Nitrogen Attached Directly To The Hetero Ring By Nonionic Bonding Patents (Class 540/605)
  • Publication number: 20020133005
    Abstract: The present invention provides an AP-1 activation inhibitor, a NF-kappaB activation inhibitor, an inflammatory cytokine production inhibitor, a production inhibitor for matrix metalloprotease or an inflammatory cell adhesion factor expression inhibitor, which contains a heterocyclic compound or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Application
    Filed: December 31, 2001
    Publication date: September 19, 2002
    Applicant: AJINOMOTO CO., INC.
    Inventors: Yukio Iino, Koichi Fujita, Ariko Kodaira, Toshihiro Hatanaka, Kenji Takehana, Tsuyoshi Kobayashi, Atsushi Konishi, Takashi Yamamoto
  • Publication number: 20020119964
    Abstract: Homoiminopiperidinyl Hexanoic Acid derivatives and pharmaceutically acceptable salts thereof useful in the inhibition of the inducible isoform of nitric oxide synthase are disclosed.
    Type: Application
    Filed: August 1, 2001
    Publication date: August 29, 2002
    Inventors: Donald W. Hansen, Jeffrey S. Snyder, Alan E. Moormann, Alok K. Awasthi, Ronald Keith Webber, Thaddeus S. Franczyk, Mahima Trivedi
  • Publication number: 20020065269
    Abstract: Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Application
    Filed: June 22, 2001
    Publication date: May 30, 2002
    Applicant: Amgen Inc.
    Inventors: Kevin Koch, Andreas Termin, John A. Josey
  • Publication number: 20020042413
    Abstract: Compound of formula (I): 1
    Type: Application
    Filed: September 26, 2001
    Publication date: April 11, 2002
    Inventors: Sylvain Rault, Olivier Renault, Jean Guillon, Patrick Dallemagne, Pierre Renard, Bruno Pfeiffer, Pierre Lestage, Marie-Cecile Lebrun
  • Publication number: 20020028797
    Abstract: This invention provides compounds of Formula I having the structure 1
    Type: Application
    Filed: July 12, 2001
    Publication date: March 7, 2002
    Applicant: American Home Products Corporation
    Inventors: Fuk-Wah Sum, Michael S. Malamas
  • Publication number: 20020022605
    Abstract: This invention provides compounds of Formula I having the structure 1
    Type: Application
    Filed: July 12, 2001
    Publication date: February 21, 2002
    Applicant: American Home Products Corporation
    Inventors: Fuk-Wah Sum, Baihua Hu
  • Publication number: 20020013310
    Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
    Type: Application
    Filed: July 30, 2001
    Publication date: January 31, 2002
    Inventors: Yong Mi Choi-Sledeski, Heinz W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong, Julian Levell
  • Patent number: 6300497
    Abstract: A process for distillative removal of part or all of an azepine derivative (III) selected from the group consisting of aminohexylideneimine, tetrahydroazepine, hexylhexahydroazepine and aminohexylhexahydroazepine from a mixture (II) comprising an azepine derivative (III) and an amine (I) comprises conducting the distillation with an overhead temperature of from 160 to 250° C.
    Type: Grant
    Filed: September 7, 2000
    Date of Patent: October 9, 2001
    Inventors: Alwin Rehfinger, Hermann Luyken
  • Patent number: 5914351
    Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: June 22, 1999
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.
    Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
  • Patent number: 5880286
    Abstract: A process for acetylating diamines having a sterically hindered amino function and a further, sterically unhindered amino function where the acetylation takes place at the sterically unhindered amino function is provided comprises reacting the diamine with ketene. A preferred diamine is 4-amino-2,2,6,6-tetramethylpiperidine (TAD).
    Type: Grant
    Filed: October 21, 1997
    Date of Patent: March 9, 1999
    Assignee: BASF Aktiengesellschaft
    Inventor: Manfred Julius
  • Patent number: 5856318
    Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 11, 1997
    Date of Patent: January 5, 1999
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 5854234
    Abstract: The current invention discloses useful pharmaceutical compositions containing azepine derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 29, 1998
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
  • Patent number: 5852009
    Abstract: The present invention relates to compositions and methods for inhibiting protein aging. Accordingly, a composition is disclosed which comprises an agent or compound capable of inhibiting the formation of advanced glycosylation end products of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. Suitable agents may contain an active nitrogen-containing group, such as a hydrazine group. Particular agents comprise aminoguanidine, .alpha.-hydrazinohistidine and mixtures thereof. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
    Type: Grant
    Filed: January 16, 1997
    Date of Patent: December 22, 1998
    Assignee: The Rockefeller University
    Inventors: Anthony Cerami, Peter C. Ulrich, Michael A. Brownlee
  • Patent number: 5792820
    Abstract: An organolithium compound according to the present invention containing a cyclic amino group, has the general formula: ##STR1## wherein R.sub.1 is a divalent alkylene, an oxy- or amino-alkylene, or substituted alkylene having from 6 to about 20 carbon atoms; R.sub.2 is a linear-, branched-, or cyclo-alkylene having from about 2 to about 20 carbon atoms; and the lithium, Li, is bonded directly to a carbon atom of R.sub.2. A method of preparing an organolithium compound containing a cyclic amino group, comprising reacting a cyclic amino organo halide having the general formula ##STR2## where R.sub.1 and R.sub.2 are as above, and X is bromine or chlorine bonded directly to a carbon atom of R.sub.2, with a lithium reactant selected from lithium metal or an organolithium compound.
    Type: Grant
    Filed: February 23, 1996
    Date of Patent: August 11, 1998
    Assignee: Bridgestone Corporation
    Inventors: David F. Lawson, Thomas A. Antkowiak, James E. Hall, Mark L. Stayer, Jr., John R. Schreffler
  • Patent number: 5733934
    Abstract: Indenoylguanidines of formula I and formula II, the process for their preparation, their use as medicaments, medicaments containing them, their use as diagnostic agents and medicaments containing them are described. Compounds I are useful for treating cardiac arrhythmias. Further they are useful as cardioprotective agents in mammals, which comprises administering the compound of formula-I or II with the above properties in combination with pharmaceutically accepted carrier to said mammal.
    Type: Grant
    Filed: April 16, 1996
    Date of Patent: March 31, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Nigrogi Venkata Satya Ramakrishna, Tulsidas Sitaram More, Anagha Suhas Kulkarni, Bansi Lal, Rao Venkata Satya Veerabhadra Vadlamudi, Anil Vasantrao Ghate, Ravindra Dattatraya Gupte, Wolfgang Scholz, Hans Jochen Lang
  • Patent number: 5721255
    Abstract: The present invention relates to novel substituted benzylamino nitrogen containing non-aromatic heterocycles and, specifically, to compounds of the formula ##STR1## wherein W, R.sup.1, R.sup.2, R.sup.3 and A are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.
    Type: Grant
    Filed: February 15, 1995
    Date of Patent: February 24, 1998
    Assignee: Pfizer Inc.
    Inventors: Harry R. Howard, Masami Nakane, Masaya Ikunaka, Kunio Satake, Terry J. Rosen, John A. Lowe, III, Brian T. O'Neill, Fumitaka Ito
  • Patent number: 5703065
    Abstract: The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein A, W, P, R.sup.3, Q and R.sup.1 are as defined herein. The compounds of formula I, and pharmaceutically acceptable salts thereof, are substance P antagonists and as such are useful in the treament of various inflammatory and central nervous system disorders.
    Type: Grant
    Filed: May 7, 1996
    Date of Patent: December 30, 1997
    Assignee: Pfizer Inc.
    Inventor: Harry R. Howard, Jr.
  • Patent number: 5688804
    Abstract: The present invention relates to the derivatives of the compound of formula (I), which are useful in the treatment of inflammatory and central nervous system disorders, as well as other diorders ##STR1##
    Type: Grant
    Filed: January 31, 1995
    Date of Patent: November 18, 1997
    Assignee: Pfizer Inc.
    Inventor: Terry J. Rosen
  • Patent number: 5612332
    Abstract: The present invention relates to compounds, compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a di- or tri-aminoguanidine capable of inhibiting the formation of advanced glycosylation endproducts of target proteins. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 18, 1997
    Assignees: Alteon Inc., The Rockefeller University
    Inventors: Dilip R. Wagle, Peter C. Ulrich, Anthony Cerami
  • Patent number: 5530118
    Abstract: A novel benzenesulfonamide derivative represented by the formula: ##STR1## has an inhibitory activity against phospholipase A.sub.2, so that it is effective in the treatment of diseases for which such an activity is efficacious.
    Type: Grant
    Filed: December 6, 1993
    Date of Patent: June 25, 1996
    Assignee: Eisai Co., Ltd.
    Inventors: Hitoshi Oinuma, Takashi Hasegawa, Tadanobu Takamura, Kenichi Nomoto, Yoshiharu Daiku, Toshihiko Naito, Sachiyuki Hamano
  • Patent number: 5519018
    Abstract: Substituted phenols of the formula I ##STR1## processes for their preparation and compositions containing substituted phenols of the formulae I and II ##STR2## for the treatment of disorders caused by cell proliferation, such as psoriasis, tumor disorders and immunological disorders, are described.
    Type: Grant
    Filed: May 1, 1995
    Date of Patent: May 21, 1996
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Rudolf Matusch, Manfred Hunz, Jorg Czech, Hans-Harald Sedlacek
  • Patent number: 5423998
    Abstract: Amino-derivative (poly)peroxycarboxylic acids which have the formula: ##STR1## wherein the symbols have the following meanings: R, R.sub.1, and R.sub.2, which may be equal to or different from one another, represent hydrogen atoms, alkyl groups or groups selected from R, R.sub.1 and R.sub.2, which taken together with the nitrogen atom to which they are linked, give rise to an aliphatic heterocyclic group, all of them being optionally substituted;A represents a (cyclo)alkylene group, an arylene group which may also be condensed with cycloaliphatic groups, a cycloalkylene-alkylene or an alkylene-cycloalkylene group, an arylene-alkylene or an alkylene-arylene group, which may be condensed with cyclo-aliphatic groups, wherein said alkylene group may also be interrupted by --CONR.sub.3 groups, wherein R.sub.3 represents a hydrogen atom or an alkyl or aryl group;X.sup.- represents HSO.sub.4.sup.- or CH.sub.3 SO.sub.3.sup.- ; a process for their preparation; and their use as bleaching agents.
    Type: Grant
    Filed: April 13, 1993
    Date of Patent: June 13, 1995
    Assignee: Ausimont S.r.l.
    Inventors: Carlo Venturello, Claudio Cavallotti
  • Patent number: 5393762
    Abstract: The present invention relates to a method of treating or preventing emesis in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, azanorbornane derivatives and related compounds.
    Type: Grant
    Filed: June 4, 1993
    Date of Patent: February 28, 1995
    Assignee: Pfizer Inc.
    Inventors: Manoj C. Desai, John A. Lowe, III, John W. Watson
  • Patent number: 5326911
    Abstract: Ortho-amides of the formula ##STR1## can be prepared by reacting salts of the formula ##STR2## with alcoholates of the formulaM.sup.1 OR.sup.1 (III)where the radicals R.sup.1 to R.sup.4, M.sup.1 and X.sup..crclbar. have the meaning given in the description. The alcoholates are employed in highly active form with an effective content of 98-100% M.sup.1 OR.sup.1.
    Type: Grant
    Filed: July 20, 1992
    Date of Patent: July 5, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz-Ulrich Blank, Helmut Kraus, Gerhard Marzolph, Nikolaus Muller
  • Patent number: 5232929
    Abstract: The present invention relates to novel 3-aminopiperidine derivatives and related nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, Y and m are as defined below. These novel compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders. The invention also relates to novel intermediates used in the synthesis of compounds of the formula I.
    Type: Grant
    Filed: July 1, 1991
    Date of Patent: August 3, 1993
    Assignee: Pfizer Inc.
    Inventors: Manoj C. Desai, Terry J. Rosen
  • Patent number: 5196439
    Abstract: A cyclic amine is defined by the formula: ##STR1## in which A is naphthyl, phenyl, quinolyl or alkyl, X is a group containing carbonyl, n is 2 or 3 and B is alkyl, halogen, phenyl or --YZ, Y being --O--, --CO-- or --NH--, Z being phenyl, naphthyl, pyridyl, alkyl or cycloalkyl. It is useful to treat mental symptoms associated with a cerebrovascular disease.
    Type: Grant
    Filed: January 24, 1992
    Date of Patent: March 23, 1993
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Norio Karibe, Isao Saito, Kunizo Higurashi, Masahiro Yonaga, Takeru Kaneko, Takahiro Nakazawa, Masataka Ueno, Kiyomi Yamatsu, Kohshi Ueno, Masuhiro Ikeda
  • Patent number: 5189174
    Abstract: Heterocyclic thiol sulfenimide compounds are useful as an accelerator in the curing of natural and/or synthetic rubbers. The compound can be represented by the formula ##STR1## wherein each of A.sup.1 and A.sup.2, independently, is at least one heterocyclic ring containing one or more nitrogen atoms therein, or at least one heterocyclic ring containing one or more nitrogen atoms therein and (1) one or more hydrocarbyl substituents, or (2) one or more electron withdrawing groups, or (3) one or more electron releasing groups, wherein A.sup.
    Type: Grant
    Filed: September 23, 1991
    Date of Patent: February 23, 1993
    Assignee: Monsanto Company
    Inventor: Charles J. Rostek, Jr.
  • Patent number: 5041545
    Abstract: 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: Grant
    Filed: April 6, 1989
    Date of Patent: August 20, 1991
    Assignee: Atochem North America, Inc.
    Inventor: Terry N. Myers
  • Patent number: 4906678
    Abstract: Compounds of the formula (I) ##STR1## wherein R.sub.1 and R.sub.5 are independently hydrogen, C.sub.1 -C.sub.12 -alkyl, C.sub.5 -C.sub.7 -cycloalkyl or a group of the formula (II), ##STR2## R.sub.2, R.sub.3 and R.sub.4 are independently C.sub.2 -C.sub.12 -alkylene, R is a group of the formula (III) ##STR3## wherein R.sub.6 is C.sub.2 -C.sub.8 -dialkylamino, C.sub.1 -C.sub.4 -alkoxy, a 5-membered to 7-membered heterocyclic group containing a nitrogen atom which is attached to the triazine residue or a group of the formula (IV), ##STR4## R.sub.7 and R.sub.8 are independently C.sub.1 -C.sub.12 -alkyl, C.sub.5 -C.sub.7 -cycloalkyl, benzyl or a group of the formula (II), subject to the proviso that both, R.sub.1 and R.sub.5 are different from hydrogen, if R is a group ##STR5## are useful as light stabilizers, heat stabilizers and/or oxidation stabilizers for organic materials, in particular synthetic polymers.
    Type: Grant
    Filed: October 31, 1988
    Date of Patent: March 6, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Giuseppe Cantatore, Francois Gugumus
  • Patent number: 4877874
    Abstract: There is disclosed a process for producing N-aminohexamethyleneimine, which comprises allowing hexamethyleneimine to react with hydroxylamine-O-sulfonic acid in the presence of an aqueous solvent and an inorganic base.
    Type: Grant
    Filed: May 26, 1987
    Date of Patent: October 31, 1989
    Assignee: Ube Indrustries, Ltd.
    Inventors: Minoru Kawano, Katsumi Simizu, Eiji Isonaga, Shigeo Kurata
  • Patent number: 4822792
    Abstract: Compounds of formula: ##STR1## in which R and R' each denote an alkyl or cycloalkyl radical having 1 to 7 carbon atoms; X denotes --O-- or H.sub.2 ; and Y and Z denote hydrogen or one or more radicals chosen from halogeno, hydroxy, straight or branched alkyl having 1 to 6 carbon atoms, alkoxy having 1 to 6 carbon atoms, trifluoromethyl or methylenedioxy; n being able to assume the values 2 or 3; and their pharmaceutically acceptable salts.Application as a cardiovascular medicinal product.
    Type: Grant
    Filed: December 22, 1987
    Date of Patent: April 18, 1989
    Assignee: Riom Laboratoires C.E.R.M.
    Inventors: Patrick Carlier, Jacques A. Simond, Andre J. Monteil
  • Patent number: 4774331
    Abstract: A process for ortho-cyanation of phenols or phenylamines which comprises reacting a phenyl compound having hydroxy or optionally substituted amino or cyclic amino, of which ortho position is vacant, with trichloroacetonitrile, C.sub.1 -C.sub.5 alkyl thiocyanate or C.sub.6 -C.sub.12 aryl thiocyanate in the presence of a boron trihalide and treating the resultant product with an alkali is provided, and said process is useful in the synthesis of intermediates for medicinals or pesticides.
    Type: Grant
    Filed: August 21, 1987
    Date of Patent: September 27, 1988
    Assignee: Shionogi & Co., Ltd.
    Inventors: Makoto Adachi, Hiromu Matsumura, Tsutomu Sugasawa
  • Patent number: 4698442
    Abstract: .alpha.-amino acids having a substituted .omega.-guanidino group are disclosed herein.
    Type: Grant
    Filed: June 13, 1986
    Date of Patent: October 6, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John J. Nestor, Brian H. Vickery
  • Patent number: 4629739
    Abstract: Novel substituted sulfonamidobenzamides are described as useful antiarrhythmic agents. Their use in the treatment of cardiac arrhythmias, especially re-entrant arrhythmias, via the prolongation of the action potential of cardiac tissue is provided. Pharmaceutical formulations containing such compounds are also disclosed.
    Type: Grant
    Filed: September 23, 1985
    Date of Patent: December 16, 1986
    Assignee: Schering A.G.
    Inventors: David D. Davey, William C. Lumma, Jr., Ronald A. Wohl