Amide Patents (Class 562/450)
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Publication number: 20100324140Abstract: The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.Type: ApplicationFiled: August 26, 2010Publication date: December 23, 2010Applicant: ELI LILLY AND COMPANYInventors: Scott Eugene CONNER, Guoxin ZHU, Jianke LI
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Publication number: 20100305131Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: May 27, 2010Publication date: December 2, 2010Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
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Publication number: 20100286427Abstract: A compound represented by the following general formula (I): [R1 to R5 represent hydrogen atom, an alkyl group, or a trialkylsilyl group, X represents —NH—CO—, —CO—NH—, —N(COR6)—CO—, —CO—N(COR7)— (R6 and R7 represent a lower alkoxy group, or a carboxy-substituted phenyl group) etc.; and Z represents —Y—CH(R12)—COOH, —CHO, —CH?CH—COOH, or —COOR13 (Y represents a single bond, —CH2—, —CH(OH)—, —CO—, —CO—NH—, or —CO—NH—CH2—CO—NH—, R12 represents hydrogen atom or a lower alkyl group, and R13 represents hydrogen atom, —CH(R14)—COOH(R14 represents hydrogen atom, a lower alkyl group, or hydroxy group), —[CH2CH2—O]n—CH2—CH2—OH, —CH2—O—[CH2CH2—O]m—CH2—OH, or —[CH(CH3)—CO—O]p—CH(CH3)—COOH (m, n and p represent an integer of 1 to 100))], a salt thereof or an ester thereof, which has a property of being converted into a retinoid after absorption in vivo.Type: ApplicationFiled: October 31, 2007Publication date: November 11, 2010Applicant: RESEARCH FOUNDATION ITSUU LABORATORYInventors: Hideaki Muratake, Koichi Shudo
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Publication number: 20100273725Abstract: The present invention relates to photosensitizer compounds for use in cosmetic and therapeutic applications of photodynamic therapy. The compounds of the present invention are designed for topical application and are characterized by a low permeability to the stratum corneum (the outer skin layer of an individual) and/or a low allergenic potential. Surprisingly, such compounds have beneficial properties in the treatment of certain diseases and lack the undesired damages to healthy skin entailed by prior art compounds. ALA (5-aminolevulinic acid)-esters of body-owned, natural compound such as aminoacids, steroids, carbohydrades, alcohols are preferred, examples of photosensitizers of the present invention. The compounds of the present invention are used in the treatment of skin diseases such as psoriasis, sebaceous glands related conditions including acne, seborrhoic dermatitis, rosacea, skin cancer and precancer, as well as in cosmetic hair removal.Type: ApplicationFiled: December 12, 2008Publication date: October 28, 2010Inventors: Thomas Glanzmann, Jérôme Barge, Georges Wagnieres
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Patent number: 7816557Abstract: The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.Type: GrantFiled: June 8, 2005Date of Patent: October 19, 2010Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, Guoxin Zhu
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Publication number: 20100256414Abstract: The invention relates to N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine (nateglinide) in the novel crystalline form “G” and a process for the preparation thereof. A process for the preparation of chirally pure nateglinide by treating a lower alkyl ester thereof with a base to yield an alkali salt and liberating the product from said salt by proper addition of an acid, is also provided. Still another aspect of the invention is a process for the preparation of nateglinide in the crystalline form “H” from other crystalline modifications of nateglinide.Type: ApplicationFiled: April 7, 2010Publication date: October 7, 2010Inventors: Maria Gazdag, Tibor Gizur, Bela Hegedus, Attila Szemzo, Gabor Tarkanyi, Jozsef Törley, Monika Babjak
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Publication number: 20100234307Abstract: This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: ApplicationFiled: May 6, 2010Publication date: September 16, 2010Applicant: Bayer HealthCare LLCInventors: Roger A. Smith, Derek Lowe, Tatiana Shelekhin, Georgiy Bondar, Philip Coish, Stephen J. O'Connor
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Patent number: 7790770Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.Type: GrantFiled: November 13, 2006Date of Patent: September 7, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Mark E. Salvati, Heather Finlay, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
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Publication number: 20100216886Abstract: Disclosed are novel polymorphic forms of N2-(1,1?-biphenyl-4-ylcarbonyl)-N1-[2-(4-fluorophenyl)-1,1-dimethylethyl]-L-?-glutamine, methods of preparing the polymorphic forms, compositions containing the polymorphic forms, and methods of treatment using the polymorphic forms.Type: ApplicationFiled: November 9, 2007Publication date: August 26, 2010Applicant: WyethInventors: Qiuxia Wang, Jennifer Qianying Liang, Mannching Sherry Ku, Ronald Stanley Michalak, Wen James Huang
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Patent number: 7781470Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.Type: GrantFiled: April 13, 2009Date of Patent: August 24, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
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Patent number: 7767847Abstract: The invention relates to N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine (nateglinide) in the novel crystalline form “G” and a process for the preparation thereof. A process for the preparation of chirally pure nateglinide by treating a lower alkyl ester thereof with a base to yield an alkali salt and liberating the product from said salt by proper addition of an acid, is also provided. Still another aspect of the invention is a process for the preparation of nateglinide in the crystalline form “H” from other crystalline modifications of nateglinide.Type: GrantFiled: July 8, 2004Date of Patent: August 3, 2010Assignee: Richter Gedeon Vegyeszeti Gyar RT.Inventors: Maria Gazdag, Tibor Gizur, Bela Hegedus, Attila Szemzo, Gabor Tarkanyi, Jozsef Törley, Monika Babjak
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Patent number: 7754897Abstract: This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R3, R4 and R5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.Type: GrantFiled: June 15, 2006Date of Patent: July 13, 2010Assignee: Cardiome Pharma Corp.Inventors: Grace Jung, James Gee Ken Yee, Doug Ta Hung Chou, Bertrand M. C. Plouvier
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Publication number: 20100172844Abstract: The invention relates to portable albumin binders, which are useful for improving the pharmacokinetic properties of diagnostic or therapeutic agents, in particular increasing the blood circulations time and/or the tissue penetration capacity of such agents.Type: ApplicationFiled: November 2, 2007Publication date: July 8, 2010Inventors: Dario Neri, Christoph Dumelin
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Patent number: 7750181Abstract: This invention relates to certain dioxodihydropyridine derivatives and certain methacrylic acid and furan derivative precursors thereof, processes for their preparation, pharmaceutical compositions containing such compounds and their use as anti-proliferative agents, especially tumour growth inhibitors and anti-cancer agents, antibiotics and/or antiviral agents.Type: GrantFiled: March 9, 2005Date of Patent: July 6, 2010Assignee: EPX Research LimitedInventors: Washington Odur Ayuko, Michael John Tisdale, Eric Lattmann
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Publication number: 20100168079Abstract: The present invention relates to biaryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: December 21, 2009Publication date: July 1, 2010Inventors: Daniela Angst, Birgit Bollbuck, Philipp Janser, Jean Quancard
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Patent number: 7745489Abstract: Specific, highly potent 2-oxo-amide based inhibitors of phospholipase A2 (PLA2) activity are provided. A role for PLA2 activity in spinally mediated inflammatory processes is established, and a method for treating hyperalgesia and other inflammatory conditions associated with PLA2 activity is provided.Type: GrantFiled: March 7, 2003Date of Patent: June 29, 2010Assignee: The Regents of the University of CaliforniaInventors: Edward Dennis, Tony Yaksh, Karin Killermann Lucas, Camilla Svensson, David A. Six, George Kokotos, Violetta Constantinou-Kokotou
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Publication number: 20100152460Abstract: The present invention is directed to novel processes for the preparation of opioid modulators (agonists and antagonists) and intermediates in their synthesis. The opioid modulators are useful for the treatment and prevention of as pain and gastrointestinal disorders.Type: ApplicationFiled: November 25, 2009Publication date: June 17, 2010Inventors: Chaozhong Cai, Wei He
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Publication number: 20100145090Abstract: The present invention is directed to a novel process for the preparation of protected L-alanine derivatives, useful as intermediates in the synthesis of compounds useful as mu/delta opioid modulators.Type: ApplicationFiled: October 27, 2009Publication date: June 10, 2010Inventors: Luigi ANZALONE, Penina FEIBUSH, Frank J. VILLANI
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Patent number: 7732492Abstract: The present invention provides a small-sized preparation that is easy to take, containing 26% or more of nateglinide and 28% or more of at least one disintegrant selected from the group consisting of carmellose or salts thereof, sodium carboxymethyl starch, croscarmellose sodium, crospovidone, partly pregelatinized starch and low-substituted hydroxypropyl cellulose, based on the total mass of the preparation. The preparation of the present invention has high contents of nateglinide, which can be absorbed immediately to exhibit a hypoglycemic action.Type: GrantFiled: February 8, 2006Date of Patent: June 8, 2010Assignee: Ajinomoto Co., Inc.Inventors: Chisato Makino, Erika Motomura, Kunikazu Suzuki, Takahiko Andou, Nobutaka Ninomiya, Akira Yabuki
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Publication number: 20100129311Abstract: The present invention relates to new phenylalanine amide inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 23, 2009Publication date: May 27, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Publication number: 20100093536Abstract: The present disclosure concerns specific herbicide molecules, herbicidal compositions comprising the molecules and the bacterial strains that produce certain of these molecules, and methods of using these molecules and bacterial strains to control grassy weeds and other sensitive weed species.Type: ApplicationFiled: September 25, 2009Publication date: April 15, 2010Inventors: DONALD J. ARMSTRONG, MARK D. AZEVEDO, KERRY L. MCPHAIL, MICHAEL D. JACKSON, DALLICE I. MILLS, GARY BANOWETZ, MURALIDHARA THIMMAIAH, ANNE B. HALGREN
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Patent number: 7696248Abstract: The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.Type: GrantFiled: November 7, 2006Date of Patent: April 13, 2010Assignee: Eli Lilly and CompanyInventors: Jianke Li, Scott Eugene Conner, Guoxin Zhu
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Patent number: 7687662Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.Type: GrantFiled: July 2, 2008Date of Patent: March 30, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Edward J. Olhava, Mihaela Diana Danca
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Patent number: 7671090Abstract: The present invention relates to a phenylalanine derivative of Formula (I) wherein X1 is a halogen atom, X2 is a halogen atom, Q is a CH2R— is a carboxyl group which may be esterified; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 7, 2008Date of Patent: March 2, 2010Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Takayuki Kawaguchi, Sumihiro Nomura, Mikiko Tsukimoto, Toshiyuki Kume, Ila Sircar
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Patent number: 7662994Abstract: The present invention describes a novel method for the purification of dexloxiglumide by crystallization from isopropyl ether which permits the production, in a reproducible manner, of a product with morphological and particle-size characteristics such as to favor its use in the preparation of oral pharmaceutical forms on an industrial scale.Type: GrantFiled: June 21, 2004Date of Patent: February 16, 2010Assignee: Rottapharm S.p.A.Inventors: Francesco Makovec, Lucio Claudio Rovati
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Patent number: 7659311Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16 alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above.Type: GrantFiled: April 29, 2008Date of Patent: February 9, 2010Assignee: Novartis AGInventors: William Elliott Bay, Rajesh K. Agarwal, Kiran Chaudhary, Shingai Majuru, Michael M. Goldberg, JoAnne P. Corvino, Moise Azria, Joseph Ault, Simon D. Bateman, Subash Patel, Joseph Sikora, Rebecca F. Yang, Joseph L. Zielinski
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Patent number: 7642289Abstract: The present invention relates to nitrooxyderivatives or salts thereof having the following general formula (I): R—NR1c—(K)k0—(B)b0—(C)c0—NO2??(I) wherein c0, b0 and k0 are 0 or 1; R is the radical of an analgesic drug for chronic pain, for instance neurophatic pain; R1c is H or alkyl with from 1 to 5 carbon atoms; B is such that its precursor is selected from amino acids, hydroxy acids, polyalcohol, compounds; C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.Type: GrantFiled: December 3, 2003Date of Patent: January 5, 2010Assignee: Nicox S.A.Inventors: Ennio Ongini, Nicoletta Almirante, Piero Del Soldata
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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
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Publication number: 20090305891Abstract: The disclosure relates to novel cycloalkylphenyl-substituted cyclic ketoenols of the formula (I) in which J, X, Y, m and CKE are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the disclosure relates to selective herbicidal compositions comprising, firstly, the cycloalkylphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The disclosure furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.Type: ApplicationFiled: February 8, 2007Publication date: December 10, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Dieter Feucht, Eva-Maria Franken, Olga Malsam, Alfred Angermann, Guido Bojack, Christian Arnold, Martin Jeffrey Hills, Heinz Kehne, Christopher Hugh Rosinger
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Publication number: 20090291978Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, C(?O)—, —S(?O)2—, —C(—O)O—, —C(O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L is a divalent radical of formula -(Alk1)m(O)n(Alk2)p— wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or hetero-cyclic rType: ApplicationFiled: May 4, 2006Publication date: November 26, 2009Applicant: CHROMA THERAPEUTICS LTD.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Moffat, Kenneth William John Baker, Alistair David Graham Donald
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Publication number: 20090281160Abstract: This invention relates to a process for the synthesis of ketomethylene derivatives of the tripeptide Phe-Gly-Pro (“keto-ACE”, compound 5a) and analogues thereof. The synthesis process proceeds via an ?,?-unsaturated keto intermediate. A key feature of the process involves a Horner-Emmons olefination of the, -unsaturated keto-phosphonate with ethyl glyoxylate. Keto-ACE analogues produced by the process of the invention display C-domain selectivity.Type: ApplicationFiled: May 29, 2006Publication date: November 12, 2009Inventors: Edward Sturrock, Aloysius Nchinda, Kelly Chibale
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Patent number: 7605180Abstract: The present invention discloses, as a immediate-release preparation useful as an antidiabetic, a nateglinide-containing preparation comprising nateglinide as an active ingredient wherein the nateglinide is amorphous.Type: GrantFiled: April 24, 2003Date of Patent: October 20, 2009Assignee: Ajinomoto Co., Inc.Inventors: Nobutaka Ninomiya, Chisato Makino, Akira Yabuki
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Patent number: 7601729Abstract: Compounds of Formula (I): wherein: A represents bond, C1-6alkyl or CH?CH—C1-4alkyl; B represents bond, O, S, SO, SO2, CO, CR7R8, CO2R14, CONR14R15, N(COR14)(COR15), N(SO2R14)(COR15) or NR14R15; D represents bond, or C1-6alkyl; E represents substituted aryl or substituted or unsubstituted heteroaryl; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, SO, SO2, CO, CNR5, CNOR5, CNNR5R6, NR11 or CR7R8; Y represents CR5OR11, CR5SR11, NOR5, CR5NR6R11, SO, SO2, CO, CNR5, CNOR5 or CS; R1 and R1? each independently represents H, C1-6alkyl or C1-4alkylaryl; R2 represents CO2R12, CH2OR12 or CONR12R13, CONR12OR13, NR12COR13, SR12, PO(OH)2, PONHR12 or SONHR12; R3 represents H, C1-6alkyl or C1-4alkylaryl; R4 represents optionally substituted aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR5, OCR5R6, CR9R10O or Z, R4 and Q together form an optionally substituted fused tricyclic group; R5 and R6 each independently represent H, C1-6 alkyl or C1-4 alkylaryl;Type: GrantFiled: September 10, 2004Date of Patent: October 13, 2009Assignee: Glaxo Group LimitedInventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
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Publication number: 20090253933Abstract: Nateglinide M-type crystals (main peaks in powder X-ray diffraction: 6.0°, 14.2°, 15.2°, 18.8° (2?)) can be produced by dissolving nateglinide in a solvent in which nateglinide is highly soluble and then adding a solvent in which nateglinide is difficultly soluble.Type: ApplicationFiled: June 16, 2009Publication date: October 8, 2009Applicant: Ajinomoto Co., Inc.Inventors: Yoshihito KOGUCHI, Tomoko Nakao, Michito Sumikawa
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Publication number: 20090252676Abstract: The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.Type: ApplicationFiled: January 8, 2009Publication date: October 8, 2009Applicant: Lantheus Medical Imaging, IncInventors: Richard R. Cesati, Thomas D. Harris, Simon P. Robinson, Richard J. Looby, Edward H. Cheesman, Padmaja Yalamanchili, David S. Casebier
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Patent number: 7569723Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are useful as reverse transcriptase inhibitors against HIV. In particular, the compounds are active against wild type and single or double mutant strains of HIV.Type: GrantFiled: January 15, 2008Date of Patent: August 4, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Bruno Simoneau, Jeffrey O'Meara, Christiane Yoakim
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Patent number: 7553873Abstract: The present invention relates to modulators of metalloproteinase activity.Type: GrantFiled: July 11, 2006Date of Patent: June 30, 2009Assignee: WyethInventors: Phaik-Eng Sum, Jerauld Stanley Skotnicki, Steve Yik-Kai Tam, Tarek Suhayl Mansour, David Brian How, Joshua James Sabatini, Jason Shaoyun Xiang, Eric Feyfant
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Patent number: 7544834Abstract: A method for producing B-type crystals of nateglinide substantially free of H-type crystals is provided, which comprises drying solvated wet crystals of nateglinide at a low temperature until no solvent remains and making a crystal conversion thereof. According to this method, B-type crystals of nateglinide can be produced at an industrial scale without allowing other forms of the crystalline polymorphism to coexist.Type: GrantFiled: June 4, 2007Date of Patent: June 9, 2009Assignee: Ajinomoto Co., Inc.Inventors: Michito Sumikawa, Makoto Maruo, Kazuo Miyazaki, Shigehiro Nishina, Yukiko Matsuzawa
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Publication number: 20090143469Abstract: The present invention relates to salts of organic acid, in particular salt of nateglinide, combined preparations comprising one or more salts of nateglinide and, optionally, one or more additional ingredients and the use thereof in pharmaceutical compositions for preventing or treating diabetes, cardiovascular disease, or conditions associated therewith.Type: ApplicationFiled: February 6, 2009Publication date: June 4, 2009Inventors: Paul Allen Sutton, Richard V. Vivilecchia, David John Parker, Marilyn De La Cruz
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Patent number: 7541485Abstract: The present invention relates to novel methods for the preparation of glutamic acid derivatives and intermediates thereof, and such compounds prepared by the novel methods.Type: GrantFiled: July 11, 2006Date of Patent: June 2, 2009Assignee: WyethInventors: Ronald S. Michalak, Joseph Zeldis, Mel Jennings, David M. Blum, Timothy Doyle
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Publication number: 20090131384Abstract: The invention provides novel compounds, methods for treating or preventing a condition related to ER-stress, e.g. hypercholesterolemia, atherosclerosis and related conditions, and pharmaceutical compositions related thereto.Type: ApplicationFiled: March 22, 2007Publication date: May 21, 2009Applicant: SYNDEXA PHARMACEUTICALS CORPORATIONInventors: Teoman Uysal, Nicholas D.P. Cosford
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Publication number: 20090131441Abstract: Metabolites of 2-(R)-4-isobutylarylpropionamides and pharmaceutical compositions containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: ApplicationFiled: January 24, 2006Publication date: May 21, 2009Applicant: DOMPE phar.r.ma S.p.A.Inventors: Riccardo Bertini, Cinzia Bizzarri, Marco Mosca, Marcello Allegretti, Francesco Colotta
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Patent number: 7534913Abstract: Provided are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, O, P, Q, T, U, V, Y, ?, ?, ?, ?, ?, ?, ? and ?, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.Type: GrantFiled: December 24, 2003Date of Patent: May 19, 2009Assignee: Teva Pharmaceutica Industries Ltd.Inventors: Gustavo Frenkel, Boaz Gome, Shlomit Wizel
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Patent number: 7534914Abstract: This invention provides a compound of the formula (I): wherein X represents a carbon atom or the like: Y represents imino, or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or the like: R2 and R3 independently represents a hydrogen atom or the like. These compounds are useful for the treatment of disease conditions mediated by prostaglandin such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.Type: GrantFiled: April 29, 2005Date of Patent: May 19, 2009Assignee: ReQualia Pharma Inc.Inventors: Hiroki Koike, Kana Kon-i, Yukari Matsumoto, Kazunari Nakao, Yoshiyuki Okumura, Tatsuya Yamagishi
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Publication number: 20090124669Abstract: Novel compounds for the prevention and treatment of dermatological disorders with an immunoallergic, hyperproliferative and inflammatory component, and a method of producing such compounds. The compounds are bioisosteres of substances with avenanthramide structures.Type: ApplicationFiled: February 21, 2006Publication date: May 14, 2009Inventor: Carlo Ghisalberti
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Publication number: 20090111874Abstract: The present invention relates to novel phenyl-N-acyl derivatives of biogenic amines and amino acids of general formula (I) as cyclooxynease inhibitors, possessing analgetic and anti-inflammatory properties and devoid of side effects in particular ulcerogeneity and pro-spasmodic actions, as well as capability to potentiate effect of other analgetics, and possessing in addition antihypoxic, antidepressant and anti-Parkinsonistic action; as well as to the processes for the preparation novel and known phenyl-N-acyl derivatives of biogenic amines, to a pharmaceutical composition and to an agent comprising compounds of general formula (I) as well as to use thereof and a method of treating.Type: ApplicationFiled: March 24, 2006Publication date: April 30, 2009Applicant: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU PHARMENTERPRISESInventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina, Violetta Leonidovna Kovaleva
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Patent number: 7517896Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.Type: GrantFiled: August 8, 2005Date of Patent: April 14, 2009Assignee: Bayer AktiengesellschaftInventors: Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
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Publication number: 20090076301Abstract: There is provided methods for producing nateglinide crystals, which comprises the steps of adding an acid(s) to a reaction mixture containing nateglinide to make it acidic, the reaction mixture being obtained by reacting trans-4-isopropylcyclohexylcarbonyl chloride with D-phenylalanine in a mixed solvent of ketone solvent and water in the presence of an alkali; and then adjusting the temperature of the mixture to 58° C. to 72° C. and the concentration of ketone solvent to more than 8 wt % and less than 22 wt % to conduct precipitation of nateglinide crystals. This producing method is the industrially beneficial methods for crystallization of nateglinide.Type: ApplicationFiled: October 31, 2008Publication date: March 19, 2009Applicant: AJINOMOTO CO. INCInventors: Daisuke TAKAHASHI, Seiichi NISHI, Satoji TAKAHASHI
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Publication number: 20090069593Abstract: The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.Type: ApplicationFiled: October 28, 2008Publication date: March 12, 2009Inventors: Vinod Kumar Kansal, Brijnath P. Chaurasia, V. Govardhan Rao, Anand Prakash Tiwari
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Patent number: 7501538Abstract: This invention provides aryl and heteroaryl compounds of Formula (I) as described herein, and methods of their preparation. Also provided are pharmaceutical compositions made with the compounds of Formula (I) and methods for making such compositions. The compounds of Formula (I) may activate an erythropoietin receptor and thus, may be useful to induce red blood cell production. The compounds of Formula (I) and compositions including compounds of Formula (I) may be useful in a variety of applications including the management, treatment and/or control of diseases caused at least in part by deficient (or inefficient) EPO production relative to hemoglobin level.Type: GrantFiled: August 6, 2004Date of Patent: March 10, 2009Assignee: TransTech Pharma, Inc.Inventors: Adnan M. M. Mjalli, Guoxiang Huang, Murty N. Arimilli, Thomas Scott Yokum, Jeff Jiqun Zhu, Muralidhar Bondlela