1. A compound represented by the formula (I):
wherein
A is an acyl group or an optionally substituted 5- or 6-membered aromatic ring group;
ring M is an optionally fused 5- to 7-membered ring which is optionally further substituted;
as to ring P and ring Q,
(1) ring P is optionally further substituted 5-membered heterocycle, ring Q is optionally further substituted 6-membered ring, and ring P and ring Q are condensed to form an optionally further substituted bicyclic aromatic heterocycle, or
(2) ring P is an optionally further substituted 5-membered non-aromatic ring, ring Q is an optionally substituted 6-membered aromatic ring, and ring P and ring Q are condensed to form an optionally substituted bicyclic non-aromatic ring;
R1 is an optionally substituted C1-6 alkyl group or an optionally substituted C3-6 cycloalkyl group; and
as to L1 and L2,
(1) L1 and L2 are independently optionally substituted methylene, O, S, SO or SO2, or
(2) L1 and L2 in combination form optionally substituted vinylene, or ethynylene,
provided that the following compounds are excluded:
(a) a compound wherein A is an \u03b1-aminoisobutyloyl group; and
(b) a compound wherein A is a 5- or 6-membered aromatic ring group substituted by a group represented by the formula: \u2014CO\u2014(CH2)3\u2014COORA1 wherein RA1 is a hydrogen atom or a C1-6 alkyl group, or a group represented by the formula: \u2014CO\u2014NRA2\u2014CRA3RA4\u2014CRA5RA6\u2014COORA7 wherein RA2, RA3, RA4, RA5 and RA7 are independently a hydrogen atom or a C1-6 alkyl group; and RA6 is a hydrogen atom, a C1-6 alkyl group or a hydroxy group,
or a salt thereof.
2. A compound represented by the formula (I):
wherein
A is an acyl group or an optionally substituted 5- or 6-membered aromatic ring group;
ring M is an optionally fused 5- to 7-membered ring which is optionally further substituted;
ring P is optionally further substituted 5-membered heterocycle, ring Q is optionally further substituted 6-membered ring, and ring P and ring Q are condensed to form an optionally further substituted bicyclic aromatic heterocycle;
R1 is an optionally substituted C1-6 alkyl group or an optionally substituted C3-6 cycloalkyl group;
L1 and L2 are independently optionally substituted methylene, O, S, SO or SO2,
provided that the following compounds are excluded:
(a) a compound wherein A is an \u03b1-aminoisobutyloyl group; and
(b) a compound wherein A is a 5- or 6-membered aromatic ring group substituted by a group represented by the formula: \u2014CO\u2014(CH2)3\u2014COORA1 wherein RA1 is a hydrogen atom or a C1-6 alkyl group, or a group represented by the formula: \u2014CO\u2014NRA2\u2014CRA3RA4\u2014CRA5RA6\u2014COORA7 wherein RA2, RA3, RA4, RA5 and RA7 are independently a hydrogen atom or a C1-6 alkyl group; and RA6 is a hydrogen atom, a C1-6 alkyl group or a hydroxy group,
or a salt thereof.
3. The compound of claim 1, wherein R1 is a C1-6 alkyl group or a C3-6 cycloalkyl group.
4. The compound of claim 1, wherein R1 is a C1-6 alkyl group.
5. The compound of claim 1, wherein A is
(1) a C1-6 alkyl-carbonyl group, or
(2) a 5-membered aromatic heterocyclic group optionally substituted by 1 to 3 substituents selected from (i) a halogen atom and (ii) a C1-6 alkyl group.
6. The compound of claim 1, wherein ring M is a benzene ring or pyridine ring, each of which is optionally substituted by 1 to 3 substituents selected from
(1) a halogen atom,
(2) a C1-6 alkyl group,
(3) a C1-6 alkoxy group optionally substituted by 1 to 3 substituents selected from (i) a halogen atom, (ii) a C1-6 alkoxy group, (iii) a C3-10 cycloalkyl group, (iv) a heterocyclic group and (v) a C6-14 aryl group,
(4) a C3-10 cycloalkoxy group optionally substituted by 1 to 3 substituents selected from (i) a halogen atom and (ii) a C1-6 alkoxy group, and
(5) a hydroxy group.
7. The compound of claim 1, wherein ring P and ring Q are condensed to form
8. The compound of claim 1, wherein
(1) L1 and L2 are independently methylene or O, or
(2) L1 and L2 in combination form ethynylene or vinylene.
9. The compound of claim 1, wherein
A is
(1) a C1-6 alkyl-carbonyl group, or
(2) a 5-membered aromatic heterocyclic group optionally substituted by 1 to 3 substituents selected from (i) a halogen atom and (ii) a C1-6 alkyl group;
R1 is a C1-6 alkyl group;
ring M is
a benzene ring or pyridine ring, each of which is optionally substituted by 1 to 3 substituents selected from
(1) a halogen atom,
(2) a C1-6 alkyl group,
(3) a C1-6 alkoxy group optionally substituted by 1 to 3 substituents selected from (i) a halogen atom, (ii) a C1-6 alkoxy group, (iii) a C3-10 cycloalkyl group, (iv) a heterocyclic group and (v) a C6-14 aryl group,
(4) a C3-10 cycloalkoxy group optionally substituted by 1 to 3 substituents selected from (i) a halogen atom and (ii) a C1-6 alkoxy group, and
(5) a hydroxy group;
ring P and ring Q are condensed to form
and
as to L1 and L2,
(1) L1 and L2 are independently methylene or O, or
(2) L1 and L2 in combination form ethynylene or vinylene.
10. N-{(1S)-1-(2S)-6-{4-(Cyclopropylmethoxy)-2-fluorobenzyloxy}-2,3-dihydro-1-benzofuran-2-ylethyl}acetamide or a salt thereof.
11. N-1-(5-{6-(Cyclopropylmethoxy)-4-fluoropyridin-3-ylmethoxy}-1-benzofuran-2-yl)ethylacetamide or a salt thereof.
12. N-(1-{6-2-(4-Ethoxyphenyl)ethyl-1-benzofuran-2-yl}ethyl)acetamide or a salt thereof.
13. N-1-(5-{4-(Cyclopropylmethoxy)benzyloxy}-1-benzofuran-2-yl)ethylacetamide or a salt thereof.
14. A prodrug of the compound of claim 1.
15. A medicament comprising the compound of claim 1 or a prodrug thereof.
16. The medicament of claim 15, which is an acetyl-CoA carboxylase inhibitor.
17. The medicament of claim 15, which is an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia or cancer.
18. A method for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia or cancer in a mammal, which comprises administering an effective amount of the compound of claim 1 or a prodrug thereof to the mammal.
19. (canceled)
The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.
What is claimed is:
1. A ceramic sculpture for storing and releasing fragrance, comprising:
a bowl-like body with a indentation at the bottom thereof, the bowl-like body being formed with a layer of vapor permeation barrier on the surface of the indentation;
an unglazed ceramic base disposed in the indentation; and
a fragrant substance that is absorbed and retained by the base while fragrance is released from the surface of the base.
2. The ceramic sculpture as set forth in claim 1, wherein a space is formed between the surface of the said indentation and the base embedded into this indentation.
3. The ceramic sculpture as set forth in claim 2, wherein a refractory wool is inserted into the said space.
4. The ceramic sculpture as set forth in claim 1, wherein the base is formed with small holes to allow injection of fragrant substances into the base andor the refractory wool.
5. The ceramic sculpture as set forth in claim 1, wherein the vapor permeation barrier formed on the surface of the indentation is a layer of glaze.
6. The ceramic sculpture as set forth in claims 1, wherein the fragrant substance is an essence.
7. The method of making the ceramic sculpture for storing and releasing fragrance as set forth in claim 1, comprising the steps of:
preparing the main body of the unglazed ceramic sculpture and the unglazed base separately,
glazing the surface of the indentation.
inserting the base into the indentation of the ceramic sculpture and seal with porcelain clay;
burning the unglazed ceramic body at a temperature of the least 1050 C.;
injecting the fragrant substance into the base under a high pressure after the burnt sculpture has cooled down, so that the base is completely filled with the fragrant substance.
8. The method as set forth in claim 7, wherein the remaining portion of the ceramic sculpture other than the indentation is to be coated with glaze upon completion of inserting the base into the indentation of the ceramic sculpture and seal with porcelain clay.
9. The method as set forth in claim 7, wherein the base is formed with small holes through which the essence is injected.
10. The method as set forth in claim 7, wherein the refractory wool is inserted when the base is embedded into the indentation.
11. The method as set forth in claim 7, wherein both the base and the refractory wool are injected with essence.