Chalcogen Bonded Directly To Piperazine Ring Carbon Patents (Class 544/384)
  • Patent number: 9249109
    Abstract: The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor intermediates. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used in mass production by improving yield.
    Type: Grant
    Filed: October 3, 2014
    Date of Patent: February 2, 2016
    Assignee: DONG-A PHARMACEUTICAL CO., LTD.
    Inventors: Woo Young Kwak, Heung Jae Kim, Jong Pil Min, Tae Hyun Yoon, Moohi Yoo, Geun Gho Lim, Sun Ki Chang
  • Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Patent number: 8999990
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: April 7, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Barbara Pio, Nardos Teumelsan, Alexander Pasternak, Reynalda DeJesus
  • Patent number: 8999991
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: April 7, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Barbara Pio, Harry R. Chobanian
  • Publication number: 20150025241
    Abstract: The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used in mass production by improving yield.
    Type: Application
    Filed: October 3, 2014
    Publication date: January 22, 2015
    Inventors: Woo Young KWAK, Heung Jae KIM, Jong Pil MIN, Tae Hyun YOON, Moohi YOO, Geun Gho LIM, Sun Ki CHANG
  • Patent number: 8889863
    Abstract: The present invention provides methods and intermediates are provided for the preparation of (?)-Nutlin-3. Methods and intermediates are also provided for the enantioselective addition of aryl nitromethanes to aldimines. Bis(amidine) catalysts for the use in these and other reactions are also provided.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: November 18, 2014
    Assignee: Vanderbilt University
    Inventors: Jeffrey N. Johnston, Tyler A. Davis
  • Publication number: 20140296225
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Application
    Filed: October 22, 2012
    Publication date: October 2, 2014
    Inventors: Haifeng Tang, Barbara Pio, Nardos Teumelsan, Alexander Pasternak, Reynalda DeJesus
  • Publication number: 20140288077
    Abstract: In one aspect, the invention relates to substituted 4-phenoxyphenol analogs, derivatives thereof, and related compounds, which are useful as inhibitors of proliferating cell nuclear antigen (PCNA); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating hyperproliferative disorders associated with PCNA using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: July 5, 2012
    Publication date: September 25, 2014
    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL
    Inventors: Naoaki Fujii, Marcelo Actis, Chandanamali Punchihewa, Michele Connelly, Sean Wu
  • Patent number: 8703947
    Abstract: Described herein are compounds, and pharmaceutical compositions, methods, and uses thereof for treating Alzheimer's disease.
    Type: Grant
    Filed: October 9, 2009
    Date of Patent: April 22, 2014
    Assignee: Purdue Research Foundation
    Inventor: Arun K. Ghosh
  • Publication number: 20140038945
    Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds ate inhibitors of PDE4function and are useful for improving cognitive function in animals.
    Type: Application
    Filed: July 31, 2013
    Publication date: February 6, 2014
    Applicant: DART NEUROSCIENCE (CAYMAN) LTD
    Inventors: Terence P. Keenan, Alan P. Kaplan
  • Patent number: 8629149
    Abstract: Compounds of formula (I) which are useful in ameliorating conditions characterized by unwanted sodium and/or calcium channel actrvrh, particularly Nav 1, 7, Nav 1, 8, or Cav 3, 2 channel activity are disclosed. More specifically, compounds for use in the treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's disease, depression, schizophrenia, psychosis, and tinnitus are disclosed.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: January 14, 2014
    Assignee: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan Pajouhesh, Yanbing Ding
  • Patent number: 8598347
    Abstract: The present invention relates to an improved method for manufacturing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention allows reduction of production costs by reacting low cost reagents, improves yield and is adaptable for mass production.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: December 3, 2013
    Assignee: Dong-A Pharmaceutical. Co., Ltd
    Inventors: Woo Young Kwak, Heung Jae Kim, Jong Pil Min, Tae Hyun Yoon, Hyun Joo Shim, Moohi Yoo
  • Publication number: 20130244995
    Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
    Type: Application
    Filed: November 21, 2011
    Publication date: September 19, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Per Vedsø, Lars Kristian Albert Blæhr
  • Publication number: 20130137689
    Abstract: The invention relates to novel acylpiperazinone compounds, to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
    Type: Application
    Filed: January 15, 2013
    Publication date: May 30, 2013
    Applicant: FAB PHARMA S.A.S.
    Inventor: FAB PHARMA S.A.S.
  • Patent number: 8435992
    Abstract: Methods for treating cancer by using compound PM00104, in particular, for treating multiple myeloma are provided.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: May 7, 2013
    Assignee: Pharma Mar S.A.
    Inventors: Enrique Ocio, Atanasio Pandiella, Jesús San Miguel, Pablo Manuel Avilés Marín
  • Patent number: 8357679
    Abstract: The present invention relates to hexafluoroisopropanol derivatives having the general formula I to pharmaceutical compositions comprising the same and to the use of these hexafluoroisopropanol derivatives in the treatment of atherosclerosis.
    Type: Grant
    Filed: May 13, 2009
    Date of Patent: January 22, 2013
    Assignee: MSD Oss B.V.
    Inventors: Andrew John Cooke, Andrew Stanley Edwards, Fiona Elizabeth Andrews, David Jonathan Bennett, Olaf Nimz, Emma Louise Carswell
  • Publication number: 20130004518
    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: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: Merck, Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, 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: 20120232079
    Abstract: The invention relates to novel acylpiperazinone compounds, to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
    Type: Application
    Filed: October 20, 2010
    Publication date: September 13, 2012
    Inventors: Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Francois Moreau
  • Publication number: 20120220603
    Abstract: Compounds of formula (I) which are useful in ameliorating conditions characterized by unwanted sodium and/or calcium channel activity, particularly unwanted NaV 1.7, NaV 1.8, or CaV 3.2 channel activity are disclosed. Specifically, a series of compounds containing piperidine or piperazine linked through an amide, isoxazole or similar linker to an aryl ring are described and are shown to be useful for the treatment of pain or epilepsy. A is selected from Formulae (i) or (ii).
    Type: Application
    Filed: September 3, 2010
    Publication date: August 30, 2012
    Applicant: ZALICUS PHARMACEUTICALS LTD.
    Inventors: Hassan Pajouhesh, Mike Grimwood, Yongbao Zhu, Yanbing Ding, Richard Holland
  • Publication number: 20120220605
    Abstract: Compounds of formula (I) which are useful in ameliorating conditions characterized by unwanted sodium and/or calcium channel actrvrh, particularly Nav1.7, Nav 1.8, or Cav 3.2 channel activity are disclosed. More specifically, compounds for use in the treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's disease, depression, schizophrenia, psychosis, and tinnitus are disclosed.
    Type: Application
    Filed: September 3, 2010
    Publication date: August 30, 2012
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan Pajouhesh, Yanbing Ding
  • Publication number: 20120202794
    Abstract: Disclosed herein are compounds useful for treating a viral infection, such as HCV.
    Type: Application
    Filed: January 19, 2012
    Publication date: August 9, 2012
    Applicant: PHARMASSET, INC.
    Inventors: MICHAEL JOSEPH SOFIA, RAMESH KAKARLA, JIAN LIU, DEVAN NADUTHAMBI, RALPH MOSLEY, HOLLY MICOLOCHICK STEUER
  • Publication number: 20120116080
    Abstract: The present invention relates to a process for the stereoselective preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.
    Type: Application
    Filed: July 23, 2009
    Publication date: May 10, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Markus Ostermeier, Stefan Braith, Juergen Daeubler, Guenther Huchler, Waldemar Pfrengle
  • Patent number: 8158790
    Abstract: The present invention provides an excellent antihypertensive medicament. The medicament of the present invention comprises a compound having the general formula (I) and the like: [wherein R1: H, substitutable alkyl, substitutable alkenyl, substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; R2: H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R3, R4; H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R5, R6: H, substitutable alkyl, substitutable cycloalkyl, substitutable alkoxy or the like; R7, R8: H, substitutable alkyl, substitutable cycloalkyl or the like; X: the formula (II) or the like; A: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; Y: a single bond, substitutable alkylene, substitutable alkenylene, —(CH2)a—X1—(CH2)b—(X1: the formula —NH—, —O— or the like; a, b: 0-5) or the like; B: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like].
    Type: Grant
    Filed: June 22, 2007
    Date of Patent: April 17, 2012
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Shojiro Miyazaki, Yuji Nakamura, Takahiro Nagayama, Taro Tokui, Yasuyuki Ogawa
  • Publication number: 20120088915
    Abstract: The present invention provides methods and intermediates are provided for the preparation of (?)-Nutlin-3. Methods and intermediates are also provided for the enantioselective addition of aryl nitromethanes to aldimines. Bis(amidine) catalysts for the use in these and other reactions are also provided.
    Type: Application
    Filed: July 14, 2011
    Publication date: April 12, 2012
    Inventors: Jeffrey N. Johnston, Tyler A. Davis
  • Publication number: 20120016125
    Abstract: The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used in mass production by improving yield.
    Type: Application
    Filed: March 30, 2010
    Publication date: January 19, 2012
    Applicant: DONG-A PHARMACEUTICAL. CO., LTD
    Inventors: Woo Young Kwak, Heung Jae Kim, Jong Pil Min, Tae Hyun Yoon, Moohi Yoo, Geun Gho Lim, Sun Ki Chang
  • Publication number: 20120016126
    Abstract: The present invention relates to an improved method for manufacturing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention allows reduction of production costs by reacting low cost reagents, improves yield and is adaptable for mass production.
    Type: Application
    Filed: March 30, 2010
    Publication date: January 19, 2012
    Applicant: DONG-A PHARMACEUTICAL. CO., LTD
    Inventors: Woo Young Kwak, Heung Jae Kim, Jong Pil Min, Tae Hyun Yoon, Hyun Joo Shim, Moohi Yoo
  • Patent number: 8076328
    Abstract: Process for the protection of fish and invertebrates and all their stages of development against or for the treatment of mycoses caused by fungi of the genera Saprolegnia, Aphanomyces, Achlyaflagellata and other species important in aquacultures by use of 2-[[[[1-[3-(1-fluoro-2-phenylethyl)oxy]phenyl]ethylidene]amino]oxy]methyl]alpha-(methoxyimino)-N-methyl-alphaE-benzeneacetamide, amisulbrom, cyazofamid, enestrobin, famoxadone, fenamidone, fluoxastrobin, orysastrobin, picoxystrobin and pyribencarb. This use leads to an inhibition or destruction of pathogenic fungi. The composition, comprising at least one fungicide selected from the abovementioned group for use in fish farming and keeping is suitable for the prophylaxis and therapy of diseases of fish in aquaculture, in breeding ponds, breeding tanks, aquariums, natural stretches of game fish waters, ponds, and marine fish farms. Addition to the water and feed and direct application are the associated use forms.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: December 13, 2011
    Assignee: Bayer CropScience AG
    Inventors: Isolde Häuser-Hahn, Klaus Stenzel, Ulrike Wachendorff-Neumann
  • Publication number: 20110294775
    Abstract: Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumour pain and headache diseases.
    Type: Application
    Filed: August 12, 2008
    Publication date: December 1, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
  • Publication number: 20110275797
    Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.
    Type: Application
    Filed: January 29, 2010
    Publication date: November 10, 2011
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
  • Patent number: 8030315
    Abstract: The present invention provides a novel heterocyclic compound containing a beta-amino group, a method for preparing the same, and a pharmaceutical composition comprising the same heterocyclic compound or a pharmaceutically acceptable salt thereof as an active ingredient. The heterocyclic compound of the present invention exhibits excellent DPP-IV inhibitory activity and bioavailability and therefore can be useful for the prophylaxis or treatment of DPP-IV-related diseases such as diabetes or obesity.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: October 4, 2011
    Assignee: Dong-A Pharm. Co., Ltd.
    Inventors: Heung Jae Kim, Woo Young Kwak, Chang Yell Shin, Hadong Kim, Jong Pil Min, Kyung Jin Park, Jae Young Lee, Song-Hyen Choi, Tae Hyun Yoon, Hae-Sun Kim, Ji Myun Jang, Mi-Kyung Kim, Moon-Ho Son, Soon Hoe Kim, Moohi Yoo
  • Patent number: 7767666
    Abstract: Certain substituted butyl and butynyl benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.
    Type: Grant
    Filed: June 21, 2007
    Date of Patent: August 3, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: John M. Keith, Michael A. Letavic, Emily M. Stocking
  • Patent number: 7763620
    Abstract: The present invention relates to piperazinone compounds, pharmaceutical compositions containing those compounds and methods of treating tumors and cancer, among other disease states and conditions in mammalian patients, especially including humans.
    Type: Grant
    Filed: August 23, 2002
    Date of Patent: July 27, 2010
    Assignees: Yale University, University of South Florida
    Inventors: Andrew D. Hamilton, Said Sebti, Hairuo Peng
  • Publication number: 20100181527
    Abstract: This invention relates to a stable secondary battery utilizing as active principle the oxidation and reduction cycle of a sterically hindered nitroxide radical, a sterically hindered oxoammonium cation, a sterically hindered hydroxylamine or a sterically hindered aminoxide anion containing a piperazin-2,6-dione, a piperazin-2-one or morpholin-2-one structural unit. Further aspects of the invention are a method for providing such a secondary battery, the use of the respective compounds as active elements in secondary batteries and selected novel compounds.
    Type: Application
    Filed: June 9, 2008
    Publication date: July 22, 2010
    Inventors: Peter Nesvadba, Lucienne Bugnon Folger, Tobias Hintermann
  • Publication number: 20100048550
    Abstract: The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta(TR-Beta). Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.
    Type: Application
    Filed: October 15, 2007
    Publication date: February 25, 2010
    Inventors: Saurin Raval, Preeti Raval, Braj Lohray, Vidya Bhushan Lohray, Pankaj R. Patel
  • 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: 20090312328
    Abstract: [Object] A compound that can be used as an agent for treating a disease associated with an EP1 receptor, in particular, a lower urinary tract symptom. [Means for Solution] It was confirmed that a sulfonamide compound having an amide structure and characterized by a chemical structure in which a carbon atom in the amide bonds to the N atom in sulfonamide through lower alkylene, or a salt thereof, has a potent EP1 receptor antagonistic activity, accomplishing the present invention. Since the sulfonamide compound of the present invention or a pharmaceutically acceptable salt thereof has a potent EP1 receptor antagonistic activity, it is useful as an agent for treating a disease associated with an EP1 receptor, in particular, a lower urinary tract symptom.
    Type: Application
    Filed: August 9, 2007
    Publication date: December 17, 2009
    Applicant: Astellas Pharma Inc.
    Inventors: Hideki Kubota, Susumu Toda, Issei Tsukamoto, Yuta Fukuda, Ryutaro Wakayama, Kazuki Ono, Toru Watanabe, Hidenori Azami
  • 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
  • Publication number: 20090253713
    Abstract: Compounds of the general formula: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, and X are as defined. Further provided are methods for treatment of sexual dysfunction, including erectile dysfunction and female sexual dysfunction, and combination drugs and method of use thereof, including a compound of the invention and one or more second sexual dysfunction pharmaceutical agents.
    Type: Application
    Filed: June 19, 2009
    Publication date: October 8, 2009
    Applicant: Palatin Technologies, Inc.
    Inventor: Shubh D. Sharma
  • Patent number: 7572787
    Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.
    Type: Grant
    Filed: August 25, 2006
    Date of Patent: August 11, 2009
    Assignee: Biovitrum AB
    Inventors: Patrizia Caldirola, Ulf Bremberg, Gary Johansson, Andrew Mott, Annika Jenmalm Jensen, Katarina Beierlien, Markus Thor, Lars Tedenborg
  • Patent number: 7538114
    Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: June 26, 2007
    Date of Patent: May 26, 2009
    Assignee: Amgen Inc.
    Inventors: Stephen Hitchcock, Albert Amegadzie, Wenyuan Qian, Xiaoyang Xia, Scott S. Harried
  • Patent number: 7479493
    Abstract: Certain substituted benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.
    Type: Grant
    Filed: June 21, 2007
    Date of Patent: January 20, 2009
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Brett Allison, Michael P. Curtis, Cheryl A. Grice, John M. Keith, Michael A. Letavic, Jennifer M. B. Miller, Emily M. Stocking
  • Publication number: 20080255150
    Abstract: The invention relates to substituted aryl acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: November 1, 2006
    Publication date: October 16, 2008
    Applicant: ASTRAZENECA AB
    Inventor: Timothy Luker
  • Publication number: 20080242662
    Abstract: The invention relates to substituted 3,4- or higher substituted piperazine compounds, the use thereof for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds are especially of the formula I, wherein R1, R2, R11, C, E and D are as defined in the specification.
    Type: Application
    Filed: May 29, 2006
    Publication date: October 2, 2008
    Inventors: Atsuko Nihonyanagi, Atsushi Toyao, Yuki Iwaki, Keiichi Masuya
  • Publication number: 20080221123
    Abstract: The present invention relates to piperazinone compounds, pharmaceutical compositions containing those compounds and methods of treating tumors and cancer, among other disease states and conditions in mammalian patients, especially including humans.
    Type: Application
    Filed: August 23, 2002
    Publication date: September 11, 2008
    Inventors: Andrew D. Hamilton, Said Sebti, Hairuo Peng
  • Patent number: 7393852
    Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: June 21, 2004
    Date of Patent: July 1, 2008
    Assignee: Amgen Inc.
    Inventors: Jian J. Chen, Ben C. Askew, Kaustav Biswas, Jennifer N. Chau, Derin C. D'Amico, Scott Harried, Thomas Nguyen, Wenyuan Qian, Jiawang Zhu, Christopher H. Fotsch, Aiwen Li, Qingyian Liu, Nobuku Nishimura, Tanya Peterkin, Babak Riahi, Chester Chenguang Yuan, Nianhe Han, Rana Nomak, Kevin Yang
  • Patent number: 7268140
    Abstract: This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.
    Type: Grant
    Filed: October 13, 2005
    Date of Patent: September 11, 2007
    Assignee: Schering AG
    Inventors: John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
  • Patent number: 7132539
    Abstract: The present invention relates to compounds which comprise a nitrogen-containing ring scaffold substituted by an R1 alkyl units selected from the group consisting of C1–C12 linear or branched alkyl, C3–C8 cyclic alkyl, C2–C12 linear or branched alkenyl, or haloalkyl, for example, the 2-keto-3-alkylpiperazines having the formula: wherein R is selected from the group consisting of phenyl, 3-fluorophenyl, 4-fluorophenyl, 3,5-difluorophenyl, and 4-chlorophenyl; R1 is selected from the group consisting of methyl, ethyl, propyl, iso-propyl, butyl, iso-butyl, sec-butyl, tert-butyl, cyclopropyl, cyclopropylmethyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexylmethyl, benzyl, allyl, 1-methylallyl, 2-methylallyl, but-2-enyl, and propargyll; R7a is selected from the group consisting of hydrogen, —CO2H, —CONH2, —CONHCH3, and —CON(CH3)2; R8 is benzyl, substituted benzyl, or naphthalen-2-ylmethyl.
    Type: Grant
    Filed: October 20, 2003
    Date of Patent: November 7, 2006
    Assignee: The Procter & Gamble Company
    Inventors: Frank Hallock Ebetino, Xinrong Tian, Wieslaw Adam Mazur, Anny-Odile Colson
  • Patent number: 7115611
    Abstract: This invention relates to compounds of the formula wherein one of R5, R6 and R7 is and X1, X2, Y1 to Y4, R1 to R13 and m and n are defined in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR? and/or PPAR? agonists.
    Type: Grant
    Filed: October 29, 2004
    Date of Patent: October 3, 2006
    Assignee: Hoffmann-la Roche Inc.
    Inventors: Jean Ackermann, Johannes Aebi, Alfred Binggeli, Uwe Grether, Georges Hirth, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer, Peter Mohr, Matthew Blake Wright
  • Patent number: 7105507
    Abstract: The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
    Type: Grant
    Filed: May 16, 2001
    Date of Patent: September 12, 2006
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain
  • Patent number: 7041826
    Abstract: The present invention describes an industrially advantageous process to prepare highly pure 1-Methyl-3-phenylpiperazine of Formula I that makes use of a novel piperazine derivative, 4-Benzyl-1-methyl-2-oxo-3-phenylpiperazine, represented by Formula II 1-Methyl-3-phenylpiperazine is a useful intermediate in the preparation of antidepressant Mirtazapine.
    Type: Grant
    Filed: August 26, 2003
    Date of Patent: May 9, 2006
    Assignee: Aurobindo Pharma Ltd.
    Inventors: Vijay Kumar Handa, Divvela Venkata Naga Srinivasa Rao, Meenakshisunderam Sivakumaran