The Additional Hetero Ring Is Bonded Directly To A Ring Carbon Of The Bicyclo Ring System Patents (Class 548/466)
-
Publication number: 20130131060Abstract: The present invention relates to a compound of formula (I) wherein R1, R2 and R3 are as defined in the description and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula I and of the salts thereof. The compounds of formula I are suitable for treating tumors.Type: ApplicationFiled: December 10, 2010Publication date: May 23, 2013Applicant: Johannes Gutenberg-Universität MainzInventors: Gerd Dannhardt, Jan-Peter Kramb, Stanislav Plutizki
-
Publication number: 20130123259Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: December 20, 2012Publication date: May 16, 2013Applicant: Allergan, Inc.Inventor: Allergan, Inc.
-
Publication number: 20130123242Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.Type: ApplicationFiled: October 26, 2012Publication date: May 16, 2013Applicant: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen-Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constantin G. Yannopoulos
-
Publication number: 20130118570Abstract: Provided is a dye for photoelectric conversion containing at least one or more kind of a compound represented by the following General Formula (1) (in Formula (1), R1 and R2 represent any one of —CN, —SO2R, —COOR, and —CONR2 (R represents a hydrogen atom, a substituted or unsubstituted alkyl group, a cycloalkyl group, or an aryl group); R3 represents a direct bond or a substituted or unsubstituted alkylene group; X represents an acidic group; and D represents an organic group having an electron donating substituent or a substituted or unsubstituted heterocyclic group).Type: ApplicationFiled: November 18, 2010Publication date: May 16, 2013Applicant: NEC CORPORATIONInventors: Katsumi Maeda, Shin Nakamura, Kentaro Nakahara
-
Patent number: 8420638Abstract: The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.Type: GrantFiled: June 29, 2011Date of Patent: April 16, 2013Assignee: Gemin X Pharmaceuticals Canada Inc.Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elise Rioux, Sasmita Tripathy, Terrance W. Deyle
-
Publication number: 20130059899Abstract: The present invention is related to a method of determining a test compound's ability to modify the biological activity of a GPR17. Said method comprises, among others, the step of contacting the test compound with a GPR17, or a functional GPR17 fragment in the presence of a suitable amount of a GPR17 agonist of formula I.Type: ApplicationFiled: February 28, 2012Publication date: March 7, 2013Applicant: RHEINISCHE FRIEDRICH-WILHELMS-UNIVERSITAT BONNInventors: Evi Kostenis, Andreas Spinrath, Stephanie Hennen, Lucas Peters, Christa E. Müller, Rhalid Akkari, Younis Baqi, Kirsten Ritter
-
Patent number: 8367665Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.Type: GrantFiled: April 16, 2009Date of Patent: February 5, 2013Assignee: Karo Bio ABInventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
-
Patent number: 8367664Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: January 23, 2007Date of Patent: February 5, 2013Assignee: Allergan, Inc.Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
-
Patent number: 8350055Abstract: The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6, and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.Type: GrantFiled: July 20, 2010Date of Patent: January 8, 2013Assignee: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Hornberger, Herve Geneste, Daryl Richard Sauer, Wolfgang Wernet, Andrea Hager-Wernet, legal representative, Liliane Unger, Wilfried Lubisch
-
Publication number: 20130001540Abstract: Disclosed are a compound including an indole derivative in which two tertiary amines are substituted, an organic electronic element using the same, and a terminal thereof.Type: ApplicationFiled: March 9, 2011Publication date: January 3, 2013Applicant: DUKSAN HIGH METAL CO., LTD.Inventors: Dongha Kim, Jungcheol Park, Jinuk Ju, Jangyeol Baek, Wonsam Kim, Eunkyung Kim, Daehyuk Choi, Junghwan Park
-
Publication number: 20120322808Abstract: The present invention relates to novel ?4?2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them. The present invention relates to novel ?4?2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them.Type: ApplicationFiled: May 3, 2010Publication date: December 20, 2012Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Kana Ram Kumawat, Ishtiyaque Ahmad, Pradeep Jayarajan, Anil Karbhari Shinde, Nagaraj Vishwottam Kandikere, Koteshwara Mudigonda, Venkateswarlu Jasti
-
Publication number: 20120316171Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.Type: ApplicationFiled: November 4, 2010Publication date: December 13, 2012Inventor: Tamas Oravecz
-
Publication number: 20120252836Abstract: The present invention relates to compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.Type: ApplicationFiled: June 18, 2012Publication date: October 4, 2012Applicant: EVOLVA SAInventors: Alexandra Santana Sorensen, Jean-Phillippe Meyer, Peteris Alberts, Mainkar Prathama
-
Patent number: 8268803Abstract: The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: GrantFiled: December 17, 2007Date of Patent: September 18, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Frank Bennett, Srikanth Venkatraman, F. George Njoroge, Kevin X. Chen, Neng-Yang Shih, Stuart B. Rosenblum, Joseph A. Kozlowski
-
Publication number: 20120220782Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.Type: ApplicationFiled: April 30, 2012Publication date: August 30, 2012Inventors: Ulrich BERENS, Oliver DOSENBACH, Daniel SPRENGER
-
Publication number: 20120202861Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined in the specification.Type: ApplicationFiled: October 6, 2010Publication date: August 9, 2012Applicant: KARO BIO ABInventors: Mattias Wennerstål, Patrik Rhönnstad, Aiping Cheng, Sandra Gordon, Theresa Apelqvist, Lars Hagberg
-
Publication number: 20120184582Abstract: The present invention relates to novel compounds which are effective as an inhibitor for xanthine oxidase, a process for preparing the same, and a pharmaceutical composition comprising a therapeutically effective amount of the same.Type: ApplicationFiled: October 4, 2010Publication date: July 19, 2012Inventors: Jeong Uk Song, Geun Tae Kim, Sung Pil Choi, Cheol Kyu Jung, Deok Seong Park, Eun Sil Choi, Tae Hun Kim, Hyun Jung Park, Wan Su Park, Heui Sul Park, Ki Chul Koo, Vasily Artemov
-
Patent number: 8222279Abstract: Compounds of Formula I are described along with pharmaceutical formulations thereof, and methods of treating disorders such as diabetes and neurodegenerative diseases with such compounds.Type: GrantFiled: October 11, 2010Date of Patent: July 17, 2012Assignee: Duke UniversityInventor: Michael C. Pirrung
-
Publication number: 20120178764Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.Type: ApplicationFiled: January 5, 2012Publication date: July 12, 2012Inventors: Roger Bonnert, Rukhsana (née RASUL, Rukhsana) Mohammed, Mark Robert Dickinson
-
Publication number: 20120129100Abstract: An actinic ray-sensitive or radiation-sensitive resin composition including: (PA) a compound having a proton acceptor functional group and undergoing decomposition upon irradiation with an actinic ray or radiation to generate a compound reduced in or deprived of proton acceptor property or changed to be acidic from being proton acceptor-functioning, wherein a molar extinction coefficient ? of the compound (PA) at a wavelength of 193 nm as measured in acetonitrile solvent is 55,000 or less, and a pattern forming method using the composition are provided.Type: ApplicationFiled: August 17, 2010Publication date: May 24, 2012Applicant: FUJIFILM CORPORATIONInventors: Akinori Shibuya, Shuhei Yamaguchi, Shohei Kataoka, Michihiro Shirakawa, Takayuki Kato, Naohiro Tango
-
Publication number: 20120122839Abstract: The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (I) or (Ia) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (I) or (Ia) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.Type: ApplicationFiled: January 17, 2012Publication date: May 17, 2012Applicant: Priaxon AGInventors: Christoph BURDACK, Cedric Kalinski, Vladimir Khazak, Gunther Ross, Lutz Weber
-
Publication number: 20120122931Abstract: A compound represented by the general formula (I) of the present invention, which has an EP1 receptor antagonism: [wherein A represents a benzene ring or the like; Y represents a C1-6 alkylene group or the like; RN represents a hydrogen atom or a C1-6 alkyl group; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic group which may have a substituent, a 6-membered aromatic heterocyclic group which may have a substituent or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.Type: ApplicationFiled: July 26, 2010Publication date: May 17, 2012Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Tatsuhiro Kondo, Atsushi Kondo, Kazuya Tatani, Naohiro Kawamura
-
Publication number: 20120115842Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein substituents A, B, X and Y are defined as in claim 1, medicaments containing said derivatives, and the use thereof in the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.Type: ApplicationFiled: December 30, 2005Publication date: May 10, 2012Inventors: Wilfried Lubisch, Thorsten Oost, Liliane Unger, Wilfried Hornberger, Herve Geneste
-
Patent number: 8168672Abstract: Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.Type: GrantFiled: February 2, 2010Date of Patent: May 1, 2012Assignee: WyethInventor: Bogdan Kazimierz Wilk
-
Publication number: 20120101196Abstract: There are provided a novel diarylamine compound represented by the following formula (I), (II) or (III), which has at least one signal attributable to the hydrogen of the N—H moiety at 8.30 ppm to 9.00 ppm when a deuterated dimethyl sulfoxide solution of the diarylamine compound is analyzed by 1H-NMR; and an aging inhibitor, a polymer composition, a crosslinked rubber product and a molded article thereof, and a method of producing a diarylamine compound. In the formulas, A1 to A6 each represent an aromatic group which may have a substituent; A represents an aromatic group or a cyclic aliphatic group, which may both have a substituent; L represents 1 or 2; and n represents 0 or 1.Type: ApplicationFiled: June 30, 2010Publication date: April 26, 2012Inventors: Kei Sakamoto, Tomonori Ogawa, Satoshi Kiriki, Masanobu Shinohara, Yasushi Nakano
-
Publication number: 20120083495Abstract: Compounds useful for the treatment of spinal muscular atrophy or other uses, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced by mutation or frameshift.Type: ApplicationFiled: December 5, 2011Publication date: April 5, 2012Applicants: SCIENCE APPLICATIONS INTERNATIONAL INC. (SAIC), ALBANY MOLECULAR RESEARCH, INC., DEPARTMENT OF HEALTH AND HUMAN SERVICESInventors: Jill Heemskerk, Keith D. Barnes, John M. McCall, Graham Johnson, David Fairfax, Matthew Robert Johnson
-
Publication number: 20120040958Abstract: The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
-
Patent number: 8114901Abstract: The present invention relates to crystalline 2,5-dione-3-(1-methyl-1H-indol-3-yl)-4-[1-(pyridin-2-yl-methyl)piperidin-4-yl]-1H-indol-3-yl]-1H-pyrrole mono-hydrochloride salt, a pharmaceutical formulation containing said salt and to methods for treating cancer and for inhibiting tumor growth using said salt.Type: GrantFiled: July 8, 2003Date of Patent: February 14, 2012Assignee: Eli Lilly and CompanyInventors: Julie Kay Bush, Margaret Mary Faul, Susan Marie Reutzel-Edens
-
Publication number: 20120028990Abstract: A 3-aryl or heteroaryl-substituted indole derivative which is effective as a preventive or remedy for various diseases is provided. [Means for Resolution] A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof is provided. In the formula, R1 represents a hydrogen atom, C1-6 alkyl et al; R2 represents a hydrogen atom, C1-6 alkyl et al; Z represents aryl or heteroaryl (with the proviso that imidazolyl is excluded); and W represents a group represented by the formula (w-1) or (w-2). In the formula, R3 represents C1-6 alkyl et al; Yl and Y2 both represent a hydrogen atom or Y1 and Y2 together form —CH2-CH2-; Q represents CH or N; Ar represents phenyl, furyl et al; R4 and R5 each independently represent a hydrogen atom or C1-6 alkyl or R4 and R5 together with the nitrogen atom form pyrrolidine et al.Type: ApplicationFiled: April 14, 2010Publication date: February 2, 2012Inventors: Takashi Fujimura, Hiroyuki Kishino, Takashi Mizutani, Shunji Sakuraba, Takahide Sasaki, Nagaaki Sato
-
Patent number: 8106052Abstract: The present invention provides methods, compositions, substrates, and kits useful for analyzing the metabolic activity in cells, tissue, and animals and for screening test compounds for their effect on cytochrome P450 activity. In particular, a one-step and two-step methods using luminogenic molecules, e.g. luciferin or coelenterazines, that are cytochrome P450 substrates and that are also bioluminescent enzyme, e.g., luciferase, pro-substrates are provided. Upon addition of the luciferin derivative or other luminogenic molecule into a P450 reaction, the P450 enzyme metabolizes the molecule into a bioluminescent enzyme substrate, e.g., luciferin and/or luciferin derivative metabolite, in a P450 reaction. The resulting metabolite(s) serves as a substrate of the bioluminescent enzyme, e.g., luciferase, in a second light-generating reaction. Luminescent cytochrome P450 assays with low background signals and high sensitivity are disclosed and isoform selectivity is demonstrated.Type: GrantFiled: April 5, 2010Date of Patent: January 31, 2012Assignee: Promega CorporationInventors: James J. Cali, Dieter Klaubert, William Daily, Samuel Kin Sang Ho, Susan Frackman, Erika Hawkins, Keith V. Wood
-
Patent number: 8097645Abstract: Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-? signaling are described.Type: GrantFiled: October 10, 2008Date of Patent: January 17, 2012Assignees: The Board of Trustees of the Leland Stanford Junior University, SRI InternationalInventors: Anton Wyss-Coray, Mary J. Tanga
-
Patent number: 8071584Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: GrantFiled: March 20, 2008Date of Patent: December 6, 2011Assignee: GlaxoSmithKline LLCInventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
-
Publication number: 20110275689Abstract: The present invention relates to novel intermediates and further to the use of said intermediates in processes for the preparation of indolinone derivatives, in particular 3-pyrrole substituted 2-indolinones having amide moieties on the pyrrole ring. Such compounds are useful in die treatment of abnormal cell growth, such as cancer, in mammals.Type: ApplicationFiled: July 1, 2009Publication date: November 10, 2011Applicant: GENERICS [UK] LIMITEDInventors: Abhay Gaitonde, Bharati Choudhari, Prakash Bansode, Sunanda Phadtare
-
Publication number: 20110269668Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.Type: ApplicationFiled: October 13, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alexander Heim-Riether, Shuang Liang, Sabine Schlyer
-
Publication number: 20110265878Abstract: The present invention relates to a dye comprising a chromophore to which an acyloin group as anchoring group is attached, to a method of synthesis of such dye, to an electronic device comprising such dye and to the use of such dye.Type: ApplicationFiled: September 23, 2009Publication date: November 3, 2011Applicant: Sony CorporationInventors: Gerda Fuhrmann, Gabriele Nelles, Ameneh Bamedi Zilai, Markus Obermaier
-
Publication number: 20110263614Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.Type: ApplicationFiled: March 14, 2011Publication date: October 27, 2011Inventors: Roger Bonnert, Rukhsana Mohammed, Mark Robert Dickinson
-
Patent number: 8044103Abstract: The present invention provides 4-substituted-2-azetidinone compounds, bicyclic 2-5-diketopiperazine compounds, and pharmaceutical compositions thereof that are potent, safe and effective neuroprotective agents. Due to their strong central nervous system (CNS) activity, the compounds can be used to enhance memory and to treat a variety of neurological disorders. The compounds are particularly useful for treating neurological disorders caused by, or associated with, CNS trauma.Type: GrantFiled: February 22, 2007Date of Patent: October 25, 2011Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Alan I. Faden, Gian Luca Araldi
-
Patent number: 8030499Abstract: It is intended to provide a drug which is efficacious against pathological conditions relating to arginine-vasopressin V1b receptor. More particularly speaking, it is intended to provide a drug which has a therapeutic or preventive effect on depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug addiction, epilepsy, brain infarction, brain ischemia, brain edema, head injury, inflammation, immune diseases, alopecia and so on. As the results of intensive studies, a novel 1,3-dihydro-2H-indol-2-one compound and a pyrrolidin-2-one compound fused with a heteroaromatic ring, which are highly selective antagonists of arginine-vasopressin V1b receptor, have high metabolic stabilities and show favorable brain penetration and high plasma concentrations, are found, thereby achieving the above objective.Type: GrantFiled: January 30, 2006Date of Patent: October 4, 2011Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Yoshinori Sekiguchi, Takeshi Kuwada, Masato Hayashi, Dai Nozawa, Yuri Amada, Tsuyoshi Shibata, Shuji Yamamoto, Hiroshi Ohta, Taketoshi Okubo, Takeshi Koami
-
Patent number: 8008339Abstract: The invention relates to a compound of formula (I), or a pharmacologically or cosmetically acceptable salt or derivative thereof, wherein R1 to R5 are selected from the groups R1 representing -alkyl, -vinyl, —CHOH—CH2OH, R2 representing H, —OH, —Oalkyl, —Oacyl, saccharide groups, modified saccharide groups (e.g. malonylated), R3 representing —H, —OH, —Oalkyl, —Oacyl, modified —Oacyl (e.g. malonylated), saccharide groups, modified saccharide groups (e.g. malonylated), R4, R5 representing —COOH, -carbonic esters, for use as drug, antioxidant, food supplement. The invention also relates to a method for producing the compound of formula (I).Type: GrantFiled: March 11, 2008Date of Patent: August 30, 2011Assignee: Leopold-Franzens-Universitat InnsbruckInventors: Bernhard Kräutler, Thomas Müller
-
Patent number: 8008491Abstract: The present invention relates to a series of substituted aza-indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.Type: GrantFiled: June 17, 2008Date of Patent: August 30, 2011Assignee: Aventis Pharmaceuticals, Inc.Inventors: John Ziqi Jiang, Jack Roger Koehl, Shujaath Mehdi, Neil Moorcroft, Kwon Yon Musick, Philip Marvin Weintraub, Paul Robert Eastwood
-
Patent number: 8008299Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: GrantFiled: June 5, 2008Date of Patent: August 30, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
-
Publication number: 20110207941Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.Type: ApplicationFiled: May 2, 2011Publication date: August 25, 2011Inventors: ULRICH BERENS, OLIVER DOSENBACH, DANIEL SPRENGER
-
Publication number: 20110201555Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 , R10 and R11 are as defined in the specification.Type: ApplicationFiled: September 18, 2009Publication date: August 18, 2011Inventors: Patrik Rhönnstad, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng, Sandra Gordon
-
Publication number: 20110190294Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.Type: ApplicationFiled: April 16, 2009Publication date: August 4, 2011Inventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
-
Publication number: 20110166159Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: March 17, 2011Publication date: July 7, 2011Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
-
Publication number: 20110144103Abstract: The present invention relates to substituted pyrrole compounds and compositions comprising substituted pyrrole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted pyrrole compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: June 4, 2009Publication date: June 16, 2011Inventors: Dinesh U. Chimmanamada, Weiwen Ying
-
Publication number: 20110144090Abstract: Indole compounds are disclosed. Also disclosed are methods for using the compounds to treat human and animal disease, pharmaceutical compositions of the compounds, and kits including the compounds.Type: ApplicationFiled: August 10, 2010Publication date: June 16, 2011Inventors: Amy Elder, Geraldine Harriman, Silvana Leit, Jie Li, Howard Sard, Yiliang Zhang, Doug Wilson
-
Publication number: 20110136794Abstract: A compound represented by the following formula (1) or a salt thereof: The compound has an inhibitory activity on the production of interleukin-6, and is therefore useful as a preventive and/or therapeutic agent for a disease associated with interleukin-6, ocular inflammatory diseases and the like. In the formula, R1 represents a halogen atom, a hydrogen atom, a lower alkyl group which may have a substituent, a formyl group, or a lower alkylcarbonyl group which may have a substituent, R2 represents a bicyclic hydrocarbon group which may have a substituent or a bicyclic heterocyclic group which may have a substituent, R3 represents a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, or an acyl group.Type: ApplicationFiled: August 25, 2009Publication date: June 9, 2011Inventors: Kenji Kawashima, Noriko Kawashima, Hiroshi Enomoto, Minoru Yamamoto, Massaaki Murai
-
Patent number: 7956049Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1a, R1b, R1c, Q, A, R3, W, D and R2 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.Type: GrantFiled: May 15, 2009Date of Patent: June 7, 2011Assignee: Bristol-Myers Squibb CompanyInventor: Guohua Zhao
-
Patent number: 7951940Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.Type: GrantFiled: March 13, 2008Date of Patent: May 31, 2011Assignee: NeurAxon, Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi