Two Of The Cyclos Share At Least Three Ring Members Or A Ring Carbon Is Shared By Three Of The Cyclos (i.e., Bridged Or Peri-fused) Patents (Class 546/72)
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Patent number: 11944616Abstract: The present invention relates to compounds of formula (I): for use as peripheral NMDA receptor antagonists.Type: GrantFiled: May 26, 2022Date of Patent: April 2, 2024Assignees: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITÉ PARIS-SACLAY, ASSISTANCE PUBLIQUE—HOPITAUX DE PARIS (APHP), HOPITAL MARIE LANNELONGUEInventors: Sylvia Cohen-Kaminsky, Marc Humbert, Sebastien Dumas, Gilles Bru-Mercier, Samir Messaoudi, Jean-Daniel Brion, Mouad Alami, Gilles Galvani
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Publication number: 20150087633Abstract: Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.Type: ApplicationFiled: December 1, 2014Publication date: March 26, 2015Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Donald D. Payan, Sylvia Braselmann
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Publication number: 20150031887Abstract: An organocatalyst for oxidizing alcohols in which a primary alcohol is selectively oxidized in a polyol substrate having a plurality of alcohols under environmentally-friendly conditions. The organic oxidation catalyst has an oxygen atom bonded to a nitrogen atom of an azanoradamantane skeleton and at least one alkyl group at positions 1 and 5. The oxidation catalyst has higher activity than TEMPO, which is an existing oxidation catalyst, in the selective oxidation reaction of primary alcohols, and better selectivity than AZADO and 1-Me-AZADO. This DMN-AZADO can be applied to the selective oxidation reaction of primary alcohols that contributes to shortening the synthesizing process for pharmaceuticals, pharmaceutical raw materials, agricultural chemicals, cosmetics, organic materials, and other such high value-added organic compounds.Type: ApplicationFiled: February 22, 2013Publication date: January 29, 2015Inventors: Yoshiharu Iwabuchi, Masatoshi Shibuya, Ryusuke Doi
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Patent number: 8933220Abstract: The present invention relates to photochromic fused naphthopyrans having a benzene ring which is adjacent to the pyran oxygen and is linked to the para substituent via both meta positions, and to the use thereof in plastics of all types, in particular for ophthalmic purposes.Type: GrantFiled: December 21, 2011Date of Patent: January 13, 2015Assignee: Rodenstock GmbHInventors: Manfred Melzig, Yven Rohlfing, Udo Weigand
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Publication number: 20130310556Abstract: The present invention relates to photochromic fused naphthopyrans having a benzene ring which is adjacent to the pyran oxygen and is linked to the para substituent via both meta positions, and to the use thereof in plastics of all types, in particular for ophthalmic purposes.Type: ApplicationFiled: December 21, 2011Publication date: November 21, 2013Applicant: Rodenstock GMBHInventors: Manfred Melzig, Yven Rohlfing, Udo Weigand
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Patent number: 8133656Abstract: An oxime ester compound represented by general formula (I): wherein R1 and R2 each independently represent R11, OR11, COR11, SR11, CONR12R13, or CN; R11, R12, and R13 each independently represent a hydrogen atom, an alkyl group having 1 to 20 carbon atoms, an aryl group having 6 to 30 carbon atoms, an arylalkyl group having 7 to 30 carbon atoms, or a heterocyclic group having 2 to 20 carbon atoms, R3 and R4 each independently represent R11, OR11, SR11, COR11, CONR12R13, NR12COR11, OCOR11, COOR11, SCOR11, OCSR11, COSR11, CSOR11, CN, a halogen atom, or a hydroxyl group; a and b each independently represent 0 to 4; X represents an oxygen atom, a sulfur atom, a selenium atom, CR31R32, CO, NR33, or PR34; R31, R32, R33, and R34 each independently represent R11, OR11, COR11, SR11, CONR12R13, or CN.Type: GrantFiled: December 21, 2007Date of Patent: March 13, 2012Assignee: Adeka CorporationInventors: Daisuke Sawamoto, Koichi Kimijima
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Patent number: 8003795Abstract: Compositions comprising extracts or isolated or purified compounds from plants of the genus Corydalis provide prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Corydalis compounds and their derivatives of natural and synthetic origins lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression and activate AMP-activated protein kinase. Specific stereoisomers of Corydalis compounds with lipid lowering activity include 14R-(+)-corypalmine, 14R,13S-(+)-corydaline, 14R-(+)-tetrahydropalmatin, (+)-corlumidin, d-(+)-bicuculline, and (+)-egenine.Type: GrantFiled: June 20, 2008Date of Patent: August 23, 2011Assignee: CVI Pharmaceuticals LimitedInventors: Haiyan Liu, Junbo Wang, Rui Zhang, Nicholas Cairns, Jingwen Liu
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Publication number: 20110142717Abstract: The present invention generally relates to luminescent and/or optically absorbing compositions and/or precursors to those compositions, including solid films incorporating these compositions/precursors, exhibiting increased luminescent lifetimes, quantum yields, enhanced stabilities and/or amplified emissions. The present invention also relates to sensors and methods for sensing analytes through luminescent and/or optically absorbing properties of these compositions and/or precursors. Examples of analytes detectable by the invention include electrophiles, alkylating agents, thionyl halides, and phosphate ester groups including phosphoryl halides, cyanides and thioates such as those found in certain chemical warfare agents. The present invention additionally relates to devices and methods for amplifying emissions, such as those produced using the above-described compositions and/or precursors, by incorporating the composition and/or precursor within a polymer having an energy migration pathway.Type: ApplicationFiled: November 15, 2010Publication date: June 16, 2011Applicant: Massachusetts Institute of TechnologyInventors: Timothy M. Swager, Tae-Hyun Kim, Shi-Wei Zhang
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Patent number: 7745628Abstract: The present invention relates to a method for obtaining Dolasetron that comprises: a) Esterification of the alcohol of formula (IV) with indole-3-carboxylic acid (compound (III)) or a reactive derivative thereof, to give a compound of formula (V), followed by step b) which includes Dieckmann reaction of the intermediate (V), by reaction with a strong organic or inorganic base, to give the intermediate (VI), and step c) which comprises dealcoxycarbonylation of the intermediate (VI) to give Dolasetron base and, if desired, a pharmaceutically acceptable salt thereof, hydrates or solvates of the base of said salt. The invention also relates to the intermediates (V) and (VI), and methods for obtaining them. With the method of the present invention Dolasetron is obtained at industrial scale with good yields, with decreased use of reactants and solvents, while said method is also of greater atomic efficiency.Type: GrantFiled: June 26, 2006Date of Patent: June 29, 2010Assignee: Inke, S.A.Inventors: Juan Antonio Perez Andres, Pere Dalmases Barjoan
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Patent number: 7662831Abstract: The present invention is directed to compounds of Formula I: that are potassium channel modulators and pharmaceutical compositions thereof. The present invention is further directed to methods of treatment using the compounds and pharmaceutical compositions of the invention. The present invention is still further directed to synthetic processes for producing the compounds of the invention.Type: GrantFiled: July 26, 2007Date of Patent: February 16, 2010Assignee: Wyeth LLCInventors: Matthew A. Wilson, Gregory S. Welmaker, Eugene J. Trybulski, John A. Butera, Ronald L. Magolda
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Publication number: 20100004278Abstract: The present invention provides pharmaceutical compositions comprising dextromethorphan hydrochloride.Type: ApplicationFiled: July 3, 2008Publication date: January 7, 2010Inventor: Chandra Singh
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Patent number: 7608714Abstract: The present invention provides an improved process for the preparation of Dolasetron salts, in particularly Dolasetron mesylate. Also provided are intermediates for the process and methods of preparing the intermediates.Type: GrantFiled: January 5, 2007Date of Patent: October 27, 2009Assignee: TEVA Gyógyszergyár Zártkörúen Müködö RészvénytársaságInventors: Janos Hajko, Tivadar Tamas, Adrienne Kovacsne-Mezei, Erika Magyar Molnarne, Csaba Peto, Csaba Szabo
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Publication number: 20090253731Abstract: The present invention relates to a method of identifying agents suitable for use in treating epilepsy and other brain disorders, including but not limited to bipolar disorder, schizophrenia and depression. The invention further relates to methods of treatment based on the use of agents so identifiable.Type: ApplicationFiled: April 9, 2009Publication date: October 8, 2009Applicant: DUKE UNIVERSITYInventor: John Wesseling
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Publication number: 20090124806Abstract: To provide an industrially-useful and environmentally-friendly novel oxidation reaction.Type: ApplicationFiled: May 6, 2008Publication date: May 14, 2009Applicant: Nissan Chemical Industries, Ltd.Inventors: Yoshiharu IWABUCHI, Masatoshi Shibuya, Masaki Tomizawa, Takahisa Sato, Susumu Sato
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Publication number: 20080027090Abstract: The present invention is directed to compounds of Formula I: that are potassium channel modulators and pharmaceutical compositions thereof. The present invention is further directed to methods of treatment using the compounds and pharmaceutical compositions of the invention. The present invention is still further directed to synthetic processes for producing the compounds of the invention.Type: ApplicationFiled: July 26, 2007Publication date: January 31, 2008Applicant: WYETHInventors: Matthew A. WILSON, Gregory S. WELMAKER, Eugene J. Trybulski, John A. BUTERA, Ronald L. MAGOLDA
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Patent number: 7101890Abstract: New derivatives of benzazepine, particularly of benzofuro[3a,3,2,ef][2]benzazepin of the general formula (I) and new compounds of the general formula (III) Drugs, containing compounds of formulas (I) and/or (III), which can be used successfully for the treatment of Alzheimer's disease and related dementia conditions, as well as for the treatment of Langdon-Down syndrome, are also described.Type: GrantFiled: August 26, 2003Date of Patent: September 5, 2006Assignee: Sanochemia Ltd.Inventors: Laszlo Czollner, Johannes Frohlich, Ulrich Jordis, Bernhard Kuenburg
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Patent number: 7045626Abstract: A compound of formula (I): useful in the treatment and prophylaxis of conditions mediated by s-CD23Type: GrantFiled: November 25, 2002Date of Patent: May 16, 2006Assignee: SmithKline Beecham p.l.c.Inventors: Desmond John Best, Gordon Bruton, Barry Sidney Orlek
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Patent number: 6908927Abstract: The invention relates to pyridopyranoazepine derivatives, to pharmaceutical compositions containing them, to process for preparing them, and to the method of use thereof in the treatment or prevention of disorders associated with a dysfunction of the nicotine receptors.Type: GrantFiled: February 6, 2003Date of Patent: June 21, 2005Assignee: Sanofi-SynthelaboInventors: Frédéric Galli, Samir Jegham, Alistair Lochead, Axelle Samson
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Publication number: 20030187012Abstract: The invention relates to pyridopyranoazepine derivatives, to pharmaceutical compositions containing them, to process for preparing them, and to the method of use thereof in the treatment or prevention of disorders associated with a dysfunction of the nicotine receptors.Type: ApplicationFiled: February 6, 2003Publication date: October 2, 2003Inventors: Frederic Galli, Samir Jegham, Alistair Lochead, Axelle Samson
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Publication number: 20030144516Abstract: Crystalline form VII of cabergoline, a pharmaceutical composition containing it and a process for its preparation are disclosed. The process may comprise a slurry procedure using form I or mixture of forms I and VII of cabergoline in a solvent at a temperature above 30° C.Type: ApplicationFiled: September 18, 2002Publication date: July 31, 2003Inventors: Ilaria Candiani, Raffaella Budelli, Marco Pandolfi, Mario Ungari
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Patent number: 6476021Abstract: Novel fused tetracyclic heterocyclic compounds having a potent and highly selective effect of inhibiting cyclic GMP phosphodiesterase (cGMP-PDE) and a high safety; a process for producing the same; drugs characterized by containing at least one of these compounds as the active ingredient, in particular, preventives and/or remedies for pulmonary hypertension, ischemic heart diseases, erectile insufficiency, female sexual dysfunction or diseases against which cGMP-PDE inhibitory effects are efficacious and intermediates useful in producing the above compounds.Type: GrantFiled: May 26, 2000Date of Patent: November 5, 2002Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Masayuki Ohashi, Hidemitsu Nishida, Toshiyuki Shudo
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Publication number: 20020128281Abstract: Compounds of formula (I), wherein X is selected from the group consisting of O, and NR3, where R3 represents a lower alkyl group; Y is selected from the group consisting of CH and N; R1 and R2 are independently selected from the group consisting of NH2, NHR4 and NR52, where R4 and R5 each represent a lower alkyl group, or R1 and R2 together represent a cycle selected from (a), (b) and (c), wherein R6, R7 and R8 are independently selected from the group consisting of hydrogen atoms, lower alkyl groups, hydroxy groups and lower alkoxy groups; and Z is selected from the group consisting of O.Type: ApplicationFiled: September 24, 2001Publication date: September 12, 2002Applicant: Universidad Complutense de madridInventors: Jose Luis Fernandez Puentes, Dolores Garcia Gravalos, Carmen Avendano Lopez, Maria del Mar Blanco Castro, Jose Carlos Menendez Ramos
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Patent number: 6423842Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.Type: GrantFiled: October 5, 2001Date of Patent: July 23, 2002Assignee: UCB, S.A.Inventors: Gurmit Grewal, Anna Toy-Palmer, Xiong Cai, George Mark Latham
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Patent number: 6365743Abstract: The invention relates to a method for the preparation of an enantiomerically pure imidazolyl compound of the general formula wherein: n is 0 or 1; m is 1 or 2; R1 is hydrogen, methyl or ethyl; and C* denotes a chiral center; as well as its pharmaceutically acceptable acid addition salt. The invention further relates to a method of racemization and to a new acid addition salt of this formula I compound and D-pyroglutamic acid and to the hydrochloride monohydrate of the compound of formula I.Type: GrantFiled: August 16, 2000Date of Patent: April 2, 2002Assignee: Duphar International Research B.V.Inventors: Paulus F.C. van der Meij, Jan-Maarten Verbeek
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Patent number: 6346536Abstract: Poly(ADP-ribose) polymerase (“PARP”) inhibitors and methods for treating neurodegenerative diseases, neural tissue damage related to cerebral ischemia and reperfusion injury, and cardiovascular in an animal.Type: GrantFiled: September 3, 1997Date of Patent: February 12, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Paul F. Jackson, Keith M. Maclin, Jie Zhang
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Patent number: 6251916Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.Type: GrantFiled: May 9, 2000Date of Patent: June 26, 2001Assignee: UCB, S. A.Inventors: Gurmit Grewal, Anna Toy-Palmer, Xiong Cai, George Mark Latham
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Patent number: 5840903Abstract: This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of ##STR2## R.sub.1 is alkoxy of one to six carbon atoms; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are selected from the group consisting of hydrogen, halogen, CF.sub.3, hydroxy, alkoxy of one to six carbon atoms, acyl of two to seven carbon atoms, amino, amino substituted by one or two alkyl groups of one to six carbon atoms, C.sub.2 -C.sub.7 acylamino, aminocarbonyl, aminosulfone optionally substituted by one or two alkyl groups of one to six carbon atoms, C.sub.1 -C.sub.6 alkylsulfone and nitro;m is 1 or 2;X is O or NR.sub.7 ; andR.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms.Type: GrantFiled: July 27, 1992Date of Patent: November 24, 1998Assignee: G. D. Searle & Co.Inventors: Daniel Lee Flynn, Robert L. Shone
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Patent number: 5831095Abstract: A powerful new anti-convulsant and anti-ischemic pharmaceutical, 5-aminocarbonyl-5H-dibenzo?a,d!cycloheptene-5,10-imine is prepared according to a novel synthesis which converts the starting material, commercially available dibenzosubernone to ADCI without the use of chromatographic purification, hazardous reagents or extreme conditions. The starting material is converted to the corresponding imine through ammonia exposure, and directly converted with acetone cyanohydrin in the presence of sodium cyanide to a 5-amino, 5-cyanocycloheptene intermediate. The intermediate is cyclized using bromine, followed by a reduction of the bromine-carbon bond using sodium cyanoborohydride. The target compound is obtained through selective hydrolysis. An overall yield of 46 percent or better is obtained.Type: GrantFiled: September 18, 1996Date of Patent: November 3, 1998Assignee: Research Triangle InstituteInventors: Javier Gonzalez, F. Ivy Carroll
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Patent number: 5814642Abstract: A novel compound of the formula ##STR1## wherein Ar represents a tetracyclic fused heterocyclic group which may be substituted; R.sup.1 represents H or a hydrocarbon group which may be substituted; Y represents an amino acid or nitrogen-containing saturated heterocyclic group which may be substituted, its salt, inhibiting excellent cholinesterase inhibitory activity and monoamine uptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.Type: GrantFiled: July 30, 1996Date of Patent: September 29, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Yuji Ishihara, Masaomi Miyamoto
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Patent number: 5739337Abstract: Disclosed are a process and novel compounds useful for preparing compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, inorganic or optionally substituted organic substituents; andR.sub.3 is hydrogen, or an optionally substituted organic group,the process comprising cyclizing a tetrahydroisoquinoline of the formula ##STR2## where Y is a leaving group, in the presence of a stong base. The invention also encompasses a process for preparing the tetrahydroisoquinoline; and a process for converting the tetrahydroisoquinoline to the final amide I.Type: GrantFiled: March 8, 1996Date of Patent: April 14, 1998Assignee: Neurogen CorporationInventor: Philip D. Magnus
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Patent number: 5731317Abstract: The present invention is directed to certain novel compounds identified as bridged piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.1a, R.sup.2a, R.sup.3, R.sup.3a,R.sup.4, R.sup.5, A, X, and Y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: March 10, 1995Date of Patent: March 24, 1998Assignee: Merck & Co., Inc.Inventors: Zhijian Lu, Arthur A. Patchett, James R. Tata
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Patent number: 5686614Abstract: Disclosed are processes for resolving a racemic mixture of 5-aminocarbonyl-5H-dibenzo?a,d!cyclohepten-5,10-imines into component enantiomers comprising recrystallizaton of diasteriomeric tartrate salts.Type: GrantFiled: April 11, 1995Date of Patent: November 11, 1997Assignee: Neurogen CorporationInventors: Tappey H. Jones, Kenner C. Rice
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Patent number: 5663343Abstract: The invention relates to a method for the preparation of an enantiomerically pure imidazolyl compound of the general formula ##STR1## wherein n is 0 or 1; m is 1 or 2;R.sub.Type: GrantFiled: October 10, 1996Date of Patent: September 2, 1997Assignee: Duphar International Research B.V.Inventors: Paulus F. C. van der Meij, Jan-Maarten Verbeek
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Patent number: 5631264Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: May 24, 1995Date of Patent: May 20, 1997Assignee: Sanofi Winthrop, Inc.Inventors: Diane L. DeHaven-Hudkins, John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5624929Abstract: Compounds of the formula ##STR1## wherein the broken line represents an optional double bond; X is O, S, CH.sub.2 or CH.sub.2 CH.sub.2 ; R.sup.1 is selected from the group consisting of hydrogen, halogen, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkyl substituted with 1, 2 or 3 halogen atoms; R.sup.2 is selected from the group consisting of phenyl, substituted phenyl, heterocyclic groups, and substituted heterocyclic groups, said substituted phenyl and substituted heterocyclic groups being substituted with 1 or 2 substituents independently selected from the group consisting of C.sub.1 -C.sub.6 alkyl, trifuluoromethyl, and halogen; R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, or trifluoromethyl, or R.sup.3 and R.sup.Type: GrantFiled: May 22, 1995Date of Patent: April 29, 1997Assignee: Pfizer Inc.Inventors: Banavara L. Mylari, Joseph G. Lombardino, James M. McManus
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Patent number: 5620973Abstract: A novel compound of the formula ##STR1## wherein Ar represents a tetracyclic fused heterocyclic group which may be substituted; R.sup.1 represents H or a hydrocarbon group which may be substituted; Y represents an amino or nitrogen-containing saturated heterocyclic group which may be substituted, its salt, inhibiting excellent cholinesterase inhibitory activity and monoamine uptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.Type: GrantFiled: October 25, 1994Date of Patent: April 15, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Yuji Ishihara, Masaomi Miyamoto
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Patent number: 5554620Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment of neurodegenerative disorders or neurotoxic injuries utilizing them, wherein the substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts have the formula: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and p are as defined in the specification.Type: GrantFiled: July 29, 1994Date of Patent: September 10, 1996Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5534521Abstract: This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof; pharmaceutical compositions containing the compounds and a method for treating serotonin mediated condition with the compositionswhich act as 5-HT.sub.4 agonists or antagonists and/or 5-HT.sub.3 antagonists.Type: GrantFiled: November 8, 1994Date of Patent: July 9, 1996Assignee: G. D. Searle & Co.Inventors: Daniel L. Flynn, Alan E. Moormann, Daniel P. Becker, Michael S. Dappen, Roger Nosal, Robert L. Shone, Clara I. Villamil
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Patent number: 5461057Abstract: A compound of formula I ##STR1## wherein X, V, W, Y, Z, R, a, b, c, and d are as described herein. These compounds are useful in the treatment of tumors, allergies, bronchoconstriction and CNS diseases and conditions.Type: GrantFiled: September 8, 1994Date of Patent: October 24, 1995Assignee: Schering CorporationInventors: Joel G. Berger, David J. Blythin, Ronald J. Doll, Jonathan A. Pachter
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Patent number: 5196415Abstract: This invention is in the field of clinical neurology and relates specifically to compounds, compositions and methods for treatment of patients with generalized epilepsy or partial (symptomatic) epilepsy using compounds of the formula: ##STR1## This invention also relates to compounds, compositions and methods of treatment for drug craving in patients addicted to cocaine.Type: GrantFiled: January 29, 1992Date of Patent: March 23, 1993Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: James A. Monn, Andrew Thurkauf, Shunichi Yamaguchi, Michael A. Rogawski, Kenner C. Rice, Mariena V. Mattson, Arthur E. Jacobson
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Patent number: 5098820Abstract: Solid particle dispersions of dyes according to the formula: ##STR1## are disclosed as filter dyes for photograhic elements. In this formula,m is 0 or 1.R.sub.1 and R.sub.2 are each independently substituted or unsubstituted alkyl or substituted or unsubstituted aryl, or together with R.sub.3 and R.sub.4 form a heterocyclic ring.R.sub.3 and R.sub.4 are each H or together with R.sub.1 and R.sub.2 form a heterocyclic ring.A is a ketomethylene residue.X represents a carboxyphenyl or sulfonamidophenyl, or a carboxy or sulfonamido substituent that is appended to an aryl ring that is part of A.Type: GrantFiled: May 7, 1990Date of Patent: March 24, 1992Assignee: Eastman Kodak CompanyInventors: Michael J. McManus, Donald R. Diehl, Glenn M. Brown
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Patent number: 5082942Abstract: The invention concerns new derivatives of tetrahydro-2,3,6,7,1H,5H,11H-(1)benzopyrano(6,7,8, ij)quinolizinone in accordance with formula: ##STR1## in which R.sup.1 represents a radical having formula: ##STR2## wherein m is equal to 0 or 1, and n is equal to 0 or is a whole number from 1 to 12, provided that n is equal to 0 when m is 0, or the radical having the formula:--NH--(CH.sub.2).sub.n --NH.sub.2,in which n has the above meaning.Said derivatives can be used as markers for organic compounds, in order to detect them by chemiluminescence or fluorescence.Type: GrantFiled: January 31, 1991Date of Patent: January 21, 1992Assignee: Laboratories EurobioInventors: Georges Mahuzier, Joseph Chalom, Robert Farinotti, Michel Tod
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Patent number: 5045545Abstract: The invention relates to tetracyclic ketones of the general formula (I) ##STR1## wherein n represents 1, 2 or 3;Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3 -7cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;Y represents a group --(CH.sub.2)m--, where m represents 2, 3 or 4, or a group --X(CH.sub.2).sub.p --, where p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.4, where R.sup.4 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule;and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.Type: GrantFiled: May 26, 1989Date of Patent: September 3, 1991Assignee: Glaxo Group LimitedInventors: David E. Bays, Ian H. Coates, John Bradshaw, William L. Mitchell
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Patent number: 4939136Abstract: The invention relates to new anellated indole derivatives of general formula 2, ##STR1## wherein p1 R.sub.0 is alkyl or alkoxy having 1-4 C-atoms, phenylalkoxy having 1-3 C-atoms in the alkoxy group, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, or a group R.sub.7 S(O).sub.p, wherein R.sub.7 is alkyl having 1-4 C-atoms and p has the value 0, 1 or 2, or R.sub.0 is a group R.sub.8 R.sub.9 N, R.sub.8 R.sub.9 N--CO--CH.sub.2 -- or R.sub.8 R.sub.9 --N--CO wherein R.sub.8 and R.sub.9 are hydrogen or alkyl having 1-4 C-atoms or R.sub.8 R.sub.9 N forms a saturated 5- or 6-membered ring and n has the value 0, 1 or 2, Z together with the carbon atom and nitrogen atom to which Z is bound and the intermediate carbon atom, forms a heterocyclic group consisting of 5-8 ring atoms, in which, in addition to the nitrogen atom already present, a --CO--group or a second hetero atom from the group N, O, S, S-O or SO.sub.Type: GrantFiled: June 24, 1988Date of Patent: July 3, 1990Assignee: Duphar International Research B.V.Inventors: Hans H. Haeck, Derk Hamminga, Ineke Van Wijngaarden, Wouter Wouters
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Patent number: 4906755Abstract: The present invention is directed to a group of esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(3H)-ones and related compounds. The compounds are prepared from the appropriate carboxylic acids and alcohols by standard procedures or, where steric factors are significant, a new process which makes use of heavy metal salts of super acids can be used. The compounds involved are useful in the treatment of migraine and similar disorders and in cytotoxic drug-induced vomiting.Type: GrantFiled: June 30, 1989Date of Patent: March 6, 1990Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Maurice W. Gittos
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Patent number: 4870079Abstract: Fluoro-and hydroxy-derivatives of 5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines wherein the substituents are on non-benzenoid carbons are active anticonvulsants and antagonists of N-methyl-D-aspartate.Type: GrantFiled: March 30, 1988Date of Patent: September 26, 1989Assignee: Merck & Co., Inc.Inventors: Susan F. Britcher, Wayne J. Thompson, Terry A. Lyle, Sandor L. Varga
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Patent number: 4870080Abstract: 10,11-Dihydro-5H-dibenzo[a,d] cyclohepten-5,10-imines and derivatives thereof wherein one or the other or both benzo rings are hydrogenated are active anticonvulsants and atagonists of N-methyl-D-aspartate.Type: GrantFiled: May 5, 1988Date of Patent: September 26, 1989Assignee: Merck & Co., Inc.Inventors: Theresa R. Lamanec, Terry A. Lyle
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Patent number: 4868191Abstract: Novel alkaloid compounds that are derivatives of methaniminoetheno[d,e]acridine are derived from marine sponges of the genus Dercitus. These compounds and pharmaceutical compositions containing therapeutic effective amounts thereof are useful as antitumor and immunomodulatory medications.Type: GrantFiled: March 3, 1988Date of Patent: September 19, 1989Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: Shigeo Komoto, Y. A. Gunawardana
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Patent number: 4762831Abstract: A process for the preparation of a 1,8-bridged 4-quinolone-3-carboxylic acid of the formula ##STR1## wherein the substituents are defined hereinbelow. Some of the compound are new. The old and new compounds are antibacterials and promote animal growth.Type: GrantFiled: June 13, 1986Date of Patent: August 9, 1988Assignee: Bayer AktiengesellschaftInventors: Klaus Grohe, Michael Schriewer
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Patent number: 4668803Abstract: Novel organic compound of the basic formula ##STR1## which have substantial luminescent emission characteristics and advantages.Type: GrantFiled: July 1, 1985Date of Patent: May 26, 1987Assignee: Atlantic Richfield CompanyInventors: Elliot Berman, Brian A. Zentner