Triazine Ring Patents (Class 544/112)
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Patent number: 6458950Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):Type: GrantFiled: August 3, 2000Date of Patent: October 1, 2002Assignee: Shionogi & Co., Ltd.Inventors: Yasuhiro Nishitani, Koji Ishikura
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Patent number: 6458952Abstract: The invention relates to substituted polycyclic aryl and heteroaryl uracil compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: May 18, 2000Date of Patent: October 1, 2002Assignee: Pharmacia CorporationInventors: Michael South, Darin E. Jones, Melvin L. Rueppel
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Publication number: 20020137930Abstract: The present invention relates to a process for the preparation of sulphonamide-substituted imidazotriazinones of the general formula (I) 1Type: ApplicationFiled: December 17, 2001Publication date: September 26, 2002Inventors: Marc Nowakowski, Reinhold Gehring, Werner Heilmann, Karl-Heinz Wahl
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Patent number: 6417187Abstract: 3-(Substituted aryl)-5-{substituted aryl-(alkynyl-aryl)}-[1,2,4]- triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.Type: GrantFiled: April 13, 2001Date of Patent: July 9, 2002Assignee: Dow AgroSciences LLCInventors: Vidyadhar Babu Hegde, Scott Jerome Bis, Emilie Chassat Heo, Christopher Thomas Hamilton, Peter Lee Johnson, Laura Lee Karr, Timothy Patrick Martin, Paul Allen Neese, Nailah Orr, Francis Eugene Tisdell, Maurice Chee Hoong Yap, Yuanming Zhu
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Publication number: 20020040019Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.Type: ApplicationFiled: August 10, 2001Publication date: April 4, 2002Inventors: Hui Cai, James P. Edwards, Steven P. Meduna, Barbara A. Pio, Jianmei Wei
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Patent number: 6362178Abstract: The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.Type: GrantFiled: July 21, 2000Date of Patent: March 26, 2002Assignee: Bayer AktiengesellschaftInventors: Ulrich Niewöhner, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Karl-Heinz Schlemmer, Jörg Keldenich, Erwin Bischoff, Elisabeth Perzborn, Klaus Dembowsky, Peter Serno, Marc Nowakowski
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Patent number: 6350748Abstract: A sulfamoyl compound of the general formulae (1): wherein R1 and R2 are each independently C1-4 alkyl, or R1 and R2 together are C4-6 alkylene or C4-6 alkyleneoxy, Y is H, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylthio, C1-8 haloalkyl, C1-8 haloalkoxy or C1-8 haloalkylthio, A is a predetermined heterocyclic group, B is a predetermined heterocyclic group which is identical with or different from A, W is a chemical bond or O, V is O or S, D, E, F and G are each independently N, CR7, CR8, CR9 or CR10, and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are each independently predetermined group such as H, or an unsubstituted or substituted aliphatic, aromatic or heterocyclic group. The sulfamoyl compound is useful as an agricultural and horticultural fungicide.Type: GrantFiled: June 2, 2000Date of Patent: February 26, 2002Assignee: Nissan Chemical Industries Ltd.Inventors: Toshiaki Takeyama, Toshimasa Hamada, Hiroaki Takahashi, Junichi Watanabe, Kazuhiro Yamagishi, Masanori Nishioka, Hiroyuki Suzuki
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Publication number: 20020019397Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: June 22, 2001Publication date: February 14, 2002Applicant: Pharmacia & Upjohn CompanyInventors: Mark E. Schnute, Valerie A. Vaillancourt, Scott D. Larsen
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Publication number: 20010049379Abstract: The present invention relates to 2-aminopyridine derivatives of the formula 1Type: ApplicationFiled: December 20, 2000Publication date: December 6, 2001Inventor: John Adams Lowe
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Publication number: 20010039341Abstract: Biphenyl-substituted triazines of the formulae 1Type: ApplicationFiled: May 3, 2001Publication date: November 8, 2001Inventors: Ian John Fletcher, Jurgen Kaschig, Georges Metzger, Dieter Reinehr, Pascal Hayoz
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Patent number: 6288082Abstract: This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.Type: GrantFiled: September 24, 1999Date of Patent: September 11, 2001Assignee: American Cyanamid CompanyInventors: Allan Wissner, Hwei-Ru Tsou, Dan M. Berger, Middleton B. Floyd, Jr., Philip R. Hamann, Nan Zhang, Mark E. Salvati, Philip Frost
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Patent number: 6235738Abstract: The invention relates to novel diphenyl-substituted heterocycles with 6-membered ring of general formula (I) in which A, X and the residues R1, R2, R3, R4 and R5 are as defined in the claims, processes for the preparation thereof and the use thereof as medicaments.Type: GrantFiled: April 12, 1999Date of Patent: May 22, 2001Assignees: Boehringer Ingelheim Pharma KG, Boehringer Ingelheim Italia S.p.A.Inventors: Michael Brenner, Rainer Palluk, Marion Wienrich, Thomas Weiser, Enzo Cereda, Maura Bignotti, Carlo Maria Pellegrini, Giovanni Battista Schiavi, Raffaele Cesana
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Patent number: 6218391Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I) and their use in treating psychiatric disorders and neurological diseases including major depression, anxiety-related disorders, post-traumatic stress disorders, supranuclear palsy and eating disorders.Type: GrantFiled: August 16, 1999Date of Patent: April 17, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Argyrios Georgios Arvanitis, Richard E. Olson, Charles R. Arnold, III, William E. Frietze
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Patent number: 6197750Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: GrantFiled: October 22, 1998Date of Patent: March 6, 2001Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Robert J. Ternansky
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Patent number: 6194413Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.Type: GrantFiled: May 12, 1998Date of Patent: February 27, 2001Assignee: SmithKline Beecham CorporationInventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding
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Patent number: 6096886Abstract: Novel morpholino end-capped polyamino-1,3,5-triazines, methods for their use as light stabilizers for materials which are subject to degradation (for example, by actinic radiation), stabilizer compositions based on these morpholino end-capped polyamino-1,3,5-triazines and methods for their synthesis are herein described.Type: GrantFiled: November 3, 1998Date of Patent: August 1, 2000Assignee: Cytec Technology Corp.Inventor: Martin L. Cohen
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Patent number: 5837869Abstract: An asymmetric dioxazine compound represented, when shown in free acid form, by the general formula (I): ##STR1## wherein T.sub.1 and T.sub.2 represent a hydrogen atom, a chlorine atom, a bromine atom, a lower alkyl group, a phenoxy group or others, A.sub.1 represents an alkyl group, a chlorine atom, a carboxyl group or others, A.sub.2 represents a hydrogen atom, an alkyl group, a chlorine atom, a carboxyl group or others, R represents a hydrogen atom or a lower alkyl group, X and Y represent a halogen atom, a fiber-reactive group or others, respectively, with the proviso that at least one of X and Y is a fiber-reactive group is provided.The compound is suitable for dyeing or printing of a fiber material or the like which has a hydroxy group and/or an amide group, and provides a blue-dyed product with various fastness, including particularly chlorine fastness.Type: GrantFiled: January 23, 1997Date of Patent: November 17, 1998Assignee: Sumitomo Chemical Company, LimitedInventors: Masato Inoue, Junya Hada, Toshiyuki Araki
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Patent number: 5756732Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-?4-(3-pyridyl)-3,5-difluorophenyl!-2-oxazolid inone.Type: GrantFiled: June 6, 1995Date of Patent: May 26, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Steven J. Brickner
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Patent number: 5633248Abstract: A compound of the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; P and Q independently represent a divalent aliphatic hydrocarbon group having at least 2 carbon atoms and optionally having either oxygen or sulfur in the carbon chain; R.sup.1 and R.sup.3 independently represent --CO--R, --CONH--R (R represents a hydrocarbon group or a heterocyclic group) or a hydrocarbon group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4, taken together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic group; and j represents 0 or 1, or a salt thereof, has excellent GnRH-receptor antagonizing activity and is useful as a prophylactic and therapeutic agent for hormone-dependent and other diseases.Type: GrantFiled: November 21, 1995Date of Patent: May 27, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato
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Patent number: 5563139Abstract: Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein A is selected from ##STR2## wherein m is one; wherein R.sup.1 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, benzyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R.sup.Type: GrantFiled: June 14, 1993Date of Patent: October 8, 1996Assignee: G. D. Searle & Co.Inventor: David B. Reitz
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Patent number: 5489603Abstract: An insecticidal composition containing a guanidine derivative of the formula: ##STR1## wherein R.sup.1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R.sup.2 is a hydrogen atom or an optionally substituted hydrocarbon group, R.sup.3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R.sup.1 is an optionally substituted heterocyclic group or a salt thereof.Type: GrantFiled: July 15, 1993Date of Patent: February 6, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideki Uneme, Koichi Iwanaga, Noriko Higuchi, Isao Minamida, Tetsuo Okauchi
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Patent number: 5470984Abstract: This invention relates to 1-dimethylcarbamoyl-3-substituted-5-substituted-1H-1,2,4-triazoles as defined herein, compositions containing those compounds and methods of use.Type: GrantFiled: May 10, 1994Date of Patent: November 28, 1995Assignee: Shell Research LimitedInventors: Richard M. Jacobson, J. Roger Ramsay, Harold E. Aller, Muthuvelu Thirugnanam
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Patent number: 5420099Abstract: A compound having the formula ##STR1## wherein A is CR.sub.7 ; and R.sup.1 through R.sup.7 are substituents such as hydrogen, halogen, branched and straight chain hydrocarbons, cyclic hydrocarbons, aromatics, and sulfur and nitrogen containing functional groups. Further, R.sup.5 and R.sup.6 may be taken together with the atom to which they are attached to form a group ##STR2## in which R.sup.9 and R.sup.10 are further functional groups. The compounds are useful in herbicidal compositions, particularly in combination with carriers and surfactants. A process for making this compound is also presented.Type: GrantFiled: December 21, 1992Date of Patent: May 30, 1995Assignee: Shell Research LimitedInventor: Trevor W. Newton
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Patent number: 5319092Abstract: This invention relates to 1-dimethylcarbamoyl-3-substituted-5-substituted-1H-1,2,4-triazoles as defined herein, compositions containing those compounds and methods of use.Type: GrantFiled: October 22, 1990Date of Patent: June 7, 1994Assignee: Shell Research LimitedInventors: Richard M. Jacobson, J. Roger Ramsay, Harold E. Aller, Muthuvelu Thirugnanam
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Patent number: 5290931Abstract: Water-insoluble naphthalic acid imide dyestuffs of the following formula: ##STR1## wherein D is ##STR2## wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl which may be substituted, R.sup.2 is hydrogen, halogen, lower alkyl, lower alkoxy or cyano, X is oxygen or sulfur, and m is 0 or 1; A is phenylene, alkylene, aralkylene or --C.sub.2 H.sub.4 OC.sub.2 H.sub.4 --; B is oxygen, sulfur or ##STR3## wherein R.sup.3 is hydrogen or lower alkyl; Y is a 6-membered nitrogen-containing heterocyclic ring having at least one active halogen atom; and n is 0 or 1.Type: GrantFiled: September 4, 1992Date of Patent: March 1, 1994Assignee: Hoechst Mitsubishi Kasei Co., Ltd.Inventors: Kiyoshi Himeno, Toshio Hihara
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Patent number: 5256667Abstract: Substituted quinazolinones and pyridopyrimidines of structural formula I ##STR1## are angiotensin II antagonists useful in the treatment of disorders related to the renin-angiotensin system (RAS) such as hypertension, congestive heart failure, ocular hypertension and certain CNS disorders.Type: GrantFiled: July 31, 1992Date of Patent: October 26, 1993Assignees: Merck & Co., Inc., E. I. Du Pont De Nemours & Co.Inventors: Eric E. Allen, Richard E. Olson
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Patent number: 5188832Abstract: A method of using certain triazine-dione compounds for the control of endo- and ectoparasites of fish and/or insects. The compounds may be combined with aids to form an agent for controlling the endo- or ectoparasites.Type: GrantFiled: February 14, 1990Date of Patent: February 23, 1993Assignee: Hoechst AktiengesellschaftInventors: Heinz Mehlhorn, Horst Taraschewski, Gunter Schmahl, Wolfgang Raether, Manfred Rosner
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Patent number: 5102880Abstract: Substituted Imidazo-fused 6-membered heterocycles of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogren atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.Type: GrantFiled: September 5, 1991Date of Patent: April 7, 1992Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, Thomas F. Walsh
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Patent number: 5047404Abstract: This invention relates to fused pyrimidine derivatives which have bronchodilator and anti-allergic activities. A compound of the invention is 2-(2-propoxyphenyl)pyrido[2,3-d]pyrimid-4(3H)-one.Type: GrantFiled: June 13, 1989Date of Patent: September 10, 1991Assignee: Smith Kline & French Laboratories, Ltd.Inventors: William J. Coates, Sean T. Flynn, Derek A. Rawlings
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Patent number: 5043443Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4- (4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.Type: GrantFiled: July 24, 1990Date of Patent: August 27, 1991Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Randall K. Carlson, Chung-Ho Park, Walter A. Gregory
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Patent number: 4994448Abstract: The new compounds of the general Formula I ##STR1## (wherein R.sub.1 stands for C.sub.1-4 alkyl or aralkyl; andR.sub.2 represents hydroxy; orR.sub.1 and R.sub.2 together form a valency bond;R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl, amino, alkylthio or a group of the Formula --NR.sub.7 R.sub.8 in which R.sub.7 and R.sub.8 may be the same or different and stand for hydrogen, C.sub.1-4 alkyl, phenyl-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkyl or di-(C.sub.1-4 alkyl)-amino-C.sub.1-4 alkyl or together with the nitrogen atom they are attached to form a 6-membered heterocyclic ring which may optionally contain a further nitrogen, oxygen or sulfur atom; orR.sub.2 and R.sub.3 together form an oxo (.dbd.O) or thixo (.dbd.S) group;R.sub.4 represents hydrogen, C.sub.1-4 alkyl or phenyl which may optionally bear one or two halogen or nitro substituent(s);Z is a group of the Formula (a) or (b) ##STR2## A.sup.Type: GrantFiled: September 30, 1988Date of Patent: February 19, 1991Assignee: Egis GyogyszergyarInventors: Andras Messmer, Gyorgy Hajos, Zsuzsa Juhasz nee Riedl, Pal Benko, Laszlo Pallos, Lujza Petocz, Eniko Szirt nee Kiszelly, Gabor Gigler, Istvan Gyertyan, Maria Hegedus
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Patent number: 4921527Abstract: The invention relates to sulfonylurea compounds with a substituted or unsubstituted bicyclic nine-membered ring having one to five heteroatoms which are preemergent and/or postemergent herbicides or plant growth regulants.Type: GrantFiled: May 4, 1988Date of Patent: May 1, 1990Assignee: E. I. du Pont de Nemours and CompanyInventor: Chi-Ping Tseng
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Patent number: 4916129Abstract: Imidazole compounds such as ##STR1## which have angiotensin II antagonizing properties as well as .beta.-adrenoceptor antagonizing properties are useful as antihypertensives and for treatment of congestive heart failure.Type: GrantFiled: January 19, 1989Date of Patent: April 10, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventors: David J. Carini, John J. V. Duncia
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Patent number: 4912106Abstract: Novel 5,6-dihydro-2-(substituted phenyl)-1,2,4-triazine-3,5(2H, 4H)-diones which are effective in destroying or preventing the growth of Protozoa in subjects suffering from such Protozoa.Type: GrantFiled: April 22, 1988Date of Patent: March 27, 1990Assignee: Janssen Pharmaceutica N. V. Frame-319Inventors: Gustaaf M. Boeckx, Alfons H. M. Raeymaekers, Victor Sipido
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Patent number: 4908056Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: February 17, 1989Date of Patent: March 13, 1990Assignee: E. I. Du Pont De Nemours and CompanyInventor: Chi-Ping Tseng
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Patent number: 4908364Abstract: Novel substituted 3-phenyl-7H-thiazolo[3,2-b][1,2,4]-triazin-7-ones of the formula I are disclosed ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the meaning recited in the specification. The compounds are suitable for prevention and treatment of inflammatory disorders.Type: GrantFiled: January 28, 1988Date of Patent: March 13, 1990Assignee: Hoechst AktiengesellschaftInventors: Werner Thorwart, Ulrich Gebert, Rudolf Schleyerbach, Robert R. Bartlett
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Patent number: 4898862Abstract: Compounds of formula (I): ##STR1## (in which: R.sup.1 is hydrogen or alkl; R.sup.2 is a variety of groups or atoms; R.sup.3 is optionally substituted hydroxy or --(NH).sub.n --NR.sup.5 R.sup.6, wherein R.sup.5 and R.sup.6 are a variety of groups or atoms, preferably alkyl substituted by heterocyclic, and n is 0 or 1; Q is oxygen or sulfur; and A is a C.sub.1 -C.sub.6 alkylene group) have valuable cardiotionic activity and may be used for the treatment of cardiac disorders. They may be prepared from corresponding compounds containing a benzene ring with a group --QH at the 1-position and a group --CO--CHR.sup.1 --NH--COOR.sup.7 at the 4-position by ring closure and introduction of the group of formula --A--CO--R.sup.3 in any order.Type: GrantFiled: March 16, 1987Date of Patent: February 6, 1990Assignee: Sankyo Company LimitedInventors: Yasuhiro Morisawa, Mitsuru Kataoka, Mitsuo Sugiyama, Fujio Saito, Hiroyuki Koike, Takeshi Oshima, Yasuo Simoji, Hitoshi Nagahori
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Patent number: 4892946Abstract: N-(heterocyclicaminocarbonyl)arylsulfonamides in which the aryl radical is substituted in the 2-position by a carboxy radical, ester, thioester, or amide thereof; e.g. N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-2-methoxycarbonylbenzenesulf onamide or N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-2-methoxycarbonylbenze nesulfonamide; are useful for the regulation of plant growth and as pre-emergence and post-emergence herbicides.Type: GrantFiled: November 24, 1980Date of Patent: January 9, 1990Assignee: E. I. Du Pont De Nemours and CompanyInventor: George Levitt
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Patent number: 4870174Abstract: The synthesis of 7-n-alkyl-imidazolium[4,5-d]-pyrimidines, 6-substituted-3n-alkyl-benzimidazolium- and 3n-alkyl-5,6-substituted-benzthiazolium salts are described. There N.sup.+ -surfactants having a substituted heterocycle as a head group have distinguished small critical micelle concentrations (CMC) in the range of 10.sup.-5 -10.sup.-7 Mol/Liter. The size and shape of these micelles in watery solutions are determined by the nature of the anion. The N-surfactants can be used as pharmaceuticals as well as reporter groups in fluorescence studies including immunological assays.Type: GrantFiled: August 6, 1987Date of Patent: September 26, 1989Assignee: Medice chem.-pharm. FabrikInventor: Henrich H. Paradies
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Patent number: 4853394Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof:Ar--CO--X--Y--Z--OR.sub.1 (I)wherein: Ar is a group of formula (a): ##STR1## wherein either R.sub.2 is C.sub.1-6 alkoxy and one of R.sub.3, R.sub.4 and R.sub.5 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, CX.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-6 alkoxy, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O)n wherein n is 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.2 is hydrogen and R.sub.3, R.sub.4 and R.sub.5 are independently selected from hydrogen, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or halo; or any two on adjacent carbon atoms together are C.sub.Type: GrantFiled: November 3, 1986Date of Patent: August 1, 1989Assignee: Beecham Group p.l.c.Inventors: Francis D. King, Roger T. Martin, Eric A. Watts
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Patent number: 4782056Abstract: Compounds of the formula I ##STR1## with n=1-3, R=H, Hal, CF.sub.3, alkyl, cycloalkyl, alkyloxy, alkylthio, alkylsulfinyl, alkylsulfonyl, benzylsulfinyl, benzylsulfonyl, nitro, cyano, amino, alkylamino, dialkylamino, piperidino, morpholino, pyrrolidinyl, 4-methyl-1-piperazinyl, acylamino or substituted phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl, benzoyl, benzoylamino or anilino, with R.sup.2 =H, alkyl, cycloalkyl, optionally substituted benzyl, alkanoyl or benzoyl and R.sup.3 =H, alkyl, cycloalkyl or optionally substituted benzyl, at least R.sup.2 or R.sup.3 not being H, are obtained by alkylation or acylation of a compound II ##STR2## in which R.sup.1 is as defined above, with compounds R.sup.3 X (X=leaving group) or R.sup.2 Y (Y=leaving group), R.sup.2 and R.sup.3 being defined as indicated.Compounds I are coccidiostatics.Type: GrantFiled: September 5, 1986Date of Patent: November 1, 1988Assignee: Hoechst AktiengesellschaftInventors: Manfred Rosner, Wolfgang Raether
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Patent number: 4698352Abstract: This invention relates to a novel 4-oxo-1,4-dihydronicotinic acid derivative ##STR1## or a salt thereof, wherein R.sup.1 is hydrogen or carboxyl-protecting group;R.sup.2 is substituted phenyl and naphthyl, or a substituted or unsubstituted heterocyclic group; andR.sup.3 is haloalkyl, aminoalkyl, or substituted or unsubstituted alkenyl, phenylalkenyl, naphthylalkenyl, phenylalkyl, naphthylalkyl, phenylalkynyl, naphthylalkynyl, heterocyclic alkyl, heterocyclic alkenyl, phenyl, naphthyl, cycloalkyl, cycloalkenyl, carboxylic acyl, iminoalkyl, heterocyclic or bridged hydrocarbon, which has a broad antibacterial spectrum and a low toxicity, and are useful for treatment of diseases of human beings and animals, to a process for producing the same and to an antibacterial agent containing the same.Type: GrantFiled: October 27, 1983Date of Patent: October 6, 1987Assignee: Toyama Chemical Co., Ltd.Inventors: Hirokazu Narita, Yoshinori Konishi, Jun Nitta, Shunjiro Misumi, Hideyoshi Nagaki, Isao Kitayama, Yoriko Nagai, Yasuo Watanabe, Nobuyuki Matsubara, Shinzaburo Minami, Isamu Saikawa
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Patent number: 4689072Abstract: N-(heterocyclicaminocarbonyl)arylsulfonamides in which the aryl radical is substiuted in the 2-position by a carboxy radical, ester, thioester, or amide thereof; e.g. N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-2-methoxycarbonylbenzenesulf onamide or N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-2-methoxycarbonylbenze nesulfonamide; are useful for the regulation of plant growth and as pre-emergence and post-emergence herbicides.Type: GrantFiled: July 30, 1986Date of Patent: August 25, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: George Levitt
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Patent number: 4689414Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3 or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;R.sub.5 is hydrogen, alkyl, aryl, arylalkyl, cyano, nitro, ##STR2## Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl-(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl-(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## amino, or substituted amino; m is 0 or an integer of 1 to 6;n is an integer of 1 to 6; andp is an integer of 2 to 6.Type: GrantFiled: February 24, 1986Date of Patent: August 25, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 4684656Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR2## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR3## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.Type: GrantFiled: March 14, 1986Date of Patent: August 4, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 4683228Abstract: A guanidine derivative of the formula I: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is substituted by a hydroxy radical and into which is optionally inserted, as part of the backbone of the chain, one or two groups selected from oxygen and sulphur atoms and NH and 1-6C N-alkyl radicals; and the pharmaceutically-acceptable acid additions salts thereof. Pharmaceutical compositions and methods of manufacture are also described. The compound of the formula I is a histamine H-2 antagonist and is therefore useful in ulcer therapy.Type: GrantFiled: January 22, 1985Date of Patent: July 28, 1987Assignees: ICI Americas Inc., Imperial Chemical Industries PLCInventors: Karin M. Kirkland, Derrick M. Mant
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Patent number: 4640917Abstract: Substituted 2-phenyl-hexahydro-1,2,4-triazine-3,5-diones of the formula ##STR1## in which n is one, two or three and the individual substituents R are independently of one another (a) hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl, alkyl having 1 to 6 carbon atoms, cycloalkyl having 3 to 6 carbon atoms, alkoxy, alkylthio, alkylsulfinyl or alkylsulfonyl each having 1 to 6 carbon atoms in the alkyl moiety, nitro, cyano, amino, alkylamino or dialkylamino each having 1 to 12 carbon atoms in the alkyl moiety, piperidino, morpholino, thiomorpholino, 1-pyrrolidinyl, 4-methyl-1-piperazinyl or acylamino having 1 to 6 carbon atoms in the acyl moiety, or (b) a phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl, benzoyl, benzoylamino or aniline radical which is in each case R.sub.(a) -substituted, and the alkali metal salts, alkaline earth metal salts or ammonium salts thereof, a process for their preparation, their use, veterinary drugs and a process for controlling protozoal diseases.Type: GrantFiled: March 8, 1985Date of Patent: February 3, 1987Assignee: Hoechst AktiengesellschaftInventors: Manfred Rosner, Wolfgang Raether
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Patent number: 4622397Abstract: The invention relates to a process for the preparation of aminotriazinone derivatives of the formula I ##STR1## wherein R.sub.1 and R.sub.2 are each independently alkyl, cycloalkyl, aralkyl or aryl, andR.sub.3 and R.sub.4 are each independently hydrogen, alkyl or cycloalkyl, or together with the nitrogen atom to which they are attached are a piperidine or morpholine ring, which process comprises phosgenating a compound of formula II ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, and reacting the resultant compound of formula III ##STR3## wherein R.sub.1 and R.sub.2 are as defined above, without isolation or after isolation, with a compound of formula IV ##STR4## wherein R.sub.3 and R.sub.4 are as defined above. The invention also relates to the novel compounds of formula I and to the use thereof for controlling undesirable plant growth, as well as to compounds of the formula III.Type: GrantFiled: July 5, 1985Date of Patent: November 11, 1986Assignee: Ciba-Geigy CorporationInventor: Beat Bohner
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Patent number: 4616002Abstract: Compounds of the formula I ##STR1## in which n represents 1, 2 or 3, Ar represents a carbocyclic or heterocyclic aryl radical, Ac represents the acyl radical of an acid, Z represents a radical --OR.sub.7 or --NR.sub.8 R.sub.9, R.sub.1 represents hydrogen, unsubstituted or substituted lower alkyl, a carbocyclic or heterocyclic aryl radical or free, etherified or esterified hydroxy, R.sub.2 and R.sub.3, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl, formyl or functionally modified formyl, carboxy or functionally modified carboxy, a carbocyclic or heterocyclic aryl radical or unsubstituted or mono- or di-substituted amino, R.sub.4 represents hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl or a carbocyclic or heterocyclic aryl radical, R.sub.7, R.sub.8 and R.sub.Type: GrantFiled: January 6, 1986Date of Patent: October 7, 1986Assignee: Ciba-Geigy CorporationInventors: Bruno Kamber, Thomas Leutert, Hans Kuhnis, Kurt Eichenberger
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Patent number: 4585861Abstract: This invention relates to certain amino-5,6-diaryl-1,2,4-triazines and -pyrazines useful as activators of GABA and benzodiazepine binding.Type: GrantFiled: January 4, 1985Date of Patent: April 29, 1986Assignee: Eli Lilly and CompanyInventors: David T. Wong, William B. Lacefield