- ASYMMETRIC SYNTHESIS OF A SUBSTITUTED PYRROLIDINE-2-CARBOXAMIDE
-
The present invention provides an improved method for the large scale production of the compound 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic a
- -
-
Page/Page column 22
(2014/09/03)
-
- COMPOUNDS FOR THE TREATMENT OF PARAMOXYVIRUS VIRAL INFECTIONS
-
Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
- -
-
Paragraph 0553
(2014/03/25)
-
- Substituted benzamides with activity towards EP4 receptors
-
The present invention belongs to the field of EP4 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP4 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP4 receptor as well as to pharmaceutical compositions comprising them.
- -
-
Paragraph 0100-0101
(2014/08/20)
-
- SUBSTITUTED BENZAMIDES WITH ACTIVITY TOWARDS EP4 RECEPTORS
-
The present invention belongs to the field of EP4 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP4 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP4 receptor as well as to pharmaceutical compositions comprising them.
- -
-
Page/Page column 37; 38
(2014/08/20)
-
- PYRAZOLOTHIAZOLE COMPOUND
-
A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism wherein X is a nitrogen atom or CH; R1 is -A11-A12; A11 is a single bond or a C1-6 alkylene group; A12 is a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group, etc.; R2 is -A21-A22; A21 is a single bond or a C1-6 alkylene group; A22 is a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a non-aromatic heterocyclic group, or a heteroaryl group, etc.; R3 is a C 1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C3-6 cycloalkoxy C1-6 alkyl group, di-C1-6 alkyl amino group, a halogen atom, a cyano group, a formyl group, or a carboxyl group, etc; R4 is a hydrogen atom or a C1-6 alkoxy group; R5 is a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; R6 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylthio group, or a C1-6 alkyl sulfinyl group etc.; and R7 is a C1-6 alkyl group, a C1-6 alkoxy group, or a C1-6 alkylthio group
- -
-
Page/Page column 27
(2011/04/25)
-
- Synthesis of symmetric diester-functionalised Troeger's base analogues
-
The yields of ester-functionalised Troeger's base analogues are dramatically improved by incorporating an electron-donating group on the aromatic ring and/or enhancing solubil- ity of the aniline unit. In addition to 2,8-diester compounds, 1,7-, 3,9- and 4,10-diester-functionalised Troeger's base analogues have been prepared for the first time.
- Bhuiyan, M. Delower H.,Zhu, Kai-Xian,Jensen, Paul,Try, Andrew C.
-
supporting information; experimental part
p. 4662 - 4670
(2010/10/19)
-
- 3-PHENYLPYRAZOLO[5,1-b]THIAZOLE COMPOUNDS
-
A compound represented by the following formula (I), or salt thereof exhibits excellent CRF receptor antagonism, and sufficient pharmacological activity, safety and pharmacokinetic properties as a drug. wherein R1 represents the formula -A11-A12; R2 represents tetrahydrofurylmethyl, tetrahydropyranylmethyl or tetrahydropyranyl; A11 represents a single bond, methylene or 1,2-ethylene; A12 represents C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl having methyl; R3 represents methoxy, cyano, cyclobutyloxymethyl, methoxymethyl or ethoxymethyl; and R4 represents methoxy or chlorine.
- -
-
Page/Page column 12
(2009/10/21)
-
- Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains
-
Novel diarylpyrimidines (DAPY), which represent next generation of non-nucleoside reverse transcriptase inhibitors (NNRTIs), were synthesized and their activities against human immunodeficiency virus type I (HIV-1) assessed. Modulations at positions 2 and
- Mordant, Celine,Schmitt, Benoit,Pasquier, Elisabeth,Demestre, Christophe,Queguiner, Laurence,Masungi, Chantal,Peeters, Anik,Smeulders, Liesbeth,Bettens, Eva,Hertogs, Kurt,Heeres, Jan,Lewi, Paul,Guillemont, Jerome
-
p. 567 - 579
(2008/02/10)
-
- Aromatic amine substituted bridged nitrogen and sulfur donor atom ligands for imaging
-
The present invention provides aromatic amine substituted metal chelating compounds, chelates and chelate-targeting moiety conjugates formed from the chelating compounds, and methods for making and using these compounds. Metals capable of being chelated by the chelating compounds include radionuclides, such as 99mTc and 186188Re.
- -
-
-
- Antibody-catalyzed decarboxylative oxidation of vanillylmandelic acid
-
The most important industrial process for the synthesis of vanillin is performed in two steps involving an electrophilic aromatic substitution of glyoxylic acid on guaiacol followed by an oxidative decarboxylation of the intermediary α-hydroxy acids formed, thereby producing not only vanillin, but also byproducts which have to be eliminated. In the present study, we took advantage of the high specificity of catalytic antibodies to improve the synthesis of vanillin. Among 11 monoclonal antibodies elicited against the quaternary ammonium hapten H3, antibody H3-12 was found to catalyze the oxidative decarboxylation of vanillylmandelic acid (VMA), the precursor of vanillin, in the presence of sodium metaperiodate. The kinetic data of the antibody-catalyzed reaction are consistent with an ordered binding mechanism. At pH 9.0, H3-12 catalyzed the transformation of VMA into vanillin with a k(cat) of 2.70 min-1, a Michaelis-Menten constant K(a) for the binary complex of 260 μM, and a K(b) for the ternary complex of 2100 μM. The catalyzed reaction was fully inhibited by a hapten analogue with a K(i) of 10 μM. The fine specificity of anti-H3 monoclonal antibodies was determined using H3-related compounds with a competitive enzyme immunoassay. Controls demonstrating that catalytic activity is actually related to antibody binding, and mechanistic studies, are also presented.
- Taran,Renard,Bernard,Mioskowski,Frobert,Pradelles,Grassi
-
p. 3332 - 3339
(2007/10/03)
-
- Synthesis of Benzothiazoles. α-Amino-(4-hydroxy-6-benzothiazolyl)propionic Acid.
-
The tentative structure assigned to the photobiologically important skin pigment pheomelanin is based on degradative studies of the natural chromophore.The title compound was reported to be one of several key amino acids isolated in these studies.The identity of this benzothiazole derivative has now been confirmed via an unambiguous eight-step total synthesis starting from 5-methyl-2-nitrophenol.
- Ismail, Ibrahim A.,Sharp, Dale E.,Chedekel, Miles R.
-
p. 2243 - 2246
(2007/10/02)
-