The Additional Hetero Ring Is A Cyclo In A Polycyclo Ring System [e.g., 2-(1-isothiochromanyl)-2-imidazoline Hydrochloride, Etc.] Patents (Class 548/311.4)
-
Publication number: 20070197620Abstract: The present invention relates to a method for treating a disorder selected from depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R1, R2, Q, W, X, Y, m, and n are as defined in the specification d or not; and their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms.Type: ApplicationFiled: January 19, 2007Publication date: August 23, 2007Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
-
Patent number: 7235584Abstract: Novel non-psychotropic cannabinoids are disclosed and pharmaceutical compositions comprising these novel compounds are described for preventing neurotoxicity, neuroinflammation, immune or inflammatory disorders comprising as active ingredient the stereospecific (+) enantiomer, having (3S,4S) configuration of ?6 tetrahydrocannabinol type compounds. The compositions are particularly effective in alleviating and even preventing neurotoxicity due to acute injuries to the central nervous system, including mechanical trauma, compromised or reduced blood supply as may occur in cardiac arrest or stroke, or poisonings. They are also effective in the treatment of certain inflammatory disorders and chronic degenerative diseases characterized by neuronal loss and chronic pain including neuropathic pain.Type: GrantFiled: June 25, 2003Date of Patent: June 26, 2007Assignee: Pharmos CorporationInventors: Aaron Garzon, George Fink
-
Patent number: 7220770Abstract: A class of imidazolyl compounds is described for use in treating inflammation.Type: GrantFiled: July 15, 2005Date of Patent: May 22, 2007Inventors: Ish K. Khanna, Richard M. Weier, Paul W. Collins, Yi Yu, Xiangdong Xu, Richard A. Partis, Francis J. Koszyk, Renee M. Huff
-
Patent number: 7157585Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.Type: GrantFiled: May 11, 2005Date of Patent: January 2, 2007Assignee: Tularik LimitedInventors: Sarah Elizabeth Lively, Bohdan Waszkowycz, Martin James Harrison, Christopher Neil Farthing, Keith Michael Johnson
-
Patent number: 7125904Abstract: Compounds of formula I: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkylaryl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies hydrogen, alkyl or alkylaryl group; X is CH2, O or S, and n is 1, 2 or 3, with the proviso that if X is CH2, n is not 1, and a method for their preparation. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.Type: GrantFiled: October 8, 2003Date of Patent: October 24, 2006Assignee: Portela & C.A., S.A.Inventors: David Alexander Learmonth, Patricio Manuel Viera Araújo Soares da Silva, Alexander Beliaev
-
Patent number: 7119104Abstract: A compound represented by the formula (I) or a salt of the compound, and a PPAR-? activator which contains the compound or salt as the active ingredient: (wherein A represents O or S; B1 represents N, etc.; B2 represents O, etc.; each of X1 and X2 represents O, S, a bond, etc.; Y represents C1-8 alkylene chain; Z represents O or S; R1 represents aryl, etc. which can have substituents; R2 represents C1-8 alkyl, etc.; R3 represents C1-8 alkyl, C2-8 alkenyl, etc.; each of R4 and R5 represents hydrogen, C1-8 alkyl, etc.; and R6 represents hydrogen, etc.; provided that each of Z and R3 is attached to the benzene ring, and X2 is not attached to the benzene ring).Type: GrantFiled: October 9, 2002Date of Patent: October 10, 2006Assignee: Nippon Chemiphar, Co., Ltd.Inventors: Shogo Sakuma, Tomio Yamakawa, Takashi Kanda, Seiichiro Masui
-
Patent number: 7105513Abstract: The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.Type: GrantFiled: July 31, 2003Date of Patent: September 12, 2006Assignee: Sanofi-Avertis Deutschland GmbHInventors: Hartmut Strobel, Paulus Wohlfart
-
Patent number: 7098345Abstract: A process for preparing ondansetron by transamination of an ondansetron structural analog that can be readily prepared conveniently by a Mannich reaction is provided. The process represents an improvement upon known procedures for making ondansetron by transamination because of its rapid rate, selectivity and the ease with which the product can be isolated from the reaction mixture.Type: GrantFiled: April 29, 2003Date of Patent: August 29, 2006Assignee: TEVA Gyógyszergyár Zárkörüen Müködö RészvénytársaságInventors: Sandor Molnar, Csaba Szabo, Erzsebet Meszaros Sos, Szabolcs Salyi, Tivadar Tamas
-
Patent number: 7071220Abstract: The present invention relates to an N-substituted benzothiophenesulfonamide derivative or a pharmaceutically acceptable salt thereof and applications thereof. Furthermore, it provides an agent for preventing or treating cardiac or circulatory disease and so on caused by abnormal increase of production of angiotensin II or endothelin I based on chymase activity, or by activation of mast cell, and an agent for preventing adhesion after surgery, wherein the agent has a selective inhibitory action on chymase.Type: GrantFiled: March 13, 2003Date of Patent: July 4, 2006Assignee: Toa Eiyo Ltd.Inventors: Shoji Satoh, Akira Tatsui, Takeshi Hasegawa, Hideki Yamada, Shin-ichi Kazayama, Takahiro Morita, Hidekazu Masaki, Atsuo Takahashi, Fumiya Yoneyama, Tetsuo Kuze, Yusuke Mizuno, Mizuo Miyazaki, Shinji Takai
-
Patent number: 7067552Abstract: Taxanes containing electron-affinic radiosensitizing functional groups, their pharmaceutical preparations, and methods of making and using this new class of highly potent radiosensitizers of tumor cells.Type: GrantFiled: October 16, 2001Date of Patent: June 27, 2006Assignee: Florida State UniversityInventors: Robert A. Holton, Hossain Nadizadeh, Li-Xi Yang
-
Patent number: 7060721Abstract: Imidazole compounds represented by general formula (I): wherein each symbol is as defined in the specification, and salts thereof, and a pharmaceutical composition containing same are provided. These compounds are useful in treating the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy inhibitory action.Type: GrantFiled: December 20, 1999Date of Patent: June 13, 2006Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Noriko Oku, legal representative, Chikako Oku, legal representative, Tomohito Oku, legal representative, Hiroshi Kayakiri, Yoshito Abe, Hitoshi Hamashima, Hitoshi Sawada, Naoki Ishibashi, Hiroyuki Setoi, Noritsugu Yamasaki, Takafumi Imoto, Takahiro Hiramura, Teruo Oku, deceased
-
Patent number: 7053114Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: April 5, 2004Date of Patent: May 30, 2006Assignee: Sugen, Inc.Inventors: Connie Li Sun, Chung Chen Wei, Peng Cho Tang, Marcel Koenig, Yong Zhou, Tomas Vojkovsky, Asaad S. Nematalla
-
Patent number: 7053223Abstract: The present invention discloses the identification of the novel inhibitors of farnesyl protein transferase and ras protein farnesylation. The compounds and pharmaceutical compositions disclosed herein are useful in treating diseases associated with farnesyl protein transferase, such as cancer.Type: GrantFiled: February 10, 2004Date of Patent: May 30, 2006Assignee: Bristol-Myers Squibb CompanyInventor: Rajeev S. Bhide
-
Patent number: 7041834Abstract: A process useful for making ondansetron that comprises reacting a carbazolone in a reaction mixture comprising a carbazolone of formula (2), a formaldehyde or precursor thereof, and an amine of formula (3) in a non-aqueous polar solvent and in the presence of a water binding agent. The reaction product(s) can be reacted with an amine of formula (5) to form ondansetron.Type: GrantFiled: January 23, 2004Date of Patent: May 9, 2006Assignee: Synthon IP Inc.Inventors: Dusan Hesoun, Jiri Hykl
-
Patent number: 7026357Abstract: Compound of formula (I): and medicinal products containing the same are useful as dual ?2/5-HT2c antagonist receptors.Type: GrantFiled: June 7, 2004Date of Patent: April 11, 2006Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Anne Dekeyne, Mauricette Brocco
-
Patent number: 7019004Abstract: The invention provides compounds of formula (I) wherein X, Y, R1, R2, R3 and R4 are as defined in the description, and the preparation thereof.Type: GrantFiled: May 7, 2001Date of Patent: March 28, 2006Assignee: Novartis AGInventors: Daniel Berney, Robin Breckenridge, Peter Neumann, Gideon Shapiro, Max Peter Seiler, Thomas J. Troxler
-
Patent number: 7015333Abstract: A method for preparing an imidazolyl compound corresponding to the formula (I) by reacting a compound corresponding to formula (II) with a compound corresponding to formula (III) and then reacting the product with a compound corresponding to formula (IV)Type: GrantFiled: November 14, 2003Date of Patent: March 21, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Jan-Maarten Verbeek, Paulus F. C. Van Der Meij
-
Patent number: 6960586Abstract: The present invention provides a compound having a steroid C17,20-lyase inhibitory activity, which is useful as a prophylactic or therapeutic agent of prostatism and tumor such as breast cancer and the like. A compound represented by the formula: wherein R is a hydrogen atom or a protecting group, R1 is a lower alkyl group or a cyclic alkyl group, and ring A and ring B are each an optionally substituted 5-membered or 6-membered ring having an amide bond in the ring, or a salt thereof.Type: GrantFiled: November 19, 2001Date of Patent: November 1, 2005Assignee: Takeda Pharmaceutical Company LimitedInventors: Akihiro Tasaka, Nobuyuki Matsunaga, Akio Ojida, Masami Kusaka
-
Patent number: 6958356Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.Type: GrantFiled: March 13, 2002Date of Patent: October 25, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Amy Qi Han, Renhua Li, Donald J. Pinto, James R. Pruitt, Mimi L. Quan
-
Patent number: 6924376Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: April 11, 2003Date of Patent: August 2, 2005Assignees: Cytokinetics, Inc., Smithkline Beecham CorporationInventors: Andrew McDonald, Gustave Bergnes, Bainian Feng, David J. Morgans, Jr., Steven David Knight, Kenneth A. Newlander, Dashyant Dhanak, Christopher A. Brook
-
Patent number: 6864273Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R6 is hydrogen or phenylmethyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical.Type: GrantFiled: May 23, 2000Date of Patent: March 8, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Marcel Frans Leopold De Bruyn
-
Patent number: 6852726Abstract: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: wherein X is —S(O)n— or —C(O)—, A is C1-6alkyl, aryl, heteroaryl, hydroxyalkyl, or —(CH2)p—NRaRb, and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: January 31, 2003Date of Patent: February 8, 2005Assignee: Syntex LLCInventors: Robert Greenhouse, Saul Jaime-Figueroa, Lubica Raptova
-
Publication number: 20040235902Abstract: A compound represented by the following general formula (I) or a salt thereof: 1Type: ApplicationFiled: June 15, 2004Publication date: November 25, 2004Inventors: Tetsuo Nagano, Kazuya Kikuchi, Tomoya Hirano, Satoko Maruyama
-
Publication number: 20040235905Abstract: Therapeutically active compounds of formula (I): wherein X is —O—, —CH2— or —C(O)—; Z is —CHR9— or valence bond; Y is —CH2—, —C(O)—, CH(OR10)—, —CH(NR11R12)—, —O—, —S—, —S(O)— or —S(O2)—, provided that in case Z is a valence bond, Y is not C(O); the dashed line represents an optional double bond in which case Z is —CR9— and Y is —CH—, C(OR10)— or —C(NR11R12)—; R1 is —(CH2)nNR4R7 or one of the following groups: n is 1-4; R2 and R3 are independently H, lower alkyl, lower alkoxy, —NO2, halogen, —CF3, —OH, —NHR8 or —COOH, R4 and R7 are independently H, lower alkyl or lower hydroxyalkyl; R5 is H, lower alkoxy, —CF3, —NH2 or —CN; R6 is —NO2, —NR14R19, —CF3 or R8 and R16 are independently H or acyl; R9 is H or lower alkyl; R10 is H, alkylsulfonyl or acyl; R11 and R12 aType: ApplicationFiled: June 8, 2004Publication date: November 25, 2004Inventors: Tuula Koskelainen, Leena Otsomaa, Arto Karjalainen, Pekka Kotovuori, Jukka Tenhunen, Sirpa Rasku, Pentti Nore, Eija Tiainen, Olli Tormakangas
-
Publication number: 20040210045Abstract: Nucleic acid labeling compounds containing heterocyclic derivatives are disclosed. The heterocyclic derivative containing compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.Type: ApplicationFiled: May 11, 2004Publication date: October 21, 2004Inventors: Glenn McGall, Anthony D. Barone
-
Publication number: 20040204417Abstract: The invention concerns compounds of general formula (1), wherein, in particular; W represents H, SO2R5. CO(CH2)nR5, (CH2)nR6, CS(CH2)nR5; X represents S or NH; Y represents (CH2)p, CO, (CH2)pCO, CH═CH—CO; Z represents a hetcrocycle, imidazole, benzimidazole, isoxazole, tetrazole, oxadiazole, thiadazole, pyridine, quinazoline, quinoxaline, quinoline, thiophene; R1 represents COOR6, CONR6R7, CO—NH—CH(R6)—COOR7, CH2NR6R7, CH2OR6, (CH2)pR6, CH═CHR6; R2 represents in particular hydrogen, C1-C10 alkyl, a substituted or unsubstituted phenyl; R5 and R6 represents hydrogen, C1—C6 alkyl; R5 represents a substituted or unsubstituted phenyl or naphthyl; R6 and R7, identical or different, represent hydrogen, C1—C15 alkyl, a hetcrocycle. an aryl; n represents 0 to 10; p represents 1 to 6.Type: ApplicationFiled: May 20, 2004Publication date: October 14, 2004Inventors: Michel Perez, Marie Lamothe, Bridget Hill, Chantal Etievant
-
Patent number: 6803372Abstract: Compounds of the general formula (I): wherein Ar1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.Type: GrantFiled: March 8, 2002Date of Patent: October 12, 2004Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh
-
Publication number: 20040198794Abstract: Ondansetron forms are identified and processes for making the same are provided. The ondansetron can be used in various pharmaceutical applications.Type: ApplicationFiled: January 2, 2004Publication date: October 7, 2004Inventors: Raymond J. H. Westheim, Frans van Dalen
-
Patent number: 6797708Abstract: This invention provides substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.Type: GrantFiled: November 22, 2002Date of Patent: September 28, 2004Assignee: WyethInventors: John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark
-
Patent number: 6797725Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: April 9, 2002Date of Patent: September 28, 2004Assignee: Sugen, Inc.Inventors: Connie Li Sun, Chung Chen Wei, Peng Cho Tang, Marcel Koenig, Yong Zhou, Tomas Vojkovsky, Asaad S. Nematalla
-
Publication number: 20040176379Abstract: The present invention is directed to imidazolyl derivatives of formula (I) where the substituents are defined in the specification, which are useful as agonists or antagonists of somatostatin receptors.Type: ApplicationFiled: February 4, 2004Publication date: September 9, 2004Inventors: Christopher Alain Thurieau, Lydie Francine Poitout, Marie-Odile Galcera, Christophe Philippe Moinet, Thomas D. Gordon, Barry A. Morgan
-
Patent number: 6780859Abstract: This invention relates to novel benzofuran and dihydrobenzofuran compounds, pharmaceutical compositions containing such compounds, and methods of treating beta-3 adrenoreceptor-mediated conditions with such compositions.Type: GrantFiled: September 10, 2002Date of Patent: August 24, 2004Assignee: Bayer Pharmaceuticals CorporationInventors: Gaetan H. Ladouceur, William R. Schoen, Michael J. Burke
-
Patent number: 6770655Abstract: The subject invention provides useful and novel 5-HT3 antagonists. The subject invention also provides methods for synthesizing the compounds of invention. The invention also provides methods for the treatment of irritable bowel syndrome and other such conditions.Type: GrantFiled: January 21, 2003Date of Patent: August 3, 2004Assignee: Aryx TherapeuticsInventors: Xiaoming Zhang, Jurg R. Pfister, Cyrus Becker, Pascal Druzgala
-
Publication number: 20040142996Abstract: Compounds of formula I: t,0010Type: ApplicationFiled: October 8, 2003Publication date: July 22, 2004Applicant: Portela & C.A., S.A.Inventors: David Alexander Learmonth, Patricio Manuel Viera Araujo Soares da Silva, Alexander Beliaev
-
Patent number: 6759428Abstract: Compounds of the formula (I) wherein m, n, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.Type: GrantFiled: June 2, 2003Date of Patent: July 6, 2004Assignee: Roche Palo Alto LLCInventors: Joe Timothy Bamberg, Tobias Gabriel, Nancy Elisabeth Krauss, Taraneh Mirzadegan, Wylie Solang Palmer, David Bernard Smith
-
Patent number: 6756395Abstract: Compounds of the Formula: where R1-R6 are those defined herein and methods for producing the same. Also provided are pharmaceutical compositions comprising a Compound of Formula I and methods for their use as therapeutic agents.Type: GrantFiled: April 22, 2003Date of Patent: June 29, 2004Assignee: Roche Palo Alto LLCInventors: Michael Patrick Dillon, Clara Jeou Jen Lin, Counde O'Yang, Xiaoming Zhang
-
Publication number: 20040116706Abstract: This invention relates to urea compounds that are muscarinic receptor antagonists and agonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.Type: ApplicationFiled: April 30, 2003Publication date: June 17, 2004Inventors: Mathai Mammen, David Oare
-
Publication number: 20040110745Abstract: Provided herein is a compound represented by the Formula (I) wherein said compounds are useful for the treatment of migraine. Also provided are processes for the preparation of compounds of Formula (I) and intermediates.Type: ApplicationFiled: July 16, 2003Publication date: June 10, 2004Inventors: Marc Chapdelaine, Timothy Davenport, Markus Haeberlein, Carey Horchler, John McCauley, Edward Pierson, Daniel Sohn
-
Patent number: 6747045Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6—Alk2— (b-1), or -Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6aType: GrantFiled: April 3, 2002Date of Patent: June 8, 2004Assignee: Janssen Pharmaceutica N.V.Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn
-
Publication number: 20040106581Abstract: The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ia), 1Type: ApplicationFiled: July 1, 2003Publication date: June 3, 2004Inventors: Bansi Lal, Kalpana Joshi, Sanjeev Kulkarni, Malcolm Mascarenhas, Shrikant Kamble, Maggie Joyce Rathos, Rajendrakumar Joshi
-
Publication number: 20040102386Abstract: 3-Deoxyflavonoid compounds and methods for inhibiting T-cell activity and treating diseases and disorders (e.g., autoimmune disorders, inflammatory disorders, diabetes, ALS, MS, rheumatoid arthritis, etc.). In some cases the efficacy and/or duration of action of luteolin and/or other 3-deoxyflavonoid compounds may be increased by administering such compounds along with Rutin, a Rutin congener and/or a Rutin derivative. Also, in some cases, first pass metabolism of luteolin or other 3-deoxyflavonoids may be avoided by administering such compounds by parenteral routes (e.g., routes wherein absorption occurs at sites other than the stomach or intestinal mucosa, such as sublingual, buccal, intranasal, injection, etc.).Type: ApplicationFiled: August 29, 2003Publication date: May 27, 2004Inventors: Thomas Lahey, Vithal J. Rajadhyaksha
-
Publication number: 20040087624Abstract: Compounds of formula (I) 1Type: ApplicationFiled: December 10, 2003Publication date: May 6, 2004Inventors: Gerard Martin Paul Giblin, Stephen Vernon Frye, Susan Roomans
-
Publication number: 20040082638Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: ApplicationFiled: April 11, 2003Publication date: April 29, 2004Applicant: Cytokinetics, Inc.Inventors: Andrew McDonald, Gustave Bergnes, Bainian Feng, David J. Morgans, Steven David Knight, Kenneth A. Newlander, Dashyant Dhanak, Christopher A. Brook
-
Patent number: 6713473Abstract: A compound represented by the formula (I) [A represents a 5- to 7-membered hydrocarbon ring group; L represents —NR3—CO—, —CO—NR3— and the like (R3 represents a hydrogen atom, a lower alkyl group, a lower acyl group and the like); M represents an alkylene linking group (a carbon atom constituting the carbon chain may be replaced with a nitrogen atom, an oxygen atom and the like); X represents —S—, —O—, —NR4—, —NR5—CO— and the like (R4 and R5 represent a hydrogen atom, a lower alkyl group and the like) or a single bond; Y represents an alkyl group, an aryl group, an amino group, an aromatic heterocyclic group and the like; R1 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a lower acyl group; and R21, R22 and R23 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like] or a salt thereof.Type: GrantFiled: February 19, 2002Date of Patent: March 30, 2004Assignee: Meiji Seika Kaisha, Ltd.Inventors: Naoyuki Nishikawa, Masaharu Sugai, Kozo Aoki, Makoto Suzuki, Akihiko Ikegawa, Kazunobu Takahashi, Fukuichi Ohsawa, Naomi Masuda, Nobukazu Kakui, Jiro Tanaka, Yuji Tabata, Kenji Asai
-
Patent number: 6713498Abstract: Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the formula I:Type: GrantFiled: May 30, 2002Date of Patent: March 30, 2004Assignee: Alteon IncorporatedInventor: Martin Gall
-
Publication number: 20040058931Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure 1Type: ApplicationFiled: November 15, 2002Publication date: March 25, 2004Inventors: John Lloyd, Heather J. Finlay, Wayne Vaccaro, Karnail S. Atwal, Michael F. Gross, Kerry L. Spear
-
Publication number: 20040054187Abstract: This invention relates to urea compounds that are muscarinic receptor antagonists and agonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.Type: ApplicationFiled: April 30, 2003Publication date: March 18, 2004Inventors: Mathai Mammen, David Oare
-
Publication number: 20040048913Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: March 27, 2003Publication date: March 11, 2004Inventors: Yang Gao, Alan J. Hutchison, John M. Peterson, Wallace C. Pringle, Andrew Thurkauf, Taeyoung Yoon, He Zhao
-
Publication number: 20040048844Abstract: The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): 1Type: ApplicationFiled: May 1, 2003Publication date: March 11, 2004Applicant: Bristol-Myers Squibb Pharma CompanyInventors: David Nugiel, David Carini, Susan DiMeo, Anup Vidwans, Eddy Yue
-
Patent number: RE39663Abstract: The invention provides compositions electron-deficient nitrogen heterocycle-substituted fluorescein dyes and methods in which the dyes are conjugated to substrates and used as detection labels in molecular biology experiments. The electron-deficient nitrogen heterocycles include pyridine, quinoline, pyrazine, and the like. Substrates include polynucleotides, nucleosides, nucleotides, peptides, proteins, carbohydrates, and ligands.Type: GrantFiled: April 6, 2004Date of Patent: May 29, 2007Assignee: Applera CorporationInventors: Krishna G. Upadhva, Steven M. Menchen, Weiguo Zhen