Isoquinolinamine and phthalazinamine derivatives which...

Details Isoquinolinamine and phthalazinamine derivatives which... Isoquinolinamine and phthalazinamine derivatives which...

1999-09-20

2001-05-22

Davis, Zinna Northington (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C546S143000

Reexamination Certificate

active

06235752

ABSTRACT:

This invention provides novel compounds of Formula I which interact with CRF receptors.
The invention provides pharmaceutical compositions comprising compounds of Formula I. It further relates to the use of such compounds in treating stress related disorders such as post traumatic stress disorder (PTSD) as will as depression, headache and anxiety. Accordingly, a broad embodiment of the invention is directed to a compound of Formula I:
wherein
Ar is phenyl, 1- or 2-naphthyl, 2-, 3-, or 4-pyridinyl, 2- or 3-thienyl, 4- or 5-pyrimidinyl, each of which is mono-, di-, or trisubstituted with halogen, hydroxy, C
1
-C
6
alkyl, or C
1
-C
6
alkoxy, with the proviso that at least one of the positions on Ar ortho to the point of attachment to the phthalazinamine or isoquinolinamine ring is substituted;
R
1
and R
2
are the same or different and represent hydrogen, C
1
-C
6
alkyl, halogen, hydroxy, C
1
-C
6
alkoxy, NH
2
, NH(C
1
-C
6
alkyl), N(C
1
-C
6
alkyl)
2
, NO
2
, cyano, trifluoromethyl;
R
3
and R
4
are the same or different and represent
C
1
-C
6
alkyl optionally substituted with halogen, hydroxy, or C
1
-C
6
alkoxy; or C
1
-C
6
alkylaryl, where aryl is phenyl, 1- or 2-naphthyl, 2-, 3-, or 4-pyridinyl, 2- or 3-thienyl or 2-, 4-, or 5-pyrimidinyl, each of which is optionally mono- or disubstituted with halogen, hydroxy, C
1
-C
6
alkyl, C
1
-C
6
alkoxy; or C
1
-C
6
alkyl-Y-R
5
, wherein Y is O, S NH, N(C
1
-C
6
alkyl), and R
5
is hydrogen or C
1
-C
6
alkyl; and
W is N or C-R
6
, where in R
6
is hydrogen or C
1
-C
6
alkyl.
These compounds are highly selective partial agonists or antagonists of CRF receptors and are useful in the diagnosis and treatment of stress related disorders such as post traumatic stress disorder (PTSD) as well as depression and anxiety.
The invention further encompasses methods for treating mammals, such as, for example, humans and companion animals (i.e., cats and dogs) suffering from PTSD, depression, and/or anxiety. Such methods comprise administering to a patient mammal an amount effective of a compound of Formula I to relieve the depression, anxiety or PTSD.


REFERENCES:
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patent: 3753988 (1973-08-01), Rodway et al.
patent: 4956371 (1990-09-01), Shoupe et al.
patent: 2 063 249 (1981-06-01), None
patent: 1 303 061 (1993-01-01), None
patent: 3-284669 (1991-12-01), None
Sindler-Kulyk, M. et al., “Photocycloaddition Reactions of 3-Phenyl-1, 2-benzisothiazole and Alkynes”, Journal of Org. Chem., vol. 48 No. 8, 1983, pp. 1275-1281.
Holava, H. M. Jr. et al., “1-Substituted 4-Aryl-(or 4-Aralkyl-) phthalazines”, New Compounds, vol. 12, 1969, pp. 555-556.

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