C=o Bonded Directly To The Hetero Ring (x Is Chalcogen) Patents (Class 514/448)
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Publication number: 20080207741Abstract: Pharmaceutical compositions comprising at least one compound of the formula (I) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning —X— is e.g. and Y being e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.Type: ApplicationFiled: September 20, 2006Publication date: August 28, 2008Applicant: REVOTAR BIOPHARMACEUTICALS AGInventors: Ewald M. Aydt, Remo Kranich
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Publication number: 20080171741Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: October 25, 2007Publication date: July 17, 2008Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
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Publication number: 20080153850Abstract: The invention provides compounds of formula (I) pharmaceutically acceptable salt or solvate thereof, in which R1, A1, m and A are as defined in the specification; a process for their preparation; pharmaceutical compositions containing them; and their use in therapy.Type: ApplicationFiled: August 29, 2005Publication date: June 26, 2008Applicant: AstraZeneca ABInventors: Rhonan Ford, Barrie Martin, Toby Thompson, Nicholas Tomkinson, Paul Willis
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Publication number: 20080139640Abstract: Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the In preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: ApplicationFiled: June 13, 2005Publication date: June 12, 2008Inventors: Georg Fertig, Frank Herting, Matthias Koerner, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Ulrich Tibes
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Patent number: 7378448Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosedType: GrantFiled: March 2, 2005Date of Patent: May 27, 2008Assignee: Eli Lilly and CompanyInventors: Charles Howard Mitch, Steven James Quimby, Miles Goodman Siegel
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Patent number: 7375131Abstract: The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-? phosphorylation of I?B. In so doing these aminothiophene inhibitors block pathological activation of transcription factor NF-?B in which diseases excessive activation of NF-?B is implicated.Type: GrantFiled: May 29, 2003Date of Patent: May 20, 2008Assignee: SmithKlineBeecham Corp.Inventors: James F. Callahan, Yue Hu Li
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Patent number: 7365070Abstract: This invention provides compounds and methods for treating melanocortin receptor associated disorders, such as weight loss disorders including cachexia resulting from cancer and other chronic illnesses. The compounds are represented by formula I: wherein X is oxygen or sulfur; G is G1 or G2: L1, L2, L3 and Q are linker groups, and Rings A, B and C, and R1-R14 are described in the specification. The compounds are antagonists of melanocortin receptors.Type: GrantFiled: December 4, 2003Date of Patent: April 29, 2008Assignee: Ore Pharmaceuticals Inc.Inventors: Tricia J. Vos, Michael Patane, Michael E. Solomon, Christopher Blackburn, Mihaela D. Danca
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Patent number: 7365094Abstract: The present invention relates to compounds of the general formula (II) and salts and physiologically functional derivatives thereof, for the use as a medicament.Type: GrantFiled: December 17, 2003Date of Patent: April 29, 2008Assignee: 4SC AGInventors: Johann Leban, Stefan Tasler
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Publication number: 20080085924Abstract: This invention relates to novel biphenylcarboxamides of the formula (I) in which R, Z, X, Y, m, n and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: ApplicationFiled: December 1, 2003Publication date: April 10, 2008Applicant: BAYER CROPSCINCE AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wachendorff-Neumann, Peter Dahmen, Peter Losel, Karl-Heinz Kuck, Astrid Mauler-Machnik, Jorg Nico Greul
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Patent number: 7351841Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13 SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: GrantFiled: December 6, 2005Date of Patent: April 1, 2008Assignee: Nissan Chemical Industries, Ltd.Inventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
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Publication number: 20080058389Abstract: The invention relates to novel carboxamides of formula (I), in which M represents a phenyl ring, pyridine ring or pyrimidine, pyridazine or pyrazine ring, respectively monosubstituted by R8, or represents a thiazole ring substituted by R8-A; R8 represents hydrogen, fluorine, chlorine, methyl, isopropyl, methylthio or trifluoromethyl; R8 can also represent methoxy; R8-A represents hydrogen, methyl, methylthio or trifluoromethyl; L1 represents C1-C10 alkene (alkanediyl); Q represents O, S, SO, SO2 or NR9; L2 represents a direct bond, SiR10R11 or CO; R represents hydrogen, C1-C8 alkyl, C1-C8 alkoxy, C1-C4 alkoxy-C1-C4-alkyl, C1-C4 alkylthio-C1-C4-alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C1-C6 haloalkyl, C2-C6-haloalkenyl, C2-C6 haloalkynyl or C3-C6 cycloalkyl; A represents the group of formula (AI); the remaining substituents are defined in claim 1.Type: ApplicationFiled: January 22, 2005Publication date: March 6, 2008Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Benoit Hartmann, Jorg Nico Greul, Stefan Herrmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
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Patent number: 7332518Abstract: The invention concerns novel carboxamides of formula (I) wherein A is (A1), (A2), (A3), (A4), (A5); Q is (Q1), (Q2), (Q3), (Q4), (Q5), (Q6); R1 is CH2 R2, CH2CH?CHR2, CH?C?CHR2 or COR3; R2 is hydrogen, C1-C6alkyl, C1-C6haloalkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C7cycloalkyl, COOC1-C4alkyl, COOC3-C6alkenyl, COOC3-C6alkynyl or CN; R3 is C1-C6alkyl, C1-C6alkyl substituted by halogen, C1-C6alkoxy or C1-C6haloalkoxy; or is C1-C6alkylthio, C1-C6haloalkylthio, C1-C6alkoxy, C1-C6haloalkoxy; C3-C6alkenyloxy or C3-C6haloalkenyloxy; C3-C6haloalkenyloxy; C3-C6alkynyloxy or C3-C6haloalkynyloxy; R4 is methyl, CF2Cl, CF3, CF2H, CFH2, Cl or Br, R5 is methyl, CF3, CH2OCH3 or CH2OCF3; R6 is hydrogen, fluoro, CF3 or methyl; R7 is hydrogen, methyl or halogen; and Z is phenyl, halophenyl, C5-C7cycloalkyl, C5-C7cycloalkyl substituted by C1-C3alkyl, C1C3haloalkyl or halogen, or a group of the form —CHR8—CH2—CHR9R10 wherein R8, R9 and R10 are independently of each other C1-C3alkyl.Type: GrantFiled: January 24, 2002Date of Patent: February 19, 2008Assignee: Syngenta Crop Protection, Inc.Inventors: Harald Walter, Stephan Trah
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Patent number: 7332513Abstract: Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or decreased. Also disclosed are methods of preparing such NO-donating compounds, pharmaceutical compositions and medical devices containing such compounds and methods utilizing such compounds in the treatment of various medical conditions.Type: GrantFiled: November 4, 2005Date of Patent: February 19, 2008Assignee: Renopharm Ltd.Inventors: Peter Assaf, Elham Gazaleen-Mariee, Michael Naveh
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Patent number: 7332516Abstract: The present invention encompasses compounds of Formula I (I) or pharmaceutically acceptable salts thereof, wherein A is the base molecule of a propionic acid or acetic acid NSAID, or a derivative thereof, X is —CO2H, 1H-tetrazol-5-yl or 2H-tetrazol-5-yl and R1 and R2 are each independently selected from the group consisting of: C1-6alkyl and C3-6cycloalkyl, as well as pharmaceutical composition comprising said compounds and methods of using said compounds. The compounds of the present invention lower the level of A?42 and are therefore useful for preventing, delaying or reversing the progression of Alzheimer's Disease.Type: GrantFiled: January 9, 2004Date of Patent: February 19, 2008Assignee: Merck + Co., Inc.Inventors: Benito Munoz, Petpiboon Prasit, Nicholas Simon Stock
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Publication number: 20080015219Abstract: Disclosed and described herein are compounds of the formula or a pharmaceutically acceptable salt thereof, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed and described.Type: ApplicationFiled: May 14, 2007Publication date: January 17, 2008Inventors: DAVID W. OLD, VINH X. NGO
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Publication number: 20080015231Abstract: A compound having a formula is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: July 10, 2007Publication date: January 17, 2008Inventors: David W. Old, Vinh X. Ngo
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Patent number: 7317034Abstract: Substituted C-furan-2-yl-methylamine and C-thiophen-2-yl-methylamine compounds, processes for their preparation, medicaments and pharmaceutical compositions containing them, and their use in treatment methods and in the preparation of analgesics, in the preparation of a local anaesthetic, an antiarrhythmic, an antiemetic, a nootropic agent and/or a medicament for the treatment and/or prophylaxis of cardiovascular diseases, urinary incontinence, diarrhea, pruritus and/or inflammations, and/or a medicament for the treatment of depression and/or alcohol and/or drug and/or medicament abuse, and/or a medicament for increasing vigilance.Type: GrantFiled: March 7, 2005Date of Patent: January 8, 2008Assignee: Gruenenthal GmbHInventors: Corrina Sundermann, Michael Przewosny
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Patent number: 7317125Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: January 31, 2006Date of Patent: January 8, 2008Assignee: Hoffman-La Roche Inc.Inventors: David Robert Bolin, Christophe Michoud
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Patent number: 7291647Abstract: The present invention relates to compounds having the formula: salts thereof; compositions comprising one or more of the compounds and/or salts thereof; methods of using; and methods of making.Type: GrantFiled: August 17, 2005Date of Patent: November 6, 2007Assignee: Cytokine Pharmasciences, Inc.Inventor: Thais Sielecki-Dzurdz
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Patent number: 7259172Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: July 2, 2004Date of Patent: August 21, 2007Assignee: MethylGene Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 7244763Abstract: This invention relates to compounds that alter PPAR activity. The invention also relates to pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing dyslipidemia, hypercholesterolemia, obesity, hyperglycemia, atherosclerosis, hypertriglyceridemia and hyperinsulinemia in a mammal. The present invention also relates to methods for making the disclosed compounds.Type: GrantFiled: February 6, 2004Date of Patent: July 17, 2007Assignee: Warner Lambert Company LLCInventors: Larry D. Bratton, Xue-Min Cheng, Noe Erasga, Gary F. Filzen, Andrew G. Geyer, Chitase Lee, Bharat K. Trivedi, Paul C. Unangst
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Patent number: 7173060Abstract: The present invention relates to compounds of formula I, their pharmaceutically acceptable salts as well as their enantiomeric forms, diastereoisomers and racemates; the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds as inhibitors of histone deacetylase (HDAC) and therefore in the control or prevention of illnesses and disorders as mentioned above, or in the manufacture of corresponding pharmaceutical compositions.Type: GrantFiled: March 31, 2004Date of Patent: February 6, 2007Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
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Patent number: 7169768Abstract: A method of decreasing atherosclerosis and its complications including but not limited to myocardial infarction, stroke and peripheral vascular disease wherein the method involves administering to a human or an animal an amount of an inhibitor of the release of LHRH or GnRH.Type: GrantFiled: June 3, 1998Date of Patent: January 30, 2007Inventors: Kenneth M. Weisman, Michael Goldberg
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Patent number: 7166590Abstract: A compound of the formula (I): [wherein R1 is (substituted) alkyl, alkoxy, phenyl, hetero ring etc.; A is bond, CO, SO2; R2 is H, (substituted) alkyl etc.; D is alkylene etc.; E is COO, OCO, O, S, SO, SO2 etc.; R3 is (substituted) alkyl, carbocyclic ring, hetero ring; J is O, NR16 (R16 is H, substituted alkyl); R4 is (substituted) alkyl, carbocyclic ring, hetero ring.] or non-toxic salt thereof, and an N-type calcium channel blocker comprising it as an active ingredient. The compounds of the formula (I) possess an inhibitory action on N-type calcium channel, so they are useful as agent for the prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis or epilepsy etc. or agent for the treatment of pain.Type: GrantFiled: May 28, 2002Date of Patent: January 23, 2007Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Masashi Kato
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Patent number: 7160910Abstract: The provides compounds for the treatment of sickle-cell disease. In particular, the invention provides 5-membered heterocyclic anti-sickling agents that are highly effective and non-toxic, and methods for their use. The compounds include analogues and derivatives of naturally occurring occurring 5-hydroxymethyl-2-furfuraldehyde, 5-Ethyl-2-furfuraldehyde, 5-Methyl-2-furfuraldehyde, and 2-furfuraldehyde, and prodrug forms of the compound.Type: GrantFiled: December 3, 2003Date of Patent: January 9, 2007Assignee: Xechem International, Inc.Inventors: Martin K. Safo, Richmond Danso-Danquah, Samuel Nokuri, Faik N. Musayev, Gajanan S. Joshi, James C. Burnett, Donald J. Abraham
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Patent number: 7125908Abstract: The present invention provides methods of treating chronic pain in a mammal by administering to the mammal an effective amount of a selective persistent sodium channel antagonist that has at least 20-fold selectivity for persistent sodium current relative to transient sodium current.Type: GrantFiled: August 27, 2004Date of Patent: October 24, 2006Assignee: Allergan, Inc.Inventors: George R. Ehring, Joseph S. Adorante, John E. Donello, Larry A. Wheeler, Thomas Malone
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Patent number: 7115654Abstract: The invention provides compounds of Formula I and derivatives thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of treatment utilizing such compounds and compositions: wherein: R1 is chosen from optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl; L is a linker; R2 is chosen from optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl; and or single stereoisomers, mixtures of stereoisomers, or the pharmaceutically acceptable salts, amides, or esters thereof.Type: GrantFiled: June 5, 2003Date of Patent: October 3, 2006Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Darin Allen, Bruce Fahr, Johan Oslob, Brian C. Raimundo, Michael J. Romanowski
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Patent number: 7109243Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: GrantFiled: March 23, 2004Date of Patent: September 19, 2006Assignee: IRM LLCInventors: Hong Liu, David Tully, Robert Epple, Badry Bursulaya, Jennifer Williams, Arnab Chatterjee, Jennifer Leslie Harris, Jun Li
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Patent number: 7105564Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.Type: GrantFiled: March 2, 2000Date of Patent: September 12, 2006Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Akinori Arimura
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Patent number: 7098241Abstract: The (R) and (S) enantiomers of a compound of formula I are novel antiproliferative therapeutic agents. These compounds have HDAC inhibitor activity and are useful in the treatment of cancer. Also disclosed are methods of making and using compounds of formula (I), as well as pharmaceutical compositions containing compounds of formula (I).Type: GrantFiled: December 10, 2003Date of Patent: August 29, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Adelbert Grossmann, Frank Herting, Matthias Koerner, Klaus-Peter Kuenkele, Anja Limberg, Olaf Mundigl, Ulrich Tibes
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Patent number: 7094911Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.Type: GrantFiled: October 31, 2002Date of Patent: August 22, 2006Assignee: Bayer AktiengesellschaftInventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
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Patent number: 7067542Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: July 10, 2002Date of Patent: June 27, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Heinrich Josef Schostarez, Robert A. Chrusciel
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Patent number: 7060723Abstract: The present invention provides methods of treating neurological disorders in a mammal by administering to the mammal an effective amount of a selective persistent sodium channel antagonist that has at least 20-fold selectivity for persistent sodium current relative to transient sodium current.Type: GrantFiled: August 27, 2004Date of Patent: June 13, 2006Assignee: Allergan, Inc.Inventors: George R. Ehring, Joseph S. Adorante, Larry A. Wheeler, Thomas Malone, Scott M. Whitcup
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Patent number: 7053094Abstract: Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: January 20, 2005Date of Patent: May 30, 2006Assignee: Cytokinetics, Inc.Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans, Jr.
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Patent number: 7053109Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: July 10, 2002Date of Patent: May 30, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Heinrich Josef Schostarez, Robert Alan Chrusciel
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Patent number: 7041702Abstract: The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.Type: GrantFiled: October 20, 1998Date of Patent: May 9, 2006Assignee: Scion Pharmaceuticals, Inc.Inventors: Graham J. Durant, Seetharamaiyer Padmanabhan
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Patent number: 7034053Abstract: The present invention disclosed compounds of Formula I. The present invention also discloses beta-3 agonists of formula I and methods for treating beta-3 mediated diseases and condition using the compounds of formula I, in particular methods for treating diabetes or obesity.Type: GrantFiled: December 17, 2001Date of Patent: April 25, 2006Assignee: SmithKline Beecham CorporationInventors: David N. Deaton, Barry George Shearer, David Edward Uehling
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Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 6992047Abstract: A method of producing a controlled release form of an agricultural active material includes the provision of an organic liquid composition in which the active is present, but where the liquid composition is free from aromatic solvents and is maintained below the normal melting point of the active. The liquid composition is formed into small droplets and the droplets are enclosed by a non-water soluble shell to provide microcapsules, the shell of which is designed to release the agricultural active at a pre-selected controlled rate when the microcapsule is exposed to natural environmental conditions. Controlled release forms of agricultural actives are also provided.Type: GrantFiled: April 3, 2002Date of Patent: January 31, 2006Assignee: Monsanto Technology LLCInventors: Jawed Asrar, Yiwei Ding
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Patent number: 6982279Abstract: Compounds of the formulae IA and Ib. in which X, R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(30) and R(31) have the meanings indicated in the claims, are very particularly suitable as novel antiarrhythmic active compounds, in particular for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.Type: GrantFiled: December 12, 2001Date of Patent: January 3, 2006Assignee: Aventis Pharm Deutschland GmbHInventors: Stefan Peukert, Joachim Brendel, Horst Hemmerle, Heinz-Werner Kleemann
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Patent number: 6960594Abstract: A novel compound which inhibits certain integrins, particularly ?v integrins. Additionally, the novel compound may be used in a method of treating tumors or cancer which comprises administering a pharmaceutically effective amount of the compound to a patient. Additionally, the novel compound may be used in a method of inhibiting angiogensis. Finally, a method of producing the novel compound is disclosed.Type: GrantFiled: January 16, 2002Date of Patent: November 1, 2005Assignee: Shire BioChem Inc.Inventors: Denis Labrecque, Serge Lamothe, Marc Courchesne, Laval Chan, Giorgio Attardo, Karen Meerovitch
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Patent number: 6953812Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism, such as dyslipidemia, and obesity.Type: GrantFiled: February 24, 2003Date of Patent: October 11, 2005Assignee: Novo Nordisk, Inc.Inventors: Anker Steen Jorgensen, Inge Thoger Christensen, Janos Tibor Kodra, Christian Sams, Carsten Behrens, Peter Madsen, Jesper Lau
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Patent number: 6933317Abstract: Compounds of the general formula (I) which are metabolically stable and have an antagonistic activity against PGD2 receptor: ? wherein Y is bicyclic ring; R1 is optionally substituted heteroaryl; R2 is hydrogen, etc.; R3 is —CH2—CH2—CH2—CH2—CH?CH—COOR4, —CH2—CH2—CH2—CH2—X1—CH2—COOR4, —CH2—CH?CH—CH2—X1—CH2—COOR4 or —CH2—CH2—CH2—COOR4; R4 is hydrogen, etc.; X1 is —O—, etc.Type: GrantFiled: October 26, 2001Date of Patent: August 23, 2005Assignee: Shionogi & Co. Ltd.Inventors: Norihiko Tanimoto, Yoshiharu Hiramatsu, Tsunetoshi Honma, Masanao Inagaki
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Patent number: 6908923Abstract: Certain substituted benzamide derivatives of Formula I: selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: December 20, 2002Date of Patent: June 21, 2005Assignee: Cytokinetics, Inc.Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans, Jr.
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Patent number: 6906086Abstract: The current invention provides methods and pharmaceutical formulations that are useful for inhibiting the loss of bone. These methods and formulations can be used without the associated adverse effects of estrogen therapy, and thus serve as an effective and acceptable treatment for osteoporosis.Type: GrantFiled: May 27, 2003Date of Patent: June 14, 2005Assignee: Eli Lilly and CompanyInventor: Larry J. Black
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Patent number: 6887903Abstract: The compounds of formula 1 wherein R and R2 are as defined in the disclosure, are useful in the prevention and treatment of tissue damage due to exacerbated recruitment of polymorphonuclear neutrophils (PMN leukocytes) at the inflammatory sites.Type: GrantFiled: October 14, 1999Date of Patent: May 3, 2005Assignee: Dompe S.p.A.Inventors: Riccardo Bertini, Cinzia Bizzarri, Vilma Sabbatini, Gianfranco Caselli, Marcello Allegretti, Maria Candida Cesta, Carmelo Gandolfi, Marco Mantovanini, Francesco Colotta, Stefano Porzio
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Patent number: 6878743Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein A, B, D, E, G, J, n, and R1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof as caspase inhibitors and for the treatment of disorders caused by excessive apoptotic activity.Type: GrantFiled: September 17, 2002Date of Patent: April 12, 2005Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Ingrid Choong, Matthew Burdett, Warren DeLano, Daniel Erlanson, Dennis Lee, Willard Lew
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Patent number: 6878706Abstract: Compounds according to the following formula (I): wherein the variables Q and R1 to R6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F, L and B; pharmaceutical compositions containing such compounds, and method of treating diseases and pathological conditions exacerbated by these cysteine proteases such as, but not limited to rheumatoid arthritis, multiple sclerosis and other autoimmune diseases, osteoporosis, asthma, Alzheimer's disease, atherosclerosis and endometriosis.Type: GrantFiled: March 27, 2003Date of Patent: April 12, 2005Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Thomas A. Gilmore, Eugene Richard Hickey, Weimin Liu, Peter Allen Nemoto, Denice M. Spero
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Patent number: RE38761Abstract: A method of inhibiting cell proliferation in a patient suffering from such disorder comprising administering to said patient an effective amount of a composition comprising, in admixture with a pharmaceutically acceptable carrier, a compound, or a pharmaceutically acceptable salt thereof, which is a substituted styrene compound which can also be a naphthalene, an indane or a benzoxazine; including nitrile and molononitrile compounds, and pharmaceutical compositions comprising, in admixture with a pharmaceutically acceptable carrier, a pharmaceutically-effective amount of such compound.Type: GrantFiled: October 14, 1994Date of Patent: July 19, 2005Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Alexander Levitzki, Chaim Gilon, Michael Chorev, Aviv Gazit
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Patent number: RE39049Abstract: The current invention provides methods and pharmaceutical formulations that are useful for inhibiting the loss of bone. These methods and formulations can be used without the associated adverse effects of estrogen therapy, and thus serve as an effective and acceptable treatment for osteoporosis.Type: GrantFiled: February 27, 2003Date of Patent: March 28, 2006Assignee: Eli Lilly and CompanyInventors: Larry J. Black, George J. Cullinan