Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/471)
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Patent number: 5985869Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R.sup.2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R.sup.3 is a group: --NR.sup.4 R.sup.5 or --CO--NR.sup.11 R.sup.12 ; R.sup.4 is H, optionally substitued benzoyl, alkyl; R.sup.5 is a group: ##STR2## [R.sup.16 is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO.sub.2, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: --O--A--NR.sup.6 R.sup.7 ; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenylalkanoyl, etc.; R.sup.11 is H or alkyl; R.sup.12 is cycloalkyl or optionally substituted phenyl; and W is a group: --(CH.sub.2).sub.p (p is 3 to 5) or --CH.dbd.CH--(CH.sub.2).sub.q (q is 1 to 3), the carbon atom of these groups beign optionally replaced by O, S, SO, SO.sub.Type: GrantFiled: July 15, 1997Date of Patent: November 16, 1999Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Hajime Komatsu, Michinori Tanaka, Shinya Kora, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5945423Type: GrantFiled: January 14, 1998Date of Patent: August 31, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: James Francis Bereznak, Zen-Yu Chang, Thomas Paul Selby, Charlene Gross Sternberg
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Patent number: 5853699Abstract: The disclosed metal complexes are suitable as contrast media for computer tomography of the liver and the biliary tracts.Type: GrantFiled: November 30, 1995Date of Patent: December 29, 1998Assignee: Schering AktiengesellschaftInventors: Franz-Karl Maier, Michael Bauer, Werner Krause, Ulrich Speck, Gabriele Schuhmann-Giampiere, Andreas Muhler, Thomas Balzer, Wolf-Rudiger Press
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Patent number: 5821365Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2, X, W, and Y are as defined in the specification. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.Type: GrantFiled: November 14, 1997Date of Patent: October 13, 1998Assignee: Eli Lilly and CompanyInventors: Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
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Patent number: 5786352Abstract: Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.C<, --CO--N< or --CS--N< as the partial structure --X . . . Y<; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Ring C is optionally substituted homocyclic or heterocyclic ring; Ring Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.Type: GrantFiled: March 25, 1996Date of Patent: July 28, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Takenori Ishimaru, Takayuki Doi, Yoshinori Ikeura, Chiharu Kimura
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Patent number: 5750518Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: May 27, 1997Date of Patent: May 12, 1998Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Henrik Sune Andersen, Rolf Hohlweg, Peter Madsen, Uffe Bang Olsen
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Patent number: 5739322Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## wherein R1, R2, X, W, and Y are as defined in the specification. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.Type: GrantFiled: March 20, 1997Date of Patent: April 14, 1998Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
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Patent number: 5733924Abstract: DC107 derivatives represented by the formula (I): ##STR1## or pharmacologically acceptable slats thereof, ?wherein R.sup.1 is hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR.sup.4 or the like; R.sup.2 represents hydrogen or COR.sup.5 ; R.sup.3 represents lower alkyl, lower alkenyl, aralkyl which may be substituted with substituted or unsubstituted aryl, lower alkoxyalkyl, aralkyloxyalkyl, substituted or unsubstituted aryloxyalkyl, lower alkoxycarbonylalkyl, lower alkanoyloxyalkyl, alicyclic alkanoyloxyalkyl or the like, or bonds to Y to represent a single bond; Y bonds to R.sup.3 to represent a single bond, or bonds to Z to represent a single bond; Z represents hydrogen or bonds to Y to represent a single bond; W represents oxygen or NR.sup.6, with the proviso that the compound wherein R.sup.1, R.sup.2 and Z each represents hydrogen, R.sup.3 bonds to Y to represent a single bond, and W represents oxygen (DC107) is excluded.Type: GrantFiled: April 17, 1997Date of Patent: March 31, 1998Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yutaka Kanda, Yutaka Saitoh, Hiromitsu Saito, Tadashi Ashizawa, Kazuyo Sugiyama, Katsushige Gomi, Shingo Kakita, Yuichi Takahashi, Chikara Murakata
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Patent number: 5731299Abstract: The present invention relates to phosphonsulfonates and the pharmaceutically-acceptable salts and esters thereof, having the following structure according to formula (I): ##STR1## The present invention further relates to pharmaceutical compositions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients. Finally, the present invention relates to methods for treating or preventing pathological conditions characterized by abnormal calcium and phosphate metabolism in humans or other mammals, including treating or preventing osteoporosis and arthritis, especially rheumatoid arthritis and osteoarthritis. This method comprises administering to a human or other mammal in need of such treatment of a safe and effective amount of a compound or composition of the present invention.Type: GrantFiled: May 7, 1993Date of Patent: March 24, 1998Assignee: The Procter & Gamble CompanyInventors: Frank Hallock Ebetino, Allan Vincent Bayless, Susan Mary Dansereau
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Patent number: 5714604Abstract: A novel process for the preparation of azamacrocyclic or acyclic aminophosphonate ester derivatives is disclosed. The process concerns the reaction of an appropriate azamacrocyclic or acyclic primary or secondary amine with trialkyl phosphite and paraformaldehyde.Type: GrantFiled: May 6, 1993Date of Patent: February 3, 1998Assignee: The Dow Chemical CompanyInventor: Garry E. Kiefer
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Patent number: 5712396Abstract: .alpha.-Phosphonosulfonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is H, alkyl, arylalkyl or aryl; R4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.Type: GrantFiled: July 5, 1994Date of Patent: January 27, 1998Inventors: David R. Magnin, Scott A. Biller, John K. Dickson, Jr., R. Michael Lawrence, Richard B. Sulsky
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Patent number: 5698546Abstract: Linked polyamine cyclic compounds of general formula V--R--A--R'--W where V and W are independently cyclic polyamine moieties having from 9 to 32 ring members and 3 to 8 amine nitrogens and having either one or more aromatic rings fused thereto or a heteroatom other than nitrogen incorporated in the ring, A is an aliphatic or aromatic moiety and R and R' are each a linking chain, possess improved partition coefficients at biologically relevant pH compared to known compounds, and possess high anti-HIV activity.Type: GrantFiled: June 20, 1996Date of Patent: December 16, 1997Assignee: Johnson Matthey Public Limted CompanyInventors: Gary J. Bridger, Sreenivasan Padmanabhan, Renato T. Skerlj
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Patent number: 5608059Abstract: Ion-sensitive compounds have the formula A.sup.2+ B.sup.2- wherein A represents a cation capable of forming a receptor-substrate complex with an anion, and B represents one or more counter anions, the cation being an anion receptor of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each independently a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group or R.sup.1 and R.sup.2 taken together with the atoms separating them represent the atoms necessary to complete a (2)-cryptand; and,R.sup.3 and R.sup.4 are each independently H or a lower alkyl group having from 1 to 4 carbon atoms, or R.sup.3 and R.sup.4 taken together represent an ethylene bridging group.The compounds may be used for sensing anions.Type: GrantFiled: December 19, 1994Date of Patent: March 4, 1997Assignee: Eastman Kodak CompanyInventors: Trevor J. Wear, Christopher P. Moore, Alistair J. Goulden, Paul D. Beer, Nicholas C. Fletcher
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Patent number: 5554751Abstract: Aminoureidofullerene and aminothioureidofullerene derivatives and the process for the preparation thereof Aminoureido and aminothioureido compounds of the fullerenes C.sub.60 and/or C.sub.70 and processes for the preparation thereof and use thereof are described.Type: GrantFiled: November 10, 1994Date of Patent: September 10, 1996Assignee: Hoechst AktiengesellschaftInventor: Klaus-Dieter Kampe
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Patent number: 5482936Abstract: Compounds and pharmaceutically acceptable salts thereof formally derived by bridging the 1- and 2-positions of 1H-imidazo[4,5-c]quinolin-4-amines. Also, methods of using such compounds and pharmaceutical formulations containing such compounds. Said compounds are useful to induce interferon biosynthesis in an animal.Type: GrantFiled: January 12, 1995Date of Patent: January 9, 1996Assignee: Minnesota Mining and Manufacturing CompanyInventor: Kyle J. Lindstrom
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Patent number: 5434262Abstract: A method for the synthesis of cyclic polyamines preceeds by reaction of a diamine with the acrylonitrile wherein the reduction steps are carried out with Raney alloy instead of using hydrogen under pressure in the presence of Raney nickel. Compounds so prepared have the formula: ##STR1## wherein A and B are: an alkyl chain --(CH.sub.2)-- in which x is an integer of 2 to 4, substituted or not by an alkyl group of 1 to 5 carbon atoms, which may be substituted or not by an aromatic ring, heterocyclic ring, amine ketone, carboxylic acid, amide, cyano, alkyl, alkoxy, hydroxy, nitro or halogen and R.sub.1 and R.sub.2 are the same moieties as those substituting the alkyl claim above.Type: GrantFiled: September 16, 1992Date of Patent: July 18, 1995Assignee: L'Air Liquide, Societe Anonyme pour l'Etude et l'Exploitation des Procedes Georges ClaudeInventors: Roger Guilard, Isabelle Meunier, Christophe Jean, Brigitte Boisselier-Cocolios
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Patent number: 5302589Abstract: The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10whereinR.sup.9 and R.sup.Type: GrantFiled: August 7, 1992Date of Patent: April 12, 1994Assignee: Glaxo, Inc.Inventors: Stephen V. Frye, David Middlemiss, Francis G. Fang
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Patent number: 5271927Abstract: The conjugation of antibodies to a macrocyclic conjugate compound wherein the conjugate compound has the structure (I), wherein R.sup.1 is --(CH.sub.2).sub.p --R.sup.6 --CH.sub.2).sub.q -- where p and q are the same or different and are 0, 1 or 2, and --R.sup.6 -- is --((CH.sub.2).sub.n --, where n is 0 or 1, --NH--, --O--, --S-- or (II), R.sup.1 optionally being alkyl substituted, provided that neither p nor q is 0 unless R.sup.6 is --CH.sub.2 --; R.sup.2 are --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 --, optionally alkyl, alkoxyalkyl or hydroxyalkyl substituted; R.sup.3 are the same or different and are --H, alkyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl, carboxyalkyl ester, phosphate, sulphonate or phosphonate; R.sup.4 is one of the compounds of formula (III) optionally alkyl substituted, wherein R.sup.7 is --H, alkyl, hydroxyalkyl, or alkoxyalkyl provided that when R.sup.4 is (III d), R.sup.3 is not carboxyalkyl, R.sup.5 is a linker, and Ab is an antibody.Type: GrantFiled: March 18, 1993Date of Patent: December 21, 1993Assignee: Celltech LimitedInventors: David Parker, Thomas A. Millican
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Patent number: 5252580Abstract: Disclosed are indole derivatives of formula (I) ##STR1## wherein Y represents H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or halogen;Z represents --CH.sub.2 N(R.sub.5)--;R represents H or --CH.sub.2 CH.sub.2 X where X represents pyridyl, aralkyloxy or substituted amino of NR.sub.6 R.sub.7 where R.sub.6 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl, C.sub.1 -C.sub.6 alkoxycarbonyl, aralkyloxycarbonyl or halogenated C.sub.1 -C.sub.6 alkoxycarbonyl and R.sub.7 represents H, C.sub.1 -C.sub.6 alkyl or aralkyl, or together with R.sub.2 may form a ring of --(CH.sub.2).sub.n -- (n is 1-4) or ##STR2## R.sub.1 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl or arylsulfonyl; R.sub.2 represents C.sub.1 -C.sub.6 alkyl, hydroxy, C.sub.1 -C.sub.6 alkoxy or aralkyloxy;R.sub.3 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl or halogenated C.sub.1 -C.sub.6 alkyl;R.sub.4 and R.sub.5 may be the same or different and each represents H, C.sub.1 -C.sub.6 alkyl or aralkyl or both may together form a ring of --(CH.sub.2).sub.Type: GrantFiled: September 18, 1992Date of Patent: October 12, 1993Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Toshihiro Takahashi, Hitoshi Inoue, Masato Horigome, Kenichi Momose, Masanori Sugita, Kouichi Katsuyama, Chikako Suzuki, Shinji Nagai, Masao Nagase, Koichi Nakamaru
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Patent number: 5238936Abstract: The compounds are trisubstituted triazines and pyrimidines useful for the suppressing the resistance of tumour cells to anti-cancer agents and for suppressing the resistance of parasites to anti-parasitic agents.A compound disclosed is 2,4-diallylamino-6-{4-[(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl) methylamino]piperidin-1-yl}-1,3,5-triazine.Type: GrantFiled: March 6, 1992Date of Patent: August 24, 1993Assignee: Adir et CompagnieInventors: Gilbert Regnier, Alain Dhainaut, Ghanem Atassi, Alain Pierre, Stephane Leonce
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Patent number: 5218112Abstract: Compounds containing carbohydrate moieties or carboxyl groups are linked to either compounds containing thiol moieties or electron-deficient moieties by the use of linking agents of the formula ##STR1## in which R.sup.1 is NH.sub.2 -- or NH.sub.2 --NH--; R.sup.2 is --NH--C(O)--, --C(O)--NH--, or --C(O)--; R.sup.3 is C.sub.1 -C.sub.10 alkylene, C.sub.5 -C.sub.7 cyclic alkylene, arylene, phenyl-substituted C.sub.1 -C.sub.10 alkylene, benzyl-substituted C.sub.1 -C.sub.10 alkylene, or amino-substituted C.sub.1 -C.sub.10 alkylene; R.sup.4 is H, acetyl, ##STR2## where R.sup.5 is C.sub.1 -C.sub.5 alkyl; m is zero or 1; and n ia zero or 1.Type: GrantFiled: August 27, 1990Date of Patent: June 8, 1993Assignee: Xoma CorporationInventors: Dayton T. Reardan, Dane A. Goff
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Patent number: 5208330Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl, or oxygen-bridged diaryllowerallyl; A is a direct bond or (CHR.sub.3).sub.m, m being 1-3; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl; Y is O, S or NR.sub.7 ; and each R.sub.2, each R.sub.3 and R.sub.Type: GrantFiled: February 25, 1992Date of Patent: May 4, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Gregory M. Shutske, Richard C. Effland
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Patent number: 5087696Abstract: A conjugate compound has the structure (I), wherein R.sup.1 is --(CH.sub.2).sub.p --R.sup.6 --(CH.sub.2).sub.q -- where p and q are the same or different and are 0, 1 or 2, and --R.sup.6 -- is --(CH.sub.2).sub.n --, where n is 0 or 1, --NH--, --O--, --S-- or (II), R.sup.1 optionally being alkyl substituted, provided that neither p nor q is 0 unless R.sup.6 is --CH.sub.2 --; R.sup.2 are --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 --, optionally alkyl, alkoxyalkyl or hydroxyalkyl substituted; R.sup.3 are the same or different and are --H, alkyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl, carboxyalkyl ester, phosphate, sulphonate or phosphonate; R.sup.4 is one of the compounds of formula (III) optionally alkyl substituted, wherein R.sup.7 is --H, alkyl, hydroxyalkyl, or alkoxyalkyl provided that when R.sup.4 is (III d), R.sup.3 is not carboxyalkyl, R.sup.5 is a linker, and Ab is an antibody.Type: GrantFiled: December 14, 1987Date of Patent: February 11, 1992Assignee: Celltech LimitedInventors: David Parker, Thomas A. Millican
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Patent number: 5081197Abstract: This invention provides novel azlactone-functional oligomers of 2-alkenyl azlactones in which oligomerization has occurred predominantly via the 2-alkenyl group. Oligomerization of the 2-alkenyl group provides oligomers having 2 to 15 mer units with predominantly carbon-carbon backbone segments. Oligomerized in this fashion, the novel compositions possess azlactone groups which can be reacted with nucleophiles in the normal ring-opening sense. The oligomers are prepared by a novel process in which both Lewis and Bronsted acidic catalysts are effective. The reactive oligomers find utility as crosslinking agents for polymers containing azlactone-reactable nucleophilic groups.Type: GrantFiled: October 23, 1990Date of Patent: January 14, 1992Assignee: Minnesota Mining and Manufacturing CompanyInventors: Steven M. Heilmann, Dean M. Moren, Jerald K. Rasmussen, Larry R. Krepski, Sadanand V. Pathre
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Patent number: 5070086Abstract: Imidazo- and pyrimido-quinoline, naphthyridine and pyridopyrazine compounds, methods of making said compounds and their use as anti-allergy, antiinflammatory and/or agents for the treatment of hyperproliferative skin disease are disclosed.Type: GrantFiled: June 15, 1990Date of Patent: December 3, 1991Assignee: Schering CorporationInventor: Richard Friary
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Patent number: 5068324Abstract: The present invention deals with novel amphoteric polymers and their application as softening, anti-tangle, and conditioning agents. The properties of these novel compositions which make them well suited for these applications is their substantivity to fibers, hair and skin and that they are very mild to the skin and eyes. The subject compositions are prepared by the polymerization of amphoteric monomers compounds with epichlorohydrin. The amphoteric monomer compounds are prepared by the reaction of commercially available multifunctional amines with an alpha beta unsaturated acid.Type: GrantFiled: September 5, 1989Date of Patent: November 26, 1991Assignee: LCE PartnershipInventor: Anthony J. O'Lenick, Jr.
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Patent number: 5066800Abstract: A novel process and intermediates used therein for linking a cephalosporin compound to a quinolone are disclosed. According to the disclosed process, the 2-carboxylic acid moiety of the cephalosporin compound is treated with an organic base. The resulting salt is then reacted with a quinolone compound which has been activated using a haloformate. The reaction is run in a non-aqueous organic solvent. 4-Dimethylaminopyridine is used to promote the reaction between the cephalosporin salt and the activated quinolone.Type: GrantFiled: April 27, 1990Date of Patent: November 19, 1991Assignee: Hoffmann-La Roche Inc.Inventor: Masami Okabe
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Patent number: 5011860Abstract: Aryl-substituted naphthyridines and pyridopyrazines are disclosed which are useful in treating allergic reactions, inflammation, peptic ulcers and/or hyperproliferative skin disease. Pharmaceutical compositions and methods of treatment employing such compounds are also disclosed.Type: GrantFiled: June 26, 1989Date of Patent: April 30, 1991Assignee: Schering CorporationInventors: David J. Blythin, Ho-Jane Shue
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Patent number: 4987227Abstract: A 13 or 14 member macrocyclic compound having the following ring nucleus: ##STR1##This work was supported by grants from the National Institutes of Health (GM-34841) and the National Science Foundation (CHE-8706616).Type: GrantFiled: February 23, 1990Date of Patent: January 22, 1991Assignee: The Research Foundation of State University of New YorkInventors: Cynthia Burrows, Heungsik Yoon, Thomas R. Wagler
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Patent number: 4970303Abstract: Compounds containing carbohydrate moieties or carboxyl groups are linked to either compounds containing thiol moieties or electron-deficient moieties by the use of linking agents of the formula ##STR1## in which R.sup.1 is NH.sub.2 -- or NH.sub.2 --NH--; R.sup.2 is --NH--C(O)--, --C(O)--NH--, or --C(O)--; R.sup.3 is C.sub.1 -C.sub.10 alkylene, C.sub.5 -C.sub.7 cyclic alkylene, arylene, phenyl-substituted C.sub.1 -C.sub.10 alkylene, benzyl-substituted C.sub.1 -C.sub.10 alkylene, or amino-substituted C.sub.1 -C.sub.10 alkylene; R.sup.4 is H, acetyl, ##STR2## where R.sup.5 is C.sub.1 -C.sub.5 alkyl; m is zero or 1; and n is zero or 1.Type: GrantFiled: February 3, 1988Date of Patent: November 13, 1990Assignee: Xoma CorporationInventors: Dayton T. Reardan, Dane A. Goff
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Patent number: 4962113Abstract: Novel pyridinium derivatives represented by the formula (I): ##STR1## wherein ##STR2## is an optionally substituted pyridinium ring; R.sup.1 is a lower alkyl group or aralkyl group;R.sup.7 and R.sup.10 are independently hydrogen, a lower alkyl group, aryl group or aralkyl group;l is 0 or 1;R.sup.5 is a phenylene group or an alkylene group which may be substituted;R.sup.11 is an alkyl group or aryl group;X is a group of the formula: --CH.sub.2 OCH.sub.2 -- or a group of the formula: ##STR3## wherein R.sup.6 is hydrogen, a lower alkyl or a lower alkoxy, and m is an integer of 0 to 3;U is a group of the formula: ##STR4## wherein R.sup.Type: GrantFiled: July 26, 1988Date of Patent: October 9, 1990Assignee: Takeda Chemical Industries, LtdInventors: Susumu Tsushima, Muneo Takatani, Kohei Nishikawa
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Patent number: 4880923Abstract: There are disclosed macrocyclic and polycyclic polyamine lubricating oil additives formed by cyclodehydration of reaction products of hydrocarbon substituted succinic anhydrides or carboxylic acids with poly 3-amino propyl compounds or by acylation of macrocyclic polyamines and polycyclic polyamines with hydrocarbon substituted succinic anhydride or carboxylic acids. These compounds are useful as dispersants and dispersants-V.I. improvers in both gasoline and diesel engine lubricating oil compositions and are also useful fuel additives.Type: GrantFiled: September 2, 1986Date of Patent: November 14, 1989Assignee: Exxon Research & Engineering CompanyInventors: Stanley J. Brois, Antonio Gutierrez
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Patent number: 4694003Abstract: A method of treating depression with 5-(aminoalkyl)-11-phenyl-5H-dibenzo[b,e][1,4]diazepines having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are selected from hydrogen or methyl and X is selected from hydrogen, chlorine, bromine or fluorine is disclosed.Type: GrantFiled: July 30, 1982Date of Patent: September 15, 1987Assignee: A. H. Robins Company, IncorporatedInventor: Chandler R. Taylor, Jr.