Hetero Ring In Ionically Bonded Moiety Patents (Class 544/109)
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Patent number: 10414747Abstract: Compounds of general formula (Ia), compounds of general formula (Ia?), compounds of general formula (Ib), compounds of general formula (Ib?), compounds of general formula (I), compounds of general formula (I?), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, R6, R8, R9, X1, X2, and X3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds of the disclosure.Type: GrantFiled: October 2, 2017Date of Patent: September 17, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Michael D. Altman, Brandon D. Cash, Wonsuk Chang, Jared N. Cumming, Andrew M. Haidle, Timothy J. Henderson, James P. Jewell, Matthew A. Larsen, Rui Liang, Jongwon Lim, Min Lu, Ryan D. Otte, Tony Siu, Benjamin Wesley Trotter, Sriram Tyagarajan
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Publication number: 20140094602Abstract: Described is pentamycin in a purity exceeding 95%, certain polymorphs and solvates of pentamycin, processes for their manufacture, and a method for decreasing the rate of degradation of pentamycin.Type: ApplicationFiled: July 22, 2013Publication date: April 3, 2014Applicant: Biolotus Biotechnology AGInventors: Karl REUTER, Victor Meier, Florian Stolz, Dieter Krimmer, Cees Winninps
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Publication number: 20140005384Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.Type: ApplicationFiled: September 3, 2013Publication date: January 2, 2014Applicant: Pfizer Inc.Inventors: Anthony Michael Campeta, Joseph Francis Krzyzaniak, Jason Albert Leonard
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Publication number: 20120264934Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.Type: ApplicationFiled: June 29, 2012Publication date: October 18, 2012Inventors: Anthony Michael Campeta, Joseph F. Krzyzaniak, Jason Albet Leonard
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Patent number: 8067412Abstract: Disclosed are macrocyclic compounds of formulae I-V, which are analogs of the pochonin resorcylic acid lactones, and processes for the preparation of the compounds. The compounds disclosed are useful as inhibitors of kinases and Heat Shock Protein 90 (HSP 90). Also disclosed are pharmaceutical compositions comprising an effective kinase-inhibiting amount or an effective HSP90-inhibiting amount of the compounds and methods for the treatment of disorders that are mediated by kinases and HSP90.Type: GrantFiled: August 10, 2007Date of Patent: November 29, 2011Assignees: Universite de Strasbourg, Le Centre National de la Recherche ScientifiqueInventors: Nicolas Winssinger, Sofia Barluenga, Martin Karplus
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Patent number: 8034811Abstract: The invention relates to compounds of general formula I wherein D, E, F, G, W, Y, R1, A, R9, X, B, R8 are as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for treating diseases associated with deregulated angiogenesis, such as cancer.Type: GrantFiled: December 2, 2004Date of Patent: October 11, 2011Assignee: Leo Pharma A/SInventors: Jef Fensholdt, Jacob Thorhauge, Bjarne Nørremark
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Publication number: 20110166133Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Ros, KDR, FMS, C-FMS, FLT3, c-Kit, JAK2, JAK3, Aurora, PDGFR, Lck, TrkA, TrkB, TrkC, IGF-IR, ALK4, ALK5 and ALK or combinations thereof.Type: ApplicationFiled: May 7, 2009Publication date: July 7, 2011Applicant: IRM LLCInventors: Pamela A. Albaugh, Ha-Soon Choi, Gregory Chopiuk, Yi Fan, Paul Vincent Rucker, Zhicheng Wang
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Publication number: 20110077398Abstract: Described is pentamycin in a purity exceeding 95%, certain polymorphs and solvates of pentamycin, processes for their manufacture, and a method for decreasing the rate of degradation of pentamycin.Type: ApplicationFiled: March 20, 2009Publication date: March 31, 2011Inventors: Karl Reuter, Viktor Meier, Florian Stolz, Dieter Krimmer, Cees Winninps
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Patent number: 7897601Abstract: A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, is useful in treating diseases, disorders, or conditions such as obesity, metabolic disorders, addiction, diseases of the central nervous system, cardiovascular disorders, respiratory disorders, and gastrointestinal disorders.Type: GrantFiled: January 16, 2007Date of Patent: March 1, 2011Assignees: Intervet, Inc., Intervet International B.V.Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Martin C. Clasby, Keith A. Eagen, Jack D. Scott, Yuguang Wang, Yan Xia, William J. Greenlee
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Publication number: 20100292467Abstract: Disclosed is a chemical compound having the structure: wherein R1 is an all group, aryl group, alkylaryl group or arylalkyl group with at least 23 carbon atoms, R2 is an alkylene group, arylene group, alkyarylene group or arylalkylene group with at least 2 carbons and X is a quaternary ammonium salt.Type: ApplicationFiled: May 18, 2009Publication date: November 18, 2010Applicant: XEROX CORPORATIONInventors: Adela GOREDEMA, Aaron STRONG, Peter ODELL, C. Geoffrey ALLEN, Mihaela Maria BIRAU
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Patent number: 7767671Abstract: This invention provides a compound of Formula 1 where Ar, X, R1, R2, R3, and R4 are defined herein, or a pharmaceutically acceptable salt thereof useful in the prevention or inhibition of diseases associated with the Ras/Raf/MEK signaling cascade in a mammal, such as neoplasms, strokes, osteoporosis, cancer, rheumatoid arthritis, inflammatory disease, polycystic kidney disease, and colonic polyps, and methods of making the compounds of formula 1 and intermediates.Type: GrantFiled: September 23, 2008Date of Patent: August 3, 2010Assignee: WyethInventors: Dan Maarten Berger, Dennis William Powell, Biqi Wu
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Patent number: 7745436Abstract: This invention relates to disalt nitrogen-heteroaryl inhibitors of IL-12 production, and related methods and pharmaceutical compositions.Type: GrantFiled: April 13, 2005Date of Patent: June 29, 2010Assignee: Synta Pharmaceuticals CorporationInventors: Elena Kostik, Lijun Sun
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Patent number: 7622497Abstract: The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: December 17, 2004Date of Patent: November 24, 2009Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Songchun Jiang, Han-Zhong Zhang
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Publication number: 20090253905Abstract: The invention relates to a method for producing onium salts comprising alkyl anions or aryl sulfonate anions or alkyl carboxylate anions or acryl carboxylate anions by reacting an onium halide with an alkyl silyl ester or trialkyl silyl ester of an alkyl sulfonic acid or aryl sulfonic acid or an alkyl carboxylic acid or aryl carboxylic acid or the anhydrides thereof.Type: ApplicationFiled: November 18, 2005Publication date: October 8, 2009Inventors: Nikolai (Mykola) Ignatyev, Urs Weiz-Biermann, Andriy Kucheryna, Helge Willner
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Patent number: 7449460Abstract: This invention provides a compound of Formula 1 where Ar, X, R1, R2, R3, and R4 are defined herein, or a pharmaceutically acceptable salt thereof useful in the prevention or inhibition of diseases associated with the Ras/Raf/MEK signaling cascade in a mammal, such as neoplasms, strokes, osteoporosis, cancer, rheumatoid arthritis, inflammatory disease, polycystic kidney disease, and colonic polyps, and methods of making the compounds of formula 1 and intermediates.Type: GrantFiled: February 16, 2005Date of Patent: November 11, 2008Assignee: WyethInventors: Dan Maarten Berger, Dennis William Powell, Biqi Wu
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Patent number: 6903094Abstract: The present invention relates to a compound of the formula [1?] ? wherein R2 is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R5 is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R5 may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1?] as an active ingredient. The compound [1?] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1?] as a nociceptin antagonist or analgesic.Type: GrantFiled: May 10, 2002Date of Patent: June 7, 2005Assignee: Japan Tabacco, Inc.Inventors: Hisashi Shinkai, Takao Ito, Hideki Yamada
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Patent number: 6699858Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R1 and R2 each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 and R4 are both halogen; or R3 is halogen and R4 is hydrogen; or R3 is hydrogen and R4 is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.Type: GrantFiled: November 12, 2002Date of Patent: March 2, 2004Inventors: José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Pilar Gil-Lopetegui
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Patent number: 6613762Abstract: The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III: wherein R1-R5 are defined in the specification.Type: GrantFiled: February 6, 2002Date of Patent: September 2, 2003Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Han-Zhong Zhang, Shailaja Kasibhatla, Federico C. Gaeta
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Patent number: 6511976Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R1 and R2 each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 and R4 are both halogen; or R3 is halogen and R4 is hydrogen; or R3 is hydrogen and R4 is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.Type: GrantFiled: April 6, 2000Date of Patent: January 28, 2003Assignee: Jannsen Pharmaceutica, N.V.Inventors: José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Pilar Gil-Lopetegui, Adolfo Díaz-Martinez
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Patent number: 6472388Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.Type: GrantFiled: November 6, 2001Date of Patent: October 29, 2002Assignee: Pfizer IncInventor: Harry Ralph Howard
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Patent number: 6462041Abstract: The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III: wherein R1-R5 are defined herein. The present invention also relates to the discovery that compounds having Formula I-III are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled cell growth and spread of abnormal cells occurs.Type: GrantFiled: February 1, 2000Date of Patent: October 8, 2002Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Han-Zhong Zhang, Yan Wang, Ben Tseng, Shailaja Kasibhatla, John A. Drewe
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Patent number: 6403791Abstract: A compound of the formula wherein R1 is C1-3 alkyl optionally substituted with one or more fluorines; R2 is C1-6 alkyl, cycloalkyl or NR4R5; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) NR4R5 is a nitrogen-containing heterocyclic ring; R6 is C1-3 alkyl; and R7 and R8, which are the same or different, each represents C1-3 alkyl, halogen, CF3 or CN; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: February 9, 2001Date of Patent: June 11, 2002Assignee: Darwin Discovery, Ltd.Inventors: Hazel Joan Dyke, Alan Findlay Haughan, Christopher Lowe, George Martin Buckley, Richard John Davenport, Andrew Sharpe, Hannah Jayne Kendall, Verity Margaret Sabin, John Gary Montana, Catherine Louise Picken
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Patent number: 6376489Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory disease and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.Type: GrantFiled: December 7, 2000Date of Patent: April 23, 2002Assignee: ICOS CorporationInventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Laurence E. Burgess, Stephen T. Schlachter
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Patent number: 6342497Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1 and R2 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.Type: GrantFiled: September 7, 1999Date of Patent: January 29, 2002Assignee: Pfizer IncInventor: Robert Gerald Linde, II
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Patent number: 6096740Abstract: The present invention relates to pharmaceutical compositions for preventing or alleviating neurotoxicity. Said pharmaceutical compositions comprise as their active ingredient the stereospecific (+) enantiomers, having (3S,4S) configuration, of .DELTA..sup.6 -tetrahydrocannabinol (THC) type compounds of general formula (I), as defined hereinbelow.Type: GrantFiled: September 28, 1998Date of Patent: August 1, 2000Assignees: Ramot University Authority for Applied Research and Industrial Development Ltd., Yissum Research Develpoment Company of the Hebrew University in JersusalemInventors: Raphael Mechoulam, Emil Pop, Mordechai Sokolovsky, Yoel Kloog, Anat Biegon
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Patent number: 6030952Abstract: The present invention provides novel heteroaryl compounds having the general formula (I): ##STR1## their pharmaceutical compositions to be used as human and veterinary medicine, particularly in the treatment of dermatological, rheumatic, respiratory, cardiovascular and ophthalmologic conditions, and their use in cosmetic compositions.Type: GrantFiled: October 13, 1998Date of Patent: February 29, 2000Assignee: Centre International de Recherches Dermatologioues galdermaInventors: Philippe Diaz, Bruno Charpentier
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Patent number: 5856520Abstract: A novel substituted benzenedithiol metal complex represented by the general formula (1) is provided. The substituted benzenedithiol metal complex is useful as a singlet oxygen quencher and as an optical data recording medium per se. ##STR1## wherein M is a transition metal; A.sup.+ is a quaternary ammonium group; and R is an organic group selected from the group consisting of organic groups represented by the formulae (i), (ii), (iii) and (iv): ##STR2## (wherein R.sup.1 is an alkyl group having 1 to 4 carbon atoms), ##STR3## (wherein n is 3, 4 or 5), ##STR4## (wherein R.sup.2 is one of a hydrogen atom and a substitutent having 1 to 4 carbon atoms).Type: GrantFiled: October 20, 1997Date of Patent: January 5, 1999Assignee: Sumitomo Seika Chemicals Co., Ltd.Inventors: Kazuyoshi Hirako, Satoshi Kimura, Michio Suzuki
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Patent number: 5739318Abstract: The present invention relates to labelling agents comprising non-proteinaceous boronic acid conjugates having absorption maxima at not less than 600 nm, said label being provided by e.g., an azine, triphenylmethane, cyanine or phthalocyanine dye. The labelling agents are useful in the estimation and quantification of cisdiols such as glycosylated haemoglobin, by virtue of the substantially total absence of overlap with the absorption spectrum of haemoglobin. Oxazine and thiazine dyes exhibiting similar absorption characteristics and containing other activated moieties are similarly useful labelling agents, especially in the presence of haemoglobin.Type: GrantFiled: July 12, 1993Date of Patent: April 14, 1998Assignee: Axis Research ASInventors: Frank Frantzen, Erling Sundrehagen
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Patent number: 5637703Abstract: The invention concerns chemical compounds, derivatives of genistein, which exhibit pronounced immunosuppressant and antitumor activity. In particular, the invention concerns compounds having general formula 1, where R.sup.1, R.sup.2, R.sup.3 are the same or different, R.sup.1 denotes hydrogen or alkyl, R.sup.2 and R.sup.3 are the same or different and denote hydrogen, alkyl or aryl, or R.sup.2 and R.sup.3 are taken together with the nitrogen to which they are connected to form a heterocycle ring.Type: GrantFiled: August 13, 1996Date of Patent: June 10, 1997Assignee: Drug InstituteInventors: Aleksander P. Mazurek, Krzysztof Biniecki, Lech Kozerski
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Patent number: 5475119Abstract: Ionic monomeric diallylammonium compounds having a targeted combination of diallylammonium cations with selected anions have particularly high and constant charge control properties and very good heat stabilities and dispersibilities.The compounds according to the invention are outstandingly suitable for use as colorless charge control agents in toners and developers for electrophotographic recording processes and for use as charge-improving agents in powders and paints for surface coating, in particular in triboelectrically or electrokinetically sprayed powder paints.Type: GrantFiled: December 17, 1992Date of Patent: December 12, 1995Assignee: Hoechst AktiengesellschaftInventors: Rudiger Baur, Hans-Tobias Macholdt
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Patent number: 5373018Abstract: The invention relates to the compound of formula (I) ##STR1## wherein A represents an unsubstituted ethenyl group in the trans (E) configuration or a physiologically acceptable salt or metabilically labile ester thereof which are antagonists of excitatory amino acids, to processes for their preparation and to their use in medicine.Type: GrantFiled: April 15, 1993Date of Patent: December 13, 1994Assignee: Glaxo S.p.A.Inventors: Alfredo Cugola, Giovanni Gaviraghi
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Patent number: 5364859Abstract: Disclosed are imidazonaphthyridine derivatives represented by formula (I) ##STR1## wherein: R.sup.1 represents lower alkyl or substituted or unsubstituted aryl; andX-Y-Z represents ##STR2## wherein R.sup.2 represents hydrogen, lower alkyl, alkenyl, aralkenyl, or --C (R.sup.5) H--(CH.sub.2).sub.n --R.sup.4 (wherein R.sup.4 represents substituted or unsubstituted aryl, substituted or unsubstituted pyridyl, substituted or unsubstituted furyl, hydroxy-substituted lower alkyl, lower alkanoyloxy, morpholino, lower alkanoyl, carboxy, lower alkoxycarbonyl, cycloalkyl, hydroxy, lower alkoxy, halogen or NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 independently represents hydrogen or lower alkyl; R.sup.5 represents hydrogen, lower alkyl, or phenyl; and n represents an integer of 0 to 3); and R.sup.3 represents hydrogen, mercapto, hydroxy, lower alkyl, or aryl and pharmaceutically acceptable sails thereof.The compounds show a potent anti-inflammatory, anti-allergic and broncho-dilative activity.Type: GrantFiled: December 29, 1992Date of Patent: November 15, 1994Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Fumio Suzuki, Takeshi Kuroda, Shigeto Kitamura, Kenji Ohmori
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Patent number: 5243053Abstract: This invention provides new stabilized methylene Meldrum's acid precursors, a process for their preparation, and a process for using such compounds in the preparation of methylene Meldrum's acid.Type: GrantFiled: February 26, 1992Date of Patent: September 7, 1993Assignee: Eli Lilly and CompanyInventor: Mohammad Zia-Ebrahimi
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Patent number: 5126368Abstract: The invention describes the novel compound 6(Z)-8-([2,4,5-cis]-4-o-hydroxyphenyl-2-trifluoromethyl-1,3-dioxan-5-yl)oc tenoic acid of formula I and its pharmaceutically acceptable salts and pharmaceutical compositions, which are of value in treating certain pulmonary and/or vascular disorders. Also described are various processes for the manufacture of the novel compound and intermediates for use therein.Type: GrantFiled: August 10, 1990Date of Patent: June 30, 1992Assignee: Imperial Chemical Industries plcInventor: Michael J. Smithers
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Patent number: 5091169Abstract: N,N'-bis-(pyridoxal-5-phosphate)-alkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal-5-phosphate)-1,2-cycloalkylenediamine-N,N'-diacetic acids, and N,N'-bis-(pyridoxal-5-phosphate)-1,2-arylenediamine-N,N'-diacetic acids, the corresponding monophosphate compounds and monoacetic acid compounds, and their salts and esters form stable, highly soluble chelates with paramagnetic metal ions, and are highly effective NMRI contrast agents. Preferred contrast agents are paramagnetic ion chelates of N,N'-bis-(pyridoxal-5-phosphate)ethylenediamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-cyclohexylenediamine-N,N'diaceti c acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-arylenediamine-N,N'-diacetic acid, and the soluble calcium salts thereof.Type: GrantFiled: June 23, 1989Date of Patent: February 25, 1992Assignee: Salutar, Inc.Inventors: Scott M. Rocklage, Steven C. Quay
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Patent number: 4992555Abstract: N,N'-bis-(pyridoxal-5-phosphate)-alkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal-5-phosphate)-1,2-cycloalkylenediamine-N,N'-diacetic acids, and N,N'-bis-(pyridoxal-5-phosphate)-1,2-arylenediamine-N,N'-diacetic acids, the corresponding monophosphate compounds and monoacetic acid compounds, and their salts and esters form stable, highly soluble chelates with paramagnetic metal ions, and are highly effective NMRI contrast agents. Preferred contrast agents are paramagnetic ion chelates of N,N'-bis-(pyridoxal-5-phosphate)ethylenediamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-cyclohexylenediamine-N,N'-diacet ic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-arylenediamine-N,N'-diacetic acid, and the soluble calcium salts thereof.Type: GrantFiled: June 23, 1989Date of Patent: February 12, 1991Assignee: Salutar, Inc.Inventors: Scott M. Rocklage, Steven C. Quay
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Patent number: 4969950Abstract: Triazole compounds of the formulae Ia and Ib ##STR1## where R.sup.1 is hydrogen or cyclopropyl, or is C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.4 -alkenyl or C.sub.2 -C.sub.4 -alkynyl, each of which is unsubstituted or substituted by methyl, ethyl, ethenyl, ethynyl, hydroxyl, fluorine, chlorine, bromine or C.sub.1 -C.sub.4 -alkoxy, or is C.sub.1 -C.sub.4 -alkoxy, C.sub.2 -C.sub.4 -alkenyloxy or C.sub.2 -C.sub.4 -alkynyloxy,R.sup.2 and R.sup.3 independently of one another are each hydrogen, straight-chain or branched C.sub.1 -C.sub.3 -alkyl, and R.sup.2 and R.sup.3 together may furthermore form a carbocyclic ring which has up to six members in each ring system and may possess bridge members, with the proviso that, in formula Ia, two or more of the radicals R.sup.1 -R.sup.3 are not hydrogen, and is hydrogen, an acyl radical CO-R.sup.5 or a sulfonyl radical SO.sub.2 R.sup.5, R.sup.5 being straight-chain or branched C.sub.1 -C.sub.Type: GrantFiled: May 17, 1988Date of Patent: November 13, 1990Assignee: BASF AktiengesellschaftInventors: Manfred Lauer, Hubert Sauter, Karl Roeser, Johann Jung, Wilhelm Rademacher, Wolfgang Will
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Patent number: 4933456Abstract: N,N'-bis-(pyridoxal-5-phosphate)-alkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal-5-phosphate)-1,2-cycloalkylenediamine-N,N'-diacetic acids, and N,N'-bis-(pyridoxal-5-phosphate)-1,2-arylenediamine-N,N'-diacetic acids, the corresponding monophosphate compounds and monoacetic acid compounds, and their salts and esters form stable, highly soluble chelates with paramagnetic metal ions, and are highly effective NMRI contrast agents. Preferred contrast agents are paramagnetic ion chelates of N,N'-bis-(pyridoxal-5-phosphate)ethylene-diamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-cyclohexylenediamine-N,N'-diacet ic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-arylenediamine-N,N'-diacetic acid, and the soluble calcium salts thereof.Type: GrantFiled: May 8, 1987Date of Patent: June 12, 1990Assignee: Salutar, Inc.Inventors: Scott M. Rocklage, Steven C. Quay
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Patent number: 4902712Abstract: The invention describes the novel compound 4(Z)-6-([2,4,5-cis]-4-o-hydroxyphenyl-2-trifluoromethyl-1,3-dioxan-5-yl)he xenoic acid of formula I and its pharmaceutically acceptacle salts and pharmaceutical compositions, which are of value in treating certain pulmonary and/or vascular disorders. Also described are various processes for the manufacture of the novel compound and intermediates for use therein.Type: GrantFiled: May 9, 1986Date of Patent: February 20, 1990Assignee: Imperial Chemical Industries plcInventor: Michael J. Smithers
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Patent number: 4892899Abstract: Composition of matter containing(a) a compound of the formula I ##STR1## in which A is one of the groups of the formulae ##STR2## in which B is --O--, --S--, --SO.sub.2 --, --N.dbd.N--, --CH.sub.2 --, --CH.dbd.CH--, ##STR3## --CONH--, --NHCONH--, or --CONHNHCO--, Q is --O-- or --NH-- and Z is --O-- or --S-- and R and R' are independently of each other hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or phenoxy, and(b) a compound of the formula II ##STR4## in which A' is as defined above for A, D is hydrogen, amino or a group of the formula III ##STR5## E is --O-- or --S--, T.sub.1, T.sub.2 and T.sub.3 independently of one another are chlorine or a group --ET', T' is a group of the formulae ##STR6## X.sup..sym. is H.sup..sym. or a group of the formulae M.sup.n.sym. /n or N.sup..beta. (R.sub.1)(R.sub.2)(R.sub.3)(R.sub.4), Mhu n.sym. is an n-valent metal cation, n is 1, 2 or 3, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently of one another hydrogen, C.sub.1 -C.sub.18 -alkyl, C.sub.Type: GrantFiled: December 8, 1987Date of Patent: January 9, 1990Assignee: Ciba-Geigy CorporationInventors: Edward E. Jaffe, Jost von der Crone, Bernhard Medinger
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Patent number: 4866093Abstract: The dihydro-M-4 and dihydro-IsoM-4 hydroxy carboxylic acids of the formula (II): ##STR1## wherein one of R.sup.1 represents a hydrogen atom and the other represents a hydroxy group and wherein the structure shown as ##STR2## represents a structure of formula ##STR3## and the salts and esters of said acids. The invention also provides pharmaceutical compositions containing said acids, salts and/or esters which are useful for inhibiting cholesterol biosynthesis in the liver.Type: GrantFiled: March 19, 1984Date of Patent: September 12, 1989Assignee: Sankyo Company LimitedInventors: Akira Terahara, Minoru Tanaka
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Patent number: 4855423Abstract: Sulfatobetaines are prepared by reacting an addition compound of sulfur trioxide and a tertiary amine with an alkylene carbonate.Type: GrantFiled: October 13, 1987Date of Patent: August 8, 1989Assignee: BASF AktiengesellschaftInventors: Gerold Braun, Chung-Ji Tschang, Christos Vamvakaris, Klaus Glaser
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Patent number: 4831046Abstract: The invention describes various novel tetrazole derivatives of the formula I in which R.sup.1 and R.sup.2 are independently hydrogen, trifluoromethyl or (1-6C)alkyl (but R.sup.1 and R.sup.2 is not greater than 6 carbon atoms), or R.sup.1 is optionally substituted phenyl and R.sup.2 is hydrogen, Y is vinylene, n is 1 or 2 and m is 1, 2 or 3, or a pharmaceutically acceptable salt thereof, for use in conjunction with their pharmaceutical compositions in the treatment of various pulmonary and/or vascular disorders. Also described are various processes and intermediates for the manufacture of the novel compounds.Type: GrantFiled: May 9, 1986Date of Patent: May 16, 1989Assignee: Imperial Chemical Industries PLCInventors: George R. Brown, Michael J. Smithers
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Patent number: 4829063Abstract: Fungicidally active novel saccharine salts of substituted amines of the formula ##STR1## in which A represents in each case optionally substituted 2-decahydronaphthyl or .beta.-naphthyl andR.sup.1 and R.sup.2 independently of one another in each case represent alkyl or alkenyl or, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical, which can contain further heteroatoms.Type: GrantFiled: November 5, 1987Date of Patent: May 9, 1989Assignee: Bayer AktiengesellschaftInventors: Joachim Weissmuller, Stefan Dutzmann, Paul Reinecke
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Patent number: 4824844Abstract: Fungicidally active saccharine salts of substituted amines of the formula ##STR1## in which A represents in each case optionally substituted cyclohexyl, cyclohexenyl or phenyl,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl,R.sup.3 and R.sup.4 independently of one another represent alkyl or, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical which can contain further hetero atoms andn represents the number 0 or 1.Type: GrantFiled: November 5, 1987Date of Patent: April 25, 1989Assignee: Bayer AktiengesellschaftInventors: Joachim Weissmuller, Paul Reinecke, Gerd Hanssler
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Patent number: 4803220Abstract: The invention concerns the novel racemic and laevorotatory optically active forms of the thromboxane A.sub.2 antagonist 5(Z)-7-([ 2,4,5-cis]-4-o-hydroxyphenyl-2-trifluoromethyl-1,3-dioxan-5-yl)heptenoic acid of formula I, their salts, pharmaceutical compositions, and processes for their manufacture and intermediates therefor. The pharmaceutical agents and their compositions are of value in certain pulmonary and/or vascular disorders.Type: GrantFiled: June 28, 1985Date of Patent: February 7, 1989Assignee: Imperial Chemical Industries PLCInventors: Andrew G. Brewster, George R. Brown, Michael J. Smithers
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Patent number: 4726835Abstract: Imidazoline derivatives represented by the general formula: ##STR1## (wherein all the symbols are as defined in appended claims), a process for preparation of said derivatives, and a herbicide or a plant growth regulator containing said derivative as an active component are described. These derivatives are novel compounds, and the herbicide containing said derivative as an active component exhibits excellent herbicidal activity against various weeds without phytotoxicity on useful agricultural products. The plant growth regulator containing said derivatives as an active component exhibits excellent growth regulating activity against turf etc. without phytotoxicity thereon.Type: GrantFiled: November 24, 1986Date of Patent: February 23, 1988Assignee: Idemitsu Kosan Company LimitedInventors: Masatoshi Uemura, Masashi Sakamoto, Nobuyuki Kikkawa
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Patent number: 4719297Abstract: Acylphosphine compounds of the formula I ##STR1## where X is oxygen, sulfur or an electron pair, R.sup.1 is R.sub.4 or OR.sup.4, R.sup.2 is --OM, where M is a monovalent cation, R.sup.3 is aryl which is substituted at least at the two positions ortho to the carbonyl group, and R.sup.4 is hydrogen, alkyl or aryl, are very effective photoinitiators for photopolymerizable materials, such as coating compositions, finishes, printing inks, unsaturated polyesters, recording media and preferably aqueous polymer dispersions or solutions.Type: GrantFiled: November 20, 1984Date of Patent: January 12, 1988Assignee: BASF AktiengesellschaftInventors: Andreas Henne, Anton Hesse, Manfred Jacobi, Guenter Wallbillich, Bernd Bronstert
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Patent number: 4695587Abstract: Tetrahydro-M-4 and tetrahydro-IsoM-4 hydroxy carboxylic acids of the formula (II): ##STR1## wherein one of R.sup.1 and R.sup.2 represents a hydrogen atom and the other represents a hydroxy group, and the salts and esters of said acids which are useful for inhibiting chloresterol biosynthesis in the liver. The invention also provides pharmaceutical compositions containing said acid(s).Type: GrantFiled: April 26, 1984Date of Patent: September 22, 1987Assignee: Sankyo Company LimitedInventors: Akira Terahara, Minoru Tanaka
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Patent number: 4678496Abstract: As new compound is provided a cyclohexane derivative of the formula ##STR1## wherein R represents a hydrogen atom or an alkyl group, an alkylthioalkyl group or an unsubstituted or substituted phenyl group; and R.sup.1 represents an alkyl group, an unsubstituted or substituted benzyl group, a phenethyl group, a phenoxymethyl group, a 2-thienylmethyl group, an alkoxymethyl group or an alkylthiomethyl group, or a salt of said cyclohexane compound.This cyclohexane compound exhibits useful plant-growth regulating effects on crop-plants and also non-crop plants such as lawn and may be prepared by cyclization of an acetonylsuccinic acid dialkyl ester, followed by reaction with an organic acid chloride and by intermolecular rearrangement.Type: GrantFiled: August 1, 1985Date of Patent: July 7, 1987Assignee: Kumiai Chemical Industry Co., Ltd.Inventors: Kenji Motojima, Takeshige Miyazawa, Yasufumi Toyokawa, Masafumi Matsuzawa, Hiroshi Hokari, Shoji Kusano