At Least Three Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 548/359.5)
-
Publication number: 20150141455Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: June 27, 2013Publication date: May 21, 2015Applicant: NOVARTIS AGInventors: Eva Altmann, Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Jean Quancard, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
-
Patent number: 8946279Abstract: The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy and n are as presented in the description.Type: GrantFiled: August 18, 2011Date of Patent: February 3, 2015Assignee: KBP Biosciences Co., Ltd.Inventors: Zhenhua Huang, Jinyuan Wang, Dedong Zhang
-
Publication number: 20140343294Abstract: Compounds of formula (I): wherein: A, R, T, Q, L, Z, G, X and A? are as defined in the description. B and D, equal to or different from each other, are selected between heteroaryl and aryl, wherein at least one of the hydrogen atoms of said heteroaryl and aryl are substituted with groups selected from SO3?, SO3H, COO?, COOH, and one or more of the other hydrogen atoms of said heteroaryl and aryl are optionally substituted as reported in the description.Type: ApplicationFiled: April 10, 2014Publication date: November 20, 2014Inventors: Paolo LAZZARI, Matteo ZANDA, Monica SANI
-
Patent number: 8853207Abstract: The present invention relates to a compound of formula (I): or hydrates, solvates, prodrugs, or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, ring A, R3 and R4 are as defined in the detailed description and claims. The compound of formula (I) are receptor tyrosine kinase (RTK) inhibitors and have efficacy for the treatment, prevention, or amelioration of RTK-related diseases.Type: GrantFiled: April 12, 2012Date of Patent: October 7, 2014Assignee: Development Center for BiotechnologyInventors: Chu-Bin Liao, Chao-Cheng Chiang, Huei-Ru Yang, Yuan-Chun Liao, Paonien Chen
-
Patent number: 8697744Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, Y, Z1, Z2, Z3, M and (A)m are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: GrantFiled: January 12, 2010Date of Patent: April 15, 2014Assignee: Addex Pharma S.A.Inventors: Christelle Boléa, Sylvain Celanire
-
Publication number: 20130274255Abstract: The present invention relates to a compound of formula (I): or hydrates, solvates, prodrugs, or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, ring A, R3 and R4 are as defined in the detailed description and claims. The compound of formula (I) are receptor tyrosine kinase (RTK) inhibitors and have efficacy for the treatment, prevention, or amelioration of RTK-related diseases.Type: ApplicationFiled: April 12, 2012Publication date: October 17, 2013Applicant: DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Chu-Bin LIAO, Chao-Cheng CHIANG, Huei-Ru YANG, Yuan-Chun LIAO, Paonien CHEN
-
Publication number: 20130177529Abstract: Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.Type: ApplicationFiled: November 15, 2012Publication date: July 11, 2013Inventors: Youhong Hu, Bin Xu, Yun Liao, Kenneth Nawoschik, Yixin Liu, Anthony Sandrasagra, Reza Fathi, Zhen Yang
-
Patent number: 8481585Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.Type: GrantFiled: September 13, 2012Date of Patent: July 9, 2013Assignee: Nerviano Medical Sciences S.R.L.Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
-
Publication number: 20130158024Abstract: The present invention features compounds, pharmaceutical compositions, and methods for treating trauma, ischemia, stroke, degenerative diseases associated with cellular necrosis, and other conditions. Screening assays for identifying compounds useful for treating these conditions are also described.Type: ApplicationFiled: October 31, 2012Publication date: June 20, 2013Inventors: Junying Yuan, Alexei Degterev, Junichi Hitomi, Gregory D. Cuny, Prakash Jagtap
-
Patent number: 8426438Abstract: The present invention is directed to heterocyclic fused pyrazole[4,3-c]pyridine-3-one compounds of formula (I): which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: September 20, 2010Date of Patent: April 23, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Douglas C. Beshore, Scott D. Kuduk
-
Publication number: 20130017149Abstract: Condensed tricyclic compounds having a condensed structure containing one phenyl and one pyrazole ring linked with each other by a central ring comprising from five to eight atoms, having affinity for the CB1 and/or CB2 receptors, with central nervous system and/or peripheral activity, of formula (I): wherein the various substituents are as defined in the description. The compounds show affinity for the CB1 and/or CB2 cannabinoidergic receptors.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna, Luca Pani
-
Publication number: 20120253036Abstract: An agent for treating fibromyalgia containing a 5-HT2C receptor agonist as an active ingredientType: ApplicationFiled: December 10, 2010Publication date: October 4, 2012Inventors: Yukinori Nagakura, Mina Tsukamoto, Tomonari Watabiki
-
Publication number: 20120238541Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: September 17, 2010Publication date: September 20, 2012Applicant: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
-
Patent number: 8232393Abstract: An electron transport material based on fused aromatic electron-deficient compounds. The accumulation of aromatic rings with an electron deficiency allows free-radical anions to be stabilized very efficiently in these systems.Type: GrantFiled: July 3, 2007Date of Patent: July 31, 2012Assignee: OSRAM Opto Semiconductors GmbHInventors: Jürgen Adler, Andreas Kanitz
-
Patent number: 8207180Abstract: The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, means either simple or double carbon-carbon bond and R1, R2 and R3 are as defined in the specification. Further objects of the invention are a process for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Cdc7 and AKT kinase activity, like cancer.Type: GrantFiled: November 23, 2007Date of Patent: June 26, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Ermes Vanotti, Marina Caldarelli, Francesco Casuscelli, Barbara Forte, Maria Menichincheri, Alessandra Scolaro, Gabriella Traquandi, Paola Vianello
-
Patent number: 8158638Abstract: Problem to be Solved To provide a novel compound inhibiting the effect of HSP90, in particular a novel compound inhibiting the function of HSP90 as a chaperone protein and having antitumor activity. Solution The present invention provides a pyrazolopyrimidine compound represented by the formula (1) having various substituents which inhibits the ATPase activity of HSP90 and which has antitumor activity, an HSP90 inhibitor comprising the compound represented by the formula (1), a medicament comprising the compound represented by the formula (1), an anticancer agent comprising the compound represented by the formula (1), a pharmaceutical composition comprising the compound represented by the formula (1) and a method for treating cancer using the compound represented by the formula (1).Type: GrantFiled: September 14, 2007Date of Patent: April 17, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Satoru Ohsuki, Atsushi Tengeiji, Masahiro Ikeda, Yoshihiro Shibata, Chikahiro Nagata, Takashi Shimada
-
Publication number: 20120035131Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.Type: ApplicationFiled: October 20, 2011Publication date: February 9, 2012Inventors: Marvin J. Meyers, Graciela B. Arhancet, Xiangyang Chen, Susan Hockerman, Scott A. Long, Matthew W. Mahoney, David B. Reitz, Joseph G. Rico
-
Patent number: 8106218Abstract: Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: A represents a group selected from one of the following: (CH2)t—, —(CH2)—S(O)z—, or —S(O)z—(CH2)—, B is a heteroaryl, optionally substituted; R is a group selected from the following: alkyl, aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; R? is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R?, a ketonic group of formula —C(O)—Z?, wherein Z? is as defined below; a substituent having an hydroxyl function of formula —CH(OH)—Z?; an amide substituent of formula —C(O)—NH-T?.Type: GrantFiled: December 8, 2008Date of Patent: January 31, 2012Assignee: Neuroscienze Pharmaness S.C. A R.L.Inventors: Paolo Lazzari, Stefania Ruiu, Gerard Aime Pinna, Gabriele Murineddu
-
Publication number: 20110263588Abstract: The present invention relates to compounds that may be negative allosteric modulators of metabotropic receptors-subtype 5, and methods of making and using same.Type: ApplicationFiled: October 23, 2009Publication date: October 27, 2011Applicant: GLAXO GROUP LIMITEDInventors: Peter Bertinato, Merav Fichman, Shomir Ghosh, Jian Lin, Dalia Segal, Zhaoda Zhang
-
Publication number: 20110112088Abstract: This invention relates to compounds of the formula: to compositions containing these compounds, and to methods of treatment employing the compounds and compositions.Type: ApplicationFiled: January 13, 2011Publication date: May 12, 2011Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
-
Patent number: 7897634Abstract: This invention relates to compounds of the formulas (1), (2) and (3) having pharmacological activity, to compositions containing these compounds, and to methods of treatment employing the compounds and compositions.Type: GrantFiled: January 30, 2007Date of Patent: March 1, 2011Assignee: Athersys, Inc.Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
-
Publication number: 20100280016Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.Type: ApplicationFiled: July 12, 2010Publication date: November 4, 2010Inventors: Marvin J. Meyers, Graciela B. Arhancet, XiangYang Chen, Susan Hockerman, Scott A. Long, Matthew W. Mahoney, David B. Reitz, Joseph G. Rico
-
Publication number: 20100273791Abstract: The present invention relates to novel compounds of general formula (I), their regioisomers, tautomeric forms, novel intermediates involved in their synthesis. The present invention also relates to a process of preparing compounds of general formula (I), their regioisomers, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.Type: ApplicationFiled: April 29, 2010Publication date: October 28, 2010Inventors: Braj Bhushan LOHRAY, Vidya Bhushan Lohray, Brijesh Srivastava
-
Publication number: 20100234609Abstract: Provided are a compound represented by Formula (I): wherein R1, R2, R3, and R4 are each independently selected from a hydrogen atom, a C1-6 alkyl group which may be substituted, a C7-14 aralkyl group which may be substituted and —C(?O)Rx; n denotes an integer selected from 1 and 2; and ring Ar is selected from the groups represented by the following Formula (a) to (f). or a prodrug thereof or a pharmaceutically acceptable salt thereof as well as a pharmaceutical agent and a pharmaceutical composition containing such a compound or a prodrug thereof, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 27, 2007Publication date: September 16, 2010Inventors: Tsutomu Sato, Yoshihito Ohtake, Masahiro Nishimoto, Takashi Emura, Takamitsu Kobayashi, Marina Yamaguchi, Kyouko Takami
-
Patent number: 7795440Abstract: The invention is directed to N-substituted tricyclic 3-AMINOPYRAZOLE derivatives, which are useful as inhibitors of platelet-derived growth factor receptor (PDGF-R) kinase, and methods for the preparation of said derivatives. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as tumors and other cell proliferative disorders.Type: GrantFiled: January 25, 2007Date of Patent: September 14, 2010Assignee: Janssen Pharmaceutica NVInventors: Chih Yung Ho, Bengt Anders Brunmark, Stuart Emanuel, Robert A. Galemmo, Jr., Dana L. Johnson, Donald W. Ludovici, Umar Maharoof, Jay M. Mei, Jan L. Sechler, Eric D. Strobel, Robert W. Tuman, Hwa Kwo Yen
-
Publication number: 20100215759Abstract: Condensed tricyclic pyrazole compounds having affinity for the CB1 and/or CB2 cannabinoidergic receptors, with activity both on the peripheral and central nervous system, of formula (I): wherein: A represents a group selected from —(CH2)t—, —(CH2)r—O—(CH2)s— and —(CH2)r—S(O)p—(CH2)s— B is an heteroaryl, R is a group selected from heteroaryl, heteroarylalkyl, aryl, arylalkyl, arylalkenyl or bivalent aliphatic chain, R? is a group selected from the following: R?1: a substituent bearing a keto group of formula —C(O)— (Z?)v—Z? R?2: a substituent having an hydroxylic function of formula —CH(OH)—(Z?)v-Z?, R?3: an amide substituent of formula —C(O)—NH—(Z?)v-T?.Type: ApplicationFiled: February 25, 2010Publication date: August 26, 2010Applicant: NEUROSCIENZE PHARMANESS S.C.A.R.L.Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna
-
Publication number: 20100215741Abstract: Condensed tricyclic compounds having a condensed structure containing one phenyl and one pyrazole ring linked with each other by a central ring comprising from five to eight atoms, having affinity for the CB1 and/or CB2 receptors, with central nervous system and/or peripheral activity, of formula (I): wherein the various substituents are as defined in the description. The compounds show affinity for the CB1 and/or CB2 cannabinoidergic receptors.Type: ApplicationFiled: February 25, 2010Publication date: August 26, 2010Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna, Luca Pani
-
Publication number: 20100216785Abstract: Microemulsions of pharmaceutical compositions comprising, the following components (% by weight), the sum of the components being 100%: S) from 0.01 to 95% of one or more compounds selected from surfactants, polymers, forming organized structures as: aggregates, micelles, liquid crystals, vesicles, in the liquid in which they are solubilized, O) from 0.01 to 95% of one or more oils selected from esters of C4-C32 acids or C4-C32 acids, PA) from 0.001 to 90% of compounds having affinity for the CB1 and/or CB2 cannabinoidergic receptors of formula A?: AD) from 0 to 60% by weight of one or more compounds selected from modifiers of the water and/or oil polarity, modifiers of the film curvature of component S), co-surfactants, water or a saline aqueous solution the difference to 100%, wherein the ratio by weight S)/PA) is lower than that of microemulsions wherein component O) is absent.Type: ApplicationFiled: February 25, 2010Publication date: August 26, 2010Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.Inventors: Paolo LAZZARI, Giovanni LORIGA, Ilaria MANCA, Gerard Aime PINNA, Luca PANI
-
Patent number: 7732435Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: GrantFiled: December 5, 2006Date of Patent: June 8, 2010Assignee: Novartis AGInventors: Andrew James Culshaw, Christopher Thomas Brain, Edward Karol Dziadulewicz, Lee Edwards, Terance William Hart, Timothy John Ritchie
-
Patent number: 7691888Abstract: The present invention encompasses compounds of the general formula (1) in which R1 to R3 are defined as in claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties.Type: GrantFiled: October 5, 2005Date of Patent: April 6, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Bodo Betzemeier, Trixi Brandl, Steffen Breitfelder, Ralph Brueckner, Thomas Gerstberger, Michael Gmachl, Matthias Grauert, Frank Hilberg, Christoph Hoenke, Matthias Hoffmann, Maria Impagnatiello, Dirk Kessler, Christian Klein, Bernd Krist, Udo Maier, Darryl McConnell, Charlotte Reither, Stefan Scheuerer, Andreas Schoop, Norbert Schweifer, Oliver Simon, Martin Steegmaier, Steffen Steurer, Irene Waizenegger, Ulrike Weyer-Czernilofsky, Andreas Zoephel
-
Publication number: 20100075998Abstract: The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, means either simple or double carbon-carbon bond and R1, R2 and R3 are as defined in the specification. Further objects of the invention are a process for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Cdc7 and AKT kinase activity, like cancer.Type: ApplicationFiled: November 23, 2007Publication date: March 25, 2010Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Ermes Vanotti, Marina Caldarelli, Francesco Casuscelli, Barbara Forte, Maria Menichincheri, Alessandra Scolaro, Gabriella Traquandi, Paola Vianello
-
Publication number: 20100069374Abstract: This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3Type: ApplicationFiled: November 17, 2009Publication date: March 18, 2010Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Kazuhiko Ohrai, Yukohiro Shigeta, Osamu Uesugi, Takumi Okada, Tomoyuki Matsuda
-
Publication number: 20090291948Abstract: Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.Type: ApplicationFiled: August 3, 2009Publication date: November 26, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Georgeta Hategan, Peng Yu, David Zembower, Nian Zhou
-
Publication number: 20090081123Abstract: Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: A represents a group selected from one of the following: (CH2)t—, —(CH2)—S(O)z—, or —S(O)z—(CH2)—, B is a heteroaryl, optionally substituted; R is a group selected from the following: alkyl, aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; R? is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R?, a ketonic group of formula —C(O)-Z?, wherein Z? is as defined below; a substituent having an hydroxyl function of formula —CH(OH)-Z?; an amide substituent of formula —C(O)—NH-T?.Type: ApplicationFiled: December 8, 2008Publication date: March 26, 2009Applicant: CeNeRx BioPharmaInventors: Paolo LAZZARI, Stefania RUIU, Gerard Aime PINNA, Gabriele MURINEDDU
-
Patent number: 7485730Abstract: Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: A represents a group selected from one of the following: (CH2)t—, —(CH2)—S(O)z—, or —S(O)z—(CH2)—, B is a heteroaryl, optionally substituted; R is a group selected from the following: alkyl, aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; R? is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R?, a ketonic group of formula —C(O)-Z?, a substituent having an hydroxyl function of formula —CH(OH)-Z?; and an amide substituent of formula —C(O)—NH-T?.Type: GrantFiled: May 23, 2005Date of Patent: February 3, 2009Assignee: Neuroscienze Pharmaness S.C. A R.L.Inventors: Paolo Lazzari, Stefania Ruiu, Gerard Aime Pinna, Gabriele Murineddu
-
Publication number: 20090023779Abstract: The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.Type: ApplicationFiled: October 14, 2005Publication date: January 22, 2009Applicant: Laboratoire TheramexInventors: Benoit Rondot, Jean Lafay, Paule Bonnet, Thierry Clerc, Igor Duc, Eric Duranti, Francois Puccio, Jacqueline Shields, Christian Blot, Philippe Maillos
-
Patent number: 7425572Abstract: Novel dioxinoindazole compounds and dioxoloindazole compounds are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions of one or more of the compounds of the present invention.Type: GrantFiled: December 2, 2005Date of Patent: September 16, 2008Assignee: Alcon, Inc.Inventors: Hwang-Hsing Chen, Jesse A. May
-
Publication number: 20080182843Abstract: The present invention relates to tricyclic pyrazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: February 6, 2006Publication date: July 31, 2008Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Lou Anne Neilson, David B. Whitman
-
Publication number: 20080033183Abstract: Described are methods of making pyranoindazoles comprising reacting with a reducing agent a protected halohydrin comprising a secondary carbamate to form a pyranoindazole. In preferred embodiments the secondary carbamate is a benzyl carbamate. Also preferred are embodiments wherein the reacting is preceded by reacting a protected halohydrin with a first organometallic compound. The pyranoindazoles thus formed by the described methods are preferably pharmaceutically active products.Type: ApplicationFiled: August 1, 2007Publication date: February 7, 2008Applicant: ALCON MANUFACTURING, LTD.Inventor: Raymond E. CONROW
-
Patent number: 7320986Abstract: Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: March 3, 2004Date of Patent: January 22, 2008Assignee: Abbott LabortoriesInventors: Yunsong Tong, Akiyo K. Claiborne, Gaoquan Li, Nan-Horng Lin, Hing L. Sham, Thomas J. Sowin, Zhi-Fu Tao
-
Publication number: 20070259850Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: ApplicationFiled: May 1, 2007Publication date: November 8, 2007Inventors: Stephen E. Mercer, Prasad V. Chaturvedula
-
Patent number: 7291612Abstract: The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.Type: GrantFiled: May 30, 2006Date of Patent: November 6, 2007Assignee: Active Biotech A.B.Inventors: Ian Richard Matthews, Thomas Stephen Coutler, Chiara Ghiron, Chris James Brennan, Muhammed Kamal Uddin, Lars Olof Goran Pettersson, Dorthe da Graca Thrige, Philip Huxley
-
Publication number: 20070244179Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.Type: ApplicationFiled: April 11, 2007Publication date: October 18, 2007Applicant: WyethInventors: Alexander Alexei Greenfield, Cristina Grosanu, Hassan Mahmoud Elokdah, Albert Jean Robichaud
-
Patent number: 7253292Abstract: A process for preparing cyclopentadiene derivatives comprising the steps of: a) coupling a five membered heterocycle ring with a five or six membered heterocycle ring; b) reacting the obtained compound with a carbonilating system: c) reducing the obtained compound.Type: GrantFiled: May 8, 2002Date of Patent: August 7, 2007Assignee: Basell Polyolefine GmbHInventors: Ilya E. Nifant'ev, Igor A Kashulin, Pavel V. Ivchenko, Peter A. A. Klusener, Frans M. Kornorffer, Kees P. De Kloe, Jos J. H. Rijsemus
-
Patent number: 7081456Abstract: The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.Type: GrantFiled: November 21, 2003Date of Patent: July 25, 2006Assignee: Active Biotech ABInventors: Ian Richard Matthews, Thomas Stephen Coulter, Chiara Ghiron, Chris James Brennan, Muhammed Kamal Uddin, Lars Olof Göran Pettersson, Dorthe da Graca Thrige, Philip Huxley
-
Patent number: 6906080Abstract: The subject of the invention is tricyclic derivatives of pyrazolecarboxylic acid of formula: in which R1 represents a C3-C15 carboxyl radical or an NR2R3 group. The invention also relates to the method for preparing the compounds of formula (I), pharmaceutical compositions containing them. The compounds of formula (I) are active on cannabinoid CB1 receptors.Type: GrantFiled: November 2, 2000Date of Patent: June 14, 2005Assignee: Sanofi-AventisInventors: Francis Barth, Christian Congy, Serge Martinez, Murielle Rinaldi
-
Patent number: 6881749Abstract: Pyranoindazoles are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.Type: GrantFiled: November 24, 2003Date of Patent: April 19, 2005Assignee: Alcon, Inc.Inventors: Hwang-Hsing Chen, Jesse A. May, Bryon S. Severns
-
Patent number: 6838193Abstract: This invention features a dipyrazolo-pyridine compound of formula (I): each of R1, R2, R3, and R4, independently, is H, alkyl, alkenyl, cycloalkyl, aryl, or heteroaryl; and each of R5 and R6, independently, is aryl or heteroaryl, or R5 and R6, together with the N atom they are attached to, are heteroaryl. The dipyrazolo-pyridine compound can be used in an electro-luminescence device.Type: GrantFiled: November 14, 2002Date of Patent: January 4, 2005Assignee: Academia SinicaInventors: Yu-Tai Tao, Chung-Wen Ko, Chang-Hao Chuen, Jing-Wen Peng
-
Publication number: 20040259904Abstract: Compounds having the formula (I) 1Type: ApplicationFiled: March 3, 2004Publication date: December 23, 2004Inventors: Yunsong Tong, Akiyo K. Claiborne, Gaoquan Li, Nan-Horng Lin, Hing L. Sham, Thomas J. Sowin, Zhi-Fu Tao
-
Publication number: 20040116461Abstract: The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.Type: ApplicationFiled: November 21, 2003Publication date: June 17, 2004Applicant: ACTIVE BIOTECH ABInventors: Ian Richard Matthews, Thomas Stephen Coulter, Chiara Ghiron, Chris James Brennan, Muhammed Kamal Uddin, Lars Olof Goran Pettersson, Dorthe da Graca Thrige, Philip Huxley