- DIPEPTIDE ANALOGS AS TGF-BETA INHIBITORS
-
The present disclosure is concerned with dipeptide analogs that are capable of inhibiting TGF-β and methods of treating cancers such as, for example, multiple myeloma and a hematologic malignancy, methods for immunotherapy, and methods of treating fibroti
- -
-
Paragraph 0457-0458; 0462
(2019/05/15)
-
- 4-Isopropyl-6-methoxyphenyl glucitol compound
-
A compound, which inhibits SGLT1 (sodium-dependent glucose transporter 1) activity to suppress absorption of glucose or the like, thereby suppressing abnormal glucose tolerance or postprandial hyperglycemia in diabetes, is provided. Specifically, a 4-isopropyl-6-methoxyphenyl glucitol compound represented by the following formula (I), or a pharmaceutically acceptable salt thereof, is provided:
- -
-
Paragraph 0088
(2015/11/16)
-
- 4-ISOPROPYL-6-METHOXYPHENYL GLUCITOL COMPOUND
-
A compound, which inhibits SGLT1 (sodium-dependent glucose transporter 1) activity to suppress absorption of glucose or the like, thereby suppressing abnormal glucose tolerance or postprandial hyperglycemia in diabetes, is provided. Specifically, a 4-isopropyl-6-methoxyphenyl glucitol compound represented by the following formula (I), or a pharmaceutically acceptable salt thereof, is provided:
- -
-
Paragraph 0159; 0160; 0161
(2013/07/05)
-
- PYRIDINE DERIVATIVES AS SODIUM CHANNEL BLOCKERS
-
Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein; each of R1 to R4 is independently selected from hydrogen and C1-4 alkyl, and each of rings A and B independently is optionally further substi
- -
-
Page/Page column 26
(2010/11/30)
-
- Methods and compositions for treating amyloid-related diseases
-
Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
- -
-
Page/Page column 157
(2010/11/24)
-
- NITROGENOUS FUSED-RING DERIVATIVES, MEDICINAL COMPOSITIONS CONTAINING THE DERIVATIVES, AND USE THEREOF AS DRUGS
-
The present invention provides nitrogen-containing fused-ring derivatives represented by the following general formula, or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, in the formula R 1 represent H, an optionally substituted alkyl group, an alkenyl group, etc.; R 2 represent H, a halogen atom or an alkyl group; R 3 and R 4 represent H, OH, a halogen atom, an optionally substituted alkyl group, etc. ; Y represents CH or N; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G-1)or(G-2) (in which E 1 represents H, F or OH; and E 2 represents H, F, a methyl group, etc.), and pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.
- -
-
Page/Page column 34
(2010/11/24)
-
- PYRAZOLE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE FOR PRODUCTION THEREOF
-
The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents a single bond, a C1-6 alkylene group etc. ; Z represents CO or SO2; R4 and R5 represent H, an optionally substituted C1-6 alkyl group etc.; and R3, R6 and R7 represent H, a halogen atom etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT1 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.
- -
-
Page/Page column 33
(2008/06/13)
-
- PYRAZOLE DERIVATIVES, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE FOR PRODUCTION THEREOF
-
The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents an optionally substituted C1-6 alkylene group etc.; Z represents -RB, -CORC etc. in which RB represents an optionally substituted C1-6 alkyl group etc.; and RC represents an optionally substituted C1-6 alkyl group etc.,; R4 represents H, an optionally substituted C1-6 alkyl group etc.; and R3, R5 and R6 represent H, a halogen atom etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT1 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, impaired glucose tolerance, impaired fasting glycemia, diabetic complications or obesity, and a disease associated with the increase of blood galactose level such as galactosemia, and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.
- -
-
Page/Page column 43
(2010/02/12)
-
- Substituted 2-aminoacetamides and the use thereof
-
This invention is related to substituted 2-aminoacetamides represented by formula (II): or a pharmaceutically acceptable salt or prodrug thereof, wherein the substituents are defined herein. The invention also is directed to the use of substituted 2-amino
- -
-
-
- Substituent effect on acidity of substituted 2-(4-nitrobenzoylamino)alkanamidesin methanol-dimethyl sulfoxide mixtures
-
The dissociation constants of substituted 2-(4-nitrobenzoylamino)alkanamides, N-[2-(4-nitrobenzoylamino)aikanoyl]pyrrolidines, and N-alkyl-4-nitrobenzamides have been measured spectrophotometrically in 60 and 80% v/v DMSO. The pKA values of these N-acids are discussed from the point of view of substituents at the acetamide a-carbon atom.
- Mitas, Petr,Sedlak, Milos,Kavalek, Jaromir
-
-
- α-Aminonitrile hydration in the presence of hydrogen peroxide in aqueous basic medium
-
α-Aminonitriles are hydrated into α-aminoamides in the presence of hydrogen peroxide in sodic or ammoniacal basic medium. While the hydration mechanism is close to the mechanism described previously in the case of aromatic nitrites, we showed that, in weakly basic conditions, the amine function of α-aminonitrile is competitively oxidized via a peroxyimidic acid by an intramolecular process. In the case of 2-aminopropanenitrile, this reaction leads to pyruvamide oxime. Furthermore, the study of structurereactivity relationships in the hydration of aliphatic and aromatic monofunctional nitriles and α-aminonitriles showed that the reactivity of the substrates towards hydroperoxide onion, which mostly depends on inductive effects of the substituents, is sufficiently enhanced to allow hydration of tertiary α-aminonitriles with low steric hindrance and regioselective hydration of dissymmetric α-aminodinitriles. Eisevier,.
- Taillades, Jacques
-
-
- SYNTHESIS OF α-AMINOAMIDES AND α-AMINO ACIDS FROM α-AMINONITRILES
-
The transformations of α-aminonitriles in the presence of water and manganese(IV) oxide were investigated for the case of 2-amino-2-methylpropionitrile and 2-amino-2-methylbutyronitrile.The conditions for highly selective synthesis of α-aminoamides and α-amino acids from the corresponding α-aminonitriles were determined.
- Zil'berman, E. N.,Eremeev, I. V.,Abramov, A. V.
-
p. 1243 - 1247
(2007/10/02)
-
- SYSTEMES DE STRECKER ET APPARENTES-XII. CATALYSE PAR LES ALDEHYDES DE L'HYDRATATION INTRAMOLECULAIRE DES α-AMINONITRILES
-
Aqueous basic hydration of α-aminopropionitrile is first order either in acetaldehyde (formed by decomposition of α-aminopropionitrile) or different aldehydes added in the medium.The rate determining step involves a rapid preequilibrium in which the catal
- Pascal, R.,Taillades, J.,Commeyras, A.
-
p. 2999 - 3008
(2007/10/02)
-
- Imidazoisoindolediones and the use thereof as herbicidal agents
-
The invention relates to novel imidazoisoindoledione compounds including the optical isomers thereof. This invention also relates to a method for the control of undesirable plant species with the imidazoisoindolediones and their optical isomers, and further, to a process for the preparation of the compounds.
- -
-
-
- Dihydroimidaz oisoindolediones and the use thereof as herbicidal agents
-
The invention relates to novel dihydroimidazoisoindoledione compounds and the optical and stereo isomers thereof. This invention also relates to a method for the control of undesirable plant species with the dihydroimidazoisoindolediones and their optical and stereo isomers, and further, to a process for the preparation of the compounds.
- -
-
-
