Chalcogen Hetero Ring Attached Directly Or Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 514/253.11)
  • Patent number: 7482347
    Abstract: Compounds of formula I in free or salt form, wherein Ar, R1, R2, R3, X and T have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3, particularly an inflammatory or allergic condition such as an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: August 9, 2005
    Date of Patent: January 27, 2009
    Inventor: Darren M Legrand
  • Patent number: 7482346
    Abstract: The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
    Type: Grant
    Filed: August 22, 2006
    Date of Patent: January 27, 2009
    Assignee: Sanofi-Aventis
    Inventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Tak Adrien Li
  • Publication number: 20090005375
    Abstract: The present invention relates to acetyl coenzyme-A carboxylase (“ACC”) inhibiting compounds of the formula wherein the variables are as defined herein. In particular, the present invention relates to ACC1 and/or ACC2 inhibitors, compositions of matter, kits and articles of manufacture comprising these compounds, methods for inhibiting ACC1 and/or ACC2, and methods of making the inhibitors.
    Type: Application
    Filed: March 21, 2008
    Publication date: January 1, 2009
    Inventors: Edcon Chang, Matthew H. McNeill
  • Publication number: 20080317671
    Abstract: Certain non-imidazole heterocyclic compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.
    Type: Application
    Filed: August 20, 2008
    Publication date: December 25, 2008
    Inventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
  • Publication number: 20080318945
    Abstract: 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: Application
    Filed: December 15, 2006
    Publication date: December 25, 2008
    Inventors: Linda N. Casillas, Robert W. Marquis, JR.
  • Patent number: 7462617
    Abstract: The invention relates to compounds of formula wherein the substituents are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention further relates to methods for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other d 1iseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
    Type: Grant
    Filed: September 1, 2004
    Date of Patent: December 9, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniela Alberati-Giani, Synese Jolidon, Robert Narquizian, Matthias Heinrich Nettekoven, Roger David Norcross, Emmanuel Pinard, Henri Stalder
  • Patent number: 7446106
    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 4, 2008
    Assignee: SmithKline Beecham plc
    Inventors: David Kenneth Dean, Andrew Kenneth Takle, David Matthew Wilson
  • Patent number: 7435736
    Abstract: The invention concerns substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine having neurokinin antagonistic activity, in particular NK1 and NK1/NK3-antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety, depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Grant
    Filed: December 17, 2003
    Date of Patent: October 14, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Frans Eduard Janssens, François Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
  • Patent number: 7432264
    Abstract: Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistant S. aureus strain.
    Type: Grant
    Filed: August 9, 2004
    Date of Patent: October 7, 2008
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Elizabeth Anne Jefferson, Eric E. Swayze, Punit P. Seth, Dale E. Robinson, Jr.
  • Patent number: 7425558
    Abstract: Methods and compositions are provided for treating sexual dysfunction, e.g., sexual dysfunction associated with drug treatment, using 5-HT1A receptor antagonists.
    Type: Grant
    Filed: August 18, 2006
    Date of Patent: September 16, 2008
    Assignee: Wyeth
    Inventors: Stacey J. Sukoff Rizzo, Sharon Joy Rosenzweig-Lipson, Wayne Everett Childers, Michael Kelly, Lee Erwin Schechter
  • Patent number: 7423039
    Abstract: The invention relates to substituted (4-phenylpiperazin-1-yl)acylpiperidine derivatives of formula (I) in the form of a base or an addition salt with an acid, and also in the form of a hydrate or solvate, and their preparation process and therapeutic application.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: September 9, 2008
    Assignee: Sanofi-aventis
    Inventors: Victor Dos Santos, Jean Wagnon
  • Patent number: 7419980
    Abstract: The present invention is directed to fused-aryl and heteroaryl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
    Type: Grant
    Filed: October 12, 2004
    Date of Patent: September 2, 2008
    Assignee: Wyeth
    Inventors: Eugene John Trybulski, Paige Erin Mahaney, Lori Krim Gavrin, Joseph Peter Sabatucci, Gary Paul Stack
  • Publication number: 20080176842
    Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.
    Type: Application
    Filed: November 14, 2007
    Publication date: July 24, 2008
    Applicant: G.D. SEARLE LLC
    Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
  • Publication number: 20080153845
    Abstract: The present invention is directed to the use of TRPV1 antagonists as inhibitors of certain taste perceptions and functions. The invention is also directed to, among other things, compositions comprising the TRPV1 antagonists that can be used in pharmaceutical, food, and other products to inhibit certain taste functions and perceptions.
    Type: Application
    Filed: October 29, 2007
    Publication date: June 26, 2008
    Applicant: REDPOINT BIO CORPORATION
    Inventors: R. Kyle PALMER, Daniel Long, Heather Devantier, S. Paul Lee, M.N. Tulu Buber, Robert Bryant
  • Publication number: 20080139557
    Abstract: At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
    Type: Application
    Filed: September 11, 2007
    Publication date: June 12, 2008
    Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Tony Lee, James W. Darrow, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt
  • Patent number: 7384944
    Abstract: The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v.
    Type: Grant
    Filed: September 23, 2003
    Date of Patent: June 10, 2008
    Assignee: Schering Corporation
    Inventors: Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Elizabeth M. Smith, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin, Eric Gilbert, Marc A. Labroli
  • Publication number: 20080096898
    Abstract: Compounds of formula I in free or salt form, wherein Ar, R1, R2, R3, X and T have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3, particularly an inflammatory or allergic condition such as an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Application
    Filed: August 9, 2005
    Publication date: April 24, 2008
    Applicant: NOVARTIS AG
    Inventor: Darren Mark Legrand
  • Patent number: 7345042
    Abstract: The present invention discloses methods of using antagonists for melanin-concentrating hormone (MCH), to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes, as well as novel compounds which are antagonists for melanin-concentrating hormone (MCH). In other aspects, the invention is directed to pharmaceutical compositions comprising such MCH antagonists as well as methods for preparing such compounds. Compounds of the invention generally have the structure: where the substituents are as defined herein.
    Type: Grant
    Filed: June 28, 2004
    Date of Patent: March 18, 2008
    Assignee: Schering Corporation
    Inventors: Anandan Palani, Sherry A. Shapiro, Hubert B. Josien, Thomas A. Bara, John W. Clader, Pradeep B. Pushpavanam, Shengjian Li, Mark D. McBriar
  • Patent number: 7307081
    Abstract: The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein the various moieties 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: December 17, 2003
    Date of Patent: December 11, 2007
    Assignee: Schering Corporation
    Inventors: Michael W. Miller, Jack D. Scott
  • Patent number: 7288545
    Abstract: This invention relates to a method for treating an angiogenesis-related disease. The method includes administering to a subject in need thereof an effective amount of a piperazinedione compound having the formula: In the above formula, each of and , independently, is a single bond or a double bond; A is H or CH(RaRb) when is a single bond, or C(RaRb) when is a double bond; Z is CH(RcRd) when is a single bond, or C(RcRd) when is a double bond; each of R1 and R2, independently, is H, C(O)Re, C(O)ORe, C(O)NReRf, or SO2Re; and each of Ra, Rb, Rc, Rd, Re, and Rf, independently, is H, C1-C6 alkyl, aryl, heteroaryl, C3-C8 cycloalkyl, or C3-C8 heterocycloalkyl; or Ra and Rb taken together are C3-C8 cycloalkyl, C3-C8 heterocycloalkyl, aryl, or heteroaryl; or R1 and Ra or R1 and Rb taken together are C3-C8 cycloalkyl, C3-C8 heterocycloalkyl, aryl, or heteroaryl; provided that one of Rc and Rd is aryl or heteroaryl.
    Type: Grant
    Filed: October 20, 2003
    Date of Patent: October 30, 2007
    Assignee: AngioRx Corporation
    Inventors: Che-Ming Teng, Hui-Po Wang, Eric I. C. Li, On Lee, Jih-Hwa Guh, Huei-Ting Chen, Ya-Bing Fan, Ya-Lan Chen
  • Patent number: 7247631
    Abstract: Methods for treating treatment-naive as well as treatment-experienced adult and pediatric patients having HIV-1 infections as well as patients co-infected with HIV-1 and HCV involving administering a therapeutically effective amount of pegylated interferon-alfa, e.g., pegylated interferon alfa-2b, in association with a therapeutically effective amount of a CCR5 antagonist or preferably further in association with a therapeutically effective amount of at least one of ribavirin, IL-2, IL-12, pentafuside alone or in combination with a therapeutically effective amount of an anti-HIV-1 drug therapy, e.g., HAART are disclosed.
    Type: Grant
    Filed: May 6, 2003
    Date of Patent: July 24, 2007
    Assignee: Schering Corporation
    Inventor: Mark A. Laughlin
  • Patent number: 7241764
    Abstract: Compounds of general formula:[Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared.
    Type: Grant
    Filed: November 5, 2003
    Date of Patent: July 10, 2007
    Assignee: AstraZeneca AB
    Inventors: William Brown, Andrew Griffin
  • Patent number: 7229997
    Abstract: Compounds of the general formula (I): wherein R1, R2, R3 and R4 are as described in the specification. Further included are pharmaceutical compositions comprising the compounds, processes for their preparation, as well as the use of the compounds for the preparation of a medicament which particularly acts on the central nervous system, particularly for use as anti-obesity agents.
    Type: Grant
    Filed: May 16, 2003
    Date of Patent: June 12, 2007
    Assignee: Biovitrum AB
    Inventors: Björn M. Nilsson, Erik Ringberg
  • Patent number: 7214679
    Abstract: Compounds of the formula: wherein the substituents are as defined herein are useful for treating conditions mediated by p38 kinase.
    Type: Grant
    Filed: January 13, 2004
    Date of Patent: May 8, 2007
    Assignee: Scios, Inc.
    Inventors: Babu J. Mavunkel, Sundeep Dugar, Gregory R. Luedtke, Xuefei Tan, Glen McEnroe
  • Patent number: 7196106
    Abstract: The present invention addresses substituted cyanothiophene derivatives of the formula I: as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists. The compounds block the action of glucagon at its receptor and thereby decrease the levels of plasma glucose providing a treatment of diabetes.
    Type: Grant
    Filed: November 4, 2003
    Date of Patent: March 27, 2007
    Assignee: Merck & Co., Inc
    Inventors: Joseph L. Duffy, Elizabeth Louise Campbell, Brian A. Kirk, Rui Liang, James R. Tata, Kevin T. Chapman, Zenon Konteatis
  • Patent number: 7196080
    Abstract: The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. (wherein R1, R2: hydrogen, a halogen, a lower alkyl, a lower alkoxy, or the like, R3, R4: hydrogen, a (substituted) lower alkyl, a halogen, or the like, R5: hydrogen, a lower alkyl, a lower alkoxycarbonyl, or the like, and n: 0 or 1).
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: March 27, 2007
    Assignee: Astellas Pharma Inc.
    Inventors: Masahiro Iwata, Noriyuki Kawano, Hiroyuki Kaizawa, Tomofumi Takuwa, Issei Tsukamoto, Ryushi Seo, Kiyoshi Yahiro, Miki Kobayashi, Makoto Takeuchi
  • 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
  • Patent number: 7101885
    Abstract: The present invention relates to compounds of formula I wherein Ar, Y and G are as defined in the specification, a is 1 to 4, Z and W are carbon or nitrogen and n is 1, 2 or 3; and to pharmaceutical compositions comprising the compound of formula I and a pharmaceutically effective carrier; and to a method useful in treating or preventing in mammals, including humans, a disorder or condition selected from the group consisting of anxiety, depression, dysthymia, major depressive disorder, migraine, post-traumatic stress disorder, avoidant personality disorder, borderline personality disorder and phobias.
    Type: Grant
    Filed: June 15, 2004
    Date of Patent: September 5, 2006
    Assignee: Pfizer Inc
    Inventors: John Lowe, III, Mark A. Sanner
  • Patent number: 7098213
    Abstract: Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4–R7 and R13 are H or alkyl; R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl-SO2—, cycloalkyl-SO2—, fluoroalkyl-SO2—, R9-aryl-SO2—, R9-heteroaryl-SO2—, N(R22)(R23)—SO2—, alkyl-C(O)—, cycloalkyl-C(O)—, fluoroalkyl-C(O)—, R9-aryl-C(O)—, NH-alkyl-C(O)— or R9-aryl-NH—C(O)—; R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—; or R2 and R3 together are ?O, ?NOR10, ?N—NR11R12 or ?CH-alkyl; R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, alpha-substituted benzyl or alpha-substituted heteroarylmethyl; R9–R12 are as defined; are disclosed for the treatment of HIV, solid organ transplant rejection, gra
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: August 29, 2006
    Assignee: Schering Corporation
    Inventor: Michael W. Miller
  • Patent number: 7091219
    Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.
    Type: Grant
    Filed: April 17, 2003
    Date of Patent: August 15, 2006
    Assignee: G. D. Searle & Co.
    Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
  • Patent number: 7071191
    Abstract: Substituted non-imidazole aryloxypiperidine compounds, compositions containing them, and methods of making and using them to treat or prevent histamine-mediated conditions.
    Type: Grant
    Filed: August 6, 2001
    Date of Patent: July 4, 2006
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Richard Apodaca, Nicholas I. Carruthers, Curt A. Dvorak, Chandravadan R. Shah, Wei Xiao
  • Patent number: 7067518
    Abstract: A compound having 5-HT1A receptor activity, represented by the chemical formula wherein: Ar is 2-methoxyphenyl, 1H-indol-4-yl or 2,3-dihydro-1,4-benzodioxin-5-yl; R1 is 2-, 3- or 4-pyridyl; R2 is H or C1-6alkyl; R3 is H or C1-6alkyl; and R4 is H or methyl, or an optical isomer thereof, or a pharmaceutically acceptable salt of such a compound or optical isomer. The invention also includes compositions containing such a compound, as well as methods for using a compound of the invention.
    Type: Grant
    Filed: August 29, 2003
    Date of Patent: June 27, 2006
    Assignee: Wyeth
    Inventors: Lynne P. Greenblatt, Michael G. Kelly, Yvette L. Palmer
  • Patent number: 7067517
    Abstract: Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: June 27, 2006
    Assignee: Nero Nordisk A/S
    Inventors: Soren Ebdrup, Johannes Cornelis de Jong, Poul Jacobsen, Holger Claus Hansen, Per Vedso
  • Patent number: 7057042
    Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction, wherein A, L, D and B1 are as described in the specification.
    Type: Grant
    Filed: May 23, 2003
    Date of Patent: June 6, 2006
    Assignee: Abbott Laboratories
    Inventors: Marlon D. Cowart, Steven P. Latshaw, Sherry L. Nelson, Andrew O. Stewart
  • Patent number: 7026320
    Abstract: Novel piperazine derivatives are provided having the formula wherein R1 is cyano, nitro, trifluoromethyl or halogen, or pharmaceutically acceptable acid addition salts thereof, which are useful as 5-HT1A receptor antagonists.
    Type: Grant
    Filed: May 20, 2003
    Date of Patent: April 11, 2006
    Assignee: Wyeth
    Inventors: Wayne E. Childers, Michael G. Kelly, Sharon J. Rosenzweig-Lipson
  • Patent number: 7026314
    Abstract: Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating, disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B antagonists. Also provided herein are processes for making compounds of Formula (I) and intermediate compounds.
    Type: Grant
    Filed: January 15, 2002
    Date of Patent: April 11, 2006
    Assignee: AstraZeneca AB
    Inventors: Marc Chapdelaine, Timothy Davenport, Markus Haeberlein, Carey Horchler, John McCauley, Edward Pierson, Daniel Sohn
  • Patent number: 7019008
    Abstract: A compound of Formula (I): wherein: R1 is C1-6 alkyl, benzyl, or (CH2)n—C(O)NH2; wherein the benzyl may be unsubstituted or substituted by one or two C1-6 alkyl, halogen, C1-6 alkoxy, or methylenedioxy groups; R2 is benzimidazolyl, quinolinyl, benzofuranyl, napthyl, indolyl, benzothiophenyl, phenyl, furanyl, thienyl, or pyridyl substituted or unsubstituted by one, two or three halogen, C1-3 alkyl, C1-3 alkoxy, or methylenedioxy groups; X1 and X2 are independently hydrogen, halogen, C1-3 alkyl, C1-3 alkoxy, nitro, CF3, or CN; n is 1, 2, or 3; m is 1, 2 or 3; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 29, 2005
    Date of Patent: March 28, 2006
    Assignee: SmithKline Beecham Corporation
    Inventors: Dashyant Dhanak, Steven D. Knight, Jian Jin, Ralph A. Rivero, Anthony Sapienza
  • Patent number: 7008946
    Abstract: Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4–R7 and R13 are H or alkyl; R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl-SO2—, cycloalkyl-SO2—, fluoroalkyl-SO2—, R9-aryl-SO2—, R9-heteroaryl-SO2—, N(R22)(R23)—SO2—, alkyl-C(O)—, cycloalkyl-C(O)—, fluoroalkyl-C(O)—, R9-aryl-C(O)—, NH-alkyl-C(O)— or R9-aryl-NH—C(O)—; R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—; or R2 and R3 together are ?O, ?NOR10, ?N—NR11R12 or ?CH-alkyl; R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, alpha-substituted benzyl or alpha-substituted heteroarylmethyl; R9–R12 are as defined; are disclosed for the treatment of HIV, solid organ transplant rejection, gra
    Type: Grant
    Filed: October 21, 2004
    Date of Patent: March 7, 2006
    Assignee: Schering Corporation
    Inventor: Michael W. Miller
  • Patent number: 6992189
    Abstract: In its several embodiments, this invention discloses novel processes to prepare the compounds of formula II and formula IV:
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: January 31, 2006
    Assignee: Schering Corporation
    Inventors: William Leong, Minzhang Chen, Bosco A. D'sa, Man Zhu, Tong Xiao, Xiongwei Shi, Suhan Tang, Dinesh Gala, Andrew J. Goodman, Christopher M. Nielsen, Gary M. Lee, Juan A. Gamboa, Andrew D. Jones
  • Patent number: 6958331
    Abstract: The invention relates to sulfonyl amine derivatives of formula IA wherein R5A, X1, X2, R9 and R10 are as defined herein, which derivatives are useful as bradykinin B1 receptor antagonists.
    Type: Grant
    Filed: June 2, 2000
    Date of Patent: October 25, 2005
    Assignee: Novartis AG
    Inventors: Christopher Thomas Brain, William Cantrell, Andrew James Culshaw, Edward Karol Dziadulewicz, Terance William Hart, Timothy John Ritchie, Liladhar Waykole
  • Patent number: 6916817
    Abstract: Arylpiperazines of Formula I useful as metalloproteinase inhibitors, especially as MMP13 inhibitors.
    Type: Grant
    Filed: May 31, 2000
    Date of Patent: July 12, 2005
    Assignee: AstraZeneca AB
    Inventor: Howard Tucker
  • Patent number: 6900315
    Abstract: The present invention relates to novel compounds, compositions and methods for inhibiting the growth, elaboration and/or replication of HIV in human patients and to the prevention and treatment of human acquired immunodeficiency syndrome (AIDS) and other diseases caused by retroviral infection. More particularly, in preferred aspects, the present invention provides a method for the use of novel prodrug forms of 9-(2,3-Dideoxy-?-D-glycero-pent-2-enofuranosyl) guanine (d4G) for the prevention and treatment of both wild type and drug-resistant Human Immunodeficiency Virus (HIV), the causative pathogen of AIDS. Compounds according to the present invention are based upon the chemical formula: where X is OCH3, N3, NHCH3, N(CH3)2 or an aminocyclopropyl group; R1 is H or a C1 to C20 acyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group; and R2 is H or a C1 to C20 acyl or alkyl group.
    Type: Grant
    Filed: February 5, 2002
    Date of Patent: May 31, 2005
    Assignees: Yale University, University of Georgia Research Foundation, Inc.
    Inventors: Karen S. Anderson, Adrian Staffin Ray, Chung K. Chu, Yang Zhenjun
  • Patent number: 6900211
    Abstract: Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4-R7 and R13 are H or alkyl; R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl-SO2—, cycloalkyl-SO2—, fluoroalkyl-SO2—, R9-aryl-SO2—, R9-heteroaryl-SO2—, N(R22)(R23)—SO2—, alkyl-C(O)—, cycloalkyl-C(O)—, fluoroalkyl-C(O)—, R9-aryl-C(O)—, NH-alkyl-C(O)— or R9-aryl-NH—C(O)—; R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—; or R2 and R3 together are ?O, ?NOR10, ?N—NR11R12 or ?CH-alkyl; R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, alpha-substituted benzyl or alpha-substituted heteroarylmethyl; R9-R12 are as defined; are disclosed for the treatment of HIV, solid organ transplant rejection, gra
    Type: Grant
    Filed: February 6, 2004
    Date of Patent: May 31, 2005
    Assignee: Schering Corporation
    Inventor: Michael W. Miller
  • Patent number: 6900222
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a
    Type: Grant
    Filed: May 23, 2000
    Date of Patent: May 31, 2005
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 6867230
    Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3 and R10 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, methods of treating bacterial and protozoal infections by administering the compounds of formula 1.
    Type: Grant
    Filed: June 1, 2001
    Date of Patent: March 15, 2005
    Assignee: Pfizer, Inc.
    Inventors: Matthew Merrill Hayward, Michael S. Visser, Robert G. Linde, II, Takushi Kaneko
  • Patent number: 6849621
    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 H. receptor antagonist.
    Type: Grant
    Filed: March 11, 2002
    Date of Patent: February 1, 2005
    Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.
    Inventors: Stuart B. Rosenblum, Qingbei Zeng, Mwangi Wa Mutahi, Robert G. Aslanian, Pauline C. Ting, Neng-Yang Shih, Daniel M. Solomon, Jianhua Cao, Henry A. Vaccaro, Kevin D. McCormick, John J. Baldwin, Ge Li
  • Publication number: 20040254195
    Abstract: One aspect of the present invention relates to piperidine-piperazine compounds. A second aspect of the present invention relates to the use of the piperidine-piperazine compounds as ligands for various mammalian cellular receptors or transporters or both, including dopamine, serotonin or norepinephrine receptors or transporters, any combination of them, or all of them. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome.
    Type: Application
    Filed: March 24, 2004
    Publication date: December 16, 2004
    Inventors: Paul E. Persons, Heike Radeke
  • Publication number: 20040242575
    Abstract: This invention relates to N-aroyl piperazine derivatives of formula (I), wherein: Y represents NR2; m represents 1, 2 or 3; p represents 0 or 1; X is O, S, C═O, SO2, or CH═CH—; Ar1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar2 represents phenyl or a 5- or 6-membered heterocyclyl group containing 1 to 3 heteroatoms selected from N, O and S, wherein the phenyl heterocyclyl group is substituted by R1 and further optional substituents; or Ar2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing 1 to 4 heteroatoms selected from N, O and S; R1 represents optionally substituted (C1-4)alkoxy, halo, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S; R?2 represents hydrogen, optionally substituted (C1-4)alkyl, opt
    Type: Application
    Filed: July 2, 2004
    Publication date: December 2, 2004
    Inventors: Clive Leslie Branch, Chirstopher Norbert Johnson, David John Nash, Geoffrey Stemp
  • Patent number: 6825200
    Abstract: The present invention a compound represented by the formula (I): where the structural variables R1-R6 are defined herein.
    Type: Grant
    Filed: May 6, 2002
    Date of Patent: November 30, 2004
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Ichiro Shima, Takehiko Ohkawa, Kazuhiko Ohne, Kentaro Sato, Naoki Ishibashi, Kenichiro Imamura
  • Publication number: 20040224959
    Abstract: Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein from the liver and particularly have excellent inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein, are free from side effect of accumulation of lipids in the liver, and are useful for the treatment and prevention of hyperlipidemia and arteriosclerotic diseases.
    Type: Application
    Filed: June 16, 2004
    Publication date: November 11, 2004
    Inventors: Naoto Ohkura, Yukiko Hiraiwa, Tetsuya Matsushima, Kazue Sasaki, Takehiro Yamamoto, Masaharu Shiotani, Shigeki Suzuki, Yuuko Nakatani, Chizuko Kuroda, Mieko Nagasawa, Kiyoaki Katano