Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The Additional Six-membered Hetero Ring (e.g., Nicotinic Acid, Etc.) Patents (Class 544/365)
  • Patent number: 8008305
    Abstract: The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.
    Type: Grant
    Filed: July 28, 2008
    Date of Patent: August 30, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Publication number: 20110207734
    Abstract: The present invention relates to Azine Derivatives, pharmaceutical compositions comprising the Azine Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Application
    Filed: April 14, 2011
    Publication date: August 25, 2011
    Inventors: Anandan Palani, Dong Xiao, Robert G. Aslanian, Michael Y. Berlin, Ashwin U. Rao, Xiao Chen, Yoon Joo Lee, Sylvia Degrado, Ning Shao, Ying R. Huang, Zhidan Liu
  • Publication number: 20110201581
    Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: February 11, 2011
    Publication date: August 18, 2011
    Inventors: Mark Furber, Christopher Andrew Luckhurst, Hitesh Jayantilal Sanganee, Linda Anne Stein, Peter Alan Cage
  • Publication number: 20110201811
    Abstract: A dihydropyridine (DHP) calcium antagonist compound and its preparation method and medical use are related to preparation methods of compounds of general formulas (I) and (II) as shown below and their pharmaceutical salts and applications for treating cardiovascular diseases, and R1 represents a substituted or unsubstituted heterocyclic, aromatic ring or aralkyl group, and the substituent may be C1-C4 alkyl, C1-C4 alkoxyl, halogen, cyano, trifluoromethyl, trifluoromethoxyl, methylthio, nitro, amino or hydroxyl group; R2 represents a C1-C8 alkyl group; R3 and R4 are the same or different, and each represents a hydrogen, halogen, cyano, trifluoromethyl, trifluoromethoxyl, methylthio, nitro or amino group or a C1-C4 alkyl, C1-C4 alkoxyl, C1-C4 alkenyl, or C1-C4 alkinyl group; R5 and R6 are the same or different, and each represents a C1-C4 alkyl group; X represents O, S or a single bond; m=0-6, n=1-6, and m and n are the same or different.
    Type: Application
    Filed: January 5, 2009
    Publication date: August 18, 2011
    Inventors: Guo-hua Chen, Li Wang
  • Patent number: 7994175
    Abstract: Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging.
    Type: Grant
    Filed: December 29, 2008
    Date of Patent: August 9, 2011
    Assignee: Avon Products, Inc
    Inventors: Dmitri S. Ptchelintsev, Hong Hu, Gopinathan K. Menon, Kristine Schmalenberg, John W Lyga
  • Patent number: 7993663
    Abstract: Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: August 9, 2011
    Assignee: Avon Products, Inc.
    Inventors: Dmitri S. Ptchelintsev, Hong Hu, Gopinathan K. Menon, Kristine Schmalenberg, John W. Lyga
  • Publication number: 20110136735
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: November 30, 2010
    Publication date: June 9, 2011
    Inventors: David BARNES, Gregory Raymond BEBERNITZ, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Herbert Franz SCHUSTER, Wei ZHANG
  • Publication number: 20110130379
    Abstract: The present invention relates to novel piperazine derivatives (I); to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.
    Type: Application
    Filed: July 15, 2009
    Publication date: June 2, 2011
    Applicant: CONVERGENCE PHARMACEUTICALS LIMITED
    Inventors: Paul John Beswick, Alister Campbell, Andrew Peter Cridland, Robert James Gleave, Jag Paul Heer, Neville Hubert Nicholson, Lee William Page, Sadie Vile
  • Publication number: 20110129419
    Abstract: The present invention relates to the field of medical imaging, and in particular to imaging of disease states associated with the upregulation of the chemokine receptor 5 (CCR5). Imaging agents, precursors and methods are provided which are useful in imaging such disease states.
    Type: Application
    Filed: December 19, 2007
    Publication date: June 2, 2011
    Applicants: GE HEALTHCARE LIMITED, HAMMERSMITH IMANET LIMITED
    Inventors: Anthony Eamon Storey, Julie Davis, Erik Arstad, Benedicte Guilbert, Alessandra Gaeta
  • Patent number: 7939532
    Abstract: Objects of the present invention are the compounds of formula I, their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: May 10, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Frederick Brookfield, Jonathan Gridley, Lothar Kling, Michael Prime, Ulrike Reiff, Wolfgang Von Der Saal, Thomas Von Hirschheydt
  • Patent number: 7919494
    Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.
    Type: Grant
    Filed: August 19, 2009
    Date of Patent: April 5, 2011
    Assignee: Astellas Pharma, Inc.
    Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
  • Patent number: 7919495
    Abstract: To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: April 5, 2011
    Assignee: Astellas Pharma, Inc.
    Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
  • Publication number: 20110077395
    Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein G, L, Q, Z, R6, R7, and R8 are defined herein.
    Type: Application
    Filed: December 2, 2010
    Publication date: March 31, 2011
    Inventors: James J. Li, Lawrence G. Hamann, Zheming Ruan, Christopher B. Cooper, Shung C. Wu, Ligaya M. Simpkins, Haixia Wang, Akbar Nayeem, Stanley R. Krystek
  • Publication number: 20110034463
    Abstract: The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as Yersinia Pestis. In some aspects, the invention relates to methods for discovering inhibitors of the Type III secretion system and uses of such inhibitors in the treatment and prevention of disease.
    Type: Application
    Filed: April 1, 2009
    Publication date: February 10, 2011
    Inventors: Jon Goguen, Ning Pan, Kyungae Lee
  • Patent number: 7884105
    Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: October 23, 2006
    Date of Patent: February 8, 2011
    Assignee: Janssen Pharmaceutica, N.V.
    Inventor: Kristof Van Emelen
  • Publication number: 20110014226
    Abstract: A method to identify small molecules useful as therapeutics and/or vaccines to prevent, alleviate or ameliorate a pathogenic infection or an autoimmune disorder. The method can be used to screen small molecule test compounds for the ability to disrupt particular antigen-antibody interactions of interest. In one embodiment, the antigen is a pathogen-derived antigen and the antibody decreases or inhibits virulence of the pathogen when bound to the antigen (e.g., a neutralizing antibody, antibody with serum bactericidal activity, etc.). In another embodiment, the antigen is a self-antigen (autoantigen) and the antibody is an autoantibody that is known to be associated with a pathological condition (e.g., autoimmune disorder). Compounds that bind to the antigen or antibody disrupt binding can be used as therapeutics to decrease or inhibit the autoimmune disorder.
    Type: Application
    Filed: March 17, 2009
    Publication date: January 20, 2011
    Inventors: Michael J. Caulfield, Michael D. Miller, Joseph G. Joyce, Paul D. Zuck, Krista L. Getty, Vadim Dudkin, Elizabeth A. Ottinger
  • Publication number: 20110009407
    Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.
    Type: Application
    Filed: April 27, 2010
    Publication date: January 13, 2011
    Inventors: Ying-Zi Xu, Shendong Yuan, David Wone, Andrei Konradi
  • Publication number: 20110003991
    Abstract: The use of a compound of formula I wherein Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; the ring is a 6-membered aromatic or is a 5 or 6 membered heteroaromatic ring; Ra, R1, R2, R4 and R8 are specified organic groups; n and p are independently 0-4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.
    Type: Application
    Filed: September 15, 2010
    Publication date: January 6, 2011
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Jérôme CASSAYRE, Peter MAIENFISCH, Fredrik CEDERBAUM, Louis-Pierre MOLLEYRES, Camilla CORSI, Thomas PITTERNA
  • Publication number: 20100305088
    Abstract: This invention is directed to a 3-(amido or sulphamido)-4-(4-substituted-azinyl)benzamide or benzsulphonamide compound as defined herein. The 3-(amido or sulphamido)-(4-substituted-azinyl)benzamide or benzsulphonamide compound is useful as a inhibitor of the chemokine receptor CxCR3, and for preventing or treating a CxCR3 chemokine receptor mediated disease or condition related thereto in a patient in need of such.
    Type: Application
    Filed: August 6, 2010
    Publication date: December 2, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: David S. Thorpe, Martin Smrcina, Dagmar D. Cabel
  • Publication number: 20100305138
    Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): wherein W, V, x, y, R1, R2, R3, R4, R5, R6, R7, R7a, R8, R8a, R9, R9a, R10 and R10a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
    Type: Application
    Filed: June 15, 2010
    Publication date: December 2, 2010
    Inventors: Melwyn Abreo, Daniel F. Harvey, Mikhail A. Kondratenko, Wenbao Li, Rajender Kamboj, Vishnumurthy Kodumuru, Michael D. Winther, Heinz W. Gschwend, Nagasree Chakka, Shifeng Liu, Serguei Sviridov, Shaoyi Sun
  • Publication number: 20100280005
    Abstract: Disclosed are compounds of Formula I, wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
    Type: Application
    Filed: April 4, 2008
    Publication date: November 4, 2010
    Inventors: Jonh J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, John Gleason, Alexey V. Ishchenko, Brian Lawhorn, Gerard McGeehan, Jaclyn R. Patterson, Simon F. Semus, Robert D. Simpson, Suresh B. Singh, Colin Tice, Tritin Tran, Zhenrong Xu, Jing Yuan, Wei Zhao
  • Publication number: 20100273795
    Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Application
    Filed: April 21, 2010
    Publication date: October 28, 2010
    Applicant: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Jared Andrew Forrester
  • Publication number: 20100267701
    Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Application
    Filed: July 1, 2010
    Publication date: October 21, 2010
    Inventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
  • Publication number: 20100256126
    Abstract: The present application relates to compounds of formula wherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: March 11, 2010
    Publication date: October 7, 2010
    Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Publication number: 20100256359
    Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to hetero isonipecotic amides that are potent modulators of VR1 which are useful for the treatment and prevention of disease conditions in mammals.
    Type: Application
    Filed: October 6, 2009
    Publication date: October 7, 2010
    Inventors: Micheal D. Gaul, Bao-Ping Zhao, Daniel A. Hutta
  • Publication number: 20100240640
    Abstract: The present invention relates to new D3 and D2 dopamine receptor subtype preferring ligands of formula (I): wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, aryl, cycloalkyl, aroyl, or R1 and R2 may form a heterocyclic ring with the adjacent nitrogen atom; X represents an oxygen or sulphur atom; n is an integer of from 1 to 2, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of a condition which requires modulation of dopamine receptors.
    Type: Application
    Filed: May 12, 2010
    Publication date: September 23, 2010
    Applicant: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Eva Againe Csongor, Janos Galambos, Katalin Nogradi, Istvan Vago, Istvan Gyertyan, Bela Kiss, Istvan Laszlovszky, Judit Laszy, Katalin Saghy
  • Publication number: 20100234377
    Abstract: The present invention relates to compounds of general formula (I): wherein A, Y, X, n and B are as defined herein; and their use in the treatment and prevention of metabolic disorders, inflammatory conditions, allergic conditions, fever, pain including allodynia and nociception, eating disorders, cachexia, brain injuries, cancer of the genitals, sleep apnea, cardiovascular disease, flush effect associated with nicotinic acid and related compounds or for the promotion of wound healing. Certain compounds of general formula (I) are new and the invention also relates to these compounds and to their use in medicine.
    Type: Application
    Filed: April 7, 2008
    Publication date: September 16, 2010
    Applicant: Evotec AG
    Inventors: Babette Aicher, Arndt-Rene Kelter, Thomas Stephen Coulter, Steven Taylor, Adams James Davenport, Thomas Hesterkamp, Christian Kirchhoff
  • Publication number: 20100179118
    Abstract: The present invention relates to a compound represented by the following formula (I), which is useful as an antiallergic agent and/or an anti-inflammatory agent, or a physiologically acceptable salt thereof and the like: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group and the like, R3 is a hydrogen atom, a C1-6 alkyl group and the like, R4 and R5 are the same or different and each is a hydrogen atom, a halogen atom, a hydroxy group, a C1-6 alkyl group and the like, X is a single bond or —C(R6)(R7)—, R6 and R7 are the same or different and each is a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group and the like, or R6 and R7 optionally form, together with the carbon atom bonded thereto, an optionally substituted C3-8 cycloalkyl group and the like, ring group A is an azetidin-1-yl group and the like, m is 0, 1 or 2, and n is 0, 1 or 2.
    Type: Application
    Filed: September 7, 2007
    Publication date: July 15, 2010
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Michinori Ozawa, Tomoya Shiro, Takaaki Sumiyoshi, Mari Itoh
  • Publication number: 20100173888
    Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are defined herein, to compositions containing such compounds and to the uses of such compounds for the treatment of allergic and respiratory conditions.
    Type: Application
    Filed: June 17, 2009
    Publication date: July 8, 2010
    Inventors: Atli Thorarensen, John I. Trujillo, Wei Huang, Steve R. Turner, Simon Mantell, Ross Strang, Siew Kuen Yeap
  • Publication number: 20100173886
    Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful for the treatment of metabolic disorders including obesity.
    Type: Application
    Filed: May 22, 2008
    Publication date: July 8, 2010
    Inventors: Jason Bloxham, Stuart Edward Bradley, Tom Banksia Dupree, Peter Timothy Fry, Patrick Eric Hanrahan, Thomas Martin Krulle, Martin James Procter, Colin Peter Sambrook-Smith, Karen Lesley Schofield, Donald Smyth, Alan John Stewart
  • Publication number: 20100168103
    Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of diaryl piperidine compounds are disclosed of the general formula (I) where X is a linker and Y may be C, O, S or N.
    Type: Application
    Filed: September 14, 2007
    Publication date: July 1, 2010
    Applicant: NEUROMED PHARMACEUTICALS LTD.
    Inventors: Hassan Pajouhesh, Yanbing Ding, Hossein Pajouhesh, Richard Holland, Gabriel Hum
  • Publication number: 20100125075
    Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C6 alkenyloxy, amino, C1-C6 alkylamino, or di-(C1-C6 alkylamino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.
    Type: Application
    Filed: December 14, 2006
    Publication date: May 20, 2010
    Applicant: British Biotech Pharmaceuticals Ltd.
    Inventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
  • Patent number: 7705149
    Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.
    Type: Grant
    Filed: August 26, 2008
    Date of Patent: April 27, 2010
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: James P. Edwards, Michael D. Hack, David E. Kindrachuk, Jennifer D. Venable
  • Patent number: 7700599
    Abstract: The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the GPR38 receptor.
    Type: Grant
    Filed: June 26, 2007
    Date of Patent: April 20, 2010
    Assignee: Glaxo Group Limited
    Inventors: Mervyn Thompson, Susan Marie Westaway
  • Patent number: 7696209
    Abstract: The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3, R4 and X are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, mixtures and salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I in which one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Grant
    Filed: January 30, 2009
    Date of Patent: April 13, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Stephan Georg Mueller, Klaus Rudolf, Philipp Lustenberger, Dirk Stenkamp, Marco Santagostino, Fabio Paleari, Henri Doods, Kirsten Arndt, Gerhard Schaenzle
  • Publication number: 20100063045
    Abstract: Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof.
    Type: Application
    Filed: March 28, 2008
    Publication date: March 11, 2010
    Applicant: Santen Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Mogi, Hasashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
  • Patent number: 7662816
    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: Grant
    Filed: August 4, 2004
    Date of Patent: February 16, 2010
    Assignee: Schering Corporation
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, 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: 20100035895
    Abstract: The present invention relates to 2-aminocarbonyl-pyridine derivatives of Formula (I) and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis.
    Type: Application
    Filed: October 12, 2007
    Publication date: February 11, 2010
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Eva Caroff, Kurt Hilpert, Emmanuel Meyers
  • Publication number: 20100022555
    Abstract: The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.
    Type: Application
    Filed: July 15, 2009
    Publication date: January 28, 2010
    Inventors: Paul John Beswick, Alister Campbell, Andrew Cridland, Robert James Gleave, Jag Paul Heer, Neville Hubert Nicholson, Lee William Page, Sadie Vile
  • Patent number: 7648990
    Abstract: The present invention provides a method for the treatment of emesis in a mammal being treated with an opiod analgesic.
    Type: Grant
    Filed: October 1, 2007
    Date of Patent: January 19, 2010
    Assignee: GlaxoSmithKline LLC
    Inventors: Giuseppe Alvaro, Paola Maragni, Marsia Tampieri
  • Publication number: 20090312307
    Abstract: Novel heterocyclo compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: August 11, 2009
    Publication date: December 17, 2009
    Inventors: John Lloyd, Yoon T. Jeon, Heather Finlay, Lin Yan, Michael F. Gross, Serge Beaudoin
  • Publication number: 20090298833
    Abstract: The present application describes substituted piperidinyl modulators of MIP-1? or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using said modulators are disclosed.
    Type: Application
    Filed: July 20, 2009
    Publication date: December 3, 2009
    Inventors: Percy H. Carter, Cullen L. Cavallaro, John V. Duncia, Daniel S. Gardner, John Hynes, Rui-Qin Liu, Joseph B. Santella, Dharmpal S. Dodd
  • Publication number: 20090286801
    Abstract: The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent.
    Type: Application
    Filed: June 21, 2007
    Publication date: November 19, 2009
    Inventors: Marc Capet, Denis Danvy, Nicolas Levoin, Isabelle Berrebi-Bertrand, Thierry Calmels, Philippe Robert, Jeanne-Marie Lecomte, Jean-Charles Schwartz, Xavier Ligneau
  • Patent number: 7615556
    Abstract: The present application describes modulators of MIP-1? of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, T, W, R1, R4, R5, R5a and R5b are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using said modulators are disclosed.
    Type: Grant
    Filed: January 23, 2007
    Date of Patent: November 10, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Percy H. Carter, Cullen L. Cavallaro, George V. De Lucca
  • Patent number: 7598250
    Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24)(R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.
    Type: Grant
    Filed: August 4, 2004
    Date of Patent: October 6, 2009
    Assignee: Schering Corporation
    Inventors: Jared N. Cumming, Ying Huang, Guoqing Li, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Jianping Pan, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie
  • Patent number: 7592347
    Abstract: The present invention relates to novel piperidine carbonyl piperazine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
    Type: Grant
    Filed: April 21, 2004
    Date of Patent: September 22, 2009
    Assignee: Glaxo Group Limited
    Inventors: Gordon Bruton, Barry Sidney Orlek, Kishore Kalidas Rana
  • Publication number: 20090221583
    Abstract: 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: Application
    Filed: June 23, 2008
    Publication date: September 3, 2009
    Applicants: FOREST LABORATORIES HOLDINGS LIMITED, AURIGENE DISCOVERY TECHNOLOGIES LIMITED
    Inventors: Alexander BISCHOFF, Hosahalli SUBRAMANYA, Kumar SUNDARESAN, Srinivasa Raju SAMMETA, Anil Kumar VAKA
  • Publication number: 20090197894
    Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where m, n, p, V, R1, R2, R3, R4, R5 and R6 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
    Type: Application
    Filed: April 14, 2009
    Publication date: August 6, 2009
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Jian-Min Fu, Vishnumurthy Kodumuru, Shaoyi Sun, Michael D. Winther, Richard M. Fine, Daniel F. Harvey, Boris Klebansky, Mark P. Gray-Keller, Heinz W. Gschwend, Wenbao Li
  • Publication number: 20090192160
    Abstract: The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the GPR38 receptor.
    Type: Application
    Filed: April 2, 2009
    Publication date: July 30, 2009
    Inventors: Darren Jason MITCHELL, Jonathan Thomas Seal, Mervyn Thompson, Susan Marie Westway, Samantha Louisa Brown
  • Publication number: 20090186876
    Abstract: The present invention relates to certain new pyridin analogues of Formula (I) [Chemical formula should be inserted here. Please see paper copy] Formula (I) to processes for preparing such compounds, to their utility in medicine in general and especially as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.
    Type: Application
    Filed: June 26, 2007
    Publication date: July 23, 2009
    Applicant: ASTRAZENECA AB
    Inventors: Kay Brickmann, Fredrik Zetterberg