[EN] 5-MEMBERED HETEROARYL COMPOUNDS CONTAINING A HYDROXAMATE MOIETY AND THEIR USE [FR] COMPOSÉS HÉTÉROARYLES À 5 CHAÎNONS CONTENANT UNE FRACTION HYDROXAMATE ET LEUR UTILISATION
SUBSTITUTED CARBAMOYLCYCLOALKYL ACETIC ACID DERIVATIVES AS NEP
申请人:KARKI Rajeshri Ganesh
公开号:US20120122764A1
公开(公告)日:2012-05-17
The present invention provides a compound of formula I;
or a pharmaceutically acceptable salt thereof, wherein R
1
, R
2
, R
3
, R
4
, R
5
, B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.
Triprenyl phenol compound, process for production of triprenyl phenol compound, and thrombolysis enhancer
申请人:Hasumi Keiji
公开号:US20090216028A1
公开(公告)日:2009-08-27
The present invention provides a triprenyl phenol compound represented by the following formula (II) and (III) and having a thrombolysis-enhancing activity, and an efficient method for producing the triprenyl phenol compound. In formula (II) and (III), R
1
represents an aromatic group having as a substituent or as a part of a substituent at least one member selected from the group consisting of a carboxyl group, a hydroxyl group, a sulfonic acid group and a secondary amino group, or an aromatic group which comprises a secondary amino group and may comprise nitrogen; R
4
in the general formula (III) represents an aromatic amino acid residue represented by the general formula (III-1) below; X represents —CHY—(CH
3
)
2
Z; and Y and Z are respectively —H or —OH or together form a single bond: (III-1) wherein R
5
represents a hydroxyl group which may be present or absent; and n represents an integer of 0 or 1.
TRIPRENYL PHENOL COMPOUND, PROCESS FOR PRODUCTION OF TRIPRENYL PHENOL COMPOUND, AND THROMBOLYSIS ENHANCER
申请人:HASUMI Keiji
公开号:US20120100579A1
公开(公告)日:2012-04-26
A triprenyl phenol compound represented by the following formula (II) and (III) and having a thrombolysis-enhancing activity, and an efficient method for producing the triprenyl phenol compound. In formula (II) and (III), R
1
represents an aromatic group having as a substituent or as a part of a substituent at least one member selected from the group consisting of a carboxyl group, a hydroxyl group, a sulfonic acid group and a secondary amino group, or an aromatic group which comprises a secondary amino group and may comprise nitrogen; R
4
in the general formula (III) represents an aromatic amino acid residue represented by the general formula (III-1) below; X represents —CHY—(CH
3
)
2
Z; and Y and Z are respectively —H or —OH or together form a single bond: (III-1) wherein R
5
represents a hydroxyl group which may be present or absent; and n represents an integer of 0 or 1.
Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving Chymase.
公开了小分子抑制剂,可用于治疗涉及Chymase的各种疾病和病况。
TRANYLCYPROMINE DERIVATIVES AS INHIBITORS OF HISTONE DEMETHYLASES LSD1 AND/OR LSD2
申请人:Minucci Saverio
公开号:US20130035377A1
公开(公告)日:2013-02-07
Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and R
3
are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof.