Nitrogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/561)
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Publication number: 20110082109Abstract: The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na+/H+ exchanger type 3) and effectively improves diseases or conditions of organs in which NHE3 is expressed.Type: ApplicationFiled: October 1, 2010Publication date: April 7, 2011Applicant: AJINOMOTO CO., INC.Inventors: Wataru MIYANAGA, Yoichiro Shima, Misato Noguchi, Akiko Oonuki, Yayoi Kawato, Hiroshi Iwata, Eri Harada, Ryuta Takashita, Hirokazu Ueno, Tadakiyo Nakagawa
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Publication number: 20110081409Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.Type: ApplicationFiled: April 15, 2009Publication date: April 7, 2011Inventors: Erik Verner, Sriram Balasubramanian, Joseph J. Buggy
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Patent number: 7906551Abstract: This invention relates to 3-substituted-1,5-diaryl-2-alkyl-pyrroles of Formula I, pharmaceutical compositions containing them, and to their use for the pharmacological treatment of pain and COX-2 over-activation associated disorders. Compounds of this invention are new pyrrole derivatives bearing in position -3 of the pyrrole ring, several variously functionalized, not aliphatic, side chains which confer to the compounds a relevant COX-2 potency and selectivity along with a remarkable oral efficacy. Phenyl rings in position -1 and -5 are variously substituted, but compounds of particular interest are those substituted in position -5 with 4-methylsulphonyl-phenyl or with 4-aminosulphonyl-phenyl groups.Type: GrantFiled: August 3, 2006Date of Patent: March 15, 2011Assignee: Rottapharm S.p.A.Inventors: Andrea Cappelli, Maurizio Anzini, Mariangela Biava, Francesco Makovec, Antonio Giordani, Gianfranco Caselli, Lucio Claudio Rovati
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Publication number: 20110054180Abstract: This invention relates to the use of nano-organocatalysts, and, more specifically, to the use of magnetic nanomaterial-supported organocatalysts. It is an object of the present invention to provide “green” catalysts and protocols. According to one embodiment of the invention, a nano-organocatalyst in the form of a magnetic nanomaterial-supported organocatalyst is provided. According to other embodiments of the invention, glutathione and cysteine are provided as organocatalysts and magnetic nanomaterial-supported glutathione and magnetic nanomaterial-supported cysteine are provided for use as nano-organocatalysts. According to another embodiment of the invention, a method of using a recyclable magnetic nanomaterial-supported organocatalyst using a totally benign aqueous protocol, without using any organic solvent in the reaction or during the workup, is provided.Type: ApplicationFiled: September 3, 2009Publication date: March 3, 2011Applicant: USA as Represented by the Administrator of U.S. Environmental Protection AgencyInventors: Rajender S. Varma, Vivek Polshettiwar
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Publication number: 20110039908Abstract: Small molecules are used to inhibit specific receptor-ligand interaction between Alzheimer's amyloid-? peptide (A?) and Receptor for Advanced Gly-cation Endproducts (RAGE). Objectives include treating Alzheimer's disease and other pathologies involving cerebral amyloid angiopathy; improving blood flow to or within the brain; decreasing the level of A? in the brain; reducing neuropathology associated with Alzheimer's disease; reducing inflammation and/or oxidant stress in the brain; improving memory and/or learning; treating other conditions involving A?/RAGE interaction at the blood-brain barrier, RAGE-mediated transport of A? into the brain, or RAGE activation in brain vasculature and/or brain parenchyma (e.g., diabetic complications); or any combination thereof.Type: ApplicationFiled: January 26, 2007Publication date: February 17, 2011Inventors: Berislav V. Zlokovic, Rashid Deane, Benjamin L. Miller
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Publication number: 20100305056Abstract: Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, strongyloidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.Type: ApplicationFiled: November 26, 2008Publication date: December 2, 2010Applicant: Merck Frosst Canada Ltd.Inventors: Elise Isabel, Christophe Mellon, Christian Beaulieu
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Patent number: 7829728Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, Ar1, Ar2, E, a, b, c and z are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: November 13, 2007Date of Patent: November 9, 2010Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes
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Publication number: 20100280248Abstract: Novel compounds of formula 1 or a pharmaceutically acceptable salt thereof inhibit cytochrome P450 monooxygenase.Type: ApplicationFiled: July 12, 2010Publication date: November 4, 2010Applicant: ABBOTT LABORATORIESInventor: Dale J. Kempf
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Publication number: 20100256115Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: ApplicationFiled: March 18, 2010Publication date: October 7, 2010Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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Publication number: 20100256156Abstract: The present invention provides a heterocyclic compound represented by the following formula (I), which has a glucagon antagonistic action and is useful for the prophylaxis or treatment of diabetes and the like, a compound represented by wherein ring A is an optionally substituted benzene ring and the like; Y is a nitrogen atom and the like; X is —O— and the like; R4 is a hydrogen atom and the like; R5 and R6 are each independently a hydrogen atom and the like; R1 is an optionally substituted hydrocarbon group and the like; R2 is a hydrogen atom and the like; and R3 is —(CH2)3—COOH and the like, or a salt thereof.Type: ApplicationFiled: October 31, 2008Publication date: October 7, 2010Inventors: Yoshihiro Banno, Ryoma Hara, Ryosuke Tokunoh
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Publication number: 20100203645Abstract: The invention relates to compositions and methods useful in the labeling and identification of proteins. The invention provides for highly soluble zwitterionic dye molecules where the dyes and associated side groups are non-titratable and maintain their net zwitterionic character over a broad pH range, for example, between pH 3 and 12. These dye molecules find utility in a variety of applications, including use in the field of proteomics.Type: ApplicationFiled: August 31, 2009Publication date: August 12, 2010Inventors: Edward A. DRATZ, Paul A. GRIECO
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Publication number: 20100204228Abstract: In one embodiment, compounds of the following structure are described, wherein R1 to R7 are described herein. Also provided are methods for preparing these compounds and methods of contraception; treating or preventing fibroids; treating or preventing uterine leiomyomata; treating or preventing endometriosis, dysfunctional bleeding, and polycystic ovary syndrome; treating or preventing hormone-dependent carcinomas; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; and treating cycle-related symptoms using the compounds described herein.Type: ApplicationFiled: April 15, 2010Publication date: August 12, 2010Applicant: Wyeth LLCInventors: Casey Cameron McComas, Andrew Fensome, Michael Anthony Marella
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Publication number: 20100174090Abstract: The present application relates to novel methods for the preparation of primary, secondary and tertiary carbinamine compounds, particularly the preparation of compounds of formulae I, IV and VI, from a carbonyl compound of formula II in the presence of ammonia or an ammonium equivalent of the formula NH4+X?, by way of allylation, crotylation, arylation, reductive amination and catalytic hydrogenation.Type: ApplicationFiled: March 28, 2008Publication date: July 8, 2010Inventors: Avinash N. Thadani, Bhartesh Dhudshia
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Patent number: 7723332Abstract: In one embodiment, compounds of the following structure are described, wherein R1to R7are described herein. Also provided are methods for preparing these compounds and methods of contraception; treating or preventing fibroids; treating or preventing uterine leiomyomata; treating or preventing endometriosis, dysfunctional bleeding, and polycystic ovary syndrome; treating or preventing hormone-dependent carcinomas; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; and treating cycle-related symptoms using the compounds described herein.Type: GrantFiled: March 4, 2008Date of Patent: May 25, 2010Assignee: Wyeth LLCInventors: Casey Cameron McComas, Andrew Fensome, Michael Anthony Marella
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Patent number: 7700607Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: July 18, 2007Date of Patent: April 20, 2010Inventors: Essa Hu, Jason Brooks Human, Roxanne Kunz, Andrew Tasker, Ryan White
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Patent number: 7691818Abstract: New peptidomimetic inhibitors of retroviral proteases are in particular for human immunodeficiency virus (HIV) protease. These inhibitors include as the core structure a new diamiriodiol isostere of the dipeptide Phe-Pro having four stereogenic centers. The inhibitors have been shown to inhibit HIV-protease and can therefore be usefully employed as antivirals for post-exposure prophylaxis and as a therapy for viral infections by a retrovirus, in particular HIV. The syntheses processes of the isosteres and inhibitors are also described.Type: GrantFiled: June 15, 2005Date of Patent: April 6, 2010Assignee: Universita' Degli Studi Di TreisteInventors: Fabio Benedetti, Alessandro Tossi, Federico Berti, Pietro Campaner, Francesca Dinon
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Patent number: 7683184Abstract: The heterocyclic compound of the present invention is represented by general formula (I) and is suitable to forming an optical recording layer in an optical recording medium to which short-wavelength light is applied for recording and playing-back.Type: GrantFiled: August 18, 2005Date of Patent: March 23, 2010Assignee: Adeka CorporationInventors: Satoshi Yanagisawa, Yusuke Kubota
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Patent number: 7671216Abstract: The present invention relates to processes for the preparation of (3R, 5R)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-[(4-hydroxy methyl phenyl amino)carbonyl]-pyrrol-1-yl]-3,5-dihydroxy-heptanoic acid hemi calcium salt.Type: GrantFiled: November 8, 2006Date of Patent: March 2, 2010Assignee: Ranbaxy Laboratories LimitedInventors: Jitendra Anant Sattigeri, Sachin Sethi, Kaushal Kishore
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Publication number: 20100022394Abstract: The present invention consists on the synthesis of new products for the treatment of the iron chlorosis. These products may have improved properties regarding the currently known treatments. The new products are non-symmetrical ethylene diamino hidroxyphenyl acetic acid derivatives possessing only five coordination sites able to chelate metals.Type: ApplicationFiled: December 20, 2007Publication date: January 28, 2010Applicant: TRADECORP, S.A.Inventors: Miguel A. Sierra, Mar Gomez-Gallego, Juan J. Lucena, Sonia Garcia-Marco, Rosa Escudero
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Patent number: 7652062Abstract: Progesterone receptor modulators of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. These compounds are useful for contraception and hormone replacement therapy. Also provided are products containing these compounds.Type: GrantFiled: September 12, 2007Date of Patent: January 26, 2010Assignee: Wyeth LLCInventors: Casey Cameron McComas, Andrew Fensome, Edward George Melenski
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Patent number: 7648738Abstract: Compounds of the formulae (I), (II), (III) and (IV), wherein Ch1 is e.g. the formula (V) or (VI); Ch2 is the formula (VII) or (VIII); Het1 is for example furyl, thienyl, pyrrolyl, pyridyl, benzothienyl, quinolyl or bithienyl; each of which is optionally substituted; Het2 and Het2? e.g. are furylene, thienylene, pyrrolylene, benzothienylene, quinolylene, furylenecarbonyl, thienylenecarbonyl, benzothienylenecarbonyl or bithienylenecarbonyl; each of which is optionally substituted; A1, and Ar1? i.a. are phenyl, naphthyl, benzoyl or naphthoyl, each of which is optionally substituted; Ar2 is for example phenylene, optionally substituted; M i.a. is C1-C20alkylene; R1 is for example C1-C12alkyl or phenyl; R2 and R2? for example are hydrogen or C1-C20 alkyl; exhibit an unexpectedly good performance in photopolymerization reactions.Type: GrantFiled: November 24, 2003Date of Patent: January 19, 2010Assignee: Ciba Specialty Chemicals CorporationInventors: Junichi Tanabe, Hisatoshi Kura, Hidetaka Oka, Masaki Ohwa
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Patent number: 7645757Abstract: The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ishaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula alkylene group; a salt thereof, or a hydrate or a solvate of said compound or said salt; where the variables are as defined in the attached specification.Type: GrantFiled: August 14, 2006Date of Patent: January 12, 2010Assignee: sanofi-aventisInventors: Ahmed Abouabdellah, Regine Bartsch-Li, Christian Hoornaert, Antoine Ravet
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Patent number: 7645799Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: November 7, 2008Date of Patent: January 12, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. P. Pinto
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Publication number: 20090318693Abstract: Estrogen-Related Receptor (ERR) modulating compounds and methods for synthesis of said compounds are described.Type: ApplicationFiled: May 29, 2009Publication date: December 24, 2009Inventors: Barry Forman, Donna Yu
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Publication number: 20090318495Abstract: Compounds of the formula (I), which are suitable for use as microbiocides, and in which A is A1, or A is A2, or A is A3, or A is A4 and B is a phenyl, naphthyl or quinolinyl group.Type: ApplicationFiled: June 14, 2007Publication date: December 24, 2009Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Daniel Stierli, John J. Taylor, Harald Walter, Paul Anthony Worthington
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Publication number: 20090306396Abstract: The present invention relates to novel compounds having a xanthine oxidase inhibitory effect and an uricosuric effect and pharmaceutical compositions comprising the same as an active ingredient. That is, the present invention relates nitrogen-containing heterocyclic compounds represented by the following general formula (I): wherein Y1 represents N or C(R4); Y2 represents N or C(R5); R4 and R5 independently represent an alkyl group, a hydrogen atom etc.; one of R1 and R2 represents an optionally substituted aryl group, an alkoxy group or an optionally substituted heterocyclic group; the other of R1 and R2 represents a haloalkyl group, a cyano group, a halogen atom etc.; and R3 represents a 5-tetrazolyl group or a carboxy group, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the same as an active ingredient.Type: ApplicationFiled: October 3, 2006Publication date: December 10, 2009Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Takahiro Toyoshima, Toshinobu Sasaki, Chikara Hoshino, Masakazu Takeda
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Publication number: 20090306371Abstract: Methods for preparing cyclic carbamates and thiocarbamates containing cyanopyrrole moieties and of the formula are provided. Z are the same or different and are H, optionally substituted C1 to C6 alkyl, or CORA; RA is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl; Q are the same or different and are H, OH, NH2, CN, halogen, optionally substituted C1 to C6 alkyl, optionally substituted C2 to C6 alkenyl, optionally substituted C1 to C6 alkynyl, optionally substituted C1 to C6 alkoxy, optionally substituted C1 to C6 aminoalkyl, or CORB; and RB is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl.Type: ApplicationFiled: July 24, 2009Publication date: December 10, 2009Applicant: WyethInventor: Bogdan Kazimierz Wilk
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Patent number: 7629493Abstract: The invention relates to a process for the crystallization of the compounds of the formula (I) or acid-addition salts thereof, in which R1, R2 and R3 have the meaning indicated in Claim 1.Type: GrantFiled: April 10, 2004Date of Patent: December 8, 2009Assignee: Merck Patent GmbHInventors: Michael Kirschbaum, Ekkehard Bartmann, Dieter Bensinger, Alexander Haas, Ricky Lippert
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Patent number: 7626034Abstract: The present invention relates to a process for producing amino acid derivatives such as optically active ?-amino acid in short steps with good yield and high optical purity, which comprises reacting a keto acid of the formula (1): wherein R1 is hydrogen, an optionally substituted hydrocarbon, etc.; R2 is a spacer; and R3 is an optionally substituted alkoxy, etc., or a salt thereof, with ammonia or an amine or a salt thereof in the presence of a chiral catalyst and in the presence or absence of an acid and/or a fluorine-containing alcohol, to give an amino acid derivative of the formula (2): wherein Q is a group formed by removing one hydrogen atom from ammonia or an amine; X? is an acid and/or a fluorine-containing alcohol; and b is 0 or 1.Type: GrantFiled: September 17, 2004Date of Patent: December 1, 2009Assignee: Takasago International CorporationInventors: Kazuhiko Matsumura, Takao Saito
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Patent number: 7619097Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.Type: GrantFiled: June 24, 2008Date of Patent: November 17, 2009Assignee: Magnesium Diagnostics, Inc.Inventor: Ibert Clifton Wells
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Patent number: 7615647Abstract: A process is provided for preparing pharmaceutical grade atorvastatin hemicalcium salt comprising: (a) deesterifying, wherein R is an ester protecting group to (b) extracting R(R*,R*)-3 into an organic solvent or mixture of solvents, (c) adding a base of formula NR1R2R3 wherein R1, R2 and R3 are independently selected from H, substituted or non-substituted C1 to C7 alkyl, C6 to C9 aryl, C8 to C10 aralkyl or aminoalkyl to form atorvastatin base salt, (d) isolating by precipitation of the above atorvastatin base salt and purifying when necessary, (e) converting atorvastatin base salt to atorvastatin hemicalcium salt by treatment with a calcium salt solution, and (f) isolating the atorvastatin hemicalcium salt.Type: GrantFiled: August 5, 2005Date of Patent: November 10, 2009Assignee: Apotex Pharmachem Inc.Inventors: K.S. Keshava Murthy, Yajun Zhao, Daqing Che, Bhaskar Reddy Guntoori, Sammy Chris Duncan, Stephen E. Horne
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Publication number: 20090275617Abstract: Disclosed is an aryl-substituted nitrogen-containing heterocyclic compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof. This compound serves as nociceptin receptor antagonist and is useful as a pharmaceutical agent for treating diseases associated with a nociceptin receptor. (I) [in the formula, A1, A2 and A3 independently represent a carbon atom or a nitrogen atom, and one or two of A1, A2 and A3 represent a carbon atom; R1 represents a lower alkyl group or the like; R2 represents a phenyl group which may be substituted with a halogen atom or the like; R3 represents a hydrogen atom, a lower alkyl group or the like; and R4 represents a lower alkyl group or the like.Type: ApplicationFiled: September 28, 2006Publication date: November 5, 2009Inventors: Hirokatsu Ito, Kensuke Kobayashi, Hisashi Ohta, Osamu Okamoto, Satoshi Ozaki, Tomohiro Tsujita
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Publication number: 20090264500Abstract: This invention relates to 3-substituted-1,5-diaryl-2-alkyl-pyrroles of Formula I, pharmaceutical compositions containing them, and to their use for the pharmacological treatment of pain and COX-2 over-activation associated disorders. Compounds of this invention are new pyrrole derivatives bearing in position-3 of the pyrrole ring, several variously functionalized, not aliphatic, side chains which confer to the compounds a relevant COX-2 potency and selectivity along with a remarkable oral efficacy. Phenyl rings in position-1 and -5 are variously substituted, but compounds of particular interest are those substituted in position-5 with 4-methylsulphonyl-phenyl or with 4-aminosulphonyl-phenyl groups.Type: ApplicationFiled: August 3, 2006Publication date: October 22, 2009Inventors: Andrea Cappelli, Maurizio Anzini, Mariangela Biava, Francesco Makovec, Antonio Giordani, Gianfranco Caselli, Lucio Claudio Rovati
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Publication number: 20090253656Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.Type: ApplicationFiled: March 29, 2006Publication date: October 8, 2009Applicant: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Patent number: 7572824Abstract: Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrile groups, and the products thereby are provided.Type: GrantFiled: November 16, 2007Date of Patent: August 11, 2009Assignee: WyethInventor: Bogdan K. Wilk
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Patent number: 7553971Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds of formula (I): wherein R1-R13 and w have any of the values described in the specification. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: April 10, 2006Date of Patent: June 30, 2009Assignee: Theravance, Inc.Inventors: Edmund J. Moran, John R. Jacobsen, Michael R. Leadbetter, James Aggen, Timothy J. Church
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Patent number: 7534541Abstract: Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula: where n is an integer between 1 and 10, inclusive; R1 comprises a functional group selected from the group consisting of a reactive ring group, an ethylenically unsaturated group, a reactive polar group, a hydrazone group, and an azine group; R2, R3, R4, R5, and R6 comprise, each independently, H, an alkyl group, an alkenyl group, an alkynyl group, an aromatic group, a heterocyclic group, or a part of a ring group; X is a bond or a linking group; and Q is O, S, or NR where R is H, an alkyl group, an acyl group, an alkenyl group, an alkynyl group, a heterocyclic group, or an aromatic group; and (b) a charge generating compound.Type: GrantFiled: January 27, 2005Date of Patent: May 19, 2009Assignee: Samsung Electronics Co., Ltd.Inventors: Maryte Daskeviciene, Vytautas Getautis, Tadeus Lozovski, Edmundas Montrimas
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Patent number: 7504521Abstract: A method for preparing a compound having the formula: including the steps of: (a) cyclizing a compound of formula II: to form a compound of formula I: (b) deprotecting the nitrogen atom of the compound of formula I by amination or hydrogenation to form compound III.Type: GrantFiled: August 5, 2005Date of Patent: March 17, 2009Assignee: Bristol-Myers Squibb Co.Inventor: Paul C. Lobben
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Publication number: 20090069558Abstract: A method of making chlorins comprises the steps of reacting (e.g. condensing) a dipyrrin western half intermediate with an eastern half intermediate to form a tetrahydrobilene, and then cyclizing the tetrahydrobilene to form a chlorin. Intermediates including tetrahydrobilenes useful in such reactions are also described.Type: ApplicationFiled: November 14, 2008Publication date: March 12, 2009Applicant: North Carolina State UniversityInventors: Jonathan S. Lindsey, Masahiko Taniguchi, Doyoung Ra, Guoning Mo, Thiagarajan Balasubramanian
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Patent number: 7495022Abstract: Disclosed are agents that inhibit histone deacetylase. More specifically, the present invention relates to novel hydroxamic acid derivatives or pharmaceutically acceptable salts thereof for anticancer agents or other therapeutic agents based on their histone deacetylase inhibitory activity.Type: GrantFiled: April 10, 2003Date of Patent: February 24, 2009Assignee: SK Chemicals Co., Ltd.Inventors: Dae-Kee Kim, Ju Young Lee, Nam Kyu Lee, Jae-Sun Kim, Junwon Lee, Suk Ho Lee, Jin Young Choi, Je Ho Ryu, Nam Ho Kim, Guang-Jin Im, Tae Kon Kim, Jung-Woo Seo, Young-Jue Bang
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Publication number: 20090042041Abstract: The present invention relates to a process for the preparation of ligands and copper complexes useful in the deposition of copper via Atomic Layer Deposition (ALD) and Chemical Vapor Deposition (CVD), and the use of the copper complexes in ALD and CVD processes.Type: ApplicationFiled: October 20, 2008Publication date: February 12, 2009Applicant: E. I. duPont de Nemours and CompanyInventor: Vladimir Grushin
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Publication number: 20090023777Abstract: This invention provides 4-amino-1-benzylpiperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome, asthma and chronic obstructive pulmonary disease, using such compounds.Type: ApplicationFiled: March 6, 2008Publication date: January 22, 2009Inventors: Mathai Mammen, Richard Wilson, Sarah Dunham, Adam Hughes, Craig Husfeld, Yu-Hua Ji, Li Li, Trevor Mischki, Ioanna Stergiades, David Oare
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Publication number: 20080287424Abstract: The present invention provides an azolylacylquanidine compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.Type: ApplicationFiled: July 15, 2008Publication date: November 20, 2008Applicant: WyethInventors: Derek Cecil Cole, Eric Steven Manas, Lee Dalton Jennings, Frank Eldridge Lovering, Joseph Raymond Stock, William Jay Moore, John Watson Ellingboe, Jeffrey Scott Condon, Mohani Nirmala Sukhdeo, Ping Zhou, Junjun Wu, Koi Michele Morris
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Patent number: 7442807Abstract: The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.Type: GrantFiled: March 15, 2006Date of Patent: October 28, 2008Assignee: Action Pharma A/SInventors: Torbjörn Lundstedt, Anna Skottner, Arne Boman, Per Andersson, Elisabeth Seifert, Victor Andrianov
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Publication number: 20080262074Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid or solvates or hydrates thereof, as well as crystalline salts characterized by their X-ray powder diffraction pattern are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.Type: ApplicationFiled: May 13, 2005Publication date: October 23, 2008Applicant: PFIZER, INC.Inventors: George Quallich, Peter Pawloy
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Publication number: 20080255095Abstract: A compound of the formula (I): wherein R1 is C1-C6 alkyl, amino, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are hydrogen or C1-C6 alkyl; Arom is phenyl, idenyl, napthyl, phenanthrenyl, furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; A is C1-C6 alkylene; Ra is hydrogen, C1-C6 alkyl or C2-C6 alkenyl; E is a single bond, oxygen, sulfur or —NR4—, wherein R4 is hydrogen or C1-C7 alkanoyl; X1 and X2 are oxygen or sulfur; or a pharmacologically acceptable salt or ester thereof.Type: ApplicationFiled: June 18, 2007Publication date: October 16, 2008Applicant: BTG INTERNATIONAL LIMITEDInventors: Kazuo Koyama, Shinji Marumoto, Narihiro Toda, Hiroshi Kogen, Keiko Suzuki
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Publication number: 20080235882Abstract: o-Aminophenol derivatives of the general formula (I) or physiologically compatible, water-soluble salts thereof, in which X is oxygen, sulfur or N—R4; R1, R2, R3 may be identical or different and, independently of one another, are hydrogen, a halogen atom, a cyano group, a C1-C4-alkoxy group, a C1-C6-alkyl group, a C1-C4-alkyl thioether group, a mercapto group, a nitro group, a trifluoromethane group, a —C(O)H group, a —C(O)CH3 group, a —C(O)CF3 group, an —Si(CH3)3 group, a C1-C4-hydroxyalkyl group or an aminomethyl group; R4 is hydrogen, a C1-C6-alkyl group, a C1-C4-hydroxy-alkyl group, a phenyl group or an acetyl group; and colorants containing said compounds for keratin fibers.Type: ApplicationFiled: May 18, 2005Publication date: October 2, 2008Inventors: Laurent Chassot, Hans-Juergen Braun
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Patent number: 7420000Abstract: Aminophosphonate and amino bisphosphonate compounds and methods for their preparation are provided. Also provided are pharmaceutical and agricultural compositions containing the compounds. The compounds and compositions are useful in methods for treatment of various diseases, including, inflammation, autoimmune disease, cardiovascular disease, bacterial infection, viral disease, abnormal cell proliferation, bone resorption disease, osteoporosis, or parasitic disease and in various agricultural methods, including, methods of eradicating weeds.Type: GrantFiled: September 10, 2004Date of Patent: September 2, 2008Assignee: University of Southern CaliforniaInventor: Nicos A. Petasis
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Publication number: 20080176838Abstract: The invention relates to compounds of formula (I) wherein R1-9, Z, n, X, A, and Rb have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament for the treatment of type 2 diabetes mellitus, obesity and lipid disorders.Type: ApplicationFiled: June 8, 2005Publication date: July 24, 2008Applicant: SANTHERA PHARMACEUTICALS (DEUTSCHLAND) AGInventors: Paul John Edwards, Silvia Cerezo-Galvez, Achim Feurer, Oliver Hill, Meinolf Thiemann, Victor Giulio Matassa, Sonja Nordhoff, Meritxell Lopez-Canet
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Publication number: 20080176924Abstract: The invention relates to compounds having formula (I): Wherein X, R1, R2, R3, R4 and R5 are as defined herein. The invention also relates to the preparation method thereof and the use of same in therapeutics.Type: ApplicationFiled: December 7, 2007Publication date: July 24, 2008Applicant: SANOFI-AVENTISInventors: Francis BARTH, Christian CONGY, Laurent HORTALA, Murielle RINALDI-CARMONA