Z Radical Contains Two Or More Nitrogen Atoms At Least One Of Which Forms A C(=x)n Group (x Is Chalcogen) Patents (Class 514/542)
-
Patent number: 6515024Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: December 11, 2001Date of Patent: February 4, 2003Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
-
Patent number: 6492421Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: July 30, 1998Date of Patent: December 10, 2002Assignees: Athena Neurosciences, Inc., American Home Products Corp.Inventors: Eugene D. Thorsett, Christopher M. Semko, Dimitrios Sarantakis, Michael A. Pleiss, Louis John Lombardo, Anthony Kreft, Andrei W. Konradi, Francine S. Grant, Darren B. Dressen, Michael S. Dappen, Reinhardt Bernhard Baudy, Susan Ashwell
-
Patent number: 6486202Abstract: Provided are novel peptidomimetic isoprenyl transferase inhibitors, methods for synthesizing such inhibitors, and methods for the use of such inhibitors for the treatment of tumors.Type: GrantFiled: April 13, 2001Date of Patent: November 26, 2002Assignee: Eisai Company, LimitedInventors: Ana Maria Garcia, James Kowalczyk, Michael D. Lewis
-
Patent number: 6472393Abstract: Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5 and R6 are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.Type: GrantFiled: March 21, 2000Date of Patent: October 29, 2002Assignee: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, Dean R. Artis, Michael S. Dina, John A. Flygare, Richard A. Goldsmith, Regina A. Munroe, Alan G. Olivero, Richard Pastor, Thomas E. Rawson, Kirk D. Robarge, Daniel P. Sutherlin, Kenneth J. Weese, Aihe Zhou, Yan Zhu
-
Patent number: 6472430Abstract: Antiatherosclerotic compounds are provided which have the following structure: wherein R is lower alkyl; R1 is hydroxy, amino, or lower alkoxy, R2 and R3 are each independently hydrogen, alkyl or aryl; Ar is phenyl, indanyl, benzhydryl, or phenyl substituted with one or more member selected from the group consisting of halogen, lower alkyl, perfluoroalkyl, lower alkoxy, perfluoroalkylalkoxy, dialkylamino, and aryloxy; or pharmaceutically acceptable salts thereof.Type: GrantFiled: September 28, 2001Date of Patent: October 29, 2002Inventors: Hassan M. Elokdah, Theodore S. Sulkowski
-
Patent number: 6403644Abstract: The present invention is related to: (i) matrix metalloproteinase inhibitors containing sulfonylamino acid derivatives of the formula (Ia); wherein R1 is hydrogen, C1-4 alkyl; R2 is hydrogen, C1-8 alkyl etc.; E is —CONR3—, in which R3 is hydrogen, C1-4 alkyl etc., —NR3CO—, —CO—O—, —O—CO— etc.; A is hydrogen, C1-8 alkyl, C3-7 cycloalkyl, or Ar; J is bond, C2-4 alkylene etc.; G is — (CH2)m—, in which m is 2, 3 or 4, or in which R6 and R7 is hydrogen, C1-8 alkyl etc.; and non-toxic salts thereof, (ii) sulfonylamino acid derivatives of the formula (Ib): wherein all the symbols are the same meaning as (i); and non-toxic salts thereof, and (iii) process for the preparation of the compound of the formula (Ib). The compounds of the formula (Ia) are useful for prevention and/or treatment of diseases induced by overexpression and excess activity of MMP.Type: GrantFiled: November 13, 2000Date of Patent: June 11, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Katsuhito Sakaki, Hidekazu Kanazawa, Tsuneyuki Sugiura, Tohru Miyazaki, Hiroyukii Ohno
-
Patent number: 6391917Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.Type: GrantFiled: April 19, 2001Date of Patent: May 21, 2002Assignee: ZymoGenetics, Inc.Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
-
Patent number: 6391918Abstract: Novel &agr;-amino acid amides of formula (I) as well as possible isomers and mixtures of isomers thereof, wherein the substituents are defined as follows: n is the number zero or one; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl; or a group NRaRb wherein Ra and Rb are each independently of the other hydrogen, alkyl or form together an alkylene bridge; R2 is hydrogen or alkyl; R3 is optionally substituted aryl or heteroaryl; A is alkylene; and B is optionally substituted aryl; with the exception of the following compounds 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methylphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-chlorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-nitrolphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methoxyphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-fluorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-phenyl-sulfonylamino-acetamide and 2-phenyl-N-(1-pType: GrantFiled: August 25, 2000Date of Patent: May 21, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: André Jeanguenat, Martin Zeller
-
Patent number: 6384076Abstract: It has now been found that N-L-alpha-aspartyl-L-phenylalanine 1-methyl ester (APM) exhibits antisickling properties. In vitro testing verified that APM significantly lowered the frequency of sickling of red blood cells from each of twelve pediatric aged patients being treated for sickle-cell anemia by exchange transfusion. Sickling was also inhibited in an “index” patient after oral administering of APM. These in vitro and in vivo results identify APM as a therapeutic agent for the family of sickle cell molecular diseases.Type: GrantFiled: March 22, 2001Date of Patent: May 7, 2002Assignee: Oklahoma Medical Research FoundationInventors: Carl V. Manion, Allen B. Edmundson
-
Patent number: 6313119Abstract: Sulfonamide derivatives, their physiologically tolerable salts and their prodrugs according to the present invention are vitronectin receptor antagonists and inhibitors of cell adhesion, as well as inhibit bone resorption by osteoclasts. These derivatives, salts and prodrugs are pharmaceutically active compounds useful in the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. Processes for the preparation of the sulfonamide derivatives according to the present invention, the use of these derivatives as pharmaceutically active ingredients, and pharmaceutical preparations comprising these derivatives also are disclosed.Type: GrantFiled: May 5, 2000Date of Patent: November 6, 2001Assignees: Adventis Pharma Deutschland GmbH, Genentech, Inc.Inventors: Anuschirwan Peyman, David William Will, Jochen Knolle, Karlheinz Scheunemann, Denis Carniato, Jean-Francois Gourvest, Thomas R. Gadek, Robert McDowell, Sarah Catherine Bodary, Robert Andrew Cuthbertson
-
Patent number: 6306881Abstract: Compounds of general formula (I) wherein R4 is an ester or thioester group and R, R1, R2, and R3 are as specified in the description, inhibit intracellular Leukotriene A4 hydrolase activity and are therefore of value for the treatment of inflammatory disease.Type: GrantFiled: July 21, 1999Date of Patent: October 23, 2001Assignee: British Biotech PharmaceuticalsInventors: Andrew Paul Ayscough, Mark Whittaker
-
Patent number: 6221913Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.Type: GrantFiled: January 20, 1999Date of Patent: April 24, 2001Assignee: ZymoGenetics, Inc.Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
-
Patent number: 6211176Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: July 1, 1999Date of Patent: April 3, 2001Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
-
Patent number: 6194463Abstract: &agr;-Amino acid amides of formula (I) wherein the substituents are defined as follows: n is a number zero or one; R1 to R7 are as defined herein; R8 is C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl; R9 is C3-C8cycloalkyl; a C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl group substituted by one or more halogen atoms; or a group (a) wherein p and q are identical or different and are each independently of the other a number zero or one; and R13, R14, R15 and R16 are identical or different and are each independently of the others hydrogen or C1-C4alkyl; X is hydrogen, in which case p and q must have the value zero; phenyl, unsubstituted or mono- or poly-substituted by halogen, nitro, cyano, carboxy, C2-C6alkenyl, C2-C6alkenyl, C1-C6haloalkyl, C3-C6alkenyloxy, C3-C6alkynyloxy, C3-C7cycloalkyl, C1-C6haloalkoxy, C1-C6alkylthio, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl, C3-C6alkynyloxycarbonyl, C1-C6or by C1-C6alkoxy, cyano, —COOR17; —COR18 or a group (b) wherein R17 and R21 are each independently of the otherType: GrantFiled: August 24, 1999Date of Patent: February 27, 2001Assignee: Novartis Crop Protection, Inc.Inventor: Martin Zeller
-
Patent number: 6187812Abstract: Phenylacetic acid derivatives of the formula I where the substituents and the index have the following meanings: X is oxygen or sulfur; R is hydrogen or alkyl; R1 is hydrogen or alkyl; R2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy; m is 0, 1 or 2, it being possible for the R2 radicals to be different if m is 2; R3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamino; R4 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, unsubstituted or substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, alkenyl, alkenyloxy, alkenylthio, alkenylamino, N-alkenyl-N-alkylamino, alkynyl, alkynyloxy, alkynylthio, alkynylamino, N-alkynyl-N-alkylamino; unsubstituted or substituted cycloalkyl, cycloalkoxy, cycloalkylthio, cycloalkylamino, N-cycloalkyl-N-alkylamino, cycloalkenyl, cycloalkenyloxy, cycloalkenylthio, cycloalkenylamino, N-cycloalkenyl-N-alkylamino, heterocyclyl, heterocyclyloxy, heterocyclyType: GrantFiled: February 3, 2000Date of Patent: February 13, 2001Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Ruth Müller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Röhl, Eberhard Ammermann, Gisela Lorenz
-
Patent number: 6177466Abstract: The present invention is related to: (i) matrix metalloproteinase inhibitors containing sulfonylamino acid derivatives of the formula (Ia): wherein R1 is hydrogen, C1-4 alkyl; R is hydrogen, C1-8 alkyl etc.; E is —CONR3—, in which R3 is hydrogen, C1-4 alkyl etc., —NR3CO—, —CO—O—, —O—CO— etc.; A is hydrogen, C1-8 alkyl, C3-7 cycloalkyl, or Ar; J is bond, C2-4 alkylene etc.; G is —(CH2)m— in which m is 2, 3 or 4, or in which R6 and R7 is hydrogen, C1-8 alkyl etc.; and non-toxic salts thereof, (ii) novel sulfonylamino acid derivatives of the formula (Ib): wherein all the symbols are the same meaning as (i); and non-toxic salts thereof, and (iii) process for the preparation of the compound of the formula (Ib). The compounds of the formula (Ia) are useful for prevention and/or treatment of diseases induced by overexpression and excess activity of MMP.Type: GrantFiled: July 29, 1996Date of Patent: January 23, 2001Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Katsuhito Sakaki, Hidekazu Kanazawa, Tsuneyuki Sugiura, Tohru Miyazaki, Hiroyukii Ohno
-
Patent number: 6174887Abstract: 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: February 20, 1998Date of Patent: January 16, 2001Assignee: Japan Tobacco Inc.Inventors: Junichi Haruta, Kazuhiko Sakuma, Yoshihiro Watanabe
-
Patent number: 6160015Abstract: The present invention relates to compositions useful in the treatment of benign proliferative disorder neurofibromatosis comprising a farnesyl protein transferase inhibitor. Further contained in this invention are methods of treating benign proliferative disorder neurofibromatosis in a mammal, which methods comprise administering to said mammal, a farnesyl protein transferase inhibitor.Type: GrantFiled: July 27, 1999Date of Patent: December 12, 2000Assignee: University of CincinnatiInventor: Nancy Ratner
-
Patent number: 6159989Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: December 15, 1999Date of Patent: December 12, 2000Assignee: Merck & Co., Inc.Inventors: Lin Chu, Mark Goulet, Thomas F. Walsh, Matthew J. Wyvratt, Stephanie L. Witkin
-
Patent number: 6153609Abstract: A compound of the formula ##STR1## wherein n, X, R.sup.3, R.sup.4 and Q are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.Type: GrantFiled: February 16, 1999Date of Patent: November 28, 2000Assignee: Pfizer IncInventors: Ralph P. Robinson, Todd A. Blumenkopf
-
Patent number: 6143776Abstract: Tosylproline analogs of formula I, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are thymidylate synthase inhibitors; and are useful as anti-tumor agents and as anti-parasitics, anti-bacterials, anti-fungals, and anti-virals.Type: GrantFiled: February 2, 2000Date of Patent: November 7, 2000Assignee: Sunesis Pharmaceuticals, Inc.Inventor: Daniel A. Erlanson
-
Patent number: 6136804Abstract: The invention provides a method for treating, preventing, or reducing the risk of developing a condition selected from the group consisting of acute coronary ischemic syndrome, thrombosis, thromboembolism, thrombotic occlusion and reocclusion, restenosis, transient ischemic attack, and first or subsequent thrombotic stroke, in a patient, comprising administering to the patient a therapeutically effective amount of an antiplatelet agent in combination with a therapeutically effective amount of a COX-2 inhibitor. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a COX-2 inhibitor, or a pharmaceutically acceptable salt thereof, and an antiplatelet agent, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 12, 1999Date of Patent: October 24, 2000Assignee: Merck & Co., Inc.Inventor: Steven A. Nichtberger
-
Patent number: 6136834Abstract: A tetrazole derivative of formula (I) ##STR1## wherein R is H, alkyl, alkoxy, carbocyclic ring, alkyl or alkoxy substituted by carbocyclic ring;AA.sup.1 and AA.sup.2 is a bond or ##STR2## and ##STR3## respectively, or AA.sup.1 and AA.sup.2, together, may have the formula (a); ##STR4## and Y is formula (b) ##STR5## wherein the Tet ring is tetrazole; Z is alkylene, alkenylene, O, S, SO, SO.sub.2, NR.sup.26, methylene in alkylene replaced by O, S, --SO--, --SO.sub.2 -- or --NR.sup.26 --; and E is H, alkyl, or COOR.sup.27.Type: GrantFiled: June 29, 1998Date of Patent: October 24, 2000Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Makoto Tanaka, Tohru Miyazaki, Hiroyuki Ohno
-
Patent number: 6130247Abstract: The invention pertains to phenylcarbamates of formula (I), wherein X is a direct bond, O or NR.sup.a ; Z is O, S or NR.sup.b- ; R.sup.1 is hydrogen, alkyl or alkyl halide; R.sup.2 is substituted methyl or optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl; R.sup.3 is optionally substituted alkyl, alkenyl or alkinyl; R.sup.4 is alkyl, alkenyl or alkinyl and, if X is NR.sup.a, hydrogen also; R.sup.5 is hydrogen or optionally substituted alkyl, alkenyl, alkinyl, alkyl carbonyl or alkoxy carbonyl. The invention also pertains to methods for their preparation and agents containing them.Type: GrantFiled: November 5, 1998Date of Patent: October 10, 2000Inventors: Herbert Bayer, Bernd Muller, Ruth Muller, Hubert Sauter, Thomas Grote, Wassilios Grammenos, Reinhard Kirstgen, Klaus Oberdorf, Arne Ptock, Norbert Gotz, Michael Rack, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
-
Patent number: 6130315Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.Type: GrantFiled: August 24, 1998Date of Patent: October 10, 2000Assignee: Merrell Pharmaceuticals Inc.Inventors: H. Michael Kolb, Joseph P. Burkhart, Michael J. Jung, Fritz E. Gerhart, deceased, Eugene L. Giroux, Bernhard Neises, Daniel G. Schirlin
-
Patent number: 6124345Abstract: The present invention relates to carbomoylcarboxamide oximes of the formula (I): ##STR1## or salts thereof, processes for preparing the carbomoylcarboxamide oximes, compositions containing the carbomoylcarboxamide oximes and processes for controlling harmful fungi with an effective amount of the carbomoylcarboxamide oximes.Type: GrantFiled: November 24, 1998Date of Patent: September 26, 2000Assignee: BASF AktiengesellschaftInventors: Frank Wetterich, Karl Eicken, Reinhard Kirstgen, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
-
Patent number: 6114382Abstract: The present invention provides novel compositions and methods relating to the treatment of Inflammatory Bowel Disease ("IBD"), most notably, Ulcerative Colitis, Crohn's Disease, Colitis and Diverticulitis. The invention relates to the discovery of a parasitic microsporidia infecting the epithelium cells lining the gastrointestinal tract of patients suffering from IBD. The discovery of this correlation between the disease and the microsporidia, described herein, led to the development of methods for the accurate diagnosis of patients suffering from IBD, and also of methods for treating such a patient in accordance with the invention. This discovery also provides for the development of animal models to further elucidate the mechanism of the disease and potential additional cures therefor.Type: GrantFiled: November 11, 1998Date of Patent: September 5, 2000Inventor: Itagiba G. Moretti
-
Patent number: 6107337Abstract: A compound of the formula ##STR1## wherein n, X, R.sup.3, R.sup.4 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, bone resorption, loosening of artificial joint implants, atherosclerosis, multiple sclerosis, occular angiogenisis and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF.Type: GrantFiled: August 6, 1998Date of Patent: August 22, 2000Assignee: Pfizer Inc.Inventor: Ralph P. Robinson
-
Patent number: 6093398Abstract: The use of an MMP inhibitor, especially a collagenase inhibitor, in the manufacture of a medicament for the treatment of a natural or artificial tissue comprising extracellular matrix components to inhibit contraction of the tissue and methods for the treatment of tissue comprising extracellular matrix components to inhibit contraction.Type: GrantFiled: November 19, 1996Date of Patent: July 25, 2000Assignees: University of Florida Research Found, Institute of Ophthalmology, Moorfields Eye Hospital NHS TrustInventors: Peng Tee Khaw, Gregory S. Schultz
-
Patent number: 6057365Abstract: The present invention relates to fungicidal compositions and their use as a method for controlling phytopathogenic fungi comprising the application of a selected fungicidally active N-acetonylbenzamide compound and a second fungicidally active compound which is [2-methyl-1-[1-(4-methylphenyl)-ethylaminocarbonyl]-propyl]-carbamic acid, isopropyl ester to plant seed, to plant foliage or to a plant growth medium. The compositions and method of use provide higher fungicidal activity than separate use of the same compounds.Type: GrantFiled: December 22, 1998Date of Patent: May 2, 2000Assignee: Rohm and Haas CompanyInventors: David Hamilton Young, Willie Joe Wilson, Anne Ritchie Egan, Enrique Luis Michelotti
-
Patent number: 6022898Abstract: Compounds of general formula (II), wherein X is a hydroxamic or carboxylic acid group, Y is sulphonyl and R.sub.1 and R.sub.2 as defined in the claims are matrix metalloproteinase inhibitors.Type: GrantFiled: December 23, 1996Date of Patent: February 8, 2000Assignee: British Biotech Pharmaceuticals LimitedInventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett
-
Patent number: 5994359Abstract: 2-Iminooxyphenylacetic acid derivatives ##STR1## where the substituents and the index have the following meanings: R.sup.1 is C(CO.sub.2 CH.sub.3).dbd.NOCH.sub.3 (Ia), C(CONHCH.sub.3).dbd.NOCH.sub.3 (Ib), C(CONH.sub.2).dbd.NOCH.sub.3 (Ic), C(CO.sub.2 CH.sub.3).dbd.CHOCH.sub.3 (Id) or C(CO.sub.2 CH.sub.3).dbd.CHCH.sub.3 (Ie);R.sup.2 is cyano, nitro, halogen, alkyl, haloalkyl or alkoxy;m is 0, 1 or 2;R.sup.3 is hydrogen, cyano, hydroxyl, halogen,alkyl, haloalkyl, alkoxyalkyl, alkoxy, haloalkoxy, alkylthio, cyclopropyl, alkenyl,unsubstituted or substituted aryloxyalkyl, benzyl or benzyloxy,R.sup.4 is hydrogen, cyano,unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and hetaryl;unsubstituted or substituted alkoxy, alkenyloxy, alkynyloxy, cycloalkoxy, heterocyclyloxy, aryloxy and hetaryloxy;unsubstituted or substituted arylthio and hetarylthio;--Q--C(R.sup.5).dbd.N--Y.sup.1 --R.sup.6 or --Q--O--N.dbd.CR.sup.7 R.sup.8,R.sup.3 and R.sup.Type: GrantFiled: June 25, 1998Date of Patent: November 30, 1999Assignee: BASF AktiengesellschaftInventors: Thomas Grote, Hubert Sauter, Reinhard Kirstgen, Herbert Bayer, Ruth Muller, Bernd Muller, Klaus Oberdorf, Wassilios Grammenos, Norbert Gotz, Michael Rack, Albrecht Harreus, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
-
Patent number: 5981581Abstract: Phenylacetic acid derivatives of the formula I ##STR1##Type: GrantFiled: January 29, 1998Date of Patent: November 9, 1999Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
-
Patent number: 5962529Abstract: Compounds of general formula (II) wherein X is a hydroxamic or carboxylic acid group, Y is carbonyl or sulphonyl and R.sub.1 and R.sub.2 are as defined in the claims, are matrix metalloproteinase inhibitors.Type: GrantFiled: December 23, 1996Date of Patent: October 5, 1999Assignee: British Biotech Pharmaceuticals LimitedInventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett
-
Patent number: 5962487Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.Type: GrantFiled: December 16, 1997Date of Patent: October 5, 1999Assignee: Agouron Pharmaceuticals, Inc.Inventors: Stephen E. Webber, Peter S. Dragovich, Thomas J. Prins, Ethel S. Littlefield, Joseph T. Marakovits, Robert E. Babine
-
Patent number: 5919824Abstract: Aminophenol derivatives represented by the following formula (1): ##STR1## wherein X is O or S; A is alkylene, R.sup.1 is phenyl, etc., R.sup.2 and R.sup.3 are H or alkyl; R.sup.4 is substituted carbamoylalkyl, etc.; R.sup.5 is substituted amino, etc.; their salts, and optical isomers of the derivatives and salts. Also disclosed are gastrin receptor antagonists, cholecystokinin receptor antagonists, and medicines for digestive diseases. The compounds have strong binding inhibition against gastrin receptor or CCK-A receptor and also they have higher selectivity to either group of CCK-A receptor or gastrin receptor, and therefore, the compounds are useful for preventing and treating gastrointestinal diseases including peptic ulcers as well as central nervous system diseases.Type: GrantFiled: September 12, 1997Date of Patent: July 6, 1999Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Shuichi Yokohama, Keiichi Kawagoe, Yasuyuki Takeda, Yoshihiro Yokomizo, Aki Yokomizo
-
Patent number: 5889053Abstract: Novel farnesyl transferase inhibitors of general formula (I), ##STR1## the preparation thereof and pharmaceutical compositions containing said inhibitors, are disclosed. In general formula (I), R.sub.1 is Y--S--A.sub.1 (where Y is a hydrogen atom, an amino acid residue, a fatty acid residue, an alkyl or alkoxycarbonyl radical or a radical R.sub.4 --S-- where R.sub.4 is a C.sub.1-4 alkyl radical optionally substituted by a phenyl radical or a radical of general formula (II) ##STR2## wherein A.sub.1, X, X.sub.1, Y.sub.1, R'.sub.1, R.sub.2, R'.sub.2 and R are defined as below, and A.sub.1 is a C.sub.1-4 alkylene radical optionally alpha-substituted in the >C(X.sub.1)(Y.sub.1) grouping by an amino or alkylamino, dialkylamino, alkanoylamino or alkoxycarbonylamino radical); X.sub.1 and Y.sub.1 are each a hydrogen atom or, taken together with the carbon atom to which they are attached, form a >C.dbd.O grouping; R'.sub.1 is hydrogen or a C.sub.1-6 alkyl radical; X is an oxygen or sulphur atom; R.sub.2 is a C.Type: GrantFiled: January 9, 1998Date of Patent: March 30, 1999Assignee: Rhone-Poulenc Rorer S.A.Inventors: Bernard Baudoin, Christopher Burns, Alain Commercon, Alain Lebrun
-
Patent number: 5847194Abstract: Carbamoylcarboxamides of the general formula I ##STR1## and their salts (R.sup.1 is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl or an unsubstituted or substituted nonaromatic carbo- or heterocycle;R.sup.2 is H or unhalogenated or halogenated alkyl or cycloalkyl;R.sup.3 is unsubstituted or substituted alkyl, cycloalkyl or phenylalkyl;R.sup.4 is H or one of the radicals R.sup.3 orR.sup.3 and R.sup.4, together with the C atom to which they are bonded, are an unsubstituted or substituted carbo- or heterocycle;R.sup.5 independently of these is one of the radicals R.sup.2 ;X independently of one another is hydrogen, unsubstituted or substituted alkyl and/or alkenyl;Y independently of one another and of these is one of the radicals X;p,q independently of one another are 0, 1 or 2;R.sup.Type: GrantFiled: March 3, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: Frank Wetterich, Oliver Wagner, Karl Eicken, Eberhard Ammermann, Gisela Lorenz
-
Patent number: 5811424Abstract: The present invention provides an amino-acid amide derivative represented by the formula: ##STR1## (wherein R.sup.1 represents a lower alkyl group (optionally having at least one same or different substituent of a halogen atom), R.sup.2 represents an ethyl group, R.sup.3 represents a hydrogen atom, R.sup.4 represents a hydrogen atom, R.sup.5, R.sup.6, and R.sup.7 independently represent a hydrogen atom or a lower alkyl group, R.sup.8 represents a hydrogen atom, Z.sup.1 and Z.sup.2 independently represent an oxygen atom or a sulfur atom, Z.sup.3 represents an oxygen atom or a sulfur atom, Q represents a phenyl group, m represents an integer from 0 to 2, and n represents 0 or 1), and an agricultural or horticultural fungicide including an effective amount of the same. The amino-acid amide derivatives exhibit a superior control of plant diseases, particularly downy mildew and late blight, and are not harmful to plants.Type: GrantFiled: July 1, 1996Date of Patent: September 22, 1998Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masaru Shibata, Kazuhiko Sugiyama, Norihisa Yonekura, Junetsu Sakai, Yoshiyuki Kojima, Shigeru Hayashi
-
Patent number: 5808139Abstract: Non-steroidal compounds which are high affinity, high specificity ligands for progesterone receptors are disclosed. The compounds include synthetic derivatives of cyclocymopol and its diastereomers, spectroscopically and chromatographically pure (3R)-cyclocymopol monomethyl ether, which functions as a progesterone receptor antagonist, and spectroscopically and chromatographically pure (3S)-cyclocymopol monomethyl ether, which functions as a progesterone receptor agonist. Also disclosed are methods for employing the disclosed compounds for modulating processes mediated by progesterone receptors and for treating patients requiring progesterone receptor agonist or antagonist therapy.Type: GrantFiled: September 8, 1994Date of Patent: September 15, 1998Assignees: Ligand Pharmaceuticals Incorporated, The Regents of the University of CaliforniaInventors: I. Charles Pathirana, Christina S. Berger, Robert B. Stein, William Fenical, Todd K. Jones, Lawrence G. Hamann, Michael G. Johnson, Luc Farmer
-
Patent number: 5783593Abstract: The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.Type: GrantFiled: April 29, 1996Date of Patent: July 21, 1998Assignee: Abbott LaboratoriesInventors: William R. Baker, Saul H. Rosenberg, Anthony K. L. Fung, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, Stephen J. O'Connor, Rajnandan N. Prasad, Wang Shen, David M. Stout, Gerard M. Sullivan
-
Patent number: 5756498Abstract: Sulfonylalkanoylamino hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.In accordance with the present invention, compounds of Formula (I) are disclosed ##STR1## wherein the substituents are as defined in the specification.Type: GrantFiled: January 11, 1996Date of Patent: May 26, 1998Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
-
Patent number: 5728875Abstract: .alpha.-Amino acid amides of the formula I ##STR1## in which n is the number zero or one;R.sub.1 is C.sub.1 -C.sub.12 alkyl, which is unsubstituted or can be substituted by C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.3 -C.sub.8 cycloalkyl, cyano, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.3 -C.sub.6 alkenyloxycarbonyl or C.sub.3 -C.sub.6 alkynyloxycarbonyl; C.sub.3 -C.sub.8 cycloalkyl; C.sub.2 -C.sub.12 alkenyl;C.sub.2 -C.sub.12 alkynyl; C.sub.1 -C.sub.12 halogenoalkyl or a group NR.sub.13 R.sub.14 ; in which R.sub.13 and R.sub.14 independently of one another are hydrogen or C.sub.1 -C.sub.6 alkyl or together are tetra- or pentamethylene;R.sub.2 and R.sub.3 independently of one another are hydrogen; C.sub.1 -C.sub.8 alkyl; C.sub.1 -C.sub.8 alkyl which is substituted by hydroxyl, C.sub.1 -C.sub.4 alkoxy, mercapto or C.sub.1 -C.sub.4 alkylthio; C.sub.3 -C.sub.8 alkenyl;C.sub.3 -C.sub.8 alkynyl; C.sub.3 -C.sub.8 cycloalkyl or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.Type: GrantFiled: August 26, 1996Date of Patent: March 17, 1998Assignee: Novartis CorporationInventor: Martin Zeller
-
Patent number: 5707994Abstract: The present invention relates to a 2,3-diaminopropionic acid derivative of the formula (1): ##STR1## or a pharmaceutically acceptable salt thereof. The compounds of the present invention are useful as a platelet aggregation inhibitor, a cancer metastasis inhibitor, a wound healing agent or a bone resorption inhibitor.Type: GrantFiled: April 19, 1996Date of Patent: January 13, 1998Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Yoshihara Ikeda, Yasuyuki Ueki, Hisakazu Kishimoto, Toshio Nishihara, Yumiko Kamikawa
-
Patent number: 5698569Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: December 16, 1997Assignee: G. D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
-
Patent number: 5631293Abstract: Amino acid-substituted benzoylguanidines, a process for their preparation, their use as a medicament or diagnostic agent and a medicament containing themBenzoylguanidines of the formula I ##STR1## in which the radicals R(1) to R(5) have the meanings given in the description, are described. They are prepared by reacting a compound of the formula II ##STR2## in which R(1) to R(5) and L have the meanings given in the description, with guanidine. The compound I is suitable for the preparation of cardiovascular medicaments.Type: GrantFiled: September 8, 1995Date of Patent: May 20, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
-
Patent number: 5622949Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: April 22, 1997Assignee: G. D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
-
Patent number: 5620977Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: April 15, 1997Assignee: G.D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
-
Patent number: 5614522Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: July 24, 1995Date of Patent: March 25, 1997Assignee: G.D. Searle & Co.Inventors: John J. Talley, Kathryn L. Reed
-
Patent number: RE37873Abstract: Phenylacetic acid derivatives of the formula IType: GrantFiled: April 16, 2001Date of Patent: October 8, 2002Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Ruth Müller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Röhl, Eberhard Ammermann, Gisela Lorenz