The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 546/235)
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Patent number: 6545022Abstract: Novel amines of formulas 1D and 1E are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed.Type: GrantFiled: April 7, 2000Date of Patent: April 8, 2003Assignee: Pfizer Inc.Inventors: Justin Stephen Bryans, David Christopher Horwell, Clare Octavia Kneen, David Juergen Wustrow
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Publication number: 20030028029Abstract: The present invention relates to a process for preparing piperidine derivative compounds of the formulae: 1Type: ApplicationFiled: August 5, 2002Publication date: February 6, 2003Inventors: Thomas E. D'Ambra, Garry M. Pilling
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Publication number: 20020193601Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas 1Type: ApplicationFiled: June 3, 2002Publication date: December 19, 2002Inventors: Daniel R. Henton, Frederick J. McCarty, Susan I. Tripp, Jill E. DeWitt
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Patent number: 6492400Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: December 17, 1999Date of Patent: December 10, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker, Ui Tae Kim
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Patent number: 6476228Abstract: A process for producing a piperidinecarbinol represented by the general formula (2), which comprises reducing the trans isomer of a compound represented by the general formula (1): wherein R1 is a hydrogen atom, a lower alkyl group or an aralkyl group, R2 is a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, and X is a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, a dialkylamino group, an alkylthio group, an arylthio group or CmF2m+1— wherein m is an integer of from 1 to 20.Type: GrantFiled: September 20, 2000Date of Patent: November 5, 2002Assignee: Asahi Glass Company Ltd.Inventors: Shu-zhong Wang, Takashi Okazoe, Yasushi Matsumura, Nobuaki Mori, Jiro Nishino, Kazuhiro Ookura
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Publication number: 20020099216Abstract: There is provided a compound of formula I, 1Type: ApplicationFiled: March 27, 2002Publication date: July 25, 2002Applicant: Pfizer Inc.Inventors: Stephen Paul Gibson, Ivan Tommasini, David Morris Gethin, Richard Edward Armer
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Publication number: 20020099077Abstract: This invention relates to novel compounds of formula: 1Type: ApplicationFiled: March 22, 2002Publication date: July 25, 2002Inventor: Timothy A. Ayers
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Patent number: 6420561Abstract: An amide compound of the formula (I): wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-&agr;, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.Type: GrantFiled: November 17, 2000Date of Patent: July 16, 2002Assignee: Japan Tobacco Inc.Inventors: Junichi Haruta, Kazuhiko Sakuma, Yoshihiro Watanabe
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Publication number: 20020040146Abstract: The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.Type: ApplicationFiled: July 17, 2001Publication date: April 4, 2002Inventors: Johannes Aebi, Daniel Bur, Alexander Chucholowski, Henrietta Dehmlow, Eric Argirios Kitas, Ulrike Obst, Hans Peter Wessel
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Patent number: 6358979Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R3, R4, R5, R6, R7, R8, X, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.Type: GrantFiled: June 8, 2000Date of Patent: March 19, 2002Assignee: Merck & Co., Inc.Inventors: Paul E. Finke, Kerry A. Hilfiker, Malcolm MacCoss, Kevin T. Chapman, Jennifer L. Loebach, Sander G. Mills, Ravi N. Guthikonda, Shrenik K. Shah, Dooseop Kim, Dong-Ming Shen, Bryan Oates
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Publication number: 20020028833Abstract: Aryl alkenamides derivatives of Formula I or a pharmaceutically acceptable salt thereof are novel MCP-1 antagonists and are thus useful in the treatment of inflammation, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection 1Type: ApplicationFiled: August 12, 1997Publication date: March 7, 2002Inventors: RICHARD JOHN BOOTH, KENNETH GORDON CARSON, DAVID THOMAS CONNOR, ROBERTA ELLEN GLYNN, BRUCE DAVID ROTH, CHARLES F. SCHWENDER, BHARAT KALIDAS TRIVEDI, PAUL CHARLES UNANGST
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Patent number: 6342509Abstract: This invention relates to certain piperidine quatemrwy salts of Formula (I): that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: November 18, 1999Date of Patent: January 29, 2002Assignee: Syntex (U.S.A.) LLCInventors: Donald Roy Hirschfeld, Denis John Kertesz, David Berard Smith
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Patent number: 6329399Abstract: Novel amine derivatives having an excellent antimycotic effect represented by general formula (1) below and salts thereof are provided. [in the formula (1, R1 represents a C1-5 alkyl group which may be halogenated, R2 represents 4-(1,1-dimethylalkyl)benzyl group, 4-(1-methyl-phenylethyl)benzyl group, 1-or 2-naphthylmethyl group, or a hydrocarbon group having 3,3-dimethyl-1-butynyl group or a phenyl group at its terminal and 1 to 3 double bonds; R3 represents oxygen atom or a methylene group which may be substituted by a C1-4 alkyl group; and R4 represents 1-or 2 naphthyl group or a phenyl group which may be substituted.Type: GrantFiled: May 18, 2000Date of Patent: December 11, 2001Assignee: Pola Chemical Industries, Inc.Inventors: Takao Itoh, Takuji Nakashima, Akira Nozawa, Kouji Yokoyama, Hiroyuki Takimoto, Masayuki Yuasa, Yukio Kawazu, Toshimitsu Suzuki, Toshiro Majima
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Patent number: 6303637Abstract: The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.Type: GrantFiled: October 21, 1999Date of Patent: October 16, 2001Assignee: Merck & Co., Inc.Inventors: Jianming Bao, Andrew Kotliar, Frank Kayser, William H. Parsons, Kathleen M. Rupprecht, Christopher F. Claiborne, David A. Claremon, Nigel Liverton, Wayne J. Thompson
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Patent number: 6291478Abstract: The present application relates to novel compounds belonging to the benzylaminodiacetamide family which have good anti-irritant and soothing properties. The invention also relates to their use in a composition comprising a physiologically acceptable medium, in particular in order to prevent and/or treat certain cutaneous disorders and more particularly in order to treat sensitive skins.Type: GrantFiled: March 13, 2000Date of Patent: September 18, 2001Assignee: L'OrealInventors: Jean-Baptiste Galey, Maria Dalko
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Patent number: 6291481Abstract: Compounds of formula I the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the substituents are as described in the specification, and process for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.Type: GrantFiled: August 27, 1998Date of Patent: September 18, 2001Assignee: Janssen Pharmaceutica, N.V.Inventors: Jean-Paul René Marie Bosmans, Christopher John Love, Marc Gustaaf Celine Verdonck, Joannes Adrianus Jacobus Schuurkes
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Publication number: 20010014741Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas 1Type: ApplicationFiled: March 9, 2001Publication date: August 16, 2001Inventors: Daniel R. Henton, Frederick J. McCarty, Susan I. Tripp, Jill E. DeWitt
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Patent number: 6255301Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Rx, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required as in thrombosis or as anticoagulants.Type: GrantFiled: July 14, 1997Date of Patent: July 3, 2001Assignee: AstraZeneca ABInventors: David Gustafsson, Jan-Erik Nyström
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Patent number: 6166013Abstract: Compounds having Formula I ##STR1## are useful for modulating the glucocorticoid receptor in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of treating immune, autoimmune, inflammatory, adrenal imbalance, cognitive and behavioral diseases in a mammal.Type: GrantFiled: July 30, 1999Date of Patent: December 26, 2000Assignee: Abbott LaboratoriesInventors: Michael J. Coghlan, Jay R. Luly, Jeffrey M. Schkeryantz, Alan X. Wang
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Patent number: 6130220Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: August 5, 1999Date of Patent: October 10, 2000Assignees: Syntex (USA) Inc., Agouron Pharmaceuticals, Inc.Inventors: Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Jian Jeffrey Chen, Robert Than Hendricks, Michael Joseph Melnick, Keith Adrian Murray Walker
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Patent number: 6063816Abstract: A compound selected from those of formula (I): ##STR1## wherein: R.sub.1 represents optionally substituted alkyl, acyl, cycloalkyl, aryl, aminocarbonylalkyl, or heterocycle,R.sub.2 represents alkylene,R.sub.3 represents X or Y as defined in the description,R.sub.4 represents--either alkyl, cycloalkyl, aryl, arylalkyl, cycloalkylalkyl, heterocycloalkylene, or heterocycle when R.sub.3 represents Y,or biaryl, arylheteroaryl or heteroarylaryl, when R.sub.3 represents X or Y,their isomers and also pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful as metalloprotease inhibitors in the treatment of cancers.Type: GrantFiled: August 9, 1999Date of Patent: May 16, 2000Assignee: Adir et CompagnieInventors: Stephen Hanessian, Ghanem Atassi, Gordon Tucker, Daniel-Henri Caignard, Pierre Renard
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Patent number: 6008220Abstract: Aromatic keto-acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, arthrities, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.Type: GrantFiled: June 8, 1998Date of Patent: December 28, 1999Assignee: Warner Lambert CompanyInventors: Donald Hupe, Linda Lea Johnson, Daniel Fred Ortwine, Claude Forsey Purchase, Jr., Andrew David White, Qi-Zhuang Ye
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Patent number: 6002009Abstract: Pharmacologically active novel esters and amides of di-substituted 1,4 piperidine as 5-HT.sub.4 antagonists of formula (I) ##STR1## wherein A, X, Y and R have the meanings specified in the description, and a process for their preparation, are disclosed.Type: GrantFiled: January 14, 1998Date of Patent: December 14, 1999Assignee: Boehringer Ingelheim Italia, S.p.A.Inventors: Enzo Cereda, Maura Bignotti, Vincenzo Martino, Giovanni Battista Schiavi, Angelo Sagrada
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Patent number: 5998412Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: January 21, 1998Date of Patent: December 7, 1999Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.Inventors: Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Jian Jeffrey Chen, Robert Than Hendricks, Michael Joseph Melnick, Keith Adrian Murray Walker
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Patent number: 5977141Abstract: Sulfonamide compounds are described which are inhibitors of matrix metalloproteinases, particularly stromelysin-1 and gelatinase A (72 kD gelatinase). Also described are methods for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes using the compounds.Type: GrantFiled: May 13, 1998Date of Patent: November 2, 1999Assignee: Warner-Lambert CompanyInventors: Daniel F. Ortwine, Claude F. Purchase, Jr., Andrew D. White
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Patent number: 5962690Abstract: 1-Alkyl-4-benzoyl-5-hydroxy-1H-pyrazole compounds in which the benzoyl moiety is substituted in the 2-position with groups such as halo or alkyl, in the 4-position with an alkylsulfonyl group, and in the 3-position with an acyclic or cyclic derivatized amino group, such as 1-ethyl-4-(2-chloro-4-methylsulfonyl-3-(morpholin-4-yl)benzoyl-5-hydroxy-1 H-pyrazole, were prepared and found to be useful for the control of a variety of broadleaf and grassy weeds. The compounds can be applied either preemergently or postemergently and can be used to control undesirable vegetation in corn, rice, and wheat crops.Type: GrantFiled: July 24, 1998Date of Patent: October 5, 1999Assignee: Dow AgroSciences LLCInventors: Zoltan L. Benko, James A. Turner, Gail M. Garvin, Johnny L. Jackson, Sharon L. Shinkle
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Patent number: 5939438Abstract: It has now been found that certain novel oximino and hydrazono derivatives of N-benzyl-4-benzhydryl- and 4-benhydrolpiperidines, and their corresponding N-oxides and agriculturally acceptable salts are useful as insecticides. These compounds are represented by Formula I: where R is hydrogen, halogen, alkyl, alkoxy, dialkylamino; R.sup.1 is hydrogen, alkyl, haloalkyl, alkoxyalkyl, alkylcarbonyl and alkylaminocarbonyl; X is oxygen, or NR.sup.2, Q is fluoro and hydroxy; Z is halogen, haloalkyl, haloalkoxy, pentahalothio, haloalkylthio, haloalkylsulfinyl, haloalkylsulfonyl, and --OCF.sub.2 O-- attached to two adjacent carbon atoms of the phenyl ring; n is 0 or 1; and, when X is NR.sup.2, R.sup.2 is hydrogen, alkyl, alkylcarbonyl, alkoxycarbonyl, or R.sup.1 and R.sup.2 taken together may be --C.sub.m H.sub.2.spsb.m, or --C.sub.2 H.sub.4 OC.sub.2 H.sub.4 --, where m is 3-9. Preferred compounds include those where R is hydrogen; R.sup.Type: GrantFiled: September 9, 1998Date of Patent: August 17, 1999Assignee: FMC CorporationInventors: Walter H. Yeager, Ian R. Silverman, Robert N. Henrie, II, Thomas G. Cullen, Clinton J. Peake
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Patent number: 5935585Abstract: Novel pharmaceutically/cosmetically-active biaromatic amido compounds have the structural formula (I): ##STR1## in which Ar is a radical selected from among those of the following formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: February 23, 1996Date of Patent: August 10, 1999Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, Laurence Vigne
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Patent number: 5932595Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.Type: GrantFiled: December 18, 1996Date of Patent: August 3, 1999Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.Inventors: Steven Lee Bender, Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Lawrence Emerson Fisher, Robert Than Hendricks, Keshab Sarma
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Patent number: 5929088Abstract: Novel cyclic amino acids of formula (Ia) or (Ib) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders.Type: GrantFiled: May 18, 1998Date of Patent: July 27, 1999Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Justin S. Bryans, Clare O. Kneen, Giles Ratcliffe
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Patent number: 5863903Abstract: The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.Type: GrantFiled: March 14, 1995Date of Patent: January 26, 1999Assignee: Novo Nordisk A/SInventors: Karsten Lundgren, Ole Kirk
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Patent number: 5859249Abstract: Disclosed is a 2-phenyl-2-(2'-piperidinylidene)acetate derivative suitably used for a raw material of a 2-phenyl-2-(2'-piperidinyl)acetate derivative and a process for manufacturing the same. Also disclosed is a process for manufacturing an optically active 2-phenyl-2-(2'-piperidinyl)acetate derivative which is a major intermediate for an antidepressant. The 2-phenyl-2-(2'-piperidinylidene)acetate derivative is manufactured by cyclizing a 7-(N-substituted amino)-3-oxo-2-heptanoate derivative. The optically active 2-phenyl-2-(2'-piperidinyl)acetate derivative is manufactured by asymmetrically hydrogenating the 2-phenyl-2-(2'-piperidinylidene)acetate derivative in the presence of a complex of a Group VIII transition metal or an acid.Type: GrantFiled: July 16, 1997Date of Patent: January 12, 1999Assignee: Takasago International CorporationInventors: Nobuo Seido, Takenobu Nishikawa, Tsukasa Sotoguchi, Yoshifumi Yuasa, Takashi Miura, Hidenori Kumobayashi
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Patent number: 5831114Abstract: Substituted N-phenyl- and N-heteroarylalkylcarbamates of formula (I), in which Q is a group (1), (2) or (3); R is halogen, trifluoromethyl, cyano, nitro or C.sub.1 -C.sub.3 haloalkoxy; Z is hydrogen or halogen; or Z and R together in the 2- and 3-position of the phenyl ring form a group --OCF.sub.2 O--; R.sub.1 is C.sub.1 -C.sub.5 alkyl; R.sub.2, R.sub.3, R.sub.4 and R.sub.5, independently of one another, are hydrogen, methyl or ethyl; X is oxygen, sulfur, --SO-- or --SO.sub.2 --, Y is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy or cyano; n is 0, 1 or 2; n.sub.1 is 0 or 1; and m is 0 or 1, with the proviso that m is 1 if Q is group (1) or (2); and the diastereomers and enantiomers thereof, exhibit pre- and post-emergence herbicidal properties. The preparation of these compounds and their use as herbicidally active ingredients are described.Type: GrantFiled: May 28, 1997Date of Patent: November 3, 1998Assignee: Novartis Finance CorporationInventors: Hermann Rempfler, Fredrik Cederbaum, Felix Spindler, Willy Urs Lottenbach
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Patent number: 5780480Abstract: Fibrinogen receptor antagonists of the general formula:X-A-Y-Z-B Iand which includes, for example, the compounds of formula ##STR1## are useful for inhibiting the binding of fibrinogen to blood platelets, inhibiting the aggregation of blood platelets, treating thrombus formation or embolus formation, and preventing thrombus or embolus formation.Type: GrantFiled: February 26, 1997Date of Patent: July 14, 1998Assignee: Merck & Co., Inc.Inventors: John Wai, Thorsten E. Fisher, Mark E. Duggan, George D. Hartman, James J. Perkins
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Patent number: 5773620Abstract: Amine compounds of the formula (Ia): ##STR1## where m, Ar', N, T and Z are defined herein and J is a group ##STR2## are useful as precursors in the production of quaternary amines and for the treatment of pathological phenomena involving the neurokin system.Type: GrantFiled: June 7, 1995Date of Patent: June 30, 1998Assignee: Elf SanofiInventors: Xavier Emonds-Alt, Vincenzo Proietto, Didier Van Broeck, Jean-Claude Breliere
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Patent number: 5763458Abstract: The present invention relates to novel 5-HT.sub.4 receptor ligands which are 1-(5-halo-4-aminophenyl) (C.sub.2-6)alkan-1-one derivatives in which the 5-halo-4-aminophenyl group is substituted at its 2-position with (C.sub.1-4)alkyloxy or phenyl(C.sub.1-4)alkyloxy and optionally substituted at its 3-position with (C.sub.1-4)alkyloxy or substituted at its 2- and 3-positions together with methylenedioxy or ethylenedioxy and the highest numbered carbon of the (C.sub.2-6)alkan-1-one is substituted with di(C.sub.1-4)alkylamino, morpholin-1-yl or pyrrolidin-1-yl or optionally substituted piperidin-1-yl, piperidin-4-yl, azacyclohept-1-yl, azabicyclo?2.2.1!hept-3-yl, azabicylo?2.2.2!oct-3-yl or azabicylo?3.2.2!non-3-yl; and the pharmaceutically acceptable salts, individual isomers and mixtures of isomers and methods of using and making such derivatives.Type: GrantFiled: May 31, 1995Date of Patent: June 9, 1998Assignee: Syntex (U.S.A.) Inc.Inventors: Robin Douglas Clark, Richard Malcolm Eglen, John Otis Gardner, Alam Jahangir, Aaron Bayne Miller
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Patent number: 5646144Abstract: 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalized carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.Type: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: Ciba-Geigy CorporationInventors: Walter Schilling, Silvio Ofner, Siem J. Veenstra
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Patent number: 5618825Abstract: Combinatorial libraries are disclosed which are represented by Formula I:(T'--L).sub.q -- S--C(O)--L'--II' Iwherein:S is a solid support; T'--L-- is an identifier residue; and --L'--II' is a ligand/linker residue. Compounds which contain aryl sulfonamides, N-acyl derivatives, and N-substituted pyrrolidines and piperidines of the formula :Y--A--CO--R.sup.1are inhibitors of serine proteases and carbonic anhydrase isozymes. They are useful in the treatment of hyper-coagulation disease and ocular diseases such as glaucoma.Type: GrantFiled: June 7, 1995Date of Patent: April 8, 1997Assignee: Pharmacopeia, Inc.Inventors: John J. Baldwin, Michael H. J. Ohlmeyer, Ian Henderson
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Patent number: 5596098Abstract: Aminoquinones and their use as additives in fluid media for providing corrosion resistance to metals in contact with the fluid medium and their use in preparing copolymers to provide corrosion resistant binder compositions for magnetic information storage media, the copolymers formed, the magnetic information storage media and a method for improving corrosion resistance in magnetic particles are provided.Type: GrantFiled: July 30, 1993Date of Patent: January 21, 1997Assignee: University of AlabamaInventors: David E. Nikles, Jeng-Li Liang
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Patent number: 5563168Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: June 16, 1995Date of Patent: October 8, 1996Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 5541201Abstract: The invention is directed to a new class of antiarrhythmic agents of the formula: ##STR1## in which R is represented by hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, CF.sub.3, SR.sub.1, NHC(O)R.sub.2, NH.sub.2, or OH; R.sub.1 is hydrogen or C.sub.1-4 alkyl; R.sub.2 is C.sub.1-4 alkyl; X is represented by CO or CHOH; R.sub.3 and R.sub.4 are each independently represented by methyl, ethyl, n-propyl, or R.sub.3 and R.sub.4 together with the carbon atom to which they each are attached form a C.sub.5 or C.sub.6 cycloalkyl; and Alk is a C.sub.1-4 alkyl; or a pharmaceutically acceptable addition salt thereof.Type: GrantFiled: June 2, 1995Date of Patent: July 30, 1996Assignee: Merrell Pharmaceuticals, Inc.Inventors: Albert A. Carr, Richard C. Dage, David A. Hay, John E. Koerner, Tung Li
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Patent number: 5532232Abstract: Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.Type: GrantFiled: November 22, 1994Date of Patent: July 2, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Paul Hadvary, Kurt Hilpert, Klaus Muller, Ludvik Labler, Gerard Schmid, Thomas B. Tschopp, Hans P. Wessel, Beat Wirz
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Patent number: 5506227Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: April 13, 1992Date of Patent: April 9, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
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Patent number: 5478846Abstract: The present invention is direct to a new class of 1-piperidinyl alkanoarylsulfonamides of the formula I ##STR1## wherein R, X, m, n, and Alk are defined in the specification, and their use as antiarrhythmic agents.Type: GrantFiled: July 22, 1994Date of Patent: December 26, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Albert A. Carr, Richard C. Dage, Thaddeus R. Nieduzak, John E. Koerner, Tung Li
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Patent number: 5457122Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: July 13, 1993Date of Patent: October 10, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5416117Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: February 28, 1994Date of Patent: May 16, 1995Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5401775Abstract: This invention relates to a tri(lower alkoxy)benzene derivative of the general formula (I), or its salt, optical isomer or solvate, ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 : same or different and each represents a lower alkyl group;A: a group of the formula ##STR2## and R.sup.4 and R.sup.5 : same or different and each represents a lower alkyl group, an aralkyl group or an aryl group, provided that R.sup.4 and R.sup.5 may, taken together with the adjacent nitrogen atom, form a pyrrolidinyl group, a piperidino group, a morpholino group, a thiomorpholino group, or a piperazinyl group optionally substituted by a lower alkyl group in 4-position;to pharmaceutical compositions containing the same, and to processes for their production. The compound of the invention is useful as value as a pulmonary-surfactant secretion promoting agent.Type: GrantFiled: December 22, 1993Date of Patent: March 28, 1995Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Hiromu Hara, Tatsuya Maruyama, Munetoshi Saito, Toshiyasu Mase
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Patent number: 5397791Abstract: Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2##Type: GrantFiled: August 9, 1993Date of Patent: March 14, 1995Assignee: Merck & Co., Inc.Inventors: George D. Hartman, John D. Prugh, Wasyl Halczenko, Melissa Egbertson, Nathan Ihle
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Patent number: 5374724Abstract: A process for the preparation of a substituted acetic acid of the Formula (2): ##STR1## wherein --X--Z is an optionally substituted aromatic or heteroaromatic optionally substituted amino radical; by reacting a compound of the Formula (7):Z--Y--H Formula 7with glyoxylic acid. The compounds of Formula (2) are useful as intermediates in the preparation of polycyclic dyes.Type: GrantFiled: November 2, 1992Date of Patent: December 20, 1994Assignee: Zeneca, LimitedInventors: Nigel Hall, Nigel Hughes, Prakash Patel
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Patent number: 5328909Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: June 25, 1992Date of Patent: July 12, 1994Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe