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)
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Patent number: 7704992Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: January 23, 2009Date of Patent: April 27, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Patent number: 7700584Abstract: The present invention provides curcumol derivatives of the following formula (I) or pharmaceutical acceptable salts thereof: wherein, Y is selected from the group consisting of ?CHR2, —CH2R2, ?O, ?—OH or —OR1;R1 is selected from H, R, RCO or HO3S; and R is selected from the group consisting of H; saturated or unsaturated linear C1-10 hydrocarbon group and the like; R2 is selected from the group consisting of F; Cl; Br; I; H; —OH; —OR; —HSO3 and the like; with the proviso that both R1 and R2 are not H. The present invention also provides anti-tumor or antiviral pharmaceutical compositions comprising said derivatives or pharmaceutical acceptable salts thereof. The present invention further provides the use of said derivatives or pharmaceutical acceptable salts thereof in the preparation of a medicament for prophylaxis and/or treatment tumor or an antiviral medicament.Type: GrantFiled: May 26, 2005Date of Patent: April 20, 2010Assignee: Hangzhou Minsheng Pharmaceuticals Co., Ltd.Inventors: Shulong Wang, Dianwu Guo, Zhaoke Meng
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Publication number: 20100093817Abstract: This invention relates to new 6,8-difluorochroman-3-yl-1,3-dihydroimidazole-2-thiones, their preparation, and their use as a medicament.Type: ApplicationFiled: January 31, 2008Publication date: April 15, 2010Applicant: BIAL - PORTELA & CA S.A.Inventors: Patrício Manuel Vieira Araújo SOARES DA SILVA, David Alexander LEARMONTH, Alexander BELIAEV
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Patent number: 7696356Abstract: The present invention provides a rapid, high-yielding process for preparing 1,2,3,9-tetrahydro-9-methyl-3-methylene-4H-carbazol-4-one from 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one without using a secondary amine as a catalyst, and without using glacial acetic acid as a solvent. The present invention further provides a rapid, high-yielding process for preparing ondansetron from 1,2,3,9-tetrahydro-9-methyl-3-methylene-4H-carbazol-4-one without using alumina as a catalyst.Type: GrantFiled: August 16, 2005Date of Patent: April 13, 2010Assignee: Taro Pharmaceutical Industries LimitedInventors: Daniella Gutman, Rosa Cyjon
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Publication number: 20100081678Abstract: Indole derivatives that are useful in the treatment of cancer as a chemotherapeutic agent or radiosensitizing agent.Type: ApplicationFiled: September 30, 2009Publication date: April 1, 2010Inventors: Peter A. Crooks, Thirupathi R. Yerramreddy, Narsimha R. Penthala, Michael L. Freeman, Sekhar R. Konjeti
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Patent number: 7678474Abstract: Disclosed herein are novel imidazole derivatives and organic electronic device using the same. The disclosed organic electronic device show excellent characteristics in terms of efficiency, driving voltage and stability.Type: GrantFiled: July 18, 2006Date of Patent: March 16, 2010Assignee: LG Chem. Ltd.Inventors: Jae Soon Bae, Dae Woong Lee, Dong Hoon Lee, Dong Seob Jeong
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Publication number: 20100062065Abstract: Provided is an oral pharmaceutical composition with improved bioavailability and pharmacokinetic properties of a drug, by increasing a bioabsorption rate and an in vivo retention time of an active ingredient via intestine-targeted formulation of a particular naphthoquinone-based compound, or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as an active ingredient.Type: ApplicationFiled: November 26, 2007Publication date: March 11, 2010Applicants: MAZENCE INC., KT & G CP., LTDInventors: In Geun Jo, Sang-Ku Yoo, Myung-gyu Park, Taehwan Kwak
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Publication number: 20100036127Abstract: A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral catalyst and a source of hydrogen, wherein: X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl, wherein: the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.Type: ApplicationFiled: December 12, 2007Publication date: February 11, 2010Applicant: BIAL-PORTELA & CA, S.A.Inventors: David Alexander Learmonth, Antonio Zanotti-Gerosa, Gabriela Alexandra Grasa, Alexander Beliaev
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Publication number: 20100029484Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.Type: ApplicationFiled: July 17, 2009Publication date: February 4, 2010Inventors: John S. Kovach, Francis Johnson
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Patent number: 7626038Abstract: The invention relates to a method for manufacturing R-(?)-sertaconazole mononitrate. The invention also relates to R-(?)-sertaconazole mononitrate hemiacetonate.Type: GrantFiled: September 13, 2005Date of Patent: December 1, 2009Assignee: Ferrer Internacional, S.A.Inventors: Inés Petschen, Xavier Camps, Juan Sallarés
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Publication number: 20090286780Abstract: To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A 2-oxochromene derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: ApplicationFiled: February 27, 2009Publication date: November 19, 2009Applicant: KOWA COMPANY, LTD.Inventors: Ayumu OKUDA, Takayuki MATSUDA, Toru MIURA, Hidefumi OZAWA, Ayako TOSAKA, Koichi YAMAZAKI, Yuki YAMAGUCHI, Sayaka KUROBUCHI, Yuuichirou WATANABE, Kimiyuki SHIBUYA
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Patent number: 7563902Abstract: The present invention relates to novel chemiluminescent compounds, to a method for synthesizing these compounds, to derivatives and conjugates comprising these compounds, to the use of these compounds or conjugates thereof in chemiluminescence based assays, especially in immunoassays.Type: GrantFiled: January 25, 2006Date of Patent: July 21, 2009Assignee: Roche Diagnostics Operations, Inc.Inventors: Dieter Heindl, Rupert Herrmann, Wolfgang Jenni
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Publication number: 20090182007Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of aldosterone synthase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosderosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, cardiac fibrosis and remodeling following hypertension and endothelial dysfunction. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: March 27, 2007Publication date: July 16, 2009Inventors: Christopher Adams, Julien Papillon, Gary Michael Ksander
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Publication number: 20090176828Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardiovascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.Type: ApplicationFiled: July 2, 2008Publication date: July 9, 2009Applicant: ALLERGAN, INC.Inventors: Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gil, John E. Donello, Michael E. Garst, Larry A. Wheeler
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Publication number: 20090170872Abstract: The present invention relates to novel compounds of the general formula (I), their analogs, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel compounds of the general formula (I).Type: ApplicationFiled: July 4, 2006Publication date: July 2, 2009Applicant: Orchid Research Laboratories LimitedInventors: Ganapavarapu Veera Raghava Sharma, Narayanan Sukunath, Thirunavukkarasu Saravanan, Pichika Nagalakshmi, Rajagopal Sriram, Mani Kamaraj
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Publication number: 20090149474Abstract: The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and R4 are as defined in the description. For example, R1 may be phenyl, R2 may be dimethylamino pyrrolidin-1-yl, R3 may be alkoxy and R4 may be alkyl, ai arylalkyl, aryloxyalkyl, aryloxy or heterocyclylalkyl.Type: ApplicationFiled: December 21, 2006Publication date: June 11, 2009Inventors: Udo Bauer, Wayne Brailsford, Linda Gustafsson, Tor Svensson
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Publication number: 20090124680Abstract: Provided is a use of a prodrug composition containing a naphthoquinone-based compound of Formula 1 for the manufacture of a medicament for treatment or prevention of metabolic syndrome diseases. wherein R1 to R10, X, m and n are as defined in the specification.Type: ApplicationFiled: October 30, 2008Publication date: May 14, 2009Applicants: Mazence Inc., KT&G CorporationInventors: Sang-Ku YOO, Sang Woo YOO, Ku Suk KANG
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Publication number: 20090105296Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: October 16, 2008Publication date: April 23, 2009Inventors: Carl R. Illig, Jinsheng Chen, Sanath K. Meegalia, Mark J. Wall
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Patent number: 7521565Abstract: 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carbazol-4-one or its salt is prepared in high yield by reacting a compound of formula 2 with a compound of formula 3 and a compound of formula 4 in the presence of an acid, an alkylsilylhalide compound or an acylhalide compound, in an solvent, and thus, such an inventive process can be favorably applied to a large-scale mass production thereof.Type: GrantFiled: October 15, 2004Date of Patent: April 21, 2009Assignee: Yuhan CorporationInventors: Tai Au Lee, Sang Sun Park, Doo Byung Lee, Sang Jung Kim
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Publication number: 20090082308Abstract: The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: April 14, 2006Publication date: March 26, 2009Inventors: Jed Lee Hubbs, Dawn M. Mampreian, Joey L. Methot, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
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Publication number: 20090076107Abstract: The present application describes deuterium-enriched ondansetron, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 5, 2008Publication date: March 19, 2009Applicant: Protia, LLCInventor: Anthony W. Czarnik
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Publication number: 20090047221Abstract: There is described compounds for use in therapy, said compounds being defined by Formula (1): There is also described an anti-proliferative composition comprising one or more compounds according to Formula (1), and a method of treatment of neoplasia comprising the administration of such a compound or composition.Type: ApplicationFiled: October 31, 2004Publication date: February 19, 2009Applicant: NIPRI LIMITEDInventors: Allen McClay, David Waugh, Paul Armstrong, Zoica Delbederi, Catherine Higgins, Hendrik Van Den Berg, Patrick Johnston, William Watters, Kelly McGarel, Timothy Mils
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Patent number: 7482374Abstract: The invention relates to compounds of formula (I): wherein substituents are as defined.Type: GrantFiled: July 17, 2004Date of Patent: January 27, 2009Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Henry Anderson Kelly, Nigel Stephen Watson, Robert John Young
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Patent number: 7482449Abstract: This invention relates to a process for making spirolactone compounds analogous to formula I.Type: GrantFiled: March 19, 2008Date of Patent: January 27, 2009Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Ralph P. Volante, David M. Tschaen, Steven A. Weissman, Matthew Heileman, Toshiaki Mase, Takehiko Iida, Kenji Maeda, Toshihiro Wada, Hiroki Sato, Kenichi Asakawa
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Publication number: 20090018149Abstract: Described are 4,5,6,7-tetrahydrobenzo[b]thiophene derivatives and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of mycobacteria-induced infections and opportunistic infections, as well as compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene derivative and/or pharmaceutically acceptable salts thereof. Furthermore, the present application refers to the use of mycobacterial protein serine/threonine kinases for developing methods for detection and determination of these kinases for recognising and monitoring diseases and for controlling therapy of diseases.Type: ApplicationFiled: April 9, 2003Publication date: January 15, 2009Inventors: Andrea Missio, Gerald Bacher, Anil Koul, Axel Choidas, Peter Banhegyi, Zoltan Greff, Gyorgy Keri, Peter Marko, Laszlo Orfi, Janos Pato, Frigyes Waczek
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Publication number: 20090012070Abstract: It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)=C(R7)N(R8)-, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)=C(R12)C(R13)=C(R14) 112, -, where R, R, R6, R7, R8, R11, R R13, R14, and X are described. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: August 22, 2008Publication date: January 8, 2009Applicant: Bayer Cropscience AGInventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
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Publication number: 20090005573Abstract: The invention relates to a method for manufacturing sertaconazole mononitrate. The invention also relates tcserta-conazole mononitrate that is characterized by it: particle size and to sertaconazole mononitrate monohydrate.Type: ApplicationFiled: September 13, 2005Publication date: January 1, 2009Applicant: Ferrer Internacional, S.A.Inventors: Ines Petschen, Xavier Camps, Juan Sallares
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Publication number: 20080318987Abstract: Methods and compositions for modulating bone formation and mineralization are described.Type: ApplicationFiled: February 15, 2008Publication date: December 25, 2008Inventor: Laurie H. GLIMCHER
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Publication number: 20080293792Abstract: Tocopherol derivatives having the general formula: wherein n is an integer of 6 to 13, R1 is hydrogen, a silyl ether or acetate, R2 is an optionally substituted nitrogen-containing heterocycle or a polycyclic nitrogen-containing heterocycle; and pharmaceutically acceptable salts thereof are provided. A method for synthesizing the compounds is also provided. The tocopherol derivatives are capable of inhibiting the primary enzyme responsible for the metabolism of the tocopherols and tocotrienols compounds of vitamin E, namely tocopherol-?-hydroxylase, and thus increase the amount and prolong the availability of these compounds in plasma and tissue.Type: ApplicationFiled: May 25, 2007Publication date: November 27, 2008Inventors: Jeffrey Atkinson, Robert S. Parker, Stephan Ohnmacht, Phillip John Nava, Ryan West
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Patent number: 7456294Abstract: It is intended to provide a pyrrole-imidazole polyamide type functional molecule having enhanced abilities of alkylating DNA and recognizing a sequence, compared with the existing functional molecules of this type, for a specific base sequence occurring on DNA. A hairpin polyamide having an alkylation site via a vinyl linker at the end of a pyrrole-imidazole polyamide. Drugs for inhibiting the expression of a specific gene and anticancer agents containing the above hairpin polyamide.Type: GrantFiled: March 3, 2003Date of Patent: November 25, 2008Assignee: Japan Science and Technology AgencyInventors: Hiroshi Sugiyama, Toshikazu Bando, Isao Saito
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Publication number: 20080221191Abstract: A method of treating a Mycobacterium tuberculosis infection in a subject in need thereof by administering to the subject an effective amount of a cationic substituted benzofuran compound. Methods of treating microbial infections, including infections from protozoan pathogens, such as Leishmania donovani, Trypanosoma brucei rhodesiense, a Trypanosoma cruzi, and Plasmodium falciparum, and fungal pathogens, such as Candida albicans, Aspergillus fumigatus, and Cryptococcus neoformans, in a subject in need thereof by administering to the subject an effective amount of a cationic substituted benzofuran compound. Methods of synthesizing novel cationic substituted benzofuran compounds and the novel compounds themselves.Type: ApplicationFiled: October 31, 2007Publication date: September 11, 2008Inventors: Richard R. Tidwell, Karl Werbovetz, Scott Gary Franzblau, Svetlana Bakunova, Stanislav Bakunov
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Patent number: 7419997Abstract: The present invention relates to novel compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds.Type: GrantFiled: June 7, 2004Date of Patent: September 2, 2008Assignee: SmithKline Beecham CorporationInventors: Sharon Davis Boggs, Kristjan S Gudmundsson
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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: 7396849Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.Type: GrantFiled: September 20, 2005Date of Patent: July 8, 2008Assignee: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gil, John E. Donello, Michael E. Garst, Larry A. Wheeler
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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: 20080153816Abstract: Indole compounds corresponding to the formula (I): as defined in the claims, pharmaceutically acceptable addition salts of such compounds, pharmaceutical compositions containing such compounds, the process for their preparation, and their use as pharmacologically active substances, especially in the treatment of hypertriglyceridemia, hyperlipidemia, hypercholesterolemia, diabetes, endothelial dysfunction, cardiovascular disease, inflammatory disease and neurodegeneration.Type: ApplicationFiled: February 28, 2008Publication date: June 26, 2008Applicant: Laboratoires Fournier S.A.Inventors: Jean BINET, Benaissa Boubia, Pierre Dodey, Christiane Legendre, Martine Barth, Olivia Poupardin-Olivier
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Patent number: 7390798Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.Type: GrantFiled: February 9, 2005Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
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Patent number: 7378421Abstract: 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: GrantFiled: April 28, 2004Date of Patent: May 27, 2008Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Teresa Mujica-Fernaud, Herwig Buchholz, Wilfried Rautenberg, Christian Sirrenberg
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Patent number: 7375125Abstract: Provided are MC4-R binding compounds of the formula XVII: wherein L2 is a linker group, and P1, P2, P3, P4, Z1, Z2, Z3, Z4, Z5, t, s, and R are as described in the specification. Methods of using the compounds to treat MC4-R associated disorders, such as disorders associated with weight loss, are also provided.Type: GrantFiled: June 16, 2003Date of Patent: May 20, 2008Assignee: Ore Pharmaceuticals, Inc.Inventors: Tricia J. Vos, Michael E. Solomon, Christopher F. Claiborne, Martin P. Maguire, Mingshi Dai, Michael Patane, Thomas H. Marsilje
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Publication number: 20080114040Abstract: Epothilone derivatives of Formula (I) and their use as a pharmaceutical.Type: ApplicationFiled: March 15, 2005Publication date: May 15, 2008Applicant: NOVARTIS AGInventor: Karl-Heinz Altmann
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Publication number: 20080108682Abstract: The invention relates to a method for manufacturing R-(?)-sertaconazole mononitrate. The invention also relates to R-(?)-sertaconazole mononitrate hemiacetonate.Type: ApplicationFiled: September 13, 2005Publication date: May 8, 2008Applicant: Ferrer Internacional, S. A.Inventors: Ines Petschen, Xavier Camps, Juan Sallares
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Patent number: 7368569Abstract: This invention relates to a process for making spirolactone compounds analogous to formula IType: GrantFiled: October 14, 2003Date of Patent: May 6, 2008Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Ralph P. Volante, David M. Tschaen, Steven A. Weissman, Matthew Heileman, Toshiaki Mase, Takehiko Iida, Kenji Maeda, Toshihiro Wada, Hiroki Sato, Kenichi Asakawa
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Patent number: 7358377Abstract: 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: GrantFiled: March 29, 2005Date of Patent: April 15, 2008Assignees: University of Iowa Research Foundation, The United States of AmericaInventors: David F. Wiemer, Jeffrey D. Neighbors, John A. Beutler
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Patent number: 7358239Abstract: 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; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; 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 isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 7323433Abstract: The invention relates to R-(?)-1-[2-(7-Chloro-benzo[b]thiophen-3-yl-methoxy)-2-(2,4-dichloro-phenyl)-ethyl]-1H-imidazole and the salts thereof. The invention also relates to compositions thereof and their use either for treating fungal infections in humans and animals or combating crop diseases. A process for their preparation is also described.Type: GrantFiled: August 5, 2004Date of Patent: January 29, 2008Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet, Jorge Ramentol, Lluis Anglada, Celia Palacin, Antonio Guglietta
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Patent number: 7304072Abstract: Compounds represented by the general formula (I) wherein Ar1 represents an aryl or heteroaryl which may be substituted; n represents 0 or 1; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine, hydroxy substituted methine or nitrogen atom; Y represents an imino which may be substituted with lower alkyl, or oxygen; and a salt, ester or N-oxide derivative thereof. The compounds exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metabolic diseases, sexual and reproductive dysfunctions, gastro-intestinal disorders, respiratory disorders, inflammation or glaucoma, and the like.Type: GrantFiled: August 23, 2004Date of Patent: December 4, 2007Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh, Masato Chiba
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Patent number: 7291642Abstract: The present invention provides bradykinin-B1 antagonists of the formula in which A, Ar, G, Q, R1 and R4 are as defined in claim 1, their enantiomers, their diastereomers, their mixtures and their salts, in particular their physiologically acceptable salts with organic or inorganic acids or bases having useful properties, their preparation, medicaments comprising the pharmacologically effective compounds, their preparation and their use.Type: GrantFiled: October 21, 2005Date of Patent: November 6, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Iris Kauffmann-Hefner, Norbert Hauel, Henri Doods, Angelo Ceci, Stefan Peters
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Patent number: 7288660Abstract: The invention provides a process for preparing ondansetron hydrochloride dihydrate particles in which at least about 70% of the particles have a particle size of less than 250 ?m, comprising the steps of: (a) preparing a solution comprising ondansetron hydrochloride and water; and (b) adding the solution into a precipitation medium which comprises a water-miscible nonsolvent for ondansetron hydrochloride, while maintaining the resulting mixture at a temperature of about 40° C. or less.Type: GrantFiled: May 5, 2005Date of Patent: October 30, 2007Assignee: Taro Pharmaceutical Industries LimitedInventors: Daniella Gutman, Rosa Cyjon
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Patent number: 7279497Abstract: The present invention relates to benzopyran derivatives substituted with secondary amines including imidazole, their preparation, and pharmaceutical compositions containing them. The present invention is pharmacologically useful for the treatment of cancer, rheumatoid arthritis, and diabetic retinopathies through anti-angiogenic properties, and also pharmacologically useful in the protection of heart and neuronal cells against ischemia-reperfusion injury or preserving organs.Type: GrantFiled: July 30, 2003Date of Patent: October 9, 2007Assignee: Korea Research Institute of Chemical TechnologyInventors: Kyu Yang Yi, Sun Kyung Lee, Sung-Eun Yoo, Jee Hee Suh, Nak Jeong Kim, Sun Kyung Hwang, Byung-Ho Lee, Ho Won Seo, Chong Ock Lee, Sang-Un Choi
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Publication number: 20070197621Abstract: The present invention relates a method for treating 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 R, R1, R2, A and n are as defined in the specification and to their pharmaceutically active salts. The invention also relates to novel compounds of formula I, pharmaceutical compositions containing them, and methods for their preparation.Type: ApplicationFiled: January 19, 2007Publication date: August 23, 2007Inventors: Guido Galley, Katrin Groebke Zbinden, Marius Hoener, Sabine Kolczewski, Roger Norcross, Henri Stalder