- Design, synthesis and biological evaluation of selective histone deacetylase 6 (HDAC6) inhibitors bearing benzoindazole or pyrazoloindazole scaffold as surface recognition motif
-
A series of compounds were designed and synthesized based on the compound 11i bearing phenylpyrazole scaffold with histone deacetylase 6 (HDAC6) inhibitory activity. Most of the compounds showed considerable inhibitory activity against HDAC6 and compound
- Xu, Qihao,Mou, Yanhua,Wang, Siyuan,Gao, Xiaoxiao,Zhang, Yulong,Wang, Zhi,Xu, Xiangwei,Han, Yu,Jia, Wenlong,Zhang, Meihui,Zhao, Linxiang,Liu, Dan
-
-
- 1,5,6,7-Tetrahydro-4H-indazol-4-ones as human neutrophil elastase (HNE) inhibitors
-
Human neutrophil elastase (HNE) is a serine protease that is expressed in polymorphonuclear neutrophils. It has been recognized as an important therapeutic target for treating inflammatory diseases, especially related to the respiratory system, but also f
- Bartolucci, Gianluca,Cantini, Niccolo,Crocetti, Letizia,Giovannoni, Maria Paola,Guerrini, Gabriella,Pallecchi, Marco,Quinn, Mark T.,Schepetkin, Igor A.,Teodori, Elisabetta,Vergelli, Claudia
-
-
- Mercaptan compound having HDAC6 (histone deacetylase 6) inhibitory activity and application thereof
-
The invention belongs to the technical field of medicines and relates to a mercaptan compound having an anti-tumor activity, in particular to a mercaptan compound containing a 6(7)-substituted-N-(6-decylhexyl)-pyrazolo[3,4-e] indazole-3-formamide fragment
- -
-
-
- Hydroxamic acid compound having HDAC6 inhibitory activity and application thereof
-
The invention belongs to the technical field of medicines, and relates to hydroxamic acid compound having HDAC6 inhibitory activity and antitumor activity, in particular to a hydroxamic acid compoundwith benzoindazole and pyrazolindazole as mother nucleus
- -
-
-
- AMINOACYLINDAZOLE IMMUNOMODULATORS FOR TREATMENT OF AUTOIMMUNE DISEASES
-
2-Acylindazole compounds of formula I or formula II are disclosed. These compounds inhibit Coagulation Factor XIIa. They are useful to treat autoimmune diseases.
- -
-
Paragraph 335
(2017/12/29)
-
- Novel crown ether functionalized imidazolium-based acidic ionic liquid catalyzed synthesis of pyrazole derivatives under solvent-free conditions
-
Abstract An innovatively designed novel crown ether functionalized imidazolium-based reusable acidic ionic liquid [crown ether MIm] [HSO4] has been efficiently implemented for the synthesis of pyrazole derivatives using various substituted enaminones, hydrazine hydrate and phenyl hydrazine under solvent-free conditions. Structural novelty and task efficiency of the catalyst, high yields of desired products, greener approach attributing high atom economy and solvent-free conditions render this protocol suitable to cope with the current demand in contemporary organic chemistry. The inventive idea of utilizing crown ether functionalized ionic liquid as a catalyst was for the first time demonstrated in this protocol.
- Patil, Dayanand,Chandam, Dattatraya,Mulik, Abhijeet,Jagdale, Suryabala,Patil, Prasad,Deshmukh, Madhukar
-
p. 6843 - 6858
(2015/08/18)
-
- Pyrazolo[3,4-h]quinolines promising photosensitizing agents in the treatment of cancer
-
A new series of pyrazolo[3,4-h]quinolines, heteroanalogues of angelicin was conveniently prepared with a broad substitution pattern. A large number of derivatives was obtained and the cellular photocytotoxicity was evaluated in vitro against 5 different h
- Spanò, Virginia,Parrino, Barbara,Carbone, Anna,Montalbano, Alessandra,Salvador, Alessia,Brun, Paola,Vedaldi, Daniela,Diana, Patrizia,Cirrincione, Girolamo,Barraja, Paola
-
p. 334 - 351
(2015/09/01)
-
- TRICYCLIC COMPOUNDS AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
-
The present invention describes and claims compounds of the Structural Formula (I), Structural Formula (II), or Structural Formula (III). In Formula (I), R1, R2, R3 and R3' are -H or methyl, or R3 and R3' taken together form a double bond, or R3' is -H and R2 and R3 taken together form a spiro-cyclopropyl substituent, R4 is -H or -F, and R5 is -H, methyl, -Cl or -Br. In Formula (II), R1 is -H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, R4 is -H or -F, and "Y" is: (a) -CH2-; (b) -CR6H-O-CR7R8-, wherein R6, R7, and R8 are independently -H or methyl; (c) -CR6H-N(R9)-CR7R8-, wherein R6, R7, and R8 are independently -H or methyl; (d) -CH2-C(R9)(R10)-C(R7)(R8)-, wherein R7, R8, R9 and R10 are independently -H or -methyl, or both R7 and R8 are -F, R9 and R10 are independently -H or -methyl, or both R9 and R10 are -F, or R9 and R10 taken together are (O=), which together with the carbon to which they are attached forms a carbonyl group.
- -
-
Page/Page column 25
(2012/02/02)
-
- TRICYCLIC COMPOUNDS AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
-
The present invention describes and claims compounds of the Structural Formula I, Structural Formula II, or Structural Formula III: wherein R1, R2, R3 and R3' are -H or methyl, or R3 and R3 taken together form a double bond, or R3' is -H and R2 and R3 taken together form a spiro-cyclopropyl substituent, R4 is -H or -F, and R5 is -H, methyl, -CI or -Br, Formula II wherein R1 is -H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, R4 is -H or -F, and "Y" is: (a) -CH2-; (b) -CR6H-0-CR7R8-, wherein R6, R7, and R8 are independently - H or methyl; (c) -CR6H-N(R9)-CR7R8-, wherein R6, R7, and R8 are independently -H or methyl; (d) -CH2-C(R9)(R10)-C(R7)(R8)-, wherein R7, R8, R9 and R10 are independently - H or -methyl, or both R7 and R8 are -F, R9 and R10 are independently -H or -methyl, or both R9 and R10 are -F, or R9 and R10 taken together are (0=), which together with the carbon to which they are attached forms a carbonyl group.
- -
-
Page/Page column 25
(2012/02/02)
-
- Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators
-
There is an increasing amount of evidence to support that activation of the metabotropic glutamate receptor 4 (mGlu4 receptor), either with an orthosteric agonist or a positive allosteric modulator (PAM), provides impactful interventions in diseases such as Parkinson's disease, anxiety, and pain. mGlu4 PAMs may have several advantages over mGlu4 agonists for a number of reasons. As part of our efforts in identifying therapeutics for central nervous system (CNS) diseases such as Parkinson's disease, we have been focusing on metabotropic glutamate receptors. Herein we report our studies with a series of tricyclic thiazolopyrazoles as mGlu4 PAMs.
- Hong, Sang-Phyo,Liu, Kevin G.,Ma, Gil,Sabio, Michael,Uberti, Michelle A.,Bacolod, Maria D.,Peterson, John,Zou, Zack Z.,Robichaud, Albert J.,Doller, Darío
-
p. 5070 - 5081
(2011/09/16)
-
- HETEROTRICYCLIC COMPOUNDS AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
-
The present invention relates to novel compounds of Formula (I), wherein wherein X1, X2, Y, Z1, Z2, Z3, M and (A)m are defined as in Formula (I); invention compounds are modulators of metab
- -
-
Page/Page column 25
(2010/08/04)
-
- An efficient solvent-free synthesis of NH-pyrazoles from β-dimethylaminovinylketones and hydrazine on grinding
-
A series of NH-pyrazoles was efficiently synthesized from the reaction of β-dimethylaminovinylketones ([R1C(O)C(R2){double bond, long}CHN(Me2)], where R1 = Me, Ph, 3-MeO-Ph, 4-Me-Ph, 4-MeO-Ph, 4-F-Ph, 4-Cl-Ph, 4
- Longhi, Kelvis,Moreira, Dayse N.,Marzari, Mara R.B.,Floss, Vagner M.,Bonacorso, Helio G.,Zanatta, Nilo,Martins, Marcos A.P.
-
supporting information; experimental part
p. 3193 - 3196
(2010/08/05)
-
- CYCLOHEXYLPYRAZOLE-LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
-
The present invention discloses novel compounds of Formula (I): having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compound
- -
-
Page/Page column 51-52
(2009/05/29)
-
- Synthesis and structural study of tetrahydroindazolones
-
Multinuclear magnetic resonance spectroscopy allowed us to characterize four 1(2),5,6,7-tetrahydro-4H-indazol-4-one derivatives (1-4) and establish the most stable tautomer in each case. The crystal structure of 6,6-dimethyl-1(2),5,6,7-tetrahydro-4H-indaz
- Claramunt, Rosa M.,López, Concepción,Pérez-Medina, Carlos,Pinilla, Elena,Torres, M. Rosario,Elguero, José
-
p. 11704 - 11713
(2007/10/03)
-
- Benzodipyrazoles: A new class of potent CDK2 inhibitors
-
The synthesis and the preliminary expansion of this new class of CDK2 inhibitors are presented. The synthesis was accomplished using a solution-phase protocol amenable to rapid parallel expansion and suitable to be scaled-up in view of possible lead devel
- D'Alessio, Roberto,Bargiotti, Alberto,Metz, Suzanne,Brasca, M. Gabriella,Cameron, Alexander,Ermoli, Antonella,Marsiglio, Aurelio,Polucci, Paolo,Roletto, Fulvia,Tibolla, Marcellino,Vazquez, Michael L.,Vulpetti, Anna,Pevarello, Paolo
-
p. 1315 - 1319
(2007/10/03)
-
- Aqueous one-pot synthesis of pyrazoles, pyrimidines and isoxazoles promoted by microwave irradiation
-
Microwave irradiation promotes the conversion of enaminoketones formed in situ into a variety of heterocycles by reaction with the appropriate bidentate nucleophile. The advantages of the method over previous approaches are short reaction times and facile purification by precipitation of the products in aqueous media. Moreover the convenient one-pot procedure makes these syntheses particularly suitable for library production. Organic reactions in aqueous media have become of great interest as water is not only more environmentally friendly, but also because organic reactions in water often display unique reactivity and selectivity.
- Molteni, Valentina,Hamilton, Matthew M.,Mao, Long,Crane, Christine M.,Termin, Andreas P.,Wilson, Dean M.
-
p. 1669 - 1674
(2007/10/03)
-
