Hetero Ring In The Polycyclo Ring System Patents (Class 514/320)
  • Patent number: 9988361
    Abstract: Disclosed is a novel anti-enterovirus 71 (EV71) 1,2,5-thiadiazolidine-1,1-dioxide derivative or a pharmaceutically acceptable salt thereof, and specifically, a compound represented by formula (II) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 21, 2015
    Date of Patent: June 5, 2018
    Assignee: Jiangsu Kanion Pharmaceutical Co., Ltd.
    Inventors: Peng Li, Haiying He, Ning Li, Jian Li, Shuhui Chen, Bailing Yang, Wang Shen, Wei Xiao
  • Patent number: 9957257
    Abstract: The present invention relates to compounds of formula (I), including their stereoisomers and pharmaceutically acceptable salts. This invention also relates to methods of making such compounds and pharmaceutical compositions comprising such compounds. The compounds of this invention are useful in the treatment of various disorders that are related to 5-hydroxytryptamine 4 (5-HT4) receptor.
    Type: Grant
    Filed: January 7, 2016
    Date of Patent: May 1, 2018
    Assignee: SUVEN LIFE SCIENCES LIMITED
    Inventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Abdul Rasheed Mohammed, Sangram Keshari Saraf, Narsimha Bogaraju, Ramkumar Subramanian, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Venkateswarlu Jasti
  • Patent number: 9890175
    Abstract: Provided are taxanes compounds having the structure of formula I, preparation method thereof, and uses of compositions having the compound, pharmaceutical salts and solvates thereof as active ingredients in the preparation of oral antitumor drugs. In the formula, R1 is —COR6, —COOR6, and —CONR7aR7b; R2 is C1-C6 alkyl, C1-C6 alkenyl group, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; R3 is —OR6, —OCOOR6, —OCOSR6, and —OCONR7aR7b; R4 is —OR6, —OCOOR6, —OCOSR6, —OCONR7aR7b, H, and OH; R6 is C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl group, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; and R7a and R7b are respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group.
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: February 13, 2018
    Assignee: JIANGSU TASLY DIYI PHARMACEUTICAL CO., LTD.
    Inventors: Wei Zhou, Yunrong Jing, Yongfeng Wang, Guocheng Wang
  • Patent number: 9856238
    Abstract: Disclosed are compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, Ra, R1, R2, R3, R4, R6, w and n1 are defined and described herein; compositions thereof; and methods of use thereof. These compounds are useful for treating a variety of neurological and psychiatric disorders, such as those described herein.
    Type: Grant
    Filed: February 11, 2016
    Date of Patent: January 2, 2018
    Assignees: SUNOVION PHARMACEUTICALS INC., PGI DRUG DISCOVERY LLC
    Inventors: Linghong Xie, Philip Glyn Jones, Kerry L. Spear, Noel Aaron Powell, Taleen G. Hanania, Vadim Alexandrov
  • Patent number: 9636335
    Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptors.
    Type: Grant
    Filed: June 10, 2015
    Date of Patent: May 2, 2017
    Assignee: SUVEN LIFE SCIENCES LIMITED
    Inventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Suresh Yarlagadda, Srinivasa Rao Ravella, Anil Karbhari Shinde, Ramasastri Kambhampati, Praveen Kumar Roayapalley, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Sriramachandra Murthy Patnala, Jyothsna Ravula, Venkateswarlu Jasti
  • Patent number: 9593376
    Abstract: The present invention relates to a method of assessing a favorable or, on the contrary, an unfavorable prognosis of a cancer in the subject, which method comprises detecting the presence of a mutated Natural Cytotoxicity-triggering Receptor 3 (NCR3) nucleic acid, an abnormal relative amount of at least one particular Natural Killer p30 (NKp30) RNA transcript isoform, and/or an abnormal Natural Killer p30 (NKp30) expression or activity of at least one particular NKp30 protein isoform in a sample from the subject, the presence of mutated NCR3 nucleic acid, abnormal relative amount of at least one particular NKp30 RNA transcript isoform, or abnormal expression or activity of at least one particular NKp30 protein isoform being indicative of the prognosis of cancer in the subject.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: March 14, 2017
    Assignees: INSTITUT GUSTAVE ROUSSY, INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM)
    Inventors: Laurence Zitvogel, Nicolas Delahaye
  • Patent number: 9498471
    Abstract: The present invention relates to the use of cyclin-dependent kinase 9 (CDK9) inhibitors to reduce, inhibit and/or prevent cartilage degradation. CDK9 inhibitors can be used to reduce, inhibit and/or prevent cartilage degradation and loss of cartilage viability during allograft storage. CDK9 inhibitors can be used as a post-injury intervention treatment to reduce, inhibit and/or prevent the acute cellular responses that lead to future cartilage degradation and osteoarthritis.
    Type: Grant
    Filed: October 19, 2012
    Date of Patent: November 22, 2016
    Assignee: The Regents of the University of California
    Inventors: Dominik Haudenschild, Paul Di Cesare, Jasper Yik, Blaine Christiansen
  • Patent number: 9469630
    Abstract: The present invention relates to a composition comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1?R,2?S,3?R,4?S)-2,3-bicyclo[2,2,1]heptanedicarboximide or a pharmaceutically acceptable acid addition salt thereof. In detail, the composition relates to a sustained release formulation for injection which maintains an effective blood level of the above-mentioned compound.
    Type: Grant
    Filed: October 18, 2011
    Date of Patent: October 18, 2016
    Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.
    Inventors: Takashi Nakagawa, Norimasa Koseki
  • Patent number: 9155724
    Abstract: In some aspects, the invention provides compositions and methods of use for treating a variety of diseases. In some aspect, the compositions and methods involve combined modulation of transcriptional modulators.
    Type: Grant
    Filed: February 4, 2011
    Date of Patent: October 13, 2015
    Assignee: Whitehead Institute for Biomedical Research
    Inventors: Peter B. Rahl, Richard A. Young
  • Patent number: 9079894
    Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptors.
    Type: Grant
    Filed: January 5, 2012
    Date of Patent: July 14, 2015
    Assignee: SUVEN LIFE SCIENCES LTD
    Inventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Suresh Yarlagadda, Srinivasa Rao Ravella, Anil Karbhari Shinde, Ramasastri Kambhampati, Praveen Kumar Roayapalley, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Sriramachandra Murthy Patnala, Jyothsna Ravula, Venkateswarlu Jasti
  • Publication number: 20150148256
    Abstract: A bioluminescence imaging-based high-throughput assay for inhibitors of ABCG2 is described. Compositions of inhibitors of ABCG2 and methods of using ABCG2 inhibitors are also described.
    Type: Application
    Filed: August 21, 2014
    Publication date: May 28, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: MARTIN GILBERT POMPER, YIMAO ZHANG, JOHN LATERRA
  • Publication number: 20150148353
    Abstract: A method of increasing the insulin sensitivity of a mammalian cell by contacting the cell with a protein phosphatase 2A (PP2A) inhibitor having the structure:
    Type: Application
    Filed: June 28, 2013
    Publication date: May 28, 2015
    Applicant: LIXTE BIOTECHNOLOGY, INC.
    Inventor: John S. Kovach
  • Publication number: 20150133498
    Abstract: Benzofuran compound, composition thereof, kit thereof, and/or method thereof. A benzofuran-2-carboxamide moiety may be N-arylated and/or N-alkylated, and the resulting benzofuran compound may be a sigma receptor ligand that binds to, e.g., a ?1 receptor and/or a ?2 receptor with relatively high affinity and/or selectivity. For example, the benzofuran compound may be 5,6-dimethoxy-3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamide, 3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamide, or 6-methoxy-3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamide. The composition may include the benzofuran compound and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: July 31, 2014
    Publication date: May 14, 2015
    Inventor: Karla-Sue C. Marriott
  • Publication number: 20150126552
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-aminated methylene or 2-esterified methylene tanshinone I derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments. When X is nitrogen, formula I indicates 2-aminated methylene tanshinone I; when X is oxygen, formula I indicates 2-esterified methylene tanshinone I.
    Type: Application
    Filed: November 30, 2012
    Publication date: May 7, 2015
    Applicant: Hangzhou Bensheng Pharmaceutical Co., Ltd.
    Inventors: Rongzhen Xu, Frank Rong, Fuwen Xie, Hongxi Lai
  • Patent number: 9018213
    Abstract: Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and clambering symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: April 28, 2015
    Assignees: Huazhong University of Science & Technology, NHWA Pharma. Corporation
    Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Xin Liu, Song Zhao, Bifeng Liu, Minquan Yu, Yinli Qiu
  • Publication number: 20150111888
    Abstract: The present invention provides a small compound targeting at TACC3. The present invention further provides a drug, particularly, an anticancer agent, comprising the small compound targeting at TACC3. A compound represented by the general formula (I) or a pharmaceutically acceptable salt, solvate, or ester derivative thereof binds to TACC3 and inhibits cell growth. Thus, these compounds can be used as drugs, particularly, anticancer agents.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 23, 2015
    Inventors: Ryoji Yao, Hiroyuki Osada, Yasumitsu Kondoh
  • Publication number: 20150105423
    Abstract: The present invention relates to the use of cyclin-dependent kinase 9 (CDK9) inhibitors to reduce, inhibit and/or prevent cartilage degradation. CDK9 inhibitors can be used to reduce, inhibit and/or prevent cartilage degradation and loss of cartilage viability during allograft storage. CDK9 inhibitors can be used as a post-injury intervention treatment to reduce, inhibit and/or prevent the acute cellular responses that lead to future cartilage degradation and osteoarthritis.
    Type: Application
    Filed: October 19, 2012
    Publication date: April 16, 2015
    Inventors: Dominik Haudenschild, Paul Di Cesare, Jasper Yik, Blaine Christiansen
  • Publication number: 20150099015
    Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.
    Type: Application
    Filed: November 24, 2014
    Publication date: April 9, 2015
    Inventor: Guochuan Emil TSAI
  • Publication number: 20150099765
    Abstract: Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventors: Michael L. Hendrickson, Jeffrey C. Ockuly, Trevor M. Twose, Melinda L. Verdone, Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson
  • Publication number: 20150099784
    Abstract: Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Vladimir KOGAN, Lev Tabachnik
  • Patent number: 8981131
    Abstract: The present invention provides compounds represented by formula I: wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: March 17, 2015
    Assignee: Piramal Enterprises Limited
    Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Roda Dalal, Sapna Parikh, Aditi Amol Tannu
  • Patent number: 8969384
    Abstract: The present invention relates to flavanoid compounds of general formula (X1) wherein: R1 is selected from a group consisting of morpholinyl, N-methyl piperizinyl, piperidinyl and N,N?-dimethylamino groups, and n ranges from 3 to 6, and process for preparation thereof. The present invention relates to the demonstration of anti Helicobacter pylori activity and gastric antisecretory activity of semisynthetically designed flavonoid compounds, to be used for the prevention and treatment of gastroduodenal disorders in general and peptic ulcer diseases in particular. The present invention also relates to a hetero-dimeric bi-functional molecule that can be used as monotherapy substituting/replacing/overcoming currently used triple/quadruple therapy, thereby implicating/anticipating/envisaging its commercial applicability.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: March 3, 2015
    Assignee: Council of Scientific & Industrial Research
    Inventors: Pratap Kumar Das, Suchandra Goswami, Annalakshmi Chinniah, Janaswamy Madhusudana Rao, Suresh Babu Katragadda
  • Patent number: 8969326
    Abstract: The present invention relates to methods and compositions for treating a subject suffering from a sclerosing disorder, comprising administering, to the subject, an effective amount of an estrogen receptor antagonist (“ERANT”), wherein said ERANT has essentially no estrogen receptor agonist activity under physiologic conditions.
    Type: Grant
    Filed: January 18, 2012
    Date of Patent: March 3, 2015
    Assignee: University of Pittsburgh—Of The Commonwealth System Of Higher Education
    Inventors: Carol A. Feghali-Bostwick, Pamela Anne Hershberger
  • 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: 20150038468
    Abstract: The present invention relates to methods and compositions for treating a subject suffering from a sclerosing disorder, comprising administering, to the subject, an effective amount of an estrogen receptor antagonist (“ERANT”), wherein said ERANT has essentially no estrogen receptor agonist activity under physiologic conditions.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Inventors: Carol A. Feghali-Bostwick, Pamela Anne Hershberger
  • Publication number: 20150024935
    Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols RA1, RA2, X, Y, L1, L2, RB1, RB2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
    Type: Application
    Filed: December 21, 2012
    Publication date: January 22, 2015
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Tomoki Tsuchiya, Pierre Wasnaire, Sebastian Hoffmann, Thomas Seitz, Stefan Hillebrand, Jürgen Benting, Jan Peter Schmidt, Pierre Cristau
  • Patent number: 8933100
    Abstract: A compound represented by Formula (1), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of paroxetine and has an improved CYP inhibitory effect: wherein R1 is a hydrogen atom or C1-6 alkyl group.
    Type: Grant
    Filed: January 29, 2013
    Date of Patent: January 13, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Keigo Tanaka, Tomoki Nishioka
  • Publication number: 20150011541
    Abstract: The present invention relates to compounds having a pipecolate sulfonamide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said pipecolate sulfonamide compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.
    Type: Application
    Filed: December 28, 2012
    Publication date: January 8, 2015
    Inventors: Ranganath Gopalakrishnan, Felix Hausch
  • Publication number: 20150011557
    Abstract: The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.
    Type: Application
    Filed: September 7, 2012
    Publication date: January 8, 2015
    Applicant: Merck Patent GmbH
    Inventors: Kai Schiemann, Wolfgang Staehle, Michael Busch, Dirk Wienke, Oliver Poeschke, Christa Burger
  • Patent number: 8927544
    Abstract: The present invention relates to benzofuran-2-sulfonamide derivatives with the following formula: or pharmaceutically acceptable salts thereof. The derivatives are useful as modulators of chemokine receptors.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: January 6, 2015
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard L. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20150005282
    Abstract: Disclosed in the present invention are polycyclic derivatives as represented by general formula (I), the preparation method thereof, pharmaceutical compositions containing the derivatives and uses thereof as therapeutic agents, especially the GPR40 agonist and in preparation of drugs for treating diseases such as diabetes and metabolic disorders, etc., wherein each substituent in the general formula (I) has the same definition as in the description.
    Type: Application
    Filed: December 27, 2012
    Publication date: January 1, 2015
    Inventors: Fanglong Yang, Qing Dong, Jihui Han, Chunfei Wang, Ling Zhang, Yang Wang
  • Publication number: 20150005286
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: December 14, 2012
    Publication date: January 1, 2015
    Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Johnny Y. Nagasawa, Andiliy G. Lai, Celine Bonnefous
  • Patent number: 8921397
    Abstract: The present invention is concerned with novel selective dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein R1, R2, R3, n, and Y are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: December 30, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • Publication number: 20140371207
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
    Type: Application
    Filed: December 13, 2013
    Publication date: December 18, 2014
    Applicants: Kyowa Hakko Kirin Co., Ltd., Millennium Pharmaceuticals, Inc.
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C.B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
  • Publication number: 20140364432
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Application
    Filed: February 12, 2014
    Publication date: December 11, 2014
    Inventors: Theodore M. KAMENECKA, Yuanjun HE, William NGUYEN, Rong Jiang, Xinyi Song
  • Publication number: 20140364433
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 11, 2014
    Inventors: Theodore M. KAMENECKA, Yuanjun HE, Rong JIANG, William NGUYEN, Xinyi SONG
  • Publication number: 20140356417
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Application
    Filed: June 12, 2014
    Publication date: December 4, 2014
    Inventors: Peter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Patent number: 8901313
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: December 2, 2014
    Assignee: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
  • Publication number: 20140349987
    Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: December 3, 2012
    Publication date: November 27, 2014
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Publication number: 20140349991
    Abstract: Compounds or pharmacologically acceptable salts thereof for promoting osteogenesis, improving bone metabolism, preventing or treating bone fracture, preventing or treating a disease associated with bone metabolism, or in the field of orthopedics for the promotion of healing of bone fracture, a bone defect, and bone diseases such as osteoarthritis as well as in the field of dentistry for the treatment of periodontal disease and the stabilization of artificial tooth root.
    Type: Application
    Filed: July 17, 2014
    Publication date: November 27, 2014
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Katsuhiro Kawakami, Toshihiro Kiho, Atsushi Tengeiji, Kentoku Gotanda, Kazumasa Aoki, Kazuki Yano
  • Patent number: 8889716
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: November 18, 2014
    Assignee: CHDI Foundation, Inc.
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas MacDonald, John Wityak
  • Publication number: 20140329857
    Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Application
    Filed: July 18, 2014
    Publication date: November 6, 2014
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
  • Publication number: 20140329809
    Abstract: A process for the characterization of rosacea is disclosed. The process can include identifying for the first time new markers in leukocyte recruitment as well as the therapeutic applications targeting rosacea.
    Type: Application
    Filed: October 26, 2012
    Publication date: November 6, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Isabelle Carlavan, Martin Steinhoff
  • Patent number: 8877778
    Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, x, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: November 4, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • Publication number: 20140323460
    Abstract: Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.
    Type: Application
    Filed: July 7, 2014
    Publication date: October 30, 2014
    Inventors: Donald Payan, Yasumichi Hitoshi, Todd Kinsella
  • Patent number: 8859589
    Abstract: Compound represented by the formulae: wherein each R individually is H or aliphatic acyl or aromatic acyl group; X is selected from the group consisting of hydrogen, fluoro, chloro, bromo, iodo, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano, aryl and nitro; pharmaceutically acceptable salts thereof, prodrugs thereof and mixtures thereof are used as inhibitors of orthopoxviruses and for treating patients suffering from an orthopoxvirus infection such as, but not limited to, smallpox, cowpox, monkeypox and camelpox.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: October 14, 2014
    Assignee: Southern Research Institute
    Inventors: John A. Secrist, III, Kamal N. Tiwari, Joseph A. Maddry
  • Patent number: 8853239
    Abstract: The present invention relates to compounds of formula I, wherein R1, LP, LQ, X, A, and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: October 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Elke Langkopf
  • Publication number: 20140296232
    Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Applicants: Massachusetts General Hospital, The Broad Institute, Inc.
    Inventors: Deborah Hung, Sarah Stanley, Tomohiko Kawate, Noriakie Iwase, Motohisa Shimizu
  • Publication number: 20140288106
    Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Applicant: Sanofi
    Inventors: Imre BATA, Peter BUZDER-LANTOS, Attila VASAS, Veronika BARTANE BODOR, Gyorgy FERENCZY, Zsuzsanna TOMOSKOZI, Gabor SZELECZKY, Sandor BATORI, Martin SMRCINA, Marcel PATEK, Aleksandra WEICHSEL, David Squire Thorpe
  • Publication number: 20140286931
    Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventor: Chengzhi Zhang