Tricyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/522)
-
Patent number: 6906056Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: March 20, 2003Date of Patent: June 14, 2005Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: Richard C. Thompson, Stephen Wilkie, Douglas R. Stack, Eldon E. Vanmeter, Qing Shi, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
-
Patent number: 6900199Abstract: This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: October 14, 2003Date of Patent: May 31, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
-
Patent number: 6846814Abstract: Compounds having the general formula wherein R1a, R1b, R1c, R2, R3, R4, R5, R6, R7, R8, X1, X2, Y, Z and n are as defined in the specification, methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: GrantFiled: April 5, 2001Date of Patent: January 25, 2005Assignee: Astra Zeneca ABInventors: Jeffrey Scott Albert, Peter Bernstein, Cyrus Ohnmacht, Jr., Keith Russell, Ashokkumar Bhikkappa Shenvi
-
Patent number: 6777550Abstract: N-formyl hydroxylamines are provided which have the structure wherein R is H, alkyl, alkenyl, aryl-(CH2)p—, heteroaryl-(CH2)p— or cycloheteroalkyl-(CH2)p— R1 is H or COR2 where R2 is alkyl, aryl-(CH2)p—, cycloheteroalkyl-(CH2)p—, heteroaryl-(CH2)p—, alkoxy or cycloalkyl-(CH2)p—, p is 0 to 8, and A is a dipeptide derived from an amino acid or is a conformationally restricted dipeptide mimic. The above compounds are useful in treating hypertension congestive heart failure, renal failure, and hepatic cirrhosis.Type: GrantFiled: April 4, 1997Date of Patent: August 17, 2004Assignee: Bristol-Myers Squibb CompanyInventor: Jeffrey A. Robl
-
Patent number: 6762177Abstract: One aspect of the present invention relates to spirocyclic compounds. Another aspect of the present invention relates to the use of the spirocyclic compounds as ligands for mammalian G-protein-coupled receptors or sigma receptors. The present invention also relates to methods of modulating the activity of a G-protein-coupled receptor or a sigma receptor in a mammal using the spirocyclic compounds of the present invention. The present invention also relates to methods of treating various diseases in a mammal using the spirocyclic compounds of the present invention.Type: GrantFiled: November 5, 2002Date of Patent: July 13, 2004Assignee: Sepracor, Inc.Inventors: Heike Radeke, Paul E. Persons, James R. Hauske
-
Patent number: 6759404Abstract: Novel cyclic malonamides having the formula (I): and their pharmaceutical compositions. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein.Type: GrantFiled: April 3, 2001Date of Patent: July 6, 2004Inventors: Richard E. Olson, Michael G. Yang
-
Patent number: 6613905Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.Type: GrantFiled: September 4, 1998Date of Patent: September 2, 2003Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima
-
Patent number: 6608175Abstract: Certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases, are prepared in various embodiments using Grignard reagents and alkyllithium reagents and various aldehydes to make oxadiazole, thiadiazole and triazole peptoid alcohols, which are then oxidized to the desired keto products.Type: GrantFiled: November 16, 2001Date of Patent: August 19, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
-
Publication number: 20030153550Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: October 7, 2002Publication date: August 14, 2003Inventors: James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
-
Patent number: 6602866Abstract: This invention discloses and claims a series of mercaptoacetylamide derivatives of formula I. Also disclosed and claimed are pharmaceutical compositions incorporating these compounds and processes for preparing said compounds.Type: GrantFiled: April 8, 2002Date of Patent: August 5, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Gary A. Flynn, Barbara A. Anderson, Manfred Gerken, Bernd Jablonka, Heinz-Werner Kleemann, Wolfgang Linz, Werner Seiz, Bernhard Seuring
-
Patent number: 6559141Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: July 27, 2001Date of Patent: May 6, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
-
Patent number: 6552013Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: June 22, 1999Date of Patent: April 22, 2003Assignees: Elan Pharmaceuticals, Inc., Eli Lilly and CompanyInventors: James E. Audia, Warren J. Porter, Richard C. Thompson, Stephen C. Wilkie, Douglas R. Stack, Qing Shi
-
Patent number: 6544978Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: July 27, 2001Date of Patent: April 8, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
-
Patent number: 6541466Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: July 27, 2001Date of Patent: April 1, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
-
Patent number: 6528505Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: June 22, 1999Date of Patent: March 4, 2003Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: James E. Audia, Bruce A. Dressman, Qing Shi
-
Patent number: 6514964Abstract: The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as &agr;v&bgr;3, &agr;v&bgr;5, &agr;v&bgr;6 and the like. The invention encompasses novel compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of such diseases and disorders. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: September 26, 2000Date of Patent: February 4, 2003Assignee: Amgen Inc.Inventors: Zhidong Chen, Celia Dominguez, Ellen Grenzer-Laber, Nianhe Han, Longbing Liu, Ofir A. Moreno, Melvin C. Rutledge, Andrew S. Tasker
-
Patent number: 6509331Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: June 21, 1999Date of Patent: January 21, 2003Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
-
Patent number: 6486350Abstract: Disclosed are biological reagents which comprise compounds that inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in determining the cellular mechanism involved in the generation of &bgr;-amyloid peptide.Type: GrantFiled: September 29, 1999Date of Patent: November 26, 2002Assignees: Elan Pharmaceuticals Inc., Eli Lilly & CompanyInventors: James E. Audia, Paul A. Hyslop, Jeffrey S. Nissen, Richard C. Thompson, Jay S. Tung, Laura I. Tanner
-
Patent number: 6476019Abstract: One aspect of the present invention relates to spirocyclic compounds. Another aspect of the present invention relates to the use of the spirocyclic compounds as ligands for mammalian G-protein-coupled receptors or sigma receptors. The present invention also relates to methods of modulating the activity of a G-protein-coupled receptor or a sigma receptor in a mammal using the spirocyclic compounds of the present invention. The present invention also relates to methods of treating various diseases in a mammal using the spirocyclic compounds of the present invention.Type: GrantFiled: August 7, 2000Date of Patent: November 5, 2002Assignee: Sepracor Inc.Inventors: Heike Radeke, Paul E. Persons, James R. Hauske
-
Publication number: 20020137739Abstract: Tricyclic triazolobenzazepine derivatives in the form of a prodrug are provided. The compounds according to the present invention are those represented by formula (I) and pharmacologically acceptable salts and solvates thereof. The compounds are useful as antiallergic agents and exhibit excellent bioavailability.Type: ApplicationFiled: February 13, 2002Publication date: September 26, 2002Inventors: Yasuo Ohtsuka, Toshio Nishizuka, Sohjiro Shiokawa, Seiji Tsutsumi, Mami Kawaguchi, Hideo Kitagawa, Hiromi Takata, Takashi Shishikura, Toyoaki Ishikura, Kenichi Fushihara, Yumiko Okada, Sachiko Miyamoto, Maki Shiobara
-
Patent number: 6433165Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.Type: GrantFiled: January 21, 1999Date of Patent: August 13, 2002Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima
-
Publication number: 20020061874Abstract: This invention relates to novel lactams having the Formula (I): 1Type: ApplicationFiled: April 3, 2001Publication date: May 23, 2002Inventors: Michael G. Yang, Hong Liu
-
Publication number: 20020052360Abstract: This invention relates to novel lactams having the formula (I): 1Type: ApplicationFiled: March 14, 2001Publication date: May 2, 2002Inventors: Richard E. Olson, Hong Liu, Lorin A. Thompson III
-
Publication number: 20020042412Abstract: A new class of cyclin dependent kinase inhibitors that also have antiproliferative activity in human tumor cell line assays are described.Type: ApplicationFiled: December 14, 2000Publication date: April 11, 2002Inventors: Daniel W. Zaharevitz, Rick P. Gussio, Ravi K. Jalluri, Edward A. Sausville, Conrad Kunick, Laurent Meijer
-
Publication number: 20020025955Abstract: This invention relates to novel lactams of Formula (I): 1Type: ApplicationFiled: April 11, 2001Publication date: February 28, 2002Inventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
-
Publication number: 20020025956Abstract: Disclosed are 1-Azatricyclic-4-benzylpiperazine compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.Type: ApplicationFiled: June 28, 2001Publication date: February 28, 2002Inventors: Kevin Hodgetts, Stanislaw Rachwal, Daniel Rosewater, Andrew Thurkauf, Xiaoyan Zhang
-
Patent number: 6313290Abstract: The invention relates to azolobenzazepine derivatives of the formula I: wherein: X is O or S; R1, R2, R3 and R4 are independently hydrogen, perfluorolower-alkyl, halogen, nitro or cyano; and C together with the carbon atoms to which it is attached forms a 5-membered aromatic heterocycle, to pharmaceutical compositions containing them and to methods for the treatment of neurological disorders utilizing them.Type: GrantFiled: September 22, 2000Date of Patent: November 6, 2001Assignee: Zeneca LimitedInventors: Joseph James Lewis, Kelly Anne Brush, Laura Enid Garcia-Davenport, William Jackson Frazee, Marc Jerome Chapdelaine
-
Patent number: 6235730Abstract: 3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 3, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases.Type: GrantFiled: October 26, 1999Date of Patent: May 22, 2001Assignee: Japan Tobacco, Inc.Inventors: Motohide Sato, Takeo Katsushima, Hajime Kinoshita
-
Patent number: 6211174Abstract: The present invention is directed to certain naphtho-fused lactams of the general structural formula: wherein and R1, R1a, R1b, R2a, R2b, R3a, R4, R5, R6, A, L, X, n, p and w are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone.Type: GrantFiled: September 24, 1998Date of Patent: April 3, 2001Assignee: Merck & Co., Inc.Inventors: Robert J. Devita, Matthew J. Wyvratt
-
Patent number: 6180786Abstract: The present invention is new 3-(heterocyclic)-propenoic acid derivatives and pharmaceutical compositions thereof. These new 3-(heterocyclic)-propenoic acid derivatives are useful as NMDA antagonist.Type: GrantFiled: July 28, 1999Date of Patent: January 30, 2001Assignee: Hoechst Marion Roussel, Inc.Inventor: William A. Metz, Jr.
-
Patent number: 6150355Abstract: A phenylpiperidine derivative or pharmaceutical acceptable salt thereof represented by formula (I): ##STR1## wherein X represents CH or N; Y--Z represents CH.sub.2 --O, CH.sub.2 --S, CH.sub.2 --CH.sub.2, CH.dbd.CH or CONR.sup.5 (wherein R.sup.5 represents hydrogen or lower alkyl); R.sup.1 represents hydrogen, lower alkyl, halogen, lower alkoxy or trifluoromethyl; and R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represents hydrogen, lower alkyl or QR.sup.6 (wherein Q represents a single bond or lower alkylene, and R.sup.6 represents hydroxy, lower alkoxyalkoxy, lower alkoxy, lower alkylthio, nitro, halogen, lower alkanoyloxy, lower alkoxycarbonyl, lower alkanoyl or carboxyl).The present invention provides novel phenylpiperidine derivatives useful as analgesics.Type: GrantFiled: March 13, 1998Date of Patent: November 21, 2000Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Toshiaki Kumazawa, Hirokazu Koshimura, Shigeru Aono, Shunji Ichikawa, Shigeto Kitamura
-
Patent number: 6066632Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description, 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 as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.Type: GrantFiled: August 17, 1999Date of Patent: May 23, 2000Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Erik Fischer, Uffe Bang Olsen, Zdenek Polivka, Karel Sindelar, Vladimir Valenta
-
Patent number: 6054448Abstract: Compounds of the formula ##STR1## in which R.sup.1 is Y or Y--C.sub.1-6 alkyl, where Y is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or optionally substituted phenyl-C.sub.1-6 alkyl,and R.sup.2, R.sup.3, R.sup.4, X and Z are as defined in the specification, possess affinity for metabotropic glutamate receptors and are useful in the treatment of disorders of the central nervous system.Type: GrantFiled: October 17, 1997Date of Patent: April 25, 2000Assignee: Eli Lilly and Company LimitedInventors: Barry Peter Clark, John Richard Harris
-
Patent number: 6054458Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and m are as defined in the detailed part of the present description, 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, as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.Type: GrantFiled: June 23, 1998Date of Patent: April 25, 2000Assignee: NovoNordiskalsInventors: Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Rolf Hohlweg, Uffe Bang Olsen, Erik Fischer, Zdenek Polivka, Kaler Sindelar
-
Patent number: 6030967Abstract: A compound of the formula: whereinQ is an optionally substituted carbon atom or N(O)p wherein p is 0 or 1;Y is an optionally substituted methylene group, S(O)q wherein q is an integer of 0 to 2, or an optionally substituted imino group;Z.sup.1 is a C.sub.1-3 alkylene group which may have an oxo group or a thioxo group and may contain etherified oxygen or sulfur within the carbon chain;Z.sup.2 is an optionally substituted C.sub.1-3 alkylene group;Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;one of R.sup.1 and R.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group;the other is a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group; orR.sup.1 and R.sup.2 taken together with adjacent --c.dbd.c-- form a ring; andring A is a benzene ring which may be substituted in addition to R.sup.1 and R.Type: GrantFiled: October 30, 1997Date of Patent: February 29, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Masaki Ogino
-
Patent number: 5977100Abstract: A substituted guanidine derivative represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a hydrogen atom, an unsubstituted alkyl group, a substituted alkyl group, a halogen atom or the like; Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4, Y.sub.5, Y.sub.6 and Y.sub.7, which may be the same or different, are independently a single bond, --CH.sub.2 --, --O--, --CO-- or the like, adjacent members of a group consisting of Y.sub.1 through Y.sub.7 being able to be taken together to represent --CH.dbd.CH--, and at least two of Y.sub.1 through Y.sub.7 being independently a group other than a single bond; Z may be absent, or one or more Zs may be present and are, the same or different, independently a substituent for a hydrogen atom bonded to any of the carbon atoms constituting the ring formed by Y.sub.1 through Y.sub.Type: GrantFiled: May 8, 1998Date of Patent: November 2, 1999Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Masahumi Kitano, Naohito Ohashi
-
Patent number: 5962449Abstract: The present invention relates to novel N-substituted amino 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: March 28, 1996Date of Patent: October 5, 1999Assignee: Novo Nordisk A/SInventors: Peter Madsen, Knud Erik Andersen, Rolf Hohlweg, Florenzio Zaragossa Dorwald, Tine Krogh J.o slashed.rgensen, Uffe Bang Olsen, Henrik Sune Andersen
-
Patent number: 5952462Abstract: Antigens capable of eliciting antibodies which can catalyze chemical reactions, in particular, the cleavage or formation of a peptide linkage, comprising a hapten or a hapten and a suitable carrier molecule are disclosed. Haptens include, among others, silicon and boron containing compounds. Antibodies which are catalytically active for chemical reactions, in particular, the cleavage or formation of a selected peptide linkage or an ester bond, and which are elicited by such antigens are disclosed as well as methods for producing the antibodies and methods for catalyzing the cleavage or formation of a peptide linkage or in ester bond in a molecule.Type: GrantFiled: November 2, 1994Date of Patent: September 14, 1999Assignee: IGEN International Inc.Inventors: Michael J. Powell, Richard C. Titmas, Richard J. Massey
-
Patent number: 5880119Abstract: The present invention relates to certain novel mercaptoacetylamido 1,3,4,5-tetrahydro-benzo?c!azepin-3-one disulfide derivatives useful as inhibitors of enkephalinase and of ACE.Type: GrantFiled: August 12, 1997Date of Patent: March 9, 1999Assignee: Merrell Pharmaceuticals Inc.Inventors: Gary A. Flynn, Douglas W. Beight, Alan M. Warshawsky, Shujaath Mehdi, John F. French, John H. Kehne
-
Patent number: 5872251Abstract: The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme.Type: GrantFiled: November 10, 1997Date of Patent: February 16, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Gary A. Flynn, Thomas D. Bannister
-
Patent number: 5854273Abstract: A compound of formula (I) ##STR1## in which: X and Y, which may be identical or different, represent hydrogen or halogen or alkyl, trihaloalkyl, alkoxy, hydroxyl, cyano, nitro, amino, alkylamino, or dialkylamino,Z represent a linear or branched C.sub.4 to C.sub.12 alkylene chain in which one or more --CH.sub.2 -- are optionally replaced by any one of the following atoms or groups: --NR--, --O--, --S--, --SO--, --SO.sub.2 --, or --CONH--,A forms, with two adjacent carbon atoms of the phenyl ring, a phenyl, naphthyl or tetrahydronaphthyl ring or a heterocycle, ##STR2## represents any one of the groups as defined in the description, its optical isomers and its addition salts with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as anticancer agents.Type: GrantFiled: July 23, 1997Date of Patent: December 29, 1998Assignee: ADIR et CompagnieInventors: Gilbert Lavielle, Patrick Hautefaye, Ghanem Atassi, Alain Pierre, Laurence Kraus-Berthier, Stephane Leonce
-
Patent number: 5849908Abstract: The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme.Type: GrantFiled: November 10, 1997Date of Patent: December 15, 1998Assignee: Hoechst Marion Roussel Inc.Inventors: Gary A. Flynn, Michael J. Genin, Douglas W. Beight
-
Patent number: 5817654Abstract: The present invention relates to novel N-substituted naphthofused lactams and salts thereof of the formula ##STR1## Compounds of the general formula I possess the ability to stimulate the release of endogenous growth hormone. Thus, these compounds may be used in the treatment of conditions which require stimulation of growth hormone production or secretion such as in humans with growth hormone deficiency or where increased growth hormone plasma levels are desired, for instance in elderly patients or in livestock.Type: GrantFiled: January 29, 1997Date of Patent: October 6, 1998Assignee: Novo Nordisk A/SInventors: Henning Thogersen, Birgit Sehested Hansen, Bernd Peschke, Thomas Kruse Hansen, Knud Erik Andersen
-
Patent number: 5750521Abstract: The present invention relates to certain mercaptoacetylamide disulfide derivatives of Formula (I) ##STR1## useful as inhibitors of enkephalinase and ACE.Type: GrantFiled: November 4, 1996Date of Patent: May 12, 1998Assignee: Hoechst Marion Roussel Inc.Inventors: Gary A. Flynn, Douglas W. Beight, Shujaath Mehdi, Alan M. Warshawsky, John F. French, John H. Kehne
-
Patent number: 5734049Abstract: The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme.Type: GrantFiled: November 4, 1996Date of Patent: March 31, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: Gary A. Flynn, Michael J. Genin, Douglas W. Beight
-
Patent number: 5708168Abstract: Disclosed are methods of preparing azepines by a multistep synthesis including a Diels-Alder reaction. Also disclosed are methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment an azepine which has high binding to the NMDA glycine site.Type: GrantFiled: October 17, 1995Date of Patent: January 13, 1998Assignees: State of Oregon, Acting by and through The Oregon State Board of Higher Education, Acting for and on behalf of The Oregon Health Sciences University and The University of Oregon, Eugene Oregon, ACEA Pharmaceuticals, Inc.Inventors: John F. W. Keana, Anthony P. Guzikowski, Daniel F. Nogales, Sui Xiong Cai
-
Patent number: 5698551Abstract: 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: March 29, 1996Date of Patent: December 16, 1997Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Henrik Sune Andersen, Rolf Hohlweg, Peter Madsen, Uffe Bang Olsen
-
Patent number: 5696111Abstract: This invention is concerned with novel compounds represented by structural formula I and II. ##STR1## which are antiarrhythmic agents.Type: GrantFiled: May 16, 1996Date of Patent: December 9, 1997Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David A. Claremon, Nigel Liverton, Harold G. Selnick
-
Patent number: 5693649Abstract: 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: October 18, 1995Date of Patent: December 2, 1997Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
-
Patent number: 5688944Abstract: The present invention provides a novel carbamazepine hydrazide compound suitable for covalent attachment to a polymer particle reagent, having the general formula ##STR1## The present invention also provides a novel carbamazepine acid compound suitable for attachment to proteins for the production of carbamazepine immunogens. The carbamazepine antigen of the present invention has the following general structure: ##STR2## where X is C.dbd.O, CH.sub.2 or SO.sub.2 ; Y is C.dbd.O, CH.sub.2, SO.sub.2 ; R is an alkyl and P is a protein or a hapten.Type: GrantFiled: June 7, 1995Date of Patent: November 18, 1997Assignee: Dade International Inc.Inventor: Chengrong Wang