Halogen Patents (Class 562/449)
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Publication number: 20150148559Abstract: The invention provides new processes for making and purifying amino acid compounds, which are useful in the preparation of AKT inhibitors used in the treatment of diseases such as cancer, including the compound (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.Type: ApplicationFiled: May 17, 2013Publication date: May 28, 2015Applicant: Genentech, Inc.Inventor: Travis Remarchuk
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Publication number: 20150148533Abstract: The present invention relates to a process for preparing ?-aminobutyryl substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-?]pyrazin-7-yl compounds.Type: ApplicationFiled: June 13, 2013Publication date: May 28, 2015Applicant: Lek Pharmaceuticals d.d.Inventors: Stefan Starcevic, Peter Mrak, Gregor Kopitar
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Publication number: 20150011773Abstract: This invention relates to novel compounds suitable for labeling by 18F and to the corresponding 18F labeled compounds themselves, 19F-fluorinated analogues thereof and their use as reference standards, methods of preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by Positron Emission Tomography (PET).Type: ApplicationFiled: April 30, 2012Publication date: January 8, 2015Applicant: PIRAMAL IMAGING SAInventors: Mathias Berndt, Andre Muller, Heribert Schmitt-Willich, Timo Stellfeld, Georg Kettschau, Thomas Brumby, Keith Graham, Lutz Lehmann, Jorma Hassfeld, Martin Kruger
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Publication number: 20140296527Abstract: The present invention relates to processes for the enantio-selective preparation of spyrrolidine derivatives useful in the manufacture of pesticidally active compounds, as well as to intermediates in the processes. The processes include those comprising (a-i) reacting a compound of formula Ia wherein P is alkyl, aryl or heteroaryl, each optionally substituted, wherein the heteroaryl is connected at P via a ring carbon atom; R1 is chlorodifluoromethyl or trifluoromethyl; R2 is aryl or heteroaryl, each optionally substituted; with a source of cyanide in the presence a chiral catalyst to give a compound of formula IIa wherein P, R1 and R2 are as defined for the compound of formula Ia; and (a-ii) oxidising the compound of formula IIa with a peroxy acid, or peroxide in the presence of an acid to give a compound of formula VI wherein R1 and R2 are as defined for the compound of formula Ia.Type: ApplicationFiled: September 28, 2012Publication date: October 2, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Tomas Smejkal, Helmars Smits, Sebastian Volker Wendeborn, Guillaume Berthon, Jerome Yves Cassayre, Myriem El Qacemi
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Publication number: 20140275539Abstract: Provided herein are stabilized radioiodinated and astatinated compounds, and to methods for their preparation.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Ground Fluor Pharmaceuticals, Inc.Inventor: Stephen G. DiMagno
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Patent number: 8816001Abstract: This invention pertains to methods for producing homogeneous recombinant proteins that contain polymer initiators at defined sites. The unnatural amino acid, 4-(2?-bromoisobutyramido)phenylalanine of formula 1, was designed and synthesized as a molecule comprising a functional group further comprising an initiator for an atom-transfer radical polymerization (‘ATRP”) that additionally would provide a stable linkage between the protein and growing polymer. We evolved a Methanococcus jannaschii (Mj) tyrosyl-tRNA synthetase/tRNACUA pair to genetically encode this unnatural amino acid in response to an amber codon. To demonstrate the utility of this functional amino acid, we produced Green Fluorescent Protein with the unnatural amino acid initiator of formula 1 site-specifically incorporated on its surface (GFP-1).Type: GrantFiled: March 7, 2013Date of Patent: August 26, 2014Assignee: Franklin and Marshall CollegeInventors: Ryan A. Mehl, Krzysztof Matyjaszewski, Saadyah Averick
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Patent number: 8796485Abstract: By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More specifically, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise a glutamic acid derivative having CaSR agonistic activity or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 4, 2011Date of Patent: August 5, 2014Assignee: Ajinomoto Co., Inc.Inventors: Masayuki Sugiki, Toru Okamatsu, Sayaka Asari, Yayoi Kawato, Toshihiro Hatanaka, Tetsuo Yano, Yukie Seki, Naohiro Miyamura, Hiroaki Nagasaki, Yuzuru Eto, Reiko Yasuda
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Publication number: 20140100357Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one aromatic amine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one alkylated amine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.Type: ApplicationFiled: August 23, 2013Publication date: April 10, 2014Applicant: Ambrx, Inc.Inventors: Zhenwei Miao, Junjie Liu, Thea Norman
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Patent number: 8673974Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, X, X1, s and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.Type: GrantFiled: November 11, 2011Date of Patent: March 18, 2014Assignee: Novartis AGInventors: Gary Mark Coppola, Rajeshri Ganesh Karki, Toshio Kawanami
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Patent number: 8669395Abstract: Provided is a new crystal A of optically active 4-amino-3-(4-chlorophenyl)butanoic acid which is far better in stability, and a process for producing the crystal and a process for producing the crystal A comprising a step of heating the following crystal B in water having a pH of 3 to 9: crystal A: a crystal of optically active 4-amino-3-(4-chlorophenyl)butanoic acid which has diffraction peaks within the range of a diffraction angle 2? of 8.7 to 9.4°, within that of 2? of 12.2 to 12.8°, and within that of 2? of 24.8 to 25.4° in a powder X-ray diffraction measurement of the crystal by use of the Cu—K? wavelength; and crystal B: a crystal of optically active 4-amino-3-(4-chlorophenyl)butanoic acid which has diffraction peaks within the range of a diffraction angle 2? of 20.8 to 21.4°, within that of 2? of 26.7 to 27.3°, and within that of 2? of 29.7 to 30.3° in a powder X-ray diffraction measurement of the crystal by use of the Cu—K? wavelength.Type: GrantFiled: December 13, 2010Date of Patent: March 11, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: Takashi Miki, Masahiro Takeda, Tetsuro Yamazaki
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Publication number: 20130261259Abstract: This invention pertains to methods for producing homogeneous recombinant proteins that contain polymer initiators at defined sites. The unnatural amino acid, 4-(2?-bromoisobutyramido)phenylalanine of formula 1, was designed and synthesized as a molecule comprising a functional group further comprising an initiator for an atom-transfer radical polymerization (‘ATRP”) that additionally would provide a stable linkage between the protein and growing polymer. We evolved a Methanococcus jannaschii (Mj) tyrosyl-tRNA synthetase/tRNACUA pair to genetically encode this unnatural amino acid in response to an amber codon. To demonstrate the utility of this functional amino acid, we produced Green Fluorescent Protein with the unnatural amino acid initiator of formula 1 site-specifically incorporated on its surface (GFP-1).Type: ApplicationFiled: March 7, 2013Publication date: October 3, 2013Applicant: FRANKLIN AND MARSHALL COLLEGEInventors: Ryan A. Mehl, Krzysztof Matyjaszewski, Saadyah Averick
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Patent number: 8524936Abstract: The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I used as oral anti-diabetic drug. Starting from L-aspartic acid derivate of formula IV the invention describes preparation of the chiral (R)-?-amino acid of formula II known as a precursor in the synthesis of Sitagliptin (formula I).Type: GrantFiled: May 18, 2011Date of Patent: September 3, 2013Inventor: Milan Soukup
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Publication number: 20130203830Abstract: The invention is related to compounds for prevention of cell injury or protection of cells. The compounds are involved in the maintenance or the increase of hydrogen sulphide in cells, which results in a protection of the cells or the prevention of cell injury. The compounds of the invention can be used in cell culture and tissue culture techniques. They can also be used in several medical conditions such as ischemia, reperfusion and hypothermia, or for preserving organs which are used for transplantation.Type: ApplicationFiled: April 18, 2011Publication date: August 8, 2013Applicant: SULFATEQ B.V.Inventors: Fatemeh Talaei, Robert Henk Henning, Adrianus C. Van der Graaf
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Patent number: 8471016Abstract: The present invention provides a process for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof, having the R-configuration, of formula (IA), or S-configuration of formula (IB), selectively over the other enantiomer.Type: GrantFiled: April 28, 2011Date of Patent: June 25, 2013Assignee: Sun Pharmaceutical Industries Ltd.Inventors: Kanaksinh Jesingbhai Jadav, Rutvij Manharlal Bhatt, Kamleshkumar Naranbhai Borkhataria, Trinadha Rao Chitturi, Rajamannar Thennati
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Publication number: 20130150331Abstract: The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: February 5, 2013Publication date: June 13, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130123496Abstract: The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: ApplicationFiled: November 5, 2012Publication date: May 16, 2013Applicant: ALLERGAN, INC.Inventor: Allergan, Inc.
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Patent number: 8431735Abstract: A four stage inexpensive method of preparing pharmaceutical grade Melphalans of Melphalan 2-HCl, Melphalan HCl and Melphalan by: reacting N-phthaloyl-4-[bis(2-hydroxyethyl)amino]-phenylalanine ethyl ester with phosphorous oxychloride, reacting the chlorinated product with HCl and alkali hydroxide and purifying, and lyophilizing to obtain Melphalans.Type: GrantFiled: February 23, 2009Date of Patent: April 30, 2013Assignee: ChemPacific CorporationInventor: Chen Zhou
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Publication number: 20130102570Abstract: A medicament having an excellent CaSR agonist action which enables the prevention or treatment of diabetes or obesity is provided by a composition comprising the compound represented by general formula (I) as defined, or a salt thereof.Type: ApplicationFiled: September 28, 2012Publication date: April 25, 2013Applicant: AJINOMOTO CO., INC.Inventor: AJINOMOTO CO., INC
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Publication number: 20130041150Abstract: The present invention provides a process for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof, having the R-configuration, of formula (IA), or S-configuration of formula (IB), selectively over the other enantiomer.Type: ApplicationFiled: April 28, 2011Publication date: February 14, 2013Applicant: SUN PHARMACEUTICAL INDUSTRIES LTDInventors: Kanaksinh Jesingbhai Jadav, Rutvij Manharlal Bhatt, Kamleshkumar Naranbhai Borkhataria, Trinadha Rao Chitturi, Rajamannar Thennati
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Publication number: 20120302641Abstract: The present invention is directed to biphenyl derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.Type: ApplicationFiled: May 23, 2012Publication date: November 29, 2012Inventors: Devraj Chakravarty, Michael Greco, Brian Shook, Guozhang Xu, Rui Zhang
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Patent number: 8273794Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: May 16, 2005Date of Patent: September 25, 2012Assignee: Emisphere Technologies, Inc.Inventors: Maria Isabel Gomez-Orellana, David Gschneidner, Andrea Leone-Bay, Destardi Moye-Sherman, Stephen V. Pusztay, Parshuram Rath, Pingwah Tang, John J. Weidner, Jianfeng Song
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Publication number: 20120214997Abstract: Disclosed are a novel, simple and low-cost method for preparing sitagliptin, as DPP-IV (dipeptidyl peptidase IV) inhibitor, which is useful in treating type 2 diabetes mellitus and key intermediates used in said preparation of sitagliptin.Type: ApplicationFiled: October 19, 2010Publication date: August 23, 2012Applicant: HANMI HOLDINGS CO., LTD.Inventors: Nam Du Kim, Ji Yeon Chang, Dong Jun Kim, Hyun Seung Lee, Jae Hyuk Jung, Young Kil Chang, Gwan Sun Lee
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Publication number: 20120190887Abstract: A four stage inexpensive method of preparing pharmaceutical grade Melphalans of Melphalan 2-HCl, Melphalan HCl and Melphalan by: reacting N- phthaloyl-4-[bis(2-hydroxyethyl)amino]-phenylalanine ethyl ester with phosphorous oxychloride, reacting the chlorinated product with HCl and alkali hydroxide and purifying, and lyophilizing to obtain Melphalans.Type: ApplicationFiled: February 23, 2009Publication date: July 26, 2012Inventor: Chen Zhou
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Publication number: 20120172392Abstract: Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.Type: ApplicationFiled: March 7, 2012Publication date: July 5, 2012Inventors: LUISA M. SALTER-CID, ERIC Y. WANG, MARY T. MACDONALD, JINGJING ZHAO
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Publication number: 20120123144Abstract: The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I used as oral anti-diabetic drug. Starting from L-aspartic acid derivate of formula IV the invention describes preparation of the chiral (R)-?-amino acid of formula II known as a precursor in the synthesis of Sitagliptin (formula I).Type: ApplicationFiled: May 18, 2011Publication date: May 17, 2012Applicant: Drug Process Licensing Associates, LLCInventor: Milan Soukup
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Publication number: 20120122977Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, X, X1, s and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: NOVARTIS AGInventors: Gary Mark COPPOLA, Rajeshri Ganesh KARKI, Toshio KAWANAMI
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Publication number: 20120029230Abstract: The present invention provides a novel method for preparing chiral Baclofen with higher yield, higher e.e. value, and lower cost via chiral Michael addition.Type: ApplicationFiled: July 27, 2010Publication date: February 2, 2012Inventors: Jen-Huang Kuo, Wei-chyun Wong
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Publication number: 20120016125Abstract: The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used in mass production by improving yield.Type: ApplicationFiled: March 30, 2010Publication date: January 19, 2012Applicant: DONG-A PHARMACEUTICAL. CO., LTDInventors: Woo Young Kwak, Heung Jae Kim, Jong Pil Min, Tae Hyun Yoon, Moohi Yoo, Geun Gho Lim, Sun Ki Chang
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Publication number: 20120010401Abstract: An industrially advantageous method for producing a 1,5-benzodiazepine compound is provided. A compound (5) is obtained according to the reaction scheme shown below, and this compound is used as an intermediate.Type: ApplicationFiled: March 29, 2010Publication date: January 12, 2012Applicant: Zeria Pharmaceutical Co., Ltd.Inventor: Masaru Terauchi
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Publication number: 20110251418Abstract: By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More specifically, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise a glutamic acid derivative having CaSR agonistic activity or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 4, 2011Publication date: October 13, 2011Applicant: AJINOMOTO CO., INC.Inventors: Masayuki Sugiki, Toru Okamatsu, Sayaka Asari, Yayoi Kawato, Toshihiro Hatanaka, Tetsuo Yano, Yukie Seki, Naohiro Miyamura, Hiroaki Nagasaki, Yuzuru Eto, Reiko Yasuda
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Publication number: 20110213157Abstract: A compound represented by the following general formula (I): [wherein R1 represents hydrogen atom or a C1-6 alkyl group, A and B represent —(CH2)2—, —(CH2)3— or —(CH2)4—, X represents —N(R2)—CO— (R2 represents hydrogen atom or a C1-6 alkyl group), —CO—N(R3)— (R3 represents hydrogen atom or a C1-6 alkyl group), —C(R4)?C(R5)— (R4 and R5 represent hydrogen atom or a C1-6 alkyl group), or —N(R6)—SO2— (R6 represents hydrogen atom or a C1-6 alkyl group), and Ar represents an aryldiyl group or a heteroaryldiyl group], which has a retinoid action and is useful as an active ingredient of a medicament.Type: ApplicationFiled: August 14, 2008Publication date: September 1, 2011Applicant: RESEARCH FOUNDATION ITSUU LABORATORYInventors: Yohei Amano, Masayuki Noguchi, Koichi Shudo
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Publication number: 20110190258Abstract: The present invention relates to substituted aryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: January 28, 2011Publication date: August 4, 2011Applicant: NOVARTIS AGInventors: Daniela ANGST, Birgit BOLLBUCK, Philipp JANSER, Jean QUANCARD, Nikolaus Johannes STIEFL
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Publication number: 20110178087Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.Type: ApplicationFiled: March 30, 2011Publication date: July 21, 2011Applicant: Compass Pharmaceuticals LLC.Inventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
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Publication number: 20110152572Abstract: Provided is a new crystal A of optically active 4-amino-3-(4-chlorophenyl)butanoic acid which is far better in stability, and a process for producing the crystal and a process for producing the crystal A comprising a step of heating the following crystal B in water having a pH of 3 to 9: crystal A: a crystal of optically active 4-amino-3-(4-chlorophenyl)butanoic acid which has diffraction peaks within the range of a diffraction angle 2? of 8.7 to 9.4°, within that of 2? of 12.2 to 12.8°, and within that of 2? of 24.8 to 25.4° in a powder X-ray diffraction measurement of the crystal by use of the Cu—K? wavelength; and crystal B: a crystal of optically active 4-amino-3-(4-chlorophenyl)butanoic acid which has diffraction peaks within the range of a diffraction angle 2? of 20.8 to 21.4°, within that of 2? of 26.7 to 27.3°, and within that of 2? of 29.7 to 30.3° in a powder X-ray diffraction measurement of the crystal by use of the Cu—K? wavelength.Type: ApplicationFiled: December 13, 2010Publication date: June 23, 2011Inventors: Takashi Miki, Masahiro Takeda, Tetsuro Yamazaki
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Publication number: 20110118353Abstract: The present invention relates to a glycine transporter-1 inhibitor having the formula (I) wherein X is 1-3 substituents selected from H, halogen, methyl, methoxy, trifluoromethyl and trifluoromethoxy and Y is 1-3 substituents selected from H, methyl and halogen or a pharmaceutically acceptable salt thereof for use in a treatment in humans to suppress the level of one or more hormone selected from luteinizing hormone, follicle-stimulating hormone, estradiol and testosterone. The present invention further relates to such a glycine transporter-1 inhibitor as part of a contraceptive regimen or as a treatment for hypersexuality.Type: ApplicationFiled: November 4, 2008Publication date: May 19, 2011Inventors: Robert Gerard Jules Marie Hanssen, Jacques Schipper, Josephus Hubertus Schoemaker
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Publication number: 20110087049Abstract: A method of producing a purified optically active 4-amino-3-(substituted phenyl)butanoic acid compound which is characterized by comprising a step of making a crude optically active 4-amino-3-(substituted phenyl)butanoic acid compound contact an organic acid in the presence of water.Type: ApplicationFiled: September 22, 2008Publication date: April 14, 2011Inventors: Kazuo Murakami, Masahiro Takeda, Hirofumi Kato
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Publication number: 20100240919Abstract: The invention provides a method for obtaining the intermediate (II), useful for manufacturing Valsartan and a drug directed to a treatment of arterial hypertension or heart failure. The process comprises a) Imination of the aldehyde group of a compound (VII) by L-Valine (IV) salts with organic or inorganic bases and a polar solvent or water, where X means halogen or an —OSO2R group, where R is CF3, tolyl, methyl or F; to give an imine-type compound (VIII), where B+ is the protonated form of an organic base or an alkaline cation; b) Reduction of the imine group of the compound (VIII) followed by acidification, to give the compound (VI); and c) N-Acylation of the compound (VI) with valeryl chloride to give the compound (II). Steps a) and b) can be performed in a “one pot” reaction.Type: ApplicationFiled: October 19, 2006Publication date: September 23, 2010Applicant: Inke, S.A.Inventors: Pere Dalmases Barjoan, Joan Huguet Clotet
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Publication number: 20100197789Abstract: Disclosed is a novel anti-obesity agent. Also disclosed is a therapeutic method using the anti-obesity agent. The anti-obesity agent comprises a GABAB receptor agonist or a pharmacologically acceptable salt thereof as an active ingredient.Type: ApplicationFiled: July 19, 2007Publication date: August 5, 2010Applicant: National University Corporation Nagoya UniversityInventors: Hiroshi Arima, Ikuko Sato, Yutaka Oiso
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Publication number: 20100197924Abstract: The present invention relates to synthetic processes for preparation of aminotetralin compounds with kinase inhibitory activity. The invention also provides synthetic intermediates useful in the processes of the invention.Type: ApplicationFiled: December 16, 2009Publication date: August 5, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Alexandra E. Gould, Sean J. Harrison, Hirotake Mizutani, Ming Shen, Thomas E. Smyser, Stephen G. Stroud
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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: 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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Publication number: 20090325962Abstract: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.Type: ApplicationFiled: August 21, 2009Publication date: December 31, 2009Applicant: Genentech, Inc.Inventors: David Y. Jackson, Frederick C. Sailes, Daniel P. Sutherlin
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Publication number: 20080280982Abstract: 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: November 14, 2006Publication date: November 13, 2008Inventors: Jianke Li, Guoxin Zhu
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Publication number: 20080221210Abstract: The invention provides compounds of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition mediated by a thyroid receptor. Formula (I), wherein R1, R2, n, Y, Y?, R3, R4, W and R5 are as defined in the specification.Type: ApplicationFiled: March 22, 2005Publication date: September 11, 2008Applicant: Karo Bio ABInventors: Ana Maria Garcia Collazo, Thomas Anders Wilson Norin, Neerai Garg, Anton Joakim Lofstedt, Tomas Fredrik Hansson, Lars Jesper Hallberg, Peter Brandt
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Publication number: 20080114175Abstract: The present invention is directed to a process for preparing certain cysteine protease inhibitors.Type: ApplicationFiled: September 16, 2005Publication date: May 15, 2008Inventor: Jiayao Li
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Patent number: 6989402Abstract: New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR?R?) or an acylsulphonamide (CONHSO2R?) derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, R4 may be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR?R?). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5=H).Type: GrantFiled: December 23, 1999Date of Patent: January 24, 2006Assignee: Karo Bio ABInventors: Jon Hangeland, Minsheng Zhang, Yolanda Caringal, Denis Ryono, Yi-Lin Li, Johan Malm, Ye Liu, Neeraj Garg, Chris Litten, Ana Maria Garcia Collazo, Konrad Koehler
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Patent number: 6849648Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, or a tautomer thereof, wherein G1, G2, and B are as defined in the application, are selective inhibitors of MMP-13. The compounds are useful for treating diseases mediated by MMP-13, including cancer and arthritis.Type: GrantFiled: October 4, 2002Date of Patent: February 1, 2005Assignee: Warner-Lambert CompanyInventors: Amy Mae Bunker, William Glen Harter, James Lester Hicks, Patrick Michael O'Brien, Ly Pham, Joseph Armand Picard, William Howard Roark
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Patent number: 6806365Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: April 5, 2002Date of Patent: October 19, 2004Assignee: Hoffmann-La Rocher Inc.Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achytharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Patent number: 6803384Abstract: A compound of formula Id and pharmaceutically acceptable salts and esters thereof, wherein the substituent designations are as provided in the specification. Compounds of the invention are useful for treating reperfusion injury.Type: GrantFiled: January 22, 2003Date of Patent: October 12, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
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Patent number: 6720306Abstract: A compound of Formula I, providing tetrapartate prodrugs is provided wherein: L1 is a bifunctional linking moiety; D is a moiety that is a leaving group, or a residue of a compound to be delivered into a cell; Z is covalently linked to [D]y, wherein Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof, Y1, Y2, Y3 and Y4 are each independently O, S, or NR12; R11 is a mono- or divalent polymer residue; R1, R4, R9, R10 and R12 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls and substituted C1-6 heteroalkyls; R2, R3, R5 and R6 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C1-6 alkoxy, phenoxy, C1-8 heteroalkyls, C1-8 heteroalkoxy, substituted C1-6 alkyls, C3-8 cycloalkyls, CType: GrantFiled: January 12, 2001Date of Patent: April 13, 2004Assignee: Enzon Pharmaceuticals, Inc.Inventors: Richard B. Greenwald, Hong Zhao