Halogen Bonded Directly To The Aryl Ring Or Ring System Patents (Class 564/345)
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Publication number: 20140170216Abstract: Polymorphous and amorphous forms of bupropion hydrobromide are described.Type: ApplicationFiled: September 4, 2013Publication date: June 19, 2014Applicant: VALEANT INTERNATIONAL BERMUDAInventors: Stefano Turchetta, Maurizio Zenoni
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Patent number: 8735454Abstract: The present application describes deuterium-enriched bupropion, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: GrantFiled: August 22, 2013Date of Patent: May 27, 2014Assignee: DeuteRx, LLCInventor: Anthony W. Czarnik
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Publication number: 20140018436Abstract: The present application describes deuterium-enriched bupropion, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2013Publication date: January 16, 2014Applicant: DEUTERX, LLCInventor: Anthony W. Czarnik
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Patent number: 8604085Abstract: Polymorphous and amorphous forms of bupropion hydrobromide are described.Type: GrantFiled: October 17, 2012Date of Patent: December 10, 2013Assignee: Valeant International BermudaInventors: Stefano Turchetta, Maurizio Zenoni
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Patent number: 8524780Abstract: The present application describes deuterium-enriched bupropion, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: GrantFiled: May 19, 2010Date of Patent: September 3, 2013Assignee: DeuteRx, LLCInventor: Anthony W. Czarnik
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Patent number: 8450376Abstract: 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: GrantFiled: June 15, 2009Date of Patent: May 28, 2013Assignee: Glenmark Generics Ltd.Inventors: Shankar Sanganabhatla, Vijay Soni, Mubeen Ahmed Khan, Nandlal Agarwal, Hemanth Kamble, Sharad Gore
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Publication number: 20130059005Abstract: Polymorphous and amorphous forms of bupropion hydrobromide are described.Type: ApplicationFiled: October 17, 2012Publication date: March 7, 2013Inventors: Stefano TURCHETTA, Maurizio ZENONI
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Patent number: 8349900Abstract: Polymorphous and amorphous forms of bupropion hydrobromide are described.Type: GrantFiled: August 6, 2009Date of Patent: January 8, 2013Assignee: Valeant International BermudaInventors: Stefano Turchetta, Maurizio Zenoni
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Publication number: 20120071560Abstract: 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: ApplicationFiled: October 12, 2011Publication date: March 22, 2012Inventors: Frank Ivy Carroll, Bruce Edward Blough, Philip Abraham
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Publication number: 20110245493Abstract: 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: ApplicationFiled: April 1, 2011Publication date: October 6, 2011Applicant: ALEXZA PHARMACEUTICALS, INC.Inventors: Joshua D. RABINOWITZ, Alejandro C. Zaffaroni
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Publication number: 20110207965Abstract: 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: ApplicationFiled: October 16, 2009Publication date: August 25, 2011Applicant: ZACH SYSTEM S.P.A.Inventors: Nicola Catozzi, Johnny Foletto, Massimiliano Forcato, Roberto Giovanetti, Giorgio Soriato, Massimo Verzini
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Publication number: 20110130463Abstract: The present application describes deuterium-enriched bupropion, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: May 19, 2010Publication date: June 2, 2011Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20110105619Abstract: 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: ApplicationFiled: June 15, 2009Publication date: May 5, 2011Applicant: Glenmark Generics Ltd.Inventors: Shankar Sanganabhatla, Vijay Soni, Mubeen Ahmed Khan, Nandlal Agarwal, Hemanth Kamble, Sharad Gore
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Patent number: 7884136Abstract: 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: GrantFiled: June 27, 2006Date of Patent: February 8, 2011Assignee: Biovail Laboratories International S.R.L.Inventors: Werner Oberegger, Fang Zhou, Paul Maes, Stefano Turchetta, Graham Jackson, Pietro Massardo, Mohammad Ashty Saleh
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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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Patent number: 7737288Abstract: 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: GrantFiled: May 26, 2006Date of Patent: June 15, 2010Assignees: Shanghai Institute of Materia Medica Chinese Academy of Sciences, Sichuan UniversityInventors: Mingwei Wang, Caihong Zhou, Xin Hui, Haoran Su, Jie Gao, Yong Deng, Dacheng Yang
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Patent number: 7723385Abstract: 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: GrantFiled: February 25, 2009Date of Patent: May 25, 2010Assignee: GlaxoSmithKline LLCInventors: Philip Stewart Turnbull, Rodolfo Cadilla, David John Cowan, Andrew Lamont Larkin, Istvan Kaldor, Eugene Lee Stewart
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Publication number: 20100075950Abstract: 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: ApplicationFiled: August 19, 2009Publication date: March 25, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Manouchehr M. Shahbaz, Sepehr Sarshar
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Publication number: 20100068270Abstract: Polymorphous and amorphous forms of bupropion hydrobromide are described.Type: ApplicationFiled: August 6, 2009Publication date: March 18, 2010Applicant: BIOVAIL LABORATORIES INTERNATIONAL S.R.L.Inventors: Stefano TURCHETTA, Maurizio Zenoni
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Patent number: 7674936Abstract: 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: GrantFiled: May 11, 2007Date of Patent: March 9, 2010Assignee: E.I. du Pont De Nemours and CompanyInventors: Kenneth Andrew Hughes, George Philip Lahm, Thomas Paul Selby, Benjamin Kenneth Smith, William Thomas Zimmerman
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Patent number: 7572935Abstract: 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: GrantFiled: June 14, 2007Date of Patent: August 11, 2009Assignee: Biovail Laboratories International S.R.L.Inventors: Werner Oberegger, Paul Maes, Stefano Turchetta, Pietro Massardo, Mohammad Ashty Saleh
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Publication number: 20090187028Abstract: 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: ApplicationFiled: January 22, 2009Publication date: July 23, 2009Inventors: Feng Xu, Mary M. Kim, Yoshinori Kohmura, Tricia Sladicka, Jonathan D. Rosen, Michael J. Zacuto
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Patent number: 7553992Abstract: 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: GrantFiled: May 31, 2007Date of Patent: June 30, 2009Assignee: Biovail Laboratories International S.R.L.Inventors: Werner Oberegger, Paul Maes, Stefano Turchetta, Pietro Massardo, Mohammad Ashty Saleh
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Patent number: 7514470Abstract: 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: GrantFiled: March 3, 2005Date of Patent: April 7, 2009Assignee: SmithKline Beecham CorporationInventors: Philip Stewart Turnbull, Rodolfo Cadilla, David John Cowan, Andrew Lamont Larkin, Istvan Kaldor, Eugene Lee Stewart
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Publication number: 20090076161Abstract: The present application describes deuterium-enriched bupropion, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 21, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20080293808Abstract: 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: ApplicationFiled: May 26, 2006Publication date: November 27, 2008Inventors: Mingwei Wang, Caihong Zhou, Xin Hui, Haoran Su, Jie Gao, Yong Deng, Dacheng Yang
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Publication number: 20080233606Abstract: Provided herein are assays for detecting enzyme activity using Raman Spectroscopy.Type: ApplicationFiled: April 22, 2008Publication date: September 25, 2008Inventors: Mustapha Haddach, Gregory S. Naeve
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Patent number: 7091382Abstract: 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: GrantFiled: May 7, 2004Date of Patent: August 15, 2006Assignee: Clariant Life Science Molecules (Italia) S.p.A.Inventors: Aldo Banfi, Alfredo Mancini
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Patent number: 6765022Abstract: 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: GrantFiled: December 2, 2002Date of Patent: July 20, 2004Assignee: Warner-Lambert CompanyInventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Patent number: 6653508Abstract: 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: GrantFiled: January 16, 2002Date of Patent: November 25, 2003Assignee: Gruenenthal GmbHInventors: Michael Sattlegger, Helmut Buschmann, Babette-Yvonne Koegel
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Publication number: 20030040483Abstract: Compounds of peptide mimetic nature having the general formula I 1Type: ApplicationFiled: March 23, 2000Publication date: February 27, 2003Inventors: Thomas Kruse Hansen, Bernd Peschke, Jesper Lau, Behrend Friedrich Lundt, Michael Ankersen, Brett Watson, Kjeld Madsen
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Patent number: 6482987Abstract: 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: GrantFiled: April 2, 2001Date of Patent: November 19, 2002Assignee: Clonmel Healthcare, Ltd.Inventors: Prakash Shriram Kulkarni, Bharat Bhogilal Shah, Amitava Maitra, Joseph Michael DeVito
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Patent number: 6462237Abstract: 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: GrantFiled: June 14, 2001Date of Patent: October 8, 2002Assignee: USV LimitedInventors: Suresh Kumar Gidwani, Purushottam Singnurkar, Prashant Kumar Tewari
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Patent number: 6350767Abstract: The present invention relates to compounds, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.Type: GrantFiled: November 19, 1999Date of Patent: February 26, 2002Assignee: Novo Nordisk A/SInventors: Jesper Lau, Bernd Peschke, Thomas Kruse Hansen, Nils Langeland Johansen, Michael Ankersen
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Patent number: 6235791Abstract: 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: GrantFiled: April 12, 1999Date of Patent: May 22, 2001Assignee: Sanofi-SynthelaboInventors: Jean Claude Breliere, Pascual Ferrara, Christine Lebouteiller, Raymond Paul, Jorge Rosenfeld, Didier Van Broeck
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Patent number: 6087346Abstract: 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: GrantFiled: February 21, 1996Date of Patent: July 11, 2000Assignees: Cambridge Neuroscience, Inc., Virginia Commonwealth UniversityInventors: Richard A. Glennon, James B. Fischer
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Patent number: 6057371Abstract: 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: GrantFiled: June 10, 1992Date of Patent: May 2, 2000Assignee: Virginia Commonwealth UniversityInventor: Richard A. Glennon
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Patent number: 5977178Abstract: 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: GrantFiled: December 18, 1996Date of Patent: November 2, 1999Assignee: Novo Nordisk A/SInventors: Thomas Kruse Hansen, Bernd Peschke, Jesper Lau, Behrend Friedrich Lundt, Michael Ankersen, Brett Watson, Kjeld Madsen
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Patent number: 5789448Abstract: 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: GrantFiled: June 25, 1996Date of Patent: August 4, 1998Assignee: Mitsubishi Chemical CorporationInventors: Yasunori Kitano, Haruki Inokawa, Hisao Takayanagi, Tamaki Yano, Hiroe Umeki, Hiroto Hara
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Patent number: 5780505Abstract: 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: GrantFiled: July 7, 1997Date of Patent: July 14, 1998Assignee: American Home Products CorporationInventors: Madelene M. Antane, David R. Herbst, Geraldine R. McFarlane, Eric G. Gundersen, Bradford H. Hirth, Dominick A. Quagliato, Russell F. Graceffa, John A. Butera
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Patent number: 5674909Abstract: 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: GrantFiled: June 6, 1995Date of Patent: October 7, 1997Assignee: Zambon GroupInventors: Stefania Montanari, Paolo Cavalleri, Cristina Fraire, Gian Carlo Grancini, Mauro Napoletano, Francesco Santangelo
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Patent number: 5561135Abstract: 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: GrantFiled: April 21, 1995Date of Patent: October 1, 1996Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet, Santiago Gubert, Jos e Ortiz, Aurelio Sacrist an, Josep M. Castell o
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Patent number: 5502233Type: GrantFiled: January 23, 1995Date of Patent: March 26, 1996Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Heinz-Wilhelm Dehne, Stefan Dutzmann, Christoph Erdelen
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Patent number: 5407961Abstract: 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: GrantFiled: May 12, 1994Date of Patent: April 18, 1995Assignee: 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
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Patent number: 5037980Abstract: 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: GrantFiled: April 18, 1988Date of Patent: August 6, 1991Assignee: American Cyanamid CompanyInventors: John P. Dusza, Jay D. Albright
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Patent number: 5036107Abstract: 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: GrantFiled: November 16, 1989Date of Patent: July 30, 1991Assignee: Marion Merrell Dow Inc.Inventors: Waclaw J. Rzeszotarski, Maria E. Guzewska, Daniel W. McPherson, Ciro J. Spagnuolo, Kenneth J. Natalie, Jr.
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Patent number: 4996318Abstract: 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: GrantFiled: September 19, 1989Date of Patent: February 26, 1991Assignee: The Upjohn CompanyInventors: Martin Gall, Robert I. Higuchi
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Patent number: 4981990Abstract: 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: GrantFiled: December 22, 1988Date of Patent: January 1, 1991Assignee: Ciba-Geigy CorporationInventor: Pierre Martin
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Patent number: 4980377Abstract: 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: GrantFiled: November 14, 1988Date of Patent: December 25, 1990Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4948813Abstract: 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: GrantFiled: July 28, 1989Date of Patent: August 14, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventor: Wendell W. Wilkerson