Plural -c(=x)- Groups Bonded Directly To The Piperazine Ring Patents (Class 544/387)
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Patent number: 11891402Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.Type: GrantFiled: November 23, 2022Date of Patent: February 6, 2024Assignee: The Regents of the University of CaliforniaInventors: Jonathan Ostrem, Ulf Peters, Kevan M. Shokat
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Patent number: 10800750Abstract: The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes.Type: GrantFiled: September 10, 2019Date of Patent: October 13, 2020Assignee: FORMA Therapeutics, Inc.Inventors: Kenneth W. Bair, David R. Lancia, Jr., Hongbin Li, James Loch, Wei Lu, Matthew W. Martin, David S. Millan, Shawn E. R. Schiller, Mark J. Tebbe
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Patent number: 8969354Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.Type: GrantFiled: November 9, 2012Date of Patent: March 3, 2015Assignee: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Publication number: 20150038493Abstract: The present invention relates to a series of molecules derived from 2,3-diaminopropionic acid (DAP), comprising or not comprising an 8-hydroxyquinoline (8-HQ) motif, and to the use of said molecules for trapping an alpha-oxoaldehyde resulting particularly from the degradation of the glucose or for trapping an alpha-beta-unsaturated aldehyde, resulting particularly from the oxidative degradation of fatty acids. These molecules can have a further application in the fields of cosmetics, food processing, and pharmaceuticals.Type: ApplicationFiled: October 5, 2012Publication date: February 5, 2015Inventors: Guy Potier, André Nobumichi Sasaki, Nicolas Audic
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Patent number: 8871765Abstract: Disclosed are compounds of general formula (I), their stereoisomers, regioisomers, tautomeric forms and novel intermediates involved in their synthesis, their pharmaceutically acceptable salts. These compounds are suitable as Poly(ADP-ribose)polymerase-1 inhibitors (PARP-1 inhibitors).Type: GrantFiled: July 7, 2011Date of Patent: October 28, 2014Assignee: Cadila Healthcare LimitedInventor: Brijesh Kumar Shrivastava
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Publication number: 20140288045Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
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Patent number: 8557820Abstract: Disclosed is the use of an aqueous dispersion comprising (a) a micronized sparingly soluble organic benzophenone derivative of formula (1), selected from the crystal modifications (B) and (C), wherein the crystal modification (B) is characterized by a peak in the X-ray diffraction pattern at a d-spacing of about 7.70; and wherein the crystal modification (C) is characterized by a peak in the X-ray diffraction pattern at a d-spacing of about 7.06; and (b) a dispersing agent selected from anionic, non-ionic and amphoteric surfactants; for protecting the human skin from browning and skin aging. The new crystal modification (C) represents a thermodynamically stable compound of formula (1) at 25° C. This modification is therefore suitable in dispersions comprising micro-fine particles.Type: GrantFiled: April 28, 2008Date of Patent: October 15, 2013Assignee: BASF SEInventors: Martin Vogt, Stefan Müller, Julie Grumelard, Cyrille Deshayes, Holger Paul, Jürg Haase, Thomas Ehlis
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Publication number: 20130190327Abstract: The invention relates to bis-fatty acid conjugates; compositions comprising an effective amount of a bis-fatty acid conjugate; and methods for treating or preventing cancer, a metabolic disease or a neurodegenerative disease comprising the administration of an effective amount of a bis-fatty acid conjugate.Type: ApplicationFiled: February 25, 2011Publication date: July 25, 2013Applicant: CATABASIS PHARMACEUTICALS INCInventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Publication number: 20130065909Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.Type: ApplicationFiled: November 9, 2012Publication date: March 14, 2013Applicant: CATABASIS PHARMACEUTICALS, INC.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Publication number: 20130035329Abstract: Compounds and compositions comprising compounds useful in the treatment of cancer are described herein.Type: ApplicationFiled: June 8, 2012Publication date: February 7, 2013Inventors: Jeffrey O. Saunders, Francesco G. Salituro
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Patent number: 8329901Abstract: The present invention provides 4,6-disubstituted pyrimidine compound useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: February 1, 2011Date of Patent: December 11, 2012Assignee: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
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Patent number: 8287969Abstract: An isosorbide derivative of Formula (I) is provided. In Formula (I), Z is —CH2—CH2—, —CH?CH—, —C?C—, —CH2—O—, —CH2—S—, —CH?N—O—, —CO—O—, —CO—S—, single bond, -ph-, —CO—O-ph- or —CO—O-ph-CO—O—, and ph represents benzene, R1 and R2 are, independently, C1-25 alkyl, —CN, —NCS, —CX3 or —OCX3, and X represents halogen, and m and n are, independently, 0, 1 or 2. The invention also provides a liquid crystal display including the isosorbide derivative.Type: GrantFiled: December 15, 2010Date of Patent: October 16, 2012Assignee: Industrial Technology Research InstituteInventors: Chun-Ming Wu, Kevin Lin, Shih-Hsien Liu, Chih-Lung Chin, An-Cheng Chen, Kung-Lung Cheng, Chien-Hsien Cheng
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Publication number: 20120258960Abstract: The invention relates to compounds of the general formula (1) or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formula (1) in medicine.Type: ApplicationFiled: August 26, 2010Publication date: October 11, 2012Applicant: IMTM GMBHInventors: Siegfried Ansorge, Ute Bank, Karsten Nordhoff, Peter Roehnert, Sofia Stefin, Frank Striggow, Michael Taeger
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Publication number: 20120238585Abstract: The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.Type: ApplicationFiled: March 22, 2012Publication date: September 20, 2012Applicant: CATABASIS PHARMACEUTICALS, INC.Inventors: Jill C. MILNE, Michael R. Jirousek, Jean E. Bemis, Jesse J. Smith
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Publication number: 20120238756Abstract: The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.Type: ApplicationFiled: March 22, 2012Publication date: September 20, 2012Applicant: CATABASIS PHARMACEUTICALS, INC.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Jesse J. Smith
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Publication number: 20120101087Abstract: The present invention relates to, in part, novel bisphenol compounds useful for the recognition, attachment and growth of unwanted biologics on natural and manmade surfaces. Another aspect of the invention relates to combinatorial libraries for producing the same. Another aspect of the invention relates to pharmaceutical formulations comprising the same.Type: ApplicationFiled: December 12, 2008Publication date: April 26, 2012Inventors: Randall S. Alberte, Robert D. Smith
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Patent number: 8114880Abstract: The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.Type: GrantFiled: October 22, 2007Date of Patent: February 14, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Joannes Theodorus Maria Linders, Libuse Jaroskova, Marcel Viellevoye, Leo Jacobus Jozef Backx, Didier Jean-Claude Berthelot, Guuske Frederike Busscher
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Patent number: 8097240Abstract: Disclosed is the use of an aqueous dispersion comprising (a) a micronized sparingly soluble organic compound which has a UV-Vis spectrum with a maximum from 380 to 420 nm; and (b) an anionic dispersing agent for protecting the human skin from browning and skin aging.Type: GrantFiled: December 11, 2006Date of Patent: January 17, 2012Assignee: BASF SEInventors: Stefan Müller, Jürg Haase, Thomas Ehlis, Gilbert Kreyer, Jochen Giesinger, Martin Vogt
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Publication number: 20120004213Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: September 15, 2011Publication date: January 5, 2012Applicant: FOREST LABORATORIES HOLDINGS LIMITEDInventors: Kumar SUNDARESAN, Sandeep N. RAIKAR, Srinivasa Raju SAMMETA, Ganesh PRABHU, Hosahalli SUBRAMANYA, Alexander BISCHOFF
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Patent number: 8044103Abstract: The present invention provides 4-substituted-2-azetidinone compounds, bicyclic 2-5-diketopiperazine compounds, and pharmaceutical compositions thereof that are potent, safe and effective neuroprotective agents. Due to their strong central nervous system (CNS) activity, the compounds can be used to enhance memory and to treat a variety of neurological disorders. The compounds are particularly useful for treating neurological disorders caused by, or associated with, CNS trauma.Type: GrantFiled: February 22, 2007Date of Patent: October 25, 2011Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Alan I. Faden, Gian Luca Araldi
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Patent number: 8039463Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: GrantFiled: March 20, 2009Date of Patent: October 18, 2011Assignee: Forest Laboratories Holdings LimitedInventors: Kumar Sundaresan, Sandeep N. Raikar, Srinivasa Raju Sammeta, Ganesh Prabhu, Hosahalli Subramanya, Alexander Bischoff
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Patent number: 8008492Abstract: Compounds of formula (I), where R1 and R3 are H or (C1-C4)-alkyl; R2 is H or a C-radical derived from one of the known ring systems with 1-4 rings; X1 is a (C1-C6)-alkyl biradical derived from a linear or branched carbon chain; and X2 is —NH—, —NH—(CH2)1-3—COO—, —NH—(CH2)1-3—S—, or —NH—CO—(CH2)1-3—S—, are useful as blood-brain barrier shuttles (BBB). BBB shuttle-cargo constructs, the cargo being a substance susceptible to form an amide or an ester or a disulfide bound with X2 and being unable to cross the blood-brain barrier by itself, are useful as medicaments.Type: GrantFiled: August 28, 2007Date of Patent: August 30, 2011Inventors: Ernest Giralt Lledó, Meritxell Teixidó Turà
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Publication number: 20110172208Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.Type: ApplicationFiled: June 26, 2009Publication date: July 14, 2011Applicant: Kissei Pharmaceutical Co., Ltd.Inventors: Takehiro Ishikawa, Satoko Kobayashi, Hitoshi Inoue, Yasunori Ueno, Masako Yoshida, Nobuyuki Tanaka
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Publication number: 20110172240Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.Type: ApplicationFiled: January 7, 2011Publication date: July 14, 2011Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Patent number: 7951943Abstract: The present invention relates to the preparation of 3-hydroxyamidino-phenylalanine derivatives in highly pure form which can be used for example as urokinase inhibitors. The present invention further relates to the use of high-purity 3-hydroxyamidinophenylalanine derivatives for preparing 3-amidinophenylalanine derivatives.Type: GrantFiled: October 14, 2005Date of Patent: May 31, 2011Assignee: Wilex AGInventor: Helmut Greiving
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Publication number: 20110002992Abstract: The present invention relates to N-sulfonylated amino acid derivatives, where an aryl radical is linked via the sulfonyl group N-terminally to the amino acid and a radical which comprises at least one imino group and at least one further basic group which represents an optionally modified amino, amidino or guanidino group is linked C-terminally via the carbonyl group. The invention likewise relates to processes for preparing these compounds and to their use, in particular as inhibitors of matriptase.Type: ApplicationFiled: July 1, 2010Publication date: January 6, 2011Applicant: The Medicines Company (Leipzig) GmbHInventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz, Anne Stürzebecher, Kerstin Uhland
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Patent number: 7842696Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: GrantFiled: June 23, 2008Date of Patent: November 30, 2010Assignee: Forest Laboratories Holdings LimitedInventors: Alexander Bischoff, Hosahalli Subramanya, Kumar Sundaresan, Srinivasa Raju Sammeta, Anil Kumar Vaka
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Patent number: 7834017Abstract: There is provided compounds having the formula of structure I: wherein the groups —C(R8)(CH2)vCH(R9)(CH2)y-Q and —C(R8)(CH2)vCH(R9)(CH2)y-J are the same, and R1a, R1b, R2a, R2b, R8, R9, J, Q, W, X, L2, v and y have meanings given in the description. The use of such compounds in the treatment of a condition responsive to changes in melanocortin receptor function in a human or non-human mammal (e.g. male sexual dysfunction, female sexual dysfunction, an eating disorder, above optimal body weight, obesity, below-optimal body weight or cachexia) is also described.Type: GrantFiled: August 10, 2007Date of Patent: November 16, 2010Assignee: Palatin Technologies, Inc.Inventors: Kevin Burris, Yi-Qun Shi, Shubh D. Sharma, Yadi Reddy Bonuga, Papireddy Purma
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Publication number: 20100280034Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100221189Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds.Type: ApplicationFiled: October 10, 2008Publication date: September 2, 2010Inventors: Ian Martin Newington, Duncan George Wynn, Veronique Morisson-Iveson, Joanna Marie Passmore
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Publication number: 20100184730Abstract: The invention relates to fatty acid acylated salicylate derivatives; compositions comprising an effective amount of a fatty acid acylated salicylate derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a fatty acid acylated salicylate derivative.Type: ApplicationFiled: February 26, 2010Publication date: July 22, 2010Inventors: Chi B. Vu, Jean E. Bemis, Michael R. Jirousek, Jill C. Milne, Jesse J. Smith
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Patent number: 7754724Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.Type: GrantFiled: June 30, 2006Date of Patent: July 13, 2010Assignee: Dow AgroSciences LLCInventors: Beth Anne Lorsbach, James Melvin Ruiz, Thomas Clarence Sparks, Michael Thomas Sullenberger, Irene Mae Morrison, Jeffery Dale Webster
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Publication number: 20100160323Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: December 22, 2009Publication date: June 24, 2010Inventors: Alexander Bischoff, Hosahalli Subramanya, Kumar Sundaresan, Srinivasa Raju Sammeta, Anil Kumar Vaka
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Plasminogen Activator Inhibitor-1 Inhibitors and Methods of Use Thereof to Modulate Lipid Metabolism
Publication number: 20100137194Abstract: The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels.Type: ApplicationFiled: November 23, 2009Publication date: June 3, 2010Applicants: EASTERN MICHIGAN UNIVERSITYInventors: Daniel A. Lawrence, Cory Emal, Jacqueline Cale, Enming J. Su, Mark Warnock, Shih-Hon Li, Jeanne A. Cupp -
Patent number: 7714131Abstract: The present invention provides a compounds the formula (IV): and methods for producing an ?-(phenoxy)phenylacetic acid compound of the formula: wherein R1 is a member selected from the group consisting of: each R2 is a member independently selected from the group consisting of (C1-C4)alkyl, halo, (C1-C4)haloalkyl, amino, (C1-C4)aminoalkyl, amido, (C1-C4)amidoalkyl, (C1-C4)sulfonylalkyl, (C1-C4)sulfamylalkyl, (C1-C4)alkoxy, (C1-C4)heteroalkyl, carboxy and nitro; the subscript n is 1 when R1 has the formula (a) or (b) and 2 when R1 has the formula (c) or (d); the subscript m is an integer of from 0 to 3; * indicates a carbon which is enriched in one stereoisomeric configuration; and the wavy line indicates the point of attachment of R1; and compounds.Type: GrantFiled: September 20, 2006Date of Patent: May 11, 2010Assignee: Metabolex, Inc.Inventors: Yan Zhu, Peng Cheng, Xin Chen, Jingyuan Ma, Zuchun Zhao
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Publication number: 20100068272Abstract: The present invention relates to novel compounds for inhibiting the urokinase plasminogen activator (uPA), which have high bioavailability and oral administerability, and also to the use thereof as therapeutic active compounds for the treatment of urokinase- or/and urokinase receptor-associated disorders such as, for example, tumors and metastasizing. The invention relates in particular to compounds containing hydroxyamidine or hydroxyguanidine groups.Type: ApplicationFiled: September 14, 2009Publication date: March 18, 2010Applicant: WILEX AGInventors: Stefan SPERL, Markus Buergle, Wolfgang Schmalix, Katja Wosikowski, Bernd Clement
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Publication number: 20090325980Abstract: The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.Type: ApplicationFiled: October 22, 2007Publication date: December 31, 2009Inventors: Lieven Meerpoel, Joannes Theodorus Maria Linders, Libuse Jaroskova, Marcel Viellevoye, Leo Jacobus Jozef Backx, Didier Jean-Claude Berthelot, Guuske Frederike Busscher
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Publication number: 20090239848Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: March 20, 2009Publication date: September 24, 2009Applicant: FOREST LABORATORIES HOLDINGS LIMITEDInventors: Kumar Sundaresan, Sandeep N. Raikar, Srinivasa Raju Sammeta, Ganesh Prabhu, Hosahalli S. Subramanya, Alexander Bischoff
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Publication number: 20090221583Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: June 23, 2008Publication date: September 3, 2009Applicants: FOREST LABORATORIES HOLDINGS LIMITED, AURIGENE DISCOVERY TECHNOLOGIES LIMITEDInventors: Alexander BISCHOFF, Hosahalli SUBRAMANYA, Kumar SUNDARESAN, Srinivasa Raju SAMMETA, Anil Kumar VAKA
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Publication number: 20090214453Abstract: Disclosed is the use of an aqueous dispersion comprising (a) a micronized sparingly soluble organic compound which has a UV-Vis spectrum with a maximum from 380 to 420 nm; and (b) an anionic dispersing agent for protecting the human skin from browning and skin aging.Type: ApplicationFiled: December 11, 2006Publication date: August 27, 2009Inventors: Stefan Müller, Jurg Haase, Thomas Ehlis, Gilbert Kreyer, Jochen Giesinger, Martin Vogt
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Publication number: 20090209520Abstract: A compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein: R2, R3, R4 and R5 are independently selected from the group consisting of H, C1-7 alkoxy, amino, halo or hydroxy; Y is —CRRC2—(CH2)m—, where m is 0 or 1, RC1 is selected from H, CH3 and CF3, and RC2 is selected from H and CH3, or RC1 and RC2? together with the carbon atom to which they are attached form the 1,1-cyclopropylene group formula (A): RN1 and RN2 are independently selected from H and R, where R is optionally substituted C1-10 alkyl, C3-20heterocyclyl and C5-20 aryl; or RN1 and RN2, together with the nitrogen atom to which they are attached form an optionally substituted 5-7 membered, nitrogen containing, heterocylic ring; Het is formula (ii): where Y1 and Y3 are independently selected from CH and N, Y2 is selected from CX and N and X is H, Cl or F.Type: ApplicationFiled: June 15, 2007Publication date: August 20, 2009Applicant: KUDOS PHARMACEUTICALS LIMITEDInventors: Muhammad Hashim Javaid, Sylvie Gomez, Xiao-Ling Fan Cockcroft, Keith Allan Menear, Niall Morrison Barr Martin
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Publication number: 20090137570Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: ApplicationFiled: January 28, 2009Publication date: May 28, 2009Applicant: IRM LLCInventors: Hong LIU, Arnab K. CHATTERJEE, David C. TULLY, Phillip B. ALPER, Badry BURSULAYA, Jianhua GUO, David H. WOODMANSEE, Daniel MUTNICK, Donald S. KARANEWSKY, Yun HE
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Publication number: 20090118169Abstract: A compound comprising the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: wherein N1 represents an atom to which a donative hydrogen atom in a hydrogen-bond donating group is bonded or a hydrogen-bond accepting atom in a hydrogen-bond accepting group; N3 represents a hydrogen-bond accepting atom in a hydrogen-bond accepting group; and N2, N4 and N5 independently represents an arbitrary carbon atom constituting a hydrophobic group and defined by the interatomic distances between N1, N2, N3, N4 and N5; and, in the optimized three-dimensional structure thereof, the distances between the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, in the optimized steric structure thereof, are the interatomic distances in a pharmacophore; or a salt thereof; inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases iType: ApplicationFiled: November 16, 2007Publication date: May 7, 2009Applicant: TOYAMA CHEMICAL CO., LTD.Inventors: Hisaaki Chaki, Tadakazu Takakura, Keiichi Tsuchida, Hironori Kotsubo, Yukihiko Aikawa, Shuichi Hirono, Shunichi Shiozawa
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Publication number: 20080318945Abstract: This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted piperazines, according to Formula I A compound of formula I wherein Z is bond or NH; R1 is aryl or optionally substituted heteroaryl; R2 is H, optionally substituted C1-6alkyl, or optionally substituted C2-6alkenyl; R3 and R7 are independently H, optionally substituted C1-6alkyl, or aryl; R4 is H or optionally substituted C1-6alkyl; R5 is H or C1-6alkyl; R6 is H or C1-6alkyl; and X and X? are independently O or H2; or wherein R3 and R4 together form a part of morpholinyl, piperadinyl, or aziridinyl ring; and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: December 15, 2006Publication date: December 25, 2008Inventors: Linda N. Casillas, Robert W. Marquis, JR.
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Publication number: 20080261981Abstract: Novel amino acid derivatives are provided that are useful for management of disorders such as obesity and immunological diseases. The derivatives are also useful in lowering blood glucose levels in hyperglycemic disorders and for treating related disorders such as body weight gain, elevated free fatty acid, cholesterol and triglyceride levels and other disorder exacerbated by obesity.Type: ApplicationFiled: June 3, 2008Publication date: October 23, 2008Inventors: DEBENDRANATH DEY, Abjiheet Nag, Bindu Pandey, Preeti Balse, Partha Neogi, Bishwajit Nag
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Publication number: 20080255151Abstract: Disclosed is a series of N-deacetylthiocolchicine derivatives of formula I in which: the linker is a bivalent straight or branched C1-C8 alkyl residue, C3-C8 cycloalkyl, a phenylene or heterocyclic C4-C6 ring; the G1 and G2 junctions, which can be the same or different, are —CO—, —CONH—, —CR2— groups in which R2 is hydrogen or a straight C1-C4 alkyl residue, or the G1-linker-G2 group is the —CO— group. The compounds of formula I have antiproliferative, antiinflammatory, antiarthritic and antiviral activity.Type: ApplicationFiled: June 19, 2008Publication date: October 16, 2008Applicant: INDENA S.P.A.Inventors: Ezio Bombardelli, Gabriele Fontana
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Publication number: 20080234274Abstract: The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition this invention also discloses processes for the preparation of such inhibitors.Type: ApplicationFiled: June 3, 2008Publication date: September 25, 2008Applicant: ASTRAZENECA ABInventors: Andrew Bailey, Garry Pairaudeau, Anil Patel, Stephen Thom
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Patent number: 7384943Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives having the formula (I) wherein X is N; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycoalkyl or (CH2)n-aryl, wherein aryl is a heteromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0-4; as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.Type: GrantFiled: June 5, 2006Date of Patent: June 10, 2008Assignee: AstraZeneca ABInventors: Stefan Berg, Martin Nylöf, Svante Ross, Seth-Olov Thorberg
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Patent number: 7208497Abstract: A novel class of substituted piperazines and diazepanes, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.Type: GrantFiled: June 27, 2002Date of Patent: April 24, 2007Assignee: Novo Nordisk A/SInventors: Florencio Zaragoza Dorwald, Knud Erik Andersen, Jan Lindy Sørensen
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Patent number: 7176207Abstract: Compounds of the following formula (I): where A, a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: GrantFiled: February 2, 2006Date of Patent: February 13, 2007Assignee: Schering AktiengesellschaftInventors: Judi A Bryant, Brad O Buckman, Imadul Islam, Raju Mohan, Michael M Morrissey, Robert Guo-Ping Wei, Wei Xu, Shendong Yuan