The Other Ring Is Alicyclic Patents (Class 564/338)
  • Patent number: 6329552
    Abstract: The invention relates to a compound of formula (I), wherein R is an alkyl unsubstituted by one or more polar substituents or an alkenyl unsubstituted or substituted by one or more polar substituents, and X is aryl, or salts thereof. The compounds are effective e.g. against protozoa and trematodes.
    Type: Grant
    Filed: December 22, 2000
    Date of Patent: December 11, 2001
    Assignee: Novartis AG
    Inventors: Thomas Allmendinger, Walther Helmut Wernsdorfer
  • Patent number: 6310102
    Abstract: Pharmaceutical compositions aryl substituted amine compounds, and in particular, 3-aminophenyl amine compounds are provided. Representative compounds are (E)-4-(3-aminophenyl)-3-buten-1-amine, (E)-N-methyl-4-(3-aminophenyl)-3-buten-1-amine and (E)-N-methyl-5-(3-aminophenyl)-4-penten-2-amine.
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: October 30, 2001
    Assignee: Targacept, Inc.
    Inventors: Gary Maurice Dull, Jared Miller Wagner, William Scott Caldwell, Craig Harrison Miller, Jeffrey Daniel Schmitt, Balwinder Singh Bhatti, Srishailkumar Basawannappa Hadimani
  • Patent number: 6268520
    Abstract: Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.
    Type: Grant
    Filed: April 5, 1999
    Date of Patent: July 31, 2001
    Assignee: Hoechst Marion Roussel
    Inventors: Francis Brion, Bernadette Chappert, Christian Diolez, Christian Marie, Alain Mazurie, Michel Middendorp, Didier Pronine, Edmond Toromanoff
  • Patent number: 6008411
    Abstract: Nortriptyline functionalized compounds are provided for conjugation to antigenic compositions, particularly poly(amino acids), and enzymes. The antigenic conjugates are employed for the production of antibodies, which find use in immunoassays for the determination of nortriptyline in a sample, while the enzyme conjugates find use in an enzyme assay for the determination of nortriptyline in a sample.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 28, 1999
    Assignee: Dade Behring Marburg GmbH
    Inventors: Mae W. Hu, Prithipal Singh
  • Patent number: 5932620
    Abstract: A 1,2-ethanediol derivative represented by the general formula ?I! or its salt: ##STR1## has a NGF activity-potentiating effect and is useful as a remedy for various diseases caused by degeneration of central nervous system or peripheral nervous system such as senile dementia of Alzheimer type, Huntington's chorea, various neuropathies, Riley-Day syndrome, traumatic nerve injury, amyotrophic lateral sclerosis (ALS) and the like.
    Type: Grant
    Filed: December 31, 1997
    Date of Patent: August 3, 1999
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Mutsuko Maekawa, Kazunari Hirata, Hirokazu Narita
  • Patent number: 5792762
    Abstract: The invention provides dihydronaphthofluorene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions.
    Type: Grant
    Filed: September 19, 1997
    Date of Patent: August 11, 1998
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones
  • Patent number: 5677454
    Abstract: Disclosed are compounds of the formula: ##STR1## where S and V are various organic or inorganic substituents;G and K are the same or different and represent N or CR' where R' is an organic or inorganic substituent;R is hydrogen or an alkyl group;R.sub.1, X, Y, Z and T are organic or inorganic substituents; andR.sub.2 and R.sub.3 represent hydrogen or organic substituents; orNR.sub.2 R.sub.3 together represents a heterocyclic ring system;and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: October 14, 1997
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Andrew Thurkauf
  • Patent number: 5612381
    Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 18, 1997
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
  • Patent number: 5538986
    Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.
    Type: Grant
    Filed: December 6, 1993
    Date of Patent: July 23, 1996
    Assignee: Schering Corporation
    Inventors: Pauline C. Ting, Daniel M. Solomon, Richard J. Friary, Frank J. Villani, John J. Piwinski, Joe F. Lee, Dhiru B. Vashi
  • Patent number: 5482964
    Abstract: Substituted phenoxyhydroxy amines and derivatives thereof are described as well as methods for the preparation and pharmaceutical compositions of same, which are central nervous system agents useful in the treatment of neurological disorders including traumatic brain surgery, stroke, migraine, acute and chronic pain, epilepsy, Parkinson's disease, Alzheimer's disease, amyotropic lateral sclerosis, multiple sclerosis, psychosis, and depression.
    Type: Grant
    Filed: October 11, 1994
    Date of Patent: January 9, 1996
    Assignee: Warner-Lambert Company
    Inventor: Sheryl J. Hays
  • Patent number: 5472984
    Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.
    Type: Grant
    Filed: December 29, 1993
    Date of Patent: December 5, 1995
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
  • Patent number: 5449693
    Abstract: The present invention relates to compounds of the formula ##STR1## in which: R.sub.1 is hydrogen or a halogen atom;R.sub.2 is a cyclohexyl or a phenyl;R.sub.3 is a (C.sub.3 -C.sub.6) cycloalkyl;R.sub.4 is hydrogen, (C.sub.1 -C.sub.6) alkyl or a (C.sub.3 -C.sub.6) cycloalkyl;A is --CO--CH.sub.2 --, --CH(Cl)--CH.sub.2 --, --CH(OH)--CH.sub.2 --, CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- and --C.tbd.C--, or their addition salts with mineral or organic acids. These compounds are active on the immune system. The present invention further relates to a method of preparing said compounds and to the pharmaceutical compounds in which they are present.
    Type: Grant
    Filed: June 22, 1994
    Date of Patent: September 12, 1995
    Assignee: Sanofi
    Inventors: Jean-Claude Breliere, Pierre Casellas, Serge Lavastre, Raymond Paul
  • Patent number: 5422367
    Abstract: Diphenylcyclopropyl analogs in which one or more of the phenyl rings includes substituents comprising a hydroxy group, a hydrogen atom, an acetate group or a substituted or unsubstituted alkoxy group. The compounds are useful as antiestrogens and anti-tumor agents.
    Type: Grant
    Filed: February 25, 1994
    Date of Patent: June 6, 1995
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Robert A. Magarian, Joseph T. Pento, Kwasi S. Avor
  • Patent number: 5420294
    Abstract: This invention provides a method of selectively antagonizing the 5-HT.sub.1A receptor in mammals by administering aryloxypropanolamines. Aryloxypropanolamines are also claimed.
    Type: Grant
    Filed: December 22, 1993
    Date of Patent: May 30, 1995
    Assignee: Eli Lilly and Company
    Inventors: Edward E. Beedle, David W. Robertson, David T. Wong
  • Patent number: 5354781
    Abstract: The present invention relates to compounds of the formula ##STR1## in which: p1 R.sub.1 is hydrogen or a halogen atom; R.sub.2 is a cyclohexyl or a phenyl;R.sub.3 is a (C.sub.3 -C.sub.6) cycloalkyl;R.sub.4 is hydrogen, (C.sub.1 -C.sub.6) alkyl or (C.sub.3 -C.sub.6)cycloalkyl;A is --CO--CH.sub.2 --, --CH(CI)--CH.sub.2 --, --CH(OH)--CH.sub.2 --, CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- and --C.tbd.C--, or their addition salt with mineral or organic acids. These compounds are active on the immune system. The present invention further relates to a method of preparing said compounds and to the pharmaceutical compounds in which they are present.
    Type: Grant
    Filed: May 24, 1991
    Date of Patent: October 11, 1994
    Assignee: Sanofi
    Inventors: Jean-Claude Breliere, Pierre Casellas, Serge Lavastre, Raymond Paul
  • Patent number: 5334628
    Abstract: Amine derivatives having the general formula (I): ##STR1## wherein X is selected from the group consisting of ##STR2## wherein Q is oxygen, sulfur or nitrogen atom, and ##STR3## wherein Q is as above; Y is selected from the group consisting of ##STR4## R.sup.1 is hydrogen atom or an alkyl group; R.sup.2 is hydrogen atom or an alkyl group; R.sup.3 is hydrogen atom, a halogen atom or an alkyl group; R.sup.4 hydrogen atom, an alkyl group, a cycloalkyl group, a halogenated alkyl group or a halogen atom; R.sup.5 is hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, nitro group or hydroxy group; R.sup.5 is attached to an arbitrary position of X, and R.sup.3 or R.sup.4 is attached to an arbitrary position of Y.The amine derivatives (I) are useful as fungicides.
    Type: Grant
    Filed: December 31, 1992
    Date of Patent: August 2, 1994
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventors: Tetsuya Maeda, Toshiyuki Yamamoto, Mituo Takase, Kazuya Sasaki, Tadashi Arika, Mamoru Yokoo, Rieko Hashimoto, Kouji Amemiya, Sakae Koshikawa
  • Patent number: 5225601
    Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: October 31, 1991
    Date of Patent: July 6, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5130339
    Abstract: New phenylethanolaminomethyltetralins of formula (I) ##STR1## wherein E represents hydrogen, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, phenyl, nitro, halogen, or trifluoromethyl,L represents hydrogen, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkyoxy, phenyl, nitro, or halogen, orE and L taken together represent a group --CH.dbd.CH--CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --, andG represents hydrogen, chloro, hydroxy or an --OG' group wherein G' represents a (C.sub.1 -C.sub.4 (alkyl group either unsubstituted or substituted with hydroxy, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkoxycarbonyl, carboxy, or (C.sub.3 -C.sub.7)cycloalkyl; a (C.sub.3 -C.sub.7)cycloalkyl group; or a (C.sub.2 -C.sub.4)alkanoyl group; and salts thereof, are described which showed to be active as intestinal motility modulating agents and intraocular hypertension lowering agents.
    Type: Grant
    Filed: December 28, 1990
    Date of Patent: July 14, 1992
    Assignee: Sanofi
    Inventors: Roberto Cecchi, Umberto Guzzi
  • Patent number: 5047432
    Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof; in which R.sub.1 and R.sub.2, which are the same or different, are H or an optionally substituted hydrocarbon group or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring;R.sub.3 is an optionally substituted aromatic hydrocarbon group; andR.sub.4 is a hydrocarbon group containing at least one substituent selected from the group consisting of hydroxy and acylated derivatives thereof, optionally substituted alkoxy groups, optionally substituted cycloalkyloxy groups, optionally substituted alkylenedioxy groups, oxo and groups of formula S(O).sub.p R.sub.5 in which p is 0, 1 or 2 and R.sub.5 is an alkyl group, said hydrocarbon group being optionally substituted by additional substituents,are useful in the treatment of depression.
    Type: Grant
    Filed: June 20, 1990
    Date of Patent: September 10, 1991
    Assignee: The Boots Company Plc
    Inventors: John R. Housley, James E. Jeffery, David N. Johnston, Bruce J. Sargent
  • Patent number: 5013761
    Abstract: This invention provides a method of selectively antagonizing the 5-HT.sub.1A receptor in mammals by administering aryloxypropanolamines. Novel aryloxypropanolamines are also claimed.
    Type: Grant
    Filed: November 8, 1989
    Date of Patent: May 7, 1991
    Assignee: Eli Lilly and Company
    Inventors: Edward E. Beedle, David W. Robertson, David T. Wong
  • Patent number: 4925879
    Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof; in which R.sub.1 and R.sub.2, which are the same or different, are H or an optionally substituted hydrocarbon group or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring;R.sub.3 is an optionally substituted aromatic hydrocarbon group; andR.sub.4 is a hydrocarbon group containing at least one substituent selected from the group consisting of hydroxy and acylated derivatives thereof, optionally substituted alkoxy groups, optionally substituted cycloalkyloxy groups, optionally substituted alkylenedioxy groups, oxo and groups of formula S(O).sub.p R.sub.5 in which p is 0, 1 or 2 and R.sub.5 is an alkyl group, said hydrocarbon group being optionally substituted by additional substituents,are useful in the treatment of depression.
    Type: Grant
    Filed: August 1, 1988
    Date of Patent: May 15, 1990
    Assignee: Boots Company, PLC
    Inventors: John R. Housley, James E. Jeffery, David N. Johnston, Bruce J. Sargent
  • Patent number: 4847414
    Abstract: 2'-substituted-spiro[benzofuran-2(3H),1'-cyclohexanes] and methods of preparing same are described. On the aromatic portion of the benzofuran ring, there may be a substituent or substituents including halogen, amino, lower-alkyl-substituted amino, lower alkyl, lower alkoxy, hydroxy and nitro. The substituents at the 2-position of the cyclohexane ring are --(CH.sub.2).sub.n NR.sup.1 R.sup.2 where n is 0, 1 or 2 and R.sup.1 and R.sup.2 are each independently hydrogen and alkyl of 1-3 carbons. These compounds are useful as antidepressants and analgesics.Various other compounds which are useful as intermediates for preparing the aforementioned compounds and methods for preparing same are also described.
    Type: Grant
    Filed: March 2, 1983
    Date of Patent: July 11, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Michael C. Jones
  • Patent number: 4820734
    Abstract: The novel phenethylamine derivatives of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each signify hydrogen, halogen, trifluoromethyl, lower alkoxy, lower alkyl, hydroxy or nitro, with the proviso that at least one of R.sup.1 and R.sup.2 is different from hydrogen, R.sup.3 and R.sup.4 each signify lower alkyl, n signifies the number 1, 2, 3 or 4 and B signifies the group --CO-- or --CHOH--, and their pharmaceutically acceptable acid addition salts have interesting analgesic and antidepressant properties. These substances can be manufactured according to various methods which are known per se and can be used as medicaments in the form of pharmaceutical preparation.
    Type: Grant
    Filed: November 4, 1987
    Date of Patent: April 11, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Hans Bruderer
  • Patent number: 4705807
    Abstract: Novel amines of formula:R--(CH.sub.2).sub.n --NR.sup.1 R.sup.2where R is cis-2-phenylbicyclo[2,2,2]octane or 2-phenylbicyclo[2,2,2]oct-2-ene nucleus, n is 1 to 3, R.sup.1 is C.sub.1-3 alkyl and R.sup.2 is hydrogen or C.sub.1-3 alkyl, and acid-addition salts thereof, which are useful for the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: December 10, 1982
    Date of Patent: November 10, 1987
    Assignee: Lilly Industries Limited
    Inventors: David C. Horwell, Graham H. Timms
  • Patent number: 4652584
    Abstract: Phenoxypropanol derivatives having a 2-acetylenic moiety on the phenyl group thereof of the following formula (I): ##STR1## and their use as anti-hypertensives, e.g. in man. Also part of the invention are pharmaceutical compositions and intermediates used in the synthesis.
    Type: Grant
    Filed: July 13, 1984
    Date of Patent: March 24, 1987
    Assignee: McNeilab, Inc.
    Inventor: John R. Carson
  • Patent number: 4647699
    Abstract: New aminoalkyl anilines having the formula: ##STR1## wherein k is 0 or 1; QNH.sub.2 is a residue of formula ##STR2## which is situated in one of the positions of the benzene ring ortho or para to the amino group and wherein n is an integer from 1 to 15, R.sub.1 is C.sub.1 -C.sub.8 alkyl, R.sub.2 is C.sub.1 -C.sub.4 alkyl or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a C.sub.5 -C.sub.8 cycloalkylene residue, R.sub.3 is H or C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or C.sub.6 -C.sub.10 aryl; and R.sub.4 and R.sub.5 are H or C.sub.1 -C.sub.4 alkyl; as well as the corresponding salts of compounds of formula I with organic or inorganic acids and metal salt complexes; process for their production; and their use as intermediates for polyamides.
    Type: Grant
    Filed: April 3, 1985
    Date of Patent: March 3, 1987
    Assignee: Ciba-Geigy Corporation
    Inventor: Frederick H. Howell
  • Patent number: 4626522
    Abstract: Novel benzoxazocines of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R.sup.1 represents hydrogen, or one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro, amino acylamino, mono- or di- (lower)alkyl-amino or cyano substituents, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each represent hydrogen or lower alkyl or R.sup.3 and R.sup.4 together represent --(CH.sub.2).sub.3 --or --(CH.sub.2).sub.4 --, R.sup.5 represents hydrogen, lower alkyl, phenyl(lower)alkyl or cycloalkyl(lower)alkyl, and Ar is a phenyl radical optionally substituted by one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro or amino groups exhibit activity on the central nervous system, particularly as antidepressants. The compounds can be prepared from novel alcohols of formula (II) ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Ar are as defined above and X is fluorine, chlorine or bromine.
    Type: Grant
    Filed: September 18, 1981
    Date of Patent: December 2, 1986
    Assignee: John Wyeth & Brother Limited
    Inventors: Alan C. White, Robin G. Shepherd
  • Patent number: 4596891
    Abstract: There is disclosed diamines of the formula ##STR1## wherein R.sub.6 is H, Cl, or CH.sub.3 ; andR.sub.8 " is H, Cl, or CH.sub.3, with the provisos that(a) if R.sub.8 " is H or CH.sub.3, R.sub.7 " is CH.sub.3 ; and(b) if R.sub.8 " is Cl, R.sub.7 " is F; and(c) if R.sub.6 and R.sub.8 " are both H, R.sub.7 " is any of CH.sub.3, F, CF.sub.3, trifluoromethoxy, trifluoromethylsulfonyl, cyclohexyl, C.sub.2 -C.sub.10 alkyl, p-chlorophenoxy or p-chlorophenyl alkyl having 7 or 8 carbon atoms. The diamines have algicidal activity.
    Type: Grant
    Filed: November 20, 1980
    Date of Patent: June 24, 1986
    Assignee: Duphar International Research B.V.
    Inventors: Jaap van Gilse, Gerard B. Paerels
  • Patent number: 4564625
    Abstract: Salts formed between penbutolol and furosemide or piretanide, pharmaceutical compositions containing such salts, and methods for treating diseases of the coronary and circulatory systems with such salts.
    Type: Grant
    Filed: May 10, 1984
    Date of Patent: January 14, 1986
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Roman Muschaweck, Werner Fulberth, Alfred Sickmuller
  • Patent number: 4554379
    Abstract: New compounds having the formula:R.sub.4 (QNH.sub.2).sub.x Iwherein x is 1 or 2 and the residues QNH.sub.2 are the same or different and each is a residue of formula: ##STR1## wherein n is an integer from 1 to 15, R.sub.1 is C.sub.1 -C.sub.8 alkyl, R.sub.2 is C.sub.1 -C.sub.4 alkyl or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a C.sub.5 -C.sub.8 cycloalkylene residue, R.sub.3 is H or C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl or C.sub.6 -C.sub.10 aryl and R.sub.4 is a mono- or polyvalent C.sub.6 -C.sub.20 aromatic or C.sub.4 -C.sub.20 .pi.-excessive heterocyclic residue; these compounds are useful as intermediates for polyamides, plastics and for compounds having biological activity.
    Type: Grant
    Filed: April 18, 1985
    Date of Patent: November 19, 1985
    Assignee: Ciba Geigy Corporation
    Inventor: Frederick H. Howell
  • Patent number: 4508732
    Abstract: Basic ethers of the formula ##STR1## wherein Z is CH.sub.3 -NR.sup.2 -CH.sub.2 CH.sub.2 -CHR.sup.1 --, (1-R.sup.2 -3-piperidyl)-CHR.sup.3 --, (1-R.sup.2 -2-piperidyl)-CH.sub.2 -CHR.sup.3 -- or 1-R.sup.2 -3-R.sup.4 -- hexahydroazepinyl; R.sup.1 is cyclopropyl or Ar; R.sup.2 is H, alkyl of 1-4 C atoms, alkenyl of 2-4 C atoms, cycloalkylalkyl of 4-8 C atoms or benzyl; R.sup.3 is H or Ar; R.sup.4 is H or alkyl of 1-4 C atoms, Y is --O-CHQ.sup.1 -CHQ.sup.2 -CH.sub.2 --, --O-CHQ.sup.1 -CHQ.sup.2 -CO--, --O-CQ.sup.1 .dbd.CQ.sup.2 -CO-- or --CH.sub.2 -CHQ.sup.1 -CHQ.sup.2 -CO--; Q.sup.1 and Q.sup.2 are independently each H, alkyl of 1-4 C atoms, cycloalkyl or alkylcycloalkyl each of 3-6 total C atoms or Ar; and Ar is phenyl or phenyl substituted by F, Cl, alkoxy or alkylthio, each of 1-4 C atoms, methylenedioxy or CF.sub.3 ; with the proviso that when Z is (CH.sub.3).sub.2 N-CH.sub.2 CH.sub.2 -CHR.sup.1 in 7-position and Y is --O-C(C.sub.6 H.sub.5).dbd.CH-CO-- or --O-C(C.sub.6 H.sub.5).dbd.C(CH.sub.3)-CO--, R.sup.
    Type: Grant
    Filed: January 21, 1983
    Date of Patent: April 2, 1985
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Hans-Heinrich Hausberg, Helmut Prucher, Jurgen Uhl, Christoph Seyfried, Klaus Minck
  • Patent number: 4399076
    Abstract: 2-Vinyl- and 2-ethylcyclopropanes having an aryl group and a nitrogen-containing radical substituted at the 1-position on the ring are provided. The novel 1,1-disubstituted 2-vinylcyclopropane and 2-ethylcyclopropane compounds of this invention have utility in herbicidal applications and are useful reactants. The 2-vinylcyclopropane derivatives are useful monomers for anionic and radical polymerizations.
    Type: Grant
    Filed: February 22, 1982
    Date of Patent: August 16, 1983
    Assignee: National Distillers and Chemical Corporation
    Inventors: Richard G. Fayter, Jr., Allen L. Hall
  • Patent number: 4336268
    Abstract: Cyclohexenes of the formula ##STR1## wherein R.sup.1 is hydroxy or lower alkoxy; n is 1 or 2; R.sup.2 is lower alkyl; and R.sup.3 is hydrogen, lower alkyl, lower alkenyl or lower cycloalkylmethyl, and their pharmaceutically acceptable acid addition salts are disclosed. The compounds of formula I have analgesic activity and are useful for the control of pains.
    Type: Grant
    Filed: January 27, 1981
    Date of Patent: June 22, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Bruderer, Albert E. Fischli, Rudolf Pfister
  • Patent number: 4322370
    Abstract: Compounds of the formula (II): ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is phenyl or naphthyl or substituted phenyl or naphthyl group; R.sub.2 is: ##STR2## wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl, R.sub.6 is hydrogen or C.sub.1-6 alkyl, phenyl, tolyl or benzyl and R.sub.7 is hydrogen; R.sub.3 and R.sub.4 are each hydrogen atom or C.sub.1-4 alkyl, and X is CO, CHOH, CHCI or C.dbd.C R.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are each hydrogen or C.sub.1-4 alkyl; or CR.sub.10 OH or CHR.sub.10, wherein R.sub.10 is C.sub.1-4 alkyl, have been found to be mood-modifying agents and anorexic agents.
    Type: Grant
    Filed: February 13, 1978
    Date of Patent: March 30, 1982
    Assignee: Beecham Group Limited
    Inventor: Derek V. Gardner
  • Patent number: 4293193
    Abstract: A group of novel, low temperature liquid crystalline compounds with terminal, primary or secondary amino polar electron donating groups are disclosed. These include, for example, p-alkyl-or alkoxy-phenylcyclohexanes, bicyclohexyls or biphenyl ring systems, substituted at the p' position with alkyl primary or secondary amines, of which one example is p-(4-trans-n-pentylcyclohexyl)benzylamine.
    Type: Grant
    Filed: August 15, 1979
    Date of Patent: October 6, 1981
    Assignee: Temple University
    Inventors: Mortimer M. Labes, John H. MacMillan
  • Patent number: 4275071
    Abstract: Imidazole derivatives of the formula I and pharmaceutically acceptable acid addition salts thereof are provided: ##STR1## In the formula, R.sub.4 1- or 2-naphthyl, optionally substituted with Cl, Br, or I; 1,2,3,4-tetrahydro-6-naphthyl; 3-duryl, optionally 6-substituted by Cl, Br, I, NO.sub.2, CH.sub.3 or benzyl; mesityl, phenyl 2-, 3- or 4-substituted by OH, NH.sub.2, NO.sub.2, CH.sub.3 CONH, phenyl, phenoxy, cyclohexyl, phenylthio, benzylthio, C.sub.1 -C.sub.6 alkyl or C.sub.1 C.sub.6 alkylthio; 4-bibenzylyl; 3,4-dihydroxyphenyl,n=0, 1 or 2 and(a) R=H, alkyl having 1 to 6 carbon atoms or phenyl R.sub.1 =H, alkyl having 1 to 6 carbon atoms or phenyl one of R.sub.2 and R.sub.3 =H the other of R.sub.2 and R.sub.3 =H, OH, benzoyloxy, C.sub.2 -C.sub.7 alkanoyloxy, N-(C.sub.1 -C.sub.6 alkyl)-carbamoyloxy, N,N-[di-(C.sub.1 C.sub.6)alkyl]-carbamoyloxy, but if R.sub.2 =R.sub.3 =H then R=R.sub.1 =H, or(b) R=H, C.sub.1 -C.sub.6 alkyl, phenyl R.sub.1 =H, C.sub.1 -C.sub.6 alkyl, phenyl R.sub.2 +R.sub.
    Type: Grant
    Filed: July 10, 1979
    Date of Patent: June 23, 1981
    Assignee: Recordati S.A.
    Inventors: Dante Nardi, Alberto Tajano, Maria J. Magistretti