Polycyclo Ring System Having One Of The Two Rings Which Form The Spiro As One Of The Cyclos Patents (Class 548/411)
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Patent number: 6911463Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.Type: GrantFiled: August 6, 2002Date of Patent: June 28, 2005Assignee: Eli Lilly and CompanyInventors: Daniel Jon Sall, Jolie Anne Bastian, Cynthia Darshini Jesudason, Theo Schotten, Gerd Reuhter, Don Richard Finley, Freddie Craig Stevens, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, John Xiaoqiang He, John Arnold Werner, William George Trankle, Andrew Michael Ratz
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Patent number: 6908926Abstract: Disclosed is a novel class of substituted imidazole compounds, pharmaceutical compositions containing them and uses of these compounds in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, these compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial. These imidazoles compounds have the formula I wherein R1, R2, R3, R4, R5, R6, A, X, Y and Z are as defined in the specification.Type: GrantFiled: April 12, 2000Date of Patent: June 21, 2005Assignee: Novo Nordisk A/SInventors: Florencio Zaragoza Dörwald, Knud Erik Andersen, Tine Krogh Jørgensen, Bernd Peschke, Birgitte Schjellerup Wulff, Ingrid Pettersson, Klaus Rudolf, Dirk Stenkamp, Rudolf Hurnaus, Stephan Georg Müller, Bernd Krist
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Patent number: 6884895Abstract: The invention relates to a process for the preparation of spiro[(4-cyclohexanone)-[3H]indol]-2?[1?H]-one derivatives of the general formula I wherein R1 and R2 independently stand for hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4polyfluoroalkyl, C1-4polyfluoroalkoxy, C3-7cycloalkyloxy, C3-7cycloalkylthio, phenoxy, benzyloxy or nitro group—, characterized by reacting an indolin-2-one derivative of the general formula II wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, selected from 2-tetrahydropyranyl, 1-diethoxy-methylene or C1-4alkoxycarbonylethyl group, coupling the compound of general formula III, thus obtained—wherein R1 and R2 are as defined above and A stands for a protective group, selected from 2-tetrahydropyranyl, 1-diethoxy-methylene or C1-4alkoxycarbonylethyl group—with an acrylic acid C1-4ester, cyclizing the resulting compound of the general formula IV wherein R1, R2 and A are as defined above, R3 stands for C1-4 alkyl grouType: GrantFiled: April 8, 2003Date of Patent: April 26, 2005Assignee: sanofi-aventisInventors: Csaba Gönczi, Éva Csikós, István Hermecz, Gergely Héja, Árpád Illár, Lajos Nagy, Andrea Sántáné Csutor, Attila Simon, Kálmán Simon, Ágota Smelkóné Esek, Tiborné Szomor, Györgyné Szvoboda
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Patent number: 6825220Abstract: The present invention relates to a &bgr;;3 adrenergic receptor agonist of formula I: (1); or a pharmaceutical salt thereof; which is useful for treating Type II diabetes and/or obesity.Type: GrantFiled: April 11, 2003Date of Patent: November 30, 2004Assignee: Eli Lilly and CompanyInventors: Cynthia Darshini Jesudason, Daniel Jon Sall, Freddie Craig Stevens, John Arnold Werner
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Patent number: 6822094Abstract: Spiro compounds of the formula (I), in which at least one of the radicals K1, L, M, N1, R1, R2, R3, R4 is one of the following groups are suitable as charge transport materials, in particular for photovoltaic cells, and as electroluminescence materials.Type: GrantFiled: July 26, 2002Date of Patent: November 23, 2004Assignee: Aventis Research & Technologies, GmbH & Co. KGInventors: Josef Salbeck, Donald Lupo
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Patent number: 6806283Abstract: Spiro[9,10-dihydroanthracene]-9,3′-pyrrolidine (SPAN) and derivatives thereof are provided as selective serotonin receptor antagonists. The compounds are selective, high affinity antagonists of 5-HT2 serotonin receptors. The compounds are useful as antidepressant and antianxiety agents.Type: GrantFiled: May 6, 2003Date of Patent: October 19, 2004Assignee: Virginia Commonwealth UniversityInventors: Richard Glennon, Richard Westkaemper
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Publication number: 20040152755Abstract: The present invention relates to inhibition of viruses, e.g., HIV using oxindoles and compounds related to oxindoles. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.Type: ApplicationFiled: October 21, 2003Publication date: August 5, 2004Applicant: IRM LLC, a Delaware LLCInventors: Yun He, Tao Jiang, Kelli L. Kuhen, David Archer Ellis, Baogen Wu, Tom Yao-Hsiang Wu, Badry Bursulaya
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Patent number: 6638942Abstract: Compounds of general structural formula I are selective NPY Y5 receptor antagonists, useful in the treatment of obesity and the complications associated therewith.Type: GrantFiled: August 26, 2002Date of Patent: October 28, 2003Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Ying-Duo Gao, Douglas J. MacNeil, Lihu Yang, Nancy R. Morin, Takehiro Fukami, Akio Kanatani, Takahiro Fukuroda, Yasuyuki Ishii, Masaki Ihara
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Patent number: 6573386Abstract: The invention relates to a process for the preparation of spiro [(4-cyclohexanone)-[3H]indol]-2′[1′H]-one derivatives of general formula I—wherein R1 and R2 independently stand for hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4polyfluoroalkyl, C1-4polyfluoroalkoxy, C3-7cycloalkyloxy, C3-7cycloalkylthio, phenoxy, benzyloxy or nitro group—, characterized by reacting an indolin-2-one derivative of general formula II—wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, coupling the compound of general formula III, thus obtained—wherein R1 and R2 are as defined above and A stands for a protective group—with acrylic acid C1-4ester; cyclizing the resulting compound of general formula IV—wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, coupling the compound of formula III thus obtained,—wherein R1 and R2 are as defined aboType: GrantFiled: April 17, 2002Date of Patent: June 3, 2003Assignee: Sanofi-SynthelaboInventors: Csaba Gönczi, Éva Csikós, István Hermecz, Gergely Héja, Árpád Illár, Lajos Nagy, Andrea Sántáné Csutor, Attila Simon, Kálmán Simon, Ágota Smelkóné Esek, Tiborné Szomor, Györgyné Szvoboda
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Patent number: 6562857Abstract: This invention provides a progesterone receptor agonist of formula 1 having the structure wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—; n=1-5; p=1-4; q=1-4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB, RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoType: GrantFiled: January 9, 2002Date of Patent: May 13, 2003Assignee: WyethInventors: Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6548679Abstract: The present invention provides compounds of general formula I or II: wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I or II, intermediates and processes useful for preparing compounds of formula I or II, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I or II.Type: GrantFiled: August 17, 2000Date of Patent: April 15, 2003Assignee: The Regents of the University of CaliforniaInventors: Trevor C. McMorris, Michael J. Kelner
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Patent number: 6541643Abstract: The invention relates to a process for the preparation of spiro[cis-4-(&bgr;-hydroxyethyloxy)cyclohexane-[3H]indol]-2′[1′H]-one derivatives of the formula (I) wherein R1 and R2 are as defined herein, by reduction of a dispiro[(1,3-dioxolane)-2,4′-cyclohexane-1′3′-[3H]indol]-2″[1″H]-one derivative of general formula (II), wherein R1 and R2 are as defined herein, which comprises carrying out the reduction (a) with sodium cyanoborohydride in the presence of a Lewis acid, or (b) with sodium borohydride in the presence of a strong acid.Type: GrantFiled: April 17, 2002Date of Patent: April 1, 2003Assignee: Sanofi-SynthelaboInventors: Gergely Héja, Éva Csikós, Csaba Gönczi, Judit Halász, Félix Hajdú, István Hermecz, László Kis, Lajos Nagy, Andrea Sántáné Csutor, Kálmán Simon, Tiborné Szomor, Györgyné Szvoboda
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Patent number: 6444819Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R1, R2 and R3 independently represent organic or inorganic substituents; R4 and R4′ independently represent hydrogen, alkyl or form a ring with the atom to which they are attached; R5 represents hydrogen, alkyl, alkoxy, or alkylthio, and R6 represents hydrogen or alkyl; or R5 and R6 form a ring together with the atoms to which they are attached; and R7, R8, R9, R10, and R11 independently represent hydrogen or alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.Type: GrantFiled: October 11, 2001Date of Patent: September 3, 2002Assignee: Neurogen CorporationInventors: Renata Xavier Kover, Salva Terdjanian, Jennifer Tran, Andrew Thurkauf
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Patent number: 6441019Abstract: This invention provides compounds of the formula: wherein A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N, one N may be optionally substituted with an C1 to C6 alkyl group; R1 and R2 are independent substituents selected from the group of H, C1 to C6 alkyl, substituted C1 to C6 alkyl, C2 to C6 alkenyl, substituted C2 to C6 alkenyl, C2 to C6 alkynyl, substituted C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, CORA, or NRBCORA; or R1 and R2 are fused to form optionally substituted 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic ring, the heterocyclic ring containing one to three heteroatoms selected from the group of O, S and N; or pharmaceutically useful salts thereof.Type: GrantFiled: July 17, 2001Date of Patent: August 27, 2002Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Arthur A. Santilli, Andrew Q. Viet, Puwen Zhang, Andrew Fensome, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6358750Abstract: The invention provides spiro[pyrrolidine-2,3′-oxindole] compounds and libraries of these compounds produced by the stereo- and regio-selective reaction of variously substituted isatins, &agr;-amino acids, and dipolarophiles (e.g., trans-chalcones, acrylate esters, or vinyl oxindoles). The new libraries can be assayed using any of many known screening procedures for activity, e.g., biological activity. For example, the libraries can be screened for activity as drugs (e.g., anticancer drugs, antibiotics, antiviral drugs, antiinflammatory drugs, analgesics, immunomodulators, neuroleptics, sedatives, stimulants, or diagnostic aids), bioseparation agents, or pesticides (e.g., herbicides, insecticides, or rodenticides).Type: GrantFiled: March 27, 2000Date of Patent: March 19, 2002Assignee: ArQule, Inc.Inventors: Demosthenes Fokas, David L. Coffen, William J. Ryan
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Patent number: 6358887Abstract: The present invention relates to new compounds of the formula (I) in which X, Y and Z have the meanings given in the description and Het represents one of the groups in which A, B, D and G have the meanings given in the description, a plurality of processes for their preparation, and to their use as pesticides and herbicides.Type: GrantFiled: August 5, 1997Date of Patent: March 19, 2002Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Norbert Lui, Michael Ruther, Arno Widdig, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Peter Dahmen, Norbert Mencke, Andreas Turberg
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Patent number: 6355648Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structures: wherein: R1 and R2 are H, alkyl, substituted alkyl; OH; O(alkyl); O(substituted alkyl); OAc; aryl; substituted aryl; heteroaryl; substituted heteroaryl; alkylaryl; alkylheteroaryl; 1-propynyl; or 3-propynyl; or R1 and R2 are joined to form an alkyl, alkenyl or heterocyclic ring; or R1 and R2 together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, alkynyl, substituted alkynyl, or CORA; RA is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NH2, NO2, C1 to C6 alkyl, or substituted C1 to C6 alkyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; R5 is optionally substituted and selected from a benzene riType: GrantFiled: April 19, 2000Date of Patent: March 12, 2002Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.Inventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Lin Zhi, Todd K. Jones, Jay E. Wrobel, Christopher M. Tegley, James P. Edwards, Edward G. Melenski
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Patent number: 6156783Abstract: Novel azabicyclic derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments are disclosed.Type: GrantFiled: October 30, 1998Date of Patent: December 5, 2000Assignee: SmithKline Beecham p.l.c.Inventor: Laramie Mary Gaster
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Patent number: 6114540Abstract: The invention provides spiro[pyrrolidine-2,3'-oxindole] compounds produced by the stereo- and regio-selective reaction of variously substituted isatins, .alpha.-amino acids, and dipolarophiles (e.g., trans-chalcones, acrylate esters, or vinyl oxindoles).Type: GrantFiled: September 8, 1998Date of Patent: September 5, 2000Assignee: ArQule, Inc.Inventors: Demosthenes Fokas, David L. Coffen, William J. Ryan
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Patent number: 6110872Abstract: The invention relates to new phenyl-substituted cyclic ketoenols of the formula (I) in whichHet represents one of the groups ##STR1## wherein A, B, D, G, X, Y and Z have the meaning given in the description, several processes and intermediate products for their preparation and their use as pest control agents and herbicides.Type: GrantFiled: December 22, 1997Date of Patent: August 29, 2000Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Alan Graff, Norbert Mencke, Andreas Turberg, Peter Dahmen
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Indolin-2-one derivatives, method for preparing them and pharmaceutical compositions containing them
Patent number: 6090818Abstract: The invention relates to compounds with formula (I), a process for their preparation and pharmaceutical compositions containing them.Type: GrantFiled: June 14, 1999Date of Patent: July 18, 2000Assignee: Sanofi-SynthelaboInventors: Loic Foulon, Claudine Serradeil-Le Gal, Gerard Valette -
Patent number: 6046341Abstract: The subject of the invention is indolin-2-one derivatives of formula: ##STR1## in which: W represents a --CH.sub.2 -- or --SO.sub.2 -- group;Cy forms, with the carbon to which it is bonded, a non-aromatic, saturated or unsaturated C.sub.3 -C.sub.12 hydrocarbon ring which is optionally condensed or substituted by one or a number of (C.sub.1 -C.sub.7)alkyl groups, it being possible for the said groups to substitute the same carbon atom one or a number of times, or by a C.sub.3 -C.sub.6 spirocycloalkyl;T represents a (C.sub.1 -C.sub.4)alkylene which is optionally interrupted by a (C.sub.3 -C.sub.6)cycloalkylene, the said alkylenes optionally being substituted one or a number of times on the same carbon atom by a (C.sub.1 -C.sub.3)alkyl; or alternatively T represents a direct bond;Z represents in particular an amino group;R.sub.1 and R.sub.2, as well as R.sub.3 and R.sub.4, are either hydrogen or substituents, such as, for example, a halogen, an alkyl, and the like.Type: GrantFiled: October 12, 1999Date of Patent: April 4, 2000Assignee: Sanofi-SynthelaboInventors: Loic Foulon, Georges Garcia, Claudine Serradeil-Le Gal, Gerard Valette
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Patent number: 5948807Abstract: Compounds of formula I: ##STR1## wherein R.sup.1, R.sup.2, W, X, Y and Z have any of the values defined in the specification, and their pharmaceutically acceptable salts, are inhibitors of monoamine re-uptake and are useful for treating diseases in mammals wherein insufficient synaptic levels of monoamine are implicated. Also disclosed are pharmaceutical compositions, processes for preparing compounds of formula I, and intermediates useful for the synthesis of compounds of formula I.Type: GrantFiled: September 3, 1997Date of Patent: September 7, 1999Assignee: Regents of the University of MinnesotaInventors: S. Mbua Ngale Efange, Deborah Carmen Mash
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Patent number: 5942532Abstract: The invention relates to benzimidazole antibacterial compounds of the Formula I: ##STR1## as described herein, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.Type: GrantFiled: September 5, 1997Date of Patent: August 24, 1999Assignee: Ortho Pharmaceutical CorporationInventors: Kwasi Adomako Ohemeng, Van Nhatton Nguyen
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Patent number: 5849780Abstract: The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.Type: GrantFiled: October 17, 1994Date of Patent: December 15, 1998Assignee: SanofiInventors: Alain Di Malta, Loic Foulon, Georges Garcia, Dino Nisato, Richard Roux, Claudine Serradeil-Legal, Gerard Valette, Jean Wagnon
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Patent number: 5808071Abstract: A commercial scale process for the production of tetrahydroisoquinolines and related heterocyclics by reaction, in mildly acidic conditions, of aryl N-sulfonylethylamines in the presence of a suitable Lewis acid, and a compound capable of in situ generation of formaldehyde. The process is further characterized by formaldehyde being generated by the reaction of the Lewis acid upon the formaldehyde generating agent, instead of being present as an initial reactant. The process further avoids the presence of initial water which destroys the Lewis acid before it can act upon the formaldehyde generating agent.Type: GrantFiled: July 15, 1997Date of Patent: September 15, 1998Assignee: Hoechst Marion Roussell, Inc.Inventor: Timothy James-Norman Watson
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Patent number: 5773448Abstract: A pharmaceutical compound of the formula ##STR1## and salts and esters thereof.Type: GrantFiled: April 14, 1997Date of Patent: June 30, 1998Assignee: Eli Lilly and Company LimitedInventors: Peter Thaddeus Gallagher, William Martin Owton, Colin William Smith
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Patent number: 5756532Abstract: The compounds of formula I: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R.sup.1 and R.sup.2, taken together, are benzylidene optionally substituted with R.sup.3 as defined below or alkylidene, or R.sup.1 and R.sup.2, taken together with the carbon to which they are attached, form a carbonyl moiety or a cycloalkyl group; R.sup.3 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aralkoxy, alkanoyloxy, amino, mono- or di-alkylamino, alkanamido or alkanesulfonamido; R.sup.4 is hydrogen or alkyl; m is an integer 0, 1 or 2; n is an integer from 0 to 6, inclusive; Z is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, polycyclo-alkyl, phenyl optionally substituted with R.sup.3 as defined above, phenoxy optionally substituted with R.sup.3 as defined above, naphthyl optionally substituted with R.sup.3 as defined above or naphthyloxy optionally substituted with R.sup.Type: GrantFiled: October 15, 1996Date of Patent: May 26, 1998Assignee: American Home Products CorporationInventors: Gary P. Stack, Richard E. Mewshaw, Byron A. Bravo, Young H. Kang
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Patent number: 5723625Abstract: To produce defined isomer mixtures of compounds with spirocyclic beta-aminocarboxyl and/or beta-aminocarbonyl systems the invention supposes that they be dissolved in solvents which have good dissolving power for these compounds, whose relative permittivity is sufficient to stabilize the amphoteric intermediates occuring in isomerization, which as proton donors constitute hydrogen bridges, whose basicity is less than that of the compounds for isomerization and whose boiling point is so high that an adequate reaction speed can be attained by raising temperature. Further, the invention proposes that the isomerization be prevented, influenced, or terminated by altering at least one of these factors and or by altering the temperature.Type: GrantFiled: October 4, 1996Date of Patent: March 3, 1998Assignee: Immodal Pharmaka Gesellschaft m.b.HInventors: Dietmar Keplinger, Klaus Keplinger, Gerhard Laus
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Patent number: 5696145Abstract: The present invention relates to 1-benzyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## to their preparation and to the pharmaceutical compositions in which they are present. These derivatives have an affinity for the vasopressin and oxytocin receptors.Type: GrantFiled: June 7, 1995Date of Patent: December 9, 1997Assignee: SanofiInventors: Loic Foulon, Georges Garcia, Daniel Mettefeu, Claudine Serradeil-Legal, Gerard Valette
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Patent number: 5633247Abstract: Spirocycles of general structural formula: ##STR1## are Class III antiarrhythmic agents.Type: GrantFiled: July 5, 1995Date of Patent: May 27, 1997Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
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Patent number: 5618833Abstract: The present invention relates to 1-benzyl-1,3-dihydroindol-2-one derivatives of the formula (I). The invention also relates to preparation of these derivatives as well as to the pharmaceutical compositions in which they are present. These derivatives have an affinity for the vasopressin and oxytocin receptors.Type: GrantFiled: July 29, 1994Date of Patent: April 8, 1997Assignee: SanofiInventors: Lo ic Foulon, Georges Garcia, Daniel Mettefeu, Claudine Serradeil-Legal, G erard Valette
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Patent number: 5616705Abstract: Compounds of the formula I ##STR1## where the substituents have the meanings given in the description, and their preparation are described. The novel compounds are suitable for the control of diseases.Type: GrantFiled: April 19, 1996Date of Patent: April 1, 1997Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Rainer Munschauer, Liliane Unger, Hans-Jurgen Teschendorf, Thomas Hoger
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Patent number: 5462913Abstract: The invention relates to new 1-H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A and B together with the carbon atom to which they are bonded represent a substituted cycle,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents 0, 1, 2 or 3,G represents hydrogen (a) or the groups ##STR2## represents a metal ion equivalent or an ammonium ion, L and M represents oxygen and/or sulphur,R.sup.1 represents in each case optionally halogen-substituted alkyl, alkenyl, alkoxyalkyl, alkylthioalkyl, polyalkoxyalkyl or cycloalkyl, which can be interrupted by hetero atoms, optionally substituted phenyl, optionally substituted phenylalkyl, substituted hetaryl, substituted phenoxyalkyl or substituted hetaryloxyalkyl,R.sup.2 represents in each case optionally halogen-substituted alkyl, alkenyl, alkoxyalkyl, polyalkoxyalkyl or in each case optionally substituted phenyl or benzyl,R.sup.3, R.sup.Type: GrantFiled: October 21, 1993Date of Patent: October 31, 1995Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kruger, Christoph Erdelen, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt, Ulrike Wachendorff-Neumann, Wilhelm Stendel
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Patent number: 5461054Abstract: The anthracene-spiro-pyrrolidines according to the invention are prepared by reacting either anthracene-spiro-furans or unsubstituted anthracene-spiropyrrolidines with appropriately substituted amines or by reacting unsubstituted anthracene derivatives with appropriately substituted methylenepyrrolidines. The substances can be used as active agents in medicaments, in particular for the production of immunomodulating medicaments.Type: GrantFiled: December 9, 1993Date of Patent: October 24, 1995Assignee: Bayer AktiengesellschaftInventors: Eckhard Schwenner, Gaetan Ladouceur, Thomas M. Aune
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Patent number: 5399562Abstract: This invention relates to compounds of the formula: ##STR1## which are useful as 5-HT.sub.4 agonists or antagonists and 5-HT.sub.3 antagonists.Type: GrantFiled: February 4, 1994Date of Patent: March 21, 1995Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Clara I. Villamil
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Patent number: 5395972Abstract: Amines are produced in high yield by the process which comprises allowing a cyclic ketone to react with ammonia in the presence of active carbon to produce imino derivatives and then, allowing the imino derivatives to react with hydrogen in the presence of a hydrogenating catalyst.Type: GrantFiled: February 8, 1994Date of Patent: March 7, 1995Assignee: Sumitomo Chemical Company, LimitedInventors: Atsushi Furutani, Takuo Hibi, Michio Yamamoto, Gohfu Suzukamo
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Patent number: 5310932Abstract: Novel compounds are disclosed having the formula ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.Type: GrantFiled: September 11, 1991Date of Patent: May 10, 1994Assignee: E. R. Squibb & Sons, Inc.Inventors: Karnail Atwal, George C. Rovnyak
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Patent number: 5292746Abstract: The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.Type: GrantFiled: August 5, 1992Date of Patent: March 8, 1994Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Albert A. Carr, Craig E. Thomas, Ronald C. Bernotas, George Ku
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Patent number: 5288877Abstract: Described is a continuous process for preparing indolenine compounds which comprises charging continuously and simultaneously to a reactor containing an acetic acid reaction medium (1) substituted phenylhydrazine and (2) unsymmetrical ketone from separate sources, continuously discharging from the reactor indolenine product in acetic acid solution, separating acetic acid from the indolenine product, recycling separated acetic acid to the reactor, neutralizing residual acetic acid remaining in the indolenine product with aqueous inorganic alkaline reagent, and separating from the indolenine product an aqueous solution of salts resulting from the preparation and neutralization of the indolenine product.Type: GrantFiled: July 3, 1991Date of Patent: February 22, 1994Assignee: PPG Industries, Inc.Inventors: Charles H. Hoelscher, Bruce R. Anderson
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Patent number: 5276026Abstract: Tetrahydronaphthaleneamine derivatives having the formula ##STR1## wherein R, R', R.sub.1 and R.sub.2 are as defined herein, are novel calcium channel blockers.Type: GrantFiled: January 21, 1993Date of Patent: January 4, 1994Assignee: E. R. Squibb & Sons, Inc.Inventors: Joel C. Barrish, Steven H. Spergel
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Patent number: 5264419Abstract: Novel peptoids of .alpha.-substituted Trp derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further the compounds are antianxiety agents and antiulcer agents. They are agents useful for preventing the response to withdrawal from chronic treatment or use of nicotine, diazepam, alcohol, cocaine, caffeine, or opioids. The compounds are also useful in the treatment and/or prevention of panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the peptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare diagnostic compositions.Type: GrantFiled: July 12, 1991Date of Patent: November 23, 1993Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Martyn C. Pritchard, Edward Roberts
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Patent number: 5264426Abstract: The present invention relates to new phosphorylated diazacycloalkanes, to processes for their preparation, and to their use as pesticides, in particular as insecticides and nematicides. The new compounds have the general formula (I) ##STR1## in which R.sup.1 represents hydrogen, or represents alkyl, alkenyl or aryl, each of which is optionally substituted by halogen or alkoxy,A represents an alkanediyl radical which is optionally substituted by alkyl,R.sup.2 represents alkyl,R.sup.3 represents alkyl andR.sup.4 represents hydrogen, or represents alkyl, alkenyl or aryl, each of which is optionally substituted by halogen or alkoxy.Type: GrantFiled: September 18, 1992Date of Patent: November 23, 1993Assignee: Bayer AktiengesellschaftInventors: Herbert Sommer, Jurgen Hartwig
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Patent number: 5252536Abstract: Substituted indolinone compounds which are effective in the control of undesirable plant species are described. Also described are a method for the herbicidal use of the compounds and a method for their preparation.Type: GrantFiled: December 31, 1991Date of Patent: October 12, 1993Assignee: American Cyanamid CompanyInventors: Michael E. Condon, Gary M. Karp
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Patent number: 5250733Abstract: Benzylideneindene compounds, which are useful not only as the photoconductive material for electrophotography, but also as a charge transporting material employed in a function-separating type photoconductor in which an organic or inorganic pigment is used as a charge generating material, and an electrophotographic photoconductor containing at least one of the above benzylideneindene compounds in a photoconductive layer thereof, are disclosed.Type: GrantFiled: February 19, 1992Date of Patent: October 5, 1993Assignee: Ricoh Company, Ltd.Inventors: Tamotsu Aruga, Masaomi Sasaki, Mitsuru Hashimoto
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Patent number: 5221751Abstract: Polymethine dyes suitable for use in an optical recording medium have the formula ##STR1## where p is 0 or 1,Z is nitrogen, oxygen, sulfur, isopropylidene, cyclohexylidene or the radical --CH.dbd.CH--,Q is a radical of the formula ##STR2## where R.sup.2 is hydrogen, chlorine, bromine or C.sub.1 -C.sub.6 -alkyl, L is C.sub.1 -C.sub.12 -alkylene, or a single bondR.sup.1 is hydrogen, substituted or unsubstituted C.sub.1 -C.sub.20 -alkyl, substituted or unsubstituted C.sub.5 -C.sub.7 -cycloalkyl or substituted or unsubstituted phenyl,X.sup..crclbar. is an anion, and the rings A may each be substituted or benzofused.Type: GrantFiled: May 20, 1991Date of Patent: June 22, 1993Assignee: BASF AktiengesellschaftInventors: Michael Acker, Bernhard Albert, Sibylle Brosius, Klaus D. Schomann, Harald Kuppelmaier
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Patent number: 5182397Abstract: There are provided aryloxy-1'-(substituted)-spiro[cycloalkane-1,3'-indolin]-2'-one compounds, their herbicidal use, particularly for the selective control of undesirable plant species in the presence of cereal crops such as rice and wheat, and a method for the preparation thereof.Type: GrantFiled: July 31, 1991Date of Patent: January 26, 1993Assignee: American Cyanamid CompanyInventors: Michael E. Condon, Gary M. Karp, Jeffrey H. Birk
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Patent number: 5180825Abstract: Disclosed in a mitomycin derivative represented by the formula (I): ##STR1## wherein W is a heterocyclic group.Type: GrantFiled: November 13, 1991Date of Patent: January 19, 1993Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hitoshi Arai, Motomichi Kono, Masaji Kasai, Katsushige Gomi, Tadashi Ashizawa
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Patent number: 5179119Abstract: This invention relates to 1,3-dihydro-1-(pyridinylamino)-2H-indol-2-ones of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl, aryl, arylloweralkyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; or R.sub.2 and R.sub.3 together form a cycloalkane ring of 4 to 6 carbons or a spiro-fused aryl cycloalkane or heterocycloalkyl selected from the group consisting of piperidine and tetrahydropyran; X and Y are independently hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; m and n are independently integers of 1 to 3, the pharmaceutically acceptable acid addition salts thereof and, where applicable the optical, geometrical and stereoisomers and racemic mixtures thereof. The compounds of this invention display utility as analgesics, anticonvulsants, for enhancing memory and for the treatment of Alzheimer's disease.Type: GrantFiled: July 26, 1991Date of Patent: January 12, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, David G. Wettlaufer
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Patent number: 5153211Abstract: Disclosed are substituted or unsubstituted planar tricyclic fluorene or nuclear analogs thereof, spiro-coupled to a five-membered ring containing a secondary amide, and the pharmaceutically acceptable salts thereof. These compounds are useful, inter alia in the treatment of diabetes. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when indicated for, inter alia, long term, prophylactic treatment of the diabetes syndrome. A particularly preferred class of compounds comprise difluoro-dialkoxy substituted spiro-(9H-fluorene-9,4'-imidazolidine)-2',5-diones.Type: GrantFiled: August 27, 1991Date of Patent: October 6, 1992Assignee: Alcon Laboratories, Inc.Inventor: Billie M. York, Jr.