Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Reexamination Certificate
2001-07-18
2004-01-13
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
C424S480000, C424S482000, C514S331000, C514S317000, C546S192000, C546S229000
Reexamination Certificate
active
06676968
ABSTRACT:
TECHNICAL FIELD
The present invention relates to medicinal compositions containing a new compound.
More particularly, the invention relates to medicinal compositions effective for improving the absorption of said new compound through digestive tracts by reducing the contact of the compound with components of bile or pancreatic juice secreted in the duodenum.
BACKGROUND ARTS
Medicinal compositions added with cyclodextrins and lipophilic substances such as medium-chain fatty acid triglycerides were disclosed in the specifications of the JP-A 9-2977 (hereinafter, JP-A means “Japanese Unexamined Patent Application”.) and JP-A 10-231254 as the compositions to improve the absorption of aromatic amidine derivatives through the digestive tracts. However, the long-term safety of cyclodextrins administered by peroral administration is not sufficiently confirmed and the lipophilic substance such as medium-chain triglyceride is possible to cause the adverse effects on the digestive tracts such as diarrhea and the risk of the failure in the barrierness of the digestive tract membrane. Further, the absorption-improving effect shown in these inventions is not expectable to be selective to the compound and have high safety. Specification of WO 98/3202 disclosed a medicinal composition containing an anion exchange resin with respect to aromatic amidine derivatives. However, cholestyramine shown as a preferable example of anion exchange resin in the specification is the active component itself used as a medicine for hyperlipemia and the substance is not expectable as a preferable material from the safety point of view owing to its new physiological action.
No proposal has been made on medicinal compositions containing the compound of the present invention to improve the absorption through the digestive tracts by reducing the contact with the components in the bile or pancreatic juice.
The object of the present invention is to provide medicinal compositions containing the compound of the present invention.
Another object of the present invention is to provide medicinal compositions containing the compound of the present invention and effective for improving the absorption through the digestive tracts by reducing the contact of the compound with the components in the bile or pancreatic juice in the case of peroral administration.
DISCLOSURE OF THE INVENTION
The present invention provides medicinal compositions containing one or more compounds selected from the compounds represented by the following formula (I), salts of these compounds, solvates of these compounds and solvates of these salts (hereinafter collectively called as “the compounds of the present invention” in some cases) and being capable of reducing the contact of the compounds with the components in the bile or pancreatic juice.
[in the Formula (I),
R
1
is hydrogen atom, fluorine atom, chlorine atom, bromine atom, hydroxyl group, amino group, nitro group, a C
1
-C
8
alkyl group or a C
1
-C
8
alkoxy group,
L is direct bond or a C
1
-C
4
alkylene group,
R
2
is fluorine atom, chlorine atom, bromine atom, hydroxyl group, amino group, a C
1
-C
8
alkoxy group, carboxyl group, a C
1
-C
8
alkoxycarbonyl group, an aryloxycarbonyl group, an aralkoxycarbonyl group, carbamoyl group (the nitrogen atom constituting the carbamoyl group may be substituted with mono- or di-C
1
-C
8
alkyl group or may be the nitrogen atom of an amino acid), a C
1
-C
8
alkylcarbonyl group, a C
1
-C
8
alkylsulfenyl group, a C
1
-C
8
alkylsulfinyl group, a C
1
-C
8
alkylsulfonyl group, a mono- or di-C
1
-C
8
alkylamino group, a mono- or di-C
1
-C
8
alkylaminosulfonyl group, sulfo group, phosphono group, bis(hydroxycarbonyl)methyl group, a bis(alkoxycarbonyl)methyl group or 5-tetrazolyl group,
R
3
is hydrogen atom, fluorine atom, chlorine atom, bromine atom, hydroxyl group, amino group, nitro group, a C
1
-C
8
alkyl group, a C
1
-C
8
alkoxy group, carboxyl group or a C
1
-C
8
alkoxycarbonyl group,
X is a group of the formulas —O—, —S—, —SO—, —SO
2
—, —NH—CO—NH—, —N(R
4
)—, —CO—N(R
5
)—, —N(R
5
)—CO—, —N(R
5
)—SO
2
— or —SO
2
—N(R
5
)— (in the formulas,
R
4
is hydrogen atom, a C
1
-C
10
alkyl group, a C
1
-C
10
alkylcarbonyl group, a C
1
-C
10
alkylsulfonyl group, a C
3
-C
8
cycloalkyl group or an aryl group,
R
5
is hydrogen atom, a C
1
-C
10
alkyl group, a C
3
-C
8
cycloalkyl group or an aryl group (the alkyl groups of R
4
and R
5
may be substituted with an aryl group, hydroxyl group, amino group, a halogen atom, a C
1
-C
8
alkoxy group, carboxyl group, a C
1
-C
8
alkoxycarbonyl group, an aryloxycarbonyl group, an aralkoxycarbonyl group, carbamoyl group or 5-tetrazolyl group),
Y is a C
4
-C
8
cycloalkyl group (in the above ring system, the methylene group may be replaced with carbonyl group and the ring system may be substituted with fluorine atom, chlorine atom, bromine atom, hydroxyl group, amino group, a C
1
-C
8
alkyl group, a C
1
-C
8
alkoxy group, carbamoyl group, a C
1
-C
8
alkoxycarbonyl group, carboxyl group, an aminoalkyl group, a mono- or di-alkylamino group or a mono- or di-alkylaminoalkyl group), or a 5- to 8-membered ring group of the following formulas I-1 or I-2
(in the formulas I-1 and I-2,
the methylene group of each ring system may be replaced with carbonyl group and unsaturated bond may be present in the ring,
R
6
is hydrogen atom, fluorine atom, chlorine atom, bromine atom, hydroxyl group, amino group, nitro group, a C
1
-C
8
alkyl group or a C
1
-C
8
alkoxy group,
W is C—H or nitrogen atom (W is not nitrogen atom when the ring is a 5-membered ring),
Z is hydrogen atom, a C
1
-C
10
alkyl group (the alkyl group may be substituted with hydroxyl group (excluding the case of C
1
alkyl group), amino group, a C
1
-C
8
alkoxy group (excluding the case of C
1
alkyl group), carboxyl group, a C
1
-C
8
alkoxycarbonyl group, an aryloxycarbonyl group or an aralkoxycarbonyl group), a C
1
-C
8
alkylcarbonyl group, an arylcarbonyl group, an aralkylcarbonyl group, amidino group or a group of the following formula I-3
(in the Formula I-3,
R
7
is a C
1
-C
8
alkyl group (the alkyl group may be substituted with hydroxyl group or a C
1
-C
8
alkoxy group), an aralkyl group or an aryl group),
m is an integer of from 1 to 3, and
n is an integer of from 0 to 3 (when n is 0 or 1, W is not nitrogen atom)].
BEST MODE FOR CARRYING OUT THE INVENTION
The present invention is explained in more detail by the following description.
In the above definition of the substituent of the compound of the general formula (I) of the present invention, the “C
1
-C
8
alkyl group” means a straight or branched carbon chain having 1 to 8 carbon atoms, for example, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, tert-butyl group, pentyl group, neopentyl group, isopentyl group, 1,2-dimethylpropyl group, hexyl group, isohexyl group, 1,1-dimethylbutyl group, 2,2-dimethylbutyl group, 1-ethylbutyl group, 2-ethylbutyl group, isoheptyl group, octyl group or isooctyl group, preferably a group having a carbon number of from 1 to 4, especially preferably methyl group or ethyl group.
The “C
1
-C
8
alkoxy group” means an alkoxy group having a carbon number of from 1 to 8, concretely methoxy group, ethoxy group, propoxy group, isopropoxy group, butoxy group, isobutoxy group, sec-butoxy group, tert-butoxy group, pentyloxy group, neopentyloxy group, tert-pentyloxy group, 2-methylbutoxy group, hexyloxy group, isohexyloxy group, heptyloxy group, isoheptyloxy group, octyloxy group, isooctyloxy group, etc., preferably a group having a carbon number of from 1 to 4, especially preferably methoxy group or ethoxy group.
The “C
1
-C
4
alkylene” means a straight-chain alkylene having a carbon number of from 1 to 4 and is methylene, ethylene, propylene or butylene.
The “C
1
-C
8
alkoxycarbonyl group” means methoxycarbonyl group, ethoxycarbonyl group, propoxycarbonyl group, isopropoxycarbonyl group, butoxycarbonyl group, isobutoxycarbonyl group, sec-butoxycarbonyl group, tert-butoxycarbonyl group, pentyloxycarbonyl g
Fujinaga Kentaro
Igarashi Yoshiaki
Mitsuhashi Hiroaki
Narasaki Masahiko
Sakon Kiyoyuki
Channavajjala Lakshmi
Page Thurman K.
Teijin Limited
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