The Additional Hetero Ring Is Five-membered Patents (Class 544/152)
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Patent number: 7446195Abstract: Inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.Type: GrantFiled: August 16, 2006Date of Patent: November 4, 2008Assignee: Schering CorporationInventors: Yongqi Deng, Lianyun Zhao, Gerald W. Shipps, Jr., Patrick J. Curran, M. Arshad Siddiqui, Rumin Zhang, Charles W. McNemar, Todd W. Mayhood, William T. Windsor, Emma M. Lees, David A. Parry
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Publication number: 20080261967Abstract: Disclosed are agents having pharmacological activity against cellular receptors and intracellular signaling, particularly receptors and signaling pathways of central nervous system (CNS) neurotransmitters. Also disclosed are related methods and compositions for the treatment or prevention of diseases or disorders using the agents.Type: ApplicationFiled: June 20, 2005Publication date: October 23, 2008Inventor: John Cashman
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Publication number: 20080234271Abstract: The present invention relates in part to compounds of formulas (I) and (III): and pharmaceutically-acceptable salts and prodrugs thereof. These compounds can be useful for treating diseases such as inflammatory and immune diseases. The present invention also relates to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a subject.Type: ApplicationFiled: April 28, 2005Publication date: September 25, 2008Applicants: ICOS Corporation, Biogen Idec MA Inc.Inventors: Kevin Guckian, Daniel Scott, Irina Jacobson, C.Gregory Sowell
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Patent number: 7375105Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. Wherein X is O, CH2 CO, S or NH, or the moiety X—R1 is hydrogen; Y1 and Y2 independently represent CH or N; Ar is a mono- or fused bicyclic aromatic or heteroaromatic group which may be optionally substituted; one of X1 and X2 is selected from O, S or NR11 and the other is CH, wherein R11 is hydrogen, C1-6alkyl, aryl or arylC1-6alkyl.Type: GrantFiled: September 5, 2002Date of Patent: May 20, 2008Assignee: SmithKline Beecham p.l.c.Inventors: David Kenneth Dean, Andrew Kenneth Takle, David Matthew Wilson
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Patent number: 7189714Abstract: Compounds useful for the treatment of pain in accord with the following structural diagram, wherein R1, R2 and R3 are any of a number of groups as defined in the specification and pharmaceutical compositions and methods of treatment utilising such compounds.Type: GrantFiled: October 31, 2001Date of Patent: March 13, 2007Assignee: Astrazeneca ABInventors: Marc Chapdelaine, Lucius Kemp, John McCauley
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Patent number: 7101878Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.Type: GrantFiled: August 20, 1999Date of Patent: September 5, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Mark Brian Anderson, Haresh N. Vazir, David Robert Luthin, Genevieve DeGuzman Paderes, Ved P. Pathak, Lance Christopher Christie, Yufeng Hong, Eileen Valenzuela Tompkins, Haitao Li, James Faust
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Patent number: 7026476Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are and pharmaceutical compositions containing, intermediate compounds and processes of making such compounds.Type: GrantFiled: April 28, 2003Date of Patent: April 11, 2006Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John R. Proudfoot, Alan D. Swinamer
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Publication number: 20040198978Abstract: A composition having immunosuppressant activity comprises at least one compound of the formula (I) in which R is an acyl group of the formula (II) wherein one of R1 and R2 is H and the other is selected from OR4, SR4 and NHR4, wherein R4 is H or 1-6C alkyl, or R1 and R2 together with the carbon atom to which they are joined form a keto group, and R3 is a straight or branched chain, saturated or unsaturated aliphatic hydrocarbyl group containing from 8 to 11 carbon atoms and is optionally substituted by one or more substituent groups selected from halo, 1-6C alkoxy, carboxy, 1-6C alkoxycarbonyl and NR5R6 wherein each of R5 and R6 is selected from H and 1-6C alkyl or R5 and R6 together with the N atom form a morpholino or piperazino group, or any enantiomer thereof; and at least one compound of the formula (III): wherein R7 is a straight or branched chain, saturated or ethylenically-unsaturated aliphatic hydrocarbyl group containing from 1 to 18 carbon atoms which may optionally be substituted by one or more suType: ApplicationFiled: May 18, 2004Publication date: October 7, 2004Inventor: David Idris Pritchard
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Patent number: 6759409Abstract: A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A,; X, W, R1, Y; R3; and R4 are as defined herein. The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.Type: GrantFiled: December 17, 2001Date of Patent: July 6, 2004Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Christiane Yoakim, Bruno Haché, William W. Ogilvie, Jeffrey O'Meara, Peter White, Nathalie Goudreau
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Publication number: 20040087585Abstract: Nobel PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: August 28, 2003Publication date: May 6, 2004Inventors: Jia-Ning Xiang, Siegfried B Christensen, Jinhwa Lee, Daniel J Mercer
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Patent number: 6730671Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.Type: GrantFiled: February 13, 2003Date of Patent: May 4, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
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Publication number: 20040023954Abstract: 9,11-Cycloendoperoxide derivatives of biologically active prostaglandin analogs, and particularly of the ocular hypotensive drugs Bimatoprost, Latanaprost, Unoprostone, Travoprost and prostaglandin H2 1-ethanolamide or of structurally closely related analogs, are pro-drugs which hydrolyze under physiological conditions to provide prostaglandin analogues that are capable of providing sustained ocular and other in vivo concentrations of the respective drugs. The compounds of the invention have the formula shown below where the variables have the meaning defined in the specification.Type: ApplicationFiled: August 5, 2002Publication date: February 5, 2004Inventors: Kah-Hiing John Ling, Wu Yang, Jinsong Ni, Haiqing Yuan, Diane D.S. Tang-Liu
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Patent number: 6686390Abstract: The present invention relates to novel heterocyclic compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their regioisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.Type: GrantFiled: May 21, 2001Date of Patent: February 3, 2004Assignee: Dr. Reddy's Laboratories LimitedInventors: Manojit Pal, Koteswar Rao Yeleswarapu, Rajagopalan Ramanujam, Parimal Misra, Prem Kumar Mamnoor, Seshagiri Rao Casturi
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Publication number: 20030203900Abstract: Cathepsin S is a highly active cysteine protease belonging to the papain superfamily. It is found mainly in lymph nodes, spleen, and macrophages and this limited occurrence suggests the potential involvement of this enzyme in the pathogenesis of degenerative disease. The invention relates to novel protease inhibitors, particularly inhibitors of the cysteine proteases of the papain superfamily and more particularly to Cathepsin S. The inhibitors are Furanone derivatives of Formula (II) which have a characteristic non-hydrogen substituent R5. They are selective over other members of the family and in particular show selectivity over other members of the Cathepsin family such as L and K.Type: ApplicationFiled: November 16, 2001Publication date: October 30, 2003Inventors: Martin Quibell, Steven Taylor, Urszula Grabowska, Magnus Nilsson, Veronique Morisson
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Patent number: 6638967Abstract: Compounds of Formula I Wherein Z2 is an Oxygen or a Sulfur, Z1 is —CH═CH— and Y is a bond, W1 and W2 are hydrogens and X1 and X2 are various heterocyclic rings are disclosed.Type: GrantFiled: August 6, 2001Date of Patent: October 28, 2003Assignee: Ortho-McNeil Phamraceutical, Inc.Inventors: Michael Bogenstaetter, Wenying Chai, Annette K. Kwok
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Publication number: 20030171371Abstract: New N-acyl homoserine lactone compounds of the formula (I) in whichR is an acyl group of the formula (II) wherein one of R1 and R2 is H and the other is selected from OR4, SR4 and NHR4, wherein R4 is H or 1-6C alkyl, or R1 and R2 together with the carbon atom to which they are joined form a keto group, and R3 containing from 8 to 11 carbon atoms and is optionally substituted by one or more substituent groups selected from halo, 1-6C alkoxy, carboxy, 1-6C alkoxycarbonyl, carbamoyl optionally mono- or disubstituted at the N atom by 1-6C alkyl and NR5R6 wherein each of R5 and R6 is selected from H and 1-6C alkyl or R5 and R6 together with the N atom form a morpholino or piperazino group, or and enantiomer thereof, with the proviso that R is not a 3-oxododecanoyl group, having immuosuppressant properties are disclosed. The compounds are shown to have an inhibitory effect on lymphocyte proliferation and down-regulate TNF-&agr; secretion by monocytes/macrophages in the animal body, including the human body.Type: ApplicationFiled: February 12, 2003Publication date: September 11, 2003Inventors: Barrie Walsham Bycroft, David Idris Pritchard, Siri Ram Chhabra, Doreen Hooi
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Patent number: 6608057Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases.Type: GrantFiled: October 24, 2001Date of Patent: August 19, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
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Patent number: 6444615Abstract: This invention relates to 1-substituted-phenyl-3-substituted-2-thioxo-4,5-imidazolidinediones and 2,4,5-imidazolidinetriones which have activity as herbicides, to compositions which contain these compounds and to methods of use of these compounds. In particular, the present invention pertains to 2-thioxo-4,5-imidazolidinediones or 2,4,5-imidazolidinetriones wherein a 2,4,5,6-tetrasubstituted phenyl ring is linked to the heterocyclic ring.Type: GrantFiled: April 18, 2000Date of Patent: September 3, 2002Assignee: Dow AgroSciences LLCInventors: Bin Li, Ying Man, Zongjian Zhang, Adam Chi-Tung Hsu
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Patent number: 6362183Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: March 26, 2002Assignee: G. D. Searle & CompanyInventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
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Publication number: 20020016324Abstract: The present invention relates to novel anticancer agents, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The present invention more particularly relates to novel derivatives of andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of andrographolide have the general formula (I).Type: ApplicationFiled: May 4, 2001Publication date: February 7, 2002Applicant: DR. REDDY'S RESEARCH FOUNDATIONInventors: Srinivas Nanduri, Sriram Rajagopal, Venkateswarlu Akella
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Patent number: 6258841Abstract: Novel tubulin binding compounds having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel tubulin binding pocket, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.Type: GrantFiled: June 29, 1999Date of Patent: July 10, 2001Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Shyi-Tai M. Jan, Chen Mao
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Patent number: 6117870Abstract: A cyclic amide derivative of formula (I): ##STR1## wherein R.sup.1 represents a substituted alkyl group, a substituted alkenyl group, a substituted amino group, a substituted alkoxyl group, a substituted alkylthio group, a substituted carbamoyl group, a substituted sulfonamide group or a substituted amide group; the ring A represents a saturated cyclic alkyl group with 5 to 7 carbon atoms or a hetero-atom-containing saturated heterocyclic group with 3 to 6 carbon atoms; R.sup.2 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted heterocyclic group; R.sup.3 represents a hydrogen atom, a group represented by the general formula R.sup.4 O-- or a group represented by the general formula R.sup.5 (R.sup.6)N-- wherein R.sup.Type: GrantFiled: November 10, 1999Date of Patent: September 12, 2000Assignee: Fujirebio Kabushiki KaishaInventors: Akihiko Hosoda, Nobuo Kobayashi, Naoko Tanabe, Tsuneo Koji, Masahiro Shibata, Akihiro Sekine, Masaharu Dozen
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Patent number: 6051571Abstract: Disclosed are methods for treating a patient with an acute central nervous system or cardiovascular disorder or a neurodegenerative, autoimmune or inflammatory disease using a pharmaceutical composition containing a pharmaceutically acceptable carrier and an effective amount of a furan nitrone compound.Type: GrantFiled: May 24, 1999Date of Patent: April 18, 2000Assignee: Centaur Pharmaceuticals, Inc.Inventors: Judith A. Kelleher, Kirk R. Maples, Lowell David Waterbury, Hong Xu, Yong-Kang Zhang
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Patent number: 6040444Abstract: Disclosed are processes for preparing furan nitrone compounds using a furan carbonyl compound and a hydroxylamine compound.Type: GrantFiled: May 24, 1999Date of Patent: March 21, 2000Assignee: Centaur Pharmaceuticals, Inc.Inventors: Allan L. Wilcox, Yong-Kang Zhang
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Patent number: 6022870Abstract: Cyclic amides of Formula I which are useful as fungicides: ##STR1## wherein A is N; G is N and the floating double bond is attached to A; W is O or S; X is OR.sup.1, S(O).sub.m R.sup.1 or halogen; R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z are defined in the disclosure, are disclosed. Also, disclosed are fungicidal compositions containing these compounds and the use of these cyclic amide compounds for controlling plant diseases caused by fungal plant pathogens.Type: GrantFiled: May 13, 1999Date of Patent: February 8, 2000Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
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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: 5942507Abstract: Disclosed are furan nitrone compounds and pharmaceutical compositions containing such compounds. The disclosed compounds are useful as analytical reagents for detecting free radicals and as therapeutics for treating a wide variety of medical dysfunctions and diseases.Type: GrantFiled: July 17, 1997Date of Patent: August 24, 1999Assignee: Centaur Pharmaceuticals, Inc.Inventors: Judith A. Kelleher, Kirk R. Maples, Lowell David Waterbury, Allan L. Wilcox, Hong Xu, Yong-Kang Zhang
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Patent number: 5922706Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: November 13, 1997Date of Patent: July 13, 1999Assignee: Merck & Co., Inc.Inventors: Conrad P. Dorn, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Tamara Ladduwahetty
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Patent number: 5914351Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.Type: GrantFiled: December 12, 1997Date of Patent: June 22, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
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Patent number: 5891876Abstract: Compounds useful for enhancing synaptic responses mediated by AMPA receptors are disclosed, as are methods for the preparation thereof, and methods for their use for treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number of excitatory synapses or in the number of AMPA receptors. The invention compounds can also he used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors and for improving memory encoding.Type: GrantFiled: June 5, 1995Date of Patent: April 6, 1999Assignee: The Regents of the University of CaliforniaInventors: Gary S. Lynch, Gary A. Rogers
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Patent number: 5744607Abstract: The invention is directed to glutamic acid and aspartic acid derivatives represented by formula (I): ##STR1## wherein R.sub.1 is selected from the group consisting of unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or di-substituted phenylamino groups, a 2(beta)naphthyl group, and heterocyclic, monocyclic and dicyclic groups; R.sub.2 is selected from heterocyclic spiro groups, aminoalkyladamantyl groups, alkylamino groups, C.sub.4 -C.sub.10 cycloalkylamino groups and dicyclic amino groups (condensed); R.sub.3 is H, CH.sub.3 or C.sub.2 H.sub.5 ; A is a bond or a linear or branched alkylene group having from 1 to 4 carbon atoms; W is a tertiary amino group or a heterocyclic group; and r is 1 or 2. The compounds have a potent antagonistic effect on gastrin and cholecystokinin and can be used to treat diseases which are linked to imbalances in the physiological levels of gastrin, cholecystokinin or other biologically active polypeptides related thereto.Type: GrantFiled: October 18, 1996Date of Patent: April 28, 1998Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Lucio C. Rovati, Luigi A. Rovati
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Patent number: 5723607Abstract: The invention generally relates to compounds of the formula I, which are in equilibrium with their 4-hydroxy tautomers, and their pharmaceutically acceptable salts: ##STR1## where n is 0 to 2; A is S, CH.sub.2, O, NH or Se, and when n is 0, A is not CH.sub.2, and when n is 1, A is not CH.sub.2 or NH; X is a substituted or unsubstituted C.sub.1 -C.sub.3 alkyl, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl or amino, or sulfur or oxygen; Ar is a substituted or unsubstituted monocyclic carbocycle or heterocycle, or fused or nonfused polycyclic carbocycle or heterocycle; and R.sub.1 and R.sub.2 are hydrogen or a moiety that forms together with the attached CO.sub.2 a readily hydrolyzable ester group. These compounds and their salts are useful as inhibitors of GARFT or as antiproliferative agents. The invention also pertains to pharmaceutical compositions and methods employing such compounds as GARFT inhibitors or antiproliferative agents.Type: GrantFiled: January 30, 1997Date of Patent: March 3, 1998Assignee: Agouron Pharmaceticals, Inc.Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer
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Patent number: 5719147Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: September 8, 1995Date of Patent: February 17, 1998Assignee: Merck & Co., Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm MacCoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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Patent number: 5714484Abstract: Cysteine protease inhibitors which deactivate the protease by covalently bonding to the cysteine protease and releasing the enolate of a 1,3-dicarbonyl (or its enolic form). The cysteine protease inhibitors of the present invention accordingly comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a .beta.-dicarbonyl enol ether leaving group.Type: GrantFiled: June 7, 1995Date of Patent: February 3, 1998Assignee: Prototek, Inc.Inventors: Mary P. Zimmerman, Robert E. Smith, Mark Becker
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Patent number: 5674811Abstract: A cyanoketone derivatives of the following formula (1) ##STR1## which are characterized by excellent herbicidal activity and effectiveness against a variety of broad leafed weeds, including barnyard grass, green foxtail, velvet leaf, livid amaranth and hairy beggar ticks.Type: GrantFiled: October 6, 1994Date of Patent: October 7, 1997Assignee: Tokuyama CorporationInventors: Toshio Kitajima, Tadashi Kobutani, Shozo Kato, Masao Yamaguchi, Masahiko Ishizaki, deceased
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Patent number: 5648486Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: May 12, 1993Date of Patent: July 15, 1997Assignee: CytoMed, Inc.Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
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Patent number: 5629265Abstract: Disclosed herein are cyanoketone derivatives of the following formula (1) ##STR1## such as 1-cyano-1-piperidinocarbonyl-3-[4-(2-chloro-4-trifluoromethylphenoxy)pheno xy]-2-butanone, 1-cyano-1-piperidinocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-pyridyloxy )phenoxy]-2-butanone, 1-cyano-1-(N-methyl-N-dichlorophenyl)aminocarbonyl-3-[4-(2-quinoxalyloxy)p henoxy]-2-butanone, 1-cyano-1-(N,N-dibutyl)aminocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-py ridyloxy)phenoxy-2-butanone, and the like, which are characterized by excellent herbicidal activity and effectiveness against a variety of gramineous weeds.Type: GrantFiled: June 22, 1994Date of Patent: May 13, 1997Assignee: Tokuyama CorporationInventors: Masahiko Ishizaki, Seiji Nagata, Junji Takenaka
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Anti-tumor compounds, pharmaceutical compositions, methods for preparation thereof and for treatment
Patent number: 5599820Abstract: The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and methods for treatment of certain cancers with these new compounds.Type: GrantFiled: June 5, 1995Date of Patent: February 4, 1997Assignees: The Research Foundation of State University of New York, Indena SpA Gruppo Inverni Della BeffaInventors: Iwao Ojima, Ezio Bombardelli -
Patent number: 5567721Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: April 28, 1995Date of Patent: October 22, 1996Assignee: Centre International de Recherches DermatologiquesInventors: Jean-Michel Bernardon, William R. Pilgrim
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Patent number: 5506227Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: April 13, 1992Date of Patent: April 9, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
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Patent number: 5472956Abstract: Cyclophosphamide analogs are provided of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are each (C.sub.2 -C.sub.6)alkyl, substituted with a leaving group such as halo or alkylsulfonyl, R.sup.3 and R.sup.4 are the same as R.sup.1 and R.sup.2 or are H and Ar is a heteroaromatic ring and the pharmaceutically acceptable salts thereof.Type: GrantFiled: January 21, 1994Date of Patent: December 5, 1995Assignee: Research Corporation Technologies, Inc.Inventors: Richard F. Borch, James P. Schmidt
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Patent number: 5462939Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is (CR.sub.5 R.sub.6).sub.n, (CR.sub.5 R.sub.6).sub.n -aryl, (CR.sub.5 R.sub.6).sub.n -heteroaryl, X-(CR.sub.5 R.sub.6).sub.n, X-(CR.sub.5 R.sub.6).sub.n -aryl or X-(CR.sub.5 R.sub.6).sub.n -heteroaryl wherein aryl and heteroaryl may be optionally substituted;X is O or NR.sub.5 ;R.sub.5 and R.sub.6 are independently H or lower alkyl;R.sub.2 is H, halo, lower alkyl or (CR.sub.5 R.sub.6).sub.n -aryl;R.sub.3 and R.sub.4 are independently H or alkyl;A is a D or L isomer of an amino acid selected from the group consisting of alanine, valine, leucine, isoleucine, proline, phenylalanine, glycine, tyrosine, methionine, asparagine, glutamine, aspattic acid, glutamic acid, lysine, arginine, histidine and .beta.-thienylalanine;Z is CH.sub.2 or O; andn is 0-4;pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1.beta.Type: GrantFiled: May 7, 1993Date of Patent: October 31, 1995Assignee: Sterling Winthrop Inc.Inventors: Roland E. Dolle, Todd L. Graybill, Gary J. Speier, Catherine P. Prouty, Stanley J. Schmidt
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Patent number: 5434151Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: August 24, 1992Date of Patent: July 18, 1995Assignee: CytoMed, Inc.Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
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Patent number: 5358938Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl terahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiphenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: July 13, 1992Date of Patent: October 25, 1994Assignee: CytoMed, Inc.Inventors: Xiong Cai, Saijat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
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Patent number: 5314889Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).Type: GrantFiled: May 29, 1992Date of Patent: May 24, 1994Assignee: Elf SanofiInventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
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Patent number: 5300500Abstract: Novel podophyllotoxin compounds and their use in treating tumors are disclosed.Type: GrantFiled: December 8, 1992Date of Patent: April 5, 1994Assignees: The University of North Carolina at Chapel Hill, Yale UniversityInventors: Kuo-Hsiung Lee, Yung-Chi Cheng, Yi-Lin Zhang
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Patent number: 5240924Abstract: An N-acylamino acid derivative of the formula: ##STR1## wherein the substituents are herein defined, or a salt thereof, which is useful as hypotensive drugs.Type: GrantFiled: December 31, 1991Date of Patent: August 31, 1993Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
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Patent number: 5227400Abstract: A taxane derivative of the formula ##STR1## wherein ##STR2## Z is --OT.sub.1, T.sub.1 is hydrogen, hydroxyl protecting group, or --COT.sub.2,T.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 alkynyl or monocylic aryl,R.sub.3 is benzoyl, substituted benzoyl or C.sub.1 -C.sub.6 alkoxycarbonyl,Ac is acetyl, andE.sub.1 and E.sub.2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.Type: GrantFiled: April 3, 1992Date of Patent: July 13, 1993Assignee: Florida State UniversityInventors: Robert A. Holton, Hossain Nadizadeh, Ronald J. Beidiger
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Patent number: 5212172Abstract: Compounds of the formula ##STR1## whereR.sub.1 is H or alkyl of 1 to 20 carbons, CO--R.sub.1 *, CO--O--R.sub.1 *, CO--NH--R.sub.1 *, or PO(OR.sub.1 *).sub.2, PO(OR.sub.1 *)R.sub.1 * where R.sub.1 * independently is H, alkyl of 1 to 20 carbons, phenyl, or substituted phenyl;R.sub.2 is H or alkyl of 1 to 20 carbons;X is H, R.sub.3, CO--R.sub.3, CO--O--R.sub.3, CO--NH--R.sub.3, CO--N--(R.sub.3).sub.2, PO(OR.sub.3).sub.2, PO(OR.sub.3)R.sub.3, and R.sub.3 independently is H, phenyl, substituted phenyl, alkyl of 1 to 20 carbons or is alkyl of 1 to 20 carbons substituted with a hydroxyl, alkoxy, substituted amino, thioalkoxy or with a COR.sub.3 * group where R.sub.3 * is H, lower alkyl, OH, OR.sub.3 **, NH.sub.2, NHR.sub.3 ** or N(R.sub.3 **).sub.2 group where R.sub.3 ** independently is H or lower alkyl, with the proviso that when X is CO--O--R.sub.3 or is CO--NH--R.sub.3 then R.sub.3 is not hydrogen;Y is H, R.sub.4, CO--R.sub.4, CO--O--R.sub.Type: GrantFiled: November 15, 1991Date of Patent: May 18, 1993Assignee: Allergan, Inc.Inventor: Gary C. M. Lee