The Additional Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 514/337)
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Patent number: 7442702Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: September 25, 2002Date of Patent: October 28, 2008Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
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Patent number: 7442701Abstract: The present invention provides a compound of formula (I): wherein V represents NR5, O, S, SO or S(O)2; W and X each independently represent CH or N; Y represents N, CH or C—Ar2, with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C—Ar2, with the proviso that when Y is N or CH then Z is C—Ar2, and with the further proviso that when Y is C—Ar2 then Z is CH; Ar1 represents a fused 9 or 10 membered heterobicyclic ring system containing one, two, three or four heteroatoms selected from nitrogen, oxygen and sulfur, wherein at least one of the rings in said ring system is aromatic; Ar2 represents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; R1 represents halogen, hydroxy, oxo, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, hydroxyC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, hydroxyC1-6alkoxy, C3-7cycloalkyl, C3-7cycloalkoxy, C3-5cycloalkylC1-4alkyl, cyano, nitro, SR6, SOR6, SO2R6, COR6, NR3COR6, CONType: GrantFiled: November 14, 2003Date of Patent: October 28, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Peter Blurton, Frank Burkamp, Stephen Robert Fletcher, Gregory John Hollingworth, A. Brian Jones, Edward Giles McIver, Christopher Richard Moyes, Lauren Rogers
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Patent number: 7432282Abstract: Novel indole derivatives of the formula (I), in which X, Y, R1, R1?, m and n have the meanings indicated in Patent Claim 1, have a strong affinity to the 5-HT1A and in some cases to the 5-HT1D receptors.Type: GrantFiled: October 30, 2003Date of Patent: October 7, 2008Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Günter Hölzemann, Kai Schiemann, Timo Heinrich, Henning Böttcher, Joachim Leibrock, Christoph van Amsterdam, Gerd Bartoszyk, Christoph Seyfried
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REDUCTION OF ADVERSE EVENTS AFTER PERCUTANEOUS INTERVENTION BY USE OF A THROMBIN RECEPTOR ANTAGONIST
Publication number: 20080234236Abstract: Disclosed are methods of preventing adverse clinical events in a patient undergoing a percutaneous coronary intervention procedure or a peripheral percutaneous interventional procedure comprising administering a therapeutically effective amount of a thrombin receptor antagonist, such as SCH 530348, to the patient. Administration of a loading dose of about 40 mg of SCH 530348 in as little as one hour prior to the procedure can result in therapeutically effective levels of platelet aggregation.Type: ApplicationFiled: March 19, 2008Publication date: September 25, 2008Inventors: Enrico P. Veltri, John T. Strony, Madhu Chintala -
Patent number: 7425568Abstract: Therapeutically active compounds of formula (I): wherein the variables shown in formula (I) are defined in the disclosure; and pharmaceutically acceptable salts and esters thereof. The compounds are potent inhibitors of the Na+/Ca2+ exchange mechanism.Type: GrantFiled: July 10, 2002Date of Patent: September 16, 2008Assignee: Orion CorporationInventors: Tuula Koskelainen, Leena Otsomaa, Arto Karjalainen, Pekka Kotovuori, Jukka Tenhunen, Sirpa Rasku, Pentti Nore, Eija Tiainen, Olli Törmäkangas
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Publication number: 20080207691Abstract: The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, Ru0 is (II), or (III) G1 is methylene or ethylene; L is a divalent linking group selected from —(C1-C4) alkylene-, —S—, —CH(OH)—, or —O—; A is methylene, —S—, —O—, or —NH—; and the other substituents are as defined in the claims.Type: ApplicationFiled: December 16, 2005Publication date: August 28, 2008Inventors: Thomas Daniel Aicher, Mark Joseph Chicarelli, Ronald Jay Hinklin, Hongqi Tian, Owen Brendan Wallace
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Publication number: 20080207696Abstract: 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 also useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: ApplicationFiled: November 21, 2007Publication date: August 28, 2008Inventors: Jose Aquino, Varghese John, John Tucker, Roy Hom, Shon Pulley, Ruth Tenbrink
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Patent number: 7417066Abstract: The invention relates to compounds of general Formula I, the production thereof, and the use thereof as a medicinal product.Type: GrantFiled: June 7, 2006Date of Patent: August 26, 2008Assignee: Schering AGInventors: Bernd Buchmann, Martin Fritsch, Duy Nguyen, Bernd Menzenbach, Ulf Boemer
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Publication number: 20080194636Abstract: The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions, regulating cellular glucose uptake and homeostasis, inducing labour and lactation, and other disorders or conditions wherein excessive or undesirable IRAP activity is implicated.Type: ApplicationFiled: September 9, 2005Publication date: August 14, 2008Applicants: Howard Florey Institute Of Experimental Physiology And Medicine, St. Vincent's Institute of Medical ResearchInventors: Siew Yeen Chai, Michael William Parker, Anthony Lloyd Albiston, Craig J. Morton, Hooi Ling Ng, Siying Ye, Frederick A.O. Mendelsohn
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Publication number: 20080194560Abstract: Disclosed is a rapidly disintegrating solid dosage form comprising an active pharmaceutical ingredient, a disintegrant and a disintegration promoter, which formulation is obtainable by a wet granulation process. In one exemplified embodiment, the active pharmaceutical agent is a thrombin receptor antagonist, the disintegrant is sodium croscarmellose, and the disintegration promoter is calcium silicate. In some embodiments, the thrombin receptor antagonist is represented by the formula: or a pharmaceutically acceptable salt thereof. Also disclosed are methods of treating patients at risk for acute coronary syndrome by administering such a rapidly disintegrating solid dosage form.Type: ApplicationFiled: December 19, 2007Publication date: August 14, 2008Inventors: Zhi Yun Wang, David Harris
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Publication number: 20080194637Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity.Type: ApplicationFiled: November 2, 2007Publication date: August 14, 2008Applicants: Curis, Inc., WyethInventors: Shirley Ann Brunton, Oivin M. Guicherit, Simon N. Haydar, Lawrence I. Kruse, Dane Springer
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Publication number: 20080193423Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity.Type: ApplicationFiled: November 2, 2007Publication date: August 14, 2008Applicant: Curis, Inc.Inventors: Shirley Ann Brunton, Oivin M. Guicherit, Lawrence I. Kruse
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Publication number: 20080194638Abstract: The present invention relates to bioavailable pharmaceutical formulations of heterocyclic compounds, such as such as N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide (oglemilast) and pharmaceutically acceptable salts thereof, to processes for their preparation and to methods of treatment using the same. The present invention also relates to substantially pure amorphous forms of heterocyclic compounds, such as oglemilast. The invention is particularly directed to bioavailable pharmaceutical oral dosage forms containing amorphous oglemilast.Type: ApplicationFiled: February 8, 2008Publication date: August 14, 2008Applicant: Forest Laboratories Holdings LimitedInventors: Mahendra G. DEDHIYA, Rahul Surana, Suneel K. Rastogi, Anil Chhetrry
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Patent number: 7411069Abstract: The invention relates to novel antihistamines and methods of modulating sleep by administering a doxepin analog or a pharmaceutically effective salt thereof.Type: GrantFiled: April 23, 2004Date of Patent: August 12, 2008Assignee: Hypnion, Inc.Inventors: Dale M. Edgar, David G. Hangauer, James F. White, Michael Solomon
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Publication number: 20080182859Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity.Type: ApplicationFiled: November 2, 2007Publication date: July 31, 2008Applicant: Curis, Inc.Inventors: Shirley Ann Brunton, Oivin M. Guicherit, Lawrence I. Kruse
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Publication number: 20080182878Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N; NR4, SO or SO2;Type: ApplicationFiled: December 28, 2007Publication date: July 31, 2008Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20080167348Abstract: The invention is concerned with the novel sulfonamide derivatives of formula (I) wherein A, R1 to R2?, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.Type: ApplicationFiled: January 8, 2008Publication date: July 10, 2008Inventors: David Banner, Harald Mauser, Rudolf E. Minder, Hans P. Wessel
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Publication number: 20080161363Abstract: The present invention is directed to 2-aminopyridine compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: October 25, 2005Publication date: July 3, 2008Inventors: Craig A. Coburn, M. Katharine Holloway, Shawn J. Stachel
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Patent number: 7393865Abstract: Compounds having the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts, esters and solvates thereof, wherein R1, R2, R3a, R3b, L1, L2 and n are as defined herein. Such compounds generally function as H1 receptor ligands, and thus have utility as sleep inducing agents. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.Type: GrantFiled: June 17, 2005Date of Patent: July 1, 2008Assignee: Neurocrine Biosciences, Inc.Inventors: Graham Beaton, Wilna (Willy) J Moree, Florence Jovic, Timothy Coon, Jinghua Yu
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Publication number: 20080152712Abstract: Disclosed is a lyophilized rapidly disintegrating solid dosage form, one embodiment of which comprises a thrombin receptor antagonist such as, or a pharmaceutically acceptable salt or hydrate thereof, a polymer such as gelatin, and a matrix forming agent such as mannitol. Systems for effectively buffering the pre-lyophilized suspension are taught, along with methods of treating patients at risk for acute coronary syndrome by administering such a rapidly disintegrating solid dosage form.Type: ApplicationFiled: September 24, 2007Publication date: June 26, 2008Inventors: David Monteith, Enrico P. Veltri, Srinivas Duggirala, Michael Angelo Falvo, John R. Erbey, Kung-I Feng, Anastasia Pavlovsky, Suliman Chawdry
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Publication number: 20080153872Abstract: Certain bis-(coumarin) compounds as well as the products of their intramolecular cyclization including pharmaceutically acceptable salts, hydrates, solvates, clathrates, prodrugs, tautomers and stereoisomers thereof are disclosed. Certain processes and intermediates for the preparation of certain bis-(coumarin) compounds, as well as for the use of these compounds as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diseases and conditions in mammals, especially humans are also disclosed.Type: ApplicationFiled: January 13, 2006Publication date: June 26, 2008Inventors: Mladen Mercep, Ivica Malnar, Boska Hrvacic, Stribor Markovic, Anita Filipovic Sucic, Berislav Bosnjak, Andreja Cempuh Klonkay, Renata Rupcic, Antun Hutinec, Ivaylo Jivkov Elenkov, Milan Mesic
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Publication number: 20080146589Abstract: Novel compounds of the formula I in which R1, R2, R3 and Het are as defined herein, which are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for the treatment of tumours, for neuroprotection and for protection of the stress proteins of the skin.Type: ApplicationFiled: January 23, 2008Publication date: June 19, 2008Inventors: Teresa MUJICA-FERNAUD, Herwig Buchholz, Wilfried Rautenberg, Christian Sirrenberg
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Patent number: 7384947Abstract: This invention relates to a novel fused tricyclic heterocycle of the formula and its use for the treatment of hyper-proliferative disorders.Type: GrantFiled: August 28, 2006Date of Patent: June 10, 2008Assignee: Bayer HealthCare LLCInventors: Chengzhi Zhang, Michael Burke, Zhi Chen, Jacques Dumas, Dongping Fan, Benjamin D. Jones, Gaetan Ladouceur, Wendy Lee, Barton Phillips, Scott M. Wilhelm, Qian Zhao
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Patent number: 7378399Abstract: What is described are a compound of the formula (I) Wherein A-B is —CH?CH— or —CH2—CH2—; n is 0 or 1; R1, is C1-C12alkyl, C3-C8cycloalkyl or C2-C12alkenyl; R2 and R3 for instance are either, (i) independently from each other for instance -Q, —C(?Y)-Q, or —C(?Y)—O-Q; or (ii) together form with the nitrogen atom to which they are bound a three- to seven-membered ring, (iii) together are ?C(R4)R5; R4 and R5 are, independently from each other, for instance -Q, —C(?Y)-Q, or —C(?Y)—O-Q; Y is O or S; Q is for instance H or unsubstituted or mono- to pentasubstituted C1-C12alkyl; or, if appropriate, an E/Z isomer, E/Z isomer mixture and/or tautomer thereof; a process for preparing these compounds, their isomers and tautomers and the use of these compounds, their isomers and tautomers; pesticidal compositions whose active compound is selected from these compounds and their tautomers; intermediates for the preparation of the said compounds of the formula (I), methods for the preparation of the compounds of the formula (Type: GrantFiled: February 3, 2004Date of Patent: May 27, 2008Assignee: Merial LimitedInventors: Jerome Cassayre, Hans Tobler, Thomas Pitterna, Peter Maienfisch, Fiona Murphy Kessabi, Laura Quaranta, Ottmar Franz Hueter
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Publication number: 20080113944Abstract: 5-vinyl-indole derivatives are chemical uncouplers useful e.g. for the treatment of obesity.Type: ApplicationFiled: May 3, 2005Publication date: May 15, 2008Applicant: Novo Nordisk A/SInventors: Preben Houlberg Olesen, Rolf Hohlweg
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Patent number: 7371874Abstract: The present invention relates to a noble 6-alkylamino-2-methyl-2?-(N-methyl substituted sulfonamido)methyl-2H-1-benzopyran derivative, a method for preparing the same with high efficiency using a parallel synthetic method, one of combinatorial chemical synthetic techniques, and a use of the novel compound showing a high inhibitory effect to 5-lipoxygenase (5-LO) activity for preventing and treating leukotriene (LTA4, B4, C4, D4) activation-related diseases such as inflammatory diseases, rheumatoid arthritis, colitis, asthma and psoriasis.Type: GrantFiled: July 21, 2006Date of Patent: May 13, 2008Assignee: Korea Research Institute of Chemical TechnologyInventors: Young-Dae Gong, Hyae-Gyeong Cheon, Moon-Kook Jeon, Cho Young Sik, Jong Yeon Hwang, Choi Hyung Sub, Jeon Hyun Suk, Soon-Hee Hwang, Song Jin Sook, Kim Chi Hyun, Sung-eun Yoo
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Patent number: 7368477Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R1?, R2, R3, R4, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.Type: GrantFiled: April 21, 2006Date of Patent: May 6, 2008Assignee: WyethInventors: Jonathan Laird Gross, Gary Paul Stack, Dahui Zhou, Hong Gao
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Patent number: 7368476Abstract: The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: GrantFiled: April 7, 2005Date of Patent: May 6, 2008Assignee: Pharmacyclics, Inc.Inventor: Eduardo L. Setti
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Patent number: 7365095Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, y, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.Type: GrantFiled: April 21, 2006Date of Patent: April 29, 2008Assignee: WyethInventors: Gavin David Heffernan, Gary Paul Stack, Jonathan Laird Gross, Dahui Zhou, Hong Gao
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Publication number: 20080085858Abstract: The present invention provides a pharmaceutical composition comprising (a) a phosphodiesterase (PDE)-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) an immunosuppressant, a therapeutic and/or preventive agent for chronic skin diseases comprising (a) a PDE-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) an immunosuppressant, a therapeutic and/or preventive agent for chronic skin diseases to be administered simultaneously or separately with an interval comprising (a) a PDE-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) an immunosuppressant, as active ingredients; and the like.Type: ApplicationFiled: October 13, 2005Publication date: April 10, 2008Applicant: KYOWA HAKKO KOGYO CO., LTD.Inventors: Daisuke Harada, Katsuya Kobayashi, Haruhiko Manabe, Etsuo Ohshima
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Publication number: 20080070951Abstract: Compounds of the formula Z: where; A is CH or N; R1 is a substituent to a carbon atom in the ring containing A selected from —S(?O)pRa, where Ra is —C1-C4 alkyl, —ORx, —NRxRx, —NHNRxRx, —NHNHC(?O)ORx, —NRxOH; —C(?O)—Rb, where Rb is —CT-C4-alkyl, ORx, —NRxRx, —NHNRxRx, —NHC1-C3-alkyl-C(?O)Orx —NRxRc, where Rc is H, C1-C4 alkyl, —NRxRx; —C(=0)Rd, —CN, S(?O)pRx, where Rd is Rd is C1-C4-alkyl, —ORx, —NRxRx C1-C3-alkyl-O—C1-C3-alkylC(?O)ORx, —C1-C3-alkyl-COORx; —C1-C3alkyl-OH or C1-C4 alkyl ethers or esters thereof (O—C1-C3alkyl)q-O—Rx a 5 or 6 membered aromatic ring having 1-3 hetero atoms p is 1 or 2; Rx is independently selected from H, C1-C4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is —O —, —S(?O)—, or —CH2—, where r is 0, 1 or 2; R3-R7 are substituents as defined in the specification; X is —(CR8R8?)n-D-(CR8R8?)m-; D is a bond, —NR9—, —O—, —S—, —S(=0)- or —S(=0)2-; and pharmaceutically acceptable salts and prodrugs thereof, have utility as HIV antivirals.Type: ApplicationFiled: December 30, 2004Publication date: March 20, 2008Applicant: Medivir ABInventors: Christian Sund, Nathalie Roue, Stefan Lindstrom, Dmitry Antonov, Christer Sahlberg, Katarina Jansson
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Patent number: 7329746Abstract: The present invention is directed to compounds of formula I which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease.Type: GrantFiled: August 10, 2004Date of Patent: February 12, 2008Assignee: Merck & Co., Inc.Inventors: Craig A. Coburn, Shawn J. Stachel, Joseph P. Vacca
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Publication number: 20080020014Abstract: The present invention is directed to implantable devices (e.g., drug-delivery stents) containing nuclear receptor ligands. The nuclear receptor ligands may be, inter alia, PPAR ligands or retinoids. The invention also provides for a method of treating or preventing vascular disorders (e.g., restenosis) and related disorders using the nuclear receptor ligand-containing devices.Type: ApplicationFiled: July 17, 2007Publication date: January 24, 2008Inventors: Paul Consigny, Jin Cheng, Wouter Erik Roorda
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Publication number: 20080015232Abstract: Methods and intermediates for preparing enantiomerically enriched Schweinfurthin analogs which are useful for the treatment of cancer, as well as novel Schweinfurthin analogs having anti-cancer activity, compositions comprising such analogs and therapeutic methods comprising administering such analogs.Type: ApplicationFiled: March 29, 2005Publication date: January 17, 2008Inventors: David F. Wiemer, Jeffrey D. Neighbors, John A. Beutler
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Publication number: 20080004318Abstract: Substituted bicyclic and tricyclic modified himbacine derivative of the formula: or a pharmaceutically acceptable salt or solvate of said compound wherein represents an optional double bond and wherein En, Fn, Gn, Zn, Jn, X, R3, R9, R10, R11, R32, R33, B and Het are herein defined are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other agents is also claimed.Type: ApplicationFiled: June 27, 2007Publication date: January 3, 2008Inventors: Mariappan V. Chelliah, Samuel Chackalamannil, Yan Xia
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Patent number: 7304079Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: GrantFiled: September 12, 2006Date of Patent: December 4, 2007Assignee: The Institute for Pharmaceutical Discovery, LLCInventors: Michael Jones, David Gunn, John Jones, Michael Van Zandt
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Patent number: 7304078Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; represents an optional double bond; n is 0–2; Q is cycloalkyl, optionally substituted by R13 and R14; R13 and R14 are independently selected from (C1–C6)alkyl, (C3–C8)cycloalkyl, —OH, (C1–C6)alkoxy, R27-aryl(C1–C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, halogen and haloalkyl; or R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3–6 atoms; Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administeringType: GrantFiled: April 14, 2003Date of Patent: December 4, 2007Assignee: Schering CorporationInventors: Samuel Chackalamannil, William J. Greenlee, Yuguang Wang, Wenxue Wu, Enrico P. Veltri, Yan Xia
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Publication number: 20070191313Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, A, X, Z, R1, o, R3, R2 and p are as defined in the specification.Type: ApplicationFiled: February 15, 2007Publication date: August 16, 2007Inventors: Richard L. Beard, John E. Donello, Haiqing Yuan, Diana F. Colon, Tien Duong, Xiaoxia Liu, Yihui Hu
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Publication number: 20070183982Abstract: Disclosed are new pharmaceutical formulations for aerosols with at least two or more active substances together with at least one surfactant for inhalative or nasal application.Type: ApplicationFiled: January 29, 2007Publication date: August 9, 2007Inventors: Erhard Berkel, Hubert Hoelz, Friedrich Schmidt
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Patent number: 7241758Abstract: Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: GrantFiled: October 15, 2002Date of Patent: July 10, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Ming-Hong Hao, Sanxing Sun
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Patent number: 7235567Abstract: A crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist compound, which exhibits a powder x-ray diffraction profile substantially the same as that shown in FIG. 1, or which exhibits a differential scanning calorimtery profile substantially the same as that shown in FIG. 3, and is represented by the formula for Compound 2: and processes for preparing Compound 2 are disclosed. Pharmaceutical compositions comprising the polymorph of the bisulfate salt and at least one excipient or carrier, and methods of using the polymorph of Compound 2 to treat a variety of physiological disorders, such as thrombosis, are also disclosed.Type: GrantFiled: January 9, 2004Date of Patent: June 26, 2007Assignee: Schering CorporationInventor: Wenxue Wu
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Patent number: 7235568Abstract: The invention provides compounds of the formula: wherein (a) is a single or double bond; W is CH, CH2, CHCH3, C(CH3)2, C(CH2)2 or C(CH2)3; X is N; and Y is H or F, and salts, hydrates, tautomers, pure enantiomers, and enantiomeric mixtures; and a method of treating schizophrenia comprising administering same.Type: GrantFiled: July 28, 2006Date of Patent: June 26, 2007Assignee: Pierre Fabre MedicamentInventors: Bernard Vacher, Stéphane Cuisiat, Wouter Koek, Francis Colpaert
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Patent number: 7230015Abstract: N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain.Type: GrantFiled: March 14, 2005Date of Patent: June 12, 2007Assignee: Aventis Pharmaceuticals Inc.Inventors: Craig P Smith, Michel P Rathbone, Margaret Petty, David Rampe
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Patent number: 7230013Abstract: Compositions comprising a taxane having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: February 28, 2005Date of Patent: June 12, 2007Assignee: Florida State University Research Foundation, Inc.Inventors: Robert A. Holton, Weishuo Fang
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Patent number: 7226944Abstract: Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: March 17, 2005Date of Patent: June 5, 2007Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 7217723Abstract: The present invention provides a compound that has an excellent inhibitory activity on STAT6 activation and is effective against allergic diseases, and a medicinal composition thereof. According to the present invention, disclosed is the compound represented by the General Formula (I) [where R1 and R2 independently represent a C1-6 alkyl group and the like that may have a hydrogen atom or a substituent; R3 represents a C1-6 alkyl group and the like that may have a substituent; R4 and R5 independent represents a hydrogen atom or a C1-6 alkyl group and the like that may have a substituent; R6 represents a hydrogen atom and the like; W represents —SO2—and the like; and X represents a sulphur atom and the like.] or a salt thereof, or a hydrate thereof.Type: GrantFiled: February 2, 2005Date of Patent: May 15, 2007Assignee: Eisai Co., Ltd.Inventors: Ichiro Yoshida, Shuichi Suzuki
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Patent number: 7214701Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: June 25, 2004Date of Patent: May 8, 2007Assignee: Bayer CropScience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 7208491Abstract: Mono-acylated o-phenylendiamines derivatives of formula I wherein X and R are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone deacetylase, such as cancer.Type: GrantFiled: February 3, 2004Date of Patent: April 24, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
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Patent number: 7205306Abstract: Compounds provided herein are novel substituted pyrazinones, pyridines and pyrimidines of Formula (I) and (II): Such compounds are particularly useful as CRF receptor ligands, and hence, in the treatment of various neurologically-related disorders such as affective disorder, anxiety and depression.Type: GrantFiled: May 14, 2002Date of Patent: April 17, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Argyrios G Arvanitis, Paul J Gilligan, Richard A Hartz
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Patent number: 7205305Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: July 17, 2003Date of Patent: April 17, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W Bemis, Francesco G Salituro, John P Duffy, John E Cochran, Edmund M Harrington, Mark A Murcko, Keith P Wilson, Michael Su, Vincent P Galullo