US2005026920A1PendingUtilityA1
Diaryl compounds
Est. expiryAug 16, 2022(expired)· nominal 20-yr term from priority
C07D 213/70C07D 213/38
50
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Claims
Abstract
The invention relates to compounds of formula I
Claims
exact text as granted — not AI-modified1 - 12 . (canceled)
13 . The method according to claim 16 , wherein the disorder is selected from hypertension, depression, generalized anxiety disorder, phobias, post-traumatic stress syndrome, avoidant personality disorder, sexual dysfunction (including premature ejaculation and male impotence), eating disorders, obesity, substance abuse disorders (including chemical dependencies), cluster headache, migraine, pain, Alzheimer's disease, obsessive-compulsive disorder, panic disorder, memory disorders, Parkinson's diseases, endocrine disorders, vasospasm, cerebellar ataxia, gastrointestinal tract disorders, negative symptoms of schizophrenia, premenstrual syndrome, fibromyalgia syndrome, stress incontinence, Tourette's syndrome, trichotillomania, kleptomania, attention deficit hyperactivity disorder (ADHD), chronic paroxysmal hemicrania, headache (associated with vascular disorders), emotional lability, pathological crying, sleeping disorder (cataplexy) and shock.
14 . The method according to claim 13 wherein the disorder is selected from depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress syndrome, substance abuse disorders and sexual dysfunction, including premature ejaculation and male impotence.
15 . The method according to claim 14 wherein the disorder is premature ejaculation.
16 . A method of treating a disorder in which the regulation of monoamine transporter function is implicated by administering a compound of Formula (I),
wherein;
X is S or CH 2 ;
L and U, which may be the same or different, are —N—, —N + (—O − )— or —C(H)—;
M and Q, which may be the same or different, are —N—, —N + (—O − )— or —C(R 4 )—;
wherein ring A contains 1 or 2 nitrogen atoms, and wherein when L, U, M or Q is —N + (—O − )—, ring A contains no other nitrogen atom;
R 1 and R 2 , which may be the same or different, are hydrogen, C 1 -C 6 alkyl, (CH 2 ) m (C 3 -C 6 cycloalkyl) wherein m=0, 1, 2 or 3, or R 1 and R 2 together with the nitrogen to which they are attached form an azetidine ring;
W, Y and Z, which may be the same or different, are hydrogen, halogen, C 1- C 6 alkyl, CF 3 , OCF 3 , C 1- C 4 alkylthio or C 1- C 4 alkoxy; or Y and Z are linked so that, together with the interconnecting atoms, Y and Z form a fused 5 to 7-membered carbocyclic or heterocyclic ring which may be saturated, unsaturated or aromatic, and wherein when Y and Z form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; and wherein W, Y and Z are not all hydrogen; and
each R 4 is independently:
—(CH 2 ) p —R 5 ;
where p is 0, 1 or 2;
R 5 is hydrogen, CONR 6 R 7 , SO 2 NR 6 R 7 , SO 2 NHC(═O)R 6 , hydroxy, C 1- C 4 alkoxy, NR 8 SO 2 R 9 , NO 2 , NR 6 R 11 , CN, CO 2 R 10 , SR 10 , S(O)R 9 or SO 2 R 10 ; R 6 , R 7 , R 8 and R 10 which may be the same or different, are hydrogen or C 1 -C 6 alkyl optionally substituted independently by one or more R 12 ; R 9 is C 1- C 6 alkyl optionally substituted independently by one or more R 12 ; R 11 is hydrogen, C 1- C 6 alkyl optionally substituted independently by one or more R 12 , C(O)R 6 , CO 2 R 9 , C(O)NHR 6 or SO 2 NR 6 R 7 ; R 12 is fluoro, hydroxy, CO 2 H, C 3- C 6 cycloalkyl, NH 2 , CONH 2 , C 1- C 6 alkoxy, C 1- C 6 alkoxycarbonyl or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O optionally substituted independently by one or more R 13 ; or R 6 and R 7 , together with the nitrogen to which they are attached, form a 4-, 5- or 6-membered heterocyclic ring optionally substituted independently by one or more R 13 ; or
a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, optionally substituted independently by one or more R 13 ;
wherein R 13 is hydroxy, C 1 -C 4 alkoxy, fluoro, C 1 -C 6 alkyl, haloalkyl, haloalkoxy, —NH 2 , —NH(C 1 -C 6 alkyl) or —N(C 1 -C 6 alkyl) 2 ; or
when both M and Q are CR 4 , the R 4 groups are linked so that together with the interconnecting atoms, the R 4 groups form a fused 5- to 7-membered carbocyclic or heterocyclic ring which may be saturated, unsaturated or aromatic.Join the waitlist — get patent alerts
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