Single Bond Between 1,2-positions And Single Bond Between 3,4-positions Patents (Class 546/165)
-
Publication number: 20100129471Abstract: The invention relates to a compound of the formula (I) in which: R1, R2 and R3 are independently a methoxy group optionally substituted by one or more fluorine atoms; R4 is a hydrogen atom; R5 and R6 are identical and each represent a hydrogen or fluorine atom; A is a cycle selected from the group including aryl and heteroaryl groups, wherein said groups can be substituted.Type: ApplicationFiled: April 4, 2008Publication date: May 27, 2010Inventors: Mouâd Alami, Jean-Daniel Brion, Olivier Provot, Jean-François Peyrat, Samir Messaoudi, Abdallah Hamze, Anne Giraud, Jérôme Bignon, Joanna Bakala, Jian-Miao Liu
-
Publication number: 20100120838Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.Type: ApplicationFiled: January 20, 2010Publication date: May 13, 2010Inventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Shankar B. Bandarpalle, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta M. Micula, Seong Heon Kim, De-Yi Yang, Razia Rizvi
-
Patent number: 7700552Abstract: Compounds of the formula (I): and N-oxides, salts and stereoisomers thereof wherein A is OR1, NHS(?O)pR2, NHR3, NRaRb, C(?O)NHR3 or C(?O)NRaRb wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl; R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl or NRaRb; R3 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl, —OC1-C6alkyl, —OC0-C3alkylenecarbocyclyl, —OC0-C3alkyleneheterocyclyl; wherein any alkyl, carbocyclyl or heterocycylyl in R1, R2 or R3 are optionally substituted p is independently 1 or 2; n is 3, 4, 5 or 6; denotes an optional double bond; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Ry and Ry? are independently C1-C6alkyl; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; W is —CH2—, —O—, —OC(?O)NH—, —OC(?O)—, —S—, —NH—, —NRa, —NHS(?O)2—, —NHC(=0)NH— or —NHC(?O)—, —NHC(?S)NH— or a bond; R8 is an optionally substituted ring system containing 1 or 2 saturated, partially saturated or unsaturated carboType: GrantFiled: July 28, 2006Date of Patent: April 20, 2010Assignee: Medivir ABInventors: Horst Wähling, Bertil Samuelsson
-
Publication number: 20100063063Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.Type: ApplicationFiled: September 9, 2009Publication date: March 11, 2010Inventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
-
Publication number: 20100048447Abstract: Bis(hydroxyquinoline)-metal complexes and the use thereof as bleach catalysts are described.Type: ApplicationFiled: October 12, 2009Publication date: February 25, 2010Applicant: Henkel AG & Co. KGaAInventors: Andre Hätzelt, Anette Nordskog, Stefan Leopold, Peter Schmiedel, Wolfgang von Rybinski, Jörg Sundermeyer, Jan Döring
-
Publication number: 20100041700Abstract: The present invention relates to 1-(Azolin-2-yl)-amino-1,2-heterocyclyl-ethane compounds, which are useful for combating insects, arachnids and nematodes. The present invention also relates to methods for combating animal pests and to compositions for combating animal pests. It has been found that animal pests can be combated by 1-(Azolin-2-yl)-amino-1,2-heterocyclyl-ethane compounds of the general formula (I): wherein A is a radical of the formulae A1 or A2: and wherein X is sulfur, oxygen or NR7, and HetA, HetB and R1 to R7 are defined as in the description.Type: ApplicationFiled: December 11, 2007Publication date: February 18, 2010Applicant: BASF SEInventors: Markus Kordes, Ronan Le Vezouet, Christopher Koradin, Ernst Baumann, Deborah L. Culbertson
-
Publication number: 20100035926Abstract: The present invention provides compounds of formula (I): a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates, and to use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation.Type: ApplicationFiled: December 19, 2007Publication date: February 11, 2010Inventors: Ian Baxter Campbell, Diane Mary Coe, Anthony William James Cooper, Graham George Adam Inglis, Haydn Terence Jones, Steven Philip Keeling, Simon John Fawcett MacDonald, Philip Alan Skone, Gordon Gad Weingarten
-
Publication number: 20100029606Abstract: The present invention provides compounds of formula (I) and compositions thereof, methods of making them, and methods of using them to modulate alpha7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.Type: ApplicationFiled: January 16, 2008Publication date: February 4, 2010Applicants: WYETH, SIENA BIOTECH S.P.A.Inventors: Chiara Ghiron, Arianna Nencini, Iolanda Micco, Riccardo Zanaletti, Laura Maccari, Hendrick Bothmann, Simon N. Haydar, Maurizio Varrone, Carmela Pratelli, Boyd L. Harrison
-
Publication number: 20100029623Abstract: The invention relates to compounds of formula (I) wherein R0 represents H or OH; R1 represents alkoxy; U and W represent N, V represents CH and R2 represents H or F, or U and V represent CH, W represents N and R2 represents H or F, or U and V represent N, W represents CH and R2 represents H, or U represents N. V represents CH, W represents CRa and R2 represents H; Ra represents CH2OH or alkoxycarbonyl; A represents the group CH?CH—B or a binuclear heterocyclic system D, B representing a mono- or di-substituted phenyl group wherein the substituents are halogen atoms and D representing one of the following groups wherein Z represents CH or N, and Q represents O or S; and to salts of such compounds. These compounds are useful as antibacterial agents.Type: ApplicationFiled: December 21, 2007Publication date: February 4, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Phillippe Surivet, Cornelia Zumbrunn
-
Publication number: 20100022535Abstract: 2-pyridyl-substituted imidazoles which are used advantageously in the treatment of diseases mediated by ALK 5 or ALK 4 inhibitors or both.Type: ApplicationFiled: June 11, 2009Publication date: January 28, 2010Applicant: SK CHEMICALS CO., LTD.Inventors: Ju Young Lee, Jae-Sun Kim, Jung-Hoon Oh, Hoe-chul Jung, Hyun Jung Lee, Sang-hwan Kang, Yong-Hyuk Kim, Sung-hoon Park, Keun-Ho Ryu, Jung Bum Yi, Hun-Taek Kim, Key-An Um, Bong-yong Lee
-
Publication number: 20090318497Abstract: This invention provides a compound of the formula (I): wherein A1 is N and A2 is CR7, or A1 is CR7 and A2 is N; Y1, Y2 and Y3 are each independently CH or N, Y4 and Y5 are each independently CR8 or N, with the proviso that when one of Y1, Y2, Y3, Y4 and Y5 is N, the others are not N; R1 and R2 are each independently hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl or hydroxy(C1-C6)alkyl; R3 and R8 are each independently hydrogen, halogen, hydroxy, (C1-C6)alkyl, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl or (C1-C6)alkylsulfonyl; R4 is halogen, (C1-C6)alkyl, (C3-C6)cycloalkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, halo(C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkylsulfonyl, halo(C1-C6)alkylsulfinyl, halo(C1-C6)alkylthio, [(C1-C6)alkyl]NH— or [(C1-C6)alkyl]2N—; and R5, R6 and R7 are each independently hydrogen, halogen, (C1-C6)alkyl, hydroxy(C1-C6)alkyl, orType: ApplicationFiled: September 10, 2007Publication date: December 24, 2009Inventors: Satoshi Nagayama, Yuji Shishido, Hirotaka Tanaka
-
Publication number: 20090312555Abstract: There is provides a process for the preparation of a compound of formula (7): wherein R is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; provides that R is not a compound of Formula (a): wherein Ra represents an alkyl group, such as a C1-16 alkyl group, and preferably an isopropyl group; Rb represents an aryl group, preferably a 4-fluorophenyl group; Rc represents hydrogen, a protecting group or an alkyl group, such as a C1-16 alkyl group, and preferably a methyl group; and Rd represents hydrogen, a protecting group or a SO2Re group where Re is an alkyl group, such as a C1-16 alkyl group, and preferably a methyl group.Type: ApplicationFiled: November 28, 2005Publication date: December 17, 2009Applicant: NPIL PHARMACEUTICAL (UK) LIMITEDInventors: David John Moody, Jonathan William Wiffen
-
Publication number: 20090298872Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorder associated with the activation of steroid hormone nuclear receptors.Type: ApplicationFiled: December 13, 2005Publication date: December 3, 2009Applicant: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, John Wityak
-
Publication number: 20090285772Abstract: Quinoline derivatives, particularly 4-anilinoquinoline derivatives, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.Type: ApplicationFiled: April 10, 2009Publication date: November 19, 2009Applicant: SuperGen, Inc.Inventors: Pasit Phiasivongsa, Sanjeev G. Redkar, Swarna Gamage, Darby Brooke, William Denny, David J. Bearss, Hariprasad Vankayalapati, Yong Xu, Krzysztof Swierczek
-
Patent number: 7618965Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, Q, Y, R1, R2, and R5 are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid cystic carcinoma, acute myelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcinoma, and prostate carcinoma.Type: GrantFiled: September 15, 2005Date of Patent: November 17, 2009Assignee: OSI Pharmaceuticals, Inc.Inventors: Andrew Crew, An-Hu Li, Bijoy Panicker
-
Publication number: 20090281103Abstract: The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: July 20, 2006Publication date: November 12, 2009Inventors: Christopher I. Bayly, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
-
Publication number: 20090278118Abstract: There are provided a novel benzofluoranthene compound and an organic light-emitting device which uses the benzofluoranthene compound, gives a blue emission hue with extremely good purity, and has an optical output with a high efficiency, a high luminance, and a long life. Specifically, there are provided a benzofluoranthene compound represented by the general formula shown below and an organic light-emitting device including a pair of electrodes including an anode and a cathode one of which is a transparent or translucent electrode material, and an organic compound layer disposed between the pair of electrodes and including a material for an organic light-emitting device containing the benzofluoranthene compound. In the general formula (1), one of X1, X2, X3, X4, X5, and X6 represents a substituted or unsubstituted fused heterocyclic group having four or less rings, and the others of X1, X2, X3, X4, X5, and X6 each represent a hydrogen atom.Type: ApplicationFiled: December 12, 2007Publication date: November 12, 2009Applicant: CANON KABUSHIKI KAISHAInventors: Hiroki Ohrui, Akihito Saitoh, Chika Negishi, Hironobu Iwawaki, Masanori Muratsubaki, Hiroyuki Tomono, Tetsuya Kosuge, Akihiro Senoo
-
Publication number: 20090278447Abstract: An organic luminescent device having organic-compound layers is provided which takes on luminous hues with very good purity and has optical power with high efficiency, high luminance and a long life. At least one of the organic-compound layers contains a benzo[k]fluoranthene compound represented by the following general formula (1): wherein R1 is a group selected from the group consisting of alkyl, aralkyl and a heterocyclic group which may be substituted, and R1 's may be the same or different; R10 to R20 are each independently a group selected from the group consisting of hydrogen, halogen, alkyl, aralkyl, phenyl, a condensed bicyclic aromatic group and a heterocyclic group which may be substituted; and a is an integer of 0 or more to 9 or less.Type: ApplicationFiled: July 18, 2007Publication date: November 12, 2009Applicant: CANON KABUSHIKI KAISHAInventors: Akihito Saitoh, Masanori Muratsubaki, Satoshi Igawa, Hiroki Ohrui, Chika Negishi, Masashi Hashimoto, Takao Takiguchi, Akihiro Senoo, Shinjiro Okada
-
Publication number: 20090281076Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful for the treatment of diabetes and as peripheral regulators of satiety, e.g. for the treatment of obesity and metabolic syndrome.Type: ApplicationFiled: April 11, 2007Publication date: November 12, 2009Inventors: Matthew Colin, Thor Fyfe, William Gattrell, Chrystelle Marie Rasamison
-
Patent number: 7615563Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: February 17, 2005Date of Patent: November 10, 2009Inventors: Jesus E. Gonzalez, III, Andreas P. Termin, Esther Martinborough, Nicole Zimmerman
-
Patent number: 7598385Abstract: The present disclosure provides the asymmetric cyanine fluorescent dyes of formula I in which X, n, R1, R2, R3, R4, R5 and Y? are as defined in the specification. The present disclosure also provides conjugates of the fluorescent dyes, methods for preparation thereof, compositions comprising the fluorescent dyes, and methods for staining biological samples using the fluorescent dyes and compositions thereof.Type: GrantFiled: December 31, 2007Date of Patent: October 6, 2009Assignee: Shenzhen Mindray Biomedical Electronics Co., Ltd.Inventors: Xiaojun Peng, Tong Wu, Jiangli Fan, Shiguo Sun, Bingshuai Wang, Bing Xu, Jianhui Shao
-
Patent number: 7592358Abstract: Alkyne compounds having MCH-receptor antagonistic activity, which are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes.Type: GrantFiled: April 13, 2005Date of Patent: September 22, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Dirk Stenkamp, Stephan Georg Mueller, Philipp Lustenberger, Thorsten Lehmann-Lintz, Gerald Juergen Roth, Klaus Rudolf, Marcus Schindler, Leo Thomas, Ralf Lotz
-
Patent number: 7576100Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.Type: GrantFiled: May 3, 2006Date of Patent: August 18, 2009Assignee: Acadia Pharmaceuticals, Inc.Inventors: Niels Skjaerbaek, Kristian Norup Koch, Bo Lennart Mikael Friberg, Bo-Ragnar Tolf
-
Publication number: 20090203710Abstract: Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnia repetitive hypersomnia, true hypersomnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's diseaseType: ApplicationFiled: March 6, 2009Publication date: August 13, 2009Inventors: Norikazu Ohtake, Ryo Yoshimoto, Shigeru Tokita, Akio Kanatani, Sayaka Mizutani
-
Patent number: 7572816Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.Type: GrantFiled: July 21, 2004Date of Patent: August 11, 2009Assignee: Auspex Pharmaceuticals, Inc.Inventors: Bruno Tse, Sepehr Sarshar
-
Publication number: 20090176270Abstract: Asymmetric cyanine fluorescent dyes are represented by general formula I. These kinds of dyes may be used as a staining agent for nucleic acids, with the spectra at 600-900 nm in the near-infrared region and without interference from background fluorescence. These kinds of dyes may be useful with small-type red semiconductor lasers as the light source (such as 633 nm). Compositions comprising these dyes and methods for staining biological samples using these dyes or compositions are also provided.Type: ApplicationFiled: December 12, 2008Publication date: July 9, 2009Applicant: SHENZHEN MINDRAY BIO-MEDICAL ELECTRONICS CO., LTD.Inventor: Jianhui Shao
-
Patent number: 7557125Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.Type: GrantFiled: December 9, 2004Date of Patent: July 7, 2009Assignee: Affinium Pharmaceuticals, Inc.Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. DeWolf, Dalia R. Jakas
-
Publication number: 20090170875Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: ApplicationFiled: December 18, 2008Publication date: July 2, 2009Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K.C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankar, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Umar Faruk Mansoor, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li
-
Publication number: 20090156586Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.Type: ApplicationFiled: February 3, 2009Publication date: June 18, 2009Inventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Bandarpalle B. Shankar, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Razia Rizvi, Lei Chen, De-Yi Yang, Robert Feltz, Seong Heon Kim
-
Publication number: 20090149440Abstract: The present invention provides an agent which exhibits excellent antibacterial activity, low toxicity, improved bioavailability, and low binding rate to serum proteins. The present invention is directed to a pyridonecarboxylic acid derivative represented by formula (1): or a salt thereof, wherein R1 represents a methyl group, a fluorine atom, or a chlorine atom; R2 represents a hydrogen atom or a lower alkyl group; R3 represents an isopropyl group or a tert-butyl group; R4 represents a methyl group or a halogen atom; and R5 represents a fluorine atom or a chlorine atom. The present invention is also directed to an antibacterial agent and a medicament containing the derivative or the salt thereof as an active ingredient.Type: ApplicationFiled: November 17, 2005Publication date: June 11, 2009Applicant: WAKUNAGA PHARMACEUTICAL CO., LTDInventors: Akira Yazaki, Yasuhiro Kuramoto, Kenji Itoh, Kazusa Yoshikai, Yuzo Hirao, Yoshihiro Ohshita, Norihiro Hayashi, Hirotaka Amano, Takayuki Amago, Hitomi Takenaka
-
Patent number: 7544804Abstract: Colorant compositions are useful for a wide variety of product applications. For example, colorants are used in tinting of polymers, providing colors to aqueous solution(s), and affording color to solid or semi-solid products such as detergents. Disclosed herein are colorant compositions having a triphenylmethane (“TPM”) structure having improved stability to alkaline conditions. Thus, the colorant compositions resist decolorization, even at relatively high pH levels.Type: GrantFiled: January 3, 2008Date of Patent: June 9, 2009Inventors: Eric B. Stephens, Pat Moore
-
Publication number: 20090131279Abstract: The present invention provides fluorescent dye compounds and methods of using the compounds for the staining of nucleic acids. In particular, the dye compounds comprise heterocyclic molecules with hydroxy alkyl and aromatic substituents, and the dye compounds form highly fluorescent complexes upon nucleic acid binding.Type: ApplicationFiled: November 15, 2007Publication date: May 21, 2009Applicant: SIGMA ALDRICH COMPANYInventors: Alexander Rueck, Bernhard Schoenenberger
-
Publication number: 20090124656Abstract: Compounds of formula (I): wherein: R1, R2, R3, R4 and X are as defined in the description, A represents an alkylene chain as defined in the description, B represents an alkyl or alkenyl group substituted by a group or R7, or B represents a group or R7. Medicinal products containing the same which are useful as hypoglycaemic and hypolipaemic agents.Type: ApplicationFiled: January 26, 2006Publication date: May 14, 2009Applicant: LES LABORATOIRES SERVIERInventors: Cicile Parmenon, Marie-Claude Viaud-Massuard, Jerome Guillard, Catherine Dacuet, Alain Ktorza, Daniel- Henri Caignard
-
Publication number: 20090113639Abstract: Disclosed are thiol dyes of formula (1), wherein R1 is hydrogen; C1-C12alkyl; or phenyl-C1-C4alkyl; X is C1-C12alkylene; C2-C12alkenylene; C5-C10cycloalkylene; C5-C10arylene; or C5-C10arylene-C1-C10alkylene; Y is the residue of an organic dye which corresponds to the formula (1a), wherein R2 is hydrogen; or C1-C5alkyl; R3 is a radical of formula (1a1): (1a2); or (1a3); or R2 and R3 together with the linking carbon atom 1C form a 6 to 10 membered carbocyclic ring which may optionally be a condensated aromatic system and may contain one or more than one hetero atom; and R4, R5 and R6 independently form each other are hydrogen, or C1-C5alkyl; Z is H; or a thio ester group of formula (1b), wherein A is O; S; or N—R9; B is —OR7; —NR7R8, or —SR7; and A is O; S; or N—R9; B is —OR7; —NR7R8, or —SR7; and R7, R8 and R9, independently from each other are hydrogen; C1-C12alkyl C6-C12aryl; or C6-C12aryl-C1-C12alkyl.Type: ApplicationFiled: September 27, 2006Publication date: May 7, 2009Inventors: Victor Paul Eliu, Beate Frohling, Achim Buhrer
-
Publication number: 20090111849Abstract: Cyclopropylamine salt of montelukast in crystalline form and its use for the preparation of highly pure amorphous montelukast sodium.Type: ApplicationFiled: December 27, 2007Publication date: April 30, 2009Applicant: INKE, SAInventors: Joan Huguet Clotet, Jordi Peirats Masia
-
Patent number: 7524844Abstract: The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: wherein X, Y, a, R1, and R2 are as defined herein.Type: GrantFiled: February 15, 2007Date of Patent: April 28, 2009Assignee: Glenmark Pharmaceuticals S.A.Inventors: Abraham Thomas, Balasubramanian Gopalan, V.S. Prasada Rao Lingam, Daisy Manish Shah
-
Publication number: 20090082372Abstract: The present invention relates to arylmethylene substituted N-Acyl-?-amino alcohols of the formula I in which Y is selected from the aryl or heteroaryl groups: and R1, R2, R3, R4, R5, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.Type: ApplicationFiled: July 24, 2008Publication date: March 26, 2009Inventors: Lars WORTMANN, Marcus Koppitz, Bernd Menzenbach, Dirk Kosemund, Norbert Schmees, Hans-Peter Muhn, Thomas Frenzel, Florian Peter Liesener, Anna Schrey, Ronald Kuehne
-
Publication number: 20090075978Abstract: The present invention relates to substituted propiolic acid amides, to methods for the production thereof, to medicaments containing these compounds and to the use thereof for producing medicaments.Type: ApplicationFiled: June 26, 2008Publication date: March 19, 2009Applicant: Grunenthal GmbHInventors: Michael HAURAND, Klaus SCHIENE, Sven KUHNERT, Melanie REICH, Saskia ZEMOLKA
-
Patent number: 7501386Abstract: Disclosed is a lubricating oil composition containing an oil of lubricating viscosity and a particularly effective mixture of a benzo[b]perhydroheterocyclic arylamine and a diarylamine which together provide superior oxidation inhibition.Type: GrantFiled: December 21, 2005Date of Patent: March 10, 2009Assignee: Chevron Oronite Company, LLCInventors: Richard E. Cherpeck, Carrie Y. Chan
-
Patent number: 7488725Abstract: Compounds are provided having the formula: wherein R1, R2, R2?, R3, R3?, R4, R4?, R5, X, Y and Z are as defined herein.Type: GrantFiled: October 30, 2006Date of Patent: February 10, 2009Assignee: Bristol-Myers Squibb Co.Inventors: Stephen P. O'Connor, Lawrence G. Hamann
-
Publication number: 20090023758Abstract: Compounds of the formula (I): and N-oxides, salts and stereoisomers thereof wherein A is OR1, NHS(?O)pR2, NHR3, NRaRb, C(?O)NHR3 or C(?O)NRaRb wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl; R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl or NRaRb; R3 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl, —OC1-C6alkyl, —OC0-C3alkylenecarbocyclyl, —OC0-C3alkyleneheterocyclyl; wherein any alkyl, carbocyclyl or heterocycylyl in R1, R2 or R3 are optionally substituted p is independently 1 or 2; n is 3, 4, 5 or 6; denotes an optional double bond; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Ry and Ry? are independently C1-C6alkyl; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; W is —CH2—, —O—, —OC(?O)NH—, —OC(?O)—, —S—, —NH—, —NRa, —NHS(?O)2—, —NHC(=0)NH— or —NHC(?O)—, —NHC(?S)NH— or a bond; R8 is an optionally substituted ring system containing 1 or 2 saturated, partially saturated or unsaturated carboType: ApplicationFiled: July 28, 2006Publication date: January 22, 2009Applicant: Medivir ABInventors: Horst Wahling, Bertil Samuelsson
-
Publication number: 20080319012Abstract: 2-pyridyl-substituted imidazoles which are used advantageously in the treatment of diseases mediated by ALK 5 or ALK 4 receptor or both.Type: ApplicationFiled: June 12, 2008Publication date: December 25, 2008Applicants: IN2GEN CO., LTD., SK CHEMICALS CO., LTD, EWHA UNIVERSITY INDUSTRY COLLABORATION FOUNDATIONInventors: Dae-Kee Kim, Yung-Jue Bang, Hun-Taek Kim, Il-Sang Cho, Myoung-Soon Park, Young Jae An, Joon Hun Choi
-
Patent number: 7468348Abstract: A polyol polymeric structure comprising a bleach activating moiety to give benefits in detergent compositions such as bleaching action, soil suspension, increased surfactant availability in the presence of free hardness.Type: GrantFiled: February 25, 2008Date of Patent: December 23, 2008Assignee: The Procter & Gamble CompanyInventors: Jeffrey John Scheibel, Julie Ann Menkhaus, George Douglas Hiler, II, Marc Eric Gustwiller
-
Patent number: 7468347Abstract: A polyol polymeric structure comprising a bleach activating moiety to give benefits in detergent compositions such as bleaching action, soil suspension, increased surfactant availability in the presence of free hardness.Type: GrantFiled: February 25, 2008Date of Patent: December 23, 2008Assignee: The Procter & Gamble CompanyInventors: Jeffrey John Scheibel, Julie Ann Menkhaus, George Douglas Hiler, II, Marc Eric Gustwiller
-
Patent number: 7459564Abstract: 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: January 12, 2006Date of Patent: December 2, 2008Assignee: Bristol-Myers Squibb CompanyInventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. Pinto
-
Patent number: 7442710Abstract: The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R? and R1, R2,R3, R4, R5, and R6 are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds can be used for the treatment of diseases related to the glycine transporter inhibitor, such as schizophrenia and Alzheimer's disease.Type: GrantFiled: January 24, 2006Date of Patent: October 28, 2008Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
-
Publication number: 20080262033Abstract: The present invention- relates to 2-methyl-4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivatives having the general Formula (I) wherein the substituents are defined as in the description, or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 2-methyl-4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivatives in therapy, more specifically for the treatment of fertility disorders.Type: ApplicationFiled: May 2, 2006Publication date: October 23, 2008Inventors: Willem Frederik Johan Karstens, Cornelis Marius Timmers
-
Publication number: 20080255068Abstract: The present application relates to a novel tetrahydroquinoline derivative, to a process for its preparation, to its use on its own or in combination for treating and/or preventing diseases and to its use for preparing medicaments, in particular as an inhibitor of the cholesterol ester transfer protein (CETP) for the treatment and/or prevention of cardiovascular disorders, in particular hypolipoproteinaemias, dyslipidaemias, hypertriglyceridaemias, hyperlipidaemias, hypercholesterolaemias and arteriosclerosis.Type: ApplicationFiled: December 15, 2005Publication date: October 16, 2008Applicant: Bayer HealthCare AGInventors: Hilmar Bischoff, Heike Gielen-Haertwig, Volkhart Li, Carsten Schmeck, Michael Thutewohl, Alexandros Vakalopoulos, Olaf Weber, Martina Wuttke
-
Publication number: 20080249111Abstract: Disclosed are compounds of formula I: wherein R1, R2, R3 and X are as defined herein, in free or salt form, which are useful as CCR5 inhibitors, e.g. in the prevention or treatment of disorders mediated by interactions between chemokine receptors and their ligands.Type: ApplicationFiled: May 2, 2008Publication date: October 9, 2008Inventors: Rainer ALBERT, Nigel Graham Cooke, Gebhard Thoma, Christian Bruns, Francois Nuninger, Markus Streiff, Hans-Gunter Zerwes
-
Patent number: 7429666Abstract: The present invention provides novel compounds of Formula I which are antagonists of the C5a receptor. Compounds of the present invention are useful for the treatment of various C5a-mediated diseases and disorders; accordingly the present invention provides a method for the treatment of C5a-mediated diseases using the novel compounds described herein, as well as pharmaceutical compositions containing them.Type: GrantFiled: February 8, 2005Date of Patent: September 30, 2008Assignee: Merck Frosst Canada Ltd.Inventors: Nicholas Lachance, Patrick Roy, Yves Leblanc