Oxy In Acid Moiety Patents (Class 560/39)
-
Publication number: 20090069579Abstract: A process for preparing intermediate compounds useful in the preparation of statins. The process is particularly useful for the preparation of atorvastatin. The process involves the reduction of two ketone groups at the same time using either a chiral transition metal catalyst or an enzyme based system.Type: ApplicationFiled: November 21, 2006Publication date: March 12, 2009Inventors: John Blacker, Robin Fieldhouse
-
Publication number: 20090042772Abstract: Novel compounds, compositions comprising compounds, and methods for methods for preparing and using compounds are described herein. Methods of treating or ameliorating various conditions, including insulin resistance, pancreatic beta cell apoptosis, obesity, pro-thrombotic conditions, myocardial infarction, hypertension, dyslipidemia, manifestations of Syndrome X, congestive heart failure, inflammatory disease of the cardiovascular system, atherosclerosis, sepsis, type 1 diabetes, liver damage, and cachexia, by administering compounds described herein. Compounds presented herein may be used to modulate serine palmitoyl transferase activity.Type: ApplicationFiled: October 13, 2008Publication date: February 12, 2009Applicant: Transition Therapeutics Inc.Inventor: John Nestor
-
Patent number: 7456217Abstract: 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: July 13, 2005Date of Patent: November 25, 2008Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Takayuki Kawaguchi, Sumihiro Nomura, Mikiko Tsukimoto, Toshiyuki Kume, Ila Sircar
-
Publication number: 20080287649Abstract: Methods for the synthesis of cyclic peptides are provided, as well as novel dipeptide compounds. The methods include the solid phase synthesis of a dipeptide, which is the coupled to a second peptide in a solid phase reaction. The peptide is then cyclized following the coupling reaction. The methods and dipeptides are particularly useful for the synthesis of MC-4 receptor agonist peptides.Type: ApplicationFiled: December 20, 2007Publication date: November 20, 2008Inventors: Lin Chen, Yeun-Kwei Han, Christopher R. Roberts
-
Patent number: 7442796Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyper-lipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed.Type: GrantFiled: April 20, 2004Date of Patent: October 28, 2008Assignee: Wellstat Therapeutics CorporationInventors: Shalini Sharma, Reid W. von Borstel
-
Patent number: 7439383Abstract: The present invention is directed to novel phenytoin derivative compounds and the use of such compounds as sodium channel blockers. Such compositions have utility as anti-cancer agents and can be used to limit or prevent PCa growth and/or metastasis.Type: GrantFiled: April 18, 2003Date of Patent: October 21, 2008Assignee: University of Virginia Patent FoundationInventor: Milton L. Brown
-
Patent number: 7399884Abstract: Histone deacetylase inhibitors and uses thereof are provided that have the general formula wherein R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted straight chained C1-12 alkyl, C2-12 aminoalkyl or C2-12 oxaalkyl, and a substituted and unsubstituted 3, 4, 5, 6, 7 or 8 membered ring, with the proviso that R3 and R4 are not both hydrogen; R5 is selected from the group consisting of a carbonyl, a substituted or unsubstituted C1-3 alkyl, a substituted or unsubstituted —C1-3 alkyl-C(O), a substituted or unsubstituted —C(O)—C1-3 alkyl, and a substituted or unsubstituted —C(O)C(O)C1-3 alkyl; M is a substituent capable of complexing with a protein metal ion; and L is a substituent comprising a chain of 3-12 atoms connecting the M substituent to the carbon atom alpha to the L substituent.Type: GrantFiled: November 7, 2006Date of Patent: July 15, 2008Assignee: Takeda San Diego, Inc.Inventors: Jerome C. Bressi, Sheldon X. Cao, Jeffrey A. Stafford, Phong H. Vu
-
Publication number: 20080139825Abstract: There is provided a process for efficiently producing an anti form of an optically active ?-hydroxy-?-aminocarboxylic acid derivative that is useful as an intermediate for pharmaceuticals and agrochemicals. The process for producing optically active ?-hydroxy-?-aminocarboxylic acid derivative of formula (2) or (3) therein R1 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, R2 is substituted or unsubstituted C1-20, alkyl group, or substituted or unsubstituted C4-12 aromatic group, comprising subjecting an ?-aminoacyl acetic acid ester compound of formula (1) wherein R1 and R2 have the same meaning as the above, to hydrogenation by catalytic asymmetric hydrogenation in the presence of an acid by using as a catalyst a rhodium complex containing as a ligand an optically active compound of formula (4), (4?) or (5) characterized in that the hydrogenation is conducted in the presence of an acetic acid salt.Type: ApplicationFiled: January 12, 2006Publication date: June 12, 2008Applicant: Nissan Chemical Industrial, Ltd.Inventors: Yasumasa Hamada, Kazuishi Makino
-
Patent number: 7375245Abstract: The present invention provides a compound of the following formula (I): wherein R1 is methyl or 4-aminobutyl, which may be acylated; X is phenyl or substituted phenyl; W is an esterified group removable by hydrogenolysis. Also disclosed is the preparation method and the application of formula (I) compound.Type: GrantFiled: July 7, 2004Date of Patent: May 20, 2008Assignee: Everlight USA, Inc.Inventors: Yu-Liang Liu, Rung-Tian Suen, Ying-Chi Chiu
-
Publication number: 20080057127Abstract: The present invention relates to compound of formula I, which are functionalized, non-phenolic amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.Type: ApplicationFiled: August 29, 2007Publication date: March 6, 2008Applicant: BEZWADA BIOMEDICAL, LLCInventor: Rao S. Bezwada
-
Patent number: 7253299Abstract: A process for purifying N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine which comprises subjecting N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine contaminated with impurities to crystallization from a solvent comprising a water-soluble non-protic organic solvent, thereby removing the impurities into the mother liquor and giving crystals of N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine, according to which N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine having a high quality can be obtained in a high yield and a high productivity and which is suitable for practice on an industrial scale.Type: GrantFiled: July 10, 2002Date of Patent: August 7, 2007Assignee: Kaneka CorporationInventors: Yasuhiro Iida, Hajime Manabe, Yasuyoshi Ueda
-
Patent number: 7235672Abstract: A probe, kit comprising the probe, and methods for using the probe are provided where the probe comprises: wherein DM is a detectable marker; and L is a straight or branched chain moiety providing between 1 and 20 atom separation between DM and the ring atom to which DM is attached.Type: GrantFiled: March 11, 2004Date of Patent: June 26, 2007Assignee: Takeda San Diego, Inc.Inventors: Christopher L. Caster, Andrew J. Jennings, Marc E. Navre, Michael B. Wallace, Yiqin Wu
-
Patent number: 7230097Abstract: A process for preparation of 7-[D-?-amino-?-(4-hydroxyphenyl)acetamido]-3-(1-propen-1-yl)-3-cephem-4-carboxylic acid viz. Cefprozil of formula (I) in high purity, substantially free of impurities, which comprises preparation of mixed acid anhydride by selecting the sequence and temperature of addition of the reagents and its subsequent condensation with a protected 7-APCA; followed by hydrolysis, isolation and purification to give Cefprozil of formula (I) in the form of a monohydrate.Type: GrantFiled: March 15, 2004Date of Patent: June 12, 2007Assignee: Lupin Ltd.Inventors: Om Dutt Tyagi, Dnyandev Ragho Rane, Tushar Kumar Srivastava, Krishnarao Tukaram Sirsath
-
Patent number: 7223793Abstract: The present invention relates to phenolic acid derivatives of the formula I and compositions for the preventing and the treating blood lipid level-related diseases comprising the phenolic acid derivatives. The compounds have excellent effects of reducing blood lipid level, inhibiting cholesterol metabolism-related enzymes and preventing and treating blood lipid level-related diseases.Type: GrantFiled: December 4, 2002Date of Patent: May 29, 2007Assignee: Bionutrigen Co., Ltd.Inventors: Songhae Bok, Sangku Lee, Taesook Jeong, Euneai Kim, Surksik Moon, Myungsook Choi, Byunghwa Hyun, Chulho Lee, Yangkyu Choi, Gootaeg Oh
-
Patent number: 7211686Abstract: The invention includes selected novel optically active ?-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.Type: GrantFiled: January 12, 2005Date of Patent: May 1, 2007Assignee: Pharmacia CorporationInventor: John J. Talley
-
Patent number: 7169776Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention also relates to dicarboxylic salicylamide delivery agent compounds for the delivery of active agents. Methods of administration are provided as well.Type: GrantFiled: January 19, 2005Date of Patent: January 30, 2007Assignee: Emisphere Technologies, Inc.Inventors: Joseph N. Bernadino, Doris C. O'Toole, William E. Bay
-
Patent number: 7153869Abstract: This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.Type: GrantFiled: March 12, 2004Date of Patent: December 26, 2006Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
-
Patent number: 7154002Abstract: Histone deacetylase inhibitors and uses thereof are provided that have the general formula wherein R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted straight chained C1-12 alkyl, C2-12 aminoalkyl or C2-12 oxaalkyl, and a substituted and unsubstituted 3, 4, 5, 6, 7 or 8 membered ring, with the proviso that R3 and R4 are not both hydrogen; R5 is selected from the group consisting of a carbonyl, a substituted or unsubstituted C1-3 alkyl, a substituted or unsubstituted —C1-3 alkyl-C(O), a substituted or unsubstituted —C(O)—C1-3 alkyl, and a substituted or unsubstituted —C(O)C(O)C1-3 alkyl; M is a substituent capable of complexing with a protein metal ion; and L is a substituent comprising a chain of 3–12 atoms connecting the M substituent to the carbon atom alpha to the L substituent.Type: GrantFiled: October 7, 2003Date of Patent: December 26, 2006Assignee: Takeda San Diego, Inc.Inventors: Jerome C. Bressi, Sheldon X. Cao, Jeffrey A. Stafford, Phong H. Vu
-
Patent number: 7135586Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: GrantFiled: November 15, 2001Date of Patent: November 14, 2006Assignee: Janssen Pharmaceutica, NVInventors: Lieven Meerpoel, Leo Jacobs Jozef Backx
-
Patent number: 7081465Abstract: This invention relates to novel {overscore (?)}-substituted-naphthyloxy-amino alkanes, their preparation and use as antihyperglycemic agents and for the treatment and prevention of cardiovascular disorders (CVS) such as lipid lowering effects.Type: GrantFiled: October 27, 2003Date of Patent: July 25, 2006Assignee: Council of Scientific and Industrial ResearchInventors: Devdutt Chaturvedi, Atul Kumar, Reema Rastogi, Arivend Srivastava, Priti Tewari, Rehan Ahmad, Ramaesh Chander, Anju Puri, Geetika Bhatia, Farhar Rivizvi, Anil Kumar Rastogi, Suprabhat Ray
-
Patent number: 7045660Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.Type: GrantFiled: March 3, 2004Date of Patent: May 16, 2006Assignee: Aventis Pharma LimitedInventors: Garry Fenton, Tahir Nadeem Majid, Malcolm Norman Palfreyman
-
Patent number: 7034178Abstract: This invention is drawn to a process for the production of (R,R)-phenylisoserine or a 1–4C-alkyl ester thereof.Type: GrantFiled: June 27, 2002Date of Patent: April 25, 2006Assignee: Altana Pharma AGInventors: Wijnand Faber, Jan Koek, Jörg Senn-Bilfinger, Ton Vries
-
Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
-
Patent number: 7026501Abstract: 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: August 27, 2001Date of Patent: April 11, 2006Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takayuki Kawaguchi, Sumihiro Nomura, Mikiko Tsukimoto, Toshiyuki Kume
-
Patent number: 7022872Abstract: The invention relates to a method for preparing F-Dopa and 18F-Dopa and intermediates that are useful in the method. The invention is a method that synthesizes F-Dopa and 18F-Dopa in good yield with high enantiopurity without the need for further transformations. The method includes the step of reacting a benzaldehyde derivative with a phosphonic acid derivative to produces an olefin intermediate that can be asymmetrically hydrogenated to produce the desired enantiomer.Type: GrantFiled: December 19, 2003Date of Patent: April 4, 2006Assignee: Molecular Technologies, Inc.Inventors: Joseph C. Walsh, Henry C. Padgett
-
Patent number: 7012071Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.Type: GrantFiled: July 16, 2004Date of Patent: March 14, 2006Assignee: Wellstat Therapeutics CorporationInventors: Shalini Sharma, Reid W. von Borstel
-
Patent number: 6946491Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.Type: GrantFiled: October 14, 2003Date of Patent: September 20, 2005Assignee: Wellstat Therapeutics CorporationInventors: Shalini Sharma, Reid W. von Borstel
-
Patent number: 6936636Abstract: Compounds of the formula: where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of reducing serum thyroxine levels and transiently increasing triglyceride levels.Type: GrantFiled: June 26, 2003Date of Patent: August 30, 2005Assignee: Allergan, Inc.Inventors: Santosh Sinha, Kwok Yin Tsang, Smita Bhat, Roshantha A. Chandraratna
-
Patent number: 6936719Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.Type: GrantFiled: December 18, 2003Date of Patent: August 30, 2005Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, R. Scott Rowland, Pooran Chand, Pravin L. Kotian, Yahya El-Kattan, Shri Niwas
-
Patent number: 6930200Abstract: Mono-substituted and di-substituted alpha-amino acids and derivatives thereof, substituted at the alpha positon with one (mono-) or two (di-) substituents (R2 and/or R3) as shown in Formula 1: N(R4R5)C(R2R3)CO(OR1).Type: GrantFiled: June 26, 2003Date of Patent: August 16, 2005Assignee: Pharmacore, Inc.Inventor: Adnan M. M. Mjalli
-
Patent number: 6924314Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.Type: GrantFiled: October 14, 2003Date of Patent: August 2, 2005Assignee: Wellstat Therapeutics CorporationInventors: Shalini Sharma, Reid W. von Borstel
-
Patent number: 6900344Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention also relates to dicarboxylic salicylamide delivery agent compounds for the delivery of active agents. Methods of administration are provided as well.Type: GrantFiled: March 21, 2001Date of Patent: May 31, 2005Assignee: Emisphere Technologies, Inc.Inventors: Joseph N. Bernadino, Doris C. O'Toole, William E. Bay
-
Patent number: 6849649Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.Type: GrantFiled: October 28, 2003Date of Patent: February 1, 2005Assignee: Pfizer Inc.Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
-
Publication number: 20040267019Abstract: The present invention relates to a new and industrially advantageous one-pot process for the preparation of alkyl 3-cyclopropyl amino-2-[2,4-dibromo-3-(difluoromethoxy)benzoyl]-2-propenoates of in which R represents methyl or ethyl, which are valuable intermediates for the production of highly active antibacterial quinolone medicaments.Type: ApplicationFiled: January 6, 2003Publication date: December 30, 2004Inventors: Prosenjit Bose, Naresh Kumar, Taro Kiyoto
-
Patent number: 6835848Abstract: The present invention relates to a new and industrially advantageous one-pot process for the preparation of alkyl 3-cyclopropyl amino-2-[2,4-dibromo-3-(difluoromethoxy) benzoyl]-2-propenoates of in which R represents methyl or ethyl, which are valuable intermediates for the production of highly active antibacterial quinolone medicaments.Type: GrantFiled: January 6, 2003Date of Patent: December 28, 2004Assignees: Ranbaxy Laboratories Limited, Toyama Chemical Co., Ltd.Inventors: Prosenjit Bose, Naresh Kumar, Taro Kiyoto
-
Publication number: 20040249187Abstract: The invention relates to a method for producing chiral amino acid derivatives, characterised in that free carboxylic acid groups in an amino acid derivative are first converted into nitro ketones, and said nitro ketones are then converted into the corresponding nitro alcohols and amino alcohols by means of reduction. The invention also relates to the nitro ketones and nitro alcohols obtained as intermediate products.Type: ApplicationFiled: July 30, 2004Publication date: December 9, 2004Inventors: Joachim Rudolph, Frithjof Hannig
-
Publication number: 20040186312Abstract: The invention relates to compounds of formula (I); wherein R1 and R2 independently selected from C1-6 alkyl; P1, P2, P3, and P4 are each independently hydrogen or a protecting group; and their use in the preparation of 18F-labelled 6-L-fluorodopa.Type: ApplicationFiled: December 24, 2003Publication date: September 23, 2004Inventors: Sajinder Kaur Luthra, Frank Brady, Harry John Wadsworth
-
Patent number: 6790865Abstract: The present invention provides novel 2-methylpropionic acid derivatives represented by the general formula: (wherein R1 represents a hydrogen atom, a lower alkyl group or an aralkyl group; R2 represents a hydrogen atom, a lower alkyl group or a halogen atom; A represents an oxygen atom or an imino group; the carbon atom marked with (R) represents a carbon atom in R configuration; and the carbon atom marked with (S) represents a carbon atom in S configuration) and pharmaceutically acceptable salts thereof, which have excellent &bgr;3-adrenoceptor stimulating effects and are useful as agents for the prevention or treatment of obesity, hyperglycemia, the diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression, or the diseases caused by biliary calculi or hypermotility of the biliary tract.Type: GrantFiled: February 5, 2003Date of Patent: September 14, 2004Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Tetsuro Tamai, Nobuyuki Tanaka, Harunobu Mukaiyama, Akihito Hirabayashi, Hideyuki Muranaka, Masaaki Sato, Masuo Akahane
-
Publication number: 20040171865Abstract: The present invention relates to a method of preparing a phenoxy alkanoic, alkenoic, or alkynoic acid or a salt thereof from a phenoxy containing compound via a dicarboxylate intermediate. The phenoxy alkanoic, alkenoic, and alkynoic acids and salts thereof prepared by this method are suitable for use in composition for delivering active agents via oral or other routes of administration to animals. Furthermore, the present invention relates to phenoxy dicarboxylic acids and their salts for delivering active agents, such as biologically or chemically active agents, to a target.Type: ApplicationFiled: April 7, 2004Publication date: September 2, 2004Inventor: Joseph N. Bernadino
-
Publication number: 20040082794Abstract: The present invention is to provide a process for producing an optically active amino alcohol which is useful for the synthesis of natural substances and as an intermediate for drugs and agricultural chemicals in a high yield, a high selectivity and an economical manner with a good working efficiency and the present invention relates to a process for producing an optically active amino alcohol represented by the following formula (2) 1Type: ApplicationFiled: October 17, 2003Publication date: April 29, 2004Inventors: Tohru Yokozawa, Kenji Yagi, Takao Saito
-
Publication number: 20040072820Abstract: The instant invention provides novel substituted naphthyl compounds, intermediates, compositions, pharmaceutical formulations, and methods of use.Type: ApplicationFiled: May 27, 2003Publication date: April 15, 2004Inventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones, Alan David Palkowitz
-
Publication number: 20040043952Abstract: The present invention relates, inter alia, to pentaerythritol lipid derivatives that are useful for the intracellular delivery of nucleic acids. Such pentaerythritol lipid derivatives are useful for the preparation of transfection complexes (such as liposomes, lipoplexes, and other lipid vesicles) that can be used to deliver nucleic acids into mammalian cells.Type: ApplicationFiled: May 30, 2003Publication date: March 4, 2004Applicant: Genteric, Inc.Inventors: Edmund J. Niedzinski, Michael Bennett
-
Patent number: 6699463Abstract: Compounds of Formula I Each R is independently linear or branched C1 to C8 alkyl, or linear or branched C1 to C8 alkoxy or one R is H and the other R is linear or branched C1 to C8 alkyl, or linear or branched C1 to C8 alkoxy; R1 is selected from the group consisting of COCH3, CO2R3, CONH2, CONH(R4)2, CN, COX(CH2)n-N—(R2)(R4)(R3), and the quaternized salt form of the formula COX(CH2)n-N—(R2)(R4)(R3)+Y−; X is O or NH; n is an integer of 1 to 5; Y is an anion; and R2, R3 and R4 are independently linear or branched C1 to C20. Hair care formulations and other compounds containing compounds of Formula I, and methods for protecting hair and substrates such as polymers, textiles, fabrics, leathers and paints using the compounds herein.Type: GrantFiled: April 10, 2002Date of Patent: March 2, 2004Assignee: EM IndustriesInventor: Ratan K. Chaudhuri
-
Patent number: 6699994Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.Type: GrantFiled: April 23, 2002Date of Patent: March 2, 2004Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, R. Scott Rowland, Pooran Chand, Pravin L. Kotian, Yahya El-Kattan, Shri Niwas
-
Publication number: 20040006137Abstract: A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below is described.Type: ApplicationFiled: March 14, 2003Publication date: January 8, 2004Inventors: Robert E. Waltermire, Silvio Campagna, Scott A. Savage, Shailendra Bordawekar, Thomas P. Maduskuie, Sridhar Desikan, Stephen R. Anderson
-
Patent number: 6670496Abstract: The invention relates to a process for the preparation of compounds of formula (I) wherein: R1 is optionally substituted alkyl, R2 is C1-C6alkyl, C3-C6cycloalkyl, C3-C6cycloalkyl-C1-C2alkyl, aryl, aryl-C1-C2alkyl, heterocyclyl, heterocycly-C1-C2alkyl, which groups are optionally substituted by alkyl, alkoxy, or halogen; in which process (I) an aniline of formula (II), is diazotized with an organic or inorganic nitrite or nitrous acid; (2) the resulting diazonium salt is reacted with an oxime of formula (III) in presence of a copper(II)-salt.Type: GrantFiled: October 10, 2001Date of Patent: December 30, 2003Assignee: Bayer AktiengesellschaftInventor: Rudolf Waditschatka
-
Patent number: 6660756Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2 R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.Type: GrantFiled: March 12, 2002Date of Patent: December 9, 2003Assignee: Pfizer Inc.Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
-
Patent number: 6660872Abstract: The present invention relates to novel processes for preparing methoxyimino-acetamides.Type: GrantFiled: November 21, 2001Date of Patent: December 9, 2003Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Bernd Gallenkamp, Peter Gerdes, Ulrich Heinemann, Walter Hübsch, Bernd-Wieland Krüger, Fritz Maurer, Holger Weintritt
-
Patent number: 6649639Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.Type: GrantFiled: September 7, 2001Date of Patent: November 18, 2003Inventors: Peter S. Dragovich, Thomas J. Prins, Ru Zhou
-
Patent number: RE39088Abstract: An amide compound of the formula (I): ? wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-?, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.Type: GrantFiled: August 15, 1996Date of Patent: May 2, 2006Assignee: Japan Tobacco, Inc.Inventors: Junichi Haruta, Kazuhiko Sakuma, Yoshihiro Watanabe