Plural Oxazine Rings Patents (Class 544/72)
  • Patent number: 9550740
    Abstract: Provided are compounds which are useful for controlling microorganisms in aqueous or water-containing systems or in systems which are exposed to moisture, including at elevated temperature. The antimicrobial compounds are of the formula I: wherein n, R1, R2, R3, R4, R5, and X are as defined herein.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: January 24, 2017
    Assignees: ROHM AND HAAS COMPANY, DOW GLOBAL TECHNOLOGIES LLC
    Inventors: Charles E. Coburn, Thomas Koehler, Heather R. Mcginley, Asghar A. Peera
  • Publication number: 20150148328
    Abstract: The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH2)m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO2 —Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)?N—ORc, —CO 2 Rd, —CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.
    Type: Application
    Filed: June 21, 2013
    Publication date: May 28, 2015
    Inventors: Youssef El-Ahmad, Bruno Filoche-Romme, Jean-Philippe Letallec, Gilbert Marciniak, Baptiste Ronan, Bertrand Vivet, Maurice Brollo
  • Publication number: 20150099730
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.
    Type: Application
    Filed: September 6, 2013
    Publication date: April 9, 2015
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Peter J. Connolly
  • Publication number: 20150080363
    Abstract: The present invention relates to compounds defined by formula I: wherein the variables A1, A2, Cy1 Cy2, Cy3, E, R1a, R1b, R2, R3, n, and Q are as defined herein, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Application
    Filed: September 26, 2014
    Publication date: March 19, 2015
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Katerina Leftheris, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Linghang Zhuang
  • Publication number: 20130244993
    Abstract: The present invention relates to compounds defined by formula I: wherein the variables A1, A2, Cy1 Cy2, Cy3, E, R1a, R1b, R2, R3, n, and Q are as defined herein, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Application
    Filed: June 15, 2011
    Publication date: September 19, 2013
    Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, VITAE PHARMACEUTICALS, INC.
    Inventors: Katerina Leftheris, Linghang Zhuang, Colin M. Tice, Suresh B. Singh, Yuanjie Ye, Zhenrong Xu
  • Publication number: 20120196863
    Abstract: The present invention provides 1,4 Oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: January 25, 2012
    Publication date: August 2, 2012
    Inventors: Matteo Andreini, Emanuele Gabellieri, Robert Narquizian, Massimiliano Travagli, Wolfgang Wostl
  • Publication number: 20120165309
    Abstract: [Object] A novel and excellent method for preventing or treating rejection in the transplantation of various organs, allergy diseases, autoimmune diseases, hematologic tumor, or the like, based on a PI3K?-selective inhibitory action and/or an IL-2 production inhibitory action, and/or a B cell proliferation inhibitory action (including an activation inhibitory action), is provided [Means for Solution] It was found that a 3-substituted triazine or 3-substituted pyrimidine derivative exhibits a PI3K?-selective inhibitory action, and/or an IL-2 production inhibitory action, and/or a B cell proliferation inhibitory action (including an activation inhibitory action), and can be an agent for preventing or treating rejection in the transplantation of various organs, allergy diseases (asthma, atopic dermatitis, etc.), autoimmune diseases (rheumatoid arthritis, psoriasis, ulcerative colitis, Crohn's disease, systemic lupus erythematosus, etc.), hematologic tumor (leukemia etc.
    Type: Application
    Filed: February 10, 2010
    Publication date: June 28, 2012
    Applicant: Astellas Pharma Inc.
    Inventors: Fumie Takahashi, Sunao Imada, Masahiko Shiwaku, Yasumasa Shiwaku, Atsuko Shiwaku, Koji Kato, Hidehiko Fukahori
  • Patent number: 8080605
    Abstract: Polymer-filler coupling compounds with the formula B-A-Sx—N are claimed. In these compounds, B is an azaheterocyclic oxygen or sulfur containing moiety, or an allyltin moiety; Sx is a polysulfide, where x is between 2 and about 10; A is a linking atom or group that forms a bridge between B and Sx; and N is a blocking group. Sx can be a disulfide. N can be a conventional blocking group or other group such as -A-B. Methods for using the polymer-filler coupling compounds to modify polymers containing unsaturated carbon-carbon bonds and promote filler dispersion are also claimed. Additionally, vulcanizable rubber compositions containing the polymer-filler coupling compounds and methods for making vulcanized rubber compositions using the polymer-filler coupling compounds are also claimed.
    Type: Grant
    Filed: December 28, 2006
    Date of Patent: December 20, 2011
    Assignee: Bridgestone Corporation
    Inventors: Yasuo Fukushima, William L. Hergenrother, Russell W. Koch
  • Publication number: 20110144098
    Abstract: This invention relates to 5,6-dihydro-4H-[1,3]oxazin-2-ylamine compounds of the formula wherein R1 to R5 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.
    Type: Application
    Filed: December 2, 2010
    Publication date: June 16, 2011
    Inventors: David Banner, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Mark Rogers-Evans
  • Publication number: 20110015157
    Abstract: This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih); (Ii); (Ij), (Ik), (II) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Application
    Filed: July 25, 2008
    Publication date: January 20, 2011
    Inventors: David A. Claremon, Wei He, Gerard McGeehan, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Wei Zhao, Linghang Zhuang, Salvacion Cacatian, Katerina Leftheris
  • Publication number: 20100249092
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: December 29, 2009
    Publication date: September 30, 2010
    Applicant: Avila Therapeutics, Inc.
    Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
  • Patent number: 7649060
    Abstract: The present invention relates to curable compositions of benzoxazines, a combination of adducts one of which is prepared from hydroxy-containing compounds, isocyanate-containing compounds and phenolic compounds and the second of which is prepared from the first adduct and epoxy-containing compounds and phenolic compounds, epoxy resins and optionally tougheners.
    Type: Grant
    Filed: December 2, 2005
    Date of Patent: January 19, 2010
    Assignee: Henkel Corporation
    Inventors: Wei Helen Li, Stanley L. Lehmann, Raymond S. Wong
  • Patent number: 7053138
    Abstract: Compounds of formula (I) or (II), wherein R1 is C1–C18alkyl; C5–C12cycloalkyl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups; C5–C22aryl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups; or C7–C30aralkyl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups, and the radicals R2 to R13 are each independently of the others hydrogen; —NO2; dialkylamino; alkylthio; alkylsulfonyl; halogen; C1–C18alkyl; C1–C18alkoxy; C1–C18alkoxyalkyl; C5–C12cycloalkyl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups; C5–C22aryl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups; or C7–C30aralkyl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups, are suitable as flame-proofing agents for thermoplastic or thermosetting polymers
    Type: Grant
    Filed: November 20, 2001
    Date of Patent: May 30, 2006
    Assignee: Huntsman Advanced Materials Americas Inc.
    Inventors: Franck Magendie, Ulrich Weidmann
  • Patent number: 6756370
    Abstract: The invention relates to compounds of formula (I), wherein R1, R2 and A have the meanings given in claim 1, are potent 5-HT2A antagonists and are suitable for treating psychoses, schizophrenia, depression, neurological disorders, impaired memory, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia and anorexia nervosa, Pre-Menstrual Syndrome and/or for positively influencing obsessive-compulsive disorders, (OCD).
    Type: Grant
    Filed: February 21, 2002
    Date of Patent: June 29, 2004
    Assignee: Merck Patent GmbH
    Inventors: Helmut Prücher, Henning Böttcher, Karl-August Ackermann, Rudolf Gottschlich, Christoph van Amsterdam, Christoph Seyfried, Jürgen Harting, Gerd Bartoszyk, Hartmut Greiner
  • Patent number: 6579982
    Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: August 9, 2000
    Date of Patent: June 17, 2003
    Assignee: Pfizer Inc.
    Inventor: Julian Blagg
  • Publication number: 20020049204
    Abstract: This invention provides compounds of Formula (I): 1
    Type: Application
    Filed: September 6, 2001
    Publication date: April 25, 2002
    Inventors: Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
  • Patent number: 6339153
    Abstract: A method making sulfhydryl scavenging agents with reduced water content comprising treating the sulfhydryl scavenging agent to remove water. The sulfyhydryl scavenging agent preferably comprises an —N—C—N— moiety produced by condensation of an alkanolamine with an aldehyde. Preferred sulfhydryl scavenging agents are bisoxazolidines.
    Type: Grant
    Filed: August 4, 2000
    Date of Patent: January 15, 2002
    Assignee: Baker Hughes Incorporated
    Inventors: Gordon T. Rivers, James Hackerott
  • Patent number: 5523411
    Abstract: The present invention relates to the synthesis of mitomycin and analogs thereof that are useful as anticancer antibiotics. The invention further relates to analogs of mitomycin, which can be prepared according to the methods of synthesis provided. The synthetic method of the invention provides for reacting a derivitized indole with a dialkylvinylsulfonium salt to yield a tricyclic skeleton having the precursors of the fourth ring in one step, followed by an oxidation step or steps to close the fourth ring and prepare mitomycin or a related compound.
    Type: Grant
    Filed: March 14, 1994
    Date of Patent: June 4, 1996
    Assignee: Rutgers University
    Inventors: Leslie Jimenez, Zheng Wang
  • Patent number: 5498686
    Abstract: An optically transparent photochromic plastic material is described which is comprised of materials with a sulphur content and which via polymerization processes contains photochromic organic compounds as solid ingredients, which possess at least two ring systems linked via carbon atom and whose photochromic tint is based on a reversible bond rupture to the spiro-C atom.
    Type: Grant
    Filed: December 9, 1994
    Date of Patent: March 12, 1996
    Assignee: Optische Werke G. Rodenstock
    Inventors: Erhard Effer, Manfred Melzig, Herbert Schuster, Guiseppe Martinuzzi
  • Patent number: 5496943
    Abstract: Disclosed is a novel heterocyclic compound selected from the group consisting of the compounds [IV] to [VII], [IX] and [X]. The heterocyclic compound is useful for reactive materials in chemical industry. A process for producing the heterocyclic compound is also disclosed.
    Type: Grant
    Filed: March 13, 1992
    Date of Patent: March 5, 1996
    Assignee: Nippon Paint Co., Ltd.
    Inventors: Otohiko Tsuge, Taizo Hatta, Satoshi Urano, Noriyuki Tsuboniwa, Ryuzo Mizuguchi
  • Patent number: 5268473
    Abstract: Azlactone-functional Michael adducts are disclosed which are the Michael reaction products of 2-alkenyl azlactones and Michael donors selected from carbon and nitrogen nucleophiles. Reaction products which contain a plurality of azlactone groups are useful as step growth monomers in adhesives, sealants, and coatings.
    Type: Grant
    Filed: June 26, 1992
    Date of Patent: December 7, 1993
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Dean M. Moren, Steven M. Heilmann, Larry R. Krepski, Jerald K. Rasmussen
  • Patent number: 5268474
    Abstract: The invention relates to an improved process for the preparation of dyestuffs based on at least one triphendioxazine which is linked to a further chromophore via a triazine at a pH of 5.5 to 2.0 and a temperature of 50 to 100.degree. C.
    Type: Grant
    Filed: January 9, 1992
    Date of Patent: December 7, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventor: Horst Jager
  • Patent number: 5250521
    Abstract: Novel substituted pyrazolopyrimidines of formula (I) which are useful as angiotensin II antagonists, are disclosed.
    Type: Grant
    Filed: November 25, 1991
    Date of Patent: October 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Eric E. Allen, William J. Greenlee, Prasun K. Chakravarty, Malcolm MacCoss, Arthur A. Patchett, Thomas F. Walsh
  • Patent number: 5217706
    Abstract: Novel magnetic resonance imaging agents comprise complexes of paramagnetic ions with hydrazide derivatives of polyaminocarboxylic acid chelating agents. These novel imaging agents are characterized by excellent NMR image-contrasting properties and by high solubilities in physiological solutions.A novel method of performing an NMR diagnostic procedure involves administering to a warm-blooded animal an effective amount of a complex as described above and then exposing the warm-blooded animal to an NMR imaging procedure, thereby imaging at least a portion of the body of the warm-blooded animal.
    Type: Grant
    Filed: June 3, 1992
    Date of Patent: June 8, 1993
    Assignee: Mallinckrodt Medical, Inc.
    Inventors: Raghavan Rajagopalan, Rebecca A. Wallace, Muthunadar P. Periasamy
  • Patent number: 5196531
    Abstract: A novel poly(N-cyclic iminoether) compound and a process for production thereof which comprises (a) reacting a polyisocyanate compound with a haloalkyleneamine or (b) reacting a polyamine with an alkyl isocyanate, and then (c) cyclizing the resulting polyurea compound. Several thermosetting compositions containing the novel poly(N-cyclic iminoether) and thermoset resins therefrom are also proposed.
    Type: Grant
    Filed: August 18, 1992
    Date of Patent: March 23, 1993
    Assignee: Teijin Limited
    Inventors: Hiroyuki Umetani, Hiroshi Mera, Hiroo Inata, Shunichi Matsumura
  • Patent number: 5149806
    Abstract: Azlactone-functional Michael adducts are disclosed which are the Michael reaction products of 2-alkenyl azlactones and Michael donors selected from carbon and nitrogen nucleophiles. Reaction products which contain a plurality of azlactone groups are useful as step growth monomers in adhesives, sealants, and coatings.
    Type: Grant
    Filed: March 28, 1990
    Date of Patent: September 22, 1992
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Dean M. Moren, Steven M. Heilmann, Larry R. Krepski, Jerald K. Rasmussen
  • Patent number: 5097027
    Abstract: Heterocyclic compounds of the formula ##STR1## are used as pigments for surface coatings and for coloring and pigmenting high molecular weight organic material.
    Type: Grant
    Filed: October 5, 1990
    Date of Patent: March 17, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventor: Hans Hochstetter
  • Patent number: 5081197
    Abstract: This invention provides novel azlactone-functional oligomers of 2-alkenyl azlactones in which oligomerization has occurred predominantly via the 2-alkenyl group. Oligomerization of the 2-alkenyl group provides oligomers having 2 to 15 mer units with predominantly carbon-carbon backbone segments. Oligomerized in this fashion, the novel compositions possess azlactone groups which can be reacted with nucleophiles in the normal ring-opening sense. The oligomers are prepared by a novel process in which both Lewis and Bronsted acidic catalysts are effective. The reactive oligomers find utility as crosslinking agents for polymers containing azlactone-reactable nucleophilic groups.
    Type: Grant
    Filed: October 23, 1990
    Date of Patent: January 14, 1992
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Steven M. Heilmann, Dean M. Moren, Jerald K. Rasmussen, Larry R. Krepski, Sadanand V. Pathre
  • Patent number: 5071636
    Abstract: A polyaminedithiol compound of the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.11 and R.sub.12 are each a lower alkyl group, R.sub.21 is a hydrogen atom or a lower alkyl group, and R.sub.3 and R.sub.13 are each a hydrogen atom or a nitrogen-containing organic group, provided that at least one of R.sub.3 and R.sub.13 is a nitrogen-containing organic group, which is used for imaging of the regional cerebral blood flow.
    Type: Grant
    Filed: December 28, 1988
    Date of Patent: December 10, 1991
    Assignee: Nihon Medi-Physics Co., Ltd.
    Inventors: Hirohiko Yamauchi, Jun Takahashi, Sakae Okano, Shigemi Seri, Makoto Azuma
  • Patent number: 4977260
    Abstract: Process for preparing mono-, bi- and tricyclic amino acids, intermediates of this process, and a process for preparing same.The invention relates to a process for preparing compounds of the formula I ##STR1## in which R stands for hydrogen, alkyl or aralkyl and R.sup.1 to R.sup.5 are identical or different radicals, (substituted) alkyl, cycloalkyl or (substituted) aryl or in which the pairs of radicals R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, and R.sup.4 and R.sup.5 together with the carbon atom(s) supporting them form a mono- or bicyclic ring system and the other radicals are hydrogen, by treating a compound of the formula II ##STR2## in which R and R.sup.1 to R.sup.5 have the abovoementioned meaning and R.sup.6 and R.sup.7 denote alkyl or aralkyl or together with the nitrogen atom supporting them form a heterocycle which can additionally contain an oxygen atom, with a reducing agent.
    Type: Grant
    Filed: April 10, 1989
    Date of Patent: December 11, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rainer Henning, Hansjorg Urbach
  • Patent number: 4908356
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 may be the same of different and are each independently hydrogen or lower alkyl which may be unsubstituted or monosubstituted with halogen, lower alkoxy or hydroxy with the proviso that the substituent is not the .alpha.-carbon or R.sup.1 and R.sup.2 taken together with the carbon to which they are attached form a morpholino ring;each R.sup.3 is independently hydrogen, lower alkyl, carboxy or carbalkoxy;n is an integer from 0, 1, 2 or 3 andR is hydrogen, lower alkyl, cycloalkyl, arylalkyl aryl or a nitrogen, sulfur or oxygen containing heterocyclic or a heterocyclic lower alkyl and pharmacuetically acceptable salts thereof.
    Type: Grant
    Filed: May 25, 1988
    Date of Patent: March 13, 1990
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, Ronald R. Valente
  • Patent number: 4897105
    Abstract: A compound of the general formula ##STR1## wherein R.sub.1 is a phenyl group which may be substituted, R.sub.2 and R.sub.3 respectively are a lower alkyl or lower alkoxy group, Z is CH or N and n is 0 or 1, or a salt thereof which is useful as a herbicide.
    Type: Grant
    Filed: March 20, 1987
    Date of Patent: January 30, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yoshiyuki Okada, Isao Aoki, Nobuyuki Okajima, Takashi Kuragano
  • Patent number: 4849524
    Abstract: The invention relates to a process for preparing compounds of the formula I ##STR1## in which R stands for hydrogen, alkyl or aralkyl and R.sup.1 to R.sup.5 are identical or different radicals, (substituted) alkyl, cycloalkyl or (substituted) aryl or in which the pairs of radicals R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, and R.sup.4 and R.sup.5 together with the carbon atom(s) supporting them form a mono- or bicyclic ring system and the other radicals are hydrogen, by treating a compound of the formula II ##STR2## in which R and R.sup.1 and R.sup.5 have the abovementioned meaning and R.sup.6 and R.sup.7 denote alkyl or aralkyl or together with the nitrogen atom supporting them form a heterocycle which can additionally contain an oxygen atom, with a reducing agent.
    Type: Grant
    Filed: November 19, 1987
    Date of Patent: July 18, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rainer Henning, Hansjorg Urbach
  • Patent number: 4838925
    Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.
    Type: Grant
    Filed: September 25, 1987
    Date of Patent: June 13, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 4748184
    Abstract: The present invention relates to new compounds of the formula ##STR1## wherein X is ##STR2## wherein R.sub.1 is hydrogen, lower alkyl, phenyl, benzyl, cinnamoyl, thiophene, furan, pyrrole, imidazole, pyrazole oxazole or thiazole; W is hydrogen or hydroxy; (Y).sub.A is positioned ortho to W and is an aminoloweralkyl having the formula --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 are the same or different and may be lower alkyl or R.sub.2 and R.sub.3 may together with N form a pyrrolidine, piperidine or azepine ring, and A is 2; n and m are independently from 0 to 5; and R is straight or branched C.sub.1 -C.sub.10 alkyl, straight or branched C.sub.3 -C.sub.10 cycloalkyl, straight or branched C.sub.2 -C.sub.4 alkenyl or straight or branched C.sub.2 -C.sub.4 alkynyl, or a pharmaceutically acceptable salt thereof.These compounds are useful in the treatment of various cardiac arrhythmias.
    Type: Grant
    Filed: December 27, 1985
    Date of Patent: May 31, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: David M. Stout, William L. Matier, Lawrence A. Black
  • Patent number: 4741765
    Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.
    Type: Grant
    Filed: April 3, 1987
    Date of Patent: May 3, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
  • Patent number: 4737184
    Abstract: Novel N-(heterocyclicaminocarbonyl) substituted thiophene-, furan- and pyrrolesulfonamides, such as N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno- [3,2-b]thiopyran-3-sulfonamide, 4,4-dioxide and N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno[3,2-b ]thiopyran-3-sulfonamide, 4,4-dioxide and their method-of-use as herbicides are described.
    Type: Grant
    Filed: May 10, 1985
    Date of Patent: April 12, 1988
    Assignee: E. I. Du Pont De Nemours and Company
    Inventor: Robert J. Pasteris
  • Patent number: 4715984
    Abstract: Dihydroazines of the formula IR.sub.1 --A.sup.1 --Z.sub.1 --A.sub.2 --R.sup.2 Iwherein R.sup.1, R.sup.2, A.sup.1, A.sup.2 and Z.sub.1 have the meanings specified herein may be used as components of liquid crystalline phases.
    Type: Grant
    Filed: January 22, 1986
    Date of Patent: December 29, 1987
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Joachim Krause, Wachtler, Bernhard Scheuble
  • Patent number: 4689414
    Abstract: 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: Grant
    Filed: February 24, 1986
    Date of Patent: August 25, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4684656
    Abstract: 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: Grant
    Filed: March 14, 1986
    Date of Patent: August 4, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4683228
    Abstract: 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: Grant
    Filed: January 22, 1985
    Date of Patent: July 28, 1987
    Assignees: ICI Americas Inc., Imperial Chemical Industries PLC
    Inventors: Karin M. Kirkland, Derrick M. Mant
  • Patent number: 4666902
    Abstract: Tetrahydropyridazinones of the formula I ##STR1## wherein R denotes an optionally substituted carbocyclic or heterocyclic radical, R.sup.1 denotes hydrogen; alkyl; aralkyl, which is optionally substituted in the aryl part; or acyl, and R.sup.2 denotes hydrogen; alkyl, which can optionally be substituted; or optionally substituted phenyl; and their acid addition compounds, if these can be prepared.The tetrahydropyridazinone derivatives of the formula I according to the invention and their physiologically acceptable salts exhibit useful pharmacological actions.
    Type: Grant
    Filed: June 8, 1984
    Date of Patent: May 19, 1987
    Assignee: Cassella Aktiengesellschaft
    Inventors: Gerhard Zoller, Rudi Beyerle, Melitta Just, Piero Martorana, Helmut Bohn, Rolf-Eberhard Nitz
  • Patent number: 4647557
    Abstract: This invention relates to novel heterocyclic derivatives bearing an amino group and to processes for making said compounds.More particularly this invention provides novel heterocyclic compounds the hetero ring of which has two hetero atoms, the same or different, substituted with a free or substituted amino group.These compounds are useful as active ingredients of drugs.
    Type: Grant
    Filed: December 23, 1983
    Date of Patent: March 3, 1987
    Inventors: Gerard Moinet, Michel Schaeffer, Pierre Bessin, Jacqueline Bonnet
  • Patent number: 4629495
    Abstract: Herbicidal compounds of the formula: ##STR1## wherein A represents R.sup.1 R.sup.2 N-- (wherein R.sup.1 represents C.sub.1-8 alkyl or C.sub.2-8 alkenyl or alkynyl unsubstituted or substituted by CN, OH, C.sub.1-6 alkoxy, carboxy, C.sub.2-9 alkoxycarbonyl, aminocarbonyl optionally substituted by C.sub.1-8 alkyl or C.sub.2-8 alkenyl, C.sub.1-8 alkoxyaminocarbonyl, C.sub.1-8 alkanesulphonamidocarbonyl, --C(.dbd.O)Het, where Het represents a nitrogen-containing heterocyclic group, or one or more halogen atoms or R.sup.1 represents C.sub.3-6 cycloalkyl optionally substituted by C.sub.1-4 alkyl and R.sup.2 represents H or R.sup.1, or R.sup.1 represents C.sub.1-4 alkylthio and R.sup.2 represents H, or A represents R.sup.p (R.sup.q)--C.dbd.N-- (wherein R.sup.p represents C.sub.1-4 alkoxy or amino substituted by one or two C.sub.1-4 alkyl groups and R.sup.q represents H or C.sub.1-4 alkyl) or A represents 2-oxo-azetidin-1-yl, 2-oxo-pyrrolidin-1-yl or 2-oxo-piperidin-1-yl optionally substituted by C.sub.
    Type: Grant
    Filed: July 13, 1983
    Date of Patent: December 16, 1986
    Assignee: May & Baker Limited
    Inventors: Leslie R. Hatton, Edgar W. Parnell, David A. Roberts
  • Patent number: 4485236
    Abstract: Azlactone-functional compounds, which are liquid above 20.degree. C., and their method of preparation from alkenyl azlactones and nucleophilic group-substituted compounds are disclosed. The azlactone-functional compounds of the invention cure in the presence of nucleophilic chain-extending or crosslinking agents to form linear or crosslinked polyamide resin systems.
    Type: Grant
    Filed: September 27, 1982
    Date of Patent: November 27, 1984
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Jerald K. Rasmussen, Steven M. Heilmann, Frederick J. Palensky
  • Patent number: 4440949
    Abstract: A new class of chemical compounds and their process of preparation is described. These compounds have valuable properties as anti-secretory, anti-spasmodic, anti-ulcerogenic and anti-diarrheal agents.
    Type: Grant
    Filed: December 30, 1980
    Date of Patent: April 3, 1984
    Assignee: William H. Rorer, Inc.
    Inventors: George H. Douglas, William L. Studt, Stuart A. Dodson
  • Patent number: 4430501
    Abstract: This disclosure describes symmetrical 1,4-bis(substituted-amino)-5,8-dihydroxyanthraquinones useful as chelating agents and for inhibiting the growth of transplanted mouse tumors.
    Type: Grant
    Filed: November 2, 1981
    Date of Patent: February 7, 1984
    Assignee: American Cyanamid Company
    Inventors: Keith C. Murdock, Frederick E. Durr
  • Patent number: 4410524
    Abstract: This disclosure describes novel 1,4,-bis(substituted-amino)-5,8-dihydroxyanthraquinones and leuco bases thereof, useful as chelating agents and for inhibiting the growth of transplanted mouse tumors. This disclosure also describes compositions of matter useful as inhibitors of transplanted mouse tumor growth and the method of inducing the regression and/or palliation of leukemia and related cancers in mammals therewith.
    Type: Grant
    Filed: June 1, 1982
    Date of Patent: October 18, 1983
    Assignee: American Cyanamid Company
    Inventor: Keith C. Murdock
  • Patent number: 4389399
    Abstract: Novel 1,4-di(substituted amino)-5,8-dihydroxyanthraquinones wherein the substituents are alkyl-oxazolidin-2-thion-3-yl or alkyl tetrahydro-2H-1,3-oxazine-2-thione-3-yl groups as antitumor agents and as chelating agents are described.
    Type: Grant
    Filed: February 4, 1982
    Date of Patent: June 21, 1983
    Assignee: American Cyanamid Company
    Inventor: Keith C. Murdock
  • Patent number: 4233206
    Abstract: A process for the production of a colored polyolefin molded articles comprising adding to a polyolefin either a compound of the formula D--CH.sub.2 O.OC--R]).sub.n as a colorant wherein D is the residue of a common organic pigment, R is an alkyl, alkenyl or aryl group having up to 20 carbon atoms and n is an integer of 1-4, or a mixture of the compound of the above formula with at least one usual pigment, to form a mixture, and then molding the mixture thereby producing the desired colored articles. This invention also relates to the compound of said formula and to a mixture thereof with at least one common pigment.
    Type: Grant
    Filed: November 6, 1975
    Date of Patent: November 11, 1980
    Assignee: Toyo Ink Manufacturing Co., Ltd.
    Inventors: Hiromitsu Katsura, Morihiko Endo, Takashi Kanno