Ketone derivatives and medical application thereof

Details Ketone derivatives and medical application thereof Ketone derivatives and medical application thereof

1999-10-19

2001-04-10

Lambkin, Deborah C. (Department: 1613)

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

C562S463000, C568S337000, C514S570000, C514S545000, C514S689000

Reexamination Certificate

active

06215016

ABSTRACT:

TECHNICAL FIELD
The present invention relates to ketone derivatives and an agent having the ketone derivatives or pharmaceutically acceptable salts thereof as an active ingredient, and in particular, relates to a hematopoietic agent.
BACKGROUND ART
Ketone derivatives include lactones and lactams. For example, carolic acid and carolynic acid are known as natural lactones and compounds disclosed in J. Chem. Soc. Perkin Trans. I, 14, 1485-1491 (1976) and Synth. Comm., 22(6), 809-816 (1992) are known as non-naturally derived compounds. In addition, compounds disclosed in J. Org. Chem., 40(13), 1927 (1975), Tetrahedron Lett., 33, 2821 (1975), Chem. Pharm. Bull., 32, 3724 (1984), Tetrahedron Lett., 163 (1973), and the like are known as compounds having the following general formula (I′) wherein R
4
is an ester group:
Lactams of the general formula (I) wherein X is nitrogen are disclosed in Japanese Patent Laid-Open Nos. 2-279691, 4-49289, 2-48591, and 1-313488, Chem. Pharm. Bull., 32(10), 4197-4204 (1984), Pharmazie, 43(7), 473-474 (1988), Monatsh. Chem., 123(1-2), 93-98 (1992), J. Inorg. Biochem., 24(3), 167-181 (1985), J. Am. Chem. Soc., 107(18), 5219-5224 (1985), J. Org. Chem., 50 (8), 1344-1346 (1985), and Chem. Rev., 95, 1981-2001 (1995).
Applications of lactones include, for example, a compound disclosed in Japanese Patent Laid-Open No.5-43568 and EP 0508690, which is known as an anti-inflammatory agent inhibiting phospholipase A2, a compound disclosed in Archive des Pharmazie (Weinhelm, Ger.) (1983), 316(2), 115-120, which is known as an anticoagulant, and a compound disclosed in Journal of Antibiotics (1994), 47(2), 143-7, which is known as an anti-AIDS agent inhibiting HIV-protease.
Applications of lactams include, for example, a compound disclosed in Chem. Pharm. Bull., 32(10), 4197-4204 (1984), which is known as an agent having antibacterial activity, and a compound disclosed in J. Antibiot., 33(2), 173-181 (1980), which is known as an anaerobic antibiotic. However, no ketone derivative has been known to have hematopoietic activity.
An object of the present invention is to provide ketone derivatives, medical agents which have such ketone derivatives or pharmaceutically acceptable salts thereof as an active ingredient, in particular, a hematopoietic agent used for preventing or treating cytopenia caused by cancer chemotherapy, radiation therapy, bone-marrow transplantation, drug therapy, immunological disorders, anemia, or the like.
DISCLOSURE OF INVENTION
The above-mentioned object is achieved by the following present invention. In other words, the present invention relates to: a medical agent composed of a ketone derivative of the following general formula (I) or a pharmacologically acceptable salt thereof
In the above general formula (I), R
1
is a hydrogen atom, a halogen atom, a hydrocarbon group having 1 to 19 carbon atoms (in which the hydrocarbon group may have one or more substituents selected from the group essentially consisting of a chlorine atom, a bromine atom, a fluorine atom, a hydroxy group, a nitro group, a methoxy group, an ethoxy group, a carboxyl group, a carboethoxy group, a carbomethoxy group, and a cyano group),
—CO(CH
2
)
q
Q (wherein q is an integer of from 0 to 10 and Q is a hydrogen atom, a hydrocarbon group having 1 to 6 carbon atoms (in which the hydrocarbon group may have one or more substituents selected from the group essentially consisting of a chlorine atom, a bromine atom, a fluorine atom, a hydroxy group, a nitro group, a methoxy group, an ethoxy group, a carboxyl group, a carboethoxy group, a carbomethoxy group, a cyano group, a trifluoromethyl group, a methylthio group, a phenylthio group, and a t-butyl group), a heterocyclic ring having 1 to 9 carbon atoms (in which the heterocyclic ring may have one or more substituents selected from the group essentially consisting of a chlorine atom, a bromine atom, a fluorine atom, a hydroxy group, a nitro group, a methoxy group, and an ethoxy group), a hydroxy group, a thiol group, a thioether group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, an acetyl group, an amino group, an acetamido group, a cyano group, a carboxyl ester group (in which the ester portion has 1 to 6 carbon atoms), a carboxyl group, a phosphoric ester group (in which the ester portion has 2 to 6 carbon atoms), a phosphoric group, a sulfonyl group having 1 to 7 carbon atoms, a t-butoxycarbonylamino group, a methylsulfoxide group, a primary amido group, or a secondary amido group),
—COCO(CH
2
)
r
V
3
(wherein r is an integer of 0 or 1 and V
3
is a hydrogen atom, a linear or branched alkyl group having 1 to 6 carbon atoms, an aryl group having 6 to 12 carbon atoms (in which the aryl group may have one or more substituents selected from the group essentially consisting of a chlorine atom, a bromine atom, a fluorine atom, a hydroxy group, a nitro group, a methoxy group, an ethoxy group, a carboxyl group, a carboethoxy group, a carbomethoxy group, and a cyano group), a heterocyclic ring having 1 to 9 carbon atoms (in which the heterocyclic ring may have one or more substituents selected from the group essentially consisting of a chlorine atom, a bromine atom, a fluorine atom, a hydroxy group, a nitro group, a methoxy group, and an ethoxy group), a hydroxy group, a thiol group, a thioether group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, an acetyl group, an amino group, an acetamido group, a cyano group, a carboxyl ester group (in which the ester portion has 1 to 6 carbon atoms), a carboxyl group, a primary amido group, or a secondary amido group),
—COCH═CHV
4
(wherein V
4
is an aryl group having 6 to 12 carbon atoms (in which the aryl group may have one or more substituents selected from the group essentially consisting of a chlorine atom, a bromine atom, a hydroxy group, a nitro group, a methoxy group, an ethoxy group, a carboxyl group, a carboethoxy group, a carbomethoxy group, a cyano group, a trifluoromethyl group, a methylthio group, and a phenylthio group) or a heterocyclic ring having 1 to 9 carbon atoms (in which the heterocyclic ring may have one or more substituents selected from the group essentially consisting of a chlorine atom, a bromine atom, a fluorine atom, a hydroxy group, a nitro group, a methoxy group, and an ethoxy group),
—CO
2
G (wherein G is a hydrogen atom, a linear or branched alkyl group having 1 to 6 carbon atoms, or an aryl group having 6 to 12 carbon atoms (in which the aryl group may have one or more substituents selected from the group essentially consisting of a chlorine atom, a bromine atom, a hydroxy group, a nitro group, a methoxy group, an ethoxy group, a carboxyl group, a carboethoxy group, a carbomethoxy group, a cyano group, a trifluoromethyl group, a methylthio group, and a phenylthio group),
—CONHV
1
(wherein V
1
is a hydrogen atom, a linear or branched alkyl group having 1 to 10 carbon atoms, an aryl group having 6 to 12 carbon atoms (in which the aryl group may have one or more substituents selected from the group essentially consisting of a chlorine atom, a bromine atom, a fluorine atom, a hydroxy group, a nitro group, a methoxy group, an ethoxy group, a carboxyl group, a carboethoxy group, a carbomethoxy group, and a cyano group), or a heterocyclic ring having 1 to 9 carbon atoms (which heterocyclic ring may have one or more substituents selected from the group essentially consisting of a chlorine atom, a bromine atom, a fluorine atom, a hydroxy group, a nitro group, a methoxy group, and an ethoxy group),
—NHCOV
2
(wherein V
2
is a hydrogen atom, a linear or branched alkyl group having 1 to 10 carbon atoms, an aryl group having 6 to 12 carbon atoms (in which the aryl group may have one or more substituents selected from the group essentially consisting of a chlorine atom, a bromine atom, a fluorine atom, a hydroxy group, a nitro group, a methoxy group, an ethoxy group, a carboxyl group, a carboethoxy group, a carbomethoxy group, and a cyano group), or heterocyclic ring having 1 to 9 carbon atoms (in which th

Affiliated with

Also associated with

Rating

Ketone derivatives and medical application thereof does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Ketone derivatives and medical application thereof, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Ketone derivatives and medical application thereof will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2465184