- Heterogeneous Catalytic Reductive Amination of Carbonyl Compounds with Ni-Al Alloy in Water as Solvent and Hydrogen Source
-
The heterogeneous catalytic reductive amination of carbonyl compounds has been achieved by reactions of ammonium hydroxide and various amines with ketones and aldehydes. The process is based on the application of Raney type Ni-Al alloy in an aqueous medium. The reaction of the carbonyl compounds with the amine provided the corresponding Schiff bases that immediately underwent a reduction to provide primary and secondary amines as products. The controlled reaction of the Al content of the alloy with the solvent water generates hydrogen, and the in situ formed Raney Ni serves as a hydrogenation catalyst. The method is a simple and efficient way of preparing a broad variety of primary and secondary amines.
- Sch?fer, Christian,Ni?anci, Bilal,Bere, Matthew P.,Da?tan, Arif,T?r?k, Béla
-
p. 3127 - 3133
(2016/09/09)
-
- FUSED TRICYCLIC COMPOUNDS FOR USE AS INHIBITORS OF JANUS KINASES
-
The invention provides novel compounds of formula (I) having the general formula (I) wherein R1, V, W, X, Y and Z are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.
- -
-
-
- 1-(DIHYDRONAPHTHALENYL)PYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
-
Provided are 1-(dihydronaphthalenyl)pyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy for the treatment of obesity and diabetes.
- -
-
-
- HETEROCYCLIC COMPOUND
-
The present invention provides to a compound having melanin-concentrating hormone receptor antagonistic action and low toxicity, and useful as a agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound re
- -
-
Page/Page column 52
(2010/12/30)
-
- NOVEL COMPOUNDS
-
The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to formula (I) and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular IKK2 activity.
- -
-
-
- Kinase inhibitor compounds
-
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.
- -
-
Page/Page column 21
(2009/04/24)
-
- NOVEL COMPOUNDS
-
The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to formula (I) and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular IKK2 activity.
- -
-
-
- PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
-
The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4 /PDE type 7 inhibitors. Compounds disclosed hereinf having the structure of Formula 1: can be useful in the treatment, prevention, inhibiti
- -
-
Page/Page column 52
(2008/12/07)
-
- PYRAZOLO (3, 4-B) PYRIDINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
-
The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4 /PDE type 7 inhibitors. Compounds disclosed herein having the structure of Formura 1: can be useful in the treatment, prevention, inhibitio
- -
-
Page/Page column 75
(2008/12/07)
-
- KINASE INHIBITOR COMPOUNDS
-
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.
- -
-
Page/Page column 48-49
(2008/06/13)
-
- PYRAZOLE COMPOUNDS HAVING CANNABINOID RECEPTOR (CB1) ANTAGONIZING ACTIVITY
-
The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: -N(R7)-, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: -N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: -N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., or a pharmaceutically acceptable salt thereof.
- -
-
Page/Page column 118
(2008/06/13)
-
- TETRAHYDROINDOLONE AND TETRAHYDROINDAZOLONE DERIVATIVES
-
Disclosed are compounds and pharmaceutically acceptable salts of Formula (I): wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined
- -
-
Page/Page column 98-99
(2008/06/13)
-
- PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS
-
The invention relates to a compound of formula (I) or a salt thereof: wherein:R1 is C1-4alkyl, C1-3fluoroalkyl, -CH2CH2OH or -CH2CH2CO2C1-2alkyl;R2 is a hydrogen atom (H), methyl or C1fluoroalkyl;R3 is optionally substituted C3-8cycloalkyl or optionally substituted mono-unsaturated-C5-7cycloalkenyl or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc); in which n1 and n2 independently are 1 or 2; and in which Y is O, S, SO2, or NR10; or R3 is a bicyclic group (dd) or (ee): ; and wherein X is NR4R5 or OR5a. The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.
- -
-
-
- Heterocyclic amides, a process for their preparation, compositions comprising them and their use
-
What is described are amides of the formula (I) and salts thereof, where the symbols and indices are as defined below: X is CH or N; Y is O or S; n is 0 or 1; R1 is (C1-C4)-haloalkyl; R2, R3 independently of one another are hydrogen, (C1-C4)-alkyl, (C1-C4)-haloalkyl or halogen, R4 is hydrogen, (C1-C10)-alkyl, (C3-C10)-cycloalkyl, (C3-C10)-alkenyl or (C3-C10)-alkynyl, where in the alkyl, cycloalkyl, alkenyl or alkynyl groups mentioned up to three hydrogen atoms may be replaced by halogen, in the case of fluorine also up to the maximum number; R5 is an aliphatic heterocycle which contains at least one oxygen, sulfur, nitrogen and/or silicon ring atom, which is unsubstituted or substituted by one to six monovalent groups and which may be part of a spirocyclic, fused or bicyclic ring system. These compounds can be used for controlling pests.
- -
-
Page/Page column 13
(2010/02/05)
-
- AZOLE COMPOUNDS
-
The present invention provides a compound represented by the formula (I) wherein R1 is a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, an optionally substituted hydroxy group, an optionally substituted thiol group or an optionally substituted amino group, A is an optionally substituted cyclic amino group or -NR2-W-D wherein R2 is a hydrogen atom or an alkyl group, W is a bond or a divalent acyclic hydrocarbon group, and D is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom, and Y is a bond or a divalent acyclic hydrocarbon group, or a salt thereof, which is useful for the prophylaxis or treatment of diabetic neuropathy and the like.
- -
-
-
- 6-Substituted pyrido-pyrimidines
-
The present invention provides compounds of the Formula I and II: wherein R1, R3, W, Z, X1, X2, Ar1, R8 and R9 are as defined herein, and methods and intermediates for their preparation and uses thereof.
- -
-
-
- Novel carbamate and oxamide compounds
-
Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
- -
-
-
- Compounds useful as anti-inflammatory agents
-
Disclosed are novel aromatic compounds of the formula(I) wherein G, E, W, Ar, X, Y and Z. The compounds are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
- -
-
-
- Imidazo-substituted compounds as p38 kinase inhibitors
-
The present invention discloses compounds corresponding to formula I: wherein A, Z, Z1, Y, R1 and R2 are as defined in the specification, as well as pharmaceutical formulations, methods of making and uses thereof.
- -
-
-
- Compounds useful as anti-inflammatory agents
-
Disclosed are novel aromatic compounds of the formula(I) wherein G, E, W, Ar, X, Y and Z. The compounds are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
- -
-
-
- Synthesis and Conformational Analysis of Substituted 4-Aminothianes
-
Reductions of substituted 4-thianone oximes by LiAlH4 gave a mixture of epimeric 4-aminothianes.Separation of the epimeric mixture was achieved via column chromatography over neutral alumina.Independent syntheses of these amines by a stereospecific route starting from the tosylate of the corresponding 4-thianols that reacted with sodium azide in DMF followed by reduction of the azide with LiAlH4 provided structure proofs for the amines.N-Acetyl derivatives were also prepared from the aminothianes.Conformational analysis of the amines was performed via an inspection of the (1)H and (13)C NMR spectra.These spectral data suggested t wist conformations for 2,2-dimethyl-trans-6-phenyl-r-4-aminothiane and 2,2-dimethyl-trans-6-p-chlorophenyl-r-4-aminothiane.
- Subramanian, Pullachipatti K.,Ramalingam, Kondareddiar,Satyamurthy, Nagichettiar,Berlin, K. Darrell
-
p. 4376 - 4383
(2007/10/02)
-
