Ring Nitrogen Is Shared By Two Of The Cyclos (e.g., Ergot, Alkaloids, Etc.) Patents (Class 544/346)
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Publication number: 20100204201Abstract: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: April 15, 2010Publication date: August 12, 2010Inventors: Joseph P. Vacca, Linda S. Payne, Richard C.A. Isaacs
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Publication number: 20100190763Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: January 21, 2010Publication date: July 29, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Patent number: 7754712Abstract: The invention provides N-cyclic sulfonamido compounds and salts of Formula I: wherein A is as described in the specification and R1 and R2 combine to form a [3.3.1] or a [3.2.1] ring system, where the nitrogen is attached to the two bridgehead carbons, and the [3.3.1] or [3.2.1] ring systems are optionally fused with an heteroaryl or heterocycloalkyl ring. Compounds of Formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's Disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of treating cognitive disorders, such as Alzheimer's disease, and the intermediates useful in preparing the compounds of Formula I.Type: GrantFiled: December 5, 2007Date of Patent: July 13, 2010Assignee: Elan Pharmaceuticals, Inc.Inventors: Simeon Bowers, Albert W. Garofalo, Roy K. Hom, Andrei W. Konradi, Matthew N. Mattson, Martin L. Neitzel, Christopher M. Semko, Anh P. Truong, Jing Wu, Ying-zi Xu
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Patent number: 7750010Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, T, U, V, W, X, Y, Z, R4, R5a?, R5b, R5c, R6, m and n are defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.Type: GrantFiled: September 9, 2005Date of Patent: July 6, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Steven N. Gallicchio, C. Blair Zartman, Cory R. Theberge, Xufang Zhang
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Publication number: 20100160334Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R5c, m and n are defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.Type: ApplicationFiled: March 5, 2010Publication date: June 24, 2010Inventors: Ian M. Bell, Steven N. Gallicchio, Graig A. Stump, Cory R. Theberge, Joseph P. Vacca, C. Blair Zartman, Xufang Zhang
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Publication number: 20100137282Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials. Z1 and Z2 are independently selected from CH and N.Type: ApplicationFiled: April 16, 2008Publication date: June 3, 2010Inventors: David Evan Davies, David Thomas Davies, Ilaria Giordano, Alan Joseph Hennessy, Neil David Pearson
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Publication number: 20100130489Abstract: The invention relates to Imidazolo-heteroaryl derivatives of formula (I). The compounds inhibit the activity of the Dlta enzyme of Gram-positive bacteria and are useful to treat Gram-positive bacterial infections. Furthermore the application discloses method for assessing the Dlta inhibitory activity of tested molecules and a method for measuring the efficacy of molecules in inhibiting bacteria proliferation in vitro.Type: ApplicationFiled: March 21, 2008Publication date: May 27, 2010Applicant: MUTABILIS SAInventors: Sonia Escaich, Alexis Denis, Vincent Gerusz, Francois Moreau, Mayalen Oxoby, Yannick Bonvin
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Publication number: 20100120781Abstract: Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating cell growth, cell cycle, apoptosis, or gene expression.Type: ApplicationFiled: June 8, 2009Publication date: May 13, 2010Inventor: Nouri Neamati
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Publication number: 20100120741Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.Type: ApplicationFiled: September 10, 2009Publication date: May 13, 2010Applicants: Kalypsys, Inc., Alcon Research, LtdInventors: Allen J. Borchardt, Clay Beauregard, Travis Cook, Robert L. Davis, Daniel A. Gamache, John M. Yanni
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Patent number: 7687086Abstract: A method for obtaining a taxane by which a taxane is isolated from a growth medium, such as soil, pumice, perlite, rocks, and/or gravel in which a taxane-producing plant has grown. A method for obtaining a taxane by which a taxane is isolated from water effluent from plantings of living plants (e.g. a yew tree) that produce a taxane have grown in a growth medium, such as soil, pumice, perlite, rocks, and/or gravel.Type: GrantFiled: September 11, 2006Date of Patent: March 30, 2010Assignee: University of PortlandInventor: Angela Marie Hoffman
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Publication number: 20100048556Abstract: The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) in the formula, R1 and R2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like, R3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like, R4 stands for hydrogen, hydroxy, alkyl or amino, R5 and R8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro, R6 and R7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR9 or SO2R9, R9 stands for hydrogen, hydroxy, alkyl, amino, pyrrolidin-1-yl, piperidin-1-yl, pyperazin-1-yl or the like, X stands for S or O, and A1, A2 and A3 each independently stands for N or C.Type: ApplicationFiled: December 12, 2007Publication date: February 25, 2010Inventors: Makoto Okada, Shuichiro Sato, Kenji Kawade, Kotaro Gotanda, Atsushi Shinbo, Youichi Nakano, Hideo Kobayashi
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Publication number: 20100022508Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: July 24, 2009Publication date: January 28, 2010Applicant: Gilead Sciences, Inc.Inventors: Evangelos Aktoudianakis, Azim Alan Celebi, Zhimin Du, Salman Y. Jabri, Haolun Jin, Choung U. Kim, Jiayao Li, Samuel E. Metobo, Michael R. Mish, Barton W. Phillips, Joseph H. Saugier, Zheng-Yu Yang, Catalin Sebastian Zonte
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Publication number: 20090318421Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.Type: ApplicationFiled: April 28, 2006Publication date: December 24, 2009Inventors: Brian Alvin Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
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Publication number: 20090312338Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: June 9, 2009Publication date: December 17, 2009Applicant: ABBOTT LABORATORIESInventors: Neil Wishart, Maria A. Argiriadi, David J. Calderwood, Anna M. Ericsson, Bryan A. Fiamengo, Kristine E. Frank, Michael Friedman, Dawn M. George, Eric R. Goedken, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Kent D. Stewart, Jeffrey W. Voss, Grier A. Wallace, Lu Wang, Kevin R. Woller
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Publication number: 20090311288Abstract: The invention proyides novel compositions comprising imidazoquinoxaline compounds of formula (I) and analogs thereof. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of administering the compositions in combination with (an) other agent (s).Type: ApplicationFiled: March 23, 2007Publication date: December 17, 2009Applicant: Novartis AGInventors: James Sutton, Feng Xu, Nicholas M. Valiante, JR., Jiong Lan
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Publication number: 20090306089Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof: (relative chemistry shown) pharmaceutical compositions comprising them, their use in therapy especially against tuberculosis, and methods of preparing them are described.Type: ApplicationFiled: May 21, 2009Publication date: December 10, 2009Inventors: Carlos Alemparte-Gallardo, Christopher Barfoot, David Barros-Aguirre, Monica Cacho-Izquierdo, Jose Maria Fiandor Roman, Alan Joseph Hennessy, Neil David Pearson, Modesto Jesus Remuinan-Blanco
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Patent number: 7625888Abstract: The present invention is directed to novel fused triazole derivatives 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: GrantFiled: August 19, 2005Date of Patent: December 1, 2009Assignee: Merck & Co., Inc.Inventors: Ann E. Weber, Wallace T. Ashton
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Patent number: 7626019Abstract: Disclosed are processes for the preparation of fused piperazin-2-one derivatives of general formula (I) wherein the groups R1 to R5, A1 and A2 have the meanings given in the claims and in the description, particularly the preparation of 7,8-dihydro-5H-pteridin-6-one derivatives and intermediates thereof.Type: GrantFiled: May 16, 2007Date of Patent: December 1, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Adil Duran, Guenter Linz
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Publication number: 20090281080Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, D2, E1, E2, E3, E4, E5, G1, G2, R6, T, U, V, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.Type: ApplicationFiled: November 14, 2006Publication date: November 12, 2009Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Steven N. Gallicchio, C. Blair Zartman
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Publication number: 20090233936Abstract: The present invention is directed to novel substituted fused aminopiperidines of structural formula (I) which are inhibitors of the dipeptidyl peptidase-4 enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-4 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-4 enzyme is involved.Type: ApplicationFiled: December 8, 2006Publication date: September 17, 2009Applicant: MERCK & CO., INC.Inventors: Jason M. Cox, Scott D. Edmondson, Anthony Mastracchio
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Publication number: 20090233274Abstract: The present invention provides novel target proteins and target genes for drug discovery, and the means that enable the development of novel drugs using the same. More particularly, the present invention provides NCS proteins and genes thereof; screening methods for drug (for example, anti-central nervous disease drug); agents for regulating disease (for example, central nervous disease); production methods of a drug derivative; a complex comprising a drug and NCS protein, and a method of producing the complex; a kits comprising a drug or a salt thereof; determination methods for the onset or risk of onset of a specified disease, determination methods for susceptibility to a drug, and determination kits used for the determination methods; and the like.Type: ApplicationFiled: October 9, 2005Publication date: September 17, 2009Applicant: Reverse Proteomics Research Institute Co.Inventors: Tadakazu Yamauchi, Hideaki Sueoka, Koichi Tsuchiya, Katsuhisa Murayama, Ken Horiuchi, Kazuo Komiya, Morikazu Kito, Takeshi Kito, Takeshi Tsutsumi, Yuko Isono, Yorimasa Suwa
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Patent number: 7579351Abstract: The present invention relates to compounds of formula I wherein A, G, r and R1 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: November 29, 2006Date of Patent: August 25, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Patent number: 7576209Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: December 4, 2007Date of Patent: August 18, 2009Assignee: Merck & Co., Inc.Inventors: Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
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Patent number: 7550465Abstract: The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating diseases of mammals including a human which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 10 activity in the central nervous system. More particularly, the invention relates to the treatment of neurologic and psychiatric disorders, for example psychosis and disorders comprising cognitive deficits as symptoms.Type: GrantFiled: May 24, 2007Date of Patent: June 23, 2009Assignee: Elbion GmbHInventors: Norbert Höfgen, Hans Stange, Barbara Langen, Ute Egerland, Rudolf Schindler, Thomas Pfeifer, Chris Rundfeldt
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Patent number: 7547699Abstract: The present invention refers to chemical compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in claim 1. These compounds can be used for the preparation of medicaments.Type: GrantFiled: April 26, 2006Date of Patent: June 16, 2009Assignees: Hoffmann-La Roche Inc., Vernalis Research LimitedInventors: Paul Hebeisen, Nathaniel Monck, Hans Richter, Stephan Roever
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Publication number: 20090143361Abstract: The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical compositions which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating central nervous system disorders, obesity, and metabolic disorders.Type: ApplicationFiled: November 25, 2008Publication date: June 4, 2009Applicants: ELBION GMBH, WYETHInventors: Michael S. Malamas, Yike Ni, James Joseph Erdei, Hans Stange, Rudolf Schindler, Norbert Hofgen, Ute Egerland, Barbara Langen
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Publication number: 20090143391Abstract: The invention relates to imidazo[1,5-a]pyrazine derivatives, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans.Type: ApplicationFiled: December 1, 2008Publication date: June 4, 2009Inventors: Norbert Hofgen, Hans Stange, Barbara Langen, Ute Egerland, Rudolf Schindler
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Publication number: 20090143367Abstract: The invention relates to imidazo[1,5-a]pyrazine derivatives, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans.Type: ApplicationFiled: November 25, 2008Publication date: June 4, 2009Applicants: ELBION GMBH, WYETHInventors: Michael S. Malamas, Yike Ni, James Joseph Erdei, Norbert Hofgen, Hans Stange, Rudolf Schindler, Ute Egerland, Barbara Langen
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Patent number: 7511041Abstract: The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-? inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-? activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoixnmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis.Type: GrantFiled: September 18, 2003Date of Patent: March 31, 2009Assignee: Bayer Pharmaceuticals CorporationInventors: Mitsuyuki Shimada, Toshiki Murata, Kinji Fuchikami, Hideki Tsujishita, Naoki Omori, Issei Kato, Mami Miura, Klaus Urbahns, Florian Gantner, Kevin Bacon
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Publication number: 20090054399Abstract: Tricyclic compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: May 5, 2006Publication date: February 26, 2009Inventors: Joseph P. Vacca, John S. Wai, Linda S. Payne, Richard C.A. Isaacs, Wei Han, Melissa Egbertson, Richard Pracitto
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Publication number: 20090042873Abstract: The invention concerns tricyclic N-heteroarylcarboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: ApplicationFiled: August 1, 2008Publication date: February 12, 2009Applicant: SANOFI-AVENTISInventors: Laurent DUBOIS, Yannick EVANNO, Luc EVEN, Catherine GILLE, Andre MALANDA, David MACHNIK, Nathalie RAKOTOARISOA
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Patent number: 7476666Abstract: Bicyclic pyrazoles of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein Z is O or N(R8); n is an integer equal to zero or 1; and R1, R2, R3, R4, R5, R6, R7 and R8 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: June 3, 2005Date of Patent: January 13, 2009Assignee: Merck & Co., Inc.Inventors: John S. Wai, Peter D. Williams, H. Marie Langford
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Publication number: 20080261974Abstract: This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 proteins.Type: ApplicationFiled: September 22, 2006Publication date: October 23, 2008Inventors: Kevin J Duffy, Duke M. Fitch, Rosanna Tedesco, Michael N. Zimmerman
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Patent number: 7432267Abstract: Disclosed are compounds having the formula (I): including compounds of formulae (Ia) and (Ib): wherein G is an optionally substituted aryl or heterocyclo, L is an optional linker, M is a bond, O, CR7R7? or NR10, and M? is a bond or NR10, with the proviso that at least one of M or M? must be a bond; E is C=Z2, CR7CR7?, SO2, P?OR2, or P?OOR2; Z1 is O, S, NH, or NR6; A1 is CR7 or N; A2 is CR7 or N; Y is J-J?-J? where J is (CR7R7?)n and n=0?3, J? is a bond or O, S, S?O, SO2, NH, NR6, C?O, CO?O, NR1C?O, CR7R7?, C?CR8R8?, R2P?O, OPOOR2, OPO2, OSO2, C?N, NHNH, NHNR6, NR6NH, N?N, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo or aryl or substituted aryl, and J? is (CR7R7?)n and n=0?3; and W, Q, R2, R6, R7, R7?, R8, R8?, R9, R9?, and R10 are as defined in the specification and/or claims herein, to methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and toType: GrantFiled: June 28, 2005Date of Patent: October 7, 2008Assignee: Bristol-Myers Squibb ComapnyInventors: Mark E. Salvati, James Aaron Balog, Weifang Shan, Sören Giese, Lalgudi S. Harikrishnan
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Patent number: 7420056Abstract: Substituted bicyclic imidazo-3-yl-amine compounds are provided, as well as processes for the production thereof and pharmaceutical formulations containing these compounds. The use of these compounds for the production of pharmaceutical formulations and related methods of treatment are also provided.Type: GrantFiled: March 14, 2007Date of Patent: September 2, 2008Assignee: Gruenenthal GmbHInventors: Sven Kuehnert, Stefan Oberboersch, Corinna Sundermann, Michael Haurand, Ruth Jostock, Klaus Schiene, Thomas Tzschentke, Thomas Christoph, Dagmar Kaulartz, Saskia Zemolka
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Publication number: 20080161317Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: December 4, 2007Publication date: July 3, 2008Inventors: Michael J. Kelly, Mark E. Layton, Philip E. Sanderson
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Patent number: 7268215Abstract: By using a bioluminescence, a method for detection of a monovalent cation is provided and the method is a high sensitive and simple method. According to the present invention, an amino acid sequence of symplectin and a base sequence encoding the protein are provided. Symplectin is a photoprotein derived from Symplectoteuthis oualaniensis (okinawan squid). By using the photoprotein of the present invention, a monovalant cation can be detected by luminescence in the presence of a chromophore.Type: GrantFiled: April 30, 2004Date of Patent: September 11, 2007Assignee: Nagoya UniversityInventors: Minoru Isobe, Tsukasa Matsuda
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Publication number: 20070173508Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders.Type: ApplicationFiled: January 23, 2007Publication date: July 26, 2007Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Thomas Jonathan Seiders, Brian Andrew Stearns, Bowei Wang, Jill Melissa Scott, Yen Pham Truong
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Patent number: 7208494Abstract: The present invention provides piperazine derivatives of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in the description. They can be used for the treatment of obesity.Type: GrantFiled: June 25, 2004Date of Patent: April 24, 2007Assignees: Hoffmann-La Roche Inc., Vernalis Research LimitedInventors: Toby Jonathan Blench, Paul Hebeisen, Hans Richter, Stephan Roever
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Patent number: 7202245Abstract: The present invention provides compounds of formula (I) the prodrugs thereof, and the pharmaceutically acceptable salts of the compounds and prodrugs, wherein Ra, Rb, R1, and R2 are as defined herein; pharmaceutical compositions thereof; and uses thereof.Type: GrantFiled: March 22, 2004Date of Patent: April 10, 2007Assignee: Pfizer Inc.Inventors: John W. Benbow, Margaret Y. Chu-Moyer, Daniel W. Kung
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Patent number: 7098338Abstract: This invention provides compounds of formula I, wherein R is hydrogen or alkyl of 1–6 carbon atoms; R? is hydrogen, alkyl of 1–6 carbon atoms, acyl of 2–7 carbon atoms, or aroyl; R1, R2, R3, and R4 are each, independently, hydrogen, alkyl of 1–6 carbon atoms, alkoxy of 1–6 carbon atoms, halogen, trifluoroalkyl, or trifluoroalkoxy of 1–6 carbon atoms; X is CR5R6 or a carbonyl group; R5 and R6 are each, independently, hydrogen or alkyl of 1–6 carbon atoms; or a pharmaceutically acceptable salt thereof, with the proviso that at least two of R1, R2, R3, or R4 are not hydrogen; which are 5HT2C receptor agonists useful for the treatment of disorders involving the central nervous system such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorders, eating disorders, obesity, type II diabetes, and epilepsy.Type: GrantFiled: December 1, 2003Date of Patent: August 29, 2006Assignee: WyethInventors: Annmarie Louise Sabb, Gregory Scott Welmaker, James Albert Nelson
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Patent number: 7098337Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts, solvates and esters thereof. These compounds can be used to prepare pharmaceutical compositions for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.Type: GrantFiled: January 24, 2003Date of Patent: August 29, 2006Assignees: Hoffmann-La Roche Inc., Vernalis Research LimitedInventors: David Reginald Adams, Jonathan Mark Bentley, Toby Jonathan Blench, Paul Hebeisen, Nathaniel Julius Thomas Monck, Hans Richter, Stephan Roever, Jonathan Richard Anthony Roffey, Sven Taylor
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Patent number: 6998485Abstract: The compound 3a,8a-bis-azidomethyl-3a,4,8a,9-tetrahydro-3H,8H-bis-[1,2,3]triazolo[1,5-a;1?,5?-d]pyrazine, whose structure is depicted below, is disclosed:Type: GrantFiled: August 15, 2003Date of Patent: February 14, 2006Assignee: The United States of America as represented by the Secretary of the ArmyInventors: Paritosh R. Dave, Raja G. Duddu, Reddy Damavarapu, Nathaniel Gelber, Kathy Yang, C. Rao Surapaneni
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Patent number: 6953801Abstract: Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: GrantFiled: May 21, 2002Date of Patent: October 11, 2005Assignee: Neurogen CorporationInventors: Alan Hutchison, Linda M. Gustavson, John M. Peterson, Dario Doller, Timothy M. Caldwell, Taeyoung Yoon, Wallace C. Pringle, Yiping Shen, Cheryl Steenstra
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Patent number: 6933294Abstract: Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates and prodrugs thereof, are useful as anti-inflammatory agents, in which R1, R2, and R3 are hydrogen, halogen, alkyl, or perfluoroalkyl; R4 is an optionally substituted alkyl or cycloalkyl group; X is a linker; A is an aryl, heteroaryl, heterocycle, cycloalkyl, or is absent; and R7 is a substituent on A as defined in the specification.Type: GrantFiled: March 27, 2003Date of Patent: August 23, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Makonen Belema, Amy Bunker, Van Nguyen, Francis Beaulieu, Carl Ouellet, Anne Marinier, Stephan Roy, Xuejie Yang, Yuping Qiu, Yunhui Zhang, Alain Martel, Christopher Zusi
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Patent number: 6869955Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric and neurological disorders.Type: GrantFiled: January 29, 2002Date of Patent: March 22, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Richard Gerald Wilde
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Publication number: 20040229879Abstract: Compounds are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, including stroke.Type: ApplicationFiled: February 23, 2004Publication date: November 18, 2004Applicant: Neurocrine Biosciences, Inc.Inventors: Mustapha Haddach, Zhiqiang Guo, James R. McCarthy
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Publication number: 20040192698Abstract: The present invention provides compounds of formula (I) 1Type: ApplicationFiled: March 22, 2004Publication date: September 30, 2004Applicant: Pfizer Inc.Inventors: John W. Benbow, Margaret Y. Chu-Moyer, Daniel W. Kung
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Publication number: 20040180898Abstract: Novel processes for the preparation of imidazoquinoxalinones, heterocyclic-substituted imidazopyrazinones, imidazoquinoxalines and heterocyclic-substituted imidazopyrazines are described.Type: ApplicationFiled: March 3, 2003Publication date: September 16, 2004Inventors: Bang-Chi Chen, Joseph E. Sundeen, Mark S. Bednarz, Ping Chen
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Publication number: 20040157851Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.Type: ApplicationFiled: November 4, 2003Publication date: August 12, 2004Applicant: Neurocrine Biosciences, Inc.Inventors: Mustapha Haddach, Brian P. Dyck, Charles Q. Huang, Jodie Nelson, Zhiqiang Guo, James R. McCarthy