Polycyclo Ring System In A Substituent E Patents (Class 564/222)
  • Patent number: 8729131
    Abstract: The present invention relates to an agomelatine hydrochloride hydrate of formula I, preparation and use thereof, and to pharmaceutical composition containing it. The agomelatine hydrohalide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps. wherein X is Cl.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: May 20, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Hanbin Shan, Zhedong Yuan, Xueyan Zhu, Peng Zhang, Hongjuan Pan, Xiong Yu
  • Patent number: 8729306
    Abstract: The present invention provides an alternative synthesis of N-substituted aminotetralines which synthesis comprises catalytic asymmetric hydrogenation of compounds of general formula (A).
    Type: Grant
    Filed: February 3, 2011
    Date of Patent: May 20, 2014
    Assignee: UCB Pharma GmbH
    Inventors: David Vasselin, Nicolas Carly, Celal Ates
  • Patent number: 8729132
    Abstract: The present invention relates to an agomelatine hydrobromide hydrate of formula I wherein X is Br, preparation and use thereof, and to pharmaceutical compositions containing it. The agomelatine hydrobromide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: May 20, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Hanbin Shan, Zhedong Yuan, Xueyan Zhu, Peng Zhang, Hongjuan Pan, Xiong Yu
  • Patent number: 8716421
    Abstract: This invention discloses and claims a series of polycyclic monomers and polymers useful in the production of optical waveguides. The polymers of the invention comprise one or more repeating units represented by the formula (IV): Wherein m, X, R1 and R2 are as defined herein. The films formed from the polymers of this invention exhibit significant changes in refractive index (greater than or equal to 0.5%) after exposure to suitable actinic or thermal energy thereby having superior optical transmission performance, which is of importance for modern optical applications such as wave guiding and optical data storage.
    Type: Grant
    Filed: May 23, 2013
    Date of Patent: May 6, 2014
    Assignees: Promerus, LLC, Sumitomo Bakelite Co., Ltd
    Inventors: Kazuyoshi Fujita, Nanae Kawate, Mari Ueda, Larry F Rhodes
  • Publication number: 20140057990
    Abstract: This invention provides a convenient method for converting oximes into enamides. The process does not require the use of metallic reagents. Accordingly, it produces the desired compounds without the concomitant production of a large volume of metallic waste. The enamides are useful precursors to amides and amines. The invention provides a process to convert a prochiral enamide into the corresponding chiral amide. In an exemplary process, a chiral amino center is introduced during hydrogenation through the use of a chiral hydrogenation catalyst. In selected embodiments, the invention provides methods of preparing amides and amines that include the 1,2,3,4-tetrahydro-N-alkyl-1-naphthalenamine or 1,2,3,4-tetrahydro-1-naphthalenamine substructure.
    Type: Application
    Filed: August 1, 2013
    Publication date: February 27, 2014
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Hang Zhao, Stefan G. Koenig, Charles P. Vandenbossche, Surendra Singh, Harold Scott Wilkinson, Roger P. Bakale
  • Publication number: 20140012015
    Abstract: The present invention provides a process for preparing a bicyclic amine derivative of the formula (Ia) or (Ib), comprising the rhodium-catalyzed asymmetric hydrogenation of an enamine of the formula (II), in the presence of a chiral ligand, wherein the chiral ligand is a chiral phosphine ligand.
    Type: Application
    Filed: July 2, 2013
    Publication date: January 9, 2014
    Inventors: Yi-Yin Ku, Steven Hannick, Ashok K. Gupta
  • Publication number: 20130274240
    Abstract: The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.
    Type: Application
    Filed: November 5, 2012
    Publication date: October 17, 2013
    Inventor: JAPAN TOBACCO INC.
  • Publication number: 20130109757
    Abstract: The invention is directed to method for the preparation of pyrrolines of the general formula (I) by catalytic hydration of a nitroketone of the general formula (II) employing a transition metal catalyst and gaseous hydrogen at an elevated pressure in a solvent, optionally in the presence of at least one additive selected among Lewis acids, Brønstedt acids, organic sulfur-containing compounds, organic or inorganic bases, and water scavengers, wherein in formulae (I) and (II) B1, B2, B3, B4, X, R, and T are as defined in the specification, and to a nitroketone of formula (II) to be used as intermediate in the process according to the invention and as pesticidal agent.
    Type: Application
    Filed: April 11, 2011
    Publication date: May 2, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Wahed Ahmed Moradi, Thomas Norbert Müller, Tetsuya Murata, Mamoru Hatazawa, Peter Bruechner, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
  • Publication number: 20130089612
    Abstract: The subject invention provides R(+)-N-formyl-propargyl-aminoindan and a composition containing N-propargyl-1(R)-aminoindan or a pharmaceutically acceptable salt thereof, and a compound of R(+)-N-formyl-propargyl-aminoindan.
    Type: Application
    Filed: October 9, 2012
    Publication date: April 11, 2013
    Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventor: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
  • Publication number: 20120323040
    Abstract: Methods for producing a compound of formula k1 or k2 by reducing a dihydronapthalene amide compound of formula i with hydrogen gas in the presence of a ruthenium catalyst of formula j1 or j2 Ru(Z)2(L)??j1; Ru(E)(E?)(L)(D)??j2; wherein m, n, Ar, Y, R1E, E?, D, Z and L are as defined herein.
    Type: Application
    Filed: January 26, 2012
    Publication date: December 20, 2012
    Inventors: Kieran Durkin, Lawrence Emerson Fisher, Arthur MEILI, Michaelangelo Scalone, Xianqing Shi, Justin Vitale
  • Publication number: 20120302790
    Abstract: The present invention provides an alternative synthesis of N-substituted aminotetralines which synthesis comprises catalytic asymmetric hydrogenation of compounds of general formula (A).
    Type: Application
    Filed: February 3, 2011
    Publication date: November 29, 2012
    Applicant: UCB PHARMA, S.A.
    Inventors: David Vasselin, Nicolas Carly, Celal Ates
  • Publication number: 20120225912
    Abstract: The invention relates to colchicine derivatives, methods and uses thereof for treatment of cancer.
    Type: Application
    Filed: July 30, 2010
    Publication date: September 6, 2012
    Inventors: Jack Tuszynski, Jonathan Y. Mane, John Torin Huzil, Boguslaw Tomanek, Dorota Bartusik
  • Publication number: 20120183468
    Abstract: Provided herein are water-soluble, functionalized fullerenes, and processes for producing water-soluble, functionalized fullerenes. The process includes sulfonating a fullerene in an acidic solution comprising sulfuric acid to produce a sulfonated fullerene, isolating the sulfonated fullerene from the acidic solution without neutralizing the acidic solution, reacting the sulfonated fullerene with hydrogen peroxide to form a reaction product, and isolating a polyhydroxylated fullerene from the reaction product produced from reacting the sulfonated fullerene with the hydrogen peroxide. The process of producing water-soluble fullerenes further includes functionalizing a polyhydroxylated fullerene with one or more pendant functional groups by reacting the polyhydroxylated fullerene with one or more functional group precursors.
    Type: Application
    Filed: January 17, 2012
    Publication date: July 19, 2012
    Applicant: MARELLE, LLC
    Inventors: Mark Farrell, Michelle Guaragno
  • Patent number: 8138375
    Abstract: The invention relates to a method for producing 1-formamido-3,5-dimethyladamantane in only two reaction steps by direct formamide formation of 1,3-dimethyladamantane, the 1,3-dimethyladamantane being reacted with formamide in concentrated acids.
    Type: Grant
    Filed: February 20, 2007
    Date of Patent: March 20, 2012
    Assignee: MERZ PHARMA GmbH & Co. KGaA
    Inventors: Peter R. Schreiner, Andrey A. Fokin, Lukas Wanka, Derek M. Wolfe
  • Publication number: 20120040930
    Abstract: The invention concerns a triterpene alkaloid of general formula (I). The invention also concerns a method for making same and use thereof as medicine.
    Type: Application
    Filed: January 13, 2006
    Publication date: February 16, 2012
    Inventors: Catherine Guillou, Jean-Yves Lallemand, Thibault Sauvaítre, Jordi Molgo, Denyse Herlem, Daniel Guenard, Françoise Khuong-Huu
  • Publication number: 20110263900
    Abstract: The present invention pertains to process for the amidation of a substituted 1-bromo-adamantane comprising a step (0) of reacting a substituted adamantane with an excess of bromine to obtain a 1-bromo-adamantane and a step (i) of reacting said substituted 1-bromo-adamantane with an amide, wherein the substituted 1-bromo-adamantane is used in the form of a mixture comprising bromine as obtained in step (0), wherein in step (0) a bromine:substituted adamantane molar ratio of from [2.5:1] to less than [5:1] is employed.
    Type: Application
    Filed: August 7, 2009
    Publication date: October 27, 2011
    Applicant: MERZ PHARMA GmbH & CO. KGaA
    Inventors: Markus-Rene Gold, Herbert Koller, Michael Pyerin
  • Publication number: 20110178180
    Abstract: Disclosed herein are deuterium-enriched colchicine, thiocolchicine, and derivatives thereof. The deuterium-enriched compounds are useful as, an antiproliferative agent, a muscle relaxant, an anti-inflammatory agent, or an anti-gout agent.
    Type: Application
    Filed: January 17, 2011
    Publication date: July 21, 2011
    Inventors: Kurt Nielsen, Rajesh Manchanda
  • Publication number: 20110130431
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: February 8, 2011
    Publication date: June 2, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Angela BERRY, Pier Francesco CIRILLO, Eugene Richard HICKEY, Doris RIETHER, David THOMSON, Renee M. ZINDELL, Nigel BLUMIRE, Chandana CHOWDHURY, Monika ERMANN, James Edward JENKINS, Innocent MUSHI, Christopher Francis PALMER, Malcolm TAYLOR
  • Patent number: 7935731
    Abstract: Methods for concomitant administration of colchicine together with one or more macrolide antibiotics, e.g., clarithromycin, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits.
    Type: Grant
    Filed: May 25, 2010
    Date of Patent: May 3, 2011
    Assignee: Mutual Pharmaceutical Company, Inc.
    Inventor: Matthew W. Davis
  • Publication number: 20110003959
    Abstract: The invention relates to a coordination complex system comprising a ligand having the formula: R1—SO2—NH—P (XR2)2 (1a); or R1—SO2—N?PH (XR2)2 (1b); or R1—SO(OH)?N—P(XR2)2 (1c); wherein X is independently O, S, NH, or a bond; R1 and R2 are independently selected from hydrogen and substituted or unsubstituted alkyl or aryl; wherein at least one equivalent of the ligand is complexed to an equivalent of a metal selected from a transition metal and lanthanide. The invention also relates to the use of said coordination complexes as catalysts in the hydroformylation, hydrogenation, transfer hydrogenation, hydrocyanation, polymerization, isomerization, carbonylation, cross-coupling, metathesis, CH activation, allylic substitution, aldol condensation, or Michael addition.
    Type: Application
    Filed: November 19, 2008
    Publication date: January 6, 2011
    Inventors: Joost Nikolaas Hendrik Reek, Frederic William Patureau, Mark Kuil, Albertus Jacobus Sandee, Jurjen Meeuwissen
  • Publication number: 20100210524
    Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, wherein W, X, Y, Z, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15 and R16 are as defined in the specification. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
    Type: Application
    Filed: July 21, 2008
    Publication date: August 19, 2010
    Inventors: Theresa Apelqvist, Joakim Löfstedt, Thomas Norin, Mattias Wennerstål, Xiongyu Wu, Lars Hagberg
  • Publication number: 20100183712
    Abstract: The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description.
    Type: Application
    Filed: March 29, 2010
    Publication date: July 22, 2010
    Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Hartmut STROBEL, Paulus WOHLFART, Alena SAFAROVA, Armin WALSER, Teri SUZUKI, Karl SCHÖNAFINGER, Ramalinga M. DHARANIPRAGADA
  • Publication number: 20090149549
    Abstract: This invention provides a convenient method for converting oximes into enamides. The process does not require the use of metallic reagents. Accordingly, it produces the desired compounds without the concomitant production of a large volume of metallic waste. The enamides are useful precursors to amides and amines. The invention provides a process to convert a prochiral enamide into the corresponding chiral amide. In an exemplary process, a chiral amino center is introduced during hydrogenation through the use of a chiral hydrogenation catalyst. In selected embodiments, the invention provides methods of preparing amides and amines that include the 1,2,3,4-tetrahydro-N-alkyl-1-naphthalenamine or 1,2,3,4-tetrahydro-1-naphthalenamine substructure.
    Type: Application
    Filed: March 30, 2007
    Publication date: June 11, 2009
    Inventors: Hang Zhao, Stefan G. Koenig, Charles P. Vandenbossche, Surendra Singh, H. Scott Wilkinson, Roger P. Bakale
  • Patent number: 7262326
    Abstract: A process for preparing indanylamine and aminotetralin derivatives from indanone or tetralone oximes by acylating the oximes with an organic anhydride, followed by catalytic hydrogenation in the presence of an organic anhydride with subsequent hydrolysis is described. The process is commercially feasible providing indanylamine and aminotetralin derivatives in high yield that are useful as intermediates in the production of therapeutically active compounds. Also described are novel intermediates, 1-indanone O-acetyl oximes and 1-tetralone O-acetyl oximes.
    Type: Grant
    Filed: September 7, 2005
    Date of Patent: August 28, 2007
    Assignee: Teva Pharmaceuticals Industries Ltd.
    Inventors: Sylvie Blanchet, Bertrand Blandine, Alain Burgos, Yvon Derrien, Marie-Laure Moreau
  • Patent number: 7157604
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
    Type: Grant
    Filed: August 9, 2002
    Date of Patent: January 2, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Dongfang Meng, Dann LeRoy Parker, Jr., Robert R. Wilkening, Ronald W. Ratcliffe
  • Patent number: 6737547
    Abstract: The present invention provides novel aminoindenes having the structure: wherein n is 1 or 2, R1 is hydrogen, linear or branched chain C1-C8 alkyl or linear or branched chain C1-C8 alkoxy and R2 is hydrogen or a halogen. Such compounds may be used to treat neurodegenerative conditions such as Alzheimer's disease, head trauma, stroke, hypoxia, anoxia, epilepsy, convulsions, seizures.
    Type: Grant
    Filed: September 15, 1999
    Date of Patent: May 18, 2004
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Benjamin Sklarz, Sasson Cohen, Tzipora Speiser, Rachel Nachman
  • Patent number: 6683220
    Abstract: A process for producing substantially optically pure sertraline utilizes chromatographic separation on a solid stationary chiral phase of spherical clay particles having an interlayer containing an optically pure metal-organic complex, and a liquid mobile phase preferably containing at least methyl acetate. The liquid mobile phase is preferably free of acetonitrile. The process is operable at temperatures above 40° C.
    Type: Grant
    Filed: September 18, 2002
    Date of Patent: January 27, 2004
    Assignee: Pfizer, Inc.
    Inventors: Laurent Berger, Raphael Duval, Philippe Taillasson, Ingo Weber, Alexander Wick
  • Patent number: 6649796
    Abstract: The invention provides a process for the preparation of diphenylmethylthioacetamide (I) as described in Scheme 4 comprising reacting of the isothiouronium salt or its corresponding base of the formula IV with an acetamide of the formula XCH2CONH2, wherein X represents a halogen, M represents an alkali metal and A represents an anion, in a protic medium at a temperature of less than 100° C.
    Type: Grant
    Filed: April 2, 2002
    Date of Patent: November 18, 2003
    Assignee: Chemagis, Ltd.
    Inventors: Vladimir Naddaka, Naim Menashe, Jael Lexner, Shadi Saeed, Joseph Kaspi, Ori Lerman
  • Patent number: 6635783
    Abstract: Bicyclic amino alcohols, whose amino group and hydroxy group are bonded in positions 1,3 adjacent to the bridge, for example are valuable ligands for metal complexes of the d-8 metals of the periodic table of elements. The metal complexes in question are catalysts or catalyst precursors for the asymmetric hydrogenation or asymmetric transfer hydrogenation with hydrogen donors of prochiral organic compounds with carbon double bonds or carbon/hetero atom double bonds, for example ketones and imines.
    Type: Grant
    Filed: March 6, 2001
    Date of Patent: October 21, 2003
    Assignee: Solvias AG
    Inventor: Peter Herold
  • Patent number: 6602903
    Abstract: The invention relates to compounds of formula (I): and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.
    Type: Grant
    Filed: August 28, 2001
    Date of Patent: August 5, 2003
    Assignee: Les Laboratories Servier
    Inventors: Gérald Guillaumet, Marie-Claude Viaud, Ahmed Mamai, Isabelle Charton, Pierre Renard, Caroline Bennejean, Béatrice Guardiola, Philippe Daubos
  • Patent number: 6313175
    Abstract: Novel meta substituted arylalkylamine compounds are disclosed. These compounds can be administered as small molecule drugs to treat diseases or conditions associated with insufficient serotonin mediated nerve transmission (e.g., depression and obesity).
    Type: Grant
    Filed: August 13, 1999
    Date of Patent: November 6, 2001
    Assignee: Biostream, Inc.
    Inventors: David R. Elmaleh, Alan J. Fischman
  • Patent number: 6297399
    Abstract: Indane compounds of general formulas (7) and (8) and their pharmaceutical use particularly to achieve smooth muscle relaxing activity and/or mast cell stabilizing activity and/or anti-inflammatory activity as described, wherein in formula (7) R2 to R13, in formula (8) R1 and R3 and R13 are selected from one or more of the same or different of: H, halo, hydroxy, alkoxy, aryloxy, acetoxy, carboxy, alkyl carbonyl, hydro carbonyl, amino, amido, alkylamino, hydroxylamino, amine oxide groups, azo groups, cyano, hydrazino groups, hydrazide groups, hydrazone groups, imide groups, iminoether groups, ureyl groups, oxime, nitro, nitrate, nitrite, nitroso groups, nitrile, heterocyclic groups containing heretro atoms containing one or more of N, O or S, aralkyl groups, mono and polybenzoid aryl groups, substituted aryl groups, thiol, thioureyl, phenylthiol groups, sulphonic acid groups, sulphoxide groups, sulphone groups, alkyl containing 1 to 10 carbon atoms or cycloalkyl groups containing 3 to 8 carbon atoms which may s
    Type: Grant
    Filed: June 8, 1998
    Date of Patent: October 2, 2001
    Assignee: Venantius Limited
    Inventors: John Walsh, Neil Frankish, Helen Sheridan, William Byrne
  • Patent number: 6262308
    Abstract: The invention relates to a process for preparing cis-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine, or racemic sertraline, corresponding to formula (I) in salt form, starting with 4-(3,4-dichlorophenyl)tetralone of formula (II) according to which (a) the 4-(3,4-dichlorophenyl)tetralone of formula (II) is reacted with N-methylformamide in the presence of formic acid, (b) the reaction medium obtained according to (a) is treated with a base, and (c) the racemic sertraline salt is separated out by selective crystallization with an acid. The invention also relates to N-methylformamide-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine and to its use to obtain racemic sertraline.
    Type: Grant
    Filed: March 29, 1999
    Date of Patent: July 17, 2001
    Assignee: Catalys
    Inventor: Patrick Bigot
  • Patent number: 6140372
    Abstract: The invention relates to derivatives of general formula I ##STR1## as defined in the description. The invention also relates to a process for their preparation and to their therapeutic use, in particular for the treatment of complaints associated with melatonin disorders, and pharmaceutical and cosmetic compositions comprising them.
    Type: Grant
    Filed: April 16, 1999
    Date of Patent: October 31, 2000
    Assignee: Cemaf and Laboratories Besins Isovesco S.A.
    Inventors: Jean-Bernard Fourtillan, Marianne Fourtillan, Jean-Claude Jacquesy, Marie-Paule Jouannetaud, Bruno Violeau, Omar Karam
  • Patent number: 6028112
    Abstract: There is provided novel spirocyclopropyl fluorene derivatives having the general Formula I ##STR1## wherein R, R.sup.1 and X are as defined herein which are useful as melatonergic agents.
    Type: Grant
    Filed: July 31, 1998
    Date of Patent: February 22, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Karen L. Leboulluec, Katherine S. Takaki
  • Patent number: 5973204
    Abstract: The present invention relates to 3-demethyl-thiocolchicine derivatives of general formula (I) ##STR1## in which R can be ##STR2## to a process for the preparation thereof, to pharmaceutical compositions containing them and to the use thereof for the preparation of medicaments with muscle relaxant and antiinflammatory activities.
    Type: Grant
    Filed: April 7, 1998
    Date of Patent: October 26, 1999
    Assignee: Indena S.p.A.
    Inventor: Ezio Bombardelli
  • Patent number: 5959146
    Abstract: Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.
    Type: Grant
    Filed: December 13, 1996
    Date of Patent: September 28, 1999
    Assignee: Hoechst Marion Roussel
    Inventors: Francis Brion, Bernadette Chappert, Christian Diolez, Christian Marie, Alain Mazurie, Michel Middendorp, Didier Pronine, Edmond Toromanoff
  • Patent number: 5849945
    Abstract: The present invention pertains to a process for the preparation of Compound (4) through the below-described reaction route: ##STR1## wherein R.sup.1 and R.sup.2 each represents H, halogen, OH or C.sub.1-6 alkyl group; X and Y each represents a protected amino group and n stands for 0 to 4. According to the above process, an aminotetralone derivative which is an intermediate useful for an industrial preparation of a camptothecin derivative can be obtained in a convenient manner and in a high yield.
    Type: Grant
    Filed: August 21, 1997
    Date of Patent: December 15, 1998
    Assignees: Daiichi Pharmaceutical Co., Ltd., Kabushikikaisha Yakult Honsha
    Inventors: Shinji Kamihara, Kazuaki Kanai, Shigeru Noguchi
  • Patent number: 5834521
    Abstract: Tetracyclic compounds having the following structure are described: ##STR1## wherein R.sub.1 -R.sub.10 are as defined. The tetracyclic compounds are capable of potent effects on steroid sensitive tissues and have demonstrated increased uterine weight, antiovulatory effects and potent steroid receptor binding. The compounds have therapeutic utility in reproductive applications such as fertility control, labor induction, ovulation induction and spermatogenesis. Methods for preparing the tetracyclic compounds from substituted indanones are also described.
    Type: Grant
    Filed: August 5, 1996
    Date of Patent: November 10, 1998
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: John H. Dodd, Lisa A. Dixon, James L. Bullington, Charles F. Schwender
  • Patent number: 5817874
    Abstract: The present invention is a process of converting a hydroxy aromatic into a 2-hydroxy-N-arylacetamide, comprising:(1) treating a reaction mixture comprising a salt of a hydroxy aromatic with an alkylating agent; and(2) treating the reaction mixture with a Smiles solvent system and raising the temperature of the reaction mixture.
    Type: Grant
    Filed: March 18, 1997
    Date of Patent: October 6, 1998
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Norton P. Peet, John J. Weidner
  • Patent number: 5739374
    Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: February 14, 1997
    Date of Patent: April 14, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5731352
    Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which A, R.sub.1, R'.sub.1, R.sub.2, R.sub.3 and n are as defined in the description, and medicinal product containing the same useful for treating a mammal afflicted with a disorder of the melatoninergic system.
    Type: Grant
    Filed: May 30, 1996
    Date of Patent: March 24, 1998
    Assignee: Adir Et Compagnie
    Inventors: Daniel Lesieur, Veronique Leclerc, Patrick Depreux, Philippe Delagrange, Pierre Renard
  • Patent number: 5663442
    Abstract: The invention relates to a process for the preparation of compounds of the formula ##STR1## characterized in that the radical X in sulphones of the formulaX--(CH.sub.2 --CH.sub.2 --O).sub.m --(CH.sub.2).sub.n --SO.sub.2 --CH.sub.2 --CH.sub.2 OH (2)is replaced by ##STR2## or a compound of the formula ##STR3## is added to the sulphone of the formulaCH.sub.2 =CH--SO.sub.2 --CH.sub.2 --CH.sub.2 --OH (3),the substituents having the meanings given in the description.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: September 2, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Harms, Udo-Winfried Hendricks, Karl-Josef Herd, Klaus Kunde
  • Patent number: 5663337
    Abstract: The present invention relates to benzoquinazoline thymidylate synthase inhibitors, processes for preparing them and pharmaceutical formulations containing them.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: September 2, 1997
    Assignee: Glaxo Wellcome Inc.
    Inventors: William Pendergast, Scott Howard Dickerson
  • Patent number: 5656619
    Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 12, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5646188
    Abstract: A compound of general formula I ##STR1## wherein n is 1 or 2; R.sub.1 and R.sub.2 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy or halogeno;R.sub.5 is hydrogen, substituted or unsubstituted C.sub.1-4 alkyl, amino or NR.sub.6 R.sub.7 ;R.sub.3, R.sub.4, R.sub.6 and R.sub.7 are each independently hydrogen or (CH.sub.2).sub.m --[NH(CH.sub.2).sub.x ].sub.y --NHR.sub.11 wherein m is from 0-5, y is from 0-5 and each x is independently from 1-5 and R.sub.11 is hydrogen or C(NH)NH.sub.2 ;provided that when R.sub.3 and R.sub.4 are both hydrogen, R.sub.5 is amino or NR.sub.6 R.sub.7 ; pharmaceutically acceptable salts and optically active isomers thereof.
    Type: Grant
    Filed: July 5, 1995
    Date of Patent: July 8, 1997
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Gad Gilad, Varda Gilad, Jeffrey Sterling, Yaacov Herzig, David Lerner, Alex Veinberg, Isaac Milman, Nina Finkelstein
  • Patent number: 5599985
    Abstract: A two-step process for the conversion of a trans-1-amino-2-hydroxycycloalkane stereoselectively to a cis-1-amino-2-hydroxycycloalkane is disclosed. The novel step, a one-step hydrolysis with formal inversion, can be used to convert an amide of a trans-1-amino-2-hydroxycycloalkane to a cis-1-amino-2-hydroxycycloalkane. Methods for obtaining the trans-1-amino-2-hydroxycycloalkanes and their amides from alkenes are also disclosed. Novel, optically active 1-amido-2-indanols and 1-amino-2-alkanols are also disclosed.
    Type: Grant
    Filed: July 21, 1994
    Date of Patent: February 4, 1997
    Assignee: Sepracor, Inc.
    Inventors: Yun Gao, Yaping Hong, Xiaoyi Nie, Roger P. Bakale, Richard R. Feinberg, Charles M. Zepp
  • Patent number: 5530002
    Abstract: Compounds of formula: ##STR1## in which X represents a hydrogen atom, a C.sub.1 -C.sub.3 alkoxy group or a cyclopropylmethoxy group and Y represents a hydrogen atom or a methoxy group, are useful in the therapy of conditions.
    Type: Grant
    Filed: February 9, 1995
    Date of Patent: June 25, 1996
    Assignee: Synthelabo
    Inventors: Phillip Manoury, Daniel Obitz, Michel Peynot, Mireille Sevrin, Pascal George
  • Patent number: 5470977
    Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.
    Type: Grant
    Filed: March 14, 1995
    Date of Patent: November 28, 1995
    Assignee: Eli Lilly and Company
    Inventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus
  • Patent number: 5463126
    Abstract: The invention provides the substantially geometrically pure cis-stereoisomeric form of a compound of formula (I) and the substantially geometrically and optically pure cis-stereoisomeric form of a compound of formula (II): ##STR1## wherein R.sup.1 is H or C.sub.1 -C.sub.4 alkyl, together with processes for their preparation. The compounds are intermediates for the preparation of the antidepressant agent known as sertraline.
    Type: Grant
    Filed: January 10, 1994
    Date of Patent: October 31, 1995
    Assignee: Pfizer Inc.
    Inventor: Michael T. Williams