Plural Ring Nitrogens In The Seven-membered Hetero Ring Patents (Class 514/211.08)
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Patent number: 6696480Abstract: A use for agents that disrupt actin cytoskeletal organization is provided. In the instant invention, agents that disrupt actin cytoskeletal organization are found to upregulate endothelial cell Nitric Oxide Synthase activity. As a result, agents that disrupt actin cytoskeletal organization are useful in treating or preventing conditions that result from the abnormally low expression and/or activity of endothelial cell Nitric Oxide Synthase. Such conditions include hypoxia-induced conditions. Subjects thought to benefit mostly from such treatments include nonhyperlipidemics and nonhypercholesterolemics, but not necessarily exclude hyperlipidemics and hypercholesterolemics.Type: GrantFiled: May 13, 2002Date of Patent: February 24, 2004Assignee: Brigham and Women's Hospital, Inc.Inventor: James K. Liao
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Publication number: 20040033207Abstract: People's hands undergo daily exposure to hot, cold, and chemicals (such as cleansers). These exposures can cause dermatitis due to activation of the Epidermal Growth Factor Receptor (EGFR). One effect of activation of the EGFR is hyperproliferation of skin cells, which presents as rough, dry, and/or peeling hands, generally known as dermatitis. The use of a natural EGFR inhibitor, such as genistein or quercetin, can help to treat or prevent these kinds of dermatitis.Type: ApplicationFiled: August 12, 2003Publication date: February 19, 2004Inventors: Sewon Kang, Gary J. Fisher, John J. Voorhees
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Patent number: 6680328Abstract: The present invention relates to novel 8-azabicyclo[3.2.1]oct-2-ene and -octane derivatives which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of chemical substances.Type: GrantFiled: May 25, 2001Date of Patent: January 20, 2004Assignee: NeuroSearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon Feldbaek Nielsen, Elsebet Ostergaard Nielsen
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Publication number: 20030236246Abstract: Disclosed are methods for decreasing or attenuating an increase in capillary permeability in the retina in a subject in need of such treatment, comprising administering a composition comprising an amount of a staurosporine derivative or a salt thereof to a subject suffering from excessive or pathological capillary permeability in the retina, the amount of staurosporine derivative or salt thereof being effective to decrease the permeability of capillaries in the retina of the subject.Type: ApplicationFiled: April 21, 2003Publication date: December 25, 2003Inventors: Romulus Kimbro Brazzell, Kenneth E. Green, Frances Elizabeth Kane, Peter Anthony Campochiaro
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Patent number: 6656932Abstract: Selective MMP-13 inhibitors are benzo thiadiazines of the Formula or a pharmaceutically acceptable salt thereof, wherein R2 is hydrogen or alkyl; R1 and R3 include hydrogen, alkyl, and aryl, with the proviso that R3 is not (CH2)m biphenyl or (CH2)m substituted biphenyl; X is O or NH, n is 0, 1, or 2. The compounds of Formula I, or a pharmaceutically acceptable salt thereof, is useful for treating diseases mediated by an MMP-13 enzyme, including diseases selected from osteoarthritis, rheumatoid arthritis, cancer, inflammation, and heart failure.Type: GrantFiled: February 13, 2002Date of Patent: December 2, 2003Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Michael William Wilson
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Patent number: 6649620Abstract: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents an aryl group or a heteroaryl group, optionally substituted by C1-4 alkyl or SO2NH2; R3 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent, or represents a cyclic group of formula Ia, or represents a chain of formula Ib, and pharmaceutically acceptable salts thereof, are useful in the treatment of a variety of disorders including benign prostatic hyperplasia.Type: GrantFiled: September 23, 2002Date of Patent: November 18, 2003Assignee: Pfizer Inc.Inventors: Alan John Collis, David Nathan Fox
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Publication number: 20030212057Abstract: The present invention relates to substituted piperidines of general formula 1Type: ApplicationFiled: November 7, 2002Publication date: November 13, 2003Inventors: Klaus Rudolf, Henri Doods, Eckhart Bauer, Rudolf Hurnaus, Wolfgang Eberlein, Alexander Dreyer, Stephan Georg Mueller
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Patent number: 6642242Abstract: The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents one or more groups independently selected from H, halogen, C1-4 alkoxy and CF3; in addition, R2 and one R3 group may together represent —OCH2—, the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceutically acceptable salts thereof.Type: GrantFiled: March 19, 2001Date of Patent: November 4, 2003Assignee: Pfizer Inc.Inventors: Alan John Collis, David Nathan Abraham Fox, Julie Newman
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Publication number: 20030203891Abstract: Novel pesticides of formula (I) 1Type: ApplicationFiled: January 21, 2003Publication date: October 30, 2003Inventors: Thomas Goebel, Eliane Humbert-Droz, Maurizio Schwarzenbach
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Publication number: 20030199469Abstract: This invention provides methods for screening a modulating agent which when combined with antitumor therapeutic agent increases apoptosis in tumor cells. This invention also provides methods for screening antitumor therapeutic agents suitable for combination therapy with a protein kinase C inhibitors capable of potentiating apoptosis in tumor cells. This invention further provides different combination therapies comprising the specific protein kinase C inhibitors and the antitumor therapeutic agents.Type: ApplicationFiled: August 7, 2002Publication date: October 23, 2003Applicant: Sloan - Kettering Institute for Cancer ResearchInventors: Gary K. Schwartz, Anthony P. Albino
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Patent number: 6635637Abstract: Cyclic oxyguanidine compounds, including compounds of Formulae I and II: wherein R1, R3-R6, R21-R26, L, Y, Z, and A are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formulae I and II. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: August 2, 2001Date of Patent: October 21, 2003Assignee: Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Tianbao Lu, Bruce Edward Tomczuk, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Publication number: 20030194749Abstract: One aspect of the present invention relates to methods and reagents for profiling cells and/or subcellular environments (e.g., membrane or nuclear cellular fractions). The invention uses small molecule probes that bind covalently to protein targets, which significantly simplifies purification and identification of proteins using full length or proteolyzed proteins. Proteins, cellular components or other binding partners (collectively known as “LBP” or “lipid binding partner”) can be naturally occurring, such as proteins or fragments of proteins cloned or otherwise derived from cells, or can be artificial, e.g., polypeptides which are selected from random or semi-random polypeptide libraries.Type: ApplicationFiled: February 18, 2003Publication date: October 16, 2003Inventors: Thomas J. Wandless, Karlene Cimprich, Gilbert Chu, Michelle Stohlmeyer, Cornelia Fas
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Patent number: 6630475Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of ParkinsoType: GrantFiled: May 24, 2001Date of Patent: October 7, 2003Assignee: Schering CorporationInventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil
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Patent number: 6624157Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof wherein: r, s and t are 0 or 1; m=0, 1, 2; p is 0, 1 or 2; X is selected from the group consisting of oxygen, hydrogen or R1, R2, R3; Y is selected from the group consisting of CHR9, SO2, CO, CO2, O, NR10, SO2NR11 and CONR12; R6, R7, R9, R10, R11, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, and R28 are selected from the group consisting of hydrogen, lower alkyl or substituted alkyl; R4, R5 are selected from the group consisting of hydrogen, halo, nitro, cyano and U-R13; R12 is selected from the group consisting of hydrogen, lower alkyl, aryl, substituted alkyl or aryl; U is selected from the group consisting of sulfur, oxygen, NR14, CO, SO, SO2, CO2, NR15CO2, NR16CONR17, NR19SO2, NR19SO2NR20, SO2NR2Type: GrantFiled: January 26, 2001Date of Patent: September 23, 2003Assignee: Bristol-Myers Squibb CompanyInventor: Charles Z. Ding
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Publication number: 20030171353Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: ApplicationFiled: December 19, 2002Publication date: September 11, 2003Applicant: WyethInventors: Derek Cecil Cole, Joseph Raymond Stock, William Joseph Lennox, Ping Zhou
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Publication number: 20030166602Abstract: The invention is a drug delivery system of a delivery vehicle having a low molecular weight hyaluronan ligand with an affinity for CD44 receptors. Preferably, the delivery vehicle is a liposome but other suitable delivery vehicles include micropspheres, micelles, emulsions, lipid discs, polymers, viral particles and viruses. The systems of the invention may further comprise a drug, which can be any anticancer agent or other therapeutic or diagnostic agent. The invention also comprises methods of delivering a drug to a cell that expresses CD44 by contacting the cell with the drug delivery system. Further methods include treating a patient with cancer and targeting drug delivery to cells that express CD44 by attaching a glycosaminoglycan ligand.Type: ApplicationFiled: February 12, 2003Publication date: September 4, 2003Inventor: Francis C. Szoka
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Patent number: 6608070Abstract: This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein Z is OH, C1-6 alkoxy, —NR2R3 or heterocycle; Q is selected from the following: (a) an optionally substituted phenyl, (b) an optionally substituted 6-membered monocyclic aromatic group containing one, two, three or four nitrogen atom(s), (c) an optionally substituted 5-membered monocyclic aromatic group containing one heteroatom selected from O, S and N and optionally containing one, two or three nitrogen atom(s) in addition to said heteroatom, (d) an optionally substituted C3-7 cycloalkyl and (e) an optionally substituted benzo-fuzed heterocycle; R1 is hydrogen, C1-4 alkyl or halo; R2 and R3 are independently hydrogen, OH, C1-4 alkoxy, C1-4 alkyl or C1-4 alkyl substituted with halo, OH, C1-4 alkoxy or CN; X is independently selected from H, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, OH, C1-4 alkoxy, halo-substituted C1-4 alkoxy, C1-4 alkylthio, NO2, NH2, di-(C1-4 alType: GrantFiled: July 28, 1999Date of Patent: August 19, 2003Inventors: Kazunari Nakao, Rodney William Stevens, Kiyoshi Kawamura, Chikara Uchida, Hiroki Koike, Stephane Caron
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Publication number: 20030153551Abstract: The invention provides a method for causing regression of ocular neovascularization in a subject by administering an effective amount of a staurosporine derivative to the subject.Type: ApplicationFiled: February 11, 2003Publication date: August 14, 2003Inventor: Romulus Kimbro Brazzell
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Publication number: 20030125343Abstract: This invention relates to combinations of an abl-, PDGF-Receptor-and/or Kit receptor-tyrosine kinase inhibitor with an organic compound capable of binding to &agr;1-acidic glycoprotein (AGP), as well as to pharmaceutical preparations and/or therapies, in relation to disease states which respond to inhibition of abl-, PDGF-Receptor- and/or Kit-receptor tyrosine kinase. In particular, the invention relates to products or combinations comprising and abl-, PDGF-Receptor- and/or Kit receptor-tyrosine kinase inhibitor with an organic compound capable of binding to AGP, either in fixed combination or for chronologically staggered or simultaneous administration, and the combined used of both classes of compounds, either in fixed combination or for chronologically staggered or simultaneous administration, for the treatment of proliferative diseases, especially tumor diseases, especially those that can be treated by inhibition of abl-, PDGF-Receptor- and/or Kit receptor-tyrosine kinase activity.Type: ApplicationFiled: October 7, 2002Publication date: July 3, 2003Inventors: Carlo Gambacorti-Passerini, Philipp Lecoutre
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Publication number: 20030119811Abstract: Compounds represented by Formula (I): 1Type: ApplicationFiled: April 2, 2002Publication date: June 26, 2003Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
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Publication number: 20030119812Abstract: The invention provides methods for decreasing or attenuating an increase in capillary permeability in a subject in need of treatment by administering a composition comprising an amount of a staurosporine derivative or salt thereof to a subject suffering from excessive or pathological capillary permeability in the retina effective to decrease the permeability of the retinal capillaries of the subject.Type: ApplicationFiled: November 4, 2002Publication date: June 26, 2003Inventors: Romulus Kimbro Brazzell, Peter Anthony Campochiaro, Kenneth Green, Frances Elizabeth Kane
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Patent number: 6579868Abstract: The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonistic action. A purine compound represented by the formula (I), its pharmacologically acceptable salt or hydrates thereof has an adenosine A2 receptor antagonistic action and is useful for prevention or therapy of diabetes mellitus and diabetic complications. In addition, adenosine A2 receptor antagonists having different structures from those of the compounds described above, for example KW6002, are also effective for prevention or therapy of diabetes mellitus and diabetic complications. In the formula, W is —CH2CH2—, —CH═CH— or —C≡C—; R1 is: (in the formula, X is hydrogen atom, hydroxyl group, a lower alkyl group, a lower alkoxy group, etc.Type: GrantFiled: July 5, 2000Date of Patent: June 17, 2003Assignee: Eisai Co., Ltd.Inventors: Osamu Asano, Hitoshi Harada, Yorihisa Hoshino, Seiji Yoshikawa, Takashi Inoue, Tatsuo Horizoe, Nobuyuki Yasuda, Kaya Nagata, Junsaku Nagaoka, Manabu Murakami, Seiichi Kobayashi
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Publication number: 20030087892Abstract: This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ═O, —O(CH2)pO— or —S(CH2)pS—; W1 is either O or S; X1 and X2 are both H, or together are ═O or ═S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants.Type: ApplicationFiled: May 23, 2002Publication date: May 8, 2003Inventors: Doreen Mary Ashworth, Gary Robert William Pitt, Peter Hudson, Chritpoher Martyn Yea, Richard Jeremy Franklin
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Patent number: 6559155Abstract: Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA2 and thereof use in treating inter alia atherosclerosis, in which: R1 is COOH or a salt thereof, COOR10, CONR11R12, CN or CH2OH; R2 is a mono- or bicyclic aromatic ring system or a mono- or bicyclic heteroaromatic ring system; R3 is C1-20alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-5alkyl, C1-10alkoxyC1-10alkyl, or an aromatic or heteroaromatic ring system; W is SO2 or a bond; X is O or S; and Y is a group of the formula A1—A2—A3 in which A1 and A3 each represent a bond or a straight chain or branched alkylene group, said alkylene group(s) containing a total of 1 to 10 carbon atoms and A2 represents a bond or O, S, SO, SO2, CO, C═CH2, CONH, NHCO, CR15R16, CH═CH or C═C, providing that when A2 is O, S, SO, SO2 or CONH, A3 contains at least two carbon atoms linking the A2 group and the CH2 group in formula (I).Type: GrantFiled: February 21, 2001Date of Patent: May 6, 2003Assignee: SmithKline Beecham p.l.c.Inventors: Colin Andrew Leach, Stephen Allan Smith
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Patent number: 6548506Abstract: Novel 1,8-benzo-naphthyridine derivatives of general formula (I): which are useful as antimicrobial agents.Type: GrantFiled: June 20, 2001Date of Patent: April 15, 2003Assignee: Aventis Pharma S.A.Inventors: Jean-François Desconclois, Guy Picaut, Philippe Girard, Michel Tabart, Sylvie Wentzler
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Publication number: 20030060457Abstract: The invention relates to the identification of cdk inhibitors as inhibitors of gene expression, replication and reactivation in pathogenic agents.Type: ApplicationFiled: December 6, 2000Publication date: March 27, 2003Inventors: Priscilla A. Schaffer, Luis M. Schang
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Publication number: 20030045516Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation.Type: ApplicationFiled: August 13, 2002Publication date: March 6, 2003Applicant: Millennium Pharmaceuticals, Inc.Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Hiroki Sone, Osamu Kotera, Geraldine C. B. Harriman
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Publication number: 20030013701Abstract: Use of the compound represented by general formula (I) for remedies of and protection against eye diseases is disclosed.Type: ApplicationFiled: August 26, 2002Publication date: January 16, 2003Inventors: Katsuhiko Nakata, Masaaki Kageyama
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Publication number: 20030013874Abstract: A compound of the having the general formula (I) or general formula (II): 1Type: ApplicationFiled: April 18, 2002Publication date: January 16, 2003Inventors: R. Richard Goehring, Zhengming Chen, John Whitehead, Parviz Gharagozloo, Sam Victory, Donald Kyle
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Patent number: 6503898Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: wherein R22 and R23 are allyl.Type: GrantFiled: July 10, 1998Date of Patent: January 7, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Yuk-Sun Lam, Prabhakar Kondaji Jadhav, Charles Joseph Eyermann, Carl Nicholas Hodge, George Vincent De Lucca, James David Rodgers
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Patent number: 6500818Abstract: Compounds having the following formula wherein L, M, R2, R3, R4, R5, R6, R7, X1 and X2 are as defined in the specification, pharmaceutically-acceptable salt thereof, useful for treating depression, anxiety, asthma, rheumatoid arthritis, Alzheimer's disease, cancer, schizophrenia, oedema, allergic rhinitis, inflammation, pain, gastrointestinal-hypermotility, emesis, Huntington's disease, psychoses, hypertension, migraine, bladder hypermotility, or urticaria, compositions including such compounds and processes for making such compounds.Type: GrantFiled: March 30, 2001Date of Patent: December 31, 2002Assignee: Astrazeneca ABInventors: Peter Robert Bernstein, Robert Frank Dedinas, Cyrus John Ohnmacht, Keith Russell
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Patent number: 6482819Abstract: 2,3-Benzodiazepines of formula (I), their stereoisomers and acid addition salts, wherein the variables have the meaning given in the specification, and pharmaceutical compositions containing them which are suitable for treating conditions associated with muscle spasms, epilepsy as well as acute and chronic forms of neurodegenerative diseases are disclosed.Type: GrantFiled: April 10, 2000Date of Patent: November 19, 2002Assignee: Gyogyszerkutato Intezet Kft.Inventors: Gizella Ábrahám, Emese Csuzdi, Sándor Sólyom, Pál Berzsenyi, István Tarnawa, Ferenc Andrási, István Ling, Tamás Hámori, Katalin Horváth, Imre Moravcsik, István Pallagi, Antal Simay
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Publication number: 20020169154Abstract: Novel methods and compositions comprising antineoplastic agents and trk tyrosine kinase inhibitors are disclosed. In preferred embodiments, the antineoplastic agents comprise nucleoside analogs, and the trk tyrosine kinase inhibitors comprise indolocarbazoles and indenocarbazoles. The methods and compositions may be suitable for the treatment of cancer, particularly pancreatic cancer.Type: ApplicationFiled: April 3, 2002Publication date: November 14, 2002Applicant: Cephalon, Inc.Inventors: Bruce A. Ruggeri, Susan E. Jones-Bolin
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Patent number: 6476016Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.Type: GrantFiled: July 17, 2001Date of Patent: November 5, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Patent number: 6472385Abstract: Compositions which abrogate DNA damage induced cell cycle arrest thereby enhancing the cell killing activity of DNA damaging anticancer agents for use in the treatment of cancer, and in particular, p53 defective cancers are provided.Type: GrantFiled: August 8, 2000Date of Patent: October 29, 2002Assignee: Trustees of Darmouth CollegeInventors: Alan Eastman, Gordon W. Gribble
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Patent number: 6472386Abstract: A compound of formula (1): wherein A is a single bond, C≡C, CONH or NHCO; W is a carbon atom or a nitrogen atom; X is CH, a nitrogen atom, an oxygen atom or a sulfur atom; Y is CH, CHR1, in which R1 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy-lower-alkyl, aryl, aryl-lower-alkyl or heteroaryl-lower-alkyl group, a nitrogen atom, an oxygen atom, a sulfur atom or NR2, in which R2 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy-lower-alkyl, aryl, aryl-lower-alkyl or heteroaryl-lower-alkyl group; Z is a nitrogen atom, an oxygen atom, a sulfur atom, CH or NR3, in which R3 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy-lower-alkyl, aryl, aryl-lower-alkyl or heteroaryl-lower-alkyl group; m is 1 or 2; and n is a number of 1 to 5, with the proviso that one or two of W, X, Y and Z are heteroatoms; an acid-addition salt thereof, or a hydrate thereof.Type: GrantFiled: June 29, 2001Date of Patent: October 29, 2002Assignee: Kowa Co., Ltd.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Takeshi Doi, Yoshinori Kyotani
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Publication number: 20020137693Abstract: Many human conditions, often skin conditions, are treated topically or orally with a retinoid such as retinoic acid or acetretin, which treatment often has the side effect of dry, irritated, and/or peeling skin. The use of soaps, detergents, chemical irritants, and such can also cause these same side effects. These side effects can be reduced or eliminated by the topical administration of an inhibitor, especially a natural inhibitor, of the epidermal growth factor receptor (EGFR), administered concomitantly with the retinoid, separately from the retinoid (such as on an as needed basis), or both. Administration of the two together is facilitated by a composition suitable for topical application and comprising both the retinoid and a natural EGFR inhibitor. Preferred natural inhibitors are genistein and other isoflavones extracted from natural occurring substances, or simple derivatives of such substances.Type: ApplicationFiled: February 27, 2002Publication date: September 26, 2002Inventors: Sewon Kang, Gray J. Fisher, John J. Voorhees
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Patent number: 6451787Abstract: Use of the compound represented by general formula (I) for remedies of and protection against eye diseases is disclosed. General formula (I): (wherein, R1 and R2 independently represent a lower alkyl group, R3 and R4 independently represent a hydrogen atom or a lower alkyl group).Type: GrantFiled: June 11, 2001Date of Patent: September 17, 2002Assignees: Cephalon, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Katsuhiko Nakata, Masaaki Kageyama
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Patent number: 6451786Abstract: Compounds defined by the following general structure are disclosed: These compounds display pharmacological activities, including inhibition of tyrosine kinase activity and enhancement of the function and/or survival of trophic factor responsive cells, e.g., cholinergic neurons.Type: GrantFiled: February 15, 2000Date of Patent: September 17, 2002Assignees: Cephalon, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Robert L. Hudkins, Diane E. Gingrich
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Patent number: 6448271Abstract: Compounds of the formula Ia or IB where A is a saturated or monounsaturated heterocyclic, 4- to 8-membered ring which contains one or two nitrogen atoms, and their tautomeric forms, possible enantiomeric and diastereomeric forms, their prodrugs and possible physiologically tolerated salts are useful as inhibitors of the enzyme poly(ADP-ribose)polymerase.Type: GrantFiled: May 24, 2001Date of Patent: September 10, 2002Assignee: BASF AktiengesellschaftInventors: Wilfried Lubisch, Michael Kock, Thomas Höger, Sabine Schult, Roland Grandel, Reinhold Müller
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Publication number: 20020115706Abstract: Methods for preventing or treating damage to sensory hair cells and cochlear neurons are disclosed. The methods comprise the administration of an effective amount of a compound of Formula I or Formula II. The method provides for the prevention/treatment of both hearing loss and loss of the sense of balance.Type: ApplicationFiled: January 8, 2002Publication date: August 22, 2002Inventors: Jukka Ylikoski, Ulla Pirvola, Mart Saarma, Kevin M. Walton, Robert L. Hudkins
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Patent number: 6436943Abstract: The invention relates to dihydropyrimidines of the general formula and to the use of dihydropyrimidines as medicaments for the treatment and prophylaxis of hepatitis B. The invention further relates to a process for the preparation of medicaments comprising the corresponding dihydropyrimidines.Type: GrantFiled: October 18, 2000Date of Patent: August 20, 2002Assignee: Bayer AktiengesellschaftInventors: Jürgen Stoltefuss, Siegfried Goldmann, Arnold Paessens, Erwin Graef, Stefan Lottmann
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Publication number: 20020107237Abstract: The present invention relates to novel N12, N13-bridged sugar derivatives of indolylopyrrolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful in inhibiting the proliferation of tumor cells.Type: ApplicationFiled: September 27, 2001Publication date: August 8, 2002Inventors: Mark G. Saulnier, Edward H. Ruediger, Neelakantan Balasubramanian, Mikael Mahler, Francis Beaulieu, Carol Bachand, David B. Frennesson
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Publication number: 20020107238Abstract: There is provided a pharmaceutical composition suitable for topical administration to an eye, the composition comprising as active agent at least one oxazolidinone antibacterial drug, for example linezolid, in a concentration effective for treatment and/or prophylaxis of a gram-positive bacterial infection of an eye, and at least one ophthalmically acceptable excipient ingredient that reduces a rate of removal of the composition from the eye by lacrimation such that the composition has an effective residence time in the eye of about 2 to about 24 hours. The composition is, for example, an in situ gellable solution, suspension or solution/suspension.Type: ApplicationFiled: October 10, 2001Publication date: August 8, 2002Inventors: Rebanta Bandyopadhyay, Pamela J. Secreast, Leslie C. Hawley, Vincent E. McCurdy, Praveen Tyle, Paramita Bandyopadhyay, Satish Kumar Singh
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Patent number: 6423751Abstract: A use for agents that disrupt actin cytoskeletal organization is provided. In the instant invention, agents that disrupt actin cytoskeletal organization are found to upregulate endothelial cell Nitric Oxide Synthase activity. As a result, agents that disrupt actin cytoskeletal organization are useful in treating or preventing conditions that result from the abnormally low expression and/or activity of endothelial cell Nitric Oxide Synthase. Such conditions include pulmonary hypertension, ischemic stroke, impotence, heart failure, hypoxia-induced conditions, insulin deficiency, progressive renal disease, gastric or esophageal motility syndrome, etc. Subjects thought to benefit mostly from such treatments include nonhyperlipidemics and nonhypercholesterolemics, but not necessarily exclude hyperlipidemics and hypercholesterolemics.Type: GrantFiled: July 14, 1998Date of Patent: July 23, 2002Assignee: The Brigham and Women's Hospital, Inc.Inventor: James K. Liao
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Patent number: 6395740Abstract: Compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. Included among the calcitonin mimetics of the present invention are substituted piperazines. The calcitonin mimetics of the present invention are also useful in libraries and in assays for the determination of calcitonin receptor activity.Type: GrantFiled: July 14, 2000Date of Patent: May 28, 2002Assignee: ZymoGenetics, Inc.Inventors: Nand Baindur, Virender Labroo, Steven Stroop, Stephanie Beigel, Theresa Martinez, Charles R. Petrie, Mark W. Orme, Patricia A. Mckernan, Emma E. Moore
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Publication number: 20020061873Abstract: Spontaneously dispersible N-benzoyl-staurosporine compositions are discussed for oral administration having high bioavailability levels and reduced variability of bioavailability levels of N-benzoyl-staurosporine, as well as their preparation and use in medical treatment.Type: ApplicationFiled: August 15, 2001Publication date: May 23, 2002Inventors: Graham Paul Matthews, Barbara Haeberlin
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Publication number: 20020058645Abstract: The invention relates to compounds of formula I 1Type: ApplicationFiled: June 22, 2001Publication date: May 16, 2002Inventors: Laszlo Vertesy, Klaus Ehrlich, Michael Kurz, Joachim Wink
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Patent number: 6387912Abstract: Use of pyrimidine derivatives of the formula I where the substituents are as defined in the description, and of their physiologically tolerated salts for producing medicaments for the prophylaxis and treatment of cerebral ischemia and strokes.Type: GrantFiled: July 11, 2001Date of Patent: May 14, 2002Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Kurt Schellhaas, Wilfried Lubisch, Uta Holzenkamp, Dorothea Starck, Monika Knopp, Laszlo Szabo, Franz Emling, Francisco Javier Garcia-Ladona, Hans-Peter Hofmann, Liliane Unger
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Patent number: RE38332Abstract: Esters of hydroxyl-containing indolocarbazoles and acids containing selected solubilizing groups are provided. Compositions including the indolocarbazole esters and methods for the use of the indolocarbazole esters are also provided.Type: GrantFiled: March 19, 2001Date of Patent: November 25, 2003Assignees: Cephalon, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: John P. Mallamo, Robert L. Hudkins