JPH10511387A - 1,3,3−(三置換)シクロヘキサンダイマーおよび関連化合物 - Google Patents
1,3,3−(三置換)シクロヘキサンダイマーおよび関連化合物Info
- Publication number
- JPH10511387A JPH10511387A JP8520430A JP52043096A JPH10511387A JP H10511387 A JPH10511387 A JP H10511387A JP 8520430 A JP8520430 A JP 8520430A JP 52043096 A JP52043096 A JP 52043096A JP H10511387 A JPH10511387 A JP H10511387A
- Authority
- JP
- Japan
- Prior art keywords
- independently
- substituted
- alkyl
- hydrogen
- ncn
- 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.)
- Ceased
Links
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
- C07C217/54—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C217/74—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C43/00—Ethers; Compounds having groups, groups or groups
- C07C43/02—Ethers
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- C07C43/253—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring and to a carbon atom of a ring other than a six-membered aromatic ring containing hydroxy or O-metal groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C61/00—Compounds having carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
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- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.式(I): [式中、 R1は独立して−(CR4R5)nC(O)O(CR4R5)mR6、 −(CR4R5)nC(O)NR4(CR4R5)mR6、 −(CR4R5)nO(CR4R5)mR6、または−(CR4R5)rR6(ここに、ア ルキル部分は、未置換または1またはそれ以上のフッ素で置換されている)から 選択され; mは0ないし2であり; nは1ないし4であり; rは0ないし6であり; R4およびR5は独立して、水素またはC1-2アルキルから選択され; R6は独立して、水素、メチル、ヒドロキシ、アリール、ハロ置換アリール、 アリールオキシC1-3アルキル、ハロ置換アリールオキシC1-3アルキル、インダ ニル、インデニル、C7-11ポリシクロアルキル、テトラヒドロフラニル、フラニ ル、テトラヒドロピラニル、ピラニル、テトラヒドロチエニル、チエニル、テト ラヒドロチオピラニル、チオピラニル、C3-6シクロアルキル、または1または 2個の不飽和結合を含有するC4-6シクロアルキル(ここに、シクロアルキルま たは複素環部分は未置換であるか、あるいは1ないし3個のメチル基または1個 のエチル基または1個のヒドロキシル基で置換されている)から選択され; ただし、 (a)R6がヒドロキシルの場合、mは2であるか;または (b)R6がヒドロキシルの場合、rは2ないし6であるか;または (c)R6が2−テトラヒドロピラニル、2−テトラヒドロチオピラニル、2 −テトラヒドロフラニル、または2−テトラヒドロチエニルの場合、mは1また は2であるか;または (d)R6が2−テトラヒドロピラニル、2−テトラヒドロチオピラニル、2 −テトラヒドロフラニル、または2−テトラヒドロチエニルの場合、rは1ない し6であり; (e)nが1であり、mが0の場合、 R6は−(CR4R5)nO(CR4R5)mR6においてH以外であり; Xは独立して、YR2、フッ素、NR4R5、またはホルミルアミンから選択さ れ; Yは独立して、OまたはS(O)m'から選択され; m'は0、1または2であり; X2は独立してOまたはNR8から選択され; X3はH、R9、OR8、CN、C(O)R8、C(O)OR8、C(O)NR8R8 、またはNR8R8から独立して選択され; R2は1またはそれ以上のフッ素で所望により置換されていてもよい−CH3ま たは−CH2CH3からなる群より独立して選択され; sは0ないし4であり; Wは2ないし6個の炭素原子を有するアルキル、2ないし6個の炭素原子を有 するアルケニルまたは2ないし6個の炭素原子を有するアルキニルであり; Zは独立して、CR8R8OR14、CR8R8OR15、CR8R8SR14、 CR8R8SR15、CR8R8S(O)m’R7、CR8R8NR10R14、 CR8R8NR10S(O)2NR10R14、CR8R8NR10S(O)2R7、 CR8R8NR10C(Y')R14、CR8R8NR10C(O)OR7、 CR8R8NR10C(Y')NR10R14、CR8R8NR10C(NCN)NR10R14 、 CR8R8NR10C(CR4NO2)NR10R14、 CR8R8NR10C(NCN)SR9、CR8R8NR10C(CR4NO2)SR9、 CR8R8C(O)OR14、CR8R8C(Y')NR10R14、 CR8R8C(NR10)NR10R14、CR8R8CN、CR8R8(テトラゾリル)、 CR8R8(イミダゾリル)、CR8R8(イミダゾリジニル)、 CR8R8(ピラゾニル)、CR8R8(チアゾリル)、 CR8R8(チアゾリジニル)、CR8R8(オキサゾリル)、 CR8R8(オキサゾリジニル)、CR8R8(トリアゾリル)、 CR8R8(イソオキサゾリル)、CR8R8(オキサジアゾリル)、 CR8R8(チアジアゾリル)、CR8R8(モルホリニル)、 CR8R8(ピペリジニル)、CR8R8(ピペラジニル)、CR8R8(ピロリル) 、 CR8R8C(NOR8)R14、CR8R8C(NOR14)R8、 CR8R8NR10C(NR10)SR9、CR8R8NR10C(NR10)NR10R14、 CR8R8NR10C(O)C(O)NR10R14または CR8R8NR10C(O)C(O)OR14であり; X5はH、R9、OR8、CN、C(O)R8、C(O)OR8、C(O)NR8R8 またはNR8R8であり; X4は独立して、H、R9、OR8、CN、C(O)R8、C(O)OR8、C( O)NR8R8またはNR8R8であり; Y’は独立してOまたはSから選択され; R7は−(CR4R5)qR12またはC1-6アルキル(ここに、R12またはC1-6ア ルキル基は、未置換であるか、あるいは未置換または1ないし3個のフッ素で置 換されているメチルまたはエチルで1回またはそれ以上置換されている)、−F 、−Br、−Cl、−NO2、−NR10R11、−C(O)R8、 −CO2R8、−O(CH2)qR8、−CN、−C(O)NR10R11、 −O(CH2)qC(O)NR10R11、−O(CH2)qC(O)R9、 −NR10C(O)NR10R11、−NR10C(O)R11、−NR10C(O)OR9 、 −NR10C(O)R13、−C(NR10)NR10R11、−C(NCN)NR10R11 、 −C(NCN)SR9、−NR10C(NCN)SR9、 −NR10C(NCN)NR10R11、−NR10S(O)2R9、−S(O)m'R9、 −NR10C(O)C(O)NR10R11、−NR10C(O)C(O)NR10、また はR13であり; qは0、1または2であり; R12は独立して、R13、C3-7シクロアルキル、(2−、3−または4−ピリ ジル)、ピリミジル、ピラゾリル、(1−または2−イミダゾリル)、ピロリル 、ピペラジニル、ピペリジニル、モルホリニル、フラニル、(2−または3−チ エニル)、キノリニル、ナフチル、またはフェニルから選択され; R8は独立して水素またはR9から選択され; R9は1ないし3個のフッ素により所望により置換されていてもよいC1-4アル キルから独立して選択され; R10は独立してOR8またはR11から選択され; R11は独立して、水素、または所望により1ないし3個のフッ素により所望に より置換されてもよいC1-4アルキルから選択されるか;あるいはR10およびR1 1 がNR10R11である場合、これらは窒素原子と一緒になって、炭素または炭素 とO、NまたはSから選択される少なくとも1個の別のヘテロ原子を含んでなる 5ないし7員環を形成してもよく; R13は独立して、オキサゾリジニル、オキサゾリル、チアゾリル、ピラゾリル 、トリアゾリル、テトラゾリル、イミダゾリル、イミダゾリジニル、チアゾリジ ニル、イソキサゾリル、オキサジアゾリル、またはチアジアゾリルから選択され 、これらの各複素環が互いに炭素原子を介して結合しており; R14は水素またはR7であるか;あるいはR8およびR14がNR8R14である場 合、これらは窒素原子と一緒になって、炭素あるいは炭素およびO、NまたはS から選択される少なくとも1個の別のヘテロ原子を含んでなる5ないし7員環を 形成してもよく; R15はC(O)R14、C(O)NR4R14、S(O)2R7またはS(O)2NR4 R14である] で示される化合物またはその医薬上許容される塩。 2.R1が−CH2−シクロプロピル、シクロペンチル、3−ヒドロキシシクロ ペンチル、メチルまたはCF2Hであり;XがYR2であり;Yが酸素であり;X2 が酸素であり;X3が水素であり;X4が水素であり;R2がCF2Hまたはメチ ルであり、Wが1,3−ブタジイニルであり、Z中のR8基がHでありZのR14基 がR4である請求項1記載の化合物。 3.1,4−ビス−{[c−3−(3−シクロペンチルオキシ−4−メトキシ フェニル)−r−1−ヒドロキシメチルシクロヘキサン]−3−イル}ブタ−1 ,3−ジイン、および 1,4−ビス−{[c−3−(3−シクロペンチルオキシ−4−メトキシフェ ニル)−r−1−アミノメチルシクロヘキサン]−3−イル}ブタ−1,3−ジ イン である請求項2記載の化合物。 4.請求項1記載の式(I)の化合物および医薬上許容される賦形剤を含んで なる医薬組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US36318094A | 1994-12-23 | 1994-12-23 | |
US08/363,180 | 1994-12-23 | ||
PCT/US1995/013267 WO1996020160A1 (en) | 1994-12-23 | 1995-10-10 | 1,3,3-(trisubstituted)cyclohexane dimers and related compounds |
Publications (1)
Publication Number | Publication Date |
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JPH10511387A true JPH10511387A (ja) | 1998-11-04 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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JP8520430A Ceased JPH10511387A (ja) | 1994-12-23 | 1995-10-10 | 1,3,3−(三置換)シクロヘキサンダイマーおよび関連化合物 |
Country Status (3)
Country | Link |
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EP (1) | EP0799185A4 (ja) |
JP (1) | JPH10511387A (ja) |
WO (1) | WO1996020160A1 (ja) |
Families Citing this family (3)
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EP2217562A2 (en) | 2007-11-26 | 2010-08-18 | Teva Pharmaceutical Industries Ltd. | Crystal forms of o-desmethylvenlafaxine fumarate |
EP2252574A1 (en) * | 2008-03-06 | 2010-11-24 | Teva Pharmaceutical Industries Ltd. | Processes for the preparation of o-desmethylvenlafaxine, free from its dimer impurities |
US8569371B2 (en) | 2010-03-29 | 2013-10-29 | Pliva Hrvatska D.O.O. | Crystal forms of O-desmethylvenlafaxine fumarate |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
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JP3333510B2 (ja) * | 1991-10-02 | 2002-10-15 | スミスクライン・ビーチャム・コーポレイション | 抗アレルギー、抗炎症および腫瘍壊死因子抑制活性を有するシクロペンタンおよびシクロペンテン誘導体 |
EP0634930A4 (en) * | 1992-04-02 | 1995-02-22 | Smithkline Beecham Corporation | Compounds useful for treating allergic and inflammatory diseases. |
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1995
- 1995-10-10 WO PCT/US1995/013267 patent/WO1996020160A1/en not_active Application Discontinuation
- 1995-10-10 JP JP8520430A patent/JPH10511387A/ja not_active Ceased
- 1995-10-10 EP EP95938251A patent/EP0799185A4/en not_active Withdrawn
Also Published As
Publication number | Publication date |
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WO1996020160A1 (en) | 1996-07-04 |
EP0799185A1 (en) | 1997-10-08 |
EP0799185A4 (en) | 1998-03-25 |
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