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkylox
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: March 17, 2015
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Pierre André Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J. M. De Waepenaert, Peter Walter Maria Roevens, Gustaaf Maria Boeckx, Petr Vladimirivich Davidenko
  • Patent number: 8980890
    Abstract: The invention relates to compounds and methods for treating cell proliferation disorders.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: March 17, 2015
    Assignee: Kinex Pharmaceuticals, LLC
    Inventor: David G. Hangauer, Jr.
  • Publication number: 20150072980
    Abstract: The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor ?t (ROR?t)/ROR?. The compounds of the present invention are useful for modulating ROR?t)/ROR? activity and for treating diseases or conditions mediated by ROR?t)/ROR? such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 12, 2015
    Inventors: Hariprasad Vankayalapati, Venkatakrishnareddy Yerramreddy
  • Publication number: 20150051194
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Publication number: 20150045357
    Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a [(1-Piperazinyl)-4-pyridinylmethyl]-Naphtho[1,2-b]furan structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Application
    Filed: March 29, 2013
    Publication date: February 12, 2015
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Zaneta Nikolovska-Coleska, Naval Bajwa, Chenzhong Liao, Lei Miao
  • Patent number: 8952157
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: February 10, 2015
    Assignees: AbbVie Inc., The Walter and Eliza Hall Institute of Medical Research
    Inventors: Hong Ding, George A. Doherty, Steven W. Elmore, Laura Hexamer, Aaron R. Kunzer, Cheol-Min Park, Xiahong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Le Wang, Michael D. Wendt, Peter Edward Czabotar, Guillaume Laurent Lessene, Peter Malcolm Colman
  • Publication number: 20150018341
    Abstract: The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.
    Type: Application
    Filed: December 28, 2012
    Publication date: January 15, 2015
    Applicant: CENTAURUS BIOPHARMA CO., LTD.
    Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Rong Yu, Wei Hu, Na Zhao, Yong Peng, Hong Luo, Yongxin Han
  • Publication number: 20150018366
    Abstract: The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof.
    Type: Application
    Filed: September 26, 2014
    Publication date: January 15, 2015
    Inventor: Laykea TAFESSE
  • Publication number: 20150011510
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor.
    Type: Application
    Filed: November 28, 2012
    Publication date: January 8, 2015
    Applicant: HELSINN HEALTHCARE SA
    Inventors: Luca Fadini, Peter Manini, Claudio Pietra, Claudio Guiliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J. Stella
  • Publication number: 20150011551
    Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 8, 2015
    Applicant: Sanford- Burnham Medical Reseach Institute
    Inventors: Anthony B. Pinkerton, Russell Dahl, Nicholas D.P. Cosford, Jose Luis Millan
  • Publication number: 20150005296
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Application
    Filed: September 18, 2014
    Publication date: January 1, 2015
    Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, JR.
  • Publication number: 20140378429
    Abstract: The disclosure relates particularly to certain carboxamide, sulfonamide and amine compounds and pharmaceutical compositions thereof, and to methods of treating and ameliorating disorders and conditions related to the adiponectin pathway, sphingolipid metabolism, oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. In certain embodiments, the compounds have the structures (I-1), (2-I) and (3-I) (The chemical formulas should be inserted here) in which the variables are as described herein.
    Type: Application
    Filed: January 31, 2013
    Publication date: December 25, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, David Carroll, Simon Shaw, Hitoshi Yasumichi
  • Patent number: 8906924
    Abstract: The disclosure relates to (heterocycle-tetrahydropyridine)(piperazinyl)-1-alkanone and (heterocycle-dihydropyrrolidine)(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, B, m, n, W, and R2 are as defined in the disclosure; to the methods of preparing said derivatives, and to the therapeutic uses thereof.
    Type: Grant
    Filed: July 18, 2013
    Date of Patent: December 9, 2014
    Assignee: Sanofi
    Inventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart, Valentina Vercesi
  • Publication number: 20140357614
    Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xioahu Zhang
  • Publication number: 20140350015
    Abstract: The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.
    Type: Application
    Filed: June 12, 2014
    Publication date: November 27, 2014
    Inventors: Edward McDonald, Julian Blagg, Mark Pichowicz, Simon Ross Crumpler
  • Publication number: 20140349986
    Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 27, 2014
    Applicant: SANOFI
    Inventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
  • Publication number: 20140350012
    Abstract: The invention further relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5- or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-
    Type: Application
    Filed: August 11, 2014
    Publication date: November 27, 2014
    Inventors: Jean-Pierre Andre Marc Bongartz, Lieven Meerpoel, Maria Gustaaf Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Nestor Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
  • Patent number: 8895586
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor.
    Type: Grant
    Filed: April 17, 2013
    Date of Patent: November 25, 2014
    Inventors: Luca Fadini, Peter Manini, Claudio Pietra, Claudio Giuliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J. Stella
  • Patent number: 8895562
    Abstract: The present invention relates to piperazin-1-yl-trifluoromethyl-substituted-pyridines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
    Type: Grant
    Filed: July 29, 2009
    Date of Patent: November 25, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: José Manuel Bartolomé-Nebreda, Gregor James MacDonald, Michiel Luc Maria Van Gool
  • Publication number: 20140343059
    Abstract: Disclosed are novel piperazine derivatives that act as agonists of the ?7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.
    Type: Application
    Filed: July 29, 2014
    Publication date: November 20, 2014
    Inventors: Roger B. CLARK, Daniel ELBAUM
  • Patent number: 8889690
    Abstract: The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof.
    Type: Grant
    Filed: March 28, 2013
    Date of Patent: November 18, 2014
    Assignee: Purdue Pharma L.P.
    Inventor: Laykea Tafesse
  • Publication number: 20140336165
    Abstract: Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.
    Type: Application
    Filed: November 14, 2012
    Publication date: November 13, 2014
    Inventors: Takeshi Hondo, Keita Nakanishi, Tatsuya Niimi, Masaichi Warizaya, Ichiji Namatame, Katsuya Harada
  • Patent number: 8883776
    Abstract: Certain cycloalkyloxy- and heterocycloalkyloxypyridine compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Grant
    Filed: November 17, 2008
    Date of Patent: November 11, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Michael A. Letavic, Emily M. Stocking
  • Patent number: 8883791
    Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: November 11, 2014
    Assignee: Intervet Inc.
    Inventors: Michael Berger, Christopher Kern, Marko Eck, Jörg Schröder
  • Patent number: 8877747
    Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: November 4, 2014
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
  • Patent number: 8871770
    Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: February 3, 2014
    Date of Patent: October 28, 2014
    Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
  • Publication number: 20140315786
    Abstract: The present invention relates to targeting an intracellular enzyme for release of covalently linked bioactives which results in a synergistic effect between the bioactives. The present invention relates to the use of bioactives that are directly connected covalently or through a covalent molecular linker which have increased therapeutic activity when released as the free bioactives by intracellular enzymes as compared to when the bioactives are administered individually (i.e. not covalently linked). Further, methods are described of administering to patients in need thereof, bioactives as linked bioactives having increased therapeutic activity. Accordingly, this invention also relates to methods of treating patients for certain diseases.
    Type: Application
    Filed: March 16, 2012
    Publication date: October 23, 2014
    Applicant: Catabasis Pharmaceuticals, Inc.
    Inventors: Michael R. Jirousek, Jill C. Milne, David Carney, Jean E. Bemis, Chi B. Vu
  • Patent number: 8859556
    Abstract: A compound of Formula (I), pharmaceutically acceptable salts thereof, enantiomers, or mixtures thereof; pharmaceutical compositions containing said compounds, enantiomers or mixtures; processes for making said compounds, enantiomers or mixtures; the use of said compounds, enantiomers or mixtures; and medicaments containing the same for treatment of pain and other conditions; and methods of treating pain and other conditions with the same.
    Type: Grant
    Filed: October 11, 2011
    Date of Patent: October 14, 2014
    Assignee: Acturum Life Science AB
    Inventors: Mats Svensson, Dirk Weigelt
  • Publication number: 20140296253
    Abstract: The present invention provides: a novel compound which has a useful pharmacological action for treating heart failure or shock without increasing heart rate; and a pharmaceutical composition using the same. The present invention relates to a diphenylmethyl piperazine derivative represented by general formula (I) (In the formula, R1 is a hydrogen atom or a hydroxy group. R2 is a hydrogen atom, a halogen atom, a hydroxy group, an alkyl group having one to five carbon atoms, or an alkoxyl group having one to five carbon atoms, excluding the case where R1 is a hydroxy group and R2 is a chlorine atom.) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same.
    Type: Application
    Filed: June 15, 2012
    Publication date: October 2, 2014
    Applicant: AETAS PHARMA CO., LTD.
    Inventor: Noboru Kaneko
  • Publication number: 20140296225
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Application
    Filed: October 22, 2012
    Publication date: October 2, 2014
    Inventors: Haifeng Tang, Barbara Pio, Nardos Teumelsan, Alexander Pasternak, Reynalda DeJesus
  • Patent number: 8846706
    Abstract: Crystalline forms of imatinib mesylate (F, G, H, I and K) and their respective characterization are disclosed.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: September 30, 2014
    Assignee: Novartis AG
    Inventor: Michael Mutz
  • Publication number: 20140288086
    Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
    Type: Application
    Filed: June 6, 2014
    Publication date: September 25, 2014
    Applicants: PFIZER INC., AGOURON PHARMACEUTICALS, INC.
    Inventors: Jingrong Jean CUI, Lee Andrew FUNK, Lei JIA, Pei-Pei KUNG, Jerry Jialun MENG, Mitchell David NAMBU, Mason Alan PAIRISH, Hong SHEN, Michelle TRAN-DUBE
  • Publication number: 20140288045
    Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu