Patents Issued in April 25, 1995
  • Patent number: 5409918
    Abstract: Crystalline cephem acid addition salts of the general formula II ##STR1## pharmaceutical preparations effective against bacterial infections which contain such cephem derivatives, processes for the preparation of the cephem derivatives and the pharmaceutical preparations, and the use of the cephem derivatives for combating bacterial infections.
    Type: Grant
    Filed: August 21, 1992
    Date of Patent: April 25, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Friedhelm Adam, Walter Durckheimer, Burkhard Mencke, Dieter Isert
  • Patent number: 5409919
    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is an amino group which may be protected, R.sup.3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S.fwdarw.O, O or CH.sub.2, R.sup.4 is a hydrogen atom, methoxy group or formamido group, R.sup.13 is a hydrogen atom, methyl group, hydroxyl group or halogen atom and A.sup..sym. is an optionally substituted imidazolium-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a pharmaceutically acceptable salt or ester thereof is novel and has excellent antibacterial activity.
    Type: Grant
    Filed: April 2, 1993
    Date of Patent: April 25, 1995
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Akio Miyake, Masahiro Kondo, Masahiko Fujino
  • Patent number: 5409920
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: October 5, 1990
    Date of Patent: April 25, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Ravindra N. Guthikonda, Frank P. DiNinno
  • Patent number: 5409921
    Abstract: Compounds characterized generally as thiazetidinyl-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 a thiazetidinyl 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--(CH.sub.2).sub.q --C.tbd.C-Vwherein 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: January 25, 1994
    Date of Patent: April 25, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Patent number: 5409922
    Abstract: Compounds characterized generally as thiazopinyl-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 a thiazopinyl 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--(CH.sub.2).sub.q --C.tbd.C--Vwherein 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: December 16, 1993
    Date of Patent: April 25, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Patent number: 5409924
    Abstract: Compounds characterized generally as benzo-fused oxazobicyclo-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 a benzo-fused oxazobicyclo 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: February 22, 1994
    Date of Patent: April 25, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Patent number: 5409925
    Abstract: Compounds characterized generally as oxazobicyclo-terminated alkylamino ethynyl alanine amino diol derivatives 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 an oxazobicyclo 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: January 25, 1994
    Date of Patent: April 25, 1995
    Assignee: G. D. Searl & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Patent number: 5409926
    Abstract: Novel disubstituted 6-aminoquinazolinones of the Formula ##STR1## are useful as angiotensin-II receptor (subtype 2) antagonists (AT.sub.2 antagonists) alone or in combination with heparin, and can act to suppress the vascular stenosis which commonly occurs during the development of atherosclerosis and the restenosis following arterial angioplasty, stent placement, bypass surgery, heart transplantation or endarterectomy.
    Type: Grant
    Filed: July 19, 1993
    Date of Patent: April 25, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Christopher F. Reilly, Stephen E. Delaszlo, Robert G. Johnson, Tsuneo Fujita
  • Patent number: 5409927
    Abstract: There are described compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or lower alkyl,R.sub.2 is hydrogen, lower alkyl, lower alkoxycarbonyl, phenyl- or naphthyl-lower alkoxycarbonyl, heterocyclylcarbonyl wherein heterocyclyl contains 5 or 6 ring atoms, is saturated and is bonded to the carbonyl group via a ring nitrogen atom and, in addition to the bonding nitrogen atom, contains as ring member one or more further hetero atoms selected from unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted NH, O, S, S.dbd.O and SO.sub.2, or is lower alkanoyl, phenyl- or naphthyl-lower alkanoyl or lower alkanesulfonyl,R.sub.3 is morpholino, thiomorpholino, S-oxothiomorpholino or S,S-dioxothiomorpholino, the heterocyclyl radical in heterocyclylcarbonyl R.sub.2 having the same definition as R.sub.3 or having a definition other than R.sub.3, andR.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, cyano, trifluoromethyl or fluorine, and salts of those compounds where salt-forming groups are present.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: April 25, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Guido Bold, Alexander Fassler, Marc Lang, Peter Schneider
  • Patent number: 5409928
    Abstract: This invention provides a condensed pyrazole derivative of the Formula (1): ##STR1## (where A denotes CH or N, R.sup.0 and R.sup.3 denote same or different, a hydrogen atom or a lower alkyl group, R.sup.1 and R.sup.2 denote same or different, a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a nitro group or a halogen atom, m denotes 1 or 2, and n denotes 1, 2 or 3, provided that, when n is 2, two R.sup.2 may be connected to each other to form a lower alkylenedioxy group), or its pharmaceutically acceptable salt. This derivative or its salt is excellent in the effect of inhibiting the expression of action of androgen, thereby being excellent in therapeutical effect of benign prostatic hypertrophy, prostatic carcinoma, etc., and has a long lasting of efficacy and high oral absorption.
    Type: Grant
    Filed: October 20, 1993
    Date of Patent: April 25, 1995
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Kiyokawa, Satoshi Yamada, Keisuke Miyajima, Koji Edamatsu, Kunihiko Tatsumi, Takeshi Yamauchi, Kazumasa Kishi, Kunihiko Kiyono
  • Patent number: 5409929
    Abstract: There are provided novel nitrogen-containing bicyclic compounds which are useful in the treatment of physiological or drug induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.
    Type: Grant
    Filed: February 17, 1993
    Date of Patent: April 25, 1995
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventor: Engelbert Ciganek
  • Patent number: 5409930
    Abstract: This invention relates to bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, it relates to the method of inhibiting abnormal cell proliferation in a patient suffering from a disorder characterized by such proliferation comprising the administration thereto of an EGF and/or PDGF receptor inhibiting effective amount of said bis mono- and/or bicyclic aryl and/or heteroaryl compound and to the preparation of said compounds and their use in pharmaceutical compositions used in this method.
    Type: Grant
    Filed: November 8, 1993
    Date of Patent: April 25, 1995
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Alfred P. Spada, Martin P. Maquire, Paul E. Persons, Michael R. Myers
  • Patent number: 5409931
    Abstract: 1,3-Substituted cycloalkenes and cycloalkanes are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
    Type: Grant
    Filed: February 4, 1994
    Date of Patent: April 25, 1995
    Assignee: Warner-Lambert Company
    Inventors: Bradley W. Caprathe, Dennis M. Downing, Juan C. Jaen, Stephen J. Johnson, William J. Smith, III, Lawrence D. Wise, Jonathan Wright, David J. Wustrow
  • Patent number: 5409932
    Abstract: The piperazine-substituted pyrroloanthracenes are prepared by reacting either furanoanthracenes with piperazinalkylamines or reacting unsubstituted pyrroloanthracenes first with dihalogenoalkyl compounds and then with appropriately substituted piperazines or by reacting furan derivatives first with piperazinalkylamines and then condensing with anthracenes. The new compounds can be employed as active ingredients in medicaments, in particular in immunomodulators.
    Type: Grant
    Filed: December 9, 1993
    Date of Patent: April 25, 1995
    Assignee: Bayer AG
    Inventors: Eckhard Schwenner, Gaetan Ladouceur, Hans-Joachim Kabbe, Thomas M. Aune
  • Patent number: 5409933
    Abstract: The present invention relates to novel quinoline derivatives of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X, Y and Z are defined as in the specification, and pharmaceutically acceptable acid addition salts thereof, and also to processes for preparing these compounds.The present invention also provides an antibacterial composition comprising a compound of formula (I) or its acid addition salt as an active ingredient and pharmaceutically acceptable excipient.The novel quinoline derivatives of the present invention have an excellent antibacterial activity against bacteria or bacteroides.
    Type: Grant
    Filed: June 8, 1993
    Date of Patent: April 25, 1995
    Inventors: Wan J. Kim, Tae S. Lee, Myung H. Park, Jae D. Ha, Bong J. Kim, Keun S. Nam, Jae Y. Kong
  • Patent number: 5409934
    Type: Grant
    Filed: July 7, 1993
    Date of Patent: April 25, 1995
    Inventors: David G. Smith, Derek R. Buckle, Ashley E. Fenwick
  • Patent number: 5409935
    Abstract: The use of xanthine derivatives for the treatment of secondary nerve cell damage and functional disorders after cranio-cerebral traumas (CCT)The use of xanthine derivatives of the formula I ##STR1## and of their physiologically tolerable salts, in which R.sup.1 is oxoalkyl, hydroxyalkyl or alkyl, R.sup.2 is hydrogen or alkyl and R.sup.3 is hydrogen, alkyl, oxoalkyl or an alkyl having up to 6 carbon atoms, whose carbon chain is interrupted by an oxygen atom, for the production of pharmaceuticals for the treatment of disorders which can occur after cranio-cerebral traumas is described.
    Type: Grant
    Filed: July 9, 1992
    Date of Patent: April 25, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans-Peter Schubert, John J. Grome, Barbara Kittner, Karl Rudolphi, Ulrich Gebert
  • Patent number: 5409936
    Abstract: An imidazopyridine derivative is disclosed of the formula [I]: ##STR1## wherein R.sup.1 is lower alkyl, R.sup.2 is a group of the formula ##STR2## where Z is oxygen atom, R.sup.0 is lower alkyl, R.sup.3 is carboxyl or lower alkoxycarbonyl and Ring A is tetrazolyl-substituted or unsubstituted phenyl, and pharmaceutically acceptable salt thereof, that are useful in prophylaxis and treatment of hypertension.
    Type: Grant
    Filed: September 3, 1992
    Date of Patent: April 25, 1995
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Yasushi Honma, Yasuo Sekine, Sumihiro Nomura, Kazuaki Naito, Hiroshi Narita
  • Patent number: 5409937
    Abstract: The invention concerns compounds of the formula I: ##STR1## wherein the variables are described in the specification which are antagonists of platelet activity factor.
    Type: Grant
    Filed: April 18, 1994
    Date of Patent: April 25, 1995
    Assignee: British Biotech Pharmaceuticals Limited
    Inventor: Mark Whittaker
  • Patent number: 5409938
    Abstract: The present invention provides new antimalarial compounds called korupensamines, korupensamine derivatives, and pharmacologically acceptable salts thereof, methods for isolating such antimalarial korupensamines from the plant Ancistrocladus korupensis, methods for obtaining new korupensamine derivatives, antimalarial compositions containing such antimalarial korupensamines or derivatives thereof or pharmacologically acceptable salts thereof, and methods of using such antimalarial compounds for the prevention of malaria infections or for treating mammals with malarial infections. The antimalarial compounds of the present invention inhibit the reproduction and cytopathicity of Plasmodium sp. parasites in vitro and in vivo.
    Type: Grant
    Filed: February 14, 1994
    Date of Patent: April 25, 1995
    Assignee: The United States of America as represented by the Secretary, Department of Health and Human Services
    Inventors: Michael R. Boyd, Guido Francois, Gerhard Bringmann, Yaii F. Hallock, Kirk P. Manfredi, John H. Cardellina, II
  • Patent number: 5409939
    Abstract: This invention relates to compounds having the following formula ##STR1## which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine thio derivatives.
    Type: Grant
    Filed: February 12, 1993
    Date of Patent: April 25, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Steven P. Adams, Richard J. Lindmark, Masateru Miyano, Joseph G. Rico
  • Patent number: 5409940
    Abstract: The invention relates to a group of new 3,4-dehydropiperidine derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl group having 1-3 carbon atoms;Y is a group of the general formula 2 ##STR2## wherein R.sub.2 is a group of the formula --(CH.sub.2).sub.n --C(.dbd.X)--NR.sub.3 R.sub.4, --(CH.sub.2).sub.n --SO.sub.2 --NR.sub.3 R.sub.4, --(CH.sub.2).sub.n --NR.sub.5 --C(.dbd.X)--R.sub.6 or --(CH.sub.2).sub.n --NR.sub.5 --SO.sub.2 --R.sub.6, wherein R.sub.3, R.sub.4 and R.sub.5 independent of each other represent hydrogen or alkyl (1-3C), R.sub.6 is alkyl (1-3C), X represents O or S; n is 0-4, andR is hydrogen or alkyl (1-3C).These compounds have interesting serotonin-1-like (partial) agonistic activity and can be used for the treatment of migraine.
    Type: Grant
    Filed: October 19, 1993
    Date of Patent: April 25, 1995
    Assignee: Duphar International Research B.V.
    Inventors: Antonius Hulkenberg, Karin J. van Charldorp, Rolf van Hes, Ineke van Wijngaarden
  • Patent number: 5409941
    Abstract: Compounds of the formula ##STR1## which are useful in treating migraine and other disorders, and intermediates used in the preparation of said compounds.
    Type: Grant
    Filed: August 6, 1993
    Date of Patent: April 25, 1995
    Assignee: Pfizer Inc.
    Inventor: Jolanta T. Nowakowski
  • Patent number: 5409942
    Abstract: This invention relates to 1-phenyl-3-aryl-2-propyne-1-ones, the use of these compounds as calcium uptake inhibitors in leukocytes and thrombocytes, and pharmaceutical compositions containing these compounds as active ingredients, and the process of their preparation.
    Type: Grant
    Filed: March 5, 1993
    Date of Patent: April 25, 1995
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Robert J. Dinerstein, Jeffrey S. Sabol, Keith A. Diekema
  • Patent number: 5409943
    Abstract: The present invention relates to N-pyridylamidine and N-pyridylguanidine derivatives of general formula (I) in which: Ar.sup.1 is an optionally substituted phenyl ring; Ar.sup.2 is an optionally substituted phenyl ring; R.sup.1 is hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is hydrogen or C.sub.1-4 alkyl; R.sup.4 is hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; X is CH.sub.2 or NR.sup.5, and R.sup.5 is hydrogen or C.sub.1-4 alkyl, and the salts thereof, and their use in therapy as gastric acid secretion inhibitors.
    Type: Grant
    Filed: July 20, 1994
    Date of Patent: April 25, 1995
    Assignee: SmithKline Beecham Intercredit B.V.
    Inventors: Robert J. Ife, Colin A. Leach, Dashyant Dhanak
  • Patent number: 5409944
    Abstract: Disclosed are compounds of Formula I useful in the treatment of cyclooxygenase mediated diseases such as pain, fever and inflammation of a variety of conditions including rheumatic fever, symptoms associated with influenza or other viral infections, common cold, low back and neck pain, dysmenorrhea, headache, toothache, sprains and strains, myositis, neuralgia, synovitis, arthritis, including rheumatoid arthritis degenerative joint diseases (osteoarthritis), gout and ankylosing spondylitis, bursitis, burns, injuries.
    Type: Grant
    Filed: March 12, 1993
    Date of Patent: April 25, 1995
    Assignee: Merck Frosst Canada, Inc.
    Inventors: W. Cameron Black, Chun-Sing Li, Daniel Guay, Petpiboon Prasit, Patrick Roy
  • Patent number: 5409945
    Abstract: Compounds characterized generally as benzo-fused thiazolidinyl-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 a benzo-fused thiazolidinyl 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--(CH.sub.2).sub.q --C.tbd.C-Vwherein 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: February 22, 1994
    Date of Patent: April 25, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Patent number: 5409946
    Abstract: Novel isoxazole isothiazole and pyrazole compounds of the formula: ##STR1## wherein A, R.sup.1, and R.sup.2 are specifically defined, or pharmaceutical salts thereof, are selective and potent cholinergic ligands at neuronal nicotinic receptors, useful in the treatment of cognitive, neurological and mental disorders characterized by decreased cholinergic function, as well as in the treatment of alcohol intoxication and petit real absence epilepsy.
    Type: Grant
    Filed: September 8, 1993
    Date of Patent: April 25, 1995
    Assignee: Abbott Laboratories
    Inventors: David S. Garvey, George M. Carrera, Jr., Stephen P. Arneric, Youe-Kong Shue, Nan-Horng Lin, Yun He, Edmund L. Lee, Suzanne A. Lebold
  • Patent number: 5409947
    Abstract: New therapeutic agents of cycloheptimidazole derivatives are disclosed, which are represented by the following formula or its alkali-addition salts. ##STR1## (wherein R.sub.1 represents H or isopropyl group; R.sub.2 represents a lower alkyl; R.sub.3 represents a carboxylic acid or tetrazole group. A and A.sub.1 are substituted groups at 4 or 8 position and A.sub.1 is a hydrogen or hydroxy group when A is a hydrogen or A and A.sub.1 is an oxo group. The dotted line "- - - -" is two double bonds or saturated single bonds).These compounds are useful as anti-hypertensive or anti-congestive heart failure agents.
    Type: Grant
    Filed: May 21, 1993
    Date of Patent: April 25, 1995
    Assignee: Kotobuki Seiyaku Co., Ltd.
    Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Takashi Yanagisawa, Naoto Ueyama, Tomoyuki Kawai, Motoharu Sonegawa, Hiromi Baba, Makoto Haketa
  • Patent number: 5409948
    Abstract: An improved method of cholinomimetic therapy for cognitive impairments associated with aging and Alzheimer's disease comprising treating a patient with an effective amount of phenserine or a pharmaceutically acceptable salt and derivatives.
    Type: Grant
    Filed: November 23, 1992
    Date of Patent: April 25, 1995
    Assignee: The United States of America as represented by the Secretary of the Department of Health and Human Services
    Inventors: Nigel H. Greig, Arnold Brossi, Timothy T. Soncrant, Harold W. Holloway, Stanley I. Rapoport, Setsu Iijima, Edward L. Spangler, Donald K. Ingram, Xue F. Pei
  • Patent number: 5409949
    Abstract: The invention provides new methylen-indole derivatives of formula (I) ##STR1## wherein R is a group ##STR2## in which R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyloxy, carboxy, nitro or NHR.sub.7, wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or halogen; andR.sub.6 is hydrogen or C.sub.1 -C.sub.6 alkyl;n is zero, 1 or 2;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, cyano, carboxyl, nitro or --NHR.sub.7 in which R.sub.7 is as defined above;R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof; and wherein, when, at the same time, R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen or cyano and R.sub.3 is hydrogen, R.sub.1 and n being as defined above, then at least one of R.sub.4, R.sub.5 and R.sub.6 is other than hydrogen, which are useful as tyrosine kinase inhibitors.
    Type: Grant
    Filed: March 12, 1993
    Date of Patent: April 25, 1995
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Franco Buzzetti, Antonio Longo, Maristella Colombo
  • Patent number: 5409950
    Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom, a hydroxyl group or a group selected from --OCOCH.dbd.CHCH(CH.sub.3)(CH.sub.2).sub.3 CH.sub.3, --OCOCH.dbd.CHC(CH.sub.3).dbd.CHCH(CH.sub.3)--CH.sub.2 CH.sub.3, or --OCO--X--CH.sub.2 CH(CH.sub.3)CH.sub.2 CH.sub.3 [where X is --CH.dbd.CHCH(CH.sub.3)--, --CH.sub.2 CH(OH)CH(CH.sub.3)--, --CH.dbd.CHC(OH)(CH.sub.3)--, --CH.sub.2 CH(OH)CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH(CH.sub.3)--)];R.sub.2 represents a hydrogen atom or a hydroxyl group;R.sub.3 represents a group selected from --C(.dbd.CH.sub.2)CH(OR.sub.7)CH(CH.sub.3)CH.sub.2 Ph (where R.sub.7 is a hydrogen atom or an acetyl group), --C(CH.sub.3).dbd.CHCH(CH.sub.2 R.sub.8)CH.sub.2 Ph (where R.sub.8 is a hydrogen or a hydroxyl group), --C(CH.sub.2 OH).dbd.CHCH(CH.sub.3)CH.sub.2 Ph, --C(.dbd.CH.sub.2)CH(OH)CH(CH.sub.2 OH)CH.sub.2 Ph, --C(.dbd.CH.sub.2)CH(NHCOCH.sub.3)CH(CH.sub.3)CH.sub.2 Ph, --C(CH.sub.2 NHCOCH.sub.3).dbd.CHCH(CH.sub.3)CH.sub.2 Ph or ##STR2## R.sub.4, R.
    Type: Grant
    Filed: October 26, 1993
    Date of Patent: April 25, 1995
    Assignee: Glaxo Group Limited
    Inventors: Michael J. Dawson, Allan Baxter, Robert M. Tait, Nigel S. Watson, David Noble, Alan Shuttleworth, Howard G. Wildman, Michael V. Hayes
  • Patent number: 5409951
    Abstract: Novel compounds of formula I ##STR1## wherein R.sup.1 is independently hydrogen, hydroxy, alkyl with 1 to 6 carbon atoms, acyloxy groups with 1 to 6 carbon atoms, alkyloxy with 1 to 6 carbon atoms or from 1 to 5 sugar moleties; and R.sup.2 is independently hydrogen, or alkyl with 1 to 6 carbon atoms.The compounds are producible by aerobic cultivation on suitable nutrient media under suitable conditions of a strain of the fungus Ascochyta sp., subsequent recovery of the active component from the fermentation medium, and optionally modifying the active compound to obtain a compound of the desired formula I.Disclosed is also microorganisms capable of producing said compounds, compositions containing said compounds, and the use of such compositions for controlling fungi in valuable crops, animals, including birds and mammals, and in the preservation of wood, paints and edible products.
    Type: Grant
    Filed: July 22, 1993
    Date of Patent: April 25, 1995
    Assignee: Novo Nordisk A/S
    Inventors: Ruby I. Nielsen, Frank W. Rasmussen
  • Patent number: 5409952
    Abstract: A compound of the formula (I) ##STR1## in which: R.sub.1 represents a hydrogen atom, a lower alkyl group, a hydroxy group or a lower alkoxy group,R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.11 are as defined in the description.Medicaments.
    Type: Grant
    Filed: October 27, 1993
    Date of Patent: April 25, 1995
    Assignee: Adir et Compagnie
    Inventors: Jean D. Brion, Guillaume Le Baut, Francoise Zammatio, Alain Pierre, Ghanem Atassi, Larbi Belachmi
  • Patent number: 5409953
    Abstract: New antineoplastic substances have been isolated, structurally elucidated and synthesized having a general structural formula of: ##STR1## wherein: R.sub.1 is OH or OCH.sub.3 ;R.sub.2 is H or OCH.sub.3 ; or R.sub.1 R.sub.2 is --OCH.sub.2 O--;R.sub.3 is H or OH;R.sub.4 is OH or OCH.sub.3.These substances have been denominated "combretastatin A-1, -A-2, -A-3, -B-1, -B-2, -B-3 and -B-4". Pharmaceutical preparation containing the substances and methods of treating a host inflicted with a neoplastic growth with the preparation is described.
    Type: Grant
    Filed: February 10, 1992
    Date of Patent: April 25, 1995
    Assignee: Arizona Board of Regents acting on behalf of Arizona State University
    Inventors: George R. Pettit, Sheo B. Singh
  • Patent number: 5409954
    Abstract: .alpha.-arylacrylic acid derivatives of the general formula I ##STR1## where X is ethylene or ethenylene; Y is a direct bond or oxygen;R.sup.1 is a mononuclear or dinuclear aromatic system substituted by C.sub.1 -C.sub.4 -alkyl, their preparation, insecticides and fungicides containing them and methods for their use.
    Type: Grant
    Filed: October 29, 1993
    Date of Patent: April 25, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Kirstgen, Albrecht Harreus, Uwe Kardorff, Thomas Kuekenhoehner, Harald Rang, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast
  • Patent number: 5409955
    Abstract: There is disclosed a composition for inhibiting uterine contractility by topical or local administration. The composition contains an omega fatty acid in combination with a cyclo-oxygenase inhibitor. Preferred omega fatty acids include docosahexaenoic acid and eicosapentaenoic acid, and preferred cyclo-oxygenase inhibitors include acetylsalicylic acid and salicylic acid. The composition may further include pharmaceutically acceptable carriers or diluents, and may be locally applied via intracervical or intrauterine application, or may be topically applied to the skin of the lower abdomen.
    Type: Grant
    Filed: May 13, 1993
    Date of Patent: April 25, 1995
    Inventors: Barry I. Bockow, Marc D. Erlitz
  • Patent number: 5409956
    Abstract: The present invention relates to indan derivatives represented by the formula (1) or pharmaceutically acceptable salts thereof: ##STR1## [wherein R.sup.1 represents C1 to C12 alkyl, benzyl, styryl, naphthyl, optionally substituted phenyl or optionally substituted thienyl; R.sup.2 represents carboxyl, C1 to C4 alkoxycarbonyl, ##STR2## Y represents --(CH.sub.2).sub.p -- (wherein p represents an integer of 0 to 5), --CO--(CH.sub.2).sub.q .about., --CH(OH)--(CH.sub.2).sub.q .about., (wherein q represents an integer of 1 to 4, and the symbol .about. represents a linkage to R.sup.2), oxymethylene or ethylene; and n represents an integer of 1 to 4]. The compounds according to the present invention potently antagonize the action of thromboxane A.sub.2, and therefore useful for the treatment and prevention of diseases caused by thromboxane A.sub.2 such as angiosis, vasospasm, asthma and the like.
    Type: Grant
    Filed: August 30, 1993
    Date of Patent: April 25, 1995
    Assignee: Zeria Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Yoshida, Yoshiaki Yamaji, Tadashi Kurimoto, Ryuichi Sato, Motoki Torizuka
  • Patent number: 5409957
    Abstract: Disclosed are a phenoxyalkylamine represented by the following general formula I and a salt of said phenoxyalkylamine represented by the following general formula II: ##STR1## wherein R represents a linear saturated hydrocarbon having 7 to 12 carbon atoms, n is an integer of from 1 to 5, m is an integer of from 2 to 4, and HX represents a mineral acid.These compounds have strong bacteriostatic and bactericidal actions for plants with no phytotoxicity. Therefore, these compounds are effectively used as the active ingredient of an agricultural and horticultural bactericide.
    Type: Grant
    Filed: March 23, 1993
    Date of Patent: April 25, 1995
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Mitsunori Oda, Kazutoshi Kikkawa, Akinori Tanaka, Satoko Imaruoka, Shigeo Yoshinaka
  • Patent number: 5409958
    Abstract: Described is a method for repelling at least one of the insect species:(a) Musca domestica L. (Diptera:Muscidae);(b) Aedes aegypti;(c) Aedes albopictus;(d) Anopheles spp.(e) Coquillettidia perturbans;(f) Culiseta spp.;(g) Culex spp.;(h) Psorophora spp.;(i) Culicoides spp.; and/or(j) Lutzomyia spp.for a finite period of time from a three dimensional space comprising the step of exposing the three dimensional space to an insect species (as named above) concentration and quantity of an alkylcyclopentanone having the structure: ##STR1## or a phenylalkanol derivative having the structure having the structure: ##STR2## or mixtures of one of the above compounds with mixtures of cycloalkanol derivatives produced according to U.S. Pat. No. 4,275,251 issued on Jun. 23, 1981.
    Type: Grant
    Filed: November 26, 1993
    Date of Patent: April 25, 1995
    Assignees: International Flavors & Fragrances Inc., The University of Florida
    Inventors: Jerry F. Butler, Craig B. Warren, Anna B. Marin, Braja D. Mookherjee, Richard A. Wilson
  • Patent number: 5409959
    Abstract: A method of inhibiting thrombus formation in a mammalian subject. The method involves administering to the subject a therapeutically effective dose of a calix(n)arene compound derivatized, at its ring positions meta to the bridge attachments to the ring, with polar substituents having terminal sulfonate groups, including esters and amides which are cleavable in vivo.
    Type: Grant
    Filed: August 6, 1992
    Date of Patent: April 25, 1995
    Assignee: Genelabs Incorporated
    Inventors: Kou M. Hwang, You M. Qi, Su-Ying Liu, Thomas C. Lee, William Choy, Jen Chen
  • Patent number: 5409960
    Abstract: Pentane (or similar light hydrocarbon) is used in a gas conversion process to consume the exothermic heat of reaction in the Fischer-Tropsch process, and expanded to produce the energy to drive the air plant compressors.
    Type: Grant
    Filed: June 15, 1994
    Date of Patent: April 25, 1995
    Assignee: Exxon Research and Engineering Company
    Inventor: Thomas M. Stark
  • Patent number: 5409961
    Abstract: There is now provided a rigid closed cell polyisocyanate based foam for use as a positive flotation material for watercraft which meets the U.S. Coast Guard immersion test (CGD 75-168, 33 C.F.R. .sctn.183.114). As a blowing agent for this foam, a mixture of 1,1,1,2-tetrafluoroethane (R-134a) as a frothing agent and water is used, where the amount of water is less than 2.5 weight percent based on the weight of the formulated polyol composition. Also, in preferable embodiments, the polyols in the polyol composition are initiated by at least one amine; and the polyol composition contains a delayed action tertiary amine catalyst. The foams used in the invention have excellent dimensional stability. In another embodiment, there is also provided a formulated polyol composition of R-134a and a polyol composition having an average OH# of less than 400 and an average functionality of greater than 4 using R-134a and less than 2.5 wt.
    Type: Grant
    Filed: July 8, 1994
    Date of Patent: April 25, 1995
    Assignee: BASF Corporation
    Inventor: Todd J. Green
  • Patent number: 5409962
    Abstract: Substantially constant boiling blowing agent compositions of 1,1,1,2-tetrafluoroethane and dimethyl ether.
    Type: Grant
    Filed: December 16, 1991
    Date of Patent: April 25, 1995
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Philip L. Bartlett, Joseph A. Creazzo
  • Patent number: 5409963
    Abstract: A silicone composition capable of being cured by both a moisture-curing mechanism and an ultraviolet (UV) curing mechanism is provided. The silicone composition comprises:1 a reactive organosiloxane prepared by a condensation reaction of a silicone (1) represented by the general formula ##STR1## where R.sup.1 and R.sup.2 are each an organo group, and a is a number corresponding to a kinematic viscosity of 25-50,000 cSt, measured at 25.degree. C., with a vinyl ether silane compound represented by the general formula: ##STR2## where m and n are each an integer of 1 to 5, R.sup.3 and R.sup.4 are each an alkyl group having 1 to 3 carbon atoms or allyl, and b is 0 or 1;2 0-70 parts by weight of a silicone oil having trimethylsilyl group as an end group;3 a catalytic amount of a photopolymerization catalyst; and4 a catalytic amount of a silicone moisture-curing catalyst.
    Type: Grant
    Filed: December 28, 1993
    Date of Patent: April 25, 1995
    Assignee: Three Bond Co., Ltd.
    Inventor: Toru Takfoka
  • Patent number: 5409964
    Abstract: Photochemically linkable polymers corresponding to formula (I)P-(A).sub.n (I)in whichP is a polymer component,A is a photochemically reactive unit andn is the number 1 or 2,and their use for immunological purposes.
    Type: Grant
    Filed: September 18, 1992
    Date of Patent: April 25, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ludger Heiliger, Eberhard Kuckert
  • Patent number: 5409965
    Abstract: An active energy ray-curing abrasion resistant coating composition is provided by incorporating following components: (a) a carboxylate-containing polyfunctional acrylate obtained by reacting a tetracarboxylic dianhydride and a hydroxyl group-containing polyfunctional acrylate having hydroxyl group(s) and at least three acryloyl groups and then neutralizing the reaction product; (b) a polyfunctional acrylate having at least three acryloyl groups; (c) an organic solvent; and (d) a photopolymerization initiator. The composition may comprise in addition to the components (e) a silica sol in an organic solvent as a dispersion medium. The composition may further comprise in addition to the components (f) an acrylic resin. Such composition is an active energy ray-curing abrasion-resistant coating composition which forms a film having excellent adhesion to a plastic sustrate, transparency, abrasion resistance and antistatic properties.
    Type: Grant
    Filed: July 26, 1994
    Date of Patent: April 25, 1995
    Assignee: Mitsubishi Petrochemical Co., Ltd.
    Inventors: Noritaka Hosokawa, Kazuhide Hayama
  • Patent number: 5409966
    Abstract: A hydrophilic, pressure-sensitive adhesive composition prepared by irradiating solid poly(N-vinyl lactam) with ionizing radiation to crosslink the poly(N-vinyl lactam) and thereafter mixing the radiation-crosslinked poly(N-vinyl lactam) with essentially unirradiated plasticizer in an amount sufficient to form a cohesive, pressure-sensitive adhesive composition. The composition is useful as a biomedical adhesive for transmitting or receiving electrical signals as a component of a biomedical electrode. The composition is also useful as a drug delivery device to deliver pharmaceuticals or other active ingredients to or through mammalian skin. The composition is also useful as a component in a skin covering for protecting mammalian skin Or mammalian skin openings with antimicrobial agents. A method of preparation of the composition is also disclosed.
    Type: Grant
    Filed: October 15, 1993
    Date of Patent: April 25, 1995
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Daniel C. Duan, Robert A. Asmus, Timothy M. Dietz, Rosa Uy, Olester Benson, Jr.
  • Patent number: 5409967
    Abstract: Impact modifiers which produce transparent, high notched Izod impact strength blends with amorphous, aromatic polyesters are described. The impact modifiers are core-shell polymers with cores comprised mainly of rubbery polymers of diolefins and vinyl aromatic monomers and shells comprised mainly of styrene copolymers (e.g. styrene and hydroxyalkyl (meth)acrylate).
    Type: Grant
    Filed: March 22, 1994
    Date of Patent: April 25, 1995
    Assignee: Rohm and Haas Company
    Inventors: William G. Carson, Choung-Houng Lai, Edward J. Troy
  • Patent number: 5409968
    Abstract: The invention provides semi-conductive, static dissipative polymeric composites comprising:a) an insulative polymeric resin, andb) from about 5 to about 35 volume percent of at least one high aspect ratio filler having a thin-film inorganic layer of from about 10 .ANG. to about 1000 .ANG. of a highly conductive metal and an overlayer of an insulative metal oxide, said layer having an average coating thickness of from about 2 .ANG. to about 200 .ANG.,the composites having volume resistivities of from about 1.times.10.sup.4 ohm-cm to about 1.times.10.sup.11 ohm-cm.
    Type: Grant
    Filed: November 6, 1992
    Date of Patent: April 25, 1995
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: William J. Clatanoff, Craig S. Chamberlain