The Additional Hetero Ring Consists Of One Oxygen And Four Carbons Patents (Class 546/214)
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Patent number: 6635658Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, or individual isomers, racemic or non-racemic mixtures of isomers, or acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use and preparation as therapeutic drugs.Type: GrantFiled: December 2, 2002Date of Patent: October 21, 2003Assignee: Syntex (U.S.A.) LLCInventors: Ann Marie Madera, Robert James Weikert
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Patent number: 6635643Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 and R2 taken together form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk—X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)— NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy orType: GrantFiled: February 22, 2001Date of Patent: October 21, 2003Assignee: Janssen Pharmaceutica, N.V.Inventors: Jean-Paul RenĂ© Marie AndrĂ© Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
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Patent number: 6627629Abstract: 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: June 29, 2001Date of Patent: September 30, 2003Assignee: Bristol-Myers Squibb PharmaInventors: Soo S. Ko, James R. Pruitt, Dean A. Wacker, Douglas G. Batt
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Patent number: 6617325Abstract: The present invention relates to biphenyl derivatives of general formula wherein Ra to Rg and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.Type: GrantFiled: May 15, 2002Date of Patent: September 9, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
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Patent number: 6605626Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 21, 2001Date of Patent: August 12, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20030139417Abstract: A compound of general formula (I) 1Type: ApplicationFiled: April 12, 2002Publication date: July 24, 2003Inventors: Wolfgang Eberlein, Wolfhard Engel, Klaus Rudolf, Henri Doods, Gerhard Hallermayer, Eckhart Bauer
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Publication number: 20030100580Abstract: P51084 The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.Type: ApplicationFiled: June 13, 2002Publication date: May 29, 2003Inventors: Dashyant Dhanak, Steven David Knight
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Patent number: 6566373Abstract: The invention relates to 3-hydroxy-and 3-keto-cyclohetero-substituted leucine compounds that are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of diseases in which inhibition of bone loss is a factor. The 3-hydroxy-or 3-keto-moiety is bonded to a tetrahydrothiophene, tetrahydrothiopyran, tetrahydrofuran or tetrahydropyran ring.Type: GrantFiled: July 30, 2001Date of Patent: May 20, 2003Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.Inventors: Andrew D Gribble, Ashley Edward Fenwick, Robert W Marquis, Daniel F Veber, Jason Witherington
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Patent number: 6525069Abstract: 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: June 21, 2000Date of Patent: February 25, 2003Assignee: Bristol-Myers Squibb Pharma Co.Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Ui Tae Kim, Dean A. Wacker, Changsheng Zheng
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Patent number: 6503926Abstract: 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: and physiologically acceptable salts thereof.Type: GrantFiled: July 28, 1999Date of Patent: January 7, 2003Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Hiroki Sone, Osamu Kotera, Geraldine C. B. Harriman
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Publication number: 20030004340Abstract: There is provided a compound of formula I, 1Type: ApplicationFiled: March 19, 2002Publication date: January 2, 2003Inventors: Stephen Paul Gibson, Ivan Tommasini, Kimberley Verrier, Christopher James Dutton, David Morris Gethin, Douglas James Critcher, Richard Edward Armer
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Patent number: 6476054Abstract: The present invention is directed to cyclic amines of the formula I: (wherein R1, R2, R3, m and n 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-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.Type: GrantFiled: October 17, 2000Date of Patent: November 5, 2002Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Paul E. Finke, Malcolm Maccoss, Sander G. Mills, Bryan Oates, Dooseop Kim, Shankaran Kothandaraman, Liping Wang
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Publication number: 20020161005Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation.Type: ApplicationFiled: July 28, 1999Publication date: October 31, 2002Inventors: JAY R. LULY, YOSHISUKE NAKASATO, ETSUO OHSHIMA, HIROKI SONE, OSAMU KOTERA, GERALDINE C. B. HARRIMAN
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Publication number: 20020137736Abstract: There are provided novel compounds of formula (I) 1Type: ApplicationFiled: February 27, 2001Publication date: September 26, 2002Inventors: Kenneth Mattes, Robert Murray, Eifion D Phillips, Hans Schmitthenner
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Patent number: 6444686Abstract: 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: September 3, 2002Assignee: Brsitol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Ui Tae Kim, Joseph B. Santella, III, Dean A. Wacker
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Publication number: 20020115864Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.Type: ApplicationFiled: January 18, 2002Publication date: August 22, 2002Inventors: MacKlin Brian Arnold, Paul Leslie Ornstein, Richard Lee Simon, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Publication number: 20020098443Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.Type: ApplicationFiled: November 28, 2001Publication date: July 25, 2002Applicant: Shin-Etsu Chemical Co., Ltd.Inventors: Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe, Takeshi Nagata
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Patent number: 6358980Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: January 27, 2000Date of Patent: March 19, 2002Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
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Patent number: 6353136Abstract: Aromatic amines of the formula (I) Ar—[NR6R7]n (I) are prepared by reacting a haloaromatic of the formula (II) Ar—Hal (II) with an amine of the formula (III) R6R7NH (III) in the presence of a palladaphosphacyclobutane and a base and in the presence or absence of an ionic halide in a solvent at temperatures of from 20 to 200° C.Type: GrantFiled: September 8, 2000Date of Patent: March 5, 2002Assignee: Clariant GmbHInventors: Holger Geissler, Steffen Haber, Stefan Scherer, Andreas Meudt, Frank Vollmueller
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Patent number: 6323217Abstract: A compound of formula (I): wherein: R1 represents hydrogen or alkyl, R2a and R2b represent a group selected from hydrogen, halogen, alkyl, hydroxy, alkoxy, trihaloalkyl, cyano, nitro, amino, alkylamino and dialkylamino, R3 represents hydrogen or hydroxy, X represents oxygen or methylene, V represents an alkylene chain that is optionally unsaturated and optionally substituted, U represents a bond or an alkylene chain, W represents a group selected from aryl and heteroaryl, each of those groups being optionally substituted by one or more identical or different groups, its isomers, its hydrates, its solvates and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in the treatment of diseases or pathological conditions in which endothelial dysfunction is known.Type: GrantFiled: January 30, 2001Date of Patent: November 27, 2001Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Aimée Dessinges, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Catherine Thollon, Marie-Pierre Bourguignon
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Patent number: 6319920Abstract: This invention relates to muscarinic receptor antagonist compounds selected from the group of compounds represented by Formula I: wherein the substituents are as defined in the specification; and their pharmaceutically acceptable salts, individual isomers or a racemic or non-racemic mixture; pharmaceutical compositions containing them; and methods for their use as therapeutic agents.Type: GrantFiled: February 1, 1999Date of Patent: November 20, 2001Assignee: Syntex (U.S.A.) LLCInventors: Joan Marie Caroon, Robin Douglas Clark, Michael Patrick Dillon, Ralph New Harris, III, Sharathchandra Surendra Hegde, Clara Jeou Jen Lin, Hans Maag, David Bruce Repke
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Patent number: 6313122Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: March 20, 2000Date of Patent: November 6, 2001Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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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: 6303620Abstract: Disclosed are 4,4-disubstituted and 3,3-disubstituted piperidine compounds of formula I wherein D, E, G, J, R1, a, b, c, and d are defined in the specification, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.Type: GrantFiled: May 6, 1999Date of Patent: October 16, 2001Assignee: Novo Nordisk A/SInventors: Thomas Kruse Hansen, Michael Ankersen
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Patent number: 6297274Abstract: Novel nonpeptide endothelin I antagonists of Formula are described wherein R1 is unsubstituted or substituted cycloalkyl, phenyl, naphthyl or heteroaryl, R2 is unsubstituted or substituted alkyl, aryl or heteroaryl, R3 is unsubstituted or substituted alkyl, cycloalkyl, aryl or heteroayl, and R1 and/or R2 and/or R3 are independently substituted by a total of from 1 to 4 substituents which enhance aqueous solubility with the proviso that when R2 is alkyl and is substituted, the substituent is not oxygen at the &agr;-position of the furanone ring.Type: GrantFiled: August 4, 1998Date of Patent: October 2, 2001Assignee: Warner-Lambert CompanyInventors: Xue-Min Cheng, Annette Marian Doherty, William Chester Patt, Joseph Thomas Repine
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Patent number: 6288085Abstract: The present invention relates to certain novel piperidine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of psychotic disorders.Type: GrantFiled: June 17, 1999Date of Patent: September 11, 2001Assignee: Akzo Nobel N.V.Inventors: Duncan Robertson Rae, Samuel George Gibson
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Patent number: 6288084Abstract: 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: September 11, 2001Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima
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Publication number: 20010011092Abstract: Novel compounds of the formula 1Type: ApplicationFiled: January 25, 2001Publication date: August 2, 2001Inventors: Deen Tulshian, Ginny D. Ho, Lisa S. Silverman, Julius J. Matasi, Robbie L. McLeod, John A. Hey, Richard W. Chapman, Ana Bercovici, Francis M. Cuss
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Patent number: 6262060Abstract: The invention relates to azacycloalkane derivatives, to pharmaceutical compositions containing them, to processes for preparing them, and to methods for the treatment of hyperglycaemia, diabetes, obesity or inflammation utilizing them.Type: GrantFiled: November 27, 2000Date of Patent: July 17, 2001Assignee: Sanofi-SynthelaboInventors: Manuel Bedoya-Zurita, Juan Antonio Diaz Martin, Marc Daumas
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Patent number: 6251919Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, epilepsy, asthma, amyotrophic lateral sclerosis, or pain and to pharmaceutical compositions that contain the compounds of Formula I.Type: GrantFiled: June 14, 1999Date of Patent: June 26, 2001Assignee: Warner-LambertInventors: Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder
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Patent number: 6222039Abstract: The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are as defined in the specification as well as to the novel intermediates obtained by said process.Type: GrantFiled: July 7, 1999Date of Patent: April 24, 2001Assignee: Hoffman-La Roche Inc.Inventors: Michelangelo Scalone, Ulrich Zutter
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Patent number: 6222048Abstract: The invention encompasses the novel compound of Formula (I) as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula (I). The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula (I).Type: GrantFiled: June 12, 1997Date of Patent: April 24, 2001Assignee: Merck Frosst Canada & Co.Inventors: Cameron Black, Erich Grimm, Serge Leger, Petpiboon Prasit, Zhaoyin Wang
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Publication number: 20010000038Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1Type: ApplicationFiled: December 1, 2000Publication date: March 15, 2001Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
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Patent number: 6172057Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: February 19, 1998Date of Patent: January 9, 2001Assignee: American Cyanamid CompanyInventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Baihua Hu, Derek Cecil Cole, Jannie Lea Baker, Marcy Pamela Jacobson, Matthew Robin O'Dell
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Patent number: 6143768Abstract: The invention concerns a compound of formula (I) in which A is a piperidin-1-yl group non-substituted or substituted by one or several groups selected among a C.sub.1 -C.sub.4 alkyl group and a hydroxy group; R.sub.1 and R.sub.2, identical or different, are selected among a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group and a hydroxy group and their edible salts.Type: GrantFiled: November 29, 1999Date of Patent: November 7, 2000Assignees: Francaise d'Aromes et Parfums, Akbar EmamiInventor: Imam Emami
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Patent number: 6143744Abstract: 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: November 7, 2000Assignees: 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: 6140349Abstract: The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, m and n 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-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.Type: GrantFiled: February 1, 1999Date of Patent: October 31, 2000Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Malcolm Maccoss, Paul E. Finke, Sander G. Mills, Bryan Oates, Shankaran Kothandaraman, Dooseop Kim, Liping Wang
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Patent number: 6113812Abstract: A photochromic article that includes a host material and a photochromic amount of a benzopyran compound, the benzopyran compound represented by one of the formulas: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are selected from hydrogen, a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound.Type: GrantFiled: August 4, 1997Date of Patent: September 5, 2000Assignee: Vision-Ease Lens, Inc.Inventor: Frank J. Hughes
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Patent number: 6096761Abstract: The present invention of compounds of formula (I), ##STR1## a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R.sup.1 is C.sub.1-6 alkyloxy, C.sub.2-6 alkenyloxy or C.sub.2-6 alkynyloxy; R.sup.2 is hydrogen or C.sub.1-6 alkyloxy, or when taken together R.sup.1 and R.sup.2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C.sub.1-6 alkyl; R.sup.3 is hydrogen or halo; R.sup.4 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.2-6 alkenyl optionally substituted with aryl, or L is a radical of formula -Alk-R.sup.5 -, Alk-X--R.sup.6, -Alk-Y--C(.dbd.O)--R.sup.8, or -Alk-Y--C(.dbd.O)--NR.sup.10 R.sup.11 wherein each Alk is C.sub.1-12 alkanediyl; and R.sup.5 is hydrogen, cyano, C.sub.1-6 alkylsulfonylamino, C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, aryl, di(aryl)methyl or a heterocyclic ringsystem; R.sup.6 is hydrogen, C.sub.Type: GrantFiled: August 11, 1998Date of Patent: August 1, 2000Assignee: Janssen Pharmaceutica N.V.Inventors: Jean-Paul Rene Marie Bosmans, John Christopher Love, Michel Anna Jozef Decleyn, Henri Elisabeth Frans D'Haen
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Patent number: 6083943Abstract: A compound of the chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein Y is C.sub.2 -C.sub.4 alkylene; Z is a valence bond or C.sub.1 -C.sub.6 alkylene; R.sup.1 is substituted or unsubstituted aryl (e.g., phenyl and naphthyl) or heteroaryl (e.g., thienyl and furyl); R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.3 is hydrogen, hydroxy or the like; R.sup.4 is substituted or unsubstituted benzyl or the like. Typical examples are (2S*,3S*,4R*,5R*)-4-Carboxy-3-[N-(5-Isopropyl-2-methoxy-benzyl)amino]-5-me thyl-2-phenylpyrrolidine and (2S*,3S*,5S*)-5-Carboxy-3-[N-(2-methoxy-5-trifluoromethoxybenzyl)amino]-2- phenylpiperidine. The novel substituted azaheterocyclecarboxylic acids in this invention have excellent substance P antagonistic activity and are thus useful for the treatment of gastrointestinal disorders, central nervous system disorders, allergy, inflammatory diseases, asthma, pain, emesis or migraine in mammals, especially humans.Type: GrantFiled: March 19, 1999Date of Patent: July 4, 2000Assignee: Pfizer IncInventors: Masaya Ikunaka, Yuji Shishido, Masami Nakane
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Patent number: 6066650Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.Type: GrantFiled: July 21, 1997Date of Patent: May 23, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Richard B. Sulsky, Joseph A. Tino, John E. Lawson, Henry M. Holava, Richard A. Partyka
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Patent number: 6037352Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.Type: GrantFiled: November 19, 1998Date of Patent: March 14, 2000Assignee: Schering CorporationInventors: Derek Lowe, Wei Chang, Joseph Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W Clader, Samuel Chackalamannil, Wang Yuguang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom
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Patent number: 6017947Abstract: R.sup.6 is H, halogen, alkyl, alkoxy, alkylthio, cyano, or nitro;R.sup.10 is phenylthio, dialkylamino, alkylthio, alkoxycarbonyl, N-morpholinyl, or N-piperidinyl;R.sup.11 is hydrogen or alkyl;Q is alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, alkoxycarbonyl, alkoxyiminomethyl, or Y--Ar;Y is --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, or --CH.sub.2 SO.sub.2 --;Ar is a substituted or unsubstituted phenyl or aromatic heterocyclic group,useful for the inhibition of the replication of HIV-1, in vitro and in vivo.Type: GrantFiled: September 17, 1999Date of Patent: January 25, 2000Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
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Patent number: 5994396Abstract: Disclosed are furansulfonic acid derivatives and pharmaceutical compositions containing such derivatives. The disclosed compositions are useful for preventing and/or treating neurodegenerative, autoimmune and inflammatory conditions in mammals.Type: GrantFiled: August 13, 1998Date of Patent: November 30, 1999Assignee: Centaur Pharmaceuticals, Inc.Inventors: Judith A. Kelleher, Kirk R. Maples, Yong-Kang Zhang
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Patent number: 5990313Abstract: Disclosed is a process for the preparation of 3-alkyltetrahydrofurans by a two-step process wherein 2,3-dihydrofuran is reacted with an acetal to form an intermediate compound which may be converted to a 3-alkyltetrahydrofuran by contacting the intermediate with hydrogen in the presence of a catalytic amount of a Group VIII noble metal or rhenium, water and a strong acid.Type: GrantFiled: September 29, 1998Date of Patent: November 23, 1999Assignee: Eastman Chemical CompanyInventor: William Anthony Beavers
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Patent number: 5969136Abstract: This invention provides a process for preparing a compound of formula III ##STR1## wherein R.sup.1 is bromo, iodo or COOR.sup.2 ;R.sup.2 is H, C.sub.1 -C.sub.4 alkyl, phenyl which may be substituted or benzyl; andA is a 5- or 6-membered aromatic residue which may contain up to three hetero atoms and which may optionally be substituted with one or two groups selected from the group consisting of halo, hydroxy, C.sub.1 -C.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy; or a salt thereof, which comprises(a) reacting a compound of formula I ##STR2## wherein R is C.sub.1 -C.sub.4 alkyl or phenyl which may be substituted; andR.sup.1, R.sup.2, and A are as defined above;or a salt thereof, with a sulfurization agent;(b) cyclizing the reaction product from step (a) with guanidine; and(c) optionally salifying the reaction product from step (b).Type: GrantFiled: July 23, 1993Date of Patent: October 19, 1999Assignee: Eli Lilly and CompanyInventors: Charles J. Barnett, Thomas M. Wilson
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Patent number: 5965574Abstract: Compounds of the formula ##STR1## wherein ring A, ring B, ring D, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.11, R.sup.12, R.sup.13, E, G, X and P are as defined below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.Type: GrantFiled: August 13, 1996Date of Patent: October 12, 1999Inventors: Yuhpyng Liang Chen, Arthur Adam Nagel
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Patent number: 5952376Abstract: Triene-containing compounds which mimic the chemical and/or biological activity of the spongistatins are provided, as are methods and intermediates useful in their preparation.Type: GrantFiled: November 7, 1997Date of Patent: September 14, 1999Assignee: The Trustees of the University of PennsylvaniaInventors: Amos B. Smith, III, Qiyan Lin
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Patent number: RE37035Abstract: Phenylacetic acid benzylamides having the following general structure wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.Type: GrantFiled: October 7, 1997Date of Patent: January 30, 2001Assignee: Boehringer Ingelheim KGInventors: Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, Robert Sauter, Manfred Reiffen, Eckhard Rupprecht
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Patent number: RE38257Abstract: A piperidine compound of the formula (I): wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH2)n, which may be substituted, in which n is 0 or an integer of 1 to 10, —CH≡CH—, —C≡C—, —O—, —S—, —NH—, —N(COCH3)—, —N(COOC2H5)—, —N(CHO)—, —N(CH3)—, —CO—, —SO—, or —SO2—; Y is —CH≡CH—, —CH2CH2—, —CH2CO—, —O—, —S—, —NH—, —OCH2—, —SCH2—, —NHCH2—, —CH(OH)CH2— or —CH(OH)CH(OH)—; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of tType: GrantFiled: February 10, 1999Date of Patent: September 23, 2003Assignee: Ajinomoto Co., Inc.Inventors: Masataka Shoji, Kozo Toyota, Chikahiko Eguchi, Ryota Yoshimoto, Yoshikatsu Koyama, Hideki Domoto, Akira Kamimura