JP2006519831A5 - - Google Patents
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- JP2006519831A5 JP2006519831A5 JP2006506264A JP2006506264A JP2006519831A5 JP 2006519831 A5 JP2006519831 A5 JP 2006519831A5 JP 2006506264 A JP2006506264 A JP 2006506264A JP 2006506264 A JP2006506264 A JP 2006506264A JP 2006519831 A5 JP2006519831 A5 JP 2006519831A5
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- JP
- Japan
- Prior art keywords
- pain
- disorder
- disorders
- tetrazol
- syndrome
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 24
- 208000035475 disorder Diseases 0.000 claims 20
- 208000024891 symptom Diseases 0.000 claims 14
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- 241000124008 Mammalia Species 0.000 claims 11
- 238000011282 treatment Methods 0.000 claims 10
- -1 1-aminomethyl-3-methyl-butyl Chemical group 0.000 claims 9
- BIGWXAGEQONZGD-UHFFFAOYSA-N 2h-oxadiazol-5-one Chemical compound O=C1C=NNO1 BIGWXAGEQONZGD-UHFFFAOYSA-N 0.000 claims 9
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Claims (15)
- 式I若しくはIIの化合物又はその薬学的に許容できる塩であって、
かつ、R1及びR2は、独立して、水素、(C1−C10)直鎖又は分岐アルキル基、(C2−C10)直鎖又は分岐アルコキシアルキル基、フェニル−(C1−C3)直鎖又は分岐アルキル基、及びフェニル−(C2−C3)アルコキシアルキル基から選ばれ、該フェニル基部分は、独立してハロゲン基又は(C1−C3)アルキル基から選ばれる1つ又は2つの置換基によって置換されてもよい;
あるいは、R1及びR2は、結合している炭素と共にシクロペンチル、シクロヘキシル、又はシクロヘプチル環を形成し、該環は上記のR1及びR2の定義で明示した置換基の群から独立して選ばれる1つ又は2つの置換基によって置換されてもよい;かつ、
R3及びR4は、水素及びメチル基から独立して選ばれることを含む化合物又は塩。 - 以下の化合物及びその薬学的に許容できる塩から選ばれる請求項1の化合物又は塩:
4−メチル−2−(1H−テトラゾール−5−イル)−ペンチルアミン;
3−(1−アミノメチル−3−メチル−ブチル)−4H−[1,2,4]オキサジアゾール−5−オン;
3−メチル−2−(1H−テトラゾール−5−イル)−ブチルアミン;
4−プロピル−2−(1H−テトラゾール−5−イル)−ヘプチルアミン;
2−シクロペンチル−2−(1H−テトラゾール−5−イル)−エチルアミン;
3−(2−アミノ−1−シクロペンチル−エチル)−4H−[1,2,4]オキサジアゾール−5−オン;
4−メチル−2−(1H−テトラゾール−5−イル)−ヘキシルアミン;
4−メチル−2−(1H−テトラゾール−5−イル)−ヘキシルアミン;
4,4−ジメチル−2−(1H−テトラゾール−5−イル)−ヘキシルアミン;
4−エチル−2−(1H−テトラゾール−5−イル)−ヘキシルアミン;
4−エチル−2−(1H−テトラゾール−5−イル)−オクチルアミン;
4,4−ジメチル−2−(1H−テトラゾール−5−イル)−ペンチルアミン;
5,5−ジメチル−2−(1H−テトラゾール−5−イル)−ヘキシルアミン;
2−(1H−テトラゾール−5−イル)−ペンチルアミン;
2−(1H−テトラゾール−5−イル)−オクチルアミン;
4,8−ジメチル−2−(1H−テトラゾール−5−イル)−ノニルアミン;
5,9−ジメチル−2−(1H−テトラゾール−5−イル)−デシルアミン;
2−シクロヘキシル−2−(1H−テトラゾール−5−イル)−エチルアミン;
3−(2−アミノ−1−シクロヘキシル−エチル)−4H−[1,2,4]オキサジアゾール−5−オン;
2−(3,5−ジメチル−シクロヘキシル)−2−(1H−テトラゾール−5−イル)−エチルアミン;
2−シクロヘプチル−2−(1H−テトラゾール−5−イル)−エチルアミン;
3−(2−アミノ−1−シクロヘプチル−エチル)−4H−[1,2,4]オキサジアゾール−5−オン;
3−シクロヘキシル−2−(1H−テトラゾール−5−イル)−プロピルアミン;
3,4−ジメチル−2−(1H−テトラゾール−5−イル)−ペンチルアミン;
3−エチル−4−メチル−2−(1H−テトラゾール−5−イル)−ペンチルアミン;
4−シクロペンチル−3−メチル−2−(1H−テトラゾール−5−イル)−ブチルアミン;
4−シクロヘキシル−3−メチル−2−(1H−テトラゾール−5−イル)−ブチルアミン;
3−フェニル−2−(1H−テトラゾール−5−イル)−プロピルアミン;
6−フェニル−2−(1H−テトラゾール−5−イル)−ヘキシルアミン;
4−(4−フルオロ−フェニル)−3−メチル−2−(1H−テトラゾール−5−イル)−ブチルアミン;
3−メチル−2−(1H−テトラゾール−5−イル)−4−(3−トリフルオロメチル−フェニル)−ブチルアミン;
3−メチル−5−フェニル−2−(1H−テトラゾール−5−イル)−ペンチルアミン;
5−(4−tert−ブチル−フェニル)−4−メチル−2−(1H−テトラゾール−5−イル)−ペンチルアミン;
2−メチル−2−(1H−テトラゾール−5−イル)−プロピルアミン;
2−メチル−3−フェニル−2−(1H−テトラゾール−5−イル)−プロピルアミン;
3−(2−アミノ−1−ベンジル−1−メチル−エチル)−4H−[1,2,4]オキサジアゾール−5−オン;
3−(1−アミノメチル−スピロ[2.3]ヘキサ−1−イル)−4H−[1,2,4]オキサジアゾール−5−オン;
C−[1−(1H−テトラゾール−5−イル)−スピロ[2.4]ヘプト−1−イル]−メチルアミン;
3−(1−アミノメチル−スピロ[2,4]ヘプト−1−イル)−4H−[1,2,4]オキサジアゾール−5−オン;
C−[2−イソプロピル−1−(1H−テトラゾール−5−イル)−シクロプロピル]−メチルアミン;
3−(1−アミノメチル−2−イソプロピル−シクロプロピル)−4H−[1,2,4]オキサジアゾール−5−オン;
C−[2−(1−エチル−プロピル)−1−(1H−テトラゾール−5−イル)−シクロプロピル]−メチルアミン;
3−(1−アミノメチル−2−イソブチル−シクロプロピル)−4H−[1,2,4]オキサジアゾール−5−オン;及び
C−[2−シクロヘキシル−1−(1H−テトラゾール−5−イル)−シクロプロピル]−メチルアミン。 - 請求項1に記載の化合物又は塩を含む医薬組成物。
- ほ乳類における、失神発作、てんかん、仮死、全身性無酸素症、低酸素症、脊髄損傷、外傷性脳損傷、頭部外傷、脳虚血、発作(血栓塞栓発作、局所性虚血、全脳虚血、一過性全脳虚血発作の他、頸動脈血管内膜切除術や、血管造影法のように一般的又は診断的血管外科手術を行う患者においてみられるような脳虚血を伴うその他の脳血管系症状を含む)、チオセミカルバジドによって生じるけいれん、カルジアゾールけいれん、及び、脳梗塞、くも膜下出血や脳水腫のような急性又は慢性脳血管系障害による脳血管系障害の内から選ばれる障害又は症状の治療に用いる請求項3に記載の医薬組成物。
- ほ乳類における、神経心臓性失神、神経原性失神、過敏性頸動脈洞、神経血管症候群、神経心臓性障害、胃腸障害に続発する不整脈を含む不整脈、パーキンソン病(PD)、ハンチントン舞踏病(HD)及びアルツハイマー病(AD)のような神経変性障害;せん妄、痴呆(例えば、アルツハイマー型老人性痴呆症、老人性痴呆症、血管性痴呆、HIV−1関連痴呆、AIDS痴呆複合体(ADC)、頭部外傷、パーキンソン病、ハンチントン舞踏病、ピック病、クロイツフェルトヤーコプ病あるいは複合した病因による痴呆)、健忘症による障害、その他の認知あるいは記憶障害、並びに、痴呆による行動症状からなる群から選ばれる障害や症状の治療に用いる請求項3に記載の医薬組成物。
- ほ乳類における、急性疼痛、慢性疼痛、急性外傷のように軟組織や末梢障害から生じる疼痛;ヘルペス後神経痛、後頭神経痛、三叉神経痛、分節性神経痛(segmental neuralgia)又は肋間神経痛、及びその他神経痛;骨関節炎及びリウマチ様関節炎に伴う疼痛;挫傷、捻挫、及び骨折のような外傷に関連した疼痛のような筋骨格系疼痛;脊椎損傷や脳幹損傷による疼痛、中枢神経系の疼痛;腰痛、坐骨神経痛、歯痛、筋筋膜痛症候群、会陰切開による疼痛、痛風による疼痛、及び熱傷に起因する疼痛;心臓痛のような深部内臓痛;筋肉痛、目痛、炎症性疼痛、口腔顔面痛、例えば歯痛;腹痛や婦人科系疼痛、例えば、月経困難症、出産痛、子宮内膜症に関連した疼痛;体因性の疼痛;神経や神経根障害に関連した疼痛、例えば、神経絞扼や腕神経叢剥離のような末梢神経障害に関連した疼痛;手足切断、疼痛チック、神経腫あるいは脈管炎に関連した疼痛;糖尿病性ニューロパシー、化学療法誘発性ニューロパシー、急性ヘルペス性神経痛およびヘルペス後神経痛;非定型顔面痛、神経因性腰痛やクモ膜炎、三叉神経痛、後頭神経痛、分節性神経痛(segmental neuralgia)あるいは肋間神経痛、HIV関連性神経痛やAIDS関連性神経痛、及びその他神経痛;異痛症、痛覚過敏症、熱傷疼痛、特発性疼痛、化学療法による疼痛;後頭神経痛、心因性疼痛、腕神経叢剥離、不穏下肢症候群に関連した疼痛;胆石痛;慢性アルコール中毒、甲状腺機能低下症、尿毒症又はビタミン欠乏症によって生じる疼痛;ガン疼痛ともしばしば呼ばれるガンに伴うニューロパシー性又は非ニューロパシー性疼痛、幻肢痛、機能性腹痛、頭重(前兆を伴う片頭痛、前兆を伴わない片頭痛その他血管性頭痛を含む)、急性又は慢性緊張性頭痛、洞性頭痛および群発頭痛;側頭骨顎痛及び上顎洞痛;強直性脊椎炎に起因する疼痛;膀胱収縮の増加による疼痛;術後痛、創部瘢痕痛、並びにHIV、関節痛、脈管炎及び線維筋肉痛に関連した疼痛のような慢性非ニューロパシー性疼痛から選ばれる障害や症状の治療に用いる請求項3に記載の医薬組成物。
- ほ乳類における、うつ病、より詳細には、うつ病性障害のような気分障害、例えば大うつ病性障害、重度な単極性再発性大うつ病エピソード、気分変調性障害、抑うつ神経症や神経症性うつ病、メランコリー性うつ病(拒食症、体重減少、不眠症、早朝覚醒あるいは精神運動遅延を含む)、非定型うつ病(あるいは反応性うつ病)(食欲亢進、過眠症、精神運動激越あるいは被刺激性を含む);治療抵抗性うつ病;季節性感情障害および小児うつ病;月経前症候群、月経前不快気分障害、熱感、双極性障害あるいは躁うつ病、例えば、双極I型障害、双極II型障害及び循環気質性;季節性情動障害、行為障害及び破壊的行為障害;小児不安障害、広場恐怖症を伴うあるいは伴わないパニック障害、パニック障害の既往歴のない広場恐怖症、特定の恐怖症(例えば特定の動物恐怖症)、社会不安障害、社会恐怖、強迫障害、外傷後ストレス障害や急性ストレス障害を含むストレス障害や全般性不安障害のような気分障害から選ばれる障害や症状の治療に用いる請求項3に記載の医薬組成物。
- ほ乳類における、境界型人格障害;統合失調症及びその他精神病性障害、例えば統合失調症様障害、統合失調症感情障害、妄想性障害、短期精神病性障害、共有精神病障害、一般身体症状による精神病性障害、妄想あるいは幻覚を伴う精神病性障害、物質誘発性精神病性障害、不安の精神病性エピソード、精神病に伴う不安、重篤な大うつ病性障害のような精神病性気分障害;急性そう病のような精神病性障害に伴う気分障害および双極性障害に伴ううつ病、統合失調症に関連した気分障害;並びに、精神遅滞に関連した行動障害からなる群から選ばれる障害や症状の治療に用いる請求項3に記載の医薬組成物。
- ほ乳類における、眼球乾燥症候群、結膜炎、春季カタル等のような眼疾患;及び、増殖性硝子体網膜症のような細胞増殖に伴う眼科系症状;自閉症、注意欠陥多動障害(ADHD)、血管新生(すなわち、血管新生阻害のために使用する)、ライター症候群、関節炎、ダウン症候群、多発性硬化症(MS)や筋萎縮性側索硬化症(ALS)のような脱髄疾患、不眠症(例えば、心理生理学的及び特発性不眠症を含む原発性不眠症、不穏下肢症候群、パーキンソン病あるいはその他の慢性障害に続発する不眠症を含む続発性不眠症、および一時的な不眠症)、夢遊病、断眠、REM睡眠障害、睡眠時無呼吸、過眠症、錯眠、睡眠覚醒サイクル障害、時差ぼけ、ナルコレプシー、交代制勤務又は不規則な勤務形態に関連する睡眠障害、薬剤その他の原因によって生じる徐波睡眠の減少による睡眠の質低下やその他睡眠障害のような睡眠障害からなる群から選ばれる障害や症状の治療に用いる請求項3に記載の医薬組成物。
- ヒト被験体において徐波睡眠を増加し、及び成長ホルモンの分泌を高めるための請求項3に記載の医薬組成物。
- ほ乳類における、慢性閉塞性気道疾患、気管支肺炎、慢性気管支炎、嚢胞性線維症、成人型呼吸窮迫症候群、及び気管支痙攣のような呼吸器系疾患、特に粘液の過剰分泌に関連した呼吸器系疾患;咳、百日咳、アンギオテンシン変換酵素(ACE)誘発性の咳、肺結核、湿疹や鼻炎のようなアレルギー;接触性皮膚炎、アトピー性皮膚炎、じんましん、及びその他湿疹様皮膚炎;そう痒、血液透析に伴うそう痒;炎症性腸疾患のような炎症性疾患、乾癬、骨関節炎、軟骨の損傷(例えば身体活動や骨関節炎に起因する軟骨損傷)、リウマチ様関節炎、乾癬性関節炎、喘息、そう痒症、及び日焼け;並びにウルシなどの過敏症からなる群から選ばれる障害や症状の治療に用いる請求項3に記載の医薬組成物。
- ほ乳類における、炎症性腸疾患のような炎症性胃腸(GI)障害、ピロリ菌が原因である障害、及び胃腸管の疾患、例えば、胃炎、直腸炎、胃十二指腸潰瘍、消化性潰瘍、消化不良、内臓の神経支配に関連した障害、潰瘍性大腸炎、慢性膵炎、クローン病、過敏性腸症候群及び、術後悪心や術後嘔吐および急性嘔吐、遅延性嘔吐、予期性嘔吐を含む嘔吐(嘔吐には、化学療法、放射線、毒素、ウイルス/細菌感染、妊娠、前庭障害(例えば動揺病、眩暈症、目眩やメニエル病)、手術、片頭痛、頭蓋内圧の変化、胃食道逆流症、胃酸過多、暴飲暴食、酸性胃、呑酸や吐逆、胸焼け(例えば、エピソード性、夜間性又は食事誘発性胸焼け、及び消化不良によって誘発される嘔吐が含まれる);ダウン症候群;シェーグレン症候群、高血圧症、造血、術後性神経腫、良性前立腺肥大、歯周病、痔疾や肛門裂創、不妊、反射性交感神経性ジストロフィー、肝炎、高脂血症に伴う腱痛、血管拡張、強皮症や好酸球増加性肝蛭症のような線維形成性疾患および膠原病;乳腫瘍、胃ガン、胃リンパ腫、神経節細胞芽腫や、小細胞肺ガンのような小細胞ガンを含む新生物;並びに、狭心症、片頭痛やレイノー病のような血管攣縮性疾患からなる群から選ばれる障害又は症状を治療の治療に用いる請求項3に記載の医薬組成物。
- ほ乳類における、乳房痛症候群、動揺病、紅斑性狼瘡や免疫不全(ストレス誘発性免疫不全、例えば、特発性免疫機能不全、感染後免疫機能不全、乳房腫瘍除去後免疫機能不全、ブタ・ストレス症候群、ウシの輸送熱、ウマの発作性細動、ニワトリの産卵機能不全(confinement dysfunction)、ヒツジの毛を刈られるストレス、イヌにおけるヒトとの相互作用によるストレス);アルコール、アンフェタミン(あるいはアンフェタミン様物質)、カフェイン、大麻(cannabis)、コカイン、幻覚剤、吸入剤やエアゾール噴霧剤(propellant)、ニコチン、オピオイド、フェニルグリシジン誘導体、鎮静剤、催眠薬、および抗不安薬の使用により生じる物質関連性障害であって、その物質関連性障害には、依存、乱用、中毒、離脱症状、中毒せん妄、離脱せん妄を含む障害;及び、行為に対する依存を含む依存性障害(例えば賭博その他の常習性行為に対する依存)からなる群から選ばれる障害や症状の治療に用いる請求項3に記載の医薬組成物。
- ほ乳類における、広汎性発達障害、線維筋肉痛、ヒト免疫不全ウイルス(HIV)感染症;HIV脳症;身体醜形障害のような解離性障害;拒食症や過食症のような摂食障害;潰瘍性大腸炎;クローン病;過敏性大腸症候群;慢性疲労症候群;乳幼児突然死症候群(SIDS);過活動膀胱;過活動膀胱の下部尿路症状;慢性膀胱炎;化学療法誘発性膀胱炎;咳、アンギオテンシン変換酵素(ACE)誘発性の咳、そう痒、しゃっくり、月経前症候群、月経前不快気分障害、月経困難のような無月経障害;肩/手症候群のような反射性交感神経性ジストロフィー;サイトカイニン化学療法に起因する血漿管外溢出;慢性膀胱炎、排尿筋過反射、尿管の炎症や尿失禁(切迫性尿失禁、過活動膀胱、緊張性尿失禁や混合型尿失禁を含む)のような膀胱機能障害;強皮症や好酸球増加性肝蛭症のような線維形成性疾患および膠原病;狭心症やレイノー病のような血管拡張性および血管攣縮性疾患によって引き起こされる血流障害;早漏や男性の勃起障害を含む性機能障害からなる群から選ばれる障害や症状の治療に用いる請求項3に記載の医薬組成物。
- ほ乳類における、原発性運動障害、無動症、運動障害(例えば家族性発作性運動障害、遅発性ジスキネジア、振戦、舞踏病、筋クローヌス、チックその他の運動障害)、痙直、トゥーレット症候群、スコット症候群、麻痺(例えばベル麻痺、脳性麻痺、分娩麻痺、上腕麻痺、消耗性麻痺、虚血性麻痺、進行性球麻痺及びその他の麻痺)、無動・筋固縮症候群(akinetic−rigid syndrome);薬物誘発性運動障害のような錐体外路性運動障害、例えば、神経遮断薬誘発性パーキンソン病、神経遮断薬性悪性症候群、神経遮断薬誘発性急性ジストニア、神経遮断薬誘発性急性アカシジア、神経遮断薬誘発性遅発性ジスキネジアや薬物誘発性姿勢振戦;不穏下肢症候群やパーキンソン病またはハンチントン舞踏病に関連した運動障害のような運動障害からなる群から選ばれる障害や症状の治療に用いる請求項3に記載の医薬組成物。
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AU2013216828B2 (en) | 2012-02-09 | 2017-01-12 | Novus International Inc. | Functionalized polymer compositions |
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US4087544A (en) * | 1974-12-21 | 1978-05-02 | Warner-Lambert Company | Treatment of cranial dysfunctions using novel cyclic amino acids |
DE2460891C2 (de) * | 1974-12-21 | 1982-09-23 | Gödecke AG, 1000 Berlin | 1-Aminomethyl-1-cycloalkanessigsäuren und deren Ester, Verfahren zu deren Herstellung und diese Verbindungen enthaltende Arzneimittel |
US6197819B1 (en) * | 1990-11-27 | 2001-03-06 | Northwestern University | Gamma amino butyric acid analogs and optical isomers |
WO1999008670A1 (en) | 1997-08-20 | 1999-02-25 | Guglietta, Antonio | Gaba analogs to prevent and treat gastrointestinal damage |
SI1045839T1 (en) * | 1997-12-16 | 2004-06-30 | Warner-Lambert Company Llc | Novel amines as pharmaceutical agents |
IL135315A0 (en) * | 1997-12-16 | 2001-05-20 | Warner Lambert Co | 4(3)-substituted-4(3)-aminomethyl-(thio)pyran or -piperidine derivatives (gabapentin analogues), their preparation and their use in the treatment of neurological disorders |
PT1047678E (pt) * | 1997-12-16 | 2004-12-31 | Warner Lambert Co | Derivados do 1-aminometil-cicloalcano substituido em 1 (=analogos da gabapentina) sua preparacao e sua utilizacao no tratamento de disturbios neurologicos |
WO1999061424A1 (en) | 1998-05-26 | 1999-12-02 | Warner-Lambert Company | Conformationally constrained amino acid compounds having affinity for the alpha2delta subunit of a calcium channel |
JP2002524551A (ja) | 1998-09-14 | 2002-08-06 | ワーナー−ランバート・カンパニー | 分枝鎖アルキルピロリジン−3−カルボン酸 |
AU2003201716B2 (en) | 2002-01-31 | 2008-04-17 | Warner-Lambert Company Llc | Alpha 2 delta ligands to treat tinnitus |
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2004
- 2004-02-23 CA CA002518218A patent/CA2518218A1/en not_active Abandoned
- 2004-02-23 JP JP2006506264A patent/JP2006519831A/ja not_active Withdrawn
- 2004-02-23 WO PCT/IB2004/000510 patent/WO2004078734A1/en active Application Filing
- 2004-02-23 BR BRPI0408110-2A patent/BRPI0408110A/pt not_active IP Right Cessation
- 2004-02-23 EP EP04713604A patent/EP1603890A1/en not_active Withdrawn
- 2004-02-23 MX MXPA05009504A patent/MXPA05009504A/es unknown
- 2004-03-08 US US10/795,760 patent/US7250433B2/en not_active Expired - Fee Related
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