Chalcogen Or Nitrogen Attached Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 540/609)
  • Patent number: 5310902
    Abstract: Novel alkylenediamine derivatives effectively employable glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5 R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.
    Type: Grant
    Filed: August 7, 1991
    Date of Patent: May 10, 1994
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Mitsuo Masaki, Masaru Satoh, Naoya Moritoh, Koichi Hashimoto, Toshiro Kamishiro, Haruhiko Shinozaki
  • Patent number: 5308840
    Abstract: Aminophenol derivatives of the following formula (I) ##STR1## wherein X is hydrogen atom, lower alkyl or a protecting group for phenolic hydroxy, Y is hydrogen atom or lower alkyl, Z is hydrogen atom, lower alkyl, halogen atom or trifluoromethyl, A is hydrogen atom or lower alkyl, t is an integer of 1 to 5, l and m are respectively an integer of 2 to 4, E and W are nitrogen atoms, F is a direct bond or oxygen atom, P and Q are each hydrogen atom, halogen atom, lower alkyl or lower alkoxy, and R.sup.8 is hydrogen atom, hydroxy or a hydroxy-protecting group, and their pharmcologically acceptable salts. Since the aminophenol derivatives (I) of the present invention have excellent antioxidative action and antiinflammatory and antiallergic action in mammalian animals including human, they are extremely useful as pharmaceuticals such as an antiinflammatory or an antiallergic.
    Type: Grant
    Filed: April 6, 1992
    Date of Patent: May 3, 1994
    Assignee: Green Cross Corporation
    Inventors: Naoki Sugiyama, Fumihiko Akaboshi, Haruko Yakumaru, Tomokazu Gotoh, Masanori Sugiura, Shigeki Kuwahara, Masahiko Kajii, Yoshiko Tanaka, Takao Kondoh, Chikara Fukaya
  • Patent number: 5304552
    Abstract: Compounds characterized generally as piperidinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is selected from a piperidinyl group, an isoindolyl group and an azabicyclononyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: April 16, 1993
    Date of Patent: April 19, 1994
    Assignee: G.D. Searle & Co.
    Inventor: Gunnar J. Hanson
  • Patent number: 5302602
    Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: May 18, 1992
    Date of Patent: April 12, 1994
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
  • Patent number: 5296596
    Abstract: The present invention relates to hexahydroazepine derivatives of formula ##STR1## in which: A=--CO--CH.sub.2 --, --CH(OH)--CH.sub.2 --; --CH.sub.2 --CH.sub.2 --; --CH.dbd.CH--; --C.tbd.C--;X=H or a halogen;Y=cyclohexyl or, when X is H, phenyl.It likewise relates to the salts of the said derivatives, to a process for the preparation of these and to the pharmaceutical compositions containing them, more particularly as antipsychotic agents.
    Type: Grant
    Filed: April 14, 1993
    Date of Patent: March 22, 1994
    Assignee: ELF SANOFI
    Inventors: Serge Lavastre, Jean-Pierre Maignan, Raymond Paul, Martine Poncelet, Vincent Santucci
  • Patent number: 5250546
    Abstract: Amino-alcohol derivatives of the formula, ##STR1## where R.sub.1 is a straight or branched alkyl group having 3 to 8 carbon atoms, R.sub.2 and R.sub.3 are each a lower alkyl group, or R.sub.2 and R.sub.3 form a 5- to 7-membered ring together with the adjacent nitrogen atom which may have an oxygen atom attached thereto, R.sub.4 is a hydrogen atom or a lower alkyl group, R.sub.5 is a hydrogen atom or a lower alkyl group, X is a hydrogen or halogen atom or a lower alkyl or lower alkoxy group, and n is an integer of 2 or 3, and acid addition salts thereof, are effectively useful as medicines and agricultural chemicals. Processes are also disclosed for preparing such compounds.
    Type: Grant
    Filed: July 11, 1990
    Date of Patent: October 5, 1993
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Mitsuo Masaki, Haruhiko Shinozaki, Masaru Satoh, Naoya Moritoh, Koichi Hashimoto, Toshiro Kamishiro
  • Patent number: 5245030
    Abstract: An IR-ray absorptive compound represented by the formula (1) or (2): ##STR1## and an optical recording medium having a substrate and an organic dye thin film, comprising the formulae (1) and/or (2).
    Type: Grant
    Filed: January 31, 1992
    Date of Patent: September 14, 1993
    Assignee: Canon Kabushiki Kaisha
    Inventors: Tetsuro Fukui, Yoshihiro Oguchi, Hiroyuki Sugata, Kyo Miura
  • Patent number: 5216167
    Abstract: Phenylacetic acid benzylamides having the following general structure ##STR1## wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.
    Type: Grant
    Filed: June 21, 1990
    Date of Patent: June 1, 1993
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, deceased, Robert Sauter, Manfred Reiffen, Eckhard Rupprecht
  • Patent number: 5166340
    Abstract: Organosilane compounds having the structural formula ##STR1## wherein R is a linear or branched C.sub.1-4 alkyl, 4-methyl-piperidyl, C.sub.6-12 aryl or C.sub.5-7 cycloalkyl; R.sup.1 is hydrogen, methyl or ethyl; R.sup.2 is methyl or ethyl and; n is 4 to 7.These organosilane compounds are useful as electron donors in Ziegler-Natta type catalyst systems.
    Type: Grant
    Filed: August 27, 1990
    Date of Patent: November 24, 1992
    Assignee: Himont Incorporated
    Inventor: Constantine A. Stewart
  • Patent number: 5155268
    Abstract: The present invention provides novel sulfonanilide and benzene-alkylaminium compounds which are the products of processes utilizing novel intermediates. Both the novel compounds and the novel intermediates are useful for the therapeutic or prophylactic treatment of arrhythmic activity.
    Type: Grant
    Filed: October 12, 1989
    Date of Patent: October 13, 1992
    Assignee: The Upjohn Company
    Inventor: Jackson B. Hester, Jr.
  • Patent number: 5147882
    Abstract: Cyclophanes of the general formula ##STR1## wherein X.sub.1, X.sub.2, A, R and R.sub.1 to R.sub.4 are as defined herein, the enantiomers, diastereomers and addition salts thereof and, more particularly, for pharmaceutical use, the physiologically acceptable addition salts thereof, which have pharmacological properties such as lowering blood pressure, dilating the coronary blood vessels and a mild heart rate lowering activity, pharmaceutical compositions which contain these compounds and processes for preparing them.
    Type: Grant
    Filed: March 28, 1991
    Date of Patent: September 15, 1992
    Assignee: Karl Thomae GmbH
    Inventors: Manfred Psiorz, Volker Trach
  • Patent number: 5147880
    Abstract: Benzo[a]fluorenes having an aminoalkoxy group on a phenyl ring at the 11-position have estrogenic and anti-estrogenic activity.
    Type: Grant
    Filed: July 22, 1991
    Date of Patent: September 15, 1992
    Assignee: Eli Lilly and Company
    Inventor: Charles D. Jones
  • Patent number: 5116984
    Abstract: The invention relates to imidazole derivatives of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of formula: ##STR2## A represents the group CH or a nitrogen atom; R.sup.1 and R.sup.2, which may be the same or different, and may be attached to either the same or different fused rings of the naphthalene moiety, each represents a hydrogen atom, a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, C.sub.1-4 alkyl or C.sub.1-4 alkylthio group, and one of R.sup.1 and R.sup.2 may also represent a group --NR.sup.3 R.sup.4 (wherein R.sup.3 and R.sup.4, which may be the same or different, each represents a hydrogen atom or a C.sub.1-4 alkyl group, or together with the nitrogen atom to which they are attached form a saturated 5 to 7 membered ring);n represents 1, 2 or 3;R.sup.5, R.sup.6, R.sup.7, are as defined in the specification; and physiologically acceptable salts and solvates thereof.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: May 26, 1992
    Assignee: Glaxo Group Limited
    Inventors: Peter C. North, Alexander W. Oxford, Ian H. Coates
  • Patent number: 5071844
    Abstract: The invention provides compounds of the formula: ##STR1## wherein k is 1, 2 or 3;m is 1, 2 or 3;n is 1, 2 or 3;p is 0, 1 or 2;X is O, S or a direct link, with the proviso that when X is O or S, n is 2 or 3;R.sup.1 is H or C.sub.1-C.sub.4 alkyl; andR.sup.2 is an optionally substituted phenyl or heteroaryl group; andpharmaceutically acceptable salts thereof.These compounds are useful for the treatment of motility disorders, particularly those of the gut such as irritable bowel syndrome.
    Type: Grant
    Filed: May 23, 1990
    Date of Patent: December 10, 1991
    Assignee: Pfizer Inc.
    Inventors: David Alker, Robert J. Bass, Peter E. Cross
  • Patent number: 5071851
    Abstract: 4-substituted cyclohexylamines of the formula ##STR1## where R is the group CR.sup.1 R.sup.2 R.sup.3, where R.sup.1, R.sup.2 and R.sup.3 are hydrogen, unsubstituted or substituted alkyl, alkoxy, alkylthio or cycloalkyl, with the proviso that at most one of the substituents R.sup.1, R.sup.2 and R.sup.3 is hydrogen, X is an alkylene group which, together with the N atom, forms a substituted or unsubstituted heterocyclic ring in which up to 2 carbon atoms may be replaced by O, N or S atoms, and salts thereof, and fungicides containing these compounds.
    Type: Grant
    Filed: July 9, 1990
    Date of Patent: December 10, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Ernst Buschmann, Norbert Goetz, Bernhard Zipperer, Eberhard Ammermann, Ernst-Heinrich Pommer
  • Patent number: 5070196
    Abstract: Novel alkylenediamine derivatives effectively employable as glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5, R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.
    Type: Grant
    Filed: August 1, 1990
    Date of Patent: December 3, 1991
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Mitsuo Masaki, Masaru Satoh, Naoya Moritoh, Koichi Hashimoto, Toshiro Kamishiro, Haruhiko Shinozaki
  • 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: 5019650
    Abstract: Known and novel 4-aryl-4-piperidinecarbinols and heterocyclic analogs are useful as analgesics. Also provided are novel pyrrolidinecarbinols and hexhydroazepine carbinols which are useful as analgesics, antidepressants and, in some cases, as anorectic agents.
    Type: Grant
    Filed: August 28, 1989
    Date of Patent: May 28, 1991
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Engelbert Ciganek, Leonard Cook
  • Patent number: 5017572
    Abstract: The present invention relates to compounds of formula: ##STR1## in which: R.sub.1 and R.sub.2 are such that:either R.sub.1 represents a methoxy group in which case R.sub.2 is a group chosen from the following: hydroxyl; C.sub.1 -C.sub.4 alkyl; C.sub.2 -C.sub.8 alkyloxy; C.sub.5 -C.sub.7 cycloalkyloxy; benzyloxy;or R.sub.2 represents a methoxy group in which case R.sub.1 is a group chosen from the following: hydroxyl; C.sub.2 -C.sub.8 alkyloxy; C.sub.2 -C.sub.8 alkyloxy substituted by a methoxy group; C.sub.1 -C.sub.4 trifluoroalkyloxy; C.sub.3 -C.sub.4 alkenyloxy; C.sub.5 -C.sub.7 cycloalkyloxy; benzyloxy; C.sub.1 -C.sub.4 alkyhlthio;n=2 or 3; andp=4, 5 or 6,as well as their addition salts with mineral or organic acids, said compounds and salts being useful as drugs.
    Type: Grant
    Filed: April 18, 1989
    Date of Patent: May 21, 1991
    Assignee: Delalande S.A.
    Inventors: Mona Ward, Pierre-Andre Ph.Settembre, Alain Renaud, Michel Langlois
  • Patent number: 5006523
    Abstract: Novel compounds of the formula ##STR1## and tautomers thereof are disclosed. These compounds possess potassium channel blocking activity and, as such, are useful as antiarrhythmic agents.
    Type: Grant
    Filed: October 26, 1989
    Date of Patent: April 9, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4996201
    Abstract: 4-(N-Substituted amino)-2-butynyl-1-carbamates and thiocarbamates and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.
    Type: Grant
    Filed: August 2, 1989
    Date of Patent: February 26, 1991
    Assignee: Warner-Lambert Co.
    Inventors: Stephen C. Bergmeier, Jeffrey A. Kester, Walter H. Moos, Haile Tecle, Anthony J. Thomas
  • Patent number: 4990505
    Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein the substituents are defined in the specification, and physiologically acceptable salts and solvates thereof.The compounds of formula (I) have a selective stimulant action at .beta..sub.2 -adrenoreceptors and are useful, in particular in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
    Type: Grant
    Filed: April 18, 1989
    Date of Patent: February 5, 1991
    Assignee: Glaxo Group Limited
    Inventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell
  • Patent number: 4990511
    Abstract: Amide compounds having glutamate receptor-inhibiting activity and having the formula: ##STR1## (wherein R.sub.1 and R.sub.2 each is hydrogen atom, an alkyl group or an acyl group, or ##STR2## is a cyclic amino group, m is an integer of 1 to 3, n is an integer of 0 to 4, x is an integer of 2 to 6 and y is an integer of 0 to 3) or salts thereof, are provided. The compounds are useful as a medicine for therapy or/and prevention of sequelae of cerebral apoplexy in warm-blooded animals.
    Type: Grant
    Filed: August 2, 1989
    Date of Patent: February 5, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Terumi Nakajima, Koichi Shudo, Giichi Goto
  • Patent number: 4933346
    Abstract: Compounds I are described ##STR1## with R.sup.1 equal to (cyclo)alk(en)yl or ##STR2## R.sup.2 /R.sup.3 equal to phenyl or phenylalkyl, A equal to ##STR3## m equal to 2-4, and n equal to 1-4.Compounds I and their salts are calcium antagonists.
    Type: Grant
    Filed: May 10, 1988
    Date of Patent: June 12, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Ruger, Hansjorg Urbach, Joachim Kaiser
  • Patent number: 4921863
    Abstract: Cyclic amine derivatives of the formula: ##STR1## or the pharmacologically acceptable salts thereof, wherein the symbols are as defined in the specification, as effective in relieving, curing or preventing mental symptoms due to cerebral vascular disorders.
    Type: Grant
    Filed: February 17, 1988
    Date of Patent: May 1, 1990
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Norio Karibe, Isao Saito, Kunizou Higurashi, Masahiro Yonaga, Takeru Kaneko, Takahiro Nakazawa, Masataka Ueno, Kiyomi Yamatsu
  • Patent number: 4910304
    Abstract: N-substituted cyclic amines of the general formula I ##STR1## where A is an alkylene group or a --(CH.sub.2).sub.n --[--O--(CH.sub.2).sub.m ].sub.r group which may be monosubstituted or polysubstituted by radicals R without the radicals R in a defined compound having to be identical, R is alkyl, alkoxyalkyl, unsubstituted or alkyl-substituted or alkoxy-substituted cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, n and m independently of one another are each from 2 to 8 and r is from 1 to 3, the --(CH.sub.2).sub.n --[O--(CH.sub.2).sub.m ].sub.r group consisting of from 5 to 12 members, are prepared by reacting a primary amine of the general formula IIR--NH.sub.
    Type: Grant
    Filed: March 31, 1989
    Date of Patent: March 20, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Roman Fischer, Herbert Mueller, Dieter Voges
  • Patent number: 4906634
    Abstract: Novel N-[4-(aminosubstituted)phenyl]methanesulfonamides and their use as cardiovascular agents, especially as antiarrhythmic agents are described. Pharmaceutical formulations containing such compounds are also discussed.
    Type: Grant
    Filed: March 8, 1988
    Date of Patent: March 6, 1990
    Assignee: Schering A.G.
    Inventors: Stanley S. Greenberg, William C. Lumma, Jr., Klaus Nickisch, Ronald A. Wohl
  • Patent number: 4898941
    Abstract: A process for preparing a diphenylalkene derivative of the formula [II] ##STR1## which comprises oxidizing a diphenylalkanoic acid derivative of the formula [I] ##STR2## wherein R.sub.1 and R.sub.2 are each substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or substituted or unsubstituted aryl, R.sub.1 and R.sub.2 may form a heteroring together theirwith or with an adjacent benzene ring, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11 are each hydrogen atom, halogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyl or substituted or unsubstituted amino, R.sub.12 and R.sub.13 are each hydrogen atom or substituted or unsubstituted alkyl, X is carboxyl, amide, ester or halide thereof.
    Type: Grant
    Filed: August 11, 1987
    Date of Patent: February 6, 1990
    Assignee: Kanzaki Paper Manufacturing Co., Ltd.
    Inventors: Nobuo Kanda, Haruo Omura, Yukihiro Abe, Mitsuru Kondo
  • Patent number: 4845098
    Abstract: Fungicidal saccharine salts of substituted hydroxypropylamines of the formula ##STR1## in which R.sup.1 is optionally substituted phenyl, phenoxy, phenylthio, phenylalkyl, phenoxyalkyl, or phenylthioalkyl, or optionally substituted cyclohexyl, cylohexyloxy, cyclohexylalkyl, cyclohexyloxyalkyl or cyclohexylthioalkyl,R.sup.2 is hydrogen or methyl,R.sup.3 is methyl or ethyl, andR.sup.4 and R.sup.5 each independently is alkyl or alkenyl, orR.sup.4 and R.sup.5, together with the nitrogen atom to which they are bonded, are an optionally substituted saturated heterocyclic radical which can optionally contain further hetero atoms.
    Type: Grant
    Filed: November 5, 1987
    Date of Patent: July 4, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Kramer, Joachim Weissmuller, Paul Reinecke, Gerd Hanssler
  • Patent number: 4835164
    Abstract: Novel heterocyclicmethanols are disclosed having the formula: ##STR1## wherein Z is pyrrolidinyl, piperidinyl, homopiperidinyl or pyridinyl; R.sup.1 is hydrogen, loweralkyl or carbethoxymethyl;R.sup.2 is hydrogen, loweralkyl, cycloalkyl, phenyl or phenyl-loweralkyl;R.sup.3 is 1 or 2-naphthalenyl, 2,3-dihydroinden-4 or 5-yl, phenyl or phenyl substituted by loweralkyl, loweralkoxy, halogen, trifluoromethyl, phenyl, methylenedioxy, nitro, amino, loweralkylamino, diloweralkylamino, loweracylamino;the 1-position of 2-pyrrolidinyl, 2-piperidinyl or 2-homopiperidinyl may be substituted by an R.sup.4 loweralkyl group, or R.sup.1 may form methylene or --CH.sub.2 -C(O)-bridges with R.sup.4 ;the pharmaceutically acceptable salts and diastereomers thereof, which compounds have antiarrhythmic and/or hypotensive activity in animals.
    Type: Grant
    Filed: February 20, 1987
    Date of Patent: May 30, 1989
    Assignee: A. H. Robins Company, Incorporated
    Inventors: James R. Shanklin, Jr., Christopher P. Johnson, III
  • Patent number: 4824844
    Abstract: Fungicidally active saccharine salts of substituted amines of the formula ##STR1## in which A represents in each case optionally substituted cyclohexyl, cyclohexenyl or phenyl,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl,R.sup.3 and R.sup.4 independently of one another represent alkyl or, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical which can contain further hetero atoms andn represents the number 0 or 1.
    Type: Grant
    Filed: November 5, 1987
    Date of Patent: April 25, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Joachim Weissmuller, Paul Reinecke, Gerd Hanssler
  • Patent number: 4820717
    Abstract: The present invention relates to new aromatic derivatives of formula: ##STR1## wherein: Alk is an alkylene group with 1 to 10 carbon atoms,R.sub.1 is hydrogen or an alkyl with 1 to 6 carbon atoms,R.sub.2 and R.sub.3 are similar or different and represent a cycloalkyl with 3 to 6 carbon atoms or a striaght or branched alkyl with 1 to 6 carbon atoms, either substituted or non-substituted by a phenyl or methyl phenyl group, or R.sub.2 and R.sub.3 form, together with the atom of nitrogen to which they are bonded, a mono-nitrogenous heterocycle containing no other heteroatom, such as pyrrolidino, piperidino, azepino, hexamethylene-imino, 4-methyl-piperidino, 4-phenyl-piperidino, 1,2,3,4-tetrahydro-2-isoquinolyl, 4-benzyl-piperidino;R.sub.4 is hydrogen, halogen, methyl or phenyl,R.sub.5 is hydrogen, halogen or methyl,or R.sub.4 and R.sub.5 together with the benzene ring to which they are bonded, constitute a 1-naphthyl or 2-naphthyl group,and the pharmaceutically acceptable salts with mineral or organic acids.
    Type: Grant
    Filed: September 30, 1986
    Date of Patent: April 11, 1989
    Assignee: Sanofi
    Inventors: Madeleine Mosse, Henri Demarne, Vincenzo Proietto
  • Patent number: 4804753
    Abstract: A process for the preparation of Schiff's bases which contain amino groups, of the formula ##STR1## wherein n is 3 to 12,by reacting cyclic lactams of the formula ##STR2## wherein n is 3 to 12,or of their ring-opened polymers of the formula ##STR3## wherein n is 3 to 12 andm is 1 to 100,000,with inorganic bases at elevated temperature, the reaction being carried out in the presence of inert, high-boiling suspending agents.
    Type: Grant
    Filed: January 8, 1986
    Date of Patent: February 14, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventor: Hans-Helmut Schwarz
  • Patent number: 4778789
    Abstract: Novel compounds of formula (I), wherein R.sub.1 is selected from hydrogen, halogen; or trifluoromethyl; X is oxygen or sulfur; R.sub.2 and R.sub.3 are the same or different and selected from hydrogen or lower alkyl; m is 2 or 3; Y is oxygen or sulphur; Z is selected from: --NR.sub.4 R.sub.5, formulae (II), (III) or (IV), wherein R.sub.4 and R.sub.5 are the same or different and selected from hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl, hydroxy-alkyl, alkoxyalkyl or alkanoyloxyalkyl, phenyl or phenyl-alkyl, wherein the phenyl groups may be unsubstituted or monosubstituted with halogen or CF.sub.3 ; n is 0, 1, 2 or 3; R.sub.6 and R.sub.7 are the same or different and selected from hydrogen, lower alkyl, hydroxy, lower alkoxy or lower alkanoyloxy; p is 2 or 3; R.sub.8 and R.sub.9 are the same or different and selected from hydrogen or lower alkyl; R.sub.10 is hydrogen, lower alkyl or lower alkanoyl. The new compounds can be used for treating mental disorders.
    Type: Grant
    Filed: November 26, 1986
    Date of Patent: October 18, 1988
    Assignee: Aktiebolaget Leo
    Inventors: Tomas Fex, Knut G. Olsson, Aina L. Abramo, Erik G. Christensson
  • 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: 4762934
    Abstract: A novel class of diaminoether compounds wherein one amino group thereof is a tertiary amine in N-heterocyclic form and the other amino group is a severely sterically hindered secondary amino group may be prepared by a three-step process and are useful in the selective removal of H.sub.2 S from mixtures containing H.sub.2 S and CO.sub.2.
    Type: Grant
    Filed: January 3, 1984
    Date of Patent: August 9, 1988
    Assignee: Exxon Research and Engineering Company
    Inventors: Eugene L. Stogryn, Guido Sartori
  • Patent number: 4762821
    Abstract: N',N"-dialkylguanidino dipeptides with angiotension converting enzyme (ACE) inhibiting activity are useful as antihypertensives. Proline and proline analogs are components of the dipeptides.
    Type: Grant
    Filed: September 10, 1986
    Date of Patent: August 9, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: John J. Nestor
  • Patent number: 4758564
    Abstract: Amines of the general formula ##STR1## where A is alkyl, alkenyl, cycloalkyl, cycloalkenyl, phenylalkyl or phenylalkenyl, X is oxygen or sulfur, B is an alkylene chain and R.sup.1 and R.sup.2 are each alkyl, alkenyl or cycloalkyl, or R.sup.1 and R.sup.2 form part of a heterocyclic structrure, and their salts, as well as fungicides containing these compounds.
    Type: Grant
    Filed: February 18, 1986
    Date of Patent: July 19, 1988
    Assignee: BASF Aktiengesellschaft
    Inventors: Costin Rentzea, Ernst Buschmann, Norbert Goetz, Eberhard Ammermann, Ernst-Heinrich Pommer
  • Patent number: 4755599
    Abstract: The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl,either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl,or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and(i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6 C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.
    Type: Grant
    Filed: February 3, 1987
    Date of Patent: July 5, 1988
    Assignee: Rhone-Poulenc Sante
    Inventors: Jean-Claude Barriere, Jean-Pierre Corbet, Claude Cotrel, Daniel Farge, Jean-Marc Paris
  • Patent number: 4732896
    Abstract: New aromatic derivatives having an activity antagonistic to calcium and corresponding to formula: ##STR1## in which: A represents a chain having any one of the following structures: ##STR2## Ar represents a group of structure: ##STR3## n takes the value 1 or 2 when R is different from H; m takes the value 2 or 3.
    Type: Grant
    Filed: June 26, 1985
    Date of Patent: March 22, 1988
    Assignee: Delalande S.A.
    Inventors: Guy R. Bourgery, Alain P. Lacour, Bernard M. Pourrias, Raphael Santamaria
  • Patent number: 4721786
    Abstract: Fungicidally active novel .beta.-naphthylalkylamines of the formula ##STR1## in which Ar represents optionally substituted .beta.-naphthyl andR.sup.1 and R.sup.2, which can be identical or different, represent alkyl or alkenyl orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical, which can contain further hetero-atoms,or plant-tolerated acid addition salts thereof.
    Type: Grant
    Filed: April 1, 1985
    Date of Patent: January 26, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Joachim Weissmuller, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
  • Patent number: 4716159
    Abstract: The present invention is directed to pyridazino[4,3-c]isoquinolines of Formula I ##STR1## wherein R represents methyl, phenyl or substituted phenyl groups, R.sub.1 represents inter alia amino or substituted amino, alkoxy or cycloalkoxy groups, having pharmacological activity, to process for preparing them and to the pharmaceutical compositions containing them. The compounds of the invention possess anti-anxiety activity.
    Type: Grant
    Filed: July 30, 1986
    Date of Patent: December 29, 1987
    Assignee: Gruppo Lepetit, S.p.A.
    Inventor: Emilio Toja
  • Patent number: 4673747
    Abstract: Substituted aminoalkylphenoxy derivatives represented by the general formula of: ##STR1## wherein the substituting group Z is either one of the following groups of: ##STR2## were prepared. These derivatives exert antagonism against Histamine H.sub.2 -receptors and hence are efficacious for the treatments of digestive ulcers.
    Type: Grant
    Filed: December 3, 1985
    Date of Patent: June 16, 1987
    Assignee: Ikeda Mohando Co., Ltd.
    Inventors: Fujio Nohara, Tomoaki Fujinawa
  • Patent number: 4663331
    Abstract: This invention relates to Mannich-alkynyl aminothiadiazole oxides having histamine H.sub.2 -antagonist activity. A particular compound of this invention is 3-amino-4-[7-piperidinohept-5-ynylamino]-1,2,5-thiadiazole-1-oxide.
    Type: Grant
    Filed: January 16, 1986
    Date of Patent: May 5, 1987
    Assignee: SmithKline & French Laboratories Limited
    Inventors: Thomas H. Brown, Peter Blurton
  • Patent number: 4656180
    Abstract: Diamine derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--A--NH--R--NH--B--Q'--(CH.sub.2).sub.n NR.sup.3 R.sup.4 (I)which have a highly selective action on histamine-H.sub.2 receptors and are therefore suitable for use as anti-ulcerative agents are described. Processes for the preparation of these compounds and pharmaceutical preparations containing these compounds are also described.
    Type: Grant
    Filed: March 5, 1985
    Date of Patent: April 7, 1987
    Assignee: Ludwig Heumann & Co., GmbH
    Inventors: Stefan Postius, Rolf Herter, Peter Morsdorf, Helmut Schickaneder, Istvan Szelenyi, Kurt H. Ahrens
  • Patent number: 4642348
    Abstract: Novel pyrrolidine, piperidine and homopiperidinecarboxamide and thiocarboxamide compounds having the formula: ##STR1## wherein X is --S--, --S(O)-- or --S(O).sub.2 --; A is a loweralkalene chain and A.sup.1 and A.sup.2 are alkalene chains when p and d are one; R, R.sup.1 and R.sup.2 are hydrogen, loweralkyl, phenyl cycloalkyl or phenylalkyl and R.sup.1 and R.sup.2 may form a heterocyclic residue with the adjacent nitrogen atom; Q is a selected aromatic radical, and the pharmaceutically acceptable acid addition salts useful as cardiac antiarrhythmia agents are disclosed.Novel chemical intermediates, unsubstituted on pyrrolidine, piperidine and homopiperidine nitrogen but with --(A.sup.2).sub.p --X--(A.sup.2).sub.d --Q side chain are also disclosed.
    Type: Grant
    Filed: July 1, 1985
    Date of Patent: February 10, 1987
    Assignee: A. H. Robins Company, Incorporated
    Inventor: James R. Shanklin, Jr.
  • Patent number: 4605673
    Abstract: The invention is concerned with 7H-dibenzo(a,c)-cyclohepten-5-one-(7) derivatives of general formula I ##STR1## wherein R.sup.1 and R.sup.2 can be the same or different, a hydrogen atom, an alkyl radical containing 1 to 3 carbon atoms, or, together with the nitrogen atom to which they are attached form a heterocyclic ring containing 3 to 6 carbon atoms,n is 2 or 3R.sup.3 is a hydrogen atom or a halogen atom andX is either a methylene radical or an oxygen atomand the pharmacologically acceptable salts thereof with inorganic and organic acids.The invention is furthermore concerned with analogous processes for the preparation thereof and their application for controlling psychic diseases and gastric and/or intestinal ulcers.
    Type: Grant
    Filed: December 19, 1983
    Date of Patent: August 12, 1986
    Assignee: Warner-Lambert Company
    Inventors: Gerhard Satzinger, Edgar Fritschi, Manfred Herrmann