Plural Nitrogens In The Heterocyclic Ring Patents (Class 540/545)
-
Patent number: 5686444Abstract: Esters of hydroxyl-containing indolocarbazoles and acids containing selected solubilizing groups are provided. Compositions including the indolocarbazole esters and methods for the use of the indolocarbazole esters are also provided.Type: GrantFiled: March 26, 1996Date of Patent: November 11, 1997Assignees: Cephalon, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: John P. Mallamo, Robert L. Hudkins
-
Patent number: 5674867Abstract: The present invention relates to therapeutic agents for thrombocytopenia which contain an indolocarbazole derivative represented by the formula (I) given below or a pharmaceutically acceptable salt thereof as an active ingredient, and to novel indolocarbazole derivatives.Type: GrantFiled: May 18, 1994Date of Patent: October 7, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tatsuya Tamaoki, Yukimasa Shiotsu, Chikara Murakata, Shiro Akinaga, Masami Okabe, Yutaka Saito, Junichi Watanabe, Takako Shiraki
-
Patent number: 5668271Abstract: Indolopyrrocarbazole derivatives represented by formula (I) and the pharmaceutically acceptable salts thereof have excellent antitumor activity as evidenced by their in vitro proliferation inhibiting activity against mouse leukemia cell, human gastric cancer cell, human lung cancer cell and human colon cancer cell, ##STR1## wherein R.sup.1 and R.sup.2 independently represent, for example, a hydrogen atom or various hydrocarbon groups which may be substituted or heterocyclic groups which may also be substituted; or a group --Y--R.sup.3 where Y represents a carbonyl group, thiocarbonyl group or sulfonyl group and R.sup.3 represents a hydrogen atom or one of various aliphatic, cycloaliphatic, aryl, nitrogen-containing (e.g. amino, hydrazino, etc) or heterocyclic groups, which groups may be substituted by various substituents; or R.sup.1 and R.sup.2 may combine to represent a lower alkylidene group which may be substituted; or R.sup.1 and R.sup.Type: GrantFiled: June 7, 1995Date of Patent: September 16, 1997Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Katsuhisa Kojiri, Hisao Kondo, Hiroharu Arakawa, Mitsuru Ohkubo, Hiroyuki Suda
-
Patent number: 5659031Abstract: There is provided a 1-(3-heterocyclylphenyl)-s-triazine-2,4,6-oxo or thiotrione compound having the structural formula I ##STR1## Further provided are a composition and a method comprising that compound for the control of undesirable plant species.Type: GrantFiled: June 2, 1995Date of Patent: August 19, 1997Assignee: American Cyanamid CompanyInventors: Alvin Donald Crews, Jr., Gary Mitchell Karp, Mark Christopher Manfredi, Michael Anthony Guaciaro
-
Patent number: 5654427Abstract: The invention features a method of treating a pathological condition of the prostate gland, e.g., benign prostatic hypertrophy or prostate cancer, in a mammal, said method comprising administering to said mammal a therapeutic amount of the indolocarbazole compound K-252a or a preferred derivative thereof. The invention also includes novel derivatives of K-252a.Type: GrantFiled: June 5, 1995Date of Patent: August 5, 1997Assignees: Kyowa Hakko Kogyo Co., Ltd., Cephalon, Inc.Inventors: Craig A. Dionne, Patricia C. Contreras, Chikara Murakata
-
Patent number: 5650407Abstract: Esters of hydroxyl-containing indolocarbazoles and acids containing selected solubilizing groups are provided. Compositions including the indolocarbazole esters and methods for the use of the indolocarbazole esters are also provided.Type: GrantFiled: April 5, 1995Date of Patent: July 22, 1997Assignees: Cephalon, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: John P. Mallamo, Robert L. Hudkins
-
Patent number: 5621098Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2, X, W, and Y are as defined in the specification. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.Type: GrantFiled: June 1, 1995Date of Patent: April 15, 1997Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
-
Patent number: 5621100Abstract: The invention features novel derivatives of K-252a, as well as novel bis-N-substituted derivatives of staurosporine. The invention also features a method for treating diseased neuronal cells involving the administration of either the novel staurosporine derivatives or specified functional derivatives of K-252a.Type: GrantFiled: October 26, 1994Date of Patent: April 15, 1997Assignees: Cephalon, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Michael E. Lewis, James C. Kauer, Nicola Neff, Jill Roberts-Lewis, Chikara Murakata, Hiromitsu Saito, Yuzuru Matsuda, Marcie A. Glicksman, Fumihiko Kanai, Masami Kaneko
-
Patent number: 5621101Abstract: The invention features novel derivatives of K-252a, as well as novel bis-N-substituted derivatives of staurosporine. The invention also features a method for treating diseased neuronal cells involving the administration of either the novel staurosporine derivatives or specified functional derivatives of K-252a.Type: GrantFiled: June 7, 1995Date of Patent: April 15, 1997Assignees: Cephalon, Inc., Kyowa Hakko KogyoInventors: Michael E. Lewis, James C. Kauer, Nicola Neff, Jill Roberts-Lewis, Chikara Murakata, Hiromitsu Saito, Yuzuru Matsuda, Marcie A. Glicksman, Fumihiko Kanai, Masami Kaneko
-
Patent number: 5618809Abstract: N-alkanoyl derivatives of staurospodne represented by the formula I ##STR1## wherein R.sub.a and R.sub.b are each H or ##STR2## wherein R.sub.1 and R.sub.2 are independently H or --OH or --OCH.sub.3 and R.sub.3 is OH, NHCH.sub.3, NCH COCH.sub.3 or NHCOCH.sub.3 and R.sub.4 is OH or H and, stereochemical isomers thereof with the provisos that (1) when R.sub.a and R.sub.b .dbd.A, and R.sub.1.dbd.H.sub.2 or OH R.sub.3 is not NHCH.sub.3 ; (2) when R.sub.a and R.sub.b.dbd. B, then R.sub.1 .dbd.R.sub.4 .dbd.OH or R.sub.1 .dbd.R.sub.4 .dbd.H; (3) when R.sub.a .dbd.R.sub.b .dbd.H R.sub.1 .dbd.--OCH.sub.3, and (4) when R.sub.a and R.sub.b .dbd.A, and R.sub.1 .dbd.H and R.sub.2 .dbd.OCH.sub.3, then R3 is not and ##STR3## pharmaceutical compositions thereof useful for inhibiting myosin light chain kinase, protein kinase C or tumor cell proliferation as well as producing an antihypertensive effect and an anti-inflammatory effect in warm-blood animals such as man are disclosed.Type: GrantFiled: February 27, 1995Date of Patent: April 8, 1997Assignee: Schering CorporationInventors: Ellen B. Barrabee, Ann C. Horan, Frank A. Gentile, Mahesh G. Patel
-
Patent number: 5610294Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: ##STR1## wherein R.sup.22 and R.sup.23 are allyl.Type: GrantFiled: February 16, 1994Date of Patent: March 11, 1997Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Patrick Y. Lam, Prabhakar K. Jadhav, Charles J. Eyermann, Carl N. Hodge, George V. De Lucca, James D. Rodgers
-
Patent number: 5605898Abstract: Disclosed are novel anellated triazole compounds of formula, in which R.sup.A, m, n, X--X, V, W and Q have the meaning stated in the specification; a method of their preapartion; and their use as herbicides.Type: GrantFiled: April 24, 1995Date of Patent: February 25, 1997Assignees: Degussa AG, E. I. DuPont de Nemours and CompanyInventors: Matthias Schafer, Karlheinz Drauz, Dieter Feit
-
Patent number: 5604219Abstract: Disclosed is an indolocarbazole derivative represented by the following formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## [wherein R.sup.1 represents substituted or unsubstituted lower alkyl, R.sup.2 represents hydrogen, substituted or unsubstituted lower alkyl, R.sup.3 and R.sup.4 are the same or different, and represent hydrogen, nitro, NR.sup.5 R.sup.6, OR.sup.9, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, or CH.dbd.NNR.sup.10 R.sup.11, W represents two hydrogen atoms or oxygen, and Me represents methyl, provided that when R.sup.1 is unsubstituted lower alkyl, R.sup.3 and R.sup.4 are not simultaneously hydrogen.Type: GrantFiled: March 16, 1995Date of Patent: February 18, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Chikara Murakata, Junichi Watanabe, Yutaka Saitoh, Yukimasa Shiotsu, Takako Shiraki, Fumihiko Kanai, Tatsuya Tamaoki, Shiro Akinaga, Masami Okabe
-
Patent number: 5591842Abstract: Indolopyrrocarbazole derivatives such as exemplified by the following compound, ##STR1## have excellent antitumor activity as evidenced by in vitro proliferation inhibiting activity against mouse leukemia cell, human gastric cancer cell, human lung cancer cell and human colon cancer cell.Type: GrantFiled: June 8, 1994Date of Patent: January 7, 1997Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Katsuhisa Kojiri, Hisao Kondo, Hiroharu Arakawa, Mitsuru Ohkubo, Hiroyuki Suda
-
Patent number: 5589472Abstract: The invention relates to compounds of the formula ##STR1## wherein X, Y, Z, R.sub.1, R.sub.2, R.sub.4, and R.sub.5, are as described herein. These compounds are useful as agents for the treatment of inflammation, tumors and psoriasis.Type: GrantFiled: March 10, 1995Date of Patent: December 31, 1996Inventor: Susan F. Vice
-
Patent number: 5585488Abstract: In the formulae, R.sup.1, R.sup.2, and R.sup.3 independently represent lower alkyl or aryl, and R.sup.4 represents lower alkyl.The present invention relates to a process for producing an indolocarbazole derivative represented by Formula (II), comprising the acidic treatment of a silylated indolocarbazole derivative represented by Formula (VI).Type: GrantFiled: February 23, 1996Date of Patent: December 17, 1996Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Masahiko Kinugawa, Yoshiaki Masuda, Yukiteru Mimura, Chikara Murakata, Hiromitsu Saito, Takehiro Ogasa, Masaji Kasai, Shinji Tomioka
-
Patent number: 5516771Abstract: The invention features a method of treating a pathological condition of the prostate gland, e.g., benign prostatic hypertrophy or prostate cancer, in a mammal, said method comprising administering to said mammal a therapeutic amount of the indolocarbazole compound K-252a or a preferred derivative thereof. The invention also includes novel derivatives of K-252a.Type: GrantFiled: May 27, 1994Date of Patent: May 14, 1996Assignees: Cephalon, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Craig A. Dionne, Patricia C. Contreras, Chikara Murakata
-
Patent number: 5506355Abstract: The present invention discloses processes for the preparation of substituted cyclic sulfamides which are useful as intermediates for the synthesis of cyclic sulfamide human immunodeficiency virus (HIV) protease inhibitors. Such substituted cyclic sulfamide intermediates contain a cyclic acetal-protected diol.Type: GrantFiled: June 30, 1994Date of Patent: April 9, 1996Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Prabhakar K. Jadhav, Wayne F. Daneker, Francis J. Woerner
-
Patent number: 5478934Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.Type: GrantFiled: November 23, 1994Date of Patent: December 26, 1995Inventors: Jun Yuan, Jan W. F. Wasley
-
Patent number: 5461146Abstract: The invention features novel derivatives of K-252a, as well as novel bis-N-substituted derivatives of staurosporine. Also, a method for treating diseased neuronal cells involving the administration of either the novel staurosporine derivatives or specified functional derivatives of K-252a.Type: GrantFiled: July 22, 1993Date of Patent: October 24, 1995Assignees: Cephalon, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Michael E. Lewis, James C. Kauer, Nicola Neff, Jill Roberts-Lewis, Chikara Murakata, Hiromitsu Saito, Yuzuru Matsuda, Marcie A. Glicksman
-
Patent number: 5455241Abstract: N-(tetrahydropyran-4-yloxy-alkanoyl)-staurosporin derivatives of formula I ##STR1## wherein R.sub.1 is hydrogen, hydroxy, lower alkoxy or oxo,R.sub.2 is hydrogen or C.sub.1-4 alkyl andR.sub.3 is hydrogen or C.sub.1-4 alkyl,processes and novel intermediates for the preparation thereof and processes for the preparation of the intermediates are described. The compounds of formula I inhibit the enzyme protein kinase C with a high degree of selectivity and can be used especially as tumour-inhibiting active ingredients.Type: GrantFiled: September 20, 1994Date of Patent: October 3, 1995Assignee: Ciba-Geigy CorporationInventor: Oskar Wacker
-
Patent number: 5382675Abstract: A tetrahydropyran-4-yloxy-alkanoic acid of formula III ##STR1## wherein R.sub.2 is hydrogen or C.sub.1-4 alkyl and R.sub.3 is hydrogen or C.sub.1-4 alkyl.Type: GrantFiled: April 28, 1994Date of Patent: January 17, 1995Assignee: Ciba-Geigy CorporationInventor: Oskar Wacker
-
Patent number: 5344926Abstract: Disclosed is a process for producing a staurosporine derivative represented by Formula (I): Q is defined as in specification: ##STR1## The staurosporine derivative (I-1) possesses selective protein kinase C-inhibitory and cell growth-inhibiting activities, and platelet-increasing activity.Type: GrantFiled: June 22, 1993Date of Patent: September 6, 1994Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Chikara Murakata, Toshimitsu Takiguchi, Shigeo Katsumata, Akira Mihara, Keiichi Takahashi, Hiromitsu Saito, Shiro Akinaga, Masami Okabe, Yutaka Saito
-
Patent number: 5264431Abstract: Staurosporin derivatives of the formula I are described, ##STR1## in which R.sub.1 is hydrogen, hydroxyl, lower alkoxy or oxo and R.sub.2 is a radical of the formula II ##STR2## in which the configuration of the sugar moiety is derived from D-glucose, D-galactose or D-mannose, and R.sub.3 -R.sub.7 are as defined below.These compounds have a pronounced and selective inhibitory action on the enzyme proteinkinase C and have, inter alia, an antitumor action.Type: GrantFiled: November 6, 1992Date of Patent: November 23, 1993Assignee: Ciba-Geigy Corp.Inventors: Oskar Wacker, Peter Traxler
-
Patent number: 5240938Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.Type: GrantFiled: August 13, 1991Date of Patent: August 31, 1993Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, Arthur A. Patchett, David Hangauer, Thomas F. Walsh, Kenneth J. Fitch, Ralph A. Rivero, Daljit S. Dhanoa
-
Patent number: 5238936Abstract: The compounds are trisubstituted triazines and pyrimidines useful for the suppressing the resistance of tumour cells to anti-cancer agents and for suppressing the resistance of parasites to anti-parasitic agents.A compound disclosed is 2,4-diallylamino-6-{4-[(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl) methylamino]piperidin-1-yl}-1,3,5-triazine.Type: GrantFiled: March 6, 1992Date of Patent: August 24, 1993Assignee: Adir et CompagnieInventors: Gilbert Regnier, Alain Dhainaut, Ghanem Atassi, Alain Pierre, Stephane Leonce
-
Patent number: 5212301Abstract: Introduction of a fluoro substituent into an aromatic ring adjacent an electron donating group is difficult producing mixed isomers and low yields of desired products.A process for the introduction of a fluoro substituent into a substantially adjacent position to an electron-donating group into an aromatic compound in high yield is disclosed.The fluoroaromatic compounds are useful as synthetic intermediates for example in the manufacture of agrochemicals, pharmaceuticals and dyestuffs.Type: GrantFiled: May 8, 1992Date of Patent: May 18, 1993Assignee: Imperial Chemical Industries PLCInventors: John S. Moilliet, Richard D. Chambers, Michael H. Rock
-
Patent number: 5202324Abstract: The imidazo[1,2-b]pyridazine compounds of the formula: ##STR1## wherein R.sub.1 is a hydrogen or halogen atom, or a lower alkyl group optionally having substituent(s), R.sub.2 and R.sub.3 are, independently, a hydrogen atom, a lower alkyl group optionally having substituent(s), a cycloalkyl group or a phenyl group optionally having substituent(s) or R.sub.2 and R.sub.3 together with the adjacent nitrogen atom to which they bond may form a heterocyclic ring optionally having substituent(s), X is an oxygen atom or S(O).sub.n (n=0 to 2), Alk is a straight or branched chain alkylene group containing 1-10 carbon atoms and optionally having substituent(s), or their pharmaceutically acceptable salts which possess antiallergic, anti-inflammatory and anti-PAF activities, and their production and use.Type: GrantFiled: January 31, 1990Date of Patent: April 13, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Masaaki Kuwahara, Hisashi Kuriki
-
Patent number: 5185260Abstract: A G.sub.1 phase kinase inhibitor is applied in a low concentration to a population of normal and transformed mammalian cells. The concentration of G.sub.1 phase kinase inhibitor is selected to reversibly arrest normal mammalian cells in the G.sub.1 cell cycle without arresting growth of transformed cells. The transformed cells may then be selectively identified and/or cloned for research or diagnostic purposes. The transformed cells may also be selectively killed by therapeutic agents that do not affect normal cells in the G.sub.1 phase, suggesting that such G.sub.1 phase kinase inhibitors may form an effective adjuvant for use with chemotherapeutic agents in cancer therapy for optimizing the killing dose of chemotherapeutic agents while minimizing undesirable side effects on normal cells.Type: GrantFiled: August 29, 1991Date of Patent: February 9, 1993Assignee: The United States of America as represented by the United States Department of EnergyInventors: Harry A. Crissman, Donna M. Gadbois, Robert A. Tobey, E. Morton Bradbury
-
Patent number: 5180418Abstract: Cycloalkanecarboxylic acid derivatives of formula I ##STR1## wherein W is ##STR2## and A is CO--R.sub.3 or CN; R.sub.1 is hydrogen or fluorine; R.sub.2 is halogen or cyano; R.sub.3 is chlorine, X--R.sub.5, amino, C.sub.1 -C.sub.4 alkylamino, d-C.sub.1 -C.sub.4 alkylamino, C.sub.2 -C.sub.4 haloalkylamino, di-C.sub.2 -C.sub.4 haloalkylamino, C.sub.1 -C.sub.4 hydroxyalkylamino, di-C.sub.1 -C.sub.4 hydroxyalkylamino, C.sub.3 -C.sub.4 alkenylamino, diallylamino, --N-pyrrolidino, --N-piperidino, --N-morpholino, --N-thiomorpholino, --N-piperidazino, the group --O--N.dbd.C--(R.sub.9)R.sub.10 or the group --N--R.sub.6 (OR.sub.6); each of R.sub.4 and R.sub.14, independently of the other, is hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 alkyl or trifluoromethyl; R.sub.5 is hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.10 alkylthio-C.sub.1 -C.sub.4 alkyl, di-C.sub.1 -C.sub.4 alkylamino-C.sub.1 -C.sub.4 alkyl, cyano-C.sub.1 -C.sub.Type: GrantFiled: July 19, 1991Date of Patent: January 19, 1993Assignee: Ciba-Geigy CorporationInventors: Georg Pissiotas, Hans Moser, Hans-Georg Brunner, Eginhard Steiner
-
Patent number: 5106840Abstract: The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## wherein R.sub.1 is lower alkyl or alkoxy, halogen, trifluoromethyl, lower alkylthio, hydroxy, amino, lower mono- or dialkyl- or acylamino.n has the value 0, 1 or 2,R.sub.2 is hydrogen, lower alkyl or acyl,R.sub.3 is hydrogen, lower alkyl or alkoxycarbonyl, or a phenyl group optionally substituted with a group R.sub.Type: GrantFiled: June 5, 1990Date of Patent: April 21, 1992Assignee: Duphar International Research B.V.Inventors: Peter H. H. Hermkens, Jan H. Van Maarseveen, Johan W. Scheeren, Cornelis G. Kruse
-
Patent number: 5093330Abstract: N-substituted derivatives of staurosporine of the general formula[Stau]--N(CH.sub.3)--R (I)in which [Stau] represents a residue of the partial formula ##STR1## and R represents a hydrocarbyl radical R.sup.o or an acyl radical Ac, which radicals preferably have a maximum of 30 carbon atoms, and salts of compounds of the formula I having salt-forming properties, are distinguished as selective inhibitors of proteinkinase C. They are manufactured by conventional alkylation or acylation, respectively, of staurosporine.Type: GrantFiled: March 21, 1991Date of Patent: March 3, 1992Assignee: Ciba-Geigy CorporationInventors: Giorgio Caravatti, Andreas Fredenhagen
-
Patent number: 5089175Abstract: Hydroxyalkane carboxylic acid derivatives of general formula I ##STR1## in which n means the numbers 7 to 18,R.sub.1 represents a hydrogen atom or an acyl group with a maximum of 16 carbon atoms, andoptionally an alkylene group with 4 to 8 carbon atoms interrupted by an oxygen atom or a nitrogen atom, are useful for the production of pharmaceutical agents for local treatment of diseases of the skin and mucous membranes.Type: GrantFiled: February 16, 1990Date of Patent: February 18, 1992Assignee: Schering AktiengesellschaftInventors: Christopher G. Earnshaw, Gerald Kirsch, Petra Rach, Ruth Thieroff-Ekerdt, Michael Topert
-
Patent number: 5073633Abstract: An antitumor antibiotic designated BMY-41950 is produced by fermentation of Streptomyces staurosporeus ATCC 55006 or Streptomyces hygroscopicus ATCC 53730. The BMY-41950 antibiotic exhibits both antimicrobial and antitumor activities.Type: GrantFiled: November 5, 1990Date of Patent: December 17, 1991Assignee: Bristol-Myers CompanyInventors: Daniel Schroeder, Kin S. Lam, Jacqueline Mattei, Grace A. Hesler
-
Patent number: 5043335Abstract: The present invention provides 9,10,11,12-tetrahydro-9,12-epoxy-1H-diindolo [1,2,3-fg: 3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-1,3(2H)-dione and 9,10,11,12-tetrahydro-2-(tetrahydro-5-methoxy-2-furanyl) -9,12-epoxy-1H-diindolo[1,2,3-fg: 3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-1,3(2H)-dione process for the preparation thereof, pharmaceutical compositions containing the compounds, and use of the compounds in heart and blood vessel diseases such as thromboses, arterioscleroses, hypertension and inflammatory diseases, allergies, cancer and certain degenerative damage of the central nervous system, as well as diseases of the immune system.Type: GrantFiled: July 23, 1990Date of Patent: August 27, 1991Assignee: Godecke AktiengesellschaftInventors: Jurgen Kleinschroth, Johannes Hartenstein, Christoph Schachtele, Claus Rudolph
-
Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
-
Patent number: 5015578Abstract: A new antitumor antibiotic designated BMY-41950 is produced by fermentation of Streptomyces staurosporeus ATCC 55006 or Streptomyces hygroscopicus ATCC 53730. The BMY-41950 antibiotic exhibits both antimicrobial and antitumor activities.Type: GrantFiled: February 20, 1990Date of Patent: May 14, 1991Assignee: Bristol-Myers Squibb CompanyInventors: Daniel Schroeder, Kin S. Lam, Jacqueline Mattei, Grace A. Hesler
-
Patent number: 5015637Abstract: There are disclosed various compounds of the formula below, ##STR1## where X is hydrogen, halogen or loweralkyl;Y is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl;R.sub.1 is hydrogen, loweralkyl, aryl, arylloweralkyl, diloweralkylaminoloweralkyl or ##STR2## R.sub.3 being hydrogen, loweralkyl or arylloweralkyl; and R.sub.2 is hydrogen, loweralkyl or arylloweralkyl;which compounds are useful as analgesic agents.Type: GrantFiled: May 25, 1990Date of Patent: May 14, 1991Assignee: Hoechst-Roussel Pharmaceutical Inc.Inventors: Richard C. Effland, Larry Davis
-
Patent number: 5011833Abstract: Novel derivatives of 11-carbonyl-6,11-dihydrodibenzo[c,f][1,2,5]thiadiazepine 5,5-dioxide of the general formula ##STR1## wherein R and R.sub.1, which can be different, represent a hydrogen atom or a (C.sub.1 -C.sub.5) alkyl or (C.sub.1 -C.sub.4)hydroxyalkyl group, or R and R.sub.1 together can form a 5-membered and/or 6-membered heterocyclic ring which may contain a further heteroatom,R.sub.2 and R.sub.3, which can be different, represent a hydrogen atom, a (C.sub.1 -C.sub.3)alkoxy, (C.sub.1 -C.sub.3)alkyl, nitro, amino or (C.sub.1 -C.sub.3)alkylamino, halogen, halogeno-alkyl or hydroxyl group,R.sub.4 represents a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl, alkylaryl or (C.sub.1 -C.sub.6)alkylamino group, andn assumes values of 0, 1 or 2, andnon-toxic, pharmaceutically acceptable salts thereof, obtained by addition of acids or alkyl halides.Type: GrantFiled: August 11, 1989Date of Patent: April 30, 1991Assignee: A. Menarini Industrie Farmaceutiche RiuniteInventors: Franco Barsini, Alberto Meli, Giovanna Volterra, Danilo Giannotti, Vittorio Pestellini
-
Patent number: 4957535Abstract: Novel bicyclic triazole compounds of the formula I have an excellent herbicidal and plant-growth regulating action.The compounds correspond to the formula I ##STR1## wherein Q is hydrogen or halogen,T is halogen, andZ is a radical --XR or --COXR, in whichX is oxygen, sulfur or a radical --NR.sub.2 --,R is hydrogen, a C.sub.1 -C.sub.6 -alkyl, C hd 3-C.sub.6 -cycloalkyl, C hd 2-C.sub.6 -alkenyl or C.sub.3 -C.sub.6 -alkynyl radical, which is unsubstituted or substituted by halogen, or is a radical --A--COXR.sub.1, in whichA is a C.sub.1 -C.sub.4 -alkylene bridge andR.sub.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.4 -alkenyl or C.sub.3 -C.sub.4 -alkynyl.Type: GrantFiled: September 29, 1988Date of Patent: September 18, 1990Assignee: Ciba-Geigy CorporationInventors: Beat Bohner, Georg Pissiotasa, Hans Moser
-
Patent number: 4943570Abstract: Benzimidazole-2-sulfonamide and imidazopyridine-2-sulfonamide derivatives corresponding to the general formula: ##STR1## and their pharmaceutically acceptable salts in which: Z.sup.1 to Z.sup.4 represent a nitrogen atom or a substituted or unsubstituted carbon atom;R.sup.3 represents a hydrogen atom or an alkyl, aryl, heteroaryl, alkylaryl, hydroxyalkyl, alkylheteroaryl, mono-, bi- or tri-cycloalkyl, alkylamino, N-alkyl-alkylamino, alkylcarboxyalkyl, acyl, alkylthioalkyl, alkylsulfinylalkyl or alkylsulfonylalkyl, alkylthioaryl, alkylsulfinylaryl or alkylsulfonylaryl, alkylthioheteroaryl, alkylsulfinylheteroaryl or alkylsulfonylheteroaryl, alkylthioalkylaryl, alkylsulfinylalkylaryl or alkylsulfonylalkylaryl, alkylthioalkylheteroaryl, alkylsulfinylalkylheteroaryl or alkylsulfonylalkylheteroaryl, halogenoalkyl, cyanoalkyl, N-alkylaryl-alkylamino, N-alkyl-N-alkylaryl-alkylamino, N,N-dialkyl-alkylamino, alkylpiperazinyl, alkylpiperidinyl or alkylmorpholinyl radical;X represents --(CHR.sup.8).sub.n --(CHR.sup.9).Type: GrantFiled: April 28, 1989Date of Patent: July 24, 1990Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Jordi F. Constansa, Juan P. Corominas, Augusto C. Pinol
-
Patent number: 4935415Abstract: UCN-01 having an anti-tumor activity and an anti-bacterial activity is produced by culturing a microorganism belonging to the genus Streptomyces.Type: GrantFiled: March 20, 1987Date of Patent: June 19, 1990Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hirofumi Nakano, Isami Takahashi, Tatsuya Tamaoki, Fusao Tomita, Isao Kawamoto, Kozo Asano, Makoto Morimoto, Hisayo Nomoto
-
Patent number: 4923986Abstract: The present invention relates to novel derivatives of K-252, (8R*, 9S*, 11S*)-(-)-9-hydroxy-9-methoxycarbonyl-8-methyl-2,3,9,10-tetrahydro-8,11-ep oxy-1H,8H, 11H-2,7b,11a-triazadibenzo[a,g]cycloocta-[c,d,e,]trinden-1-one, and the compounds are represented by formula (I): ##STR1## wherein W.sub.1, W.sub.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X and Y represent various substituents. The compounds are physiologically active substances that inhibit protein kinase C and exhibit an antitumor activity, and are useful as medicines.Type: GrantFiled: November 8, 1988Date of Patent: May 8, 1990Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Chikara Murakata, Akira Sato, Mitsuru Takahashi, Eiji Kobayashi, Makoto Morimoto, Shiro Akinaga, Tadashi Hirata, Kenichi Mochida, Hiroshi Kase, Koji Yamada, Kazuyuki Iwashashi
-
Patent number: 4871387Abstract: New pyri(mi)dyl-oxy- or -thio-benzoic acid derivatives of the formula ##STR1## are taught which have herbicidal and plant growth regulating activity. In the formula Z can be Ch or N, X is oxygen or sulphur, A is oxygen, sulphur, a radical R.sup.5 --N.dbd.or a radical R.sup.6 O--N.dbd.and B is oxygen, sulphur, a radical ##STR2## with the proviso that at least one of the radicals R.sup.1, R.sup.2 or R.sup.3 represents alkyl or a part of a 3- to 6-membered fused carbocyclic ring.Type: GrantFiled: December 4, 1986Date of Patent: October 3, 1989Assignee: Bayer AktiengesellschaftInventors: Klaus Sasse, Reiner Fischer, Hermann Hagemann, Hans-Joachim Santel, Robert R. Schmidt, Kalus Lurssen
-
Patent number: 4789394Abstract: Novel bicyclic triazole compounds of the formula I have an excellent herbicidal and plant-growth regulating action.The compounds correspond to the formula I ##STR1## wherein Q is hydrogen or halogen,T is halogen, andZ is a radical --XR or --COXR, in whichX is oxygen, sulfur or a radical --NR.sub.1 --,R is hydrogen, a C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl or C.sub.3 -C.sub.6 -alkynyl radical, which is unsubstituted or substituted by halogen, or is a radical --A--COXR.sub.1, in whichA is a C.sub.1 -C.sub.4 -alkylene bridge andR.sub.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.4 -alkenyl or C.sub.3 -C.sub.4 -alkynyl.Type: GrantFiled: July 17, 1986Date of Patent: December 6, 1988Assignee: Ciba-Geigy CorporationInventors: Beat Bohner, Georg Pissiotas, Hans Moser
-
Patent number: 4775406Abstract: The salts of 1-phenylimidazole-5-carboxylic acids substituted in the phenyl ring, of the general formula (I) ##STR1## exhibit a good plant growth-regulating activity. In the general formula the symbols have the following meaning:Y is an ammonium ion substituted up to fourfold by (substituted) alkyl, (substituted) alkenyl, alkynyl, (substituted) cycloalkyl, cycloalkenyl, and (substituted) phenyl, wherein the charged N may be part of a heterocyclic radial (NH.sub.4.sup.+ is excepted); phosphonium ion substituted fourfold by alkyl, (substituted) phenyl or (substituted) benzyl; sulfonium- or sulfoxonium ion substituted threefold by alkyl, (substituted) phenyl or (substituted) benzyl; the guanidinium ion or an O-alkylisourea cation;R.sup.1, R.sup.2 independently of each other are alkyl;R.sup.3 is alkyl, alkoxy or halogen; andn is 0, 1, 2 or 3.Type: GrantFiled: November 21, 1985Date of Patent: October 4, 1988Assignee: Hoechst AktiengesellschaftInventors: Roland Schmierer, Ernst-Friedrich Schulze, Helmut Bustell, Erwin Hacker
-
Patent number: 4769455Abstract: The invention relates to new benzodisultams of the general formula (I) ##STR1## in which R.sup.1 represents an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aralkyl and aryl,R.sup.2 represents hydrogen or an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl and aralkyl, andR.sup.3 represents an optionally substituted and/or optionally fused six-membered aromatic heterocyclic radical which contains at least one nitrogen atom,a process for their preparation and their use as herbicides.Type: GrantFiled: February 12, 1987Date of Patent: September 6, 1988Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Diehr, Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Theodor Pfister, Uwe Priesnitz, Hans-Jochem Riebel, Wolfgang Roy, Hans-Joachim Santel, Robert R. Schmidt
-
Patent number: 4751316Abstract: Novel 1,5-benzoxathiepin derivatives of the formula: ##STR1## [wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl or optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom; X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated; Y is >C.dbd.O or >CH--OR.sub.5 (wherein R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl); m is an integer of 0 to 2; n is an integer of 1 to 6] and salts thereof exhibit serotonin S.sub.Type: GrantFiled: April 15, 1987Date of Patent: June 14, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Minoru Hirata
-
Patent number: 4690929Abstract: Compounds of formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen or halogen atom or a methyl, cyano, C.sub.1 -C.sub.4 alkylthio or phenylthio group; R.sub.7 and R.sub.8 represent hydrogen atoms and R.sub.3 represents a hydrogen atom or a methoxy group, or R.sub.7 represents a hydrogen atom and R.sub.3 and R.sub.8 taken together represent a bond, or R.sub.3 represents a hydrogen atom or a methoxy group and R.sub.7 and R.sub.8 taken together represent a bond; R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; R.sub.5 represents a hydrogen atom or a hydrocarbon group having from 1 to 4 carbon atoms or a phenyl group; X represents an oxygen or sulphur atom or an imino group, R.sub.9 represents a hydrogen atom and B represents a cyano, a C.sub.2 -C.sub.5 alkoxycarbonyl or carbamoyl group, or R.sub.Type: GrantFiled: April 26, 1984Date of Patent: September 1, 1987Assignee: Farmitalia Carlo ErbaInventors: Luigi Bernardi, Laura Chiodini, Sergio Mantegani, Daniela Ruggieri, Aldemio Temperilli, Patricia Salvati
-
Patent number: 4672064Abstract: Novel 1,5-benzoxathiepin derivatives of the formula: ##STR1## [wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl or optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom; X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated; Y is ##STR2## (wherein R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl); m is an integer of 0 to 2; n is an integer of 1 to 6] and salts thereof exhibit serotonin S.sub.Type: GrantFiled: December 10, 1985Date of Patent: June 9, 1987Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Minoru Hirata