The Additional Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbon Atoms Patents (Class 514/252.03)
Polycyclo ring system having the additional six-membered hetero ring as one of the cyclos (Class 514/252.04)
  • PYRIDONE AND PYRIDAZONE ANALOGUES AS GPR119 MODULATORS
    Publication number: 20110263548
    Abstract: Novel compounds of structure Formula (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R21, T1, T2, T3 and T4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
    Type: Application
    Filed: July 15, 2009
    Publication date: October 27, 2011
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Dean A. Wacker, Karen A. Rossi, Ying Wang, Gang Wu
  • TETRASUBSTITUTED PYRIDAZINE HEDGEHOG PATHWAY ANTAGONISTS
    Publication number: 20110263602
    Abstract: The present invention provides novel tetrasubstituted pyridine hedgehog pathway antagonists of the following formula I (I) or a pharmaceutically acceptable salt thereof, wherein: X is C—R1 or N; R1 is hydrogen, fluoro or cyano; R2 is formula II (II), piperidinyl, or gem di-F-substituted cyclohexyl; R3 is methyl or trifluoromethyl; R4 is pyrrolidinyl, morpholinyl or pyridyl, amino or dimethylamino; R5 is trifluoromethyl or methylsulfonyl; R6 is hydrogen or methyl; and R7, R8, R9, R10 and R11 are independently hydrogen fluoro, cyano, chloro, methyl, trifluoromethyl, trifluoromethoxy or methylsulfonyl, provided that at least two of R7, R8, R9, R10 and R11 are hydrogen useful in the treatment of cancer.
    Type: Application
    Filed: November 5, 2009
    Publication date: October 27, 2011
    Applicant: ELI LILLY AND COMPANY
    Inventors: Jolie Anne Bastian, Julia Marie Clay, Jeffrey Daniel Cohen, Philip Arthur Hipskind, Karen Lynn Lobb, Daniel Jon Sall, Michelle Lee Thompson, Takako Wilson (nee Takakuwa)
  • Biaryl ether urea compounds
    Patent number: 8044052
    Abstract: The present invention relates to compounds of Formula (I) or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity.
    Type: Grant
    Filed: October 18, 2007
    Date of Patent: October 25, 2011
    Assignee: Pfizer Inc.
    Inventors: Lorraine Kathleen Fay, Douglas S. Johnson, Suzanne Ross Kesten, Scott E. Lazerwith, Mark Anthony Morris, Cory Michael Stiff, Marvin Jay Meyers, Lijuan Jane Wang
  • Hydrazine-Substituted Anthranilic Acid Derivatives
    Publication number: 20110257191
    Abstract: The present invention constitutes new hydrazine-substituted anthranilic acid derivatives of the general formula (I), in which R1, R2, R3, R4, R5, R6, Qx, A, Qy and n have the definitions indicated in the description, application thereof as insecticides and acaricides for controlling animal pests, alone and in combination with further agents for activity boosting, and a number of processes for their preparation.
    Type: Application
    Filed: February 8, 2011
    Publication date: October 20, 2011
    Applicant: Bayer CropScience AG
    Inventors: Rüdiger Fischer, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Christoph Grondal, Achim Hense, Arnd Voerste
  • COMPOUND FOR TREATMENT OF RESPIRATORY CONDITION OR DISEASE
    Publication number: 20110257192
    Abstract: The present invention relates to the treatment, alleviation, prevention or reduction of symptoms or exacerbations of asthma or chronic obstructive pulmonary disease (COPD), of which reduced lung function is typically symptomatic.
    Type: Application
    Filed: April 15, 2011
    Publication date: October 20, 2011
    Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTD
    Inventors: John Nicholas Lambert, Jane Ryan, Janet Marie Wilson
  • Phthalazine derivatives with angiogenesis inhibiting activity
    Patent number: 8034814
    Abstract: The invention relates to new phthalazine derivatives of formula I, and to processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof alone or in combination with one or more other pharmaceutically active compounds for the treatment especially of a disease that responds to the inhibition of especially the vascular endothelial growth factor receptor kinase, preferably the treatment of a proliferative disease, or the treatment of inflammatory rheumatic or rheumatoid arthritis and/or pain; and the use of such a compound alone or in combination with one or more other pharmaceutically active compounds for the manufacture of a pharmaceutical preparation for the treatment of said diseases in an animal.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: October 11, 2011
    Assignee: Novartis AG
    Inventors: Guido Bold, Paul William Manley
  • MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    Publication number: 20110245251
    Abstract: Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Application
    Filed: December 7, 2009
    Publication date: October 6, 2011
    Applicant: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou
  • N- (HETERO)ARYL, 2- (HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS
    Publication number: 20110237573
    Abstract: The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A1, A2, B, Y and Z all represent rings.
    Type: Application
    Filed: March 1, 2010
    Publication date: September 29, 2011
    Applicant: IRM LLC
    Inventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
  • Octahydro-pyrrolo[3,4-b]pyrrole N-oxides
    Patent number: 8026240
    Abstract: The invention relates to octahydro-pyrrolo[3,4-b]pyrrole N-oxides as prodrugs of CNS-active compounds, compositions comprising such compounds, methods for making the compounds, salts, and polymorphs, and methods of treating conditions and disorders using such compounds and compositions. Octahydro-pyrrolo[3,4-b]pyrrole N-oxides of formula (I) are prodrugs of histamine-3 antagonists, and are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole N-oxide compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.
    Type: Grant
    Filed: September 11, 2008
    Date of Patent: September 27, 2011
    Assignee: Abbott Laboratories
    Inventors: Marlon D. Cowart, Kennan C. Marsh, Huaqing Liu, Jae Y. Lee, Maria G. Beconi, Jill M. Wetter, Lawrence A. Black, Thomas C. Custer
  • 1-OXA-8-Azaspiro [4,5] Decabe-8-Carboxamide Compounds as FAAH Inhibitors
    Publication number: 20110230493
    Abstract: Provided herein are 1-oxa-8-azaspiro[4.5]decane-8-carboxamide compounds of formula I wherein Ar1, Ar2, R1, R2, R3 and R4 are as defined herein and the pharmaceutically acceptable salts of such compounds useful in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, conditions including acute pain, chronic pain, neuropathic pain, nociceptive pain, inflammatory pain, fibromyalgia, rheumatoid arthritis, inflammatory bowel disease, lupus, diabetes, allergic asthma, vascular inflammation, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease.
    Type: Application
    Filed: November 9, 2009
    Publication date: September 22, 2011
    Inventors: Scott Allen Long, Marvin Jay Meyers, Matthew James Pelc, Barbara Ann Schweitzer, Lijuan Jane Wang, Atli Thorarensen
  • PHENYL-HETEROARYL DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20110230458
    Abstract: The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof These compounds are useful in the treatment of RAGE-mediated diseases such as Alzheimer's Disease. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.
    Type: Application
    Filed: February 15, 2011
    Publication date: September 22, 2011
    Applicant: TransTech Pharma, Inc.
    Inventors: Devi R. Gohimukkula, David Jones, Ghassan Qabaja, Jeff J. Zhu, Jeremy T. Cooper, William K. Banner, Kurt Sundermann, Muralidhar Bondlela, Mohan Rao, Pingzhen Wang, Raju B. Gowda, Robert C. Andrews, Suparna Gupta, Anitha Hari
  • ANTIVIRAL AGENTS
    Publication number: 20110212966
    Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.
    Type: Application
    Filed: May 4, 2011
    Publication date: September 1, 2011
    Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTD
    Inventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
  • Inhibitors of Akt activity
    Patent number: 8003643
    Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: August 23, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
  • Novel Acylaminobenzamide Derivatives
    Publication number: 20110201603
    Abstract: The present invention relates to novel Acylaminobenzamide derivatives represented by the following formula (I) and use thereof as pesticides: wherein V represents an aromatic ring group of V1 to V5 described in the detailed description, Q represents an aromatic ring group of Q1 to Q7 described in the detailed description, G1 and G2 represent O or S, R1 represents hydrogen, alkyl, haloalkyl, alkoxy, haloalkoxy, phenyl or a heterocyclic group and R2 and R3 represent hydrogen, alkyl, haloalkyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl or haloalkoxycarbonyl.
    Type: Application
    Filed: July 30, 2009
    Publication date: August 18, 2011
    Applicant: Bayer CropScience AG
    Inventors: Jun Mihara, Tetsuya Murata, Kei Domon, Yukiyoshi Watanabe, Yasushi Yoneta, Takuma Mori, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara, Masashi Ataka, Ulrich Görgens
  • NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
    Publication number: 20110189192
    Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, and solvates thereof. Q is a tetrahydropyridinyl ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
    Type: Application
    Filed: February 19, 2009
    Publication date: August 4, 2011
    Inventors: Alan B. Cooper, Yang Nan, Yongqi Deng, Gerald W. Shipps, JR., Neng-Yang Shih, Hugh Y. Zhu, Joseph M. Kelly, Subrahmanyam Gudipati, Ronald J. Doll, Mehul F. Patel, Jagdish A. Desai, James J-S Wang, Sunil Paliwal, Hon-Chung Tsui, Sobhana Babu Boga, Abdul-Basit Alhassan, Xiaolei Gao, Liang Zhu, Xin Yao
  • ALPHA-KETO HETEROCYCLES AS FAAH INHIBITORS
    Publication number: 20110183947
    Abstract: The invention provides a series of -?ketoheterocyclic compounds, for example, compounds of formula (I). The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula (I), useful intermediates for the preparation of compounds of formula (I), and methods of using compounds of formula (I) and compositions thereof.
    Type: Application
    Filed: July 8, 2009
    Publication date: July 28, 2011
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventor: Dale L. Boger
  • Protein Kinase Targeted Therapeutics
    Publication number: 20110166153
    Abstract: The present invention relates to compositions and methods useful in treating diseases and disorders related to protein kinases. In particular, the present invention relates to compositions and methods useful for targeting protein kinases related to mitogen activated protein kinase (MAPK) pathways (e.g., p38 MAPK, JNK, ERK, and upstream and downstream protein kinases) and/or casein kinase (CK) pathways (e.g., CK1?, and upstream and downstream protein kinases), and diseases and disorders related to MAPK pathways (e.g., p38 MAPK, JNK, ERK, and upstream and downstream protein kinases) and/or CK pathways (e.g., CK1?, and upstream and downstream protein kinases).
    Type: Application
    Filed: February 24, 2011
    Publication date: July 7, 2011
    Applicant: NORTHWESTERN UNIVERSITY
    Inventors: D. Martin Watterson, Linda J. Van Eldik
  • SUBSTITUTED PYRIDAZINE CARBOXAMIDE COMPOUNDS AS KINASE INHIBITOR COMPOUNDS
    Publication number: 20110160209
    Abstract: Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.
    Type: Application
    Filed: June 18, 2009
    Publication date: June 30, 2011
    Inventors: Congxin Liang, Zhigang Li
  • Heterocyclic compounds useful as RAF kinase inhibitors
    Patent number: 7968536
    Abstract: The present invention provides compounds useful as inhibitors of protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: June 28, 2011
    Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.
    Inventors: Jennifer Cossrow, Bing Guan, Alexey Ishchenko, John Howard Jones, Gnanasambandam Kumaravel, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
  • Pyridazinone kinase inhibitors
    Patent number: 7968546
    Abstract: Disclosed are compounds of Formula I wherein X is and R2, R1, A, B, D, E, R9 are as defined herein useful for treating cancers.
    Type: Grant
    Filed: January 26, 2009
    Date of Patent: June 28, 2011
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Swen Hoelder, Gunter Muller, Karl Schoenafinger, David William Will, Hans Matter, Martin Bossart, Cecile Combeau, Christine Delaisi, Ingrid Sassoon, Anke Steinmetz, Didier Benard
  • PYRROLIDINE COMPOUNDS
    Publication number: 20110152233
    Abstract: The present application relates to compounds of formula wherein R1, R2, R3, R4, and n are defined herein or to a pharmaceutically active salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: December 10, 2010
    Publication date: June 23, 2011
    Inventors: Henner Knust, Andreas Koblet, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • BENZOPYRANS AND ANALOGS AS RHO KINASE INHIBITORS
    Publication number: 20110150833
    Abstract: Compounds useful as Rho kinase inhibitors of formula (1) wherein the variables are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.
    Type: Application
    Filed: December 18, 2008
    Publication date: June 23, 2011
    Applicant: The Scripps Research Institute
    Inventors: Yangbo Feng, Philip LoGrasso, Thomas Bannister, Thomas Schroeter, Yen Ting Chen, Yan Yin, Hampton Sessions, Michael P. Smolinski, Lei Yao, Bo Wang, Bozena Frackowiak-Wojtasek
  • OXAZOLE DERIVATIVES USEFUL AS INHIBITORS OF FAAH
    Publication number: 20110144119
    Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.
    Type: Application
    Filed: July 30, 2009
    Publication date: June 16, 2011
    Inventors: Harry Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo
  • ANTIVIRAL SALTS
    Publication number: 20110144118
    Abstract: This invention relates to antiviral agents, in particular to salts useful in the treatment of infections caused by Picornaviridae, such as human rhinovirus (HRV) and methods for their preparation. The invention also relates to the use of these salts in the treatment of picornavirus infections. The salts of this invention are especially suitable for use in the treatment of HRV, however it is to be understood that the invention is also applicable to other viruses of the picornavirus family.
    Type: Application
    Filed: May 27, 2009
    Publication date: June 16, 2011
    Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTD
    Inventors: Jane Ryan, Margaret Anne Butt
  • PYRROLIDINE DERIVATIVES
    Publication number: 20110144081
    Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: December 7, 2010
    Publication date: June 16, 2011
    Inventors: Henner Knust, Andreas Koblet, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • FUNGICIDAL COMPOSITIONS
    Publication number: 20110142802
    Abstract: A fungicidal composition suitable for control of disease caused by phytopathogens comprising (A) a compound of formula (I), wherein R1 is methyl, ethyl or isopropyl; R2 is 2-chloro-6-fluoro-phenyl, 2,4,6-trifluorophenyl or 2,6-difluoro-4-methoxy-phenyl; R3 is chloro, fluoro or methoxy; and (B) a compound selected, for example, from the group consisting of (B1) a strobilurin fungicide, (B2) an azole fungicide, (B3) a morpholine fungicide, and (B4) an anilinopyrimidine fungicide.
    Type: Application
    Filed: January 14, 2009
    Publication date: June 16, 2011
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Jeremy R. Godwin, Stephan Trah, Clemens Lamberth, Raphael Dumeunier, Valeria Grasso, Sebastian Volker Wendeborn
  • Pyridazin-3(2)-one derivatives and their use as PDE4 inhibitors
    Patent number: 7960383
    Abstract: The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives of Formula (I) and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention or suppression of pathological conditions, diseases and disorders known to be susceptible of being improved by inhibition of PDE4 such as asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis or irritable bowel disease.
    Type: Grant
    Filed: June 13, 2005
    Date of Patent: June 14, 2011
    Assignee: Laboratorios Almirall SA
    Inventors: Antonia Maria Buil Albero, Vittorio Dal Piaz, Yolanda Garrido Rubio, Jordi Gracia Ferrer, Lluis Miquel Pages Santacana, Joan Taltavull Moll
  • 6-THIOXOPYRIDAZINE DERIVATIVES
    Publication number: 20110136819
    Abstract: Compounds of the formula I, in which R1, R2 and R3 have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: July 18, 2008
    Publication date: June 9, 2011
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNG
    Inventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat, Frank Stieber
  • Diazepine and Diazocane Compounds As MC4 Agonists
    Publication number: 20110136814
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, L and n are as defined in the specification. These compounds are useful as MC4 agonists.
    Type: Application
    Filed: July 30, 2009
    Publication date: June 9, 2011
    Inventors: Mark David Andrews, Christopher Gordon Barber
  • FUNGICIDAL PYRIDAZINES
    Publication number: 20110136762
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R3, R4, X, Y and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: September 17, 2009
    Publication date: June 9, 2011
    Applicant: E.I. Du Pont de Nemours and Company
    Inventor: Paula Louise Sharpe
  • Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase
    Patent number: 7951805
    Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): Formula (I) where x, y, G, J, L, M, V, W, R2, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8, and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
    Type: Grant
    Filed: September 20, 2005
    Date of Patent: May 31, 2011
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Rajender Kamboj, Zaihui Zhang, Jianmin Fu, Serguei Sviridov, Shaoyi Sun, Mehran Seid Bagherzadeh, Vandna Raina, Duanjie Hou, Sultan Chowdhury, Shifeng Liu, Vishnumurthy Kodumuru, Nagasree Chakka
  • Certain Substituted Amides, Method of Making, and Method of Use Thereof
    Publication number: 20110118233
    Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
    Type: Application
    Filed: May 6, 2009
    Publication date: May 19, 2011
    Inventors: Peter A. Blomgren, David R. Brittelli, Kevin S. Currie, Seung H. Lee, Jeffrey E. Kropf, Scott A. Mitchell, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Zhongdong Zhao, Pavel E. Zhichkin
  • PYRIDAZINONES, THE PREPARATION AND THE USE THEREOF
    Publication number: 20110112061
    Abstract: The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.
    Type: Application
    Filed: March 18, 2009
    Publication date: May 12, 2011
    Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Youhong Hu, Liguang Lou, Shijun Lin, Hongbing Zhao, Zhende Liu, Yongping Xu, Bo Chao
  • PYRIDAZINE FUNGICIDES
    Publication number: 20110112108
    Abstract: The present invention relates to novel pyridazine derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R1 is methyl, ethyl or isopropyl; R2 is chloro, fluoro, hydroxy or C1-C2alkoxy; R3 is H, chloro, fluoro, methoxy or C1-C3alkyl; R4 is chloro, fluoro or bromo; and R3 is H, fluoro or methoxy; or an agrochemically usable salt form thereof; with the proviso that when R1 is methyl, R2 is chloro and R3 is H, then R4 or R5 is different from fluoro.
    Type: Application
    Filed: January 14, 2009
    Publication date: May 12, 2011
    Applicant: SYNGENTA CROP PROTECTION AG
    Inventors: Stephan Trah, Clemens Lamberth, Raphael Dumeunier, Sebastian Volker Wenderborn
  • Substituted Pyridazinone Derivatives as Histamine-3 (H3) Receptor Ligands
    Publication number: 20110098269
    Abstract: The present invention provides compounds according to Formulas I, II, III, IV, V, VI, VII or VIII: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.
    Type: Application
    Filed: November 17, 2010
    Publication date: April 28, 2011
    Applicant: Cephalon, Inc.
    Inventors: Nadine C. Becknell, Reddeppa reddy Dandu, Derek D. Dunn, Robert L. Hudkins, Kurt A. Josef, Babu G. Sundar, Allison L. Zulli
  • Protein kinase targeted therapeutics
    Patent number: 7919485
    Abstract: The present invention relates to compositions and methods useful in treating diseases and disorders related to protein kinases. In particular, the present invention relates to compositions and methods useful for targeting protein kinases related to mitogen activated protein kinase (MAPK) pathways (e.g., p38 MAPK, JNK, ERK, and upstream and downstream protein kinases) and/or casein kinase (CK) pathways (e.g., CK1?, and upstream and downstream protein kinases), and diseases and disorders related to MAPK pathways (e.g., p38 MAPK, JNK, ERK, and upstream and downstream protein kinases) and/or CK pathways (e.g., CK1?, and upstream and downstream protein kinases).
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: April 5, 2011
    Assignee: Northwestern University
    Inventors: D. Martin Watterson, Linda J. Van Eldik
  • PYRIDYL DERIVATIVES, THEIR PREPARATION AND USE
    Publication number: 20110077252
    Abstract: The present invention relates to pyridyl derivatives capable of inhibiting phosphatidylinositol-3-kinase (PI3k), mammalian target of rapamycin (mTOR) and/or hypoxia inducible factor 1? (HIF-1?) mediated signaling. Also disclosed are processes for preparation of the pyridyl derivatives, and their use in the manufacture of pharmaceutical compositions for the treatment of clinical conditions caused by deregulation of signaling pathways selected from one or more of PI3K, mTOR and HIF-1? pathways. The pyridyl derivatives are also useful for the treatment of conditions or disorders mediated by TNF-?.
    Type: Application
    Filed: August 6, 2008
    Publication date: March 31, 2011
    Inventors: Sanjay Kumar, Kalpana Sanjay Joshi, Vijaykumar Deore, Mandar Ramesh Bhonde, Nilambari Nilkanth Yewalkar, Amol Arun Padgaonkar, Asha Adrian Kulkarni-Almeida, Maggie Joyce Rathos, Sapna Parikh, Nilesh Madhukar Dagia
  • Azetidines as MEK inhibitors for the treatment of proliferative diseases
    Patent number: 7915250
    Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Grant
    Filed: May 5, 2010
    Date of Patent: March 29, 2011
    Assignee: Exelixis, Inc.
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • NEW HSL INHIBITORS USEFUL IN THE TREATMENT OF DIABETES
    Publication number: 20110065707
    Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof, wherein A1, A2, R1, R2, R3, R4, R5 and R6 have the significance given herein.
    Type: Application
    Filed: September 3, 2010
    Publication date: March 17, 2011
    Inventors: Jean Ackermann, Aurelia Conte, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
  • PYRIDAZINYL AMINE DERIVATIVES, THE USE THEREOF IN THE PREPARATION OF PICORNA VIRUS INHIBITORS
    Publication number: 20110059978
    Abstract: The present invention relates to substituted pyridazinylamine derivatives of the formula I or pharmaceutically acceptable salts or hydrates thereof, wherein the substituents are defined as in the description, their preparation process, pharmaceutical compositions comprising them, and uses of the said compounds as picorna virus inhibitors for prevention and/or treatment of diseases caused by picorna viruses.
    Type: Application
    Filed: November 15, 2010
    Publication date: March 10, 2011
    Inventors: Song LI, Chunlai MI, Zhibing ZHENG, Guoming ZHAO, Xinbo ZHOU, Zehui GONG
  • Piperidine/Cyclohexane Carboxamide Derivatives For Use as Vanilloid Receptor Modulators
    Publication number: 20110059979
    Abstract: Certain compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, P, P?, X, m and n are as defined in the specification, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.
    Type: Application
    Filed: August 12, 2004
    Publication date: March 10, 2011
    Applicant: GLAXO GROUP LIMITED
    Inventors: Craig Jamieson, David Drysdale Miller, Harshad Kantilal Rami, Mervyn Thompson
  • C-MET PROTEIN KINASE INHIBITORS
    Publication number: 20110059936
    Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides processes for preparing the compounds of this invention, pharmaceutically acceptable compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: November 9, 2010
    Publication date: March 10, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: David J. Lauffer, Robert J. Davies, Dean Stamos, Alexander Aronov, David D. Deininger, Ronald Grey, JR., Jinwang Xu, Pan Li, Brian Ledford, Luc Farmer, Randy Scott Bethiel, Dylan Jacobs, Kira McGinty
  • 4-[3-(ARYLOXY)BENZYLIDENE]-3-METHYL PIPERIDINE ARYL CARBOXAMIDE COMPOUNDS USEFUL AS FAAH INHIBITORS
    Publication number: 20110053949
    Abstract: The present invention relates to compounds of Formula (I), wherein Ar is optionally substituted phenyl or heteroaryl and X, Y and Z are independently N or CH; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity.
    Type: Application
    Filed: April 9, 2009
    Publication date: March 3, 2011
    Applicant: PFIZER INC.
    Inventors: Marvin Jay Meyers, Matthew James Pelc, Atli Thorarensen
  • PYRROLIDINES AS NK3 RECEPTOR ANTAGONISTS
    Publication number: 20110053948
    Abstract: The present invention relates to a compounds of formula I wherein R1, R2, Ar1, Ar2, R?, R?, m, n, and o are defined in the specification or to a pharmaceutically active salt, racemic mixture, enantiomer, optical isomer or to tautomeric form thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: August 16, 2010
    Publication date: March 3, 2011
    Inventors: Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angélique Patiny-Adam, Hasane Ratni, Claus Riemer
  • 4-BENZYLIDENE-3-METHYLPIPERIDINE ARYL CARBOXAMIDE COMPOUNDS USEFUL AS FAAH INHIBITORS
    Publication number: 20110053950
    Abstract: The present invention relates to compounds of Formula (I) wherein Ar is optionally substituted phenyl or heteroaryl; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity.
    Type: Application
    Filed: April 9, 2009
    Publication date: March 3, 2011
    Inventors: Marvin Jay Meyers, Matthew James Peic, Barbara Ann Schweitzer, Atli Thorarensen
  • Substituted Pyridazinylmethyl Sulfonamides
    Publication number: 20110039695
    Abstract: The present invention relates to pyridazinylmethyl sulfonamides of formula I wherein Ra, n, R1, R2, R3, A, Y and Het are as defined in the claims, to the N-oxides, and salts thereof and their use for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to a process and intermediates for preparing these compounds.
    Type: Application
    Filed: April 6, 2009
    Publication date: February 17, 2011
    Applicant: BASF SE
    Inventors: Alice Glättli, Wassilios Grammenos, Bernd Müller, Jan Klaas Lohmann, Marianna Vrettou
  • PYRIDAZINONE DERIVATIVES
    Publication number: 20110034474
    Abstract: Compounds of the formula (I), in which R1, R2, R3, W and D have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: March 24, 2009
    Publication date: February 10, 2011
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
  • Aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 7884104
    Abstract: The present invention is directed to novel substituted aminopiperidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: September 27, 2005
    Date of Patent: February 8, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason M. Cox, Scott D. Edmondson, Bart Harper, Ann E. Weber
  • Potassium channel inhibitors
    Patent number: 7879839
    Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: July 27, 2005
    Date of Patent: February 1, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman, Douglas C. Beshore, B. Wesley Trotter, Kausik K. Nanda, Richard Isaacs, Linda S. Payne, Lou Anne Neilson, Zhicai Wu, Mark T. Bilodeau, Peter J. Manley, Adrienne E. Balitza
  • OXAZOLE DERIVATIVES USEFUL AS INHIBITORS OF FAAH
    Publication number: 20110021531
    Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
    Type: Application
    Filed: July 27, 2009
    Publication date: January 27, 2011
    Inventors: Harry CHOBANIAN, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo