JP2008542431A5 - - Google Patents

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JP2008542431A5
JP2008542431A5 JP2008515209A JP2008515209A JP2008542431A5 JP 2008542431 A5 JP2008542431 A5 JP 2008542431A5 JP 2008515209 A JP2008515209 A JP 2008515209A JP 2008515209 A JP2008515209 A JP 2008515209A JP 2008542431 A5 JP2008542431 A5 JP 2008542431A5
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Japan
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disorder
pain
exo
aza
bicyclo
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JP2008515209A
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Japanese (ja)
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JP2008542431A (en
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Priority claimed from PCT/EP2006/062952 external-priority patent/WO2006131525A1/en
Publication of JP2008542431A publication Critical patent/JP2008542431A/en
Publication of JP2008542431A5 publication Critical patent/JP2008542431A5/ja
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Claims (10)

式Iで表される化合物、そのいずれかの異性体又はその異性体のいずれかの混合物、あるいはその薬学的に許容される塩:
Figure 2008542431

式中、
は、水素又はアルキルを表し、このアルキルはハロ、トリフルオロメチル、トリフルオロメトキシ、シアノ、ヒドロキシ、アミノ、ニトロ、アルコキシ、シクロアルコキシ、アルキル、シクロアルキル、シクロアルキルアルキル、アルケニル及びアルキニルからなる群から独立して選択される1個又は2個以上の置換基により置換されていてもよく;及び
は、アリール基を表し、このアリール基はハロ、トリフルオロメチル、トリフルオロメトキシ、シアノ、ニトロ、ヒドロキシ、アルコキシ、シクロアルコキシ、アルコキシアルキル、シクロアルコキシアルキル、メチレンジオキシ、エチレンジオキシ、アルキル、シクロアルキル、シクロアルキルアルキル、アルケニル、アルケニル、−NR’R’’、−(C=O)NR’R’’又は−NR’(C=O)R’’からなる群から独立して選択される1個又は2個以上の置換基により置換されていてもよく;ここでR’及びR’’はそれぞれ独立して水素又はアルキルを表す。
A compound of formula I, any isomer thereof or any mixture of isomers thereof, or a pharmaceutically acceptable salt thereof:
Figure 2008542431

Where
R a represents hydrogen or alkyl, which alkyl consists of halo, trifluoromethyl, trifluoromethoxy, cyano, hydroxy, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl and alkynyl Optionally substituted by one or more substituents independently selected from the group; and R b represents an aryl group, which aryl group is halo, trifluoromethyl, trifluoromethoxy, cyano , Nitro, hydroxy, alkoxy, cycloalkoxy, alkoxyalkyl, cycloalkoxyalkyl, methylenedioxy, ethylenedioxy, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkenyl, —NR′R ″, — (C═O ) NR'R "or- R ′ (C═O) R ″ may be substituted by one or more substituents independently selected from the group consisting of; R ′ and R ″ are each independently Represents hydrogen or alkyl.
が水素又はアルキルを表す、請求項1に記載の化合物。 R a represents hydrogen or alkyl, A compound according to claim 1. がフェニル基を表し、このフェニル基はハロ、トリフルオロメチル、トリフルオロメトキシ、シアノ及びアルコキシからなる群から独立して選択される1個又は2個以上の置換基により置換されていてもよい、請求項1又は2に記載の化合物。 R b represents a phenyl group, which may be substituted with one or more substituents independently selected from the group consisting of halo, trifluoromethyl, trifluoromethoxy, cyano and alkoxy. The compound according to claim 1 or 2, which is good. がフェニル基を表し、このフェニル基はハロ、トリフルオロメチル、トリフルオロメトキシ、シアノ及びアルコキシからなる群から独立して選択される2個の置換基により置換されている、請求項1又は2に記載の化合物。 Rb represents a phenyl group, which is substituted with two substituents independently selected from the group consisting of halo, trifluoromethyl, trifluoromethoxy, cyano and alkoxy. 2. The compound according to 2. がナフチル基を表し、このナフチル基はハロ、トリフルオロメチル、トリフルオロメトキシ、シアノ及びアルコキシからなる群から独立して選択される1個又は2個以上の置換基により置換されていてもよい、請求項1又は2に記載の化合物。 R b represents a naphthyl group, which may be substituted with one or more substituents independently selected from the group consisting of halo, trifluoromethyl, trifluoromethoxy, cyano and alkoxy. The compound according to claim 1 or 2, which is good. エキソ−3−(3,4−ジクロロ−フェノキシ)−8−アザ−ビシクロ[3.2.1]オクタ−6−エン;
エキソ−3−(3−ブロモ−4−クロロ−フェノキシ)−8−アザ−ビシクロ[3.2.1]オクタ−6−エン;
エキソ−3−(6−メトキシ−ナフタレン−2−イルオキシ)−8−アザ−ビシクロ[3.2.1]オクタ−6−エン;
エキソ−3−(3−クロロ−4−フルオロ−フェノキシ)−8−アザ−ビシクロ[3.2.1]オクタ−6−エン;
エキソ−3−(4−ブロモ−3−クロロ−フェノキシ)−8−アザ−ビシクロ[3.2.1]オクタ−6−エン;
エキソ−3−(4−クロロ−3−フルオロ−フェノキシ)−8−アザ−ビシクロ[3.2.1]オクタ−6−エン;
エキソ−3−(3,4−ジクロロ−フェノキシ)−8−メチル−8−アザ−ビシクロ[3.2.1]オクタ−6−エン;
エキソ−3−(3−ブロモ−4−クロロ−フェノキシ)−8−メチル−8−アザ−ビシクロ[3.2.1]オクタ−6−エン;
エキソ−3−(6−メトキシ−ナフタレン−2−イルオキシ)−8−メチル−8−アザ−ビシクロ[3.2.1]オクタ−6−エン;
エキソ−3−(3−クロロ−4−フルオロ−フェノキシ)−8−メチル−8−アザ−ビシクロ[3.2.1]オクタ−6−エン;
エキソ−3−(4−ブロモ−3−クロロ−フェノキシ)−8−メチル−8−アザ−ビシクロ[3.2.1]オクタ−6−エン;
エキソ−3−(4−クロロ−3−フルオロ−フェノキシ)−8−メチル−8−アザ−ビシクロ[3.2.1]オクタ−6−エン;
である化合物又はその薬学的に許容される塩である、請求項1に記載の化合物。
Exo-3- (3,4-dichloro-phenoxy) -8-aza-bicyclo [3.2.1] oct-6-ene;
Exo-3- (3-bromo-4-chloro-phenoxy) -8-aza-bicyclo [3.2.1] oct-6-ene;
Exo-3- (6-methoxy-naphthalen-2-yloxy) -8-aza-bicyclo [3.2.1] oct-6-ene;
Exo-3- (3-chloro-4-fluoro-phenoxy) -8-aza-bicyclo [3.2.1] oct-6-ene;
Exo-3- (4-bromo-3-chloro-phenoxy) -8-aza-bicyclo [3.2.1] oct-6-ene;
Exo-3- (4-chloro-3-fluoro-phenoxy) -8-aza-bicyclo [3.2.1] oct-6-ene;
Exo-3- (3,4-dichloro-phenoxy) -8-methyl-8-aza-bicyclo [3.2.1] oct-6-ene;
Exo-3- (3-bromo-4-chloro-phenoxy) -8-methyl-8-aza-bicyclo [3.2.1] oct-6-ene;
Exo-3- (6-methoxy-naphthalen-2-yloxy) -8-methyl-8-aza-bicyclo [3.2.1] oct-6-ene;
Exo-3- (3-chloro-4-fluoro-phenoxy) -8-methyl-8-aza-bicyclo [3.2.1] oct-6-ene;
Exo-3- (4-bromo-3-chloro-phenoxy) -8-methyl-8-aza-bicyclo [3.2.1] oct-6-ene;
Exo-3- (4-chloro-3-fluoro-phenoxy) -8-methyl-8-aza-bicyclo [3.2.1] oct-6-ene;
Or a pharmaceutically acceptable salt thereof.
治療有効量の請求項1〜6のいずれか1項に記載の化合物、そのいずれかの異性体又はその異性体のいずれかの混合物、あるいはその薬学的に許容される塩を、少なくとも1種の薬学的に許容される担体、賦形剤又は希釈剤とともに含有する医薬組成物。   7. A therapeutically effective amount of the compound of any one of claims 1-6, any isomer thereof or any mixture of isomers thereof, or at least one pharmaceutically acceptable salt thereof. A pharmaceutical composition comprising a pharmaceutically acceptable carrier, excipient or diluent. 請求項1〜6のいずれか1項に記載の化合物、そのいずれかの異性体又はその異性体のいずれかの混合物、あるいはその薬学的に許容される塩を含む医薬組成物 A pharmaceutical composition comprising the compound according to any one of claims 1 to 6, any isomer thereof or a mixture of any of the isomers, or a pharmaceutically acceptable salt thereof . ヒトを包含する哺乳動物の病気又は障害又は症状の処置、予防又は緩和用の医薬組成物であって、当該病気、障害又は症状が中枢神経系におけるモノアミン神経伝達物質再取込の阻害に応答する病気、障害又は症状である、請求項8に記載の医薬組成物A pharmaceutical composition for treating, preventing or alleviating a disease or disorder or symptom of a mammal, including a human, wherein the disease, disorder or symptom responds to inhibition of monoamine neurotransmitter reuptake in the central nervous system disease, Ru disorder or condition der pharmaceutical composition according to claim 8. 病気、障害又は症状が、気分障害、うつ病、非定型うつ病、疼痛に対する二次的うつ病、大うつ障害、気分変調、双極性障害、双極性I型障害、双極性II型障害、気分循環性障害、全般的医療症状による気分障害、物質誘発性気分障害、仮性痴呆症、ガンザー症候群、脅迫性障害、パニック障害、広場恐怖症を伴わないパニック障害、広場恐怖症を伴うパニック障害、パニック障害の病歴がない広場恐怖症、パニック発作、記憶欠損、記憶喪失、注意欠如過活動性障害、肥満症、不安症、全般性不安障害、摂食障害、パーキンソン病、パーキンソニズム、痴呆症、加齢による痴呆症、老人性痴呆症、アルツハイマー病、後天性免疫不全症候群、認知症候群、加齢による記憶機能不全、特異性恐怖症、社会恐怖症、社会不安性障害、心的外傷後ストレス障害、急性ストレス障害、薬物依存症、薬物乱用症、コカイン乱用症、ニコチン乱用症、タバコ乱用症、アルコール依存症、アルコール症、盗癖、疼痛、慢性の疼痛、炎症性疼痛、神経障害性疼痛、偏頭痛、緊張型頭痛、慢性緊張型頭痛、うつ症状を伴う疼痛、繊維筋肉痛、関節炎、変形性関節炎、リューマチ性関節炎、背中痛、癌疼痛、刺激性腸疼痛、刺激性腸症候群、手術後疼痛、乳房切除後疼痛症候群(PMPS)、発作後疼痛、薬物誘発性神経障害、糖尿病性神経障害、交感神経依存性疼痛、三叉神経痛、歯痛、筋膜痛、幻影四肢痛、過食症、月経前症候群、月経前性不快気分障害、黄体期後期精神症状、外傷後症候群、慢性疲労症候群、尿失禁、腹圧性尿失禁、切迫性尿失禁、夜行性尿失禁、性機能障害、早漏、勃起困難症、勃起機能不全、早発性女性オルガズム、下肢静止不能症候群、周期性四肢運動障害、摂食障害、神経性食欲不振、睡眠障害、広汎性発達障害、自閉症、アスペルガー障害、レッツ障害、小児期崩壊性障害、学習障害、運動技術障害、無言症、抜毛狂、ナルコレプシー、発作後うつ症、発作誘発性脳損傷、発作誘発性神経損傷、ジルドラレット病、耳鳴、チック障害、身体醜形障害、反抗挑戦性障害又は発作後障害である、請求項9に記載の医薬組成物Disease, disorder or symptom is mood disorder, depression, atypical depression, secondary depression for pain, major depression, mood modulation, bipolar disorder, bipolar I disorder, bipolar II disorder, mood Circulatory disorder, mood disorder due to general medical condition, substance-induced mood disorder, pseudodementia, Ganza syndrome, threatened disorder, panic disorder, panic disorder without agoraphobia, panic disorder with agoraphobia, panic Agoraphobia without history of disability, panic attack, memory deficit, memory loss, attention deficit hyperactivity disorder, obesity, anxiety, generalized anxiety disorder, eating disorder, Parkinson's disease, parkinsonism, dementia, addiction Age-related dementia, senile dementia, Alzheimer's disease, acquired immune deficiency syndrome, cognitive syndrome, memory dysfunction due to aging, specific phobia, social phobia, social anxiety disorder, trauma Stress disorder, acute stress disorder, drug addiction, drug abuse, cocaine abuse, nicotine abuse, tobacco abuse, alcoholism, alcoholism, stealing, pain, chronic pain, inflammatory pain, neuropathic pain Migraine, tension headache, chronic tension headache, pain with depressive symptoms, fibromyalgia, arthritis, osteoarthritis, rheumatoid arthritis, back pain, cancer pain, irritable bowel pain, irritable bowel syndrome, surgery Post-pain, post-mastectomy pain syndrome (PMPS), post-stroke pain, drug-induced neuropathy, diabetic neuropathy, sympathetic nerve-dependent pain, trigeminal neuralgia, toothache, fascia pain, phantom limb pain, bulimia, menstruation Pre-syndrome, premenstrual dysphoric disorder, late luteal phase mental symptoms, post-traumatic syndrome, chronic fatigue syndrome, urinary incontinence, stress urinary incontinence, urge incontinence, nocturnal urinary incontinence, sexual dysfunction, premature ejaculation Disease, erectile dysfunction, early-onset female orgasm, restless leg syndrome, periodic limb movement disorder, eating disorder, anorexia nervosa, sleep disorder, pervasive developmental disorder, autism, Asperger disorder, let's disorder, Childhood disintegration disorder, learning disorder, motor skill disorder, speechlessness, hair loss, narcolepsy, post-stroke depression, seizure-induced brain injury, seizure-induced nerve injury, Gildlerette disease, tinnitus, tic disorder, body dysmorphic disorder The pharmaceutical composition according to claim 9, which is a rebellious challenge disorder or a post-seizure disorder.
JP2008515209A 2005-06-08 2006-06-07 3-Aryloxy-8-aza-bicyclo [3.2.1] oct-6-ene derivatives and their use as monoamine neurotransmitter reuptake inhibitors Abandoned JP2008542431A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US68838205P 2005-06-08 2005-06-08
DKPA200500839 2005-06-08
PCT/EP2006/062952 WO2006131525A1 (en) 2005-06-08 2006-06-07 3 -aryloxy- 8 -aza-bicyclo [3.2.1.] oct- 6- ene derivatives and their use as monoamine neurotransmitter re-uptake inhibitors

Publications (2)

Publication Number Publication Date
JP2008542431A JP2008542431A (en) 2008-11-27
JP2008542431A5 true JP2008542431A5 (en) 2009-07-23

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JP2008515209A Abandoned JP2008542431A (en) 2005-06-08 2006-06-07 3-Aryloxy-8-aza-bicyclo [3.2.1] oct-6-ene derivatives and their use as monoamine neurotransmitter reuptake inhibitors

Country Status (6)

Country Link
EP (1) EP1896468A1 (en)
JP (1) JP2008542431A (en)
AU (1) AU2006256738A1 (en)
CA (1) CA2620986A1 (en)
MX (1) MX2007015488A (en)
WO (1) WO2006131525A1 (en)

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003062235A1 (en) * 2002-01-17 2003-07-31 Eli Lilly And Company Modulators of acetylcholine receptors
CA2530023A1 (en) * 2003-06-24 2004-12-29 Neurosearch A/S Novel 8-aza-bicyclo[3.2.1]octane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors

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