1,2- Or 2,1-thiazine Ring In The Tricyclo Ring System (e.g., Hydrogenated 1,2-benzothiazine In Tricyclo Ring System, Etc.) Patents (Class 544/33)
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Patent number: 9666805Abstract: The present invention relates to new semiconducting compounds having at least one optionally substituted bithiophene sulfonamide moiety. The compounds disclosed herein can exhibit high carrier mobility and/or efficient light absorption/emission characteristics, and can possess certain processing advantages such as solution-processability and/or good stability at ambient conditions.Type: GrantFiled: November 25, 2015Date of Patent: May 30, 2017Assignees: Northwestern University, Flexterra, Inc.Inventors: Antonio Facchetti, Tobin J. Marks, Yu Xia, Martin Drees, Ferdinand Melkonyan, Wei Zhao
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Patent number: 8816070Abstract: 5-[4-(2-Methylphenyl)-3-hydroxy-4H-1,2,4-triazol-5-yl]-2,4-dihydroxy-N-methyl-N-butylbenzamide is an HSP90 inhibitor and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: GrantFiled: December 11, 2007Date of Patent: August 26, 2014Assignee: Merck Patent GmbHInventors: Hans Michael Eggenweiler, Michael Wolf, Hans Peter Buchstaller, Christian Sirrenberg
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Patent number: 8618285Abstract: Novel triazole derivatives of the formula (I), in which R1-R6, and Y have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: GrantFiled: January 25, 2006Date of Patent: December 31, 2013Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Michael Wolf
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Publication number: 20130018045Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, A, B, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: July 12, 2012Publication date: January 17, 2013Applicant: ABBOTT LABORATORIESInventors: Keith W. Woods, Chunqui Lai, Thomas D. Penning, Julie M. Miyashiro
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Patent number: 8119795Abstract: Novel triazole derivatives of the formula (I) in which R1-R6 and Y have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: GrantFiled: April 20, 2007Date of Patent: February 21, 2012Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Michael Wolf, Hans-Peter Buchstaller, Christian Sirrenberg
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Patent number: 8053574Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.Type: GrantFiled: July 16, 2008Date of Patent: November 8, 2011Assignee: Novartis AGInventors: Ian Bruce, Darren Mark Legrand, James Dale, Thomas Anthony Hunt
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Publication number: 20090099159Abstract: A method of treating or preventing of a disease or condition associated with an increased level of isoforms of amyloid ? peptides (A?) and/or with a changed ratio of levels of A? isoforms and/or with the formation of plaques containing amyloid ? peptide (A?) isoforms in a mammal comprising administering to said mammal an therapeutically effective amount of a compound selected from the formulas Ia, Ib wherein V, W, Y, R2, R3, R5, R6, L1 and i are defined as in claim 1.Type: ApplicationFiled: December 17, 2008Publication date: April 16, 2009Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, BOEHRINGER INGELHEIM PHARMACEUTICALS, INC.Inventors: Klaus BORNEMANN, Guenter TRUMMLITZ, Bernd BECK, Frank SAMS-DODD, Dagmar KUGLER, Klaus KLINDER, Cornelia DORNER-CIOSSEK, Marcus KOSTKA
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Patent number: 7442790Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.Type: GrantFiled: June 28, 2007Date of Patent: October 28, 2008Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
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Patent number: 7026475Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5, n, and m, are as defined herein, or an enantiomer or diastereomer thereof, or a pharmacologically acceptable salt thereof, processes for preparing these compounds, and their use in pharmaceutical compositions.Type: GrantFiled: October 31, 2003Date of Patent: April 11, 2006Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Angelo Ceci, Klaus Klinder, Thomas Weiser, Karin Winter
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Patent number: 6974870Abstract: Disclosed are compounds of formula (I): wherein R1 and R2 are defined herein, which are useful as inhibitors of the kinase activity of the I?B kinase (IKK) complex. The compounds are therefore useful in the treatment of IKK mediated diseases including autoimmune diseases inflammatory diseases and cancer. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.Type: GrantFiled: December 6, 2003Date of Patent: December 13, 2005Assignee: Boehringer Ingelheim Phamaceuticals, Inc.Inventors: Charles L. Cywin, Can Mao, Jonathan Emeigh, Roman Wolfgang Fleck, Ming-Hong Hao, Eugene Hickey, Weimin Liu, Daniel Richard Marshall, Tina Morwick, Peter Nemoto, Ronald John Sorcek, Sanxing Sun, Jiang-Ping Wu, Erick Young, Darren DiSalvo, John Ginn, Pier Cirillo
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Publication number: 20040116412Abstract: Compounds of formula (I) 1Type: ApplicationFiled: October 31, 2003Publication date: June 17, 2004Applicant: Boehringer Ingelheim Pharma KGInventors: Angelo Ceci, Klaus Klinder, Thomas Weiser, Karin Winter
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Patent number: 6525045Abstract: The present invention relates to new positive allosteric AMPA receptor modulators of general formula (I) wherein R1, R2 R3, R4, R5 and R6 may have the meanings indicated in the specification and claims, processes for preparing them and their use as pharmaceutical compositions.Type: GrantFiled: January 31, 2001Date of Patent: February 25, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Karin Winter, Thomas Weiser, Stefan M. Blech, Angelo Ceci
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Publication number: 20020049317Abstract: The method of this invention prepares acylated cyclic compounds by contacting phenyl esters as acylating agents with cyclic compounds in the presence of a cyanide or fluoride catalyst.Type: ApplicationFiled: April 12, 2001Publication date: April 25, 2002Inventor: Paul Walter Wojtkowski
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Patent number: 6303638Abstract: Novel compounds are provided that modulate the neuronal nicotinic acetylcholine receptor (nAChR), particularly the mammalian nAChR (m-nAChR). The compounds are substituted pyridine derivatives such as analogs of 1-[(6-chloro-3-pyridinyl)methyl]-2-imidazolidine and 1-[(6-chloro-3-pyridinyl)methyl]-2-iminothiazole. Methods of using the novel m-nAChR modulators are also provided, including methods of using the compounds as m-nAChR probes and as therapeutic agents to treat mammalian individuals suffering from conditions, disorders or diseases that are responsive to administration of an m-nAChR modulator.Type: GrantFiled: August 20, 1999Date of Patent: October 16, 2001Assignee: The Regents of the University of CaliforniaInventors: Bachir Latli, John E. Casida
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Patent number: 5681834Abstract: Compounds of the following structure are disclosed: ##STR1## Wherein G, J and the two atoms of the thiophene ring to which they are attached are the group ##STR2##Type: GrantFiled: December 4, 1995Date of Patent: October 28, 1997Assignee: Alcon Laboratories, Inc.Inventors: Jesse A. May, Hwang-Hsing Chen, Anura Dantanarayana, Abdelmoula Namil
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Patent number: 5635537Abstract: A compound of the formula ##STR1## Z is hydrogen or halogen, Q is COR.sup.1 or 5-or 6-membered aryl which may contain 1 or 2 heteroatoms selected from N, 0 or S and may be substituted or fused wherein R is hydrogen or C.sub.1 -methyl (cis-configuration), R.sup.1 is C.sub.1 -C.sub.6 alkyl or an aromatic ring which may contain heteroatoms selected from O and S and may be substituted or fused to an optionally substituted benzene ring, R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.3 may be different groups defined in claim 1, and enantiomers/salts thereof, processes for preparation of said compounds, pharmaceutical preparations containing said compounds, use of and method of treatment of disorders in CNS by using said compounds.Type: GrantFiled: March 18, 1993Date of Patent: June 3, 1997Assignee: Astra AktiebolagInventors: Nils-Erik Anden, Berit C. E. Backlund Hook, Anna L. Bjork, Uli A. Hacksell, Sven-Erik Hillver, Ye Liu, Eva C. Mellin, Eva M. Persson, Karl J. Vallg.ang.rda, Hong Yu
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Patent number: 5599811Abstract: Novel benzothiazine dioxides which are antagonists of endothelin are described, as well as novel intermediates used in their preparation, methods for the preparation, and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.Type: GrantFiled: February 21, 1995Date of Patent: February 4, 1997Assignee: Warner-Lambert CompanyInventors: Kent A. Berryman, Amy M. Bunker, Annette M. Doherty, Jeremy J. Edmunds
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Patent number: 5308842Abstract: Conformationally constrained tricyclic derivatives of the thienodiazocine and thienothiadiazocine classes of compounds and ring homologs thereof are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.Type: GrantFiled: May 10, 1993Date of Patent: May 3, 1994Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello
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Patent number: 5274097Abstract: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A--denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X--denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --O--,n--denotes a number from 1 to 19, andB--denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.Type: GrantFiled: April 9, 1991Date of Patent: December 28, 1993Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Peter-Rudolf Seidel, Jorg Traber, Thomas Glaser
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Patent number: 5270307Abstract: Pyrrolo-(1,2-b)-(1,2)-benzothiazin-10-one is prepared which corresponds to the formula: ##STR1## This compound has been found to exhibit antimicrobial activity in industrial and commercial applications and compositions containing this compound are so employed.Type: GrantFiled: March 26, 1993Date of Patent: December 14, 1993Assignee: The Dow Chemical CompanyInventors: Dallas K. Bates, Kelley A. Tafel
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Patent number: 5250540Abstract: Aminomethyl-substituted 2,3-dihydropyrano[2,3-b]pyridines can be prepared by alkylation of corresponding amines. The novel aminomethyl-substituted dihydropyrano[2,3-b]pyridines can be used as active ingredients in medicaments, in particular for the treatment of disorders of the central nervous system.Type: GrantFiled: June 11, 1992Date of Patent: October 5, 1993Assignee: Bayer AktiengesellschaftInventors: Dieter Arlt, Hans-Georg Heine, Rudolf Schohe-Loop, Thomas Glaser, Jean M. V. De Vry
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Patent number: 5137892Abstract: Novel antibacterial compounds are disclosed having the formula ##STR1## as well as pharmaceutically acceptable salts, esters, amide and prodrugs thereof,wherein R.sup.1 is selected from the group consisting of (a) lower alkyl, (b) halo(lower alkyl), (c) lower alkyl(alkynyl), (d) lower cycloalkyl, (e) lower alkylamino, (f) nitrogen-containing aromatic heterocycle, (g) bicyclic alkyl and (h) phenyl;R.sup.2 is selected from the group consisting of hydrogen, lower alkyl, a pharmaceutically acceptable cation, and a prodrug ester group;R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen, halogen, amino, and lower alkyl;R.sup.5 is either a nitrogen-containing heterocycle or a nitrogen-containing spiro-bicyclic-heterocycle; andA is N or C--R.sup.6, wherein R.sup.6 is selected from the group consisting of hydrogen, halogen, lower alkyl, and lower alkoxy, or R.sup.1 and R.sup.Type: GrantFiled: December 12, 1990Date of Patent: August 11, 1992Assignee: Abbott LaboratoriesInventors: Daniel T. Chu, Curt S. Cooper
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Patent number: 5130313Abstract: This invention relates to compounds of formula: ##STR1## in which R.sub.1 denotesa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by an optionally substituted phenyl, optionally substituted 3-indolyl or 3-(5-hydroxyindolyl) radical,a 1-piperazinyl radical substituted in the 4-position by an optionally substituted phenyl, 1,2-benzisothiazol-3-yl, 1,2-benzisoxazol-3-yl or 2-pyridyl radical,a piperidino radical substituted in the 4-position by an optionally substituted phenyl, bis(4-fluorophenyl)methylene, 4-fluorobenzoyl, optionally substituted 2-oxo-1-benzimidazolinyl, optionally substituted 3-indolyl or 3-(5-hydroxyindolyl) radical, by two phenyl radicals or a hydroxyl radical and an optionally substituted phenyl radicalR.sub.2 denotes a radical SO.sub.2 R.sub.4 in which R.sub.4 denotes an alkyl or phenyl radical,R.sub.3 denotes a phenyl or naphthyl radical,or else R.sub.2 and R.sub.Type: GrantFiled: December 13, 1990Date of Patent: July 14, 1992Assignee: Rhone-Poulenc SanteInventors: Marie-Therese Comte, Claude Gueremy, Jean-Luc Malleron, Jean-Francois Peyronel, Alain Truchon
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Patent number: 5021438Abstract: Novel compounds having an affinity for 5-hydroxytryptamine receptors of the formula ##STR1## in which R.sup.1 stands for H, alkyl, aralkyl or heteroarylalkyl,X stands for H, OCH.sub.3, OH, SCH.sub.3, halogen, CN or CONH.sub.2,Y stands for a straight-chain or branched, saturated or unsaturated alkylene chain having up to 6 carbon atomsandZ stands for a group of the formula ##STR2## --OR.sup.4, --SO.sub.m R.sup.5, --COOR.sup.6 or CONR.sup.7 R.sup.8 or salts thereof.Type: GrantFiled: March 15, 1989Date of Patent: June 4, 1991Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber
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Patent number: 4968679Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: May 22, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4914101Abstract: R.sup.1 is hydrogen, halogen or C.sub.1 to C.sub.4 alkyl;R.sup.2 is hydrogen or C.sub.1 to C.sub.4 alkyl; and Ar is phenyl or phenyl substituted with one or more substituents selected from C.sub.1 to C.sub.4 alkyl, halo, trifluoromethyl, nitro, hydroxyl, halophenyl, or C.sub.1 to C.sub.4 alkoxy.The compounds are useful in treating inflammation or other prostaglandin or leukotriene mediated diseases.Type: GrantFiled: February 6, 1989Date of Patent: April 3, 1990Assignee: Pfizer Inc.Inventor: Anthony Marfat
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Patent number: 4874758Abstract: The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and method of use thereof, useful in the treatment of diseases in which products of lipoxygenase enzyme activity or the action of leukotrienes contribute to the pathological condition.Type: GrantFiled: March 4, 1988Date of Patent: October 17, 1989Assignee: Warner-Lambert CompanyInventors: Mary E. Carethers, Wiaczeslaw A. Centenko, David T. Connor, Elizabeth A. Johnson, John S. Kiely, Charles F. Schwender, Jagadish C. Sircar, Roderick J. Sorenson, Paul C. Unangst, Robert F. Bruns
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Patent number: 4873262Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: December 15, 1987Date of Patent: October 10, 1989Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4797482Abstract: The present invention relates to a process for the preparation of a 5-methyl-3-heteroaryl-2H,5H-1,3-oxazino[5,6-c] [1,2] benzothiazine-2,4-(3H)-dione 6,6-dioxide of the general formula I: ##STR1## in which R represents a heteroraryl radical, preferably substituted or unsubstituted pyrimidinyl or pyridyl, of the type consisting in reacting an amide of the general formula II: ##STR2## in which R.sup.1 represents a heteroarylamino radical, preferably substituted or unsubstituted pyrimidinylamino or pyridylamino, with a compound of the general formula III: ##STR3## in which R.sup.2 represents a C.sub.1 to C.sub.4 lower alkyl radical such as methyl or ethyl, an aryl radical such as phenyl, or an alkylaryl radical such as benzyl, wherein the reaction is carried out in an organic solvent selected from the group comprising pyridine, substituted pyridines such as 4-dimethylaminopyridine, 4-(pyrrolidin-1-yl)pyridine and 2,6-ditert.-butyl-4-methylpyridine, and mixtures thereof.Type: GrantFiled: April 15, 1987Date of Patent: January 10, 1989Assignee: Provesan S.A.Inventors: Jordi Constansa Frigola, Augusto Pinol Colombo, Juan Corominas Pares
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Patent number: 4752324Abstract: Herbicidally active novel nicotinic acid derivatives of the formula ##STR1## in which X represents hydroxyl, alkoxy or the radical --OM,whereinM represents one equivalent of an alkali metal or alkaline earth metal ion, or an optionally substituted ammonium ion, andHet represents isoxazolyl, pyrimidinyl or pyrazolyl each substituted by a substituent selected from the group consisting of alkyl, alkenyl, alkoxy, alkylthio, alkylamino, hydroxyl, mercapto, amino, alkylcarbonyl which is optionally substituted by halogen or alkoxy; cycloalkyl and in each case optionally substituted phenyl or naphthyl, or optionally substituted condensed cycloalkylpyrazolyl.Type: GrantFiled: November 5, 1986Date of Patent: June 21, 1988Assignee: Bayer AktiengesellschaftInventors: Rudolf Thomas, Peter Babczinski, Hans-Joachim Santel, Ludwig Eue, Robert R. Schmidt
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Patent number: 4741765Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.Type: GrantFiled: April 3, 1987Date of Patent: May 3, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
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Patent number: 4683306Abstract: Process for the preparation of 3,4-dihydro-2-substituted-4(or 3)-oxo-2H-1,2-thiazine-3(or 4)-carboxylic acid 1,1,-dioxide magnesium chelate derivatives and its acids by reacting appropriately 3,4-dihydro-2-substituted-4(or 3)-oxo-2H-1,2-thiazine 1,1-dixoides with alkylmagnesiumcarbonate and then hydrolyzing and its use as intermediates for the preparation of N-substituted-2-substituted-2H-1,2-thiazine-3(or 4)-carboxamide-1,1-dioxide derivatives, effective antiinflammatory agents.Type: GrantFiled: July 13, 1984Date of Patent: July 28, 1987Assignee: YuHan Corporation Co., Ltd.Inventors: Jung J. Suh, You H. Hong
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Patent number: 4678499Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]-pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.Type: GrantFiled: January 30, 1986Date of Patent: July 7, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
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Patent number: 4656265Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof wherein R is 2-pyridyl, 6-chloro-2-pyridyl, 6-methyl-2-pyridyl or 5-methylisoxazol-3-yl; useful as prodrug forms of the corresponding known oxicam antiinflammatory and analgesic agents, piroxicam, the corresponding 6-chloro-2-pyridyl and 6-methyl-2-pyridylcarboxamides, isoxicam and tenoxicam; methods for their use, pharmaceutical compositions containing them and a process for their preparation.Type: GrantFiled: June 21, 1984Date of Patent: April 7, 1987Assignee: Pfizer Inc.Inventors: Joseph G. Lombardino, Anthony Marfat
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Patent number: 4631276Abstract: Compounds of Formula I ##STR1## wherein R.sub.1 is a prostaglandin or prostacyclin residue;Y is oxygen, sulfur, imino, or N-(C.sub.1 -C.sub.4 -alkyl) imino;Q is (CR.sub.6 R.sub.7).sub.p wherein p is an integer of 0 to 3;R.sub.2 is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy or amino; C.sub.1 -C.sub.4 -alkoxycarbonyl; benzyloxycarbonyl; cyano; or di-C.sub.1 -C.sub.4 -alkylamino-carbonyl;R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 each independently is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy or amino; or aryl; andR.sub.3 and R.sub.4 together form a trimethylene, tetramethylene, or 1,3-butadienylene group when R.sub.2 and R.sub.5 together represent a direct bond;have valuable pharmacological properties, e.g., as blood-pressure-lowering or abortive agents.Type: GrantFiled: July 3, 1984Date of Patent: December 23, 1986Assignee: Schering AktiengesellschaftInventors: Helmut Vorbruggen, Walter Elger, Michael-Harold Town, Ekkehard Schillinger
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Patent number: 4563452Abstract: This invention relates to new derivatives of oxazinobenzothiazine-6,6-dioxide, to a process for the production thereof and to the use thereof as medicaments.The new derivatives according to the present invention correspond to the general formula I: ##STR1## wherein: R represents a linear or branched lower C.sub.1 -C.sub.4 alkyl radical, in particular the methyl and ethyl radicals,X represents an oxygen atom or a sulphur atom, andHet represents a mono- or bicyclic unsaturated heterocycle containing a nitrogen heteroatom in the ortho position relative to the link between the said heterocycle and the nitrogen atom of the oxazine ring, the said heterocycle optionally containing one or two other additional heteroatoms selected from nitrogen, oxygen and sulphur, and also being able to be substituted by one or two methyl radicals.Type: GrantFiled: June 8, 1983Date of Patent: January 7, 1986Assignee: Provesan S.A.Inventor: Jose Esteve Soler
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Patent number: 4563453Abstract: New thiazine derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen or acyl,R.sup.2 is hydrogen or lower alkyl,R.sup.3 is hydrogen, hydroxy, halogen, lower alkyl or lower alkoxy,Z is taken together with the adjacent carbon atoms to form an unsaturated heterocyclic ring which may be substituted with phenyl, halogen, acyl or lower alkyl, andthe heavy solid line means single or double bond,and pharmaceutically acceptable salts thereof, and processes for preparation thereof and pharmaceutical composition comprising the same.These derivatives and salts thereof are useful as antiinflammatory, analgesic and antirheumatic agents.Type: GrantFiled: October 9, 1984Date of Patent: January 7, 1986Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Masayuki Kato, Yosiharu Kasai
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Patent number: 4378358Abstract: 1,2 Benzothiazino[3,4-d]pyrazoles of the following general formula ##STR1## wherein R stands for a linear or branched (C.sub.2-4) alkyl chain bearing a substituent of formula ##STR2## in which the R" radicals may be the same or different and represent hydrogen, (C.sub.2-4)alkyl, (C.sub.4-7) cycloalkyl or, taken together with the adjacent nitrogen atom, may also represent a saturated, 5 to 7 membered heterocyclic ring containing from one to three heteroatoms independently selected from O,N and S, or R may represent the 1-ethyl-pyrrolidine-2-yl-methyl radical, and R' is hydrogen, a halogen atom or a (C.sub.1-4) alkyl radical; methods for their preparation; pharmaceutical compositions containing them. The compounds possess antiinflammatory, antipyretic and analgesic activity.Type: GrantFiled: July 1, 1981Date of Patent: March 29, 1983Assignee: Mediolanum Farmaceutici s.r.l.Inventor: Rinaldo Del Bono
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Patent number: 4348519Abstract: The invention relates to thiazine derivatives of the formula ##STR1## wherein R.sup.1 is lower alkyl and R.sup.2 is the residue of an aromatic heterocycle containing 1 to 4 hetero atoms optionally substituted by one or two lower alkyl groups, or a phenyl or benzyl group optionally substituted by halogen, hydroxy, lower alkyl, trifluoromethyl, nitro or lower alkoxy, and pharmaceutically acceptable salts thereof. The compounds of formula I are useful for the control or prevention of inflammation, pains, rheumatics and thromboses.Type: GrantFiled: May 16, 1980Date of Patent: September 7, 1982Assignee: Hoffmann-La Roche Inc.Inventor: Rudolf Pfister
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Patent number: 4311839Abstract: In one aspect, this invention relates to a method of synthesizing certain 3-(4'-OP-carbocyclic aryl)-3-(carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxides (and -2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxides) by reacting (a) a 3-(4'-OP-carbocyclic aryl)-benz[d]isothiazole-1,1-dioxide wherein P is a protecting group or a 3-(4'-OP-carbocyclic aryl)-naphtho[1,8-de]-1,2-thiazine-1,1-dioxide wherein P is a protecting group and (b) a carbocyclic aryllithium compound to give (c) the corresponding 3-(4'-OP-carbocyclic aryl)-3-(carbocyclic aryl)-2,3-dihydrobenz[d]-isothiazole-1,1-dioxide or the corresponding 3-(4'-OP-carbocyclic aryl)-3-(carbocyclic aryl)-2,3-dihydronaphtho-[1,8-de]-1,2-thiazine-1,1-dioxide.Type: GrantFiled: December 22, 1980Date of Patent: January 19, 1982Assignee: Polaroid CorporationInventors: Alan L. Borror, Louis Cincotta, James W. Foley, Marcis M. Kampe
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Patent number: 4283537Abstract: In one embodiment, the present invention is concerned with 3,3-disubstituted sulfam(na)phthaleins wherein one of the 3-substituents is derived from a perhalomethylcarbinol-substituted phenol or 1-naphthol useful as intermediates in the preparation of certain N-acylated sulfam(na)phthalein compounds, which compounds find utility, e.g., as pH-sensitive indicator dyes or photographic light-screening dyes.In another embodiment, the present invention is concerned with a method of synthesizing said sulfam(na)phthalein intermediates by reacting certain 3-substituted-benz[d]isothiazole-1,1-dioxides (or 3-substituted-naphtho[1,8-de]-1,2-thiazine-1,1-dioxides) and a 4-OLi-naphthyllithium compound or a 4-OLi-phenyllithium compound substituted in the 3-position with a lithiated perhalomethylcarbinol group.Type: GrantFiled: November 2, 1978Date of Patent: August 11, 1981Assignee: Polaroid CorporationInventors: Louis Cincotta, James W. Foley
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Patent number: 4259493Abstract: The present invention is concerned with novel 3,3-disubstituted-sulfam(na)phthaleins wherein one of the 3-substituents is derived from a 1-naphthol or a phenol substituted in the 2-position with a perhalomethylcarbinol group and wherein the N atom of the sulfam(na)phthalein ring is substituted with ##STR1## wherein R is alkyl or aryl or with ##STR2## wherein Y is hydrogen or an electron-withdrawing group, which compounds find utility, e.g., as pH-sensitive indicator dyes or as photographic light-screening dyes.Type: GrantFiled: November 2, 1978Date of Patent: March 31, 1981Assignee: Polaroid CorporationInventor: James W. Foley
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Patent number: 4259336Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen or alkyl of 1 to 3 carbon atoms; R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms; andR.sub.3 is aromatic hydrocarbyl of 6 to 10 carbon atoms or an aromatic heterocycle of 2 to 9 carbon atoms and 1 to 2 nitrogen atoms and/or an oxygen or a sulfur atom, where each of said aromatic substituents may in turn be substituted with one or two alkyls of 1 to 6 carbon atoms, halogen, hydroxyl, trifluoromethyl, halophenyl or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases; the compounds as well as their salts are useful as analgesics, antipyretics, antithrombotic and antiphlogistics.Type: GrantFiled: October 22, 1979Date of Patent: March 31, 1981Assignee: Boehringer Ingelheim GmbHInventors: Wolfhard Engel, Gunter Trummlitz, Ernst Seeger, Walter Haarmann, Gunther Engelhardt, Rainer Zimmermann
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Patent number: 4231929Abstract: This invention relates to phenol sulfam(na)phthaleins possessing a 2-(2'-halomethylbenzoyl) group substituted on the N atom of the sulfam(na)phthalein ring, which compounds find utility as photographic optical filter agents and filter agent precursors.Type: GrantFiled: September 23, 1977Date of Patent: November 4, 1980Assignee: Polaroid CorporationInventors: Stanley M. Bloom, Alan L. Borror, James W. Foley
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Patent number: 4210752Abstract: The present invention is concerned with synthesizing certain ##STR1## by reacting (a) a 3,3-disubstituted sulfam(na)phthalein wherein one of the 3-substituents is a 4'-hydroxy-1'-phenyl moiety or a 4'-hydroxy-1'-naphthyl moiety substituted in the 3'-position with a perhalomethylcarbinol group and (b) an acid halide, ##STR2## wherein W is chloro or bromo and Y is hydrogen or an electron-withdrawing group, preferably, in the presence of a zeolite molecular sieve or acid alumina to give (c) the corresponding ##STR3## The compounds produced are useful, for example, as pH-sensitive indicator dyes or as photographic light-screening dyes.Type: GrantFiled: November 2, 1978Date of Patent: July 1, 1980Assignee: Polaroid CorporationInventors: Louis Cincotta, James W. Foley
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Patent number: 4204061Abstract: This invention relates to phenol sulfam(na)phthaleins possessing a ##STR1## wherein R is selected from methyl, unsubstituted or substituted with one or two halo groups and phenyl, unsubstituted or substituted with alkyl, dimethylamino or nitro substituted on the N atom of the sulfam(na)phthalein ring, which compounds find utility as photographic optical filter agents and filter agent precursors.Type: GrantFiled: September 23, 1977Date of Patent: May 20, 1980Assignee: Polaroid CorporationInventors: Stanley M. Bloom, Alan L. Borror, James W. Foley
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Patent number: 4195180Abstract: This invention relates to 1-naphthol sulfam(na)phthaleins possessing a carbonyl moiety on the N atom of sulfam(na)phthalein ring, which compounds find utility, for example, as antihalation and filter dyes in photographic products and processes.Type: GrantFiled: September 23, 1977Date of Patent: March 25, 1980Assignee: Polaroid CorporationInventors: Alan L. Borror, Louis Cincotta, Ernest W. Ellis, James W. Foley
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Patent number: 4191689Abstract: This invention relates to certain 3,3-di(4'-OP-carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxides (and-2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxides) and to the preparation thereof by reacting (a) at least 2 equivalents of (i) a 4'-OP-carbocyclic aryllithium compound wherein P is a protecting group compatible with organometallic reagents or (ii) a 4'-OP-carbocyclic arylMgE compound wherein P is a protecting group compatible with organometallic reagents and E is chloro, bromo or iodo and (b) 1 equivalent of a compound selected from a 3-chlorobenz[d] isothiazole-1,1-dioxide and a 3-chloronaphtho[1,8-de]-1,2-thiazine-1,1-dioxide to give the corresponding 3,3-di(4'-OP-carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxide or the corresponding 3,3-di(4'-OP-carbocyclic aryl)-2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxide, which compounds are useful in the synthesis of phenol and 1-naphthol sulfam(na)-phthaleins employed, for example, as photographic optical filter agents and filter agentType: GrantFiled: September 23, 1977Date of Patent: March 4, 1980Assignee: Polaroid CorporationInventors: Stanley M. Bloom, Alan L. Borror, James W. Foley
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Patent number: 4178446Abstract: This invention relates to phenol sulfam(na)phthaleins possessing a ##STR1## group wherein Y represents an electron-withdrawing group substituted on the N atom of the sulfam(na)phthalein ring, which compounds find utility as photographic optical filter agents and filter agent precursors.Type: GrantFiled: September 23, 1977Date of Patent: December 11, 1979Assignee: Polaroid CorporationInventors: Stanley M. Bloom, Alan L. Borror, James W. Foley
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Patent number: 4178447Abstract: This invention relates to a method of synthesizing certain 3-(carbocyclic aryl)-3-(4'-OP-carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxides (and -2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxides) by reacting (a) a 4-OP-carbocyclic aryllithium compound wherein P is a protecting group and (b) a 3-(carbocyclic aryl)benz[d]isothiazole-1,1-dioxide wherein said 3-(carbocyclic aryl) moiety is other than a 3-(4'-OP-carbocyclic aryl) moiety to give (c) the corresponding 3-carbocyclic aryl)-3-(4'-OP-carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxide. The -2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxides are prepared in the same manner by reacting a 3-(carbocyclic aryl)naphtho[1,8-de]-1,2-thiazine-1,1-dioxide with said 4'-OP-carbocyclic aryllithium compound.Type: GrantFiled: September 23, 1977Date of Patent: December 11, 1979Assignee: Polaroid CorporationInventors: Alan L. Borror, James W. Foley, Marcis M. Kampe, John W. Lee, Jr.