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)
  • Patent number: 9666805
    Abstract: 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: Grant
    Filed: November 25, 2015
    Date of Patent: May 30, 2017
    Assignees: Northwestern University, Flexterra, Inc.
    Inventors: Antonio Facchetti, Tobin J. Marks, Yu Xia, Martin Drees, Ferdinand Melkonyan, Wei Zhao
  • Patent number: 8816070
    Abstract: 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: Grant
    Filed: December 11, 2007
    Date of Patent: August 26, 2014
    Assignee: Merck Patent GmbH
    Inventors: Hans Michael Eggenweiler, Michael Wolf, Hans Peter Buchstaller, Christian Sirrenberg
  • Patent number: 8618285
    Abstract: 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: Grant
    Filed: January 25, 2006
    Date of Patent: December 31, 2013
    Assignee: Merck Patent GmbH
    Inventors: Hans-Michael Eggenweiler, Michael Wolf
  • Publication number: 20130018045
    Abstract: 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: Application
    Filed: July 12, 2012
    Publication date: January 17, 2013
    Applicant: ABBOTT LABORATORIES
    Inventors: Keith W. Woods, Chunqui Lai, Thomas D. Penning, Julie M. Miyashiro
  • Patent number: 8119795
    Abstract: 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: Grant
    Filed: April 20, 2007
    Date of Patent: February 21, 2012
    Assignee: Merck Patent GmbH
    Inventors: Hans-Michael Eggenweiler, Michael Wolf, Hans-Peter Buchstaller, Christian Sirrenberg
  • Patent number: 8053574
    Abstract: 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: Grant
    Filed: July 16, 2008
    Date of Patent: November 8, 2011
    Assignee: Novartis AG
    Inventors: Ian Bruce, Darren Mark Legrand, James Dale, Thomas Anthony Hunt
  • Publication number: 20090099159
    Abstract: 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: Application
    Filed: December 17, 2008
    Publication date: April 16, 2009
    Applicants: 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
  • Patent number: 7442790
    Abstract: 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: Grant
    Filed: June 28, 2007
    Date of Patent: October 28, 2008
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
  • Patent number: 7026475
    Abstract: 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: Grant
    Filed: October 31, 2003
    Date of Patent: April 11, 2006
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Angelo Ceci, Klaus Klinder, Thomas Weiser, Karin Winter
  • Patent number: 6974870
    Abstract: 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: Grant
    Filed: December 6, 2003
    Date of Patent: December 13, 2005
    Assignee: 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
  • Publication number: 20040116412
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: October 31, 2003
    Publication date: June 17, 2004
    Applicant: Boehringer Ingelheim Pharma KG
    Inventors: Angelo Ceci, Klaus Klinder, Thomas Weiser, Karin Winter
  • Patent number: 6525045
    Abstract: 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: Grant
    Filed: January 31, 2001
    Date of Patent: February 25, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Karin Winter, Thomas Weiser, Stefan M. Blech, Angelo Ceci
  • Publication number: 20020049317
    Abstract: 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: Application
    Filed: April 12, 2001
    Publication date: April 25, 2002
    Inventor: Paul Walter Wojtkowski
  • Patent number: 6303638
    Abstract: 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: Grant
    Filed: August 20, 1999
    Date of Patent: October 16, 2001
    Assignee: The Regents of the University of California
    Inventors: Bachir Latli, John E. Casida
  • Patent number: 5681834
    Abstract: 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: Grant
    Filed: December 4, 1995
    Date of Patent: October 28, 1997
    Assignee: Alcon Laboratories, Inc.
    Inventors: Jesse A. May, Hwang-Hsing Chen, Anura Dantanarayana, Abdelmoula Namil
  • Patent number: 5635537
    Abstract: 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: Grant
    Filed: March 18, 1993
    Date of Patent: June 3, 1997
    Assignee: Astra Aktiebolag
    Inventors: 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
  • Patent number: 5599811
    Abstract: 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: Grant
    Filed: February 21, 1995
    Date of Patent: February 4, 1997
    Assignee: Warner-Lambert Company
    Inventors: Kent A. Berryman, Amy M. Bunker, Annette M. Doherty, Jeremy J. Edmunds
  • Patent number: 5308842
    Abstract: 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: Grant
    Filed: May 10, 1993
    Date of Patent: May 3, 1994
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Patent number: 5274097
    Abstract: 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: Grant
    Filed: April 9, 1991
    Date of Patent: December 28, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Schohe, Peter-Rudolf Seidel, Jorg Traber, Thomas Glaser
  • Patent number: 5270307
    Abstract: 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: Grant
    Filed: March 26, 1993
    Date of Patent: December 14, 1993
    Assignee: The Dow Chemical Company
    Inventors: Dallas K. Bates, Kelley A. Tafel
  • Patent number: 5250540
    Abstract: 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: Grant
    Filed: June 11, 1992
    Date of Patent: October 5, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Dieter Arlt, Hans-Georg Heine, Rudolf Schohe-Loop, Thomas Glaser, Jean M. V. De Vry
  • Patent number: 5137892
    Abstract: 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: Grant
    Filed: December 12, 1990
    Date of Patent: August 11, 1992
    Assignee: Abbott Laboratories
    Inventors: Daniel T. Chu, Curt S. Cooper
  • Patent number: 5130313
    Abstract: 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: Grant
    Filed: December 13, 1990
    Date of Patent: July 14, 1992
    Assignee: Rhone-Poulenc Sante
    Inventors: Marie-Therese Comte, Claude Gueremy, Jean-Luc Malleron, Jean-Francois Peyronel, Alain Truchon
  • Patent number: 5021438
    Abstract: 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: Grant
    Filed: March 15, 1989
    Date of Patent: June 4, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber
  • Patent number: 4968679
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: May 22, 1989
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4914101
    Abstract: 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: Grant
    Filed: February 6, 1989
    Date of Patent: April 3, 1990
    Assignee: Pfizer Inc.
    Inventor: Anthony Marfat
  • Patent number: 4874758
    Abstract: 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: Grant
    Filed: March 4, 1988
    Date of Patent: October 17, 1989
    Assignee: Warner-Lambert Company
    Inventors: 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
  • Patent number: 4873262
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: December 15, 1987
    Date of Patent: October 10, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4797482
    Abstract: 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: Grant
    Filed: April 15, 1987
    Date of Patent: January 10, 1989
    Assignee: Provesan S.A.
    Inventors: Jordi Constansa Frigola, Augusto Pinol Colombo, Juan Corominas Pares
  • Patent number: 4752324
    Abstract: 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: Grant
    Filed: November 5, 1986
    Date of Patent: June 21, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Thomas, Peter Babczinski, Hans-Joachim Santel, Ludwig Eue, Robert R. Schmidt
  • Patent number: 4741765
    Abstract: 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: Grant
    Filed: April 3, 1987
    Date of Patent: May 3, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
  • Patent number: 4683306
    Abstract: 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: Grant
    Filed: July 13, 1984
    Date of Patent: July 28, 1987
    Assignee: YuHan Corporation Co., Ltd.
    Inventors: Jung J. Suh, You H. Hong
  • Patent number: 4678499
    Abstract: 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: Grant
    Filed: January 30, 1986
    Date of Patent: July 7, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
  • Patent number: 4656265
    Abstract: 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: Grant
    Filed: June 21, 1984
    Date of Patent: April 7, 1987
    Assignee: Pfizer Inc.
    Inventors: Joseph G. Lombardino, Anthony Marfat
  • Patent number: 4631276
    Abstract: 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: Grant
    Filed: July 3, 1984
    Date of Patent: December 23, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Vorbruggen, Walter Elger, Michael-Harold Town, Ekkehard Schillinger
  • Patent number: 4563452
    Abstract: 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: Grant
    Filed: June 8, 1983
    Date of Patent: January 7, 1986
    Assignee: Provesan S.A.
    Inventor: Jose Esteve Soler
  • Patent number: 4563453
    Abstract: 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: Grant
    Filed: October 9, 1984
    Date of Patent: January 7, 1986
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Ikuo Ueda, Masayuki Kato, Yosiharu Kasai
  • Patent number: 4378358
    Abstract: 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: Grant
    Filed: July 1, 1981
    Date of Patent: March 29, 1983
    Assignee: Mediolanum Farmaceutici s.r.l.
    Inventor: Rinaldo Del Bono
  • Patent number: 4348519
    Abstract: 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: Grant
    Filed: May 16, 1980
    Date of Patent: September 7, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Rudolf Pfister
  • Patent number: 4311839
    Abstract: 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: Grant
    Filed: December 22, 1980
    Date of Patent: January 19, 1982
    Assignee: Polaroid Corporation
    Inventors: Alan L. Borror, Louis Cincotta, James W. Foley, Marcis M. Kampe
  • Patent number: 4283537
    Abstract: 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: Grant
    Filed: November 2, 1978
    Date of Patent: August 11, 1981
    Assignee: Polaroid Corporation
    Inventors: Louis Cincotta, James W. Foley
  • Patent number: 4259493
    Abstract: 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: Grant
    Filed: November 2, 1978
    Date of Patent: March 31, 1981
    Assignee: Polaroid Corporation
    Inventor: James W. Foley
  • Patent number: 4259336
    Abstract: 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: Grant
    Filed: October 22, 1979
    Date of Patent: March 31, 1981
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Wolfhard Engel, Gunter Trummlitz, Ernst Seeger, Walter Haarmann, Gunther Engelhardt, Rainer Zimmermann
  • Patent number: 4231929
    Abstract: 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: Grant
    Filed: September 23, 1977
    Date of Patent: November 4, 1980
    Assignee: Polaroid Corporation
    Inventors: Stanley M. Bloom, Alan L. Borror, James W. Foley
  • Patent number: 4210752
    Abstract: 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: Grant
    Filed: November 2, 1978
    Date of Patent: July 1, 1980
    Assignee: Polaroid Corporation
    Inventors: Louis Cincotta, James W. Foley
  • Patent number: 4204061
    Abstract: 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: Grant
    Filed: September 23, 1977
    Date of Patent: May 20, 1980
    Assignee: Polaroid Corporation
    Inventors: Stanley M. Bloom, Alan L. Borror, James W. Foley
  • Patent number: 4195180
    Abstract: 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: Grant
    Filed: September 23, 1977
    Date of Patent: March 25, 1980
    Assignee: Polaroid Corporation
    Inventors: Alan L. Borror, Louis Cincotta, Ernest W. Ellis, James W. Foley
  • Patent number: 4191689
    Abstract: 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 agent
    Type: Grant
    Filed: September 23, 1977
    Date of Patent: March 4, 1980
    Assignee: Polaroid Corporation
    Inventors: Stanley M. Bloom, Alan L. Borror, James W. Foley
  • Patent number: 4178446
    Abstract: 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: Grant
    Filed: September 23, 1977
    Date of Patent: December 11, 1979
    Assignee: Polaroid Corporation
    Inventors: Stanley M. Bloom, Alan L. Borror, James W. Foley
  • Patent number: 4178447
    Abstract: 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: Grant
    Filed: September 23, 1977
    Date of Patent: December 11, 1979
    Assignee: Polaroid Corporation
    Inventors: Alan L. Borror, James W. Foley, Marcis M. Kampe, John W. Lee, Jr.