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公开(公告)号:US5801253A
公开(公告)日:1998-09-01
申请号:US776087
申请日:1997-01-21
IPC分类号: A01N20060101 , A61K31/07 , A61K31/19 , A61K31/215 , A61K31/38 , A61K31/381 , A61P3/02 , A61P17/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07C45/29 , C07C45/63 , C07C47/235 , C07C47/238 , C07C47/24 , C07C47/277 , C07C51/09 , C07C57/02 , C07C57/50 , C07C57/62 , C07C63/00 , C07C67/343 , C07C69/618 , C07C69/65 , C07C69/734 , C07D333/24 , C07F9/40 , C07F9/48 , C07F9/54 , C07D333/08 , C07C69/76 , C07C233/00
CPC分类号: C07F9/4056 , C07C45/29 , C07C45/298 , C07C45/63 , C07C47/24 , C07C47/277 , C07C57/50 , C07D333/24 , C07C2101/16
摘要: Compounds of formula (I) wherein R.sup.1 -R.sup.7, R.sup.10, X and the dotted bond have the meaning given in the specification, bind selectively to retinoid RXR receptors and are useful as antiproliferative agents for dermatological and oncological indications.
摘要翻译: PCT No.PCT / EP95 / 03021 Sec。 371日期1997年1月21日 102(e)日期1997年1月21日PCT提交1995年7月29日PCT公布。 公开号WO96 / 05165 日期1996年2月22日其中R1-R7,R10,X和点键具有说明书中给出的含义的式(I)化合物选择性地结合于类视黄醇RXR受体,并且可用作皮肤病学和肿瘤学适应症的抗增生剂。
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公开(公告)号:US5391766A
公开(公告)日:1995-02-21
申请号:US57949
申请日:1993-05-05
申请人: Michael Klaus , Peter Mohr
发明人: Michael Klaus , Peter Mohr
IPC分类号: A61K31/38 , A61K31/381 , A61K31/382 , A61P17/00 , A61P37/06 , C07D333/54 , C07D335/06 , C07D337/08
CPC分类号: C07D333/54 , C07D335/06 , C07D337/08
摘要: Compounds of the formula ##STR1## in which X is --S--, --SO-- or --SO.sub.2 --; R.sup.1 is C.sub.7-10 -alkyl or C.sub.7-10 -alkoxy; R.sup.2 is a residue of the formula ##STR2## R.sup.3 is carboxy or lower-alkoxycarbonyl; and n is an integer of 1, 2 or 3; and salts of carboxylic acids of formula I can be used for the treatment of autoimmune diseases and diseases having a strong immunological component, such as psoriasis.
摘要翻译: 其中X是-S-,-SO-或-SO 2 - 的式I的化合物; R1是C7-10-烷基或C7-10-烷氧基; R 2是下式的残基:(a)或(b)R 3是羧基或低级烷氧基羰基; n为1,2或3的整数; 式I的羧酸盐可用于治疗具有强免疫组分的自身免疫性疾病和疾病,例如牛皮癣。
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公开(公告)号:US5250562A
公开(公告)日:1993-10-05
申请号:US829666
申请日:1992-02-03
申请人: Michael Klaus , Peter Mohr , Ekkehard Weiss
发明人: Michael Klaus , Peter Mohr , Ekkehard Weiss
IPC分类号: C07C211/10 , C07C317/18 , C07C323/12 , C07C323/25 , C07D295/092 , C07D295/13 , A61K31/40 , C07D207/06
CPC分类号: C07D295/088 , C07C211/10 , C07C317/18 , C07C323/12 , C07C323/25 , C07D295/13 , C07C2102/08 , C07C2102/10
摘要: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are lower-alkyl; or together are alkylene with 3-5 C-atoms in a straight chain; one of the residues R.sup.3 and R.sup.4 is hydrogen and the other is hydrogen or lower-alkyl; R.sup.6 and R.sup.7 are hydrogen or lower-alkyl; R.sup.5 and R.sup.8 are hydrogen, lower-alkyl, lower-alkoxy or halogen; X signifies --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.9 ; R.sup.9 is hydrogen, lower-alkyl or acyl; Y is --S(O).sub.m R.sup.10 or --NHet and, where X is --NR.sup.9 --, --S--, --SO-- or --SO.sub.2 --, also --N(R.sup.11).sub.2 or --OR.sup.12 ; R.sup.10 is lower-alkyl; R.sup.11 and R.sup.12 are hydrogen, lower-alkyl or acyl; --NHet is a 5-8 membered, saturated or unsaturated, monocyclic heterocycle attached via a N-atom; n is 2, 3 or 4 and m is 0, 1 or 2, are described. The compounds of formula I are useful as agents for the treatment of disorders such as neoplasms, dermatoses or ageing of the skin.
摘要翻译: 式Ⅰ的化合物,其中R 1和R 2各自独立地为低级烷基; 或一起是直链中具有3-5个C原子的亚烷基; 残基R3和R4之一是氢,另一个是氢或低级烷基; R6和R7是氢或低级烷基; R5和R8是氢,低级烷基,低级烷氧基或卤素; X表示-O - , - S - , - SO - , - SO 2 - 或-NR 9; R9是氢,低级烷基或酰基; Y是-S(O)m R 10或-NHet,且其中X是-NR 9 - , - S - , - SO-或-SO 2 - ,以及-N(R 11)2或-OR 12; R10为低级烷基; R 11和R 12是氢,低级烷基或酰基; -NHet是通过N-原子连接的5-8元饱和或不饱和的单环杂环; n为2,3或4,m为0,1或2。 式I的化合物可用作治疗诸如赘生物,皮肤病或皮肤老化的病症的药剂。
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公开(公告)号:US4935560A
公开(公告)日:1990-06-19
申请号:US467291
申请日:1990-01-16
申请人: Michael Klaus , Peter Loeliger , Peter Mohr , Ekkehard Weiss
发明人: Michael Klaus , Peter Loeliger , Peter Mohr , Ekkehard Weiss
IPC分类号: A61K31/01 , A61K31/015 , A61K31/02 , A61K31/035 , A61K31/045 , A61K31/12 , A61K31/215 , C07C13/45 , C07C13/465 , C07C13/48 , C07C15/24 , C07C15/52 , C07C15/58 , C07C25/24 , C07C25/28 , C07C35/32 , C07C35/36 , C07C39/23 , C07C43/215 , C07C43/23 , C07C45/72 , C07C49/683 , C07C49/697 , C07C49/747 , C07C69/157 , C07C205/06
CPC分类号: C07C205/06 , A61K31/015 , A61K31/035 , C07C13/465 , C07C13/48 , C07C25/24 , C07C35/32 , C07C35/36 , C07C39/23 , C07C43/215 , C07C43/23 , C07C45/72 , C07C49/683 , C07C49/697 , C07C49/747 , C07C2102/08 , C07C2102/10
摘要: Novel styryl-tetrahydromaphthalene and indane derivatives useful for treating neoplasms and dermatoses.
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公开(公告)号:US5958956A
公开(公告)日:1999-09-28
申请号:US7613
申请日:1998-01-15
申请人: Michael Klaus , Peter Mohr
发明人: Michael Klaus , Peter Mohr
IPC分类号: C07D213/79 , A61K31/44 , A61K31/455 , A61K31/57 , A61P17/00 , A61P17/02 , A61P35/00 , A61P43/00 , C07D213/80 , C07D213/803 , C07D215/48 , C07D213/63 , C07D213/70
CPC分类号: C07D213/80 , A61K31/44 , A61K31/455
摘要: A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-6 -alkyl;R.sup.2 is C.sub.1-6 -alkyl or adamantyl;R.sup.3 is C.sub.1-6 -alkyl or hydroxy; orR.sup.2 and R.sup.3 taken together are --(CR.sup.6 R.sup.7).sub.n --;R.sup.4 is C.sub.2-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.2-8 -alkynyl, --OCH.sub.2 R.sup.5 or C.sub.2-8 -alkanoyl; and hydrogen when R.sup.3 is hydroxy;R.sup.5 is C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl or C.sub.2-6 -alkynyl;R.sup.6 and R.sup.7 are hydrogen or C.sub.1-6 -alkyl;Y is oxygen or sulphur; andn is 3, 4 or 5,and pharmaceutically usable salts of carboxylic acids of formula I act as selective ligands of retinoic acid .gamma.-receptors and are useful for the treatment of epithelial lesions.
摘要翻译: 下式的化合物其中R 1是氢或C 1-6 - 烷基; R2是C1-6烷基或金刚烷基; R3是C1-6烷基或羟基; 或R 2和R 3一起为 - (CR 6 R 7)n - ; R 4是C 2-8 - 烷基,C 2-8 - 烯基,C 2-8 - 炔基,-OCH 2 R 5或C 2-8 - 烷酰基; 当R3为羟基时为氢; R5是C1-6-烷基,C2-6-烯基或C2-6-炔基; R6和R7是氢或C1-6烷基; Y是氧或硫; 并且n为3,4或5,并且式I的羧酸的药学上可用的盐作为视黄酸γ-受体的选择性配体,并且可用于治疗上皮损伤。
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公开(公告)号:US5700836A
公开(公告)日:1997-12-23
申请号:US734222
申请日:1996-10-21
申请人: Michael Klaus , Peter Mohr
发明人: Michael Klaus , Peter Mohr
IPC分类号: A61K31/19 , A61K8/04 , A61K8/11 , A61K8/19 , A61K8/34 , A61K8/36 , A61K8/368 , A61K8/37 , A61K8/41 , A61K8/58 , A61K8/67 , A61K9/06 , A61K9/08 , A61K9/10 , A61K9/12 , A61K31/192 , A61K31/215 , A61K31/216 , A61K31/325 , A61K31/40 , A61P17/00 , A61P17/02 , A61P17/10 , A61P17/16 , A61Q19/00 , A61Q19/02 , C07C57/30 , C07C57/50 , C07C59/72 , C07C63/64 , C07C63/66 , C07C65/28 , C07C65/38 , C07C69/00 , C07C69/618 , C07C69/734 , C07C69/76 , C07C69/94 , A01N37/10 , A01N37/18
CPC分类号: C07C59/72 , C07C57/50 , C07C63/66 , C07C65/28 , C07C69/618 , C07C69/734 , C07C69/76 , C07C69/94 , C07C2102/10 , C07C2102/12
摘要: Compounds of the formula ##STR1## wherein R.sup.1 is a residue of the formula ##STR2## and R.sup.2 -R.sup.10 have the significance given in the specification can be used as pharmaceuticals, particularly for the repair of photodamaged skin, other dermatological conditions, and oncological indications.
摘要翻译: 其中R1是式(a)或(IMA)(b)和R2-R10的残基具有本说明书中给出的含义的式(I)的化合物可以用作药物,特别是用于修复 皮肤光滑,其他皮肤病和肿瘤适应症。
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公开(公告)号:US5128470A
公开(公告)日:1992-07-07
申请号:US551831
申请日:1990-07-12
申请人: Michael Klaus , Peter Mohr
发明人: Michael Klaus , Peter Mohr
IPC分类号: A61K31/165 , A61K31/415 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P35/00 , A61P37/00 , C07C231/02 , C07C233/64 , C07C233/65 , C07C233/66 , C07C233/73 , C07C233/75 , C07C235/56 , C07C235/64 , C07D233/64 , C07D295/08 , C07D295/088 , C07D295/092 , C07D521/00
CPC分类号: C07D295/088 , C07C233/65 , C07C233/66 , C07C233/75 , C07C235/56 , C07D231/12 , C07D233/56 , C07D249/08 , C07C2102/08 , C07C2102/10 , C07C2102/12
摘要: Compounds of the general formula ##STR1## wherein R.sup.1 is hydrogen, halogen or OR.sup.5 ; R.sup.2 is hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.3 and R.sup.4 each independently are lower-alkyl or taken together are alkylene with 3-5 C atoms in a straight-chain; R.sup.5 is hydrogen, acyl, lower-alkoxycarbonyl, lower-alkyl, amino-lower-alkyl, mono-alkylamino-lower-alkyl, di-alkylamino-lower-alkyl or a N-containing 5-8-membered saturated or unsaturated monocyclic heterocyclic ring which is attached via a N atom to lower alkyl; and M signifies --CONH-- or --NHCO--, which can be used as medicaments, e.g., for the treatment of neoplasms and dermatological indications of an inflammatory and allergic nature.
摘要翻译: 通式为其中R 1为氢,卤素或OR 5的通式为其的化合物; R2是氢,低级烷基,低级烷氧基或卤素; R3和R4各自独立地为低级烷基或一起为直链中具有3-5个C原子的亚烷基; R5是氢,酰基,低级烷氧基羰基,低级烷基,氨基 - 低级 - 烷基,单烷基氨基 - 低级 - 烷基,二烷基氨基 - 低级 - 烷基或含N的5-8元饱和或不饱和单环杂环 环通过N原子连接到低级烷基上; 并且M表示-CONH-或-NHCO-,其可以用作药物,例如用于治疗炎性和过敏性质的赘生物和皮肤病学适应症。
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公开(公告)号:US5106981A
公开(公告)日:1992-04-21
申请号:US510705
申请日:1990-04-19
申请人: Michael Klaus , Peter Mohr , Ekkehard Weiss
发明人: Michael Klaus , Peter Mohr , Ekkehard Weiss
IPC分类号: A61K31/10 , A61K20060101 , A61K31/135 , A61K31/165 , A61K31/215 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/54 , A61P17/00 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07C20060101 , C07C15/44 , C07C67/00 , C07C209/00 , C07C211/10 , C07C211/45 , C07C223/06 , C07C225/22 , C07C317/18 , C07C317/22 , C07C317/32 , C07C323/12 , C07C323/18 , C07C323/19 , C07C323/25 , C07C323/41 , C07C323/65 , C07D20060101 , C07D207/325 , C07D233/60 , C07D279/12 , C07D295/08 , C07D295/084 , C07D295/092 , C07D295/13 , C07F9/40
CPC分类号: C07D295/088 , C07C211/10 , C07C317/18 , C07C323/12 , C07C323/25 , C07D295/13 , C07C2102/08 , C07C2102/10
摘要: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are lower-alkyl; or together are alkylene with 3-5 C-atoms in a straight chain; one of the residues R.sup.3 and R.sup.4 is hydrogen and the other is hydrogen or lower-alkyl; R.sup.6 and R.sup.7 are hydrogen or lower-alkyl; R.sup.5 and R.sup.8 are hydrogen, lower-alkyl, lower-alkoxy or halogen; X signifies --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.9 ; R.sup.9 is hydrogen, lower-alkyl or acyl; Y is --S(O).sub.m R.sup.10 or --NHet and, where X is --NR.sup.9 --, --S--, --SO-- or --SO.sub.2 --, also --N(R.sup.11).sub.2 or --OR.sup.12 ; R.sup.10 is lower-alkyl; R.sup.11 and R.sup.12 are hydrogen, lower-alkyl or acyl; --NHet is a 5-8 membered, saturated or unsaturated, monocyclic heterocycle attached via a N-atom; n is 2, 3 or 4 and m is 0, 1 or 2, are described. The compounds of formula I are useful as agents for the treatment of disorders such as neoplasms, dermatoses or ageing of the skin.
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公开(公告)号:US5001276A
公开(公告)日:1991-03-19
申请号:US350416
申请日:1989-05-11
申请人: Michael Klaus , Peter Loeliger , Peter Mohr , Ekkehard Weiss
发明人: Michael Klaus , Peter Loeliger , Peter Mohr , Ekkehard Weiss
IPC分类号: A61K31/01 , A61K31/015 , A61K31/02 , A61K31/035 , A61K31/045 , A61K31/12 , A61K31/215 , C07C13/45 , C07C13/465 , C07C13/48 , C07C15/24 , C07C15/52 , C07C15/58 , C07C25/24 , C07C25/28 , C07C35/32 , C07C35/36 , C07C39/23 , C07C43/215 , C07C43/23 , C07C45/72 , C07C49/683 , C07C49/697 , C07C49/747 , C07C69/157 , C07C205/06
CPC分类号: C07C205/06 , A61K31/015 , A61K31/035 , C07C13/465 , C07C13/48 , C07C25/24 , C07C35/32 , C07C35/36 , C07C39/23 , C07C43/215 , C07C43/23 , C07C45/72 , C07C49/683 , C07C49/697 , C07C49/747 , C07C2102/08 , C07C2102/10
摘要: Novel styryl-tetrahydromaphthalene and indane derivatives useful for treating neoplasms and dermatoses.
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公开(公告)号:US06610877B1
公开(公告)日:2003-08-26
申请号:US08904522
申请日:1997-08-01
申请人: Michael Klaus , Peter Mohr
发明人: Michael Klaus , Peter Mohr
IPC分类号: C07C6976
CPC分类号: C07C59/72 , C07C57/50 , C07C63/66 , C07C65/28 , C07C69/618 , C07C69/734 , C07C69/76 , C07C69/94 , C07C2602/10 , C07C2602/12
摘要: Compounds of the formula wherein R1 is a residue of the formula and R2-R10 have the significance given in the specification can be used as pharmaceuticals, particularly for the repair of photodamaged skin, other dermatological conditions, and oncological indications.
摘要翻译: 化学式R 1的化合物是式的残基,R2-R10具有本说明书中给出的含义,可用作药物,特别是用于修复光损伤皮肤,其它皮肤病学条件和肿瘤适应症。
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