Halogen Bonded Directly To The Aryl Ring Or Ring System Patents (Class 564/345)
  • Publication number: 20140170216
    Abstract: Polymorphous and amorphous forms of bupropion hydrobromide are described.
    Type: Application
    Filed: September 4, 2013
    Publication date: June 19, 2014
    Applicant: VALEANT INTERNATIONAL BERMUDA
    Inventors: Stefano Turchetta, Maurizio Zenoni
  • Patent number: 8735454
    Abstract: The present application describes deuterium-enriched bupropion, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Grant
    Filed: August 22, 2013
    Date of Patent: May 27, 2014
    Assignee: DeuteRx, LLC
    Inventor: Anthony W. Czarnik
  • Publication number: 20140018436
    Abstract: The present application describes deuterium-enriched bupropion, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: August 22, 2013
    Publication date: January 16, 2014
    Applicant: DEUTERX, LLC
    Inventor: Anthony W. Czarnik
  • Patent number: 8604085
    Abstract: Polymorphous and amorphous forms of bupropion hydrobromide are described.
    Type: Grant
    Filed: October 17, 2012
    Date of Patent: December 10, 2013
    Assignee: Valeant International Bermuda
    Inventors: Stefano Turchetta, Maurizio Zenoni
  • Patent number: 8524780
    Abstract: The present application describes deuterium-enriched bupropion, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Grant
    Filed: May 19, 2010
    Date of Patent: September 3, 2013
    Assignee: DeuteRx, LLC
    Inventor: Anthony W. Czarnik
  • Patent number: 8450376
    Abstract: The present invention provides an amorphous bupropion hydrobromide and an amorphous bupropion hydrobromide granulates with at least one pharmaceutically acceptable carrier, and a process for its preparation.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: May 28, 2013
    Assignee: Glenmark Generics Ltd.
    Inventors: Shankar Sanganabhatla, Vijay Soni, Mubeen Ahmed Khan, Nandlal Agarwal, Hemanth Kamble, Sharad Gore
  • Publication number: 20130059005
    Abstract: Polymorphous and amorphous forms of bupropion hydrobromide are described.
    Type: Application
    Filed: October 17, 2012
    Publication date: March 7, 2013
    Inventors: Stefano TURCHETTA, Maurizio ZENONI
  • Patent number: 8349900
    Abstract: Polymorphous and amorphous forms of bupropion hydrobromide are described.
    Type: Grant
    Filed: August 6, 2009
    Date of Patent: January 8, 2013
    Assignee: Valeant International Bermuda
    Inventors: Stefano Turchetta, Maurizio Zenoni
  • Publication number: 20120071560
    Abstract: The invention provides bupropion analogue compounds capable of inhibiting the reuptake of one or more monoamines. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin. Such compounds may be used to treat conditions that are responsive to inhibition of the reuptake of monoamines, including addiction, depression, and obesity.
    Type: Application
    Filed: October 12, 2011
    Publication date: March 22, 2012
    Inventors: Frank Ivy Carroll, Bruce Edward Blough, Philip Abraham
  • Publication number: 20110245493
    Abstract: The present invention relates to the delivery of drug amines through an inhalation route. Specifically, it relates to aerosols containing drug amines that are used in inhalation therapy. In one aspect of the present invention, a method of delivering an amine drug in an aerosol form is provided. The method comprises: a) heating a coating, which includes an amine drug salt on a substrate contained in a device to a temperature sufficient to volatilize the amine drug from the coating, h) by said heating, forming an amine drug vapor, and c) during said heating, drawing air through said device, condensing said vapor to form aerosol particles containing less than 10% degradation products of the compound.
    Type: Application
    Filed: April 1, 2011
    Publication date: October 6, 2011
    Applicant: ALEXZA PHARMACEUTICALS, INC.
    Inventors: Joshua D. RABINOWITZ, Alejandro C. Zaffaroni
  • Publication number: 20110207965
    Abstract: A process for preparing N-[(1R)-1-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)-phenyl]propan-1-amine of formula (I) i.e. Cinacalcet and its intermediates of formulae (V), (Va) and (Vb).
    Type: Application
    Filed: October 16, 2009
    Publication date: August 25, 2011
    Applicant: ZACH SYSTEM S.P.A.
    Inventors: Nicola Catozzi, Johnny Foletto, Massimiliano Forcato, Roberto Giovanetti, Giorgio Soriato, Massimo Verzini
  • Publication number: 20110130463
    Abstract: The present application describes deuterium-enriched bupropion, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: May 19, 2010
    Publication date: June 2, 2011
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Publication number: 20110105619
    Abstract: The present invention provides an amorphous bupropion hydrobromide and an amorphous bupropion hydrobromide granulates with at least one pharmaceutically acceptable carrier, and a process for its preparation.
    Type: Application
    Filed: June 15, 2009
    Publication date: May 5, 2011
    Applicant: Glenmark Generics Ltd.
    Inventors: Shankar Sanganabhatla, Vijay Soni, Mubeen Ahmed Khan, Nandlal Agarwal, Hemanth Kamble, Sharad Gore
  • Patent number: 7884136
    Abstract: The present invention relates to pharmaceutical compositions, formulations and medicaments comprising a bupropion salt, in particular, modified-release tablets comprising an effective amount of bupropion hydrobromide, and the use of the bupropion salt to prepare a medicament to treat a condition.
    Type: Grant
    Filed: June 27, 2006
    Date of Patent: February 8, 2011
    Assignee: Biovail Laboratories International S.R.L.
    Inventors: Werner Oberegger, Fang Zhou, Paul Maes, Stefano Turchetta, Graham Jackson, Pietro Massardo, Mohammad Ashty Saleh
  • Patent number: 7767672
    Abstract: 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: Grant
    Filed: November 3, 2006
    Date of Patent: August 3, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: 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
  • Patent number: 7737288
    Abstract: Non-steroidal androgen receptor modulating compounds of the general formula (I), their pharmaceutically acceptable salts, preparation process and pharmaceutically compositions containing the said compounds are disclosed. Such compounds of the general formula (I) or their pharmaceutically acceptable salts can be used for preparing non-steroidal medicines to treat and/or prevent conditions or diseases such as prostatic hyperplasia, prostate cancer, hirsutism, severe hormone-dependent alopecia or acne, etc. as a result of androgen receptor antagonistic activities.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: June 15, 2010
    Assignees: Shanghai Institute of Materia Medica Chinese Academy of Sciences, Sichuan University
    Inventors: Mingwei Wang, Caihong Zhou, Xin Hui, Haoran Su, Jie Gao, Yong Deng, Dacheng Yang
  • Patent number: 7723385
    Abstract: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
    Type: Grant
    Filed: February 25, 2009
    Date of Patent: May 25, 2010
    Assignee: GlaxoSmithKline LLC
    Inventors: Philip Stewart Turnbull, Rodolfo Cadilla, David John Cowan, Andrew Lamont Larkin, Istvan Kaldor, Eugene Lee Stewart
  • Publication number: 20100075950
    Abstract: The present invention relates to new phenylpropanone modulators of dopamine receptors, serotonin receptors, and/or nicotinic acetylcholine receptors, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: August 19, 2009
    Publication date: March 25, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Manouchehr M. Shahbaz, Sepehr Sarshar
  • Publication number: 20100068270
    Abstract: Polymorphous and amorphous forms of bupropion hydrobromide are described.
    Type: Application
    Filed: August 6, 2009
    Publication date: March 18, 2010
    Applicant: BIOVAIL LABORATORIES INTERNATIONAL S.R.L.
    Inventors: Stefano TURCHETTA, Maurizio Zenoni
  • Patent number: 7674936
    Abstract: Disclosed are compounds of Formula I, their N-oxides and agriculturally suitable salts wherein J is a phenyl ring, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused carbobicyclic or heterobicyclic ring system wherein each ring or ring system is substituted with from one to four substituents independently selected from R5; K is —NR1C(=A)-, —N?C(GR6)— or —NR1SO2—; L is —C(?B)NR2—, —C(GR6)?N—, —SO2NR2—, —C(?B)O— or —C(?B)—; and A, B, G, R1, R2, R3, R4, R5, R6 and n are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the pests or their environment with a biologically effective amount of a compound of Formula I and compositions containing the compounds of Formula I. Intermediate compounds useful in preparing the compounds of Formula I are also disclosed.
    Type: Grant
    Filed: May 11, 2007
    Date of Patent: March 9, 2010
    Assignee: E.I. du Pont De Nemours and Company
    Inventors: Kenneth Andrew Hughes, George Philip Lahm, Thomas Paul Selby, Benjamin Kenneth Smith, William Thomas Zimmerman
  • Patent number: 7572935
    Abstract: The present invention relates to pharmaceutical compositions, formulations and medicaments comprising a bupropion salt, in particular, modified-release tablets comprising an effective amount of bupropion hydrobromide, and the use of the bupropion salt to prepare a medicament to treat a condition.
    Type: Grant
    Filed: June 14, 2007
    Date of Patent: August 11, 2009
    Assignee: Biovail Laboratories International S.R.L.
    Inventors: Werner Oberegger, Paul Maes, Stefano Turchetta, Pietro Massardo, Mohammad Ashty Saleh
  • Publication number: 20090187028
    Abstract: A novel process is provided for the preparation of chiral trans-2,3-disubstituted 5-oxotetrahydropyrans of structural formula (I): wherein Ar is optionally substituted phenyl and P is a primary amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.
    Type: Application
    Filed: January 22, 2009
    Publication date: July 23, 2009
    Inventors: Feng Xu, Mary M. Kim, Yoshinori Kohmura, Tricia Sladicka, Jonathan D. Rosen, Michael J. Zacuto
  • Patent number: 7553992
    Abstract: The present invention relates to pharmaceutical compositions, formulations and medicaments comprising a bupropion salt, in particular, modified-release tablets comprising an effective amount of bupropion hydrobromide, and the use of the bupropion salt to prepare a medicament to treat a condition.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: June 30, 2009
    Assignee: Biovail Laboratories International S.R.L.
    Inventors: Werner Oberegger, Paul Maes, Stefano Turchetta, Pietro Massardo, Mohammad Ashty Saleh
  • Patent number: 7514470
    Abstract: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
    Type: Grant
    Filed: March 3, 2005
    Date of Patent: April 7, 2009
    Assignee: SmithKline Beecham Corporation
    Inventors: Philip Stewart Turnbull, Rodolfo Cadilla, David John Cowan, Andrew Lamont Larkin, Istvan Kaldor, Eugene Lee Stewart
  • Publication number: 20090076161
    Abstract: The present application describes deuterium-enriched bupropion, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: August 21, 2008
    Publication date: March 19, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Publication number: 20080293808
    Abstract: Non-steroidal androgen receptor modulating compounds of the general formula (I), their pharmaceutically acceptable salts, preparation process and pharmaceutically compositions containing the said compounds are disclosed. Such compounds of the general formula (I) or their pharmaceutically acceptable salts can be used for preparing non-steroidal medicines to treat and/or prevent conditions or diseases such as prostatic hyperplasia, prostate cancer, hirsutism, severe hormone-dependent alopecia or acne, etc. as a result of androgen receptor antagonistic activities.
    Type: Application
    Filed: May 26, 2006
    Publication date: November 27, 2008
    Inventors: Mingwei Wang, Caihong Zhou, Xin Hui, Haoran Su, Jie Gao, Yong Deng, Dacheng Yang
  • Publication number: 20080233606
    Abstract: Provided herein are assays for detecting enzyme activity using Raman Spectroscopy.
    Type: Application
    Filed: April 22, 2008
    Publication date: September 25, 2008
    Inventors: Mustapha Haddach, Gregory S. Naeve
  • Patent number: 7091382
    Abstract: A process is disclosed for manufacturing N-methyl-N-phenylaminoacrolein of formula (I) which comprises reacting N-methylformanilide and an alkyl vinyl ether of formula (III) wherein R is a C3–C4 alkyl, said process being characterized in that the reaction between N-methylformanilide and said alkyl vinyl ether of formula (III) is carried out in the presence of phosgene, diphosgene or triphosgene in a solvent selected from dioxane, acetonitrile and/or chlorobenzene.
    Type: Grant
    Filed: May 7, 2004
    Date of Patent: August 15, 2006
    Assignee: Clariant Life Science Molecules (Italia) S.p.A.
    Inventors: Aldo Banfi, Alfredo Mancini
  • Patent number: 6765022
    Abstract: Described are cyclobexylamine derivatives of Formula I, Formula II, or Formula III and their pharmaceutically acceptable salts thereof: The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease. The substituents are described in the specification.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: July 20, 2004
    Assignee: Warner-Lambert Company
    Inventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
  • Patent number: 6653508
    Abstract: Substituted 3-amino-2-benzyl-1-phenlypropane derivatives, methods for preparing them, pharmaceutical compositions containing them, and methods of using them to treat various medical conditions.
    Type: Grant
    Filed: January 16, 2002
    Date of Patent: November 25, 2003
    Assignee: Gruenenthal GmbH
    Inventors: Michael Sattlegger, Helmut Buschmann, Babette-Yvonne Koegel
  • Publication number: 20030040483
    Abstract: Compounds of peptide mimetic nature having the general formula I 1
    Type: Application
    Filed: March 23, 2000
    Publication date: February 27, 2003
    Inventors: Thomas Kruse Hansen, Bernd Peschke, Jesper Lau, Behrend Friedrich Lundt, Michael Ankersen, Brett Watson, Kjeld Madsen
  • Patent number: 6482987
    Abstract: Novel, stable formulations of bupropion hydrochloride are provided which will maintain at least 80% of initial bupropion hydrochloride potency after one year. Methods of inhibiting degradation of bupropion hydrochloride and methods of preparing stable formulations of bupropion hydrochloride are also provided.
    Type: Grant
    Filed: April 2, 2001
    Date of Patent: November 19, 2002
    Assignee: Clonmel Healthcare, Ltd.
    Inventors: Prakash Shriram Kulkarni, Bharat Bhogilal Shah, Amitava Maitra, Joseph Michael DeVito
  • Patent number: 6462237
    Abstract: An inclusion complex of bupropion hydrochloride with beta cyclodextrin that stabilizes the bupropion hydrochloride against degradation. A method of preparing an inclusion complex of bupropion hydrochloride with beta cyclodextrin that stabilizes the bupropion hydrochloride against degradation. A novel stabilized sustained-release pharmaceutical composition of bupropion hydrochloride containing an inclusion complex of bupropion hydrochloride with beta cyclodextrin. A method of preparing a novel stabilized sustained-release pharmaceutical composition containing an inclusion complex of bupropion hydrochloride with beta cyclodextrin.
    Type: Grant
    Filed: June 14, 2001
    Date of Patent: October 8, 2002
    Assignee: USV Limited
    Inventors: Suresh Kumar Gidwani, Purushottam Singnurkar, Prashant Kumar Tewari
  • Patent number: 6350767
    Abstract: The present invention relates to compounds, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.
    Type: Grant
    Filed: November 19, 1999
    Date of Patent: February 26, 2002
    Assignee: Novo Nordisk A/S
    Inventors: Jesper Lau, Bernd Peschke, Thomas Kruse Hansen, Nils Langeland Johansen, Michael Ankersen
  • Patent number: 6235791
    Abstract: The present invention relates to the use of compounds capable of displacing tritiated cis-N-cyclohexyl-N-ethyl [3-(3-chloro-4-cyclohexylphenyl)-allyl]amine from its receptors for the preparation of pharmaceutical compositions intended to combat cell proliferation.
    Type: Grant
    Filed: April 12, 1999
    Date of Patent: May 22, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Jean Claude Breliere, Pascual Ferrara, Christine Lebouteiller, Raymond Paul, Jorge Rosenfeld, Didier Van Broeck
  • Patent number: 6087346
    Abstract: The invention relates to methods for the treatment of central nervous system disorders, neurological disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof.
    Type: Grant
    Filed: February 21, 1996
    Date of Patent: July 11, 2000
    Assignees: Cambridge Neuroscience, Inc., Virginia Commonwealth University
    Inventors: Richard A. Glennon, James B. Fischer
  • Patent number: 6057371
    Abstract: The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT.sub.1A receptors.
    Type: Grant
    Filed: June 10, 1992
    Date of Patent: May 2, 2000
    Assignee: Virginia Commonwealth University
    Inventor: Richard A. Glennon
  • Patent number: 5977178
    Abstract: Compounds of peptide mimetic nature having the general formula I ##STR1## wherein a and b are independently 1 or 2, R.sup.1 and R.sup.2 are independently H or C.sub.1-6 alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.
    Type: Grant
    Filed: December 18, 1996
    Date of Patent: November 2, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Thomas Kruse Hansen, Bernd Peschke, Jesper Lau, Behrend Friedrich Lundt, Michael Ankersen, Brett Watson, Kjeld Madsen
  • Patent number: 5789448
    Abstract: Disclosed is a benzoylethylene derivative represented by the following formula (I) or a salt thereof. ##STR1## R.sup.1 to R.sup.5 : a hydrogen atom, --OR.sup.9 (R.sup.9 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc.), etc.,R.sup.6 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc.,R.sup.7 : a hydrogen atom, a cyano group, a C.sub.1 -C.sub.5 alkyl group, --SO.sub.q R.sup.15 (q: 0, 1, 2, R.sup.15 : a thienyl group, a phenyl group, etc.) etc.,R.sup.8 : a cyano group, --CR.sup.22 R.sup.23 X (R.sup.22, R.sup.23 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc., X: --NR.sup.24 R.sup.25 (R.sup.24, R.sup.25 : a C.sub.1 -C.sub.5 alkyl group, etc., an alkylene group by combining, etc.)), etc.The benzoylethylene derivative of the present invention has potent tyrosine kinase inhibiting activity and cancer cell growth inhibiting activity. The tyrosine kinase inhibitor of the present invention is useful as a carcinostatic agent.
    Type: Grant
    Filed: June 25, 1996
    Date of Patent: August 4, 1998
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Yasunori Kitano, Haruki Inokawa, Hisao Takayanagi, Tamaki Yano, Hiroe Umeki, Hiroto Hara
  • Patent number: 5780505
    Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.7 and R.sub.8 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a phenyl group with either two or three substituents of the following formula: ##STR2## wherein the positions of substitution are R.sub.2,R.sub.3 -, R.sub.2,R.sub.4 -, R.sub.2,R.sub.5 -, R.sub.2,R.sub.6 -, R.sub.3,R.sub.4 -, R.sub.3,R.sub.5 -, and R.sub.2,R.sub.4,R.sub.6 - and R.sub.2 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.3 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.4 is methyl, fluoro, bromo, methoxy or cyano; R.sub.5 is methyl, fluoro, chloro, methoxy, cyano or trifluoromethyl; R.sub.
    Type: Grant
    Filed: July 7, 1997
    Date of Patent: July 14, 1998
    Assignee: American Home Products Corporation
    Inventors: Madelene M. Antane, David R. Herbst, Geraldine R. McFarlane, Eric G. Gundersen, Bradford H. Hirth, Dominick A. Quagliato, Russell F. Graceffa, John A. Butera
  • Patent number: 5674909
    Abstract: Compounds of formula ##STR1## wherein R, R', R", R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, X, Y, m, n and p have the meanings reported in the description;and their pharmaceutically acceptable salts are described.The compounds of formula I are useful in the treatment of arterial hypertension and congestive heart failure, of renal failure, of peripheral arteriopathies, of cerebrovascular insufficiencies and of ischemic cardiopathy.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 7, 1997
    Assignee: Zambon Group
    Inventors: Stefania Montanari, Paolo Cavalleri, Cristina Fraire, Gian Carlo Grancini, Mauro Napoletano, Francesco Santangelo
  • Patent number: 5561135
    Abstract: The invention relates to new N,N,N'N'-tetra-substituted-1,2-ethanediamine compounds of the general formula (I): ##STR1## wherein X is a carbonyl (CO), hydroxymethylen (CHOH) or p-fluorophenyl-methylen (p--F--C.sub.6 H.sub.4 --CH) group and R is a benzyl group optionally substituted in p-- with an halogen, or R is a 2-pyrimidinyl group with the proviso that simultaneously X may not be p-fluorophenyl-methylen (p--F--C.sub.6 H.sub.4 --CH) and R may not be an unsubstituted benzyl group, as well as their pharmaceutically acceptable additions salts.The compounds are potentially useful in the treatment of sigma receptor-related nervous system diseases.
    Type: Grant
    Filed: April 21, 1995
    Date of Patent: October 1, 1996
    Assignee: Ferrer Internacional, S.A.
    Inventors: Rafael Foguet, Santiago Gubert, Jos e Ortiz, Aurelio Sacrist an, Josep M. Castell o
  • Patent number: 5502233
    Type: Grant
    Filed: January 23, 1995
    Date of Patent: March 26, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Heinz-Wilhelm Dehne, Stefan Dutzmann, Christoph Erdelen
  • Patent number: 5407961
    Abstract: The present invention is concerned with antiretroviral (e.g. anti HIV-1) compounds having the formula ##STR1## Pharmaceutical compositions containing said compounds of formula (I-a) or (I-b), and processes of preparing said compounds and compositions.
    Type: Grant
    Filed: May 12, 1994
    Date of Patent: April 18, 1995
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marcel A. C. Janssen, Georges H. P. Van Daele, Jean-Paul R. M. A. Bosmans, Frans M. A. Van den Keybus, Karin J. M. M. Nuyens, Paul A. J. Janssen
  • Patent number: 5037980
    Abstract: A compound of the formula: ##STR1## wherein R.sub.1 is ##STR2## where R.sub.3, R.sub.4 and R.sub.5 may be the same or different and are hydrogen, trihalomethyl, halogen or lower alkoxy having from 1 to 3 carbon atoms with the proviso that at least one of R.sub.3, R.sub.4 and R.sub.5 must be other than hydrogen; and R.sub.2 is hydrogen and lower alkyl having from 1 to 3 carbon atoms.
    Type: Grant
    Filed: April 18, 1988
    Date of Patent: August 6, 1991
    Assignee: American Cyanamid Company
    Inventors: John P. Dusza, Jay D. Albright
  • Patent number: 5036107
    Abstract: 1-Phenyl-7-substituted-hept-5-yn-2-ones substituted with a C.sub.1 to C.sub.7 alkyl, C.sub.3 to C.sub.6 cycloalkyl, aryl, heteroaryl or heterocycloalkyl group at the 1-position and an amino, a dialkylamino, a piperidyl, a pyrrolidyl or a hexahydroazepinyl group at the 7-position are disclosed which may have one or two substituents in addition to the phenyl group at the 1-position and also may have a p-fluoro substituent on the phenyl group. The preferred compounds are, 1-cyclohexyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one, 1-cyclobutyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one and 1-cyclo-1-phenyl-1-hydroxy-7-ethylaminohept-5-yn-2-one.The compounds are highly specific M.sub.1 -AChR antagonists with relatively prolonged duration of activity.
    Type: Grant
    Filed: November 16, 1989
    Date of Patent: July 30, 1991
    Assignee: Marion Merrell Dow Inc.
    Inventors: Waclaw J. Rzeszotarski, Maria E. Guzewska, Daniel W. McPherson, Ciro J. Spagnuolo, Kenneth J. Natalie, Jr.
  • Patent number: 4996318
    Abstract: The amino-9,10-secosteroids ##STR1## of the present invention contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain and are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc.
    Type: Grant
    Filed: September 19, 1989
    Date of Patent: February 26, 1991
    Assignee: The Upjohn Company
    Inventors: Martin Gall, Robert I. Higuchi
  • Patent number: 4981990
    Abstract: The invention relates to a process for the preparation of 4-phenylpyrrole derivatives of the formula I ##STR1## wherein R.sub.n, R.sub.1 and R.sub.2 are as defined in claim 1, which comprises reacting a phenacylamine of formula II ##STR2## with a compound of formula IIIT--CH.dbd.CH--R.sub.1 (III)to give an intermediate of formula IV ##STR3## and cyclizing said intermediate, in the presence of a base, to give the compound I.Important intermediates and novel final products are also described.
    Type: Grant
    Filed: December 22, 1988
    Date of Patent: January 1, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Pierre Martin
  • Patent number: 4980377
    Abstract: The present invention relates to the preparation of new 1-(aminophenyl)-2-aminopropanone derivatives of the general formula: ##STR1## in which X is NH.sub.2, Y is H or a halogen atom, Z is H or a halogen atom, R.sub.1 is C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.6 cycloalkyl and R.sub.2 is H or C.sub.1 -C.sub.4 alkyl, or R.sub.1 and R.sub.2, taken together, can form, with the nitrogen atom to which they are bonded, a heterocyclic group selected from the group consisting of the pyrrolidino, morpholino, thiomorpholino, piperidino, hexamethyleneimino, piperazino, 4-methyl-piperazino, 4-(.beta.-hydroxyethyl)piperzaino, 4-phenylpiperazino and 4-(p-chlorophenyl)piperazino groups, and addition salts thereof.These new derivatives are useful as pharmaceuticals. They are obtained by deacetylation of the corresponding acetylated products.
    Type: Grant
    Filed: November 14, 1988
    Date of Patent: December 25, 1990
    Assignee: Laboratoire L. Lafon
    Inventor: Louis Lafon
  • Patent number: 4948813
    Abstract: The invention relates to benzylketone phospholipase A.sub.2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A.sub.2 -mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylketone phospholipase A.sub.2 inhibitor. These compounds are also intermediates in the synthesis of other PLA.sub.2 inhibitors.
    Type: Grant
    Filed: July 28, 1989
    Date of Patent: August 14, 1990
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Wendell W. Wilkerson