Additional Hetero Ring Containing Patents (Class 546/187)
  • Chemical Compound
    Publication number: 20080139613
    Abstract: The present invention relates to 4-{(1R,3R)-1-(3,5-difluorophenyl)-3-[4-(3-ethyl-5-isopropyl-4H-1,2,4-triazol-4-yl)piperidin-1-yl]butyl}-1-(methylsulfonyl)piperidine (I): or a pharmaceutically acceptable salt thereof, as well as to processes for preparing such a compound, to pharmaceutical compositions comprising such a compound and to the use of such a compound in the treatment of CCR5 mediated disease states.
    Type: Application
    Filed: December 10, 2007
    Publication date: June 12, 2008
    Applicant: AstraZeneca AB
    Inventors: Dearg Sutherland Brown, Alan Wellington Faull, Steven Swallow
  • Chemical Compound
    Publication number: 20080139612
    Abstract: The present invention relates to 4-[3-(1,1-difluoroethyl)-5-methyl-4H-1,2,4-triazol-4-yl]-1-{(1R,3R)-3-(3,5-difluorophenyl)-1-methyl-3-[1-(methylsulfonyl)piperidin-4-yl]propyl}piperidine (I): or a pharmaceutically acceptable salt thereof, as well as processes for the preparation of this compound and its use in the treatment of CCR5 disease states.
    Type: Application
    Filed: December 10, 2007
    Publication date: June 12, 2008
    Applicant: ASTRAZENECA AB
    Inventors: Alan Wellington Faull, Steven Swallow
  • Piperidine derivatives useful as CCR5 antagonists
    Patent number: 7384948
    Abstract: The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R9, R10, A and B are as defined in the specification. The present invention also provides pharmaceutical compositions containing the compound of this invention, and methods of treatment using the compound of this invention. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.
    Type: Grant
    Filed: July 29, 2003
    Date of Patent: June 10, 2008
    Assignee: Schering Corporation
    Inventors: Anandan Palani, Michael W. Miller, Jack D. Scott
  • 1,2,4-Thiadiazole compounds and pests controlling composition containing the same
    Patent number: 7371746
    Abstract: The present invention relates to a 1,2,4-thiadiazole compound of the formula (I) represented by the formula (1): wherein R1? represents C3-C7 alkynyl and X represents C4-C7 straight alkylene optionally substituted with one to four of R2?, C4-C7 straight alkenylene optionally substituted with one to four of R2?, ethylene-oxy-ethylene optionally substituted with one to four of R4?, or ethylene-thio-ethylene optionally substituted with one to four of R4?, R2? represents a halogen atom, trifluoromethyl or C1-C4 alkyl, and R4 represents a fluorine atom or C1-C3 alkyl.
    Type: Grant
    Filed: September 27, 2004
    Date of Patent: May 13, 2008
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Hideki Ihara, Daisuke Takaoka, Hajime Mizuno
  • Methylene Dipiperidine Derivatives
    Publication number: 20080108624
    Abstract: The present invention relates to novel methylene dipiperidine 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: Application
    Filed: September 16, 2005
    Publication date: May 8, 2008
    Applicant: GLAXO GROUP LIMITED
    Inventors: Gordon Bruton, Vicky Johnstone, Barry Sidney Orlek
  • Indole derivatives as H3 inverse agonists
    Patent number: 7361682
    Abstract: The present invention relates to compounds of formula I: wherein X, R1, R2, R3, R4 and R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
    Type: Grant
    Filed: June 20, 2005
    Date of Patent: April 22, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Silvia Gatti McArthur, Cornelia Hertel, Matthias Heinrich Nettekoven, Susanne Raab, Olivier Roche, Rosa Maria Rodriguez-Sarmiento, Franz Schuler, Jean-Marc Plancher
  • Transition-metal-catalyzed process for the conversion of alkenes to sterically hindered substituted n-alkoxyamines
    Patent number: 7361755
    Abstract: This invention pertains to a novel process for preparing sterically hindered N-substituted alkyloxyamines from alkenes by the transition-metal-catalyzed reaction of a intermediate alkylborane with a sterically hindered nitroxyl radical.
    Type: Grant
    Filed: December 12, 2002
    Date of Patent: April 22, 2008
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Stephen Daniel Pastor, Sai Ping Shum
  • Cyclic amine compounds as CCR5 antagonists
    Patent number: 7348324
    Abstract: A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.
    Type: Grant
    Filed: October 18, 2002
    Date of Patent: March 25, 2008
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shinichi Imamura, Shohei Hashiguchi, Taeko Hattori, Osamu Nishimura, Naoyuki Kanzaki, Masanori Baba, Yoshihiro Sugihara
  • Arylpiperazines and their use as metalloproteinase inhibiting agents (MMP)
    Patent number: 7342020
    Abstract: Arylpiperazines of formula (I) useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13
    Type: Grant
    Filed: February 26, 2004
    Date of Patent: March 11, 2008
    Assignee: AstraZeneca AB
    Inventors: Bernard Christophe Barlaam, Nicholas John Newcombe, Howard Tucker, David Waterson
  • Heterocyclic piperidines as modulators of chemokine receptor activity
    Patent number: 7312222
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: March 25, 2004
    Date of Patent: December 25, 2007
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
  • Piperidine derivatives useful as modulators of chemokine receptor activity
    Patent number: 7307090
    Abstract: The invention provides a compound of formula (I), wherein: T is C(O) or S(O)2; W is C(O) or S(O)2; X is CH2, O or NH; Y is CR5 or N; R1 is optionally substituted aryl or optionally substituted heterocyclyl; R2 is hydrogen or C1-6alkyl; R3 is hydrogen or optionally substituted C1-6alkyl; and R4 is alkyl, optionally substituted aryl, optionally substituted aralkyl or optionally substituted heterocyclyl; that are modulators of chemokine (especially CCR3) activity and are especially useful for treating asthma and/or rhinitis
    Type: Grant
    Filed: July 1, 2002
    Date of Patent: December 11, 2007
    Assignee: AstraZeneca AB
    Inventors: Richard Evans, Matthew Perry, Brian Springthorpe
  • Non-imidazole compounds
    Patent number: 7300941
    Abstract: Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H1 receptor antagonist.
    Type: Grant
    Filed: October 31, 2003
    Date of Patent: November 27, 2007
    Assignee: Schering Corporation
    Inventors: Robert G. Aslanian, Neng-Yang Shih, Pauline C. Ting, Michael Y. Berlin, Stuart B. Rosenblum, Kevin D. McCormick, Wing C. Tom, Christopher W. Boyce, Pietro Mangiaracina, Mwangi W. Mutahi, John J. Piwinski
  • Nitrogen-containing heterocyclic compounds and their use as Raf inhibitors
    Patent number: 7297693
    Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: November 20, 2007
    Assignee: SmithKline Beecham P.L.C.
    Inventors: Mark James Bamford, David Kenneth Dean, Antoinette Naylor, Andrew Kenneth Takle, David Matthew Wilson
  • Certain glycine derivatives as factor Xa inhibitors for use in the treatment of thrombotic disorders
    Patent number: 7297706
    Abstract: Compounds of formula (I) in which R, R1, R2, n and X1 have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.
    Type: Grant
    Filed: July 11, 2006
    Date of Patent: November 20, 2007
    Assignee: Eli Lilly and Company
    Inventors: Michael Robert Wiley, Daniel Jon Sall, Christopher William Murray, Stephen Clinton Young, Jolie Anne Bastian
  • Indole derivatives as selective androgen receptor modulators (SARMS)
    Patent number: 7282507
    Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
    Type: Grant
    Filed: April 1, 2005
    Date of Patent: October 16, 2007
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
  • Phenylpiperidines and phenylpyrrolidines
    Patent number: 7279491
    Abstract: Substituted phenylpiperidines and phenylpyrrolidines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
    Type: Grant
    Filed: October 23, 2003
    Date of Patent: October 9, 2007
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Richard L. Apodaca, Curt A. Dvorak, Chandravadan R. Shah, Wei Xiao
  • Ophthalmic compositions for treating ocular hypertension
    Patent number: 7279490
    Abstract: This invention relates to selective m1 muscarinic agonist, their use or a formulation thereof in the treatment of glaucoma and/or other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans. In addition, the present invention relates to the use of the compounds in the treatment of dementia such as Alzheimer's disease and vascular dementia, depression, attention deficit disorder, sleep disorder, schizophrenia, pain, ischemia, atrophic gastritis, and atony of gastrointestinal tract.
    Type: Grant
    Filed: June 17, 2003
    Date of Patent: October 9, 2007
    Assignee: Merck & Co, Inc.
    Inventors: Miller J Ogidigben, Takeru Yamakawa, Yufu Sagara
  • Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
    Patent number: 7279471
    Abstract: The present invention relates to the CGRP antagonists of general formula wherein A and R1 to R3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Grant
    Filed: April 15, 2005
    Date of Patent: October 9, 2007
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Stephan Georg Mueller, Klaus Rudolf, Philipp Lustenberger, Dirk Stenkamp, Kirsten Arndt, Henri Doods, Gerhard Schaenzle
  • Process for preparing 4-(hydroxy)-[1,4?]bipiperidinyl-l'carboxylic acid tert-butyl ester
    Patent number: 7276609
    Abstract: The present invention concerns a process for preparing 4-(hydroxy)-[1,4?]bipiperidinyl-1?-carboxylic acid tert-butyl ester, comprising hydrogenating a mixture of 4-hydroxypiperidine and 1-tert-butoxycarbonyl-4-piperidone in a suitable solvent, in the presence of a suitable catalyst and at a suitable pressure.
    Type: Grant
    Filed: October 2, 2002
    Date of Patent: October 2, 2007
    Assignee: AstraZeneca AB
    Inventors: Philip O'Keefe, Mark Purdie
  • Cycloalkyl—containing 5-acylindolinones, the preparation thereof and their use as medicaments
    Patent number: 7262206
    Abstract: The present invention relates to cycloalkyl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined as in claims 1 to 6, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).
    Type: Grant
    Filed: March 10, 2005
    Date of Patent: August 28, 2007
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Armin Heckel, Gerald Jürgen Roth, Jörg Kley, Stefan Hoerer, Ingo Uphues
  • Crystalline form of a benzimidazole-carboxamide medicinal compound
    Patent number: 7256294
    Abstract: The invention provides crystalline forms of the novel benzimidazole-carboxamide 5-HT4 receptor agonist compound, 4-(4-{[(2-isopropyl-1H-benzoimidazole-4-carbonyl)amino]methyl}-piperidin-1-ylmethyl)piperidine-1-carboxylic acid methyl ester. The invention also provides pharmaceutical compositions comprising the crystalline compound, methods of using the compound to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing crystalline forms of the compound.
    Type: Grant
    Filed: May 24, 2006
    Date of Patent: August 14, 2007
    Assignee: Theravance, Inc.
    Inventors: Sean M. Dalziel, Kirsten M. Phizackerley
  • Benzimidazole compounds
    Patent number: 7244847
    Abstract: The present invention is directed to novel benzimidazoles according to representative structures I and II, and their derivatives that possess antibacterial activity. This invention is also directed to compositions including the benzimidazole derivatives, and methods for using the same.
    Type: Grant
    Filed: February 6, 2002
    Date of Patent: July 17, 2007
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Eric E. Swayze, Yun He, Punit P. Seth, Elizabeth Anne Jefferson
  • Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
    Patent number: 7241745
    Abstract: The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: July 10, 2007
    Assignee: Astellas Pharma GmbH
    Inventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt
  • Non-psychotropic cannabinoids
    Patent number: 7235584
    Abstract: Novel non-psychotropic cannabinoids are disclosed and pharmaceutical compositions comprising these novel compounds are described for preventing neurotoxicity, neuroinflammation, immune or inflammatory disorders comprising as active ingredient the stereospecific (+) enantiomer, having (3S,4S) configuration of ?6 tetrahydrocannabinol type compounds. The compositions are particularly effective in alleviating and even preventing neurotoxicity due to acute injuries to the central nervous system, including mechanical trauma, compromised or reduced blood supply as may occur in cardiac arrest or stroke, or poisonings. They are also effective in the treatment of certain inflammatory disorders and chronic degenerative diseases characterized by neuronal loss and chronic pain including neuropathic pain.
    Type: Grant
    Filed: June 25, 2003
    Date of Patent: June 26, 2007
    Assignee: Pharmos Corporation
    Inventors: Aaron Garzon, George Fink
  • Antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds
    Patent number: 7223759
    Abstract: The invention relates to antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds and pharmaceutical compositions thereof. This invention also relates to a method of using such compounds in the treatment of bacterial infections in mammals, especially humans.
    Type: Grant
    Filed: September 15, 2004
    Date of Patent: May 29, 2007
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Yuefen Zhou, Dionisios Vourloumis, Vlad E. Gregor, Geoffrey C. Winters, Thomas Hermann, Benjamin Ayida, Zhongxiang Sun, Douglas Murphy, Klaus B. Simonsen
  • Heterocyclic compounds useful to treat HCV
    Patent number: 7220745
    Abstract: The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.
    Type: Grant
    Filed: May 15, 2003
    Date of Patent: May 22, 2007
    Assignee: Rigel Pharmaceuticals
    Inventors: Rajinder Singh, Dane Goff, John Partridge
  • Selected CGRP-antagonists process for preparing them and their use as pharmaceutical compositions
    Patent number: 7205294
    Abstract: The present invention relates to substituted piperidines of general formula wherein A, B, D, E, X, R1 and R2 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Grant
    Filed: March 3, 2005
    Date of Patent: April 17, 2007
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Philipp Lustenberger, Klaus Rudolf, Stephan Georg Mueller, Dirk Stenkamp, Henri Doods, Kirsten Arndt, Gerhard Schaenzle
  • Piperidine derivatives and their use as modulators of chemokine receptor activity (especially CCR5)
    Patent number: 7192973
    Abstract: Compounds of formula (I): wherein L is CH or N; M is CH or N; provided that L and M are not both CH; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal)
    Type: Grant
    Filed: November 12, 2002
    Date of Patent: March 20, 2007
    Assignee: AstraZeneca AB
    Inventor: Howard Tucker
  • Heterocyclic substituted carbonyl derivatives and their use as dopamine Dreceptor ligands
    Patent number: 7186724
    Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.
    Type: Grant
    Filed: April 6, 2004
    Date of Patent: March 6, 2007
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: James A Hendrix, Horst Hemmerle, Matthias Urmann, Gregory M Shutske, Jospeh T Strupczewski, Kenneth J Bordeau, John G Jurcak, Thaddeus Nieduzak, Sharon A Jackson, Paul Angell, James P Carey, George Lee, David Fink, Jean-Fancois Sabuco, Yulin Chiang, Nicola Collar
  • Piperidine-2,6-diones heterocyclically substituted in the 3-position
    Patent number: 7183274
    Abstract: Piperidine-2,6-diones heterocyclically substituted in the 3-position corresponding to formula I Also the production and use of such compounds in pharmaceutical formulations and related methods of treatment.
    Type: Grant
    Filed: June 21, 2004
    Date of Patent: February 27, 2007
    Assignee: Gruenenthal GmbH
    Inventors: Helmut Heinrich Buschmann, Stefanie Frosch, Tieno Germann, Oswald Karl Zimmer, Fritz Theil
  • Water-soluble etoposide analogs and methods of use thereof
    Patent number: 7176236
    Abstract: Etoposide analogs with improved water-solubility such as 4?-O-Demethyl-4?-(N?,N?-dimethyl-glycyl)-4?-(4?-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4?-O-Demethyl-4?-(N?,N?-dimethyl-glycyl)-4?-(4?-fluoroanilino)-4-desoxy-podophyllotoxin (9) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.
    Type: Grant
    Filed: November 13, 2003
    Date of Patent: February 13, 2007
    Assignee: University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Zhiyan Xiao, Kenneth F. Bastow
  • Cyclic amide derivatives
    Patent number: 7166617
    Abstract: Novel compounds represented by the following formula (I) that act as a ligand to sigma receptor/binding cite and a medicament comprising the same as an active ingredient: wherein X represents an alkyl group, an aryl group, a heterocyclic group or the like; Q represents a group represented by —CH2—, —CO—, —O—, —CH(OR7)— or the like wherein R7 represents a hydrogen atom, an alkyl group or the like; n represents an integer of from 0 to 5; R1 and R2 each represent a hydrogen atom, an alkyl group or the like; B represents either of the following groups: wherein R3, R4, R5, and R6 each represent a hydrogen atom, a halogen atom, an alkoxyl group or the like; m represents 1 or 2; and the ring of: represents an aromatic heterocyclic ring.
    Type: Grant
    Filed: February 26, 2001
    Date of Patent: January 23, 2007
    Assignee: Mitsubishi Pharma Corporation
    Inventors: Haruko Yamabe, Masahiro Okuyama, Akira Nakao, Mitsuru Ooizumi, Ken-ichi Saito
  • N-aryl-2-oxazolidinone-5-carboxamides and their derivatives
    Patent number: 7141588
    Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.
    Type: Grant
    Filed: August 22, 2003
    Date of Patent: November 28, 2006
    Assignee: Pfizer, Inc.
    Inventors: Richard Charles Thomas, Toni-Jo Poel, Michael Robert Barbachyn, Mikhail Fedor Gordeev, Gary W. Luehr, Adam Renslo, Upinder Singh, Vara Prasad Venkata Nagendra Josyula
  • Cytotoxic agents
    Patent number: 7129261
    Abstract: The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.
    Type: Grant
    Filed: May 31, 2002
    Date of Patent: October 31, 2006
    Assignee: Medarex, Inc.
    Inventors: Howard P. Ng, Danny P.C. McGee, Oliver L. Saunders, Valeri Martichonok, Guoxian Wu, Zhihong Li, Geoffrey T. Yarranton
  • Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors
    Patent number: 7119203
    Abstract: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: October 10, 2006
    Assignee: Pharmacia Corporation
    Inventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, David L. Brown, Jeffery N. Carroll, Yiyuan Chen, Yvette M. Fobian, John N. Freskos, Alan F. Gasiecki, Margaret L. Grapperhaus, Robert M. Heintz, Susan L. Hockerman, Darren J. Kassab, Ish K. Khanna, Stephen A. Kolodziej, Mark A. Massa, Joseph J. McDonald, Brent V. Mischke, Deborah A. Mischke, Patrick B. Mullins, Mark A. Nagy, Monica B. Norton, Joseph G. Rico, Michelle A. Schmidt, Nathan W. Stehle, John J. Talley, William F. Vernier, Clara I. Villamil, Lijuan J. Wang, Thomas A. Wynn
  • Thio-substituted tricyclic and bicyclic aromatic methanesulfinyl derivatives
    Patent number: 7119214
    Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, Y, R1 and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.
    Type: Grant
    Filed: April 12, 2005
    Date of Patent: October 10, 2006
    Assignee: Cephalon France
    Inventors: Brigitte Lesur, Christophe Yue, Sophie Chasset, Olivier Renault
  • Heterocyclic compounds
    Patent number: 7115644
    Abstract: Disclosed are benzimidazolone compounds of formulas (I) & (II): wherein R1, R2, R3, R4, R5, X, L, m, n and t are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease.
    Type: Grant
    Filed: September 3, 2003
    Date of Patent: October 3, 2006
    Assignee: Boehringer Ingelheim Pharmaceuticals Inc.
    Inventors: Antonio Jose del Moral Barbosa, Jr., Daniel R. Goldberg, Abdelhakim Hammach, Pingrong Liu, Neil Moss, Mark Stephen Ralph, Gregory Paul Roth, Christopher Ronald Sarko, Fariba Soleymanzadeh, Andre White
  • Alanyl-piperidine heterocyclic derivatives useful against cardiovascular diseases
    Patent number: 7115609
    Abstract: Compounds of formula (I) in which R1, R2, n and X1 have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.
    Type: Grant
    Filed: December 9, 2002
    Date of Patent: October 3, 2006
    Assignee: Eli Lilly and Company
    Inventors: Stuart Donald Jones, Daniel Jon Sall, Michael Robert Wiley
  • Benzylpiperidine compound
    Patent number: 7115635
    Abstract: The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following benzylpiperidine derivative (the formula (1)) has a chemokine inhibitory activity. Further intensive studies have resulted in successful enhancement of the chemokine inhibitory activity and stability in blood of the present compound, as well as the completion of the present invention. wherein each symbol is as defined in the specification.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: October 3, 2006
    Assignee: Mitsubishi Pharma Corporation
    Inventors: Masatoshi Kiuchi, Takanobu Kuroita, Hideo Tomozane, Shuuzou Takeda, Yoshihito Tanaka, Hidemitsu Higashi, Shigeki Kuwahara
  • Acyclic and cyclic amine derivatives
    Patent number: 7105546
    Abstract: The present invention relates to acyclic and cyclic amine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
    Type: Grant
    Filed: January 30, 2002
    Date of Patent: September 12, 2006
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Mullican, David Lauffer, Roger Tung
  • Pharmaceutical compositions and methods for use
    Patent number: 7101896
    Abstract: The present invention relates to aryl olefinic azacyclic compounds and aryl acetylenic azacyclic compounds, including pyridyl olefinic cycloalkylamines and pyridyl acetylenic cycloalkylamines. The present invention also relates to prodrug derivatives of the compounds of the present invention.
    Type: Grant
    Filed: January 20, 2005
    Date of Patent: September 5, 2006
    Assignee: Targacept, Inc.
    Inventors: Gary Maurice Dull, Jeffrey Daniel Schmitt, Balwinder Singh Bhatti, Craig Harrison Miller
  • Maleimide group-containing polymer particles and method of producing the same
    Patent number: 7094860
    Abstract: The present invention relates to a maleimide group-containing polymer particle containing a crosslinked polymer particle containing a group represented by the following formula (1) and to a method of producing the maleimide group-containing crosslinked polymer particle by reacting hydroxymethylmaleimide with a hydroxyl group-containing polymer particle obtained by introducing a polyethylene glycol into a crosslinked polymer particle: wherein n denotes an integer of 1 or more.
    Type: Grant
    Filed: February 19, 2004
    Date of Patent: August 22, 2006
    Assignee: Fuji Xerox Co., Ltd.
    Inventors: Yoshihiro Inaba, Chisato Urano, Takako Kobayashi
  • Certain glycine derivatives as factor Xa inhibitors for use in the treatment of thrombotic disorders
    Patent number: 7078415
    Abstract: Compounds of formula (I) in which R, R1, R2, n and X1 have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.
    Type: Grant
    Filed: December 9, 2002
    Date of Patent: July 18, 2006
    Assignee: Eli Lilly and Company
    Inventors: Michael Robert Wiley, Daniel Jon Sall, Christopher William Murray, Stephen Clinton Young, Jolie Anne Bastian
  • Sulfamato hydroxamic acid metalloprotease inhibitor
    Patent number: 7067670
    Abstract: A sulfamato hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: July 8, 2004
    Date of Patent: June 27, 2006
    Assignee: Warner Lambert Company
    Inventors: Terri L. Boehm, Deborah A. Mischke, Gary A. DeCrescenzo, Joseph G. Rico, Shashidhar N. Rao, Darren J. Kassab, Jeffery N. Carroll
  • Substituted piperidines
    Patent number: 7064135
    Abstract: A novel class of substituted piperidines, 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: Grant
    Filed: October 9, 2002
    Date of Patent: June 20, 2006
    Assignee: Novo Nordisk Inc.
    Inventor: Florencio Zaragoza Dörwald
  • Compounds
    Patent number: 7064136
    Abstract: A compound having the general formula and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: June 20, 2006
    Assignee: AstraZeneca AB
    Inventor: Ashokkumar Bhikkappa Shenvi
  • 4-heteroaryl-3-heteroarylidenyl-2-indolinones and their use as protein kinase inhibitors
    Patent number: 7053086
    Abstract: The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases (“PKs”), in particular CDK2. The compounds of the present invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical composition containing these compounds and methods of preparing these compounds are also described.
    Type: Grant
    Filed: August 27, 2003
    Date of Patent: May 30, 2006
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Chung Chen Wei, Ping Huang, Jingrong Cui
  • Crystalline forms of osanetant
    Patent number: 7041679
    Abstract: The invention relates to crystalline forms of (R)-(+)-N-[[3-[1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]prop-1-yl]-4-phenylpiperidin-4-yl]-N-methylacetamide and to processes for preparing them.
    Type: Grant
    Filed: August 28, 2003
    Date of Patent: May 9, 2006
    Assignee: sanofi-aventis
    Inventors: Alain Alcade, Gilles Anne-Archard, Patrick Gros-Claude, Olivier Monnier, Jérome Roche
  • Compounds as opioid receptor modulators
    Patent number: 7041681
    Abstract: This invention is directed towards novel compounds as opioid receptor modulators, antagonists, and agonists useful for the treatment of opioid modulated disorders such as pain and gastrointestinal disorders.
    Type: Grant
    Filed: March 26, 2003
    Date of Patent: May 9, 2006
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Henry J. Breslin, Wei He, Robert W. Kavash
  • Substituted benzimidazoles and their use as PARP inhibitors
    Patent number: RE39608
    Abstract: Compounds of the formula Ia or IB where A is a saturated or monounsaturated heterocyclic, 4 - to 8-membered ring which contains one or two nitrogen atoms, and their tautomeric forms, possible enantiomeric and diastereomeric forms, their prodrugs and possible physiologically tolerated salts are useful as inhibitors of the enzyme poly(ADP-ribose)polymerase.
    Type: Grant
    Filed: November 23, 1999
    Date of Patent: May 1, 2007
    Assignee: Abbott GmbH & Co. KG
    Inventors: Wilfried Lubisch, Michael Kock, Thomas Höger, Sabine Schult, Roland Grandel, Reinhold Müller