Plural Diazine Rings Patents (Class 544/357)
  • Publication number: 20130018046
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 17, 2013
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Xiaotian Zhu, Rajeswari Sundaramoorthi, Wei-Sheng Huang, Dong Zou, R. Mathew Thomas, Jiwei Qi, Jan Antoinette C. Romero, David C. Dalgarno, William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III
  • Patent number: 8354400
    Abstract: The present invention provides benzoxazole compounds and pharmaceutically acceptable salts thereof and pharmaceutical compositions including the same. The present invention further provides methods of use as described herein.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: January 15, 2013
    Assignee: Eisai R&D Co., Ltd.
    Inventors: Wanjun Zheng, Mark Spyvee, Fabian Gusovsky, Sally T. Ishizaka
  • Patent number: 8354401
    Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, or a hydrate or solvate thereof.
    Type: Grant
    Filed: October 27, 2009
    Date of Patent: January 15, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Seigo Ishibuchi, Hidemasa Hikawa, Akiko Tarao, Jun-ichi Endoh, Kunitomo Adachi, Kazuhiro Maeda, Kaoru Tashiro
  • Publication number: 20130004518
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: Merck, Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
  • Publication number: 20120328691
    Abstract: The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Application
    Filed: October 29, 2007
    Publication date: December 27, 2012
    Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards, Hongbo Zeng, Binyuan Sun, Panduranga Adulla Reddy, Tzu T. Wong, Praveen K. Tadikonda, M. Arshad Siddiqui, Marc A. Labroli, Cory Poker, Timothy J. Guzi
  • Publication number: 20120329807
    Abstract: Disclosed are conjugates which bind VLA-4. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such conjugates are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The conjugates can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Application
    Filed: September 7, 2012
    Publication date: December 27, 2012
    Applicant: ELAN PHARMACEUTICALS, INC.
    Inventors: Andrei Konradi, Michael A. Pleiss, Christopher M. Semko, Theodore Yednock, Jenifer L. Smith
  • Patent number: 8334288
    Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent; diseases or disorders associated with the activity of GPR119.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: December 18, 2012
    Assignee: IRM LLC
    Inventors: Robert Epple, Gerald Lelais, Victor Nikulin, Lucas Westcott-Baker
  • Publication number: 20120316178
    Abstract: The invention relates to novel piperazine derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.
    Type: Application
    Filed: January 4, 2011
    Publication date: December 13, 2012
    Inventors: Hamed Aissaoui, Christoph Boss, Olivier Corminboeuf, Bibia Heidmann, Romain Siegrist
  • Publication number: 20120302538
    Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/ and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.
    Type: Application
    Filed: May 29, 2012
    Publication date: November 29, 2012
    Applicant: ACHILLION PHARMACEUTICALS, INC
    Inventors: Jason Allan Wiles, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Venkat Gadhachanda, Avinash Phadke, Milind Deshpande, Dawei Chen
  • Patent number: 8318935
    Abstract: A compound of formula (I), or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein M1, M2, L1, L2, W1, W2, X1, X2, Y1, Y2, A, R5 and R5a are as defined herein for the for treatment of conditions treatable by the blockade of an epithelial sodium channel, particularly conditions benefiting from mucosal hydration.
    Type: Grant
    Filed: May 5, 2008
    Date of Patent: November 27, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Rebecca Butler, Paul Oakley, Stephen Paul Collingwood, Nichola Smith, Emily Stanley, Maria Ines Rodriguez Perez
  • Publication number: 20120295902
    Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
    Type: Application
    Filed: December 17, 2010
    Publication date: November 22, 2012
    Applicant: MERCK PATENT GMBH
    Inventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
  • Patent number: 8314091
    Abstract: The present invention relates to N-benzyl,N?-arylcarbonylpiperazine derivatives having the general formula I to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N?-arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.
    Type: Grant
    Filed: August 19, 2008
    Date of Patent: November 20, 2012
    Assignees: MSD OSS B.V., Pharmacopeia, Inc.
    Inventors: Koc-Kan Ho, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer, Andrew John Cooke, Andrew Stanley Edwards, David Jonathan Bennett
  • Publication number: 20120289513
    Abstract: The present invention relates to compounds of formula (I) The compounds act via antagonism of the CCR2b receptor and may be used to treat inflammatory disease and/or neuropathic pain.
    Type: Application
    Filed: July 25, 2012
    Publication date: November 15, 2012
    Applicant: ASTRAZENECA AB
    Inventors: John Cumming, Alan Wellington Faull, David Waterson
  • Publication number: 20120289495
    Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, Y, Q, X, B and L are as defined herein, and methods of making and using the same.
    Type: Application
    Filed: January 13, 2011
    Publication date: November 15, 2012
    Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
  • Publication number: 20120283256
    Abstract: The present invention relates to compounds having the following Formula (I) for use in the prevention and/or the treatment of diseases involving formation of amyloid plaques and/or where a dysfunction of the APP metabolism occurs.
    Type: Application
    Filed: December 16, 2010
    Publication date: November 8, 2012
    Inventors: Andre Delacourte, Patricia Melnyk, Stephane Burlet, Nicolas Lefur
  • Publication number: 20120277208
    Abstract: [Problem]A compound which is useful as a GK activator is provided. [Means for Solution] The present inventors have conducted studies on compounds having a GK activating action, which are promising as active ingredients of pharmaceutical compositions for the treatment of diabetes, type 2 diabetes mellitus, obesity, metabolic syndrome and related diseases caused by the aforementioned diseases, and as a result, they have confirmed that a benzamide compound of the present invention has an excellent GK activating action, thereby completing the present invention. That is, the benzamide compound of the present invention has a GK activating action and can be used as an agent for preventing and/or treating diabetes, type 2 diabetes mellitus, obesity, metabolic syndrome, and related diseases caused by the aforementioned diseases.
    Type: Application
    Filed: December 9, 2010
    Publication date: November 1, 2012
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Masahiko Hayakawa, Seiji Yoshimura, Daisuke Sasuga, Takanori Koike, Takahiro Nigawara, Mitsuaki Okumura, Keisuke Maki
  • Publication number: 20120277205
    Abstract: The present invention relates to compounds corresponding to formula (I): in which: A represents a divalent aromatic radical; X represents a —CH— group or a nitrogen atom; R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; R2 represents a group Alk; R3 represents a hydroxyl or a group —NR7R8; R4 represents a hydrogen atom, a halogen atom, a cyano, a phenyl, a group Alk, a group OAlk or a group —NR9R10; R5 represents a hydrogen atom, a halogen atom or a group Alk; R6 represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH2 group.
    Type: Application
    Filed: September 13, 2011
    Publication date: November 1, 2012
    Applicant: SANOFI
    Inventors: Alain Badorc, Christophe Boldron, Nathalie Delesque, Valérie Fossey, Gilbert Lassalle, Xavier Yvon
  • Publication number: 20120277244
    Abstract: The invention relates to novel heterocyclic compounds of the formula (I) in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
    Type: Application
    Filed: December 22, 2010
    Publication date: November 1, 2012
    Applicant: NOVARTIS AG
    Inventors: Marina Tintelnot-Blomley, Siem Jacob Veenstra
  • Patent number: 8293747
    Abstract: The present invention relates to novel heterocyclic amide compounds of Formula I: as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: October 23, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Panduranga Adulla P. Reddy, Lianyun Zhao, Praveen K. Tadikonda, Tzu Tshin Wong, Shuyi Tang, Luis E. Torres, David F. Cauble, Jr., Timothy J. Guzi, M. Arshad Siddiqui
  • Patent number: 8293769
    Abstract: Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.
    Type: Grant
    Filed: May 20, 2008
    Date of Patent: October 23, 2012
    Assignee: Novartis AG
    Inventors: Simon C. Ng, Keith B. Pfister, Martin Sendzik, James Sutton, Allan S. Wagman, Marion Wiesmann
  • Publication number: 20120260825
    Abstract: Dispersants for pigments as well as dispersions containing them, and compositions such as inks and coatings containing them are described. The dispersants are the reaction product of at least one dianhydride with at least two different reactants, each of which can be an amine, alcohol, or thiol, and at least one of which is polymeric.
    Type: Application
    Filed: June 20, 2012
    Publication date: October 18, 2012
    Inventors: Tatiana N. ROMANOVA, Russell J. SCHWARTZ
  • Publication number: 20120263706
    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 29, 2012
    Publication date: October 18, 2012
    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: 20120264747
    Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.
    Type: Application
    Filed: June 21, 2012
    Publication date: October 18, 2012
    Inventors: Bing-Yan Zhu, Michael Siu, Steven R. Magnuson, Richard Pastor, He Haiying, Xiao Yisong, Zheng Jifu, Xu Xing, Zhao Junping, Wendy Liu
  • Patent number: 8288541
    Abstract: The invention is concerned with novel piperazine amide derivatives of formula (I) wherein R1 to R11, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.
    Type: Grant
    Filed: August 6, 2008
    Date of Patent: October 16, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henrietta Dehmlow, Bernd Kuhn, Ulrike Obst Sander, Stephan Roever, Tanja Schulz-Gasch, Matthew Wright, Rene Wyler
  • Publication number: 20120252797
    Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.
    Type: Application
    Filed: June 18, 2012
    Publication date: October 4, 2012
    Applicants: Vernalis (Cambridge) Limited, The Institute of Cancer Research, Cancer Research Technology Ltd.
    Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
  • Publication number: 20120252789
    Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, M4, Y1, Y2, V, W, n, m and o have the meanings given in Claim 1, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.
    Type: Application
    Filed: November 22, 2010
    Publication date: October 4, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Frank Stieber, Dirk Wienke
  • Publication number: 20120245149
    Abstract: The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyI)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.
    Type: Application
    Filed: June 7, 2012
    Publication date: September 27, 2012
    Applicant: SANOFI
    Inventors: Marco BARONI, Françoise BONO, Sandrine DELBARY-GOSSART, Valentina VERCESI
  • Publication number: 20120245150
    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: Application
    Filed: June 7, 2012
    Publication date: September 27, 2012
    Applicant: SANOFI
    Inventors: Marco BARONI, Françoise BONO, Sandrine DELBARY-GOSSART, Valentina VERCESI
  • Patent number: 8273737
    Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: January 15, 2009
    Date of Patent: September 25, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Ronald K. Chang
  • Publication number: 20120238539
    Abstract: A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with —N, —O, or —S adjacent to the —Ar substituent or adjacent to the point of attachment for the —Ar substituent; Ar is aryl or heteroaryl; R is —CH3, —CH2F, or —CH?CH2; W is —NO2, —Cl, —Br, —CHO, —CH?CH2, or —CN; X is —Cl, —CH3, or —CN; Y is —CH or —N; and Z is C1-C6 alkyl, C3-C6 cycloalkyl, substituted aryl, substituted heteroaryl, OR1, or NHR1, wherein R1 is selected from the group of H, aryl, heteroaryl, C1-C6 alkyl and C3-C6 cycloalkyl. This compound is useful in compositions for the prevention and treatment of influenza virus.
    Type: Application
    Filed: September 6, 2011
    Publication date: September 20, 2012
    Inventors: Christopher W. Cianci, Samuel Gerritz, Guo Li, Bradley C. Pearce, Annapurna Pendri, Shuhao Shi, Weixu Zhai, Shirong Zhu
  • Publication number: 20120232088
    Abstract: This invention relates to piperazinedione compounds shown in the specification. These compounds are tyrosine kinase inhibitors and can be used to treat cancer.
    Type: Application
    Filed: February 24, 2012
    Publication date: September 13, 2012
    Applicants: National Taiwan University, Taipei Medical University
    Inventors: Hui-Po Wang, Che-Ming Teng, Chun-Li Wang, Jih-hwa Guh, Shiow-Lin Pan, Yuan-Yi Wang, Jang-Feng Lian
  • Publication number: 20120232064
    Abstract: Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Application
    Filed: March 15, 2012
    Publication date: September 13, 2012
    Applicant: SCHERING CORPORATION
    Inventors: Yusheng Wu, Ulrich Iserloh, Jared N. Cumming, Xiaoxiang Liu, Robert D. Mazzola, Zhong-Yue Sun, Ying Huang, Andrew Stamford, Brian McKittrick, Zhaoning Zhu
  • Patent number: 8262945
    Abstract: Photochromic compositions are disclosed comprising a polymeric material, a photochromic dye, a hydroxyphenyl triazine UV absorber and, optionally, a further light stabilizer selected from the sterically hindered amines. These systems provide a reversible photochromic effect and show improved light stabilization and color fastness.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: September 11, 2012
    Assignee: BASF SE
    Inventors: Mara Destro, Dario Lazzari, Dirk Simon, Manuele Vitali
  • Publication number: 20120225854
    Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: August 23, 2011
    Publication date: September 6, 2012
    Applicant: AMGEN INC.
    Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, JR., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
  • Publication number: 20120225875
    Abstract: Novel hetarylaminoquinoline derivatives of formula (I) wherein X, Z, Het, R1, R2, R3 and R4 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
    Type: Application
    Filed: October 12, 2010
    Publication date: September 6, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Alfred Jonczyk, Christiane Amendt, Frank Zenke
  • Publication number: 20120220562
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Application
    Filed: February 24, 2012
    Publication date: August 30, 2012
    Applicant: ABBOTT LABAORATORIES
    Inventors: David A DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Yi Gao, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, David A. Betebenner, Kathy Sarris, Kevin R. Woller, William A. Carroll
  • Publication number: 20120220561
    Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: August 12, 2011
    Publication date: August 30, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, John D. HUBER, Ho Yin LO, Pui Leng LOKE, Weimin LIU, Tina Marie MORWICK, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
  • Publication number: 20120220596
    Abstract: The present invention provides cysteine and cystine prodrugs for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing prodrugs and methods of using the prodrugs and compositions for treatment of schizophrenia and drug addiction.
    Type: Application
    Filed: May 7, 2012
    Publication date: August 30, 2012
    Applicants: UWM RESEARCH FOUNDATION, INC., MARQUETTE UNIVERSITY
    Inventors: James M. Cook, David A. Baker, Wenyuan Yin, Edward Merle Johnson, II
  • Publication number: 20120208798
    Abstract: Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Application
    Filed: November 3, 2010
    Publication date: August 16, 2012
    Inventors: Emmanuel Hubert Demont, Neil Stuart Garton, Romain Luc Marie Gosmini, Thomas George Christopher Hayhow, Jonathan Seal, David Matthew Wilson, Michael David Woodrow
  • Publication number: 20120202823
    Abstract: The present invention accomplishes this by having multiple molecules of parent drugs attached to carrier moieties and by extending the period during which the parent drug is released and absorbed after administration to the patient and providing a longer duration of action per dose than the parent drug itself. Prodrug conjugates are suitable for sustained delivery of heteroaryl, lactam- amide-, imide-, sulfonamide-, carbamate-, urea-, benzamide-, acylaniline-, cyclic amide- and tertiary amine-containing parent drugs that are substituted at the amide nitrogen or oxygen atom with labile aldehyde-linked prodrug moieties. The carrier groups of the prodrugs can be hydrophobic to reduce the polarity and solubility of the parent drug under physiological conditions.
    Type: Application
    Filed: December 22, 2011
    Publication date: August 9, 2012
    Inventors: Tarek A. Zeidan, Laura Cook Blumberg
  • Publication number: 20120197013
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: April 9, 2012
    Publication date: August 2, 2012
    Applicant: Sirtris Pharmaceuticals, Inc.
    Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch
  • Publication number: 20120196378
    Abstract: This invention pertains to methods, mixtures, kits and compositions pertaining to analyte determination by mass spectrometry using labeling reagents that comprise a nucleophilic reactive group that reacts with a functional group of an analyte to produce a labeled analyte. The labeling reagents can be used as isobaric sets, mass differential labeling sets or in a combination of isobaric and mass differential labeling sets.
    Type: Application
    Filed: January 31, 2011
    Publication date: August 2, 2012
    Inventors: Subhasish Purkayastha, Subhakar Dey, Scott B. Daniels
  • Publication number: 20120196844
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.
    Type: Application
    Filed: March 16, 2012
    Publication date: August 2, 2012
    Applicant: IRM LLC
    Inventors: Phillip B. Alper, Mihai Azimioara, Christopher Cow, Robert Epple, Songchun Jiang, Gerald lelais, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin, Lucas Westcott-Baker
  • Patent number: 8232277
    Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.
    Type: Grant
    Filed: October 2, 2007
    Date of Patent: July 31, 2012
    Assignee: Erimos Pharmaceuticals LLC
    Inventors: Qingqi Chen, Jonathan Daniel Heller, Rocio Alejandra Lopez, Amanda Jean Morris
  • Publication number: 20120190846
    Abstract: The present invention provides a Michael addition reaction product between a specified compound having a group which functions as a Michael donor and a monomer or polymer having a group which functions as a Michael acceptor, a photoinitiator containing the Michael addition reaction product, and an active energy ray-curable composition containing the photoinitiator. The compound having a group functioning as a Michael donor used in the present invention is a phenyl ketone derivative and is characterized by having an amino group or a mercapto group as the group functioning as a Michael donor.
    Type: Application
    Filed: June 28, 2010
    Publication date: July 26, 2012
    Applicant: DIC CORPORATION.
    Inventors: Kutzner Fabian, Gaudl Kai-uwe, Yoshinobu Sakurai, Tatsushi Okuda
  • Publication number: 20120189539
    Abstract: Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.
    Type: Application
    Filed: January 24, 2012
    Publication date: July 26, 2012
    Applicant: THE REGENTS OF UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Haibin Zhou, Jianfang Chen, Angelo Aguilar, Jennifer L. Meagher, Duxin Sun, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachem, Jeanne Stuckey, Xiaoqin Li
  • Publication number: 20120190686
    Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Application
    Filed: December 22, 2011
    Publication date: July 26, 2012
    Applicant: H. LUNDBECK A/S
    Inventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
  • Publication number: 20120190687
    Abstract: Pyrazin-2-ylpyrazoles are described, as is the use thereof as insecticides and/or parasiticides. Additionally described are processes for preparation thereof, and compositions which comprise such pyrazin-2-ylpyrazoles.
    Type: Application
    Filed: May 19, 2010
    Publication date: July 26, 2012
    Inventors: Hans-Georg Schwarz, Jens Frackenpohl, Achim Hense, Simon Maechling, Stefan Schnatterer, Robert Velten, Stefan Werner, Angela Becker, Olga Malsam, Eva-Maria Franken, Arnd Voerste, Ulrich Görgens, Peter Lümmen
  • Publication number: 20120184524
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: December 1, 2011
    Publication date: July 19, 2012
    Inventors: Dean Boyall, Guy Brenchley, Damien Fraysse, Juan-Miguel Jimenez, Luca Settimo
  • Publication number: 20120183579
    Abstract: The invention relates to certain compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: January 17, 2012
    Publication date: July 19, 2012
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Gary Bohnert, Zhiqiang Xia, Shoujun Chen, Lijun Sun