Abstract: Compounds represented by the formulas wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.
Abstract: Disclosed are nitroxide modified NSAID compounds of the formula (I) or a pharmaceutically acceptable salt or enantiomer thereof: in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and n are defined herein and pharmaceutical compositions thereof. Further disclosed is a method of treating or preventing various disorders, such as inflammation, cancer, diabetes, a cardiovascular disorder, weight gain, polyps, and/or chronic pain, in a patient comprising administering an effective amount of a compound or pharmaceutically acceptable salt or enantiomer of formula (I). A method of imaging the compound or pharmaceutically acceptable salt or enantiomer of formula (I) in the body of the animal is also provided.
Type:
Application
Filed:
April 5, 2012
Publication date:
October 18, 2012
Applicants:
Wake Forest University, and Human Services
Inventors:
David A. Wink, Wilmarie Flores-Santana, S. Bruce King, Murali Krishna Cherukuri, James B. Mitchell
Abstract: Substituted 2-(2,6-dioxopiperidin-3-yl)phthalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl)isoindolines are disclosed. The compounds are useful, for example, in reducing the levels of TNF? in a mammal.
Type:
Grant
Filed:
December 10, 2009
Date of Patent:
October 16, 2012
Assignee:
Celgene Corporation
Inventors:
George W. Muller, David I. Stirling, Roger Shen-Chu Chen
Abstract: The present application describes deuterium-enriched lenalidomide, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
Abstract: The invention provides a combination comprising an Hsp90 inhibitor compound of the formula (VII): or tautomer or salt thereof and one or more therapeutic agents selected from topoisomerase I inhibitors; antimetabolites; tubulin targeting agents; DNA binder and topoisomerase II inhibitors; alkylating agents; monoclonal antibodies; anti-hormones; signal transduction inhibitors; proteasome inhibitors; DNA methyl transferases; cytokines; retinoids and HDAC or HAT modulators.
Type:
Application
Filed:
October 12, 2011
Publication date:
October 4, 2012
Inventors:
Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueron Navarro, Alison Jo-Anne Woolford
Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of arboviruses.
Type:
Application
Filed:
March 19, 2012
Publication date:
October 4, 2012
Applicant:
THE REGENTS OF THE UNIVERSITY OF MICHIGAN
Inventors:
Scott Larsen, Janice Sindac, Scott Barraza, David J. Miller
Abstract: The present application describes 2-(2?,6?-dioxo-3?-deutero-piperidin-3?-yl)isoindoles, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
Abstract: Ezatiostat is useful for inhibiting multiple myeloma cell proliferation and treating multiple myeloma, alone or when added together with another anti-myeloma drug.
Abstract: The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.
Type:
Application
Filed:
June 11, 2012
Publication date:
October 4, 2012
Inventors:
Soon Ha KIM, Hyoung Jin Kim, Sun Young Koo, Sung Bae Lee, Heui Sul Park, Seung Hyun Yoon, Seung Yup Paek, Hyo Shin Kwak, Dong Ook Seo, Eok Park
Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.
Type:
Application
Filed:
July 2, 2010
Publication date:
October 4, 2012
Inventors:
Alan Kozikowski, Kyle V. Butler, Jay H. Kalin
Abstract: There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating, diseases utilizing pharmaceutical compositions comprising these compounds.
Type:
Application
Filed:
July 6, 2010
Publication date:
September 27, 2012
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Gianluca Mariano Enrico Papeo, Alina Anatolievna Busel, Alexander Khvat, Mikhail Yurievitch Krasavin, Barbara Forte, Fabio Zuccotto
Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
Abstract: There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
Type:
Application
Filed:
July 6, 2010
Publication date:
September 27, 2012
Applicant:
NERVIANO MEDICAL SCIENCES S.r.l.
Inventors:
Gianluca Mariano Enrico Papeo, Alina Anatolievna Busel, Elena Casale, Alexander Khvat, Mikhail Yurievitch Krasavin, Paolo Orsini, Helena Posteri, Alessandra Scolaro
Abstract: The present invention discloses and claims a series of substituted indolyl-piperidinyl benzylamines of the formula wherein R1, R2, R4 and R5 are as described herein. More specifically, the compounds of this invention are inhibitors of ?-tryptase and are, therefore, useful as pharmaceutical agents. Additionally, this invention also discloses methods of preparation of substituted indolyl-piperidinyl benzylamines.
Type:
Application
Filed:
June 5, 2012
Publication date:
September 27, 2012
Applicant:
SANOFI
Inventors:
Yong Mi CHOI-SLEDESKI, Guyan LIANG, Thaddeus R. NIEDUZAK, Gregory B. POLI, Patrick Wai-Kwok SHUM, Gregory T. STOKLOSA, Zhicheng ZHAO
Abstract: The present invention relates to substituted 2-amino-N-(4-fluoro-3-{1-[1-(alkyl)-1H-indole-3-carbonyl]-piperidin-4-yl}-benzyl)-acetamides (compounds of formula I) compositions thereof, and their use in the treatment of inflammatory diseases.
Abstract: The present invention relates to compounds having pharmacological activity towards the sigma (?) receptor, and more particularly to some 4, 5, 6, 7 tetrahydrobenzo[b]thiophene derivatives, wherein n is selected from 0, 1, 2, 3 or 4; m is selected from 0, 1 or 2; the dotted line represents either a single or a double bond; to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.
Type:
Application
Filed:
May 30, 2012
Publication date:
September 20, 2012
Applicant:
LABORATORIOS DEL DR. ESTEVE, S.A.
Inventors:
Jordi CORBERA-ARJONA, Daniel MARTINEZ-OLMO, David VANO-DOMENECH
Abstract: The present invention relates to a method for the treatment of an inflammatory bowel disease by the administration of the compound [4-(5-aminomethyl-2-fluorophenyl)piperidine-1-yl][7-fluoro-1-(2-methoxyethyl)-4-trifluoromethoxy-1H-indol-3-yl]methanone, which may be represented as Formula I: or a corresponding N-oxide, prodrug, pharmaceutically acceptable salt or solvate thereof.
Type:
Application
Filed:
June 5, 2012
Publication date:
September 20, 2012
Applicant:
SANOFI
Inventors:
Anne MINNICH, Eszter BEKASI, Yong Mi CHOI-SLEDESKI
Abstract: The present invention relates to drug delivery systems comprising ocular implant, which include organic molecules, capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation, in combination with a polymer, which polymer serves to control, modify, modulate and/or slow the release of the therapeutic component into the environment of the eye in which said composite is placed.
Type:
Application
Filed:
February 26, 2009
Publication date:
September 20, 2012
Inventors:
Lon T. Spada, Jane Guo Shiah, Patrick Hughes, Thomas C. Malone, Gerald W. DeVries, Jeffrey L. Edelman, Julie A. Wurster, Xialing Guo, Sougato Boral
Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.
Type:
Application
Filed:
December 22, 2011
Publication date:
September 20, 2012
Applicants:
Cephalon France, Cephalon, Inc.
Inventors:
Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek D. Dunn, Greg A. Hostetler, Robert L. Hudkins, Brigitte Lesur, Babu G. Sundar, Allizon L. Zulli, Christophe Yue
Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
Type:
Application
Filed:
May 17, 2012
Publication date:
September 13, 2012
Applicant:
THERAVANCE, INC.
Inventors:
Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
Abstract: Compounds derived from indole, notably useful in therapeutics, selected from: i) the compounds of formula: and ii) the pharmaceutically acceptable salts of the compounds of formula (I); in which R1, R2, R3, R4, R5, R6, R8, R9 and Cy have defined meanings, and the use of such compounds in pharmaceuticals for the treatment of neurodegenerative diseases, particularly Parkinson's disease.
Type:
Application
Filed:
March 9, 2012
Publication date:
September 13, 2012
Applicant:
Laboratoires Fournier SA
Inventors:
Jerome Amaudrut, Benaissa Boubia, Maria Johanna Petronella Van Dongen, Fabrice Guillier, Olivia Poupardin-Olivier
Abstract: The present invention relates to methods of treating or preventing emesis and improving a subject's ASAS score by administering to the subject an effective amount of a growth hormone secretagogue compound or a pharmaceutically acceptable salt, hydrate or solvate thereof.
Abstract: A method for treating an autism spectrum condition includes administering an effective dose of a TNF-? inhibiting agent to a person having an autism spectrum condition or pervasive development disorder and at least one of elevated TNF-? in the cerebrospinal fluid or elevated TNF-? in the serum, as compared to normal conditions; and lowering at least one of the elevated TNF-? in the cerebrospinal fluid or elevated TNF-? in the serum. A TNF-? inhibiting agent includes at least one of Lenalinomide; Thalidomide; L-Carnosine; Infliximab; Etanercept; a stem cell preparation; derivatives thereof, isomers thereof, or pharmaceutically acceptable salts thereof.
Abstract: Melanocortin receptor-specific compounds of formula I below: wherein the variables are as defined in the specification, and enantiomers, diastereomers and pharmaceutically acceptable salts thereof. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders.
Type:
Grant
Filed:
March 29, 2011
Date of Patent:
September 11, 2012
Assignee:
Palatin Technologies, Inc.
Inventors:
Yi-Qun Shi, John H. Dodd, Elizabeth G. Rowley, Gary L. Olson, Axel Metzger
Abstract: The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.
Type:
Application
Filed:
May 8, 2012
Publication date:
August 30, 2012
Applicant:
Wyeth LLC
Inventors:
Andrew Fensome, Gary S. Grubb, Diane Deborah Harrison, Richard Craig Winneker
Abstract: The present invention provides compounds which show high effectiveness against positive symptoms, negative symptoms and cognitive dysfunction in schizophrenia and reduce conventional side-effect risks as well as have remarkable effects for central neurological diseases associated with cognitive dysfunction other than schizophrenia. N-Acyl cyclic amine derivatives of formula (1): wherein Ar1 and Ar2 are aryl or heteroaryl; V is nitrogen, or CR3; W1 is a single bond, —C(O)—, etc.; W2 is C1-alkylene; W3 is a single bond, methylene, —NH—, —CR4?CR5—, etc.; Ring Q is a group of formula (a) in which n is 0 or 1; m is 0 to 2; k is 1 to 3; Z is a single bond, methylene, oxygen, etc.; R1a, R1b and R1c are each, same or different, hydrogen, hydroxyl, halogen, cyano, C1-6 alkyl, etc.; or pharmaceutically acceptable salts thereof are provided.
Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.
Type:
Application
Filed:
April 30, 2012
Publication date:
August 23, 2012
Inventors:
Bruce E Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
Abstract: The present invention provides novel indanone derivatives which can be advantageously used for treating and/or preventing of a medical condition for which inhibition of a cholinesterase is desired.
Abstract: Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS.
Type:
Application
Filed:
August 4, 2011
Publication date:
August 9, 2012
Inventors:
Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
Abstract: Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic.
Type:
Application
Filed:
January 10, 2012
Publication date:
August 9, 2012
Applicant:
CHARLESTON LABORATORIES, INC.
Inventors:
Paul Bosse, John Ameling, Bernard Schachtel, Ray Takigiku
Abstract: The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
Type:
Grant
Filed:
March 14, 2008
Date of Patent:
July 31, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
Abstract: The present invention relates to pharmaceutical compositions for the treatment of cancer and especially for the treatment of hematological malignancies such as multiple myeloma. Specifically, the present invention relates to pharmaceutical composition for the treatment of cancer comprising: thalidomide, or a derivative thereof, or salts or solvates thereof; one or more artemisinin compounds, or salts or solvates thereof; and one or more pharmaceutically acceptable carriers and/or excipients.
Abstract: The present invention relates to acid addition salts of lenalidomide, wherein said acid has a pKa lower than 1, preferably selected from hydrochloric acid, hydrobromic acid, methane sulfonic acid, ethane sulfonic acid, benzene sulfonic acid and p-toluenesulfonic acid, to processes for their making, and use in medicine, and to purification of lenalidomide base.
Abstract: A method is provided for the prevention of cancer metastasis in a patient comprising administering an adrenergic receptor antagonist to a patient in need thereof. The invention also includes an adrenergic receptor antagonist for use in the prevention of tumour recurrence in a patient. Also provided is a kit of parts for use in such methods comprising an adrenergic receptor antagonist, and an administration vehicle. A method is further included for identifying a patient at risk of developing cancer comprising the step of assaying for levels of expression of adrenergic receptor genes and proteins in said patient.
Type:
Application
Filed:
December 8, 2011
Publication date:
July 12, 2012
Applicant:
NOTTINGHAM UNIVERSITY HOSPITALS NHS TRUST
Abstract: The present invention is directed to an indole benzylamine compound of formula I: useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
February 16, 2011
Date of Patent:
July 10, 2012
Assignee:
Sanofi
Inventors:
Yong Mi Choi-Sledeski, Nakyen Choy, Gregory Bernard Poli, John J. Shay, Jr., Patrick Wai-Kwok Shum, Adam W. Sledeski
Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
Type:
Grant
Filed:
June 18, 2009
Date of Patent:
July 10, 2012
Assignee:
Glaxo Group Limited
Inventors:
Jose Luis Castro Pineiro, Xichen Lin, Qian Liu, Kevin Meng, Feng Ren, David R Vesey, Baowei Zhao
Abstract: A method for treating cancer, preventing cancer or delaying the progression of a cancer in an animal or human comprising the step of: administering to the animal or the human having a cancer a composition in an amount effective to treat cancer, prevent cancer or delay the progression of cancer in the animal or the human. The composition comprises a pharmaceutically acceptable excipient, and ascorbate which is joined to a carrier structure containing an anti-cancer active agent, said carrier structure being capable of releasing the anti-cancer agent in the presence of a reactive oxygen species.
Abstract: This invention provides compounds of formula (I): wherein R1, R2, X, p, q, m, n, and Ring C have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
Type:
Application
Filed:
December 14, 2011
Publication date:
June 21, 2012
Inventors:
Ralph New Harris, III, David Bruce Repke, Keith A.M. Walker
Abstract: The invention concerns the use of azabicycloalkyl derivatives or pyrrolidine-2-one derivatives for the treatment, prevention or delay of progression of ataxia.
Abstract: The present application discloses compounds of the formula: and pharmaceutical compositions containing same and their use for treating and preventing various pathologies, including obesity, appetite disorders, excess weight and diabetes.
Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
Abstract: Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease.
Type:
Application
Filed:
August 11, 2010
Publication date:
June 7, 2012
Inventors:
Niall Anderson, Ann M. Bullion, Neysa Nevins, Michael R. Palovich, Steven L. Sollis, Michael D. Wall, Jakob Busch-Petersen, Brian Evans, Huijie Li
Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
Type:
Application
Filed:
November 30, 2011
Publication date:
June 7, 2012
Inventors:
James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui, Xuqing Zhang
Abstract: The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (I): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of —X1?X2—X3?X4— is a formula of —C(R1)?C(R2)—C(R3)?C(R4)— etc.; X5 is C(R5) or N; R1, R2, R3, R4 and R5 is independently a hydrogen atom, a halogen atom etc; R6 is a formula of —Z—R10 etc. wherein Z is alkylene etc., and R10 is carboxy etc.; R7 is optionally substituted alkyloxy etc.; R8 is independently a halogen atom etc.; R9 is independently optionally substituted alkyl etc.; Y is a single bond etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or a solvate thereof.
Abstract: The invention refers to the use of a sigma ligand of formula (I) to prevent or treat pain induced by a chemotherapeutic agent, especially pain induced by taxanes, vinca alkaloids or platinum-containing chemotherapeutic drugs.
Type:
Application
Filed:
August 12, 2010
Publication date:
June 7, 2012
Inventors:
José Manuel Baeyens-Cabrera, Helmut Heinrich Buschmann, José Miguel Vela Hernández, Daniel Zamanillo-Castanedo, Francisco-Rafael Nieto-López
Abstract: The present invention extends to a compound of formula I: or a pharmaceutically acceptable salt of said compound, or a pharmaceutical composition comprising the compound of formula I and a pharmaceutically acceptable carrier. The invention is also directed to the use of a compound of formula I as an inhibitor of tryptase and for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by an inhibitor of tryptase. The invention further includes methods for the preparation of a compound of formula I.
Type:
Application
Filed:
February 14, 2012
Publication date:
June 7, 2012
Applicant:
SANOFI
Inventors:
Yong- Mi CHOI-SLEDESKI, Charles J. GARDNER, Guyan LIANG, Gregory B. POLI, Patrick Wai-Kwok SHUM, Grzegory T. STOKLOSA, Zhicheng ZHAO