The Hetero Ring Contains Four Members Including Nitrogen And Carbon Patents (Class 548/950)
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Publication number: 20110105461Abstract: The present invention relates to novel 1-(2,3-dihydro-1,4-benzodioxin-2-yl)-methanamine derivatives, useful as modulators of dopamine neurotransmission, and more specifically as dopaminergic stabilizers. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: April 28, 2009Publication date: May 5, 2011Applicant: NSAB, FILIAL AF NEUROSEARCH SWEDEN AB, SVERIGEInventors: Clas Sonesson, Peder Svensson, Jonas Karlsson
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Patent number: 7935725Abstract: Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A4 hydrolase (LTA4H or LTA4H) modulation and for the treatment of disease states, disorders, and conditions mediated by LTA4H activity, such as allergy, asthma, autoimmune diseases, pruritis, inflammatory bowel disease, ulcerative colitis, and cardiovascular disease, including atherosclerosis and prevention of myocardial infarction.Type: GrantFiled: October 30, 2008Date of Patent: May 3, 2011Assignee: Janssen Pharmaceutica NVInventors: Scott D. Bembenek, Wendy Eccles, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Taraneh Mirzadegan, Alejandro Santillán, Jr.
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Publication number: 20110077231Abstract: Novel compounds, with the following being exemplary:Type: ApplicationFiled: August 12, 2008Publication date: March 31, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Walter Rainer
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Patent number: 7906652Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), and non-alcoholic steatohepatitis (NASH).Type: GrantFiled: November 21, 2006Date of Patent: March 15, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Robert K. Baker, Jeffrey J. Hale, Shouwu Miao, Kathleen M. Rupprecht
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Patent number: 7906503Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.Type: GrantFiled: October 21, 2008Date of Patent: March 15, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Robert K. Baker, Jianming Bao, Shouwu Miao, Kathleen M. Rupprecht
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Publication number: 20110053904Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.Type: ApplicationFiled: August 19, 2010Publication date: March 3, 2011Inventors: Sabine Kolczewski, Emmanuel Pinard
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Patent number: 7893099Abstract: The invention relates to a compound of formula (I) wherein A1 and R1 to R5 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: June 2, 2010Date of Patent: February 22, 2011Assignee: Hoffman-La Roche Inc.Inventors: David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher, Ruben Alvarez Sanchez
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Patent number: 7888354Abstract: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases. A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.Type: GrantFiled: November 13, 2008Date of Patent: February 15, 2011Assignee: Taisho Pharmaceutical Co., LtdInventors: Toshio Nakamura, Makoto Tatsuzuki, Dai Nozawa, Tomoko Tamita, Seiji Masuda, Hiroshi Ohta, Shuhei Kashiwa, Aya Fujino, Shigeyuki Chaki, Toshiharu Shimazaki
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Publication number: 20100317647Abstract: The invention relates to a compound of formula (I) wherein A1 and R1 to R5 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: June 2, 2010Publication date: December 16, 2010Inventors: David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher, Rubén Alvarez Sánchez
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Publication number: 20100311734Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.Type: ApplicationFiled: July 24, 2008Publication date: December 9, 2010Inventors: Maurizio Botta, Emiliano Castiglioni, Romano Di Fabio, Raffaella Spinosa, Andrea Togninelli
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Publication number: 20100297077Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.Type: ApplicationFiled: October 3, 2008Publication date: November 25, 2010Applicant: BIONOMICS LIMITEDInventors: Bernard Luke Flynn, Jonathan Bayldon Baell, Jason Hugh Chaplin, Girmit Singh Gill, Damian Wojciech Grobelny, Andrew John Harvey, Jorgen Alvar Mould, Dharam Paul
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Publication number: 20100291299Abstract: Cyclopentadienyl and Indenyl barium/strontium metal precursors and Lewis base adducts thereof are described. Such precursors have utility for forming Ba- and/or Sr-containing films on substrates, in the manufacture of microelectronic devices or structures.Type: ApplicationFiled: August 3, 2008Publication date: November 18, 2010Applicant: ADVANCED TECHNOLOGY MATERIALS, INC.Inventors: Thomas M. Cameron, Chongying Xu
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Publication number: 20100286109Abstract: The invention relates to novel amide derivatives that are positive allosteric modulators of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.Type: ApplicationFiled: July 22, 2010Publication date: November 11, 2010Applicant: ABBOTT LABORATORIESInventors: Michael R. Schrimpf, Kathleen H. Mortell, Diana L. Nersesian, Chih-Hung Lee, Bruce Clapham
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Publication number: 20100286118Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: May 6, 2010Publication date: November 11, 2010Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
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Publication number: 20100280000Abstract: Disclosed herein are compounds of formula I in which R1, R2, R3, R4, R5, A, X, Y are as described in the specification, their use in pharmaceutical compositions and in methods of treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.Type: ApplicationFiled: April 30, 2010Publication date: November 4, 2010Applicant: AstraZeneca ABInventors: Lars Anders Mikael JOHANSSON, Robert Andrew Judkins, Lanna Li, Bjorn Christian Ingvar Lofberg, Joachim Persson
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Publication number: 20100279997Abstract: A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.Type: ApplicationFiled: October 28, 2009Publication date: November 4, 2010Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Publication number: 20100261696Abstract: In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (G1yT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (G1yT1) activity 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: ApplicationFiled: March 31, 2010Publication date: October 14, 2010Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
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Patent number: 7803839Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.Type: GrantFiled: October 5, 2006Date of Patent: September 28, 2010Assignee: Exelixis, Inc.Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
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Publication number: 20100234340Abstract: Substituted spiroamide compounds corresponding to formula (I): wherein A, B, Q1, Q2, Q3, Q4, R1, R8, R9a, R9b, R12, R13, R200 and R210 have defined meanings, processes for their preparation, pharmaceutical compositions containing such compounds, and the use of such compounds for treating or inhibiting pain or other conditions mediated at least in part by the bradykinin 1 receptor (B1R).Type: ApplicationFiled: February 5, 2010Publication date: September 16, 2010Applicant: Gruenenthal GmbHInventors: Stefan Schunk, Melanie Reich, Michael Engels, Tieno Germann, Ruth Jostock, Sabine Hees
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Publication number: 20100234341Abstract: Compounds of formula (I) including pharmaceutically acceptable salts, esters, solvates and stereoisomers thereof, R1, R2 and R3 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.Type: ApplicationFiled: December 4, 2007Publication date: September 16, 2010Inventors: Marion Lanier, Deborah Slee, Emily Lin, Zhiyong Robert Luo, Yongsheng Chen, Manisha Moorjani, Binh G. Vong, John Tellew
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Patent number: 7790707Abstract: The present invention relates to compounds that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. In certain embodiments, the compounds of the invention relate to aryl oxoimidazolidinyls.Type: GrantFiled: March 21, 2007Date of Patent: September 7, 2010Assignee: EPIX Pharmaceuticals Inc.Inventors: Ashis Saha, Xiang Yu, Mercedes Lobera, Jian Lin, Srinivasa R. Cheruku, Oren Becker, Yael Marantz, Nili Schutz
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Publication number: 20100222600Abstract: The invention relates to novel azetidine compounds of formula (I), wherein R1, R2, and X are as described in the description and their use as orexin receptor antagonists.Type: ApplicationFiled: August 15, 2007Publication date: September 2, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Patent number: 7786104Abstract: The invention concerns compounds of general formula (I): Wherein n, X1, X2, X3, X4, Y, Z, Z1, Z2, Z3 and Z4 are as defined herein. The invention also concerns a process for the preparation of compounds of formula (I) and their therapeutic use.Type: GrantFiled: January 26, 2009Date of Patent: August 31, 2010Assignee: Sanofi-AventisInventors: Laurent DuBois, Yannick Evanno, Andre Malanda, David Machnik, Catherine Gille
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Publication number: 20100210696Abstract: Provided is a compound having a superior acid secretion suppressive action, which shows an antiulcer activity and the like.Type: ApplicationFiled: September 24, 2008Publication date: August 19, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Haruyuki Nishida, Yasuyoshi Arikawa, Keizo Hirase
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Publication number: 20100210620Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: September 30, 2008Publication date: August 19, 2010Inventors: Prasun K. Chakravarty, Yanbing Ding, Joseph L. Duffy, Hassan Pajouhesh, Pengeheng Patrick Shao, Sriram Tyagarajan, Feng Ye
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Publication number: 20100204196Abstract: Novel pyrrolopyrimidines as shown in formula (I): and pharmaceutically acceptable derivatives thereof. The compounds are useful in the inhibition of IGF-1R.Type: ApplicationFiled: August 6, 2008Publication date: August 12, 2010Inventors: Stanley Dawes Chamberlain, Felix Deanda, JR., Roseanne Gerding, Masaichi Hasegawa, Kevin Kuntz, Huangshu Lei, Yasushi Miyazaki, Naohiko Nishigaki, Samarjit Patnaik, Aniko Redman, John Brad Shotwell, Kirk Stevens, Joseph Wilson, Bin Yang
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Patent number: 7772223Abstract: The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.Type: GrantFiled: September 18, 2006Date of Patent: August 10, 2010Assignee: Pfizer Inc.Inventors: Paul Alan Glossop, Simon John Mantell, Anthony Wood, Christine Anne Louise Watson
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Patent number: 7767672Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: GrantFiled: November 3, 2006Date of Patent: August 3, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Michael Mortimore, Chris Davis, Dean Boyall, Simon Everitt, Daniel Robinson, Sharn Ramaya, Damien Fraysse, John Studley, Andrew Miller, Michael O'Donnell, Alistair Rutherford, Joanne Pinder
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PRO-DRUGS OF NSAIAS WITH VERY HIGH SKIN AND MEMBRANES PENETRATION RATES AND THEIR NEW MEDICINAL USES
Publication number: 20100172960Abstract: The novel positively charged pro-drugs of NSAIAs in the general formulas (1, 2a, 2b, 2c, or 2d) “Structure 1, 2a, 2b, 2c, or 2d” were designed and synthesized. The compounds of the general formulas (1, 2a, 2b, 2c, or 2d) “Structure 1, 2a, 2b, 2c, or 2d” indicated above can be prepared from metal salts, organic base salts, or immobilized base salts of NSAIAs with suitable halide compounds. The positively charged amino groups in the pro-drugs in this invention largely increase the solubility of the drugs in water and will bond to the negative charge on the phosphate head group of membrane. Thus, the local concentration of the outside of the membrane or skin will be very high and will facilitate the passage of these pro-drugs from a region of high concentration to a region of low concentration. This bonding will disturb the membrane a little bit and may make some room for the lipophilic portion of the pro-drug.Type: ApplicationFiled: June 4, 2007Publication date: July 8, 2010Inventors: Chongxi Yu, Lina Xu -
Patent number: 7745565Abstract: A description is given of azetidine derivatives and methods for producing them, and of their use as a latent curing component for resins having functional groups which are reactive toward amino groups. The particular advantages of the curing component proposed in accordance with the invention, such as effective producibility, high environmental friendliness, and excellent storage stability of the resin/curing agent mixtures, make these azetidine derivatives outstandingly suitable for one-component, moisture-hardening polymer compositions, which are of special interest in particular for the production of (floor) coatings, sealants, and adhesives.Type: GrantFiled: December 2, 2004Date of Patent: June 29, 2010Assignee: Construction Research & Technology GmbHInventors: Stefan Ingrisch, Alois Maier, Thomas Pfeuffer, Norbert Steidl, Herbert Winkelmann, Andrea Gantner, legal representative
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Publication number: 20100160289Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: ApplicationFiled: December 15, 2009Publication date: June 24, 2010Inventors: Mark J. Macielag, James J. McNally
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Patent number: 7741316Abstract: A method of treating or preventing Alzheimer's disease, Parkinson's Disease and/or schizophrenia, this method comprising administering to a patient in need of such treatment a compound of formula: in which R, R3 and R4 are as defined in the specification.Type: GrantFiled: November 12, 2004Date of Patent: June 22, 2010Assignee: Aventis Pharma S.A.Inventors: Daniel Achard, Herve Bouchard, Jean Bouquerel, Bruno Filoche, Serge Grisoni, Augustin Hittinger, Michael R. Myers
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Publication number: 20100130712Abstract: Provided is a cured resin of an adamantane derivative having a specific structure, which has excellent optical properties such as transparency and (long-term) light stability, long-term heat resistance, dielectric constant, and mechanical properties, and which can be utilized suitably in the field of electronic and optical materials.Type: ApplicationFiled: March 31, 2008Publication date: May 27, 2010Applicant: Idemitsu Kosan Co., Ltd.Inventors: Katsuki Ito, Yasunari Okada, Hideki Yamane, Shinobu Yamao
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Publication number: 20100125058Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein W, X, Y, and R1-R7 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: ApplicationFiled: November 9, 2009Publication date: May 20, 2010Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Eric Mertz, Sung-Sau So, Hong Ying Yun, Zhenshan Zhang
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Publication number: 20100099661Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R8 and R9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: June 18, 2009Publication date: April 22, 2010Applicant: Achaogen, Inc.Inventors: James Bradley Aggen, Adam Aaron Goldblum, Martin Sheringham Linsell, Paola Dozzo, Heinz Ernst Moser, Darin James Hildebrandt, Micah James Gliedt
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Patent number: 7696234Abstract: The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.Type: GrantFiled: May 24, 2005Date of Patent: April 13, 2010Assignee: Eli Lilly and CompanyInventors: Lisa Selsam Beavers, Robert Alan Gadski, Cynthia Darshini Jesudason, Richard Todd Pickard, Freddie Craig Stevens
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Patent number: 7691841Abstract: Compounds of formula I in free or salt form, wherein Ar, X, Y 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: GrantFiled: August 9, 2005Date of Patent: April 6, 2010Assignee: Novartis AGInventor: Darren M Legrand
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Patent number: 7691843Abstract: Novel N-hydroxyamide derivatives are disclosed. These N-hydroxyamide derivatives inhibit UPD-3-O—(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase, an enzyme present in gram negative bacteria and are therefore useful as antimicrobials and antibiotics. Methods of synthesis and of use of the compounds are also disclosed.Type: GrantFiled: July 11, 2003Date of Patent: April 6, 2010Assignee: Pfizer Inc.Inventors: Bore G. Raju, Hardwin O'Dowd, Hongwu Gao, Dinesh V. Patel, Jaoquim Trias
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Patent number: 7678818Abstract: Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: January 19, 2007Date of Patent: March 16, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Aurelia Conte, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Werner Mueller, Philippe Pflieger
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Patent number: 7678778Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.Type: GrantFiled: October 25, 2005Date of Patent: March 16, 2010Assignee: DEKK-TEC, Inc.Inventor: Lee Roy Morgan
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Patent number: 7678904Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 meType: GrantFiled: January 7, 2005Date of Patent: March 16, 2010Assignee: University of KentuckyInventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
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Publication number: 20100056490Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: ApplicationFiled: July 9, 2009Publication date: March 4, 2010Inventors: Emmanuelle Briard, Rainer Martin Lueoend, Rainer Machauer, Henrik Moebitz, Olivier Rogel, Jean-Michel Rondeau, Heinrich Rueeger, Marina Tintelnot-Blomley, Siem Jacob Veenstra
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Publication number: 20100048531Abstract: The present invention relates to a compound of formula I wherein R1, R2, X, Ar1 and Ar2 are as defined herein and to pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to their corresponding enantiomers and/or optical isomers thereof. Compounds of the invention are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors.Type: ApplicationFiled: August 14, 2009Publication date: February 25, 2010Inventors: Sabine Kolczewski, Robert Narquizian, Emmanuel Pinard
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Patent number: 7645752Abstract: The present invention is directed to compounds of Formula I: which are modulators of the 5-hydroxtryptamine-6 and 5-hydroxytryptamine-2A receptors and which are inhibitors of norepinephrine reuptake. The compounds of the invention, and pharmaceutical composition thereof, are useful in the treatment of disorders related to or associated with the 5-hydroxytryptamine-6 and 5-hydroxtryptamine-2A receptors or with norepinephrine reuptake inhibition.Type: GrantFiled: January 12, 2007Date of Patent: January 12, 2010Assignee: Wyeth LLCInventors: Robert E. McDevitt, Yanfang Li, Albert J. Robichaud, Gavin D. Heffernan, Richard D. Coghlan, Ronald C. Bernotas
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Patent number: 7642263Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts and prodrugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: GrantFiled: September 2, 2008Date of Patent: January 5, 2010Assignee: AstraZeneca ABInventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Patent number: 7632840Abstract: A quinazoline derivative of the formula I: wherein: R1, R2, R3, R3a, R4, R5, R5a R6, R7, a, m and p are as defined in the description. Also claimed are pharmaceutical compositions containing the quinazoline derivative, the use of the quinazoline derivatives as medicaments and processes for the preparation of the quinazoline derivative. The quinazoline derivatives of formula I, are useful in the treatment of hyperproliferative disorders such as a cancer.Type: GrantFiled: January 31, 2005Date of Patent: December 15, 2009Assignee: AstraZeneca ABInventors: Benedicte Delouvrie, Craig Steven Harris, Laurent Francois Andre Hennequin, Christopher Thomas Halsall, Janet Elizabeth Pease, Peter Mark Smith
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Patent number: 7618967Abstract: The invention provides novel indane compounds which are useful in the treatment of affective disorders, pain disorders, attention deficit hyperactivity disorder (ADHD), cognitive disorders, substance abuse, smoking cessation and stress urinary incontinence.Type: GrantFiled: August 30, 2007Date of Patent: November 17, 2009Assignee: H. Lundbeck A/SInventors: Jan Kehler, Karsten Juhl, Ask Püschl
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Publication number: 20090275524Abstract: The present invention relates to novel hypocholesterolemic compounds of formula (I) useful in the treatment and prevention of atherosclerosis and for the reduction of cholesterol levels as well as to pharmaceutical compositions comprising said compounds alone or in combination with other active agentsType: ApplicationFiled: May 7, 2009Publication date: November 5, 2009Inventors: Erick Carreira, Helmut Hauser, Lisbet Kvaerno, Tobias Ritter, Moritz Werder
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Publication number: 20090253669Abstract: Substituted sulfonamide compounds corresponding to the formula I: processes for the preparation thereof, pharmaceutical composition containing these compounds and the use of substituted sulfonamide compounds for the preparation of pharmaceutical compositions.Type: ApplicationFiled: March 16, 2009Publication date: October 8, 2009Applicant: GRUENENTHAL GmbHInventors: Stefan OBERBOERSCH, Melanie REICH, Bernd SUNDERMANN, Werner ENGLBERGER, Sabine HEES, Ruth JOSTOCK, Stefan SCHUNK, Edward BIJSTERVELD, Fritz THEIL
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Patent number: 7598236Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: December 15, 2007Date of Patent: October 6, 2009Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy