Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
1998-05-06
2002-03-12
Coleman, Brenda (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C514S063000, C514S217050, C514S228200, C514S228800, C514S233200, C540S598000, C544S058400, C544S096000, C544S114000, C544S229000, C544S238000
Reexamination Certificate
active
06355640
ABSTRACT:
TECHNICAL FIELD
The present invention relates to a novel pyrazolopyridine compound or a pharmaceutically acceptable salt thereof which are useful as a medicament.
1. Background Art
Some pyrazolopyridine compounds to be useful as psychostimulant, antihypertensive agent, remedy for renal failure, diuretics or the like are known (e.g. EP-0299209, EP-0379979, etc).
2. Disclosure of Invention
The present invention relates to a novel pyrazolopyridine compound and a pharmaceutically acceptable salt thereof useful as a medicament; the processes for the preparation of said pyrazolopyridine compound or a salt thereof; a pharmaceutical composition comprising, as an active ingredient, said pyrazolopyridine compound or a pharmaceutically acceptable salt thereof; a use of said pyrazolopyridine compound or a pharmaceutically acceptable salt thereof as a medicament; and a method for using said pyrazolopyridine compound for the therapeutic purpose, which comprises administering said pyrazolopyridine compound or a pharmaceutically acceptable salt thereof to a human being or an animal.
The pyrazolopyridine compound or a pharmaceutically acceptable salt thereof is an adenosine antagonist (especially, A
1
receptor antagonist) and possesses various pharmacological actions such as cognitive enhancing action, analgesic action, locomotor action, antidepressant action, diuretic action, cardioprotective effect, cardiotonic action, vasodilating action (e.g. cerebral vasodilating action, etc), the action of increasing the renal blood flow, renal protective effect, improvement of renal function, enhancing action of lipolysis, inhibition of anaphylactic bronchoconstriction, acceleration of the insulin release, the action of increasing the production of erythropoietin, inhibiting action of platelet aggregation, or the like; useful as cognitive enhancer, antidementia drug, psychostimulant, analgesic, cardioprotective agent, antidepressant, ameliorants of cerebral circulation, tranquilizer, drug for heart failure, cardiotonic agent, antihypertensive agent, drug for renal failure (renal insufficiency), drug for renal toxicity, renal protective agent, drug for improvement of renal function, diuretic, drug for edema, antiobesity, antiasthmatic, bronchodilator, drug for apnea, drug for gout, drug for hyperuricemia, drug for sudden infant death syndrome (SIDS), ameliorants of immunosuppressive action of adenosine, antidiabetic agent, drug for ulcer, drug for pancreatitis, drug for Ménière's syndrome, drug for anemia; drug for thrombosis, drug for myocardial infarction, drug for obstruction, drug for arteriosclerosis obliterans, drug for thrombophlebitis, drug for cerebral infarction, drug for transient ischemic attack, drug for angina pectoris, or the like; and useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, etc), anxiety, pain, cerebrovascular disease (e.g. stroke, etc), heart failure; hypertension (e.g. essential hypertension, nephrogenous hypertension, etc); circulatory insufficiency (acute circulatory insufficiency) cuased by, for example, the ischemia/reperfusion injury (e.g. myocardial ischemia/reperfusion injury, cerebral ischemia/reperfusion injury, peripheral ischemia/reperfusion injury, etc), shock (e.g. endotoxin shock, hemorrhagic shock, etc), surgical procedure, or the like; post-resuscitation asystole; bradyarrhythmia; electro-mechanical dissociation; hemodynamic collapse; SIRS (systemic inflammatory response syndrome); multiple organ failure; renal failure (renal insufficiency) (e.g. acute renal failure, etc), renal toxicity [e.g. renal toxicity induced by a drug such as cisplatins, gentamicin, FR-900506 (disclosed in EP-0184162), cyclosporin (e.g. cyclosporin A) or the like; glycerol, etc], nephrosis, nephritis, edema (e.g. cardiac edema, nephrotic edema, hepatic edema, idiopathic edema, drug edema, acute angioneurotic edema, hereditary angioneurotic edema, carcinomatous ascites, gestational edema, etc); obesity, bronchial asthma, gout, hyperuricemia, sudden infant death syndrome, immunosuppression, diabetes, ulcer such as peptic ulcer (e.g. gastric ulcer, duodenal ulcer, etc), pancreatitis, Ménière's syndrome, anemia; myocardial infarction, thrombosis (e.g. arterial thrombosis, cerebral thrombosis, etc), obstruction, arteriosclerosis obliterans, thrombophlebitis, cerebral infarction, transient ischemic attack, angina pectoris, or the like.
The novel pyrazolopyridine compound of the present invention can be shown by the following formula (I).
wherein R
1
is aryl, and
R
2
is cyclo(lower)alkyl which may have one or more suitable substituent(s);
cyclo(lower)alkenyl which may have one or more suitable substituent(s);
lower alkyl substituted with aryl and acyl;
aryl which may have one or more suitable substituent(s);
saturated 3 to 8-memberd heteromonocyclic group containing 1 to 4 nitrogen atom(s) which may have one or more suitable substituent(s);
unsaturated 3 to 8-membered heteromonocyclic group containing 1 to 4 nitrogen atom(s) which may have one or more suitable substituent(s);
saturated 3 to 8-membered heteromonocyclic group containing 1 to 4 oxygen atom(s) which may have one or more suitable substituent(s); or
saturated condensed heterocyclic group containing 1 to 4 oxygen atom(s) which may have one or more suitable substituent(s).
The object compound (I) or a salt thereof of the present invention can be prepared by the following reaction schemes.
wherein
R
1
and R
2
are each as defined above,
R
a
2
is cyclo(lower)alkyl having oxo, which may have one or more suitable substituent(s);
cyclo(lower)alkenyl having oxo, which may have one or more suitable substituent(s);
saturated 3 to 8-membered heteromonocyclic group containing 1 to 4 nitrogen atom(s) having oxo, which may have one or more suitable substituent(s);
unsaturated 3 to 8-membered heteromonocyclic group containing 1 to 4 nitrogen atom(s) having oxo, which may have one or more suitable substituent(s);
saturated 3 to 8-membered heteromonocyclic group containing 1 to 4 oxygen atom(s) having oxo, which may have one or more suitable substituent(s); or saturated condensed heterocyclic group containing 1 to 4 oxygen atom(s) having oxo, which may have one or more suitable substituent(s);
R
b
2
is cyclo(lower)alkyl having hydroxy, which may have one or more suitable substituent(s);
cyclo(lower)alkenyl having hydroxy, which may have one or more suitable substituent(s);
saturated 3 to 8-membered heteromonocyclic group containing 1 to 4 nitrogen atom(s) having hydroxy, which may have one or more suitable substituent(s);
unsaturated 3 to 8-membered heteromonocyclic group containing 1 to 4 nitrogen atom(s) having hydroxy, which may have one or more suitable substituent(s);
saturated 3 to 8-membered heteromonocyclic group containing 1 to 4 oxygen atom(s) having hydroxy, which may have one or more suitable substituent(s); or
saturated condensed heterocyclic group containing 1 to 4 oxygen atom(s) having hydroxy, which may have one or more suitable substituent(s);
R
c
2
is cyclo(lower)alkyl having oxo, which may have one or more suitable substituent(s); or
cyclo(lower)alkenyl having oxo, which may have one or more suitable substituent(s),
R
d
2
is cyclo(lower)alkyl having lower alkylidene, which may have one or more suitable substituent(s);
cyclo(lower)alkyl having acyl(lower)alkylidene, which may have one or more suitable substituent(s);
cyclo(lower)alkyl having cyano(lower)alkylidene, which may have one or more suitable substituent(s);
cyclo(lower)alkyl having heterocyclic(lower)alkylidene, which may have one or more suitable substituent(s);
cyclo(lower)alkenyl having lower alkylidene, which may have one or more suitable substituent(s);
cyclo(lower)alkenyl having acyl(lower)alkyl, which may have one or more suitable substituent(s);
cyclo(lower)alkenyl having acyl(lower)alkylidene, which may have one or more suitable substituent(s);
cyclo(lower)alkenyl having cyano(lower)alkylidene, which may have one or more suitable subs
Akahane Atsushi
Durkin Kieran P. M.
Itani Hiromichi
Nishimura Shintaro
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