Nitrogen Not Bonded Directly To A Ring Patents (Class 562/442)
  • Patent number: 5430182
    Abstract: The present invention relates to a novel sweetening agent and to its method of preparation. This novel sweetening agent is a 2-substituted acyl derivative of L-aspartic or L-glutamic acid and has the general formula ##STR1## R being an acyl group of the formula ##STR2## and R' being a group of the formula ##STR3## R.sub.1, R.sub.2, R.sub.3, X, Y and Z being variously defined. This novel sweetening agent is essentially characterized by a high sweetening potency and a high stability compatible with the conditions of industrial use, and is applied especially for sweetening soft drinks.
    Type: Grant
    Filed: March 15, 1994
    Date of Patent: July 4, 1995
    Inventors: Claude Nofre, Jean-Marie Tinti
  • Patent number: 5428065
    Abstract: Pharmaceutical compounds of the formula: ##STR1## R.sup.1 to R.sup.8 are each hydrogen or C.sub.1-4 alkyl, m, n and p are each 0, 1, or 2, q is 0, 1, 2 or 3, X and Z are each C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, nitro, cyano, halo, trihalomethyl, carboxy, C.sub.1-4 alkoxy-carbonyl or phenyl, and in addition z, together with the phenyl ring to which it is attached, can be: ##STR2## Y is --O--, --S-- or --CH.sub.2 --, V is --(CH.sub.2).sub.r -- or --(CH.sub.2).sub.r S-- where r is 1 to 15, and W is hydrogen or optionally substituted phenyl; and salts thereof.
    Type: Grant
    Filed: September 27, 1994
    Date of Patent: June 27, 1995
    Assignee: Lilly Industries Limited
    Inventors: Barry P. Clark, Graham H. Timms
  • Patent number: 5387594
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: August 4, 1992
    Date of Patent: February 7, 1995
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5378728
    Abstract: Compound of the formula ##STR1## where R is CH.sub.3 (CH.sub.2).sub.m, A and B are hydrogen, a bond or --(CH.sub.2).sub.n,X is ##STR2## m is 0, 1 , 2 or 3, n is 1 , 2, or 3, R.sub.1 is hydrogen or lower alkyl, andY is --OH, --OR.sub.2 or --NR.sub.3 R.sub.4where R.sub.2, R.sub.3 and R.sub.4 are hydrogen or unsubstituted or substituted alkyl, aryl and aralkyl substituents.
    Type: Grant
    Filed: September 20, 1993
    Date of Patent: January 3, 1995
    Assignee: Sandoz Ltd.
    Inventors: Jeffrey Nadelson, William R. J. Simpson, Robert C. Anderson, Joginder S. Bajwa
  • Patent number: 5364961
    Abstract: The invention includes selected novel optically active .alpha.-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.
    Type: Grant
    Filed: June 15, 1992
    Date of Patent: November 15, 1994
    Assignee: Monsanto Company
    Inventor: John J. Talley
  • Patent number: 5358956
    Abstract: Novel fibrinogen receptor antagonists of the formula: ##STR1## are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.
    Type: Grant
    Filed: October 14, 1992
    Date of Patent: October 25, 1994
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, Wasyl Halczenko
  • Patent number: 5356893
    Abstract: The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt or solvate thereof wherein R.sup.1 represents a halogen or hydrogen atom or a C.sub.1-6 alkyl or C.sub.1-6 alkoxy group;R.sup.2 represents a phenyl group optionally substituted by one or two substituents;R.sup.3 represents the group ##STR2## R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a halogen atom, or a group selected from hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl.The compounds may be used in the treatment or prophylaxis of depression and other CNS disorders.
    Type: Grant
    Filed: September 17, 1992
    Date of Patent: October 18, 1994
    Assignee: Glaxo Group Limited
    Inventors: John Bradshaw, John W. Clitherow, Ian B. Campbell
  • Patent number: 5298647
    Abstract: Aromatic compounds absorbing UVB and/or UVA, substituted with an amide function, selected from the group consisting of ##STR1## whose variable substituents are as defined in the specification, e.g. ##STR2## are useful as photoprotective agents or tanning accelerators.
    Type: Grant
    Filed: December 14, 1987
    Date of Patent: March 29, 1994
    Inventors: Dominique Robert, Louis Jung
  • Patent number: 5294646
    Abstract: The invention relates to new N-alkyl-N-(meth)acryloyloxyalkylcarboxamides of aromatic carboxylic acids and aromatic carboxylic acid anhydrides, their preparation and formulations of these compounds for use as adhesives for the treatment of dental hard substance.
    Type: Grant
    Filed: June 25, 1992
    Date of Patent: March 15, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Muller, Wolfgang Podszun, Werner Finger, Jens Winkel
  • Patent number: 5252317
    Abstract: Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines.
    Type: Grant
    Filed: May 22, 1992
    Date of Patent: October 12, 1993
    Assignee: The State of Oregon Acting by and through the State Board of Higher Education on Behalf of the University of Oregon
    Inventor: John F. W. Keana
  • Patent number: 5241081
    Abstract: The invention relates to new N-alkyl-N-(meth)acryloyloxyalkylcarboxamides of aromatic carboxylic acids and aromatic carboxylic acid anhydrides, their preparation and formulations of these compounds for use as adhesives for the treatment of dental hard substance.
    Type: Grant
    Filed: August 9, 1991
    Date of Patent: August 31, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Muller, Wolfgang Podszun, Werner Finger, Jens Winkel
  • Patent number: 5238958
    Abstract: The present invention is novel substituted .alpha.-amino acids, pharmaceutical compositions, methods of use, and preparations therefore having utility for treating disorders which benefit from blockade of aspartate and glutamate receptors.
    Type: Grant
    Filed: April 23, 1990
    Date of Patent: August 24, 1993
    Assignee: Warner-Lambert Company
    Inventors: Graham Johnson, Thomas C. Malone, Perry M. Novak
  • Patent number: 5232948
    Abstract: Monocyclic aryl compounds having selective LTB.sub.4 antagonists properties and comprising an amido substituent, a substituent group having a terminal carboxylic acid or derivative thereof and a lipophilic substituent, therapeutic compositions and methods of treatment of disorders which result from LTB.sub.4 activity using the monocyclic aryl compounds are disclosed.
    Type: Grant
    Filed: September 10, 1990
    Date of Patent: August 3, 1993
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Fu-Chih Huang, Wan K. Chan, Charles A. Sutherland, Robert A. Galemmo, Jr., Michael N. Chang
  • Patent number: 5228899
    Abstract: Plant growth regulators comprising, as an active ingredient, a substituted dicarboxylic acid derivative having the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, D and G are the same as defined in the present specification, the substituted dicarboxylic acid derivatives, and processes for preparing the same, are disclosed. The plant growth regulators provided according to the present invention have a regulating activity on plant growth; more specifically, an action thereof of lowering the content of endogenous ethylene in a plant is utilized.
    Type: Grant
    Filed: August 24, 1990
    Date of Patent: July 20, 1993
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Yoshikazu Itoh, Akio Manabe, Masato Mizutani, Naonori Hirata, Sachiko Uwayokote, Kazuo Izumi, Kenji Arai
  • Patent number: 5217855
    Abstract: A photographic processing composition containing at one compoud represented by formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, an aliphatic group, or an aromatic group, L.sub.1 and L.sub.2 each represents a divalent bonding group including an alkylene group and/or an arylene group; X represents a ##STR2## group (wherein R.sub.a, R.sub.b and R.sub.c each represents a hydrogen atom, an aliphatic group or an aromatic group, and R.sub.d represents an aliphatic group or an aromatic group); and Y represents a carboxy group, a hydroxy group, a phosphono group, a sulfo group or a salt thereof. The processing composition does not produce precipitate or sludge even when contaminated by metallic ions. A processing method using the processing composition is also disclosed.
    Type: Grant
    Filed: July 25, 1991
    Date of Patent: June 8, 1993
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Okada, Morio Yagihara, Shigeru Nakamura
  • Patent number: 5175299
    Abstract: A pyrazole derivative having the formula ##STR1## is disclosed; the groups A, B, Q, V, W, X, Y, and Z are defined in the description.
    Type: Grant
    Filed: November 1, 1991
    Date of Patent: December 29, 1992
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Masatoshi Baba, Takuya Kakuta, Norio Tanaka, Eiichi Oya, Takashi Ikai, Tsutomu Nawamaki, Shigeomi Watanabe
  • Patent number: 5149709
    Abstract: Amides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl;and in addition, one of R.sub.1 and R.sub.2 can be as defined above and the other can be phenyl;R.sub.3 is an alkyl chain of 2 to 25 carbon atoms, saturated or unsaturated; an alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl; an alkyl chain as defined interrupted by one or more groups independently selected from the group consisting of --O--, --S--, --SO--, --SO.sub.2 --, --NH--, --N(lower alkyl)--, --C(O)--, phenylene, X-substituted phenylene, heteroarylene and X-substituted heteroarylene; or an interrupted alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl;R.sub.
    Type: Grant
    Filed: July 3, 1990
    Date of Patent: September 22, 1992
    Assignee: Schering Corporation
    Inventors: John Clader, Sundeep Dugar, Timothy Kogan, Bradley Tait, Wayne Vaccaro
  • Patent number: 5118816
    Abstract: There are provided important pyrroline and glycine intermediates, methods for the preparation of these intermediates and their use in the manufacture of insecticidal, acaricidal and nematocidal arylpyrrole compounds. Illustrative of the pyrroline and glycine intermediates are compounds having the following structures: ##STR1## wherein A is hydrogen or C.sub.1 -C.sub.4 alkyl and W is CN, NO.sub.2 or CO.sub.2 R.sub.6.
    Type: Grant
    Filed: December 26, 1990
    Date of Patent: June 2, 1992
    Assignee: American Cyanamid Company
    Inventors: Robert F. Doehner, Jr., Jerry M. Barton, David G. Kuhn
  • Patent number: 5112868
    Abstract: The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.
    Type: Grant
    Filed: May 2, 1990
    Date of Patent: May 12, 1992
    Assignee: Warner-Lambert Company
    Inventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
  • Patent number: 5110797
    Abstract: Peptide compounds of formula (I): ##STR1## wherein A is hydrogen or an amino-protecting group; X is a member selected from the group consisting of Gly, Glu, Tyr, Asp, Phe, Ile, Ala, Pro, Leu, Hyp, Val, His, Arg, Ser, Thr, Pyr, Trp, 5-HTP, Cys, Met, .tau.-Glu, .beta.-Asp; Y is a (CH.sub.2).sub.3-6 or (CH.sub.2).sub.3-6 having an hydroxy group; R is an hydroxy group or an oxygen atom with a carboxy-protecting group; are useful as neurotropic agents.
    Type: Grant
    Filed: April 29, 1988
    Date of Patent: May 5, 1992
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Kazuharu Ienaga, Kunihiko Higashiura
  • Patent number: 5047420
    Abstract: Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.
    Type: Grant
    Filed: August 21, 1989
    Date of Patent: September 10, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Donald W. Graham, Tesfaye Biftu, John C. Chabala, Michael N. Chang, Yuan-Ching P. Chiang, Kathryn L. Thompson, Shu S. Yang
  • Patent number: 5017604
    Abstract: The present invention is novel selected hydroxamic acid derivatives of fenamic acids having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.
    Type: Grant
    Filed: April 11, 1990
    Date of Patent: May 21, 1991
    Assignee: Warner-Lambert Company
    Inventors: Thomas R. Belliotti, Catherine R. Kostlan
  • Patent number: 5001156
    Abstract: Lipophilic quaternary ammonium salicylate, characterized in that it corresponds to the formula: ##STR1## in which: (i) R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote an alkyl or alkylcycloalkyl radical, optionally substituted or interrupted;(ii) R.sub.3 and/or R.sub.4 denote(s) a group:R.sub.8 [OC.sub.2 H.sub.3 R.sub.7 ].sub.n [OCH.sub.2 CHOH--CH.sub.2 ].sub.pin which 0.ltoreq.n.ltoreq.4 and p denotes 0 or 1; R.sub.8 denotes H or an alkyl, alkenyl, alkylcycloalkyl or alkylaryl radical;(iii) R.sub.4 denotes an alkylphenyl radical;(iv), (v) R.sub.1 and R.sub.2 can form a saturated or unsaturated aromatic or non-aromatic heterocycle;(vi) R.sub.1, R.sub.2 and R.sub.3 form polycyclic derivatives with the nitrogen atoms; R.sub.5 denotes a group corresponding to the formula: ##STR2## in which n is an integer varying between 0 and 10.
    Type: Grant
    Filed: December 1, 1987
    Date of Patent: March 19, 1991
    Assignee: L'Oreal
    Inventors: Michel Philippe, Henri Sebag, Michel Hocquaux, Bernard Jacquet, Jean P. Laugier
  • Patent number: 4990533
    Abstract: Novel benzoic acid or benzoic acid ester derivatives, pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headache, such as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.
    Type: Grant
    Filed: November 10, 1986
    Date of Patent: February 5, 1991
    Assignee: Warner-Lambert Co.
    Inventors: Michael F. Rafferty, Graham Johnson
  • Patent number: 4980095
    Abstract: Novel benzoic acid or benzoic acid ester derivatives, pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headache, such as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.
    Type: Grant
    Filed: June 1, 1987
    Date of Patent: December 25, 1990
    Assignee: Warner-Lambert Company
    Inventors: Michael F. Rafferty, Graham Johnson
  • Patent number: 4973746
    Abstract: Scrap poly(ethyleneterephthalate) is converted to useful amine and diamine monomers such as para-xylylenediamine, 1,4-bis(aminomethyl)cyclohexane and 4-aminomethyl benzoic acid for the production of various polyamides. The conversion of poly(ethyleneterephthalate) to diamine monomers is achieved by a three step process involving (a) ammonolysis of the poly(ethyleneterephthalate) to produce terephthalamide and ethylene glycol; (b) pyrolytic dehydration of the terephthalamide to produce terephthalonitrile; and (c) hydrogenation of the terephthalonitrile to produce the para-xylylene diamine and/or 1,4-bis(aminomethyl)cyclohexane. The conversion of poly(ethyleneterephthalate) to 4-aminomethyl benzoic acid involves the steps of (a) ammonolysis of the poly(ethyleneterephthalate) to produce terephthalamide; (b) partial pyrolytic dehydration of said terephthalamide to produce 4-cyanobenzoic acid; and (c) hydrogenation of said 4-cyanobenzoic acid to produce 4-aminomethylbenzoic acid.
    Type: Grant
    Filed: October 24, 1988
    Date of Patent: November 27, 1990
    Assignee: General Electric Company
    Inventors: Kenneth P. Blackmon, Daniel W. Fox, Sheldon J. Shafer
  • Patent number: 4965279
    Abstract: Novel cyclopropyl aza prostaglandin analogs are disclosed having the formula ##STR1## wherein A can be carbonyl, sulfonyl or a single bond. These compounds are useful, for example, as thromboxane antagonists.
    Type: Grant
    Filed: November 18, 1988
    Date of Patent: October 23, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Raj N. Misra, David M. Floyd, Steven E. Hall
  • Patent number: 4933367
    Abstract: This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.
    Type: Grant
    Filed: March 12, 1987
    Date of Patent: June 12, 1990
    Assignee: Boehringer Mannheim GmbH
    Inventors: Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuhnle
  • Patent number: 4912221
    Abstract: The instant invention relates to optically pure, L-(S)forms of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid compounds and their method of preparation from optionally pure L-phenylalanine precursor compounds and their preparation utilizing novel in situ cationic catalyst systems.
    Type: Grant
    Filed: October 27, 1988
    Date of Patent: March 27, 1990
    Assignee: Occidental Chemical Corporation
    Inventors: Neil J. O'Reilly, Henry C. Lin
  • Patent number: 4895842
    Abstract: A phenylalanine derivative having the formula (I): ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen provided that both R.sup.1 and R.sup.2 are not hydrogen at the same time;C.sub.1 -C.sub.8 alkyl which may be substituted with hydroxy, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.1 -C.sub.4 alkylmercapto, C.sub.1 -C.sub.4 alkoxy, carbamoyl, sulfamoyl, pyridyl, or phenyl which may further be substituted with nitro, C.sub.1 -C.sub.4 alkoxy, or halogen;C.sub.6 -C.sub.8 cycloalkyl which may be substituted with hydroxy, C.sub.1 -C.sub.4 alkoxy, hydroxylcarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, or C.sub.1 -C.sub.4 alkyl;phenyl which may be substituted with halogen, nitro, trifluoromethyl, C.sub.1 -C.sub.4 alkoxy C.sub.1 C.sub.4 alkylmercapto, C.sub.1 -C.sub.4 alkylcarbonyl, phenylcarbonyl, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, carbamoyl, sulfamoyl, amidino, pyridylcarbonyl, or C.sub.1 -C.sub.6 alkyl which may further be substituted with C.sub.1 -C.sub.
    Type: Grant
    Filed: September 29, 1986
    Date of Patent: January 23, 1990
    Assignees: Shosuke Okamoto, Showa Denko Kabushiki Kaisha
    Inventors: Shosuke Okamoto, Yoshio Okada, Akiko Okunomiya, Taketoshi Naito, Yoshio Kimura, Morihiko Yamada, Norio Ohno, Yasuhiro Katsuura, Yumi Seki
  • Patent number: 4889947
    Abstract: Sunscreen compositions are described which contain certain substituted naphthalenylidenes which act as UV filters when incorporated in a carrier in amounts ranging from 0.1-50% by weight.
    Type: Grant
    Filed: July 28, 1988
    Date of Patent: December 26, 1989
    Assignee: ICI Americas Inc.
    Inventors: Charalambos J. Phalangas, Thomas P. Cleary
  • Patent number: 4883815
    Abstract: Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy carbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxy carbonyl-C.sub.2 -C.sub.5)-alky, piperidino-C.sub.2 -C.sub.
    Type: Grant
    Filed: July 5, 1988
    Date of Patent: November 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Aschwenden, Rene Imhof, Roland Jakob-Roetne, Emilio Kyburz
  • Patent number: 4871865
    Abstract: The present invention relates to compounds of formula I ##STR1## or a salt, ester or amide thereof; wherein R.sup.1 is --CH.sub.2 --CH.sub.2 --, CH.sub.2 --O-- or --O--CH.sub.2 --; R.sup.2 and R.sup.3 are the same or different and are each hydrogen, C.sub.1-4 alkyl or taken together with the nitrogen comprise a nitrogen-containing heterocyclic ring having four to six ring members; R.sup.4 is a single bond or a C.sub.1-7 bivalent aliphatic hydrocarbon group and may be joined to the aromatic ring system at the 2,3,8 or 9 positions; n is 0 to 3, and their use as anithistamine and antiasthma agents.
    Type: Grant
    Filed: August 7, 1986
    Date of Patent: October 3, 1989
    Assignee: Burroughs Wellcome Co.
    Inventors: O. William Lever, Jr., Harry J. Leighton
  • Patent number: 4870096
    Abstract: Indoles are disclosed of formula (I): ##STR1## wherein R.sub.1 represents R.sub.5 R.sub.6 NCOCH.sub.2 --, R.sub.5 CONH(CH.sub.2).sub.p --,R.sub.5 R.sub.6 NSO.sub.2 (CH.sub.2).sub.p -- or R.sub.7 SO.sub.2 NH(CH.sub.2).sub.p --, (where R.sub.5 and R.sub.6 each represents a hydrogen atom or a C.sub.1-3 alkyl group, R.sub.7 represents C.sub.1-3 alkyl and p is zero or one),R.sub.2 is hydrogen or C.sub.1-3 alkyl;R.sub.3 and R.sub.4 each represents hydrogen atom, C.sub.1-3 alkyl, or 2-propenyl;m is zero or an integer from 1 to 4; andn is an integer from 2 to 5; and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. They may be formulated as pharmaceutical compositions with pharmaceutically acceptable carriers of excipients for administration by any convenient route.Various methods for the preparation of the compounds (I) are disclosed.
    Type: Grant
    Filed: December 11, 1986
    Date of Patent: September 26, 1989
    Assignee: Glaxo Group Limited
    Inventors: Alexander W. Oxford, Ian H. Coates, David E. Bays, Colin F. Webb
  • Patent number: 4861887
    Abstract: A method for the preparation of o-carboxyl imidazolinone compounds including oxidizing the appropriate 2-{[(1-carbamoyl-1,2-dimethylpropyl)amino]methyl}-benzoic acid intermediate with a brominating agent. Compounds useful as intermediates in the oxidation method and methods for preparing them are disclosed.
    Type: Grant
    Filed: January 27, 1988
    Date of Patent: August 29, 1989
    Assignee: American Cyanamid Company
    Inventor: Robert F. Doehner, Jr.
  • Patent number: 4857660
    Abstract: 1-Phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.
    Type: Grant
    Filed: April 22, 1988
    Date of Patent: August 15, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Alex Alder, Jaroslav Stanek, Daniel Bellus
  • Patent number: 4789742
    Abstract: Novel Isomaleimido and isophthalimido derivatives of chromophoric compounds are provided which are useful in analytic techniques for the detection and measurement of biological compounds such as bacteria, enzymes, hormones and the like.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: December 6, 1988
    Inventor: Spyros Theodoropulos
  • Patent number: 4783535
    Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed. The oxazepinones and oxazepinethiones prepared by the process have utility as antihistaminics with low sedative potential. Novel intermediate compounds are also disclosed.
    Type: Grant
    Filed: March 18, 1986
    Date of Patent: November 8, 1988
    Assignee: A. H. Robins Company, Incorporated
    Inventors: Young S. Lo, Albert D. Cale, Jr.
  • Patent number: 4780535
    Abstract: Conjugates of isomaleimides and isophthalimides and organic chromophoric compounds exhibiting fluorescence, luminescence, chemiluminescence or absorption of analytical value having the structural formula I and II ##STR1## wherein R is an organic aromatic molecule which may be substituted, heteroaromatic which may be substituted, aliphatic having 1 to 50 carbon atoms and which may be substituted or an organic chromophoric molecule exhibiting fluorescence, luminescence, chemiluminiescence or absorption of analytical value. R' is an organic chromophoric molecule exhibiting fluorescence, luminescence, chemiluminescence, or absorption of analytical value; R.sub.1 is hydrogen, halogen, carboxylic, alkyl, aryl, hydroxyl, amino group which may be substituted, nitro or sulfonic group. R.sub.2, R.sub.3 and R.sub.4 have the same meaning as R.sub.
    Type: Grant
    Filed: November 21, 1986
    Date of Patent: October 25, 1988
    Inventor: Spyros Theodoropulos
  • Patent number: 4754047
    Abstract: There is provided a method for enhancing the growth rate of meat-producing animals and/or improving the efficiency of feed utilization thereby, which involves, orally or parenterally, administering to said animals a growth-enhancing amount of a phenylethanolamine compound or the acid addition salt thereof.
    Type: Grant
    Filed: December 10, 1984
    Date of Patent: June 28, 1988
    Assignee: American Cyanamid Company
    Inventors: Jane A. Kiernan, Pamela K. Baker
  • Patent number: 4749701
    Abstract: Disclosed are an aminostyryl compound represented by Formula I: ##STR1## wherein A represents a linking group having 3 to 4 chain members; B represents an unsubstituted or substituted 5 to 6-membered monocyclic type heterocyclic residue containing 1 to 2 hetero atoms, an unsubstituted or substituted condensed heterocyclic residue which contains 5 to 6-membered monocyclic type heterocycle containing 1 to 2 hetero atoms, a naphthyl group or an alkyl group having 5 to 7 carbon atoms,a composition having leukotriene antagonism which contains an aminostyryl compound represented by Formula I as the effective ingredient, and a method of antagonizing SRS based on leukotriene antagonistic activity by employing the same.
    Type: Grant
    Filed: December 15, 1986
    Date of Patent: June 7, 1988
    Assignee: Mitsubishi Chemical Industries Limited
    Inventors: Yoshio Hayashi, Tomei Oguri, Masaki Shinoda, Kazuo Takahashi
  • Patent number: 4727184
    Abstract: A composition comprising an aromatic copolyester-carbonate having flexural modulus, flexural yield and secondary transition temperature improvement over a corresponding aromatic polycarbonate effective amount of ester units of the structure ##STR1## or mixtures of the above two structures wherein R.sub.1 and R.sub.2 are the same or different and are alkyl of one to six carbon atoms, inclusive, cycloalkyl of four to seven carbon atoms, inclusive, phenyl, one to three alkyl substituted phenyl each alkyl having one to three carbon atoms, inclusive, and R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached form a ring of four to six carbon atoms, inclusive, or carbazole.
    Type: Grant
    Filed: October 20, 1986
    Date of Patent: February 23, 1988
    Assignee: General Electric Company
    Inventor: Niles R. Rosenquist
  • Patent number: 4720505
    Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic and anti-inflammatory agents.
    Type: Grant
    Filed: November 13, 1984
    Date of Patent: January 19, 1988
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Patrice C. Belanger, John W. Gillard, Joshua Rokach
  • Patent number: 4719310
    Abstract: The invention relates to novel ester and amide substituted [2,3-dihydro-4-(3-oxo-1-cyclohexen-1-yl)phenoxy]alkanoic acids and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.
    Type: Grant
    Filed: December 23, 1985
    Date of Patent: January 12, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Adolph M. Pietruszkiewicz, Otto W. Woltersdorf, Jr., Edward J. Cragoe, Jr.
  • Patent number: 4689182
    Abstract: Novel benzoic acid or benzoic acid ester derivatives, pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headache, such as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.
    Type: Grant
    Filed: December 20, 1985
    Date of Patent: August 25, 1987
    Assignee: Warner-Lambert Company
    Inventors: Michael F. Rafferty, Graham Johnson
  • Patent number: 4673744
    Abstract: A method for converting .beta.-aspartylphenylalanine derivative (1) to .alpha.-aspartylphenylalanine derivatives (2) and (3), said derivatives having the following structures: ##STR1## which comprises: reacting said .beta.-aspartylphenylalanine derivative (1) at a temperature of from 0.degree. to 200.degree. C. for a time period of from 30 minutes to 80 hours, in a C.sub.1 to C.sub.4 alcohol solvent with or without stirring, wherein R and R' represent hydrogen or an alkyl group having from 1 to 4 carbon atoms.
    Type: Grant
    Filed: May 1, 1986
    Date of Patent: June 16, 1987
    Assignee: Ajinomoto Co., Inc.
    Inventors: Kunio Hisamitsu, Tadashi Takemoto, Toshihide Yukawa, Kunio Hisamitsu
  • Patent number: 4642375
    Abstract: An improved and simplified process for preparing terephthalic acid monoamide derivatives of the formula ##STR1## in which R denotes hydrogen, an alkaline earth metal or alkali metal cation or methyl, R.sub.1 denotes C.sub.8 -C.sub.30 -alkyl, preferably C.sub.12 -C.sub.22 -alkyl, and R.sub.2 denotes C.sub.1 -C.sub.30 -alkyl or, preferably hydrogen, in which dimethyl terephthalate is reacted with an amine of the formulaHNR.sub.1 R.sub.2in methanol and in the presence of sodium methylate. The compounds thus obtained are used for gelling oils and organic solvents.
    Type: Grant
    Filed: October 24, 1985
    Date of Patent: February 10, 1987
    Inventor: Werner Ritschel
  • Patent number: 4637902
    Abstract: A base precursor represented by the following general formula (A) or (B): ##STR1## wherein A.sub.1, A.sub.2, A.sub.5, A.sub.6, A.sub.7, and A.sub.8 each represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, an alkenyl group, an aralkyl group, an aryl group, a substituted aryl group, an acyl group, or a heterocyclic group, and A.sub.1 and A.sub.2 can combine to form a ring and two of A.sub.5, A.sub.6, A.sub.7, and A.sub.8 can combine to form a ring, A.sub.3 and A.sub.4 each represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, or an aralkyl group, and A.sub.3 and A.sub.4 can combine to form a ring or A.sub.3 and A.sub.4 can be a double bond forming an imino group from ##STR2## and X represents a nucleophilic group.
    Type: Grant
    Filed: March 14, 1984
    Date of Patent: January 20, 1987
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hiroyuki Hirai, Ken Kawata
  • Patent number: 4634777
    Abstract: Compounds of the general formula: ##STR1## wherein A and B are both hydrogen, or one of A and B is a group (G) of the formula: ##STR2## and the other is a group R.sup.5 wherein R.sup.1 is an aryl group or a heterocyclic group, both of them being optionally substituted, and R.sup.4 and R.sup.5 are both hydrogen or together form a single chemical bond,R.sup.2 and R.sup.2 ' are independently hydrogen, halogen, nitro, lower alkyl or lower alkoxy, andR.sup.3 and R.sup.3 ' are independently carboxy or its functional derivative, with the proviso that (a) when A and B are both hydrogen, then R.sup.2 and R.sup.2 ' cannot be both hydrogen,and, where applicable, pharmaceuticably acceptable salts thereof are hyaluronidase inhibitors, and useful as anti-allergic agent and anti-ulcerous agent. Among the compound (I'), those wherein when one of A and B is the group (G) and the other is the group R.sup.5 wherein R.sup.4 and R.sup.5 together form a single chemical bond, R.sup.1 is unsubstituted aryl and R.sup.2 and R.sup.
    Type: Grant
    Filed: February 1, 1985
    Date of Patent: January 6, 1987
    Assignee: Sawai Pharmaceutical Co., Ltd.
    Inventors: Toshio Satoh, Hitoshi Matsumoto, Hisao Kakegawa, Yoshiko Kato, Juichi Riku, Junji Yoshinaga, Yoshifumi Kanamoto
  • Patent number: 4629737
    Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereof, in which: W is an optionally substituted phenyl group of the formula ##STR2## wherein R.sup.1 is hydrogen or fluorine, R.sup.2 is hydrogen, C.sub.1-6 alkyl, halogen or trifluoromethyl; or W is a phenoxymethyl or benzofuran-2-yl group;R.sup.3 is C.sub.1-12 alkyl or phenyl C.sub.1-6 alkyl;A is hydrogen or methyl,X is carboxy, --Z--CO.sub.2 H, --Z--OH, T--Z--CO.sub.2 H,--Z--NR.sup.4 R.sup.5, --T--Y--OM, --T--Y--NR.sup.4 R.sup.5, or --T--R.sup.6, in the para- or meta-position with respect to the --(CH.sub.2).sub.n group,whereinR.sup.4 and R.sup.5 are each hydrogen or C.sub.1-6 alkyl,R.sup.6 is C.sub.1-6 alkyl,T is 0, S, --NH or --N--R.sup.7, in which R.sup.7 is C.sub.1-6 alkylZ is C.sub.1-10 straight or branched alkylene optionally containing a carbon-carbon double bond;Y is C.sub.2-10 straight or branched alkylene, provided that the hetero atoms in --T--Y--OM and --T--Y--NR.sup.4 R.sup.
    Type: Grant
    Filed: July 14, 1983
    Date of Patent: December 16, 1986
    Assignee: Beecham Group p.l.c.
    Inventor: Barrie C. C. Cantello