The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/253)
-
Publication number: 20100130448Abstract: The present invention provides a 3?,4?,5-trimethoxy flavone derivative and a pharmaceutically acceptable salt thereof, preparation thereof, and a pharmaceutical composition for the treatment and prevention of dry eye syndrome comprising the same as an active ingredient. The 3?,4?,5-trimethoxy flavone derivative and its pharmaceutically acceptable salt inhibit corneal damage through excellent stimulatory action on mucus secretion in the conjunctiva and therefore may be effective as a prophylactic or therapeutic agent for dry eye syndrome.Type: ApplicationFiled: June 2, 2008Publication date: May 27, 2010Applicant: DONG-A PHARM. CO., LTDInventors: Seul-Min Choi, Kyung-Koo Kang, Dong-Sung Kim, Jeong-Hoon Kim, Byoung-Ok Ahn, Moo-Hi Yoo, Mi-Jeong Seo, Ju-Mi Kim, Yong-Duck Kim, Sun-Woo Jang, Yong-Sung Shon
-
Publication number: 20100121072Abstract: Provided are candesartan cilexetil forms and methods of their preparation. Also provided are pharmaceutical compositions prepared by combining at least one pharmaceutically-acceptable excipient with at least one candesartan cilexetil form of the invention.Type: ApplicationFiled: January 13, 2010Publication date: May 13, 2010Inventors: Marina Yu Etinger, Boris Fedotev, Tamas Koltai, Ziv Kurgan, Omer Malachi
-
Publication number: 20100113798Abstract: A process for the preparation of Irbesartan of formula (I) using the step of, reacting biphenyl derivative of formula (VIa) wherein R represents a group selected from —CONH2 or compound of formula wherein X represents H or C1-4 alkyl, preferably methyl; or any other such group which can be converted to cyano group, with 1-veleramido cyclopentane carboxylic acid of formula (V) in the presence of an acid in an organic solvent to give biphenyl derivative of formula (VIIa) wherein R has the same meaning as mentioned hereinabove.Type: ApplicationFiled: January 7, 2010Publication date: May 6, 2010Applicant: ALEMBIC LIMITEDInventors: Pandurang Balwant Deshpande, Parven Kumar Luthra, Dhiraj Mohansinh Rathod, Hitesh Kantilal Patel, Pinky Tarak Parikh
-
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
-
Publication number: 20100094023Abstract: Benzoylpyrazoles represented by the following formula (I), and use thereof as herbicides. R1 represents alkyl; R2 represents alkyl or cycloalkyl; R3 represents hydrogen, alkyl, alkenyl, alkynyl, aralkyl, alkylsulfonyl, optionally substituted phenylsulfonyl, acyl or acylalkyl; X represents halogen or alkyl; Y represents halogen; n represents 2 or 3, and T represents the above group T1 or T2, wherein R4 represents hydrogen, alkyl, alkoxy or alkylthio.Type: ApplicationFiled: October 2, 2007Publication date: April 15, 2010Applicant: Bayer CropScience AGInventors: Shinichi Narabu, Ysushi Yoneta, Akihiko Yanagi, Shinichi Shirakura, Seiji Ukawa, Teruyuki Ichihara, Shin Nakamura, Martin Hills, Heinz Kehne, Jan Dittgen, Dieter Feucht, Christopher Rosinger
-
Publication number: 20100081826Abstract: A compound of Formula (I):Type: ApplicationFiled: November 24, 2009Publication date: April 1, 2010Applicant: Paratek Pharmaceuticals, Inc.Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
-
Patent number: 7687481Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.Type: GrantFiled: March 9, 2007Date of Patent: March 30, 2010Assignee: Jenrin Discovery, Inc.Inventors: John Francis McElroy, Robert J. Chorvat
-
Publication number: 20100076200Abstract: The present invention provides a process for purifying olmesartan medoxomil.Type: ApplicationFiled: September 17, 2009Publication date: March 25, 2010Inventors: Lilach Hedvati, Gideon Pilarsky, Yuriy Raizi, Esti Esty Marom
-
Publication number: 20100056797Abstract: The present invention relates to an improved process for the preparation of 2-n-butyl-3-[[2?-(1H-tetrazol-5-yl)[1,1?-biphenyl]-4-yl]-1,3-diazaspiro[4.Type: ApplicationFiled: April 23, 2007Publication date: March 4, 2010Inventors: Venkata vara prasada rao Korrapati, Venkata subramanyeswara rao Inti, Rani Ananta, Ramesh Dandala, Sivakumaran Meenakshisunderam
-
Patent number: 7666857Abstract: An improved thrombopoietin mimetic, the choline salt of 2-(3,4-dimethylphenyl)-4-{[2-hydroxy-3?-(1H-tetrazol-5-yl)biphenyl-3-yl]-hydrazono}-5-methyl-2,4-dihydropyrazol-3-one.Type: GrantFiled: October 21, 2004Date of Patent: February 23, 2010Assignee: SmithKline Beecham Corp.Inventors: Christopher S. Brook, Li-Jen J. Ping
-
Patent number: 7662804Abstract: Disclosed herein are novel diazenyl pyrazole compounds and related compounds. Also disclosed herein are methods of using these compounds for the treatment of diseases and conditions associated with modulating a thrombopoietin activity.Type: GrantFiled: November 21, 2006Date of Patent: February 16, 2010Assignee: SmithKline Beecham Corp.Inventors: Lin Zhi, E. Adam Kallel, Dean P. Phillips
-
Patent number: 7659406Abstract: A process for preparing valsartan.Type: GrantFiled: January 3, 2006Date of Patent: February 9, 2010Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.Inventors: Pratap Reddy Padi, Satya Narayana Bollikonda, Ananda Mohan Jasty, Suma Latha Yasareni, Vishal Dayaram Parmar
-
Patent number: 7655680Abstract: Thiazole compounds for inhibiting the activity of phosphodiesterase 4, the production of tumor necrosis factor alpha, and the production of interleukin 4. The compounds of the invention are represented by general formula (1): wherein A is any one of the following groups (i) and (ii): (i) —CO—B— wherein B is a C1-6 alkylene group and (ii) —CO—Ba— wherein Ba is a C2-6 alkenylene group, and include optical isomers and salts of the compounds.Type: GrantFiled: May 16, 2005Date of Patent: February 2, 2010Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Isao Takemura, Kenji Watanabe, Kunio Oshima, Nobuaki Ito, Junpei Haruta, Hidetaka Hiyama, Masatoshi Chihiro, Hideki Kawasome, Yoko Sakamoto, Hironobu Ishiyama, Takumi Sumida, Kazuhiko Fujita, Hideki Kitagaki
-
Publication number: 20100022599Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: July 23, 2009Publication date: January 28, 2010Inventors: Seok-Ki CHOI, Paul R. FATHEREE, Roland GENDRON, Robert Murray MCKINNELL, Brooke BLAIR
-
Publication number: 20100009961Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.Type: ApplicationFiled: June 26, 2009Publication date: January 14, 2010Applicant: Alantos Pharmaceuticals Holding, Inc.Inventors: Heiko Kroth, Tim Feuerstein, Frank Richter, Jurgen Boer, Michael Essers, Bert Nolte, Matthias Schneider, Matthias Hochguertel, Fritz-Frieder Frickel, Arthur Taveras, Christoph Steeneck
-
Publication number: 20100010061Abstract: Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH, or tetrazolyl, and A2 is hydrogen, —COOH, or tetrazolyl, provided that one of A1 and A2 is either —COOH or tetrazolyl; p is 0 or 1 and A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; q is 0 or 1; R3 is hydrogen, C1-C4 alkyl, cycloalkyl, —CF3, or —OR9; R4 and R5 independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl, —CF3, or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, cycloalkyl, fully or partially fluorinated C1-C4 alkyl; R1 isType: ApplicationFiled: December 17, 2007Publication date: January 14, 2010Inventors: Martin Cooper, Jean-Marie Receveur, Thomas Hoegberg, Peter Aadal Nielsen, Jean-Michel Linget, Pia Karina Noeregaard, Anthony Murray, Emelie Bjurling
-
Patent number: 7645799Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: November 7, 2008Date of Patent: January 12, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. P. Pinto
-
Publication number: 20100004159Abstract: The present invention relates to polysubstituted imidazolone derivatives, to the pharmaceutical compositions comprising them and to the therapeutic uses thereof in the human and animal health fields. The present invention also relates to a process for preparing these derivatives.Type: ApplicationFiled: July 24, 2007Publication date: January 7, 2010Applicant: GENFITInventors: Edith Bouey, Christophe Masson, Karine Bertrand
-
Publication number: 20090324540Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: ApplicationFiled: June 10, 2009Publication date: December 31, 2009Applicant: Emisphere Technologies, Inc.Inventors: Donald J. Sarubbi, Eugene N. Barantsevitch
-
Publication number: 20090326220Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5 and R6 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: ApplicationFiled: August 18, 2009Publication date: December 31, 2009Inventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
-
Publication number: 20090326026Abstract: There is provided compounds of formula (I), wherein X1, X2, X3, Y4, Y1, Y2, Y3, Y4, Z1, Z2, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.Type: ApplicationFiled: September 3, 2009Publication date: December 31, 2009Inventors: Mathias ALTERMAN, Anders Rudolf HALLBERG
-
Publication number: 20090326024Abstract: The present invention provides pharmaceutically acceptable salts of imidazole-5-carboxylic acid derivatives, methods for preparing same and pharmaceutical compositions comprising same. The salts obtained by the present invention can be easily dissolved in common solvents, such as water and methanol. The bioavailability thereof is good in animal body. Thereby it is applicable to be developed as a normal preparation for treating hypertension.Type: ApplicationFiled: June 5, 2009Publication date: December 31, 2009Inventors: Jianhui Guo, Dong An
-
Patent number: 7638514Abstract: There are described compounds of formula (I) wherein X1 and X2 are each independently of the other fluorine, chlorine or bromine; A1 and A2 are, for example, a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge; R1 and R2 are, for example, halogen, OH, SH, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkyl-carbonyl, C2-C6alkenyl, C2-C6haloalkenyl or C3-C6alkynyl; R,3 is, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R4 and R5 are, for example, H, halogen, cyano, nitro, C1-C6alkyl or C1-C3haloalkyl; m is 1 or 2; Y is, for example, O, S, SO or SO2; Q is, for example, O, S, SO or SO2; W is, for example, a bond, O, S, SO, S02, —C(?O)—O— or —O—C(?O)—; T is, for example, a bond, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; and E is aryl unsubstituted or substituted from one to five times or heterocyclyl unsubstituted or, depending upon the possibilities of substitution on the ring, substituted from one to four times; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtType: GrantFiled: August 25, 2004Date of Patent: December 29, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: Werner Zambach, Stephan Trah, Roger Graham Hall, William Lutz
-
Publication number: 20090318481Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.Type: ApplicationFiled: August 28, 2009Publication date: December 24, 2009Inventors: Thomas Daniel AICHER, Guillermo S. CORTEZ, Todd Michael GROENDYKE, Albert KHILEVICH, James Allen KNOBELSDORF, Fredrik Pehr MARMSATER, Jeffrey Michael SCHKERYANTZ, Tony Pisal TANG
-
Publication number: 20090318518Abstract: The invention is directed to indole and indoline cyclopropyl amide derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: February 22, 2008Publication date: December 24, 2009Inventors: Michael Boyd, John Colucci, Yongxin Han
-
Publication number: 20090318517Abstract: This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production.Type: ApplicationFiled: June 23, 2009Publication date: December 24, 2009Applicant: ASTRAZENECA ABInventors: Jonas Branalt, David Gustafsson, Ingemar Nilsson, Magnus Polla
-
Publication number: 20090318483Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.Type: ApplicationFiled: August 28, 2009Publication date: December 24, 2009Inventors: Thomas Daniel AICHER, Guillermo S. CORTEZ, Todd Micheal GROENDYKE, Albert KHILEVICH, James Allen KNOBELSDORF, Fredrik Pehr MARMSATER, Jeffrey Michael SCHKERYANTZ, Tony Pisal TANG
-
Publication number: 20090318706Abstract: The present invention provides an improved synthesis for the manufacture of candesartan and pharmaceutically acceptable salts and esters thereof as active ingredients of a medicament for the treatment of hypertension and related diseases and conditions which comprises the removal of the tetrazolyl protecting group in an organic solvent, and in the presence of a Lewis acid.Type: ApplicationFiled: September 29, 2006Publication date: December 24, 2009Inventor: Silvo Zupancic
-
Patent number: 7635662Abstract: A urea-urethane compound having one or more urea groups and one or more urethane groups in the molecular structure, the number of said urea groups (A) and the number of said urethane groups (B) satisfying the following numerical formula: 10?(A+B)?3 wherein each of A and B is an integer of 1 or more.Type: GrantFiled: March 2, 2001Date of Patent: December 22, 2009Assignee: Chemipro Kasei Kaisha, Ltd.Inventors: Kazuo Kabashima, Hiroshi Kobayashi, Tetsurou Iwaya
-
Publication number: 20090312366Abstract: The present application is directed to novel P2X7R antagonists that are indol-3-carboxamide or azaindole-3-carboxamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.Type: ApplicationFiled: March 25, 2009Publication date: December 17, 2009Applicant: AFFECTIS PHARMACEUTICALS AGInventor: Michael Bös
-
Publication number: 20090312352Abstract: The invention generally relates to compositions and methods for treatment of disease caused by Yersinia spp. infection. More specifically, the invention relates to protein tyrosine phosphatase inhibitors and derivatives and analogs thereof, pharmaceutical compositions containing the protein tyrosine phosphatase inhibitors and analogs, methods of making the protein tyrosine phosphatase inhibitors and analogs and methods of use thereof.Type: ApplicationFiled: October 19, 2005Publication date: December 17, 2009Inventors: Tomas Mikael Mustelin, Maurizio Pellecchia, Lutz Tautz
-
Publication number: 20090304797Abstract: The present invention relates to process for preparing micronized Valsartan with particle size distribution of d10 less than 5?, d50 less than 10? and d90 less than 20? preferably d90<10?.Type: ApplicationFiled: June 22, 2007Publication date: December 10, 2009Inventors: Venkatasubramanian Radhakrishnan Tarur, Dhananjay Govind Sathe, Narayana Rao, Kamles Digambar Sawant, Sasi Kumar Mohan Thoovara, Bhupendra Shaligram Rane
-
Publication number: 20090306112Abstract: The invention is related to compounds of Formula I or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 19, 2007Publication date: December 10, 2009Applicant: Gilead Sciences, Inc.Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu, Zheng-Yu Yang
-
Publication number: 20090306078Abstract: Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer activity thanks to the inhibition activity against HIF-1, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer; stomach cancer and breast cancer. Also, the compound having inhibition activity against HIF-1 is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HIF-1-mediated VEGF expression.Type: ApplicationFiled: July 3, 2007Publication date: December 10, 2009Applicant: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGYInventors: Jung Joon Lee, Jeong-Hyung Lee, Kyeong Lee, Young-Soo Hong, B.K. Shanthaveerappa, Yinlan Jin, Jin Hwan Kim, Xuejun Jin
-
Publication number: 20090298899Abstract: The disclosure provides EP2 receptor agonist compounds and methods for using the compounds for treating conditions which can be alleviated by agonism of an EP2 receptor.Type: ApplicationFiled: December 30, 2008Publication date: December 3, 2009Inventors: Alexander William Oxford, Richard Jon Davis, Robert Alexander Coleman, Kenneth Lyle Clark, David Edward Clark, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Mark Richard Ashton, Edward Andrew Boyd, Shirley Ann Brunton
-
Patent number: 7625933Abstract: Indoles of Formula I having —X-aryl-(CH2)x-oxazolidinedione and —X-heteroaryl-(CH2)x-oxazolidinedione substituents on the N atom of the indole ring, where x is 0 or 1, and —X— is a bond or —CH2—, and their thiazolidinedione analogs, are PPAR gamma agonists or partial agonists and are useful in the treatment and control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.Type: GrantFiled: June 28, 2005Date of Patent: December 1, 2009Assignee: Merck & Co., Inc.Inventors: Kun Liu, Peter T. Meinke, Harold B. Wood
-
Patent number: 7625932Abstract: The present invention relates to pyrrole and pyrazole compounds of formula (I) and their pharmaceutically acceptable salts, and further relates to their use in treating schizophrenia, cognitive deficits associated with schizophrenia, Alzheimer's disease, dementia of the Alzheimer's type, mild cognitive impairment, or depression. The compounds act as potentiators on glutamate receptors, in particular AMPA and the GluR family.Type: GrantFiled: August 27, 2004Date of Patent: December 1, 2009Assignee: Eli Lilly and CompanyInventors: Pamela Ann Albaugh, Esteban Dominguez-Manzanares, Jian Eric Hong, William Joseph Hornback, Delu Jiang, Paul Leslie Ornstein, Michelle Lee Thompson, Eric George Tromiczak, Zhipei Wu, Hamideh Zarrinmayeh, Dennis Michael Zimmerman, Ana Maria Castano Mansanet, Larry Gene Huffman, William David Miller
-
Patent number: 7625926Abstract: The bioavailability of an anticancer agent is enhanced when the anticancer agent is administered together with a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 6, 2004Date of Patent: December 1, 2009Assignee: Hanmi Pharm. Co., LtdInventors: Keuk Chan Bang, Mi Young Cha, Young Gil Ahn, Young Jin Ham, Maeng Sup Kim, Gwan Sun Lee
-
Publication number: 20090291968Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: ApplicationFiled: March 21, 2007Publication date: November 26, 2009Inventors: Guy Georges, Bernhard Goller, Anja Limberg, Petra Rueger, Matthias Rueth, Christine Schuell, Mark Stahl
-
Publication number: 20090281326Abstract: The present invention provides a method for the preparation of N-(1-oxopentyl)-N-[[2?-(1H-tetra-zol-5-yl)[1,1?-biphenyl]-4-yl]methyl]-L-valine (Valsartan) which comprises; treating N-[[2?-(1-triphenylmethyl-tetra-zol-5-yl)biphenyl-4-yl]methyl]-L-valine methyl ester (X) with oxalic acid or its hydrates in a solvent to produce N-[[2?-(1-triph-enylmethyl-tetrazol-5-yl)biphenyl-4-yl]methy]-L-valine methyl ester oxalate (Xa) and treating the compound (Xa) with a base in a solvent followed by reacting with valeryl chloride in presence of base in a solvent to produce N-[[2?-(1-triphenylmethyl-tetra-=zol-5-yl)[1,1?biphenyl]-4-yl]methyl]-N-valeryl-L-valine methyl ester (XI), de-protecting the compound (XI) using anhydrous acidic conditions to produce N-(1-oxopentyl)-N-[[2?-(1-H-tetrazol-5-yl)[1,1?biphenyl]-4-yl]methyl-L-valine methyl ester (V) followed by <treating with base in a solvent to produce Valsartan.Type: ApplicationFiled: June 29, 2007Publication date: November 12, 2009Inventors: Sankar Reddy Budidet, Senthil Kumar Natarajan, Venkata Kishore Gowrabathina, Ramesh Dandala, Sivakumaran Meenakshisunderam
-
Publication number: 20090270421Abstract: Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having Ki's below 200 pM and activities 102-103 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, viz.: 1.) an ?-keto heterocylic head group; 2.) a hydrocarbon linkage unit employing an optimal C12-C8 chain length; and 3.) a phenyl or other ?-unsaturation corresponding to the arachidonyl ?8,9/?11,12 and/or oleyl ?9,10 positions. A preferred ?-keto heterocylic head group is ?-keto N4 oxazolopyridine, with incorporation of a second weakly basic nitrogen. Fatty acid amide hydrolase is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors).Type: ApplicationFiled: April 24, 2009Publication date: October 29, 2009Applicant: The Scripps Research InstituteInventor: Dale L. Boger
-
Patent number: 7598423Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.Type: GrantFiled: November 15, 2005Date of Patent: October 6, 2009Assignee: Eli Lilly and CompanyInventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
-
Publication number: 20090247596Abstract: The invention is directed to thiophenecarboxamide derivatives of formulae I and II as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, cancer and glaucoma. Pharmaceutical compositions and methods of use are also included. (Formulas I and II).Type: ApplicationFiled: August 10, 2007Publication date: October 1, 2009Inventors: Marc Blouin, Jason Burch, Yongxin Han, Christophe Mellon
-
Publication number: 20090247591Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain or other conditions.Type: ApplicationFiled: March 25, 2009Publication date: October 1, 2009Applicant: Grunenthal GmbHInventors: Saskia Zemolka, Bert Nolte, Klaus Linz, Derek John Saunders, Wolfgang Schroder, Wemer Englberger, Fritz Theil, Hans Schick, Jens Kaufmann, Julian Gebauer, Helmut Sonnenschein
-
Publication number: 20090247595Abstract: The invention provides a method for preparing candesartan cilexetil and related tetrazolyl compounds. More particularly, the invention relates to the preparation of candesartan cilexetil and related tetrazolyl compounds and includes a method of removing a protective group (e.g., triphenylmethane (trityl) protecting group) from an N-protected tetrazolyl compound using a Lewis acid in an inert solvent and in the presence of an alcohol (e.g., reacting an N-protected tetrazolyl compound with ZnCl2 in the presence of an alcohol).Type: ApplicationFiled: June 6, 2006Publication date: October 1, 2009Inventor: Nuria Soldevilla Madrid
-
Publication number: 20090216026Abstract: Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4?-bromobenzyl)-1,3-diazaspiro[4.4]non-1-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid.Type: ApplicationFiled: December 18, 2008Publication date: August 27, 2009Inventors: Gennady Nisnevich, Igor Rukhman, Julia Kaftanov
-
Publication number: 20090215843Abstract: The present application relates to novel tetrazole derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: October 9, 2006Publication date: August 27, 2009Inventors: Stephan Bartel, Michael Hahn, Wahed Ahmed Moradi, Eva-Maria Becker, Thomas Rölle, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Andreas Knorr
-
Patent number: 7576112Abstract: A compound having a structure and therapeutic methods, compositions, and medicaments related thereto are disclosed herein.Type: GrantFiled: February 17, 2009Date of Patent: August 18, 2009Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
-
Publication number: 20090203921Abstract: The present invention relates to processes for the preparation of intermediates of valsartan.Type: ApplicationFiled: February 12, 2009Publication date: August 13, 2009Inventors: Ira Saxena, Asok Nath, Mohan Prasad
-
Publication number: 20090203920Abstract: The invention relates to a method for isolating 5-substituted tetrazoles of general formula (I) in which R represents a substituted biphenyl radical during which the ring closure, starting from a corresponding nitrile, is carried out in organic solvents while using alkali, alkaline-earth or organotin azides. The organic phases containing the nitrile and the tetrazol are firstly mixed with water while firstly forming three liquid phases, after which the aqueous phase containing the azide and the phase containing the nitrile are separated out, and the middle organic phase containing the tetrazol is subsequently processed. In the case of ester groups to be saponified, this phase is mixed with alkali lye, after which the organic phase is separated out and the aqueous phase is acidified or otherwise, this phase is immediately acidified and purified.Type: ApplicationFiled: August 3, 2006Publication date: August 13, 2009Applicant: SANOCHEMIA PHARMAZEUTIKA AGInventors: Stefan Welzig, Anton Gerdenitsch, Wolfgang Oberleitner