Additional Hetero Ring Other Than The Six-membered Hetero Rings Patents (Class 514/333)
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Publication number: 20150119384Abstract: The present invention relates to ethynyl derivatives of formula I X, O, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined hereinor to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.Type: ApplicationFiled: January 6, 2015Publication date: April 30, 2015Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Publication number: 20150119395Abstract: The present invention relates to novel triazole Hsp90 inhibitors that possess significant inhibitory activity against Hsp90, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders. Furthermore, pharmaceutical compositions, including combination products, are also provided in the present application. Further provided are methods of using the pharmaceutical compositions and/or combination products.Type: ApplicationFiled: April 4, 2013Publication date: April 30, 2015Inventors: Dinesh U. Chimmanamada, Weiwen Ying
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Patent number: 9018234Abstract: The present invention relates to novel, fluoro-substituted 2-aryl-3,5-dicyano-4-(1H-indazol-5-yl)-6-methyl-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly Cancer and other proliferative disorders.Type: GrantFiled: November 8, 2010Date of Patent: April 28, 2015Assignee: Bayer Intellectual Property GmbHInventors: Alexandros Vakalopoulos, Martin Michels, Katja Zimmermann, Nicole Teusch, Mario Lobell, Karen Engel
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Patent number: 9017735Abstract: Disclosed herein are compositions and methods for treating a psychiatric disorder or symptoms thereof in a patient. The compositions comprise a compound that modulates KCNQ (Kv7) potassium channel activity and the methods include administering an effective amount of the compound that modulates KCNQ (Kv7) potassium channel activity.Type: GrantFiled: June 3, 2010Date of Patent: April 28, 2015Assignee: Marquette UniversityInventor: Mohammadhossein Behnam Ghasemzadeh
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Patent number: 9018233Abstract: The invention relates to diaminoaryl derivatives substituted by carbamate, salts thereof and a pesticidal composition containing the same, which exhibit superior pest control effects against various insect pests of insect species, in particular against moths such as the diamondback moth or Spodoptera litura.Type: GrantFiled: May 7, 2013Date of Patent: April 28, 2015Assignees: Kyung Nong Corporation, Korea Research Institute of Chemical TechnologyInventors: Sung Youn Chang, Jung Nyoung Heo, Hyuk Lee, Hwan Jung Lim, Bum Tae Kim, Joo Kyung Kim, Jong-Kwan Kim
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Publication number: 20150111865Abstract: An object of the present invention is to provide a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I): (wherein all symbols represent the same meanings as described in the specification), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.Type: ApplicationFiled: April 25, 2013Publication date: April 23, 2015Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Jun Takeuchi, Masahiro Ikura, Masato Higashino, Maki Iwahashi, Kazuya Hashimura
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Publication number: 20150111734Abstract: A pesticidal composition comprises at least one compounds selected from a compound of formula, or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, Q, Z, L, La, and x are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Yu Zhang, Asako Kubota, Noormohamed M. Niyaz, Thomas Barton, Tony K. Trullinger, Christian T. Lowe, Paul R. LePlae, Ann M. Buysse, Martin J. Walsh, Negar Garizi, Ricky Hunter, Daniel Knueppel
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Publication number: 20150111900Abstract: The present invention relates to compounds described herein Formula (I) and pharmaceutical acceptable salts thereof, which modulate the activity of calcium release-activated calcium (CRAC) channel. The invention also describes the compounds of Formula (I) and pharmaceutical compositions containing such compounds thereof for treating, managing, and/or lessening the severity of diseases, disorders, syndromes or conditions associated with the modulation of calcium release-activated calcium (CRAC) channel.Type: ApplicationFiled: May 1, 2013Publication date: April 23, 2015Inventors: Nageswara Rao Irlapati, Zubair Abdul Wajid Shaikh, Vijay Pandurang Karche, Gokul Keruji Deshmukh, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
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Publication number: 20150111735Abstract: A pesticidal composition comprises a pyridine triazole compound of formula I or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, Z, and x are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse
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Publication number: 20150099758Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.Type: ApplicationFiled: May 8, 2013Publication date: April 9, 2015Applicant: Anvyl LLCInventors: David Putnam, Olivier Dasse
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Publication number: 20150099736Abstract: Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1-C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, —N(R11)—R12, -Alk-N(R11)—R12, —O-Alk-N(R11)—R12, —C(?O)OH, carboxy-(C1-C3)-alkyl, or —C(?O)—NH—R13; Alk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(?O)—N(—R16)— or —N(—R17)—C(?O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substituType: ApplicationFiled: November 10, 2014Publication date: April 9, 2015Inventors: Stephen Stokes, Nicolas Foloppe, Andrea Fiumana, Martin Drysdale, Simon Bedford, Paul Webb
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Publication number: 20150099750Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: December 1, 2014Publication date: April 9, 2015Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger
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Patent number: 8999971Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.Type: GrantFiled: August 21, 2014Date of Patent: April 7, 2015Assignee: Aerpio Therapeutics Inc.Inventors: Robert Shalwitz, Joseph H. Gardner
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Patent number: 8999966Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).Type: GrantFiled: October 24, 2011Date of Patent: April 7, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, Jr.
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Patent number: 8993598Abstract: The present invention relates to a compound represented by the formula: wherein A is pyridyl group having at least one substituent wherein R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, R4 and R6 are each a hydrogen atom, a halogen atom or a C1-6 alkyl group optionally substituted by halogen, R5 is a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, and R7 is a hydrogen atom or a C1-6 alkyl group optionally substituted by halogen or a salt thereof, or a pharmaceutical composition containing the same.Type: GrantFiled: October 1, 2013Date of Patent: March 31, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Haruyuki Nishida, Yasuyoshi Arikawa, Ikuo Fujimori
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Publication number: 20150087644Abstract: The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.Type: ApplicationFiled: November 26, 2014Publication date: March 26, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Christian Lerner
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Publication number: 20150087648Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: November 10, 2014Publication date: March 26, 2015Inventors: Werngard CZECHTIZKY, John WESTON, Nils RACKELMANN, Michael PODESCHWA, Petra ARNDT, Klaus WIRTH, Heinz GOEGELEIN, Olaf RITZELER, Volker KRAFT, Patrice BELLEVERGUE, Gary McCORT
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Publication number: 20150087618Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: December 2, 2014Publication date: March 26, 2015Applicant: AbbVie Inc.Inventors: Mary E. Bellizzi, David A. Betebenner, Jean C. Califano, William A. Carroll, Daniel D. Caspi, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Yi Gao, Charles W. Hutchins, Douglas K. Hutchinson, Tammie K. Jinkerson, Warren M. Kati, Ryan G. Keddy, Allan C. Krueger, Wenke Li, Dachun Liu, Clarence J. Maring, Mark A. Matulenko, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, John K. Pratt, John T. Randolph, Todd W. Rockway, Kathy Sarris, Michael D. Tufano, Seble H. Wagaw, Rolf Wagner, Kevin R. Woller
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Patent number: 8987305Abstract: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.Type: GrantFiled: February 27, 2013Date of Patent: March 24, 2015Assignee: Aptose Biosciences Inc.Inventors: Raed H. Al-Qawasmeh, Aiping H. Young, Mario Huesca, Yoon S. Lee
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Patent number: 8987250Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: GrantFiled: April 19, 2013Date of Patent: March 24, 2015Assignee: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20150080367Abstract: The present invention provides for compounds of Formula I and various embodiments thereof, and compositions comprising compounds of Formula I and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6, m, n and the C-linked Ring have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula I as DLK inhibitors and for treating neurodegeneration diseases and disorders.Type: ApplicationFiled: November 21, 2014Publication date: March 19, 2015Applicant: Genentech, Inc.Inventors: Frederick Cohen, Malcolm Huestis, Cuong Ly, Snahel Patel, Michael Siu, Xianrui Zhao
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Publication number: 20150080412Abstract: The invention disclosed herein is directed to compounds of Formula (I) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula (I), or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a of a therapeutically effective amount of a selective PPAR? antagonist.Type: ApplicationFiled: March 7, 2013Publication date: March 19, 2015Applicant: INCEPTION 2, INC.Inventors: Nicholas Simon Stock, Austin Chih-Yu Chen, Yalda Mostofi Bravo, Jason Duarte Jacintho, Jill Melissa Baccei, Brian Andrew Stearns, Ryan Christopher Clark, Yen Pham Truong
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Patent number: 8980629Abstract: 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: GrantFiled: August 23, 2013Date of Patent: March 17, 2015Assignee: CalciMedica, Inc.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20150072859Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.Type: ApplicationFiled: November 19, 2014Publication date: March 12, 2015Applicant: DOW AGROSCIENCES LLCInventors: Noormohamed M. Niyaz, Negar Garizi, Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse, Asako Kubota, Paul R. LePlae, Jr., Daniel Knueppel, Christian T. Lowe, Dan Pernich, David A. Demeter, Timothy C. Johnson
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Patent number: 8975286Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: GrantFiled: August 16, 2010Date of Patent: March 10, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Vadim Y. Dudkin, Mark E. Fraley, Cheng Wang, Robert M. Garbaccio, Douglas C. Beshore, Scott K. Kuduk, Jason W. Skudlarek
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Patent number: 8975261Abstract: The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: May 21, 2012Date of Patent: March 10, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Michael J. Breslin, Christopher D. Cox, Timothy J. Hartingh, Joseph Pero, Izzat T. Raheem, Michael Rossi, Laura Vassallo
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Patent number: 8975282Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: GrantFiled: July 19, 2013Date of Patent: March 10, 2015Assignees: Sunshine Lake Pharma Co., Ltd., Calitor Sciences, LLCInventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
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Publication number: 20150065464Abstract: The present disclosure relates to substituted amide compounds that are inhibitors of Fatty Acid Amide Hydrolase (FAAH), their stereoisomers, tautomers, prodrugs, polymorphs, solvates, pharmaceutically acceptable salts, and pharmaceutical compositions containing them.Type: ApplicationFiled: September 21, 2012Publication date: March 5, 2015Inventors: Rajendra Kharul, Debnath Bhuniya, Kasim A. Mookhtiar, Umesh Singh, Atul Hazare, Satish Patil, Laxmikant Datrange, Mahesh Thakkar
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Publication number: 20150065500Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: September 11, 2014Publication date: March 5, 2015Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
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Publication number: 20150065483Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
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Publication number: 20150065506Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: ApplicationFiled: August 13, 2014Publication date: March 5, 2015Applicant: ROCHE PALO ALTO LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Patent number: 8969338Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, Y, R1, R2, R2?, R3, R3? and R8 are described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).Type: GrantFiled: September 27, 2012Date of Patent: March 3, 2015Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Patent number: 8969387Abstract: The present invention relates to a compound represented by the formula: wherein A is pyridyl group having at least one substituent wherein R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, R4 and R6 are each a hydrogen atom, a halogen atom or a C1-6 alkyl group optionally substituted by halogen, R5 is a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, and R7 is a hydrogen atom or a C1-6 alkyl group optionally substituted by halogen or a salt thereof, or a pharmaceutical composition containing the same.Type: GrantFiled: August 26, 2009Date of Patent: March 3, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Haruyuki Nishida, Yasuyoshi Arikawa, Ikuo Fujimori
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Patent number: 8969383Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: GrantFiled: June 12, 2014Date of Patent: March 3, 2015Assignee: RaQualia Pharma Inc.Inventors: Hirohide Noguchi, Tadashi Inoue, Mikio Morita, Yoshimasa Arano
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Patent number: 8969388Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: GrantFiled: July 19, 2013Date of Patent: March 3, 2015Assignees: Sunshine Lake Pharma Co., Ltd., Calitor Sciences, LLCInventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
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Patent number: 8969386Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating CFTR mediated diseases using compounds of the present invention.Type: GrantFiled: May 9, 2008Date of Patent: March 3, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Mark Miller, Brian Bear, Jinglan Zhou, Jason McCartney, Peter Grootenhuis
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Publication number: 20150057281Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Especially preferred compounds disrupt Nek2/Hec1 binding and are therefore useful as chemotherapeutic agent for neoplastic diseases.Type: ApplicationFiled: October 29, 2014Publication date: February 26, 2015Inventors: Johnson LAU, Jiann-Jyh HUANG
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Publication number: 20150057286Abstract: This invention relates to bis-amido pyridines of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R4 have the meanings given in the claims and in the specification.Type: ApplicationFiled: August 20, 2014Publication date: February 26, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Ulrich REISER
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Publication number: 20150057280Abstract: The invention relates to pyridylidene compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted pyridylidene compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted pyridylidene compounds. The N-substituted pyridylidene compounds of the present invention are defined by the following formula I: wherein X, Het, R1, R2, R3, R4 and R6 are defined as in the description.Type: ApplicationFiled: March 27, 2013Publication date: February 26, 2015Applicant: BASF SEInventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Korber
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Publication number: 20150057247Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.Type: ApplicationFiled: October 29, 2014Publication date: February 26, 2015Inventors: Craig C. Beeson, Christopher C. Lindsey, Yuri K. Peterson, Baerbel Rohrer
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Publication number: 20150051208Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R3 and X1 through X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.Type: ApplicationFiled: August 11, 2014Publication date: February 19, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald ENGELHARDT, Laetitia MARTIN, Christian SMETHURST
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Publication number: 20150050239Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: July 19, 2013Publication date: February 19, 2015Applicants: Calitor Sciences, LLC, Sunshine Lake Pharma Co., Ltd.Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
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Publication number: 20150051251Abstract: Premature termination codons readthrough compounds, composition thereof, and methods of making and using the same are provided.Type: ApplicationFiled: March 15, 2013Publication date: February 19, 2015Applicant: The Regents of the University of CaliforniaInventors: Richard A. Gatti, Liutao Du, Hailiang Hu, Robert Damoiseaux, Michael E. Jung, Jin-Mo Ku, Gladys Completo
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Publication number: 20150051225Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: February 19, 2015Applicant: Janssen Pharmaceutica NVInventors: Ishtiyaque Ahmad, Rajagopal Bakthavatchalam, Sivaramakrishna Battula, Henricus Jacobus, Maria Gijsen, Mark Wall
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Patent number: 8957215Abstract: The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.Type: GrantFiled: April 23, 2012Date of Patent: February 17, 2015Assignee: Navidea Biopharmaceuticals, Inc.Inventors: Ylva Gravenfors, Catrin Jonasson, Jonas Malmstrom, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Strom, David Wensbo
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Patent number: 8957213Abstract: The present invention relates to ethynyl derivatives of formula I X, G, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.Type: GrantFiled: April 23, 2012Date of Patent: February 17, 2015Assignee: Hoffman-La Roche Inc.Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Publication number: 20150045218Abstract: This document discloses molecules having the following formula (“Formula I”):Type: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Applicant: DOW AGROSCIENCES LLCInventors: Tony K. Trullinger, Ricky Hunter, Negar Garizi, Maurice C. Yap, Ann M. Buysse, Dan Pernich, Timothy C. Johnson, Kristy Bryan, Carl DeAmicis, Yu Zhang, Noormohamed M. Niyaz, CaSandra L. McLeod, Ronald Ross, JR., Yuanming Zhu, Peter Lee Johnson, Joseph D. Eckelbarger, Marshall H. Parker
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Publication number: 20150037280Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: July 19, 2013Publication date: February 5, 2015Applicants: Sunshine Lake Pharma Co., Ltd., Calitor Sciences, LLCInventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
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Publication number: 20150038517Abstract: This invention relates to modulation of the ?7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a salt thereof: wherein R1 is imidazolyl, pyridinyl or pyrimidinyl, any of which is optionally substituted by one group independently selected from C1-3alkyl and C1-3alkoxy.Type: ApplicationFiled: August 7, 2014Publication date: February 5, 2015Inventor: Kevin Dinnell
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Patent number: 8946236Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.Type: GrantFiled: August 7, 2013Date of Patent: February 3, 2015Assignee: Bayer Cropscience AGInventors: Bernd Alig, Ruediger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Goergens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald