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1.发明授权Use of 11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene derivatives and pharmaceutical compositions containing them 失效使用11,28-二氧杂-4-氮杂三环[22.3.1.04,9]二十八烷-18-烯衍生物和含有它们的药物组合物
公开(公告)号：US5366971A
公开(公告)日：1994-11-22
申请号：US982925
申请日：1992-11-30
IPC分类号： A61K31/40 , A61K31/407 , A61K31/436 , A61K31/445 , A61K31/44
CPC分类号： A61K31/436 , A61K31/40 , A61K31/407 , A61K31/445
摘要： New use of 11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene derivatives and pharmaceutical compositions containing themThe compounds of formula I, ##STR1## have been found to have excellent topical activity. They are thus indicated for use in the topical treatment of inflammatory and hyperpoliferative skin diseases and of cutaneous manifestations of immunologically-induced illnesses, such as psoriasis.
摘要翻译： 新使用11,28-二氧杂-4-氮杂三环[22.3.1.04,9]二十八烷-18-烯衍生物和含有它们的药物组合物已经发现式I化合物
I具有优异的局部活性。 因此，它们被指示用于局部治疗炎性和超增殖皮肤疾病以及免疫学诱导的疾病如牛皮癣的皮肤表现。 -
2.发明授权Use of 11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene derivatives and pharmaceutical compositions containing them 失效使用11,28-二氧杂-4-氮杂三环[22.3.1.04,9]二十八烷-18-烯衍生物和含有它们的药物组合物
公开(公告)号：US5665727A
公开(公告)日：1997-09-09
申请号：US291010
申请日：1994-08-15
IPC分类号： A61K31/40 , A61K31/407 , A61K31/436 , A61K31/445 , A61K31/44
CPC分类号： A61K31/436 , A61K31/40 , A61K31/407 , A61K31/445
摘要： The compounds of formula I, ##STR1## have been found to have excellent topical activity. They are thus indicated for use in the topical treatment of inflammatory and hyperpoliferative skin diseases and of cutaneous manifestations of immunologically-induced illnesses, such as psoriasis.
摘要翻译： 已发现式I化合物
具有优异的局部活性。 因此，它们被指示用于局部治疗炎性和超增殖皮肤疾病以及免疫学诱导的疾病如牛皮癣的皮肤表现。 -
3.发明申请Compositions comprising macrolide t-cell immunomodulators or immunosuppressants in combination with antibacterials 审中-公开包含大环内酯类T细胞免疫调节剂或免疫抑制剂与抗菌剂组合的组合物公开(公告)号：US20070117764A1
公开(公告)日：2007-05-24
申请号：US10550359
申请日：2004-04-02
申请人： Maximilian Grassberger , Johannes Hildebrandt , Stefan Hirsch , Carle Paul , Neil Ryder , Nabila Sekkat , Anton Stutz
发明人： Maximilian Grassberger , Johannes Hildebrandt , Stefan Hirsch , Carle Paul , Neil Ryder , Nabila Sekkat , Anton Stutz
IPC分类号： A61K31/7048 , A61K31/7034 , A61K31/545 , A61K31/496
CPC分类号： A61K31/635 , A61K31/436 , A61K2300/00
摘要： Highly compatible or synergistic combinations of a macrolide T-cell immunomodulator or immunosuppressant such as 33-epichloro-33-desoxyascomycin and an antibacterial such as sulfasalazin, ciprofloxacin, ofloxacin, erythromycin or gentamycin, optionally with a further pharmaceutically active agent, especially a retinoid, are provided, which are useful in particular in the treatment of diseases involving bacterial or suspected or anticipated bacterial infection, for immunomodulation or immunosuppression in conditions in which bacterial or suspected or anticipated bacterial colonization of e.g. the skin plays a role, such as atopic, contact and seborrhoeic dermatitis, eczema, psoriasis, acne, rosacea, post-peel, skin burning, itching, or IBD, and in situations of bacterial resistance.
摘要翻译： 大环内酯类T细胞免疫调节剂或免疫抑制剂如33-表氯-3-脱氧菌丝霉素和抗细菌剂如柳氮磺吡啶，环丙沙星，氧氟沙星，红霉素或庆大霉素的任何另外的药物活性剂，特别是类视色素的高度相容或协同的组合， 被提供，其特别用于治疗涉及细菌或疑似或预期的细菌感染的疾病，用于免疫调节或免疫抑制，其中细菌或疑似或预期的细菌定殖例如 皮肤起着特应性，接触性和脂溢性皮炎，湿疹，牛皮癣，粉刺，红斑痤疮，皮后，皮肤灼伤，瘙痒或IBD，以及细菌耐药的作用。
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公开(公告)号：US20070021377A1
公开(公告)日：2007-01-25
申请号：US10550356
申请日：2004-04-02
IPC分类号： A61K31/739 , A61K31/395 , A61K31/202
CPC分类号： A61K31/164 , A61K39/39 , A61K2300/00
摘要： Snyergistic combination of a macrolide T-cell immunomodulator or immunosuppressant such as 33-epichloro-33-desoxyascomycin and a ceramide such as ceramide 3, LPC-9S or linoleic acid are provided, which are useful in particular in the treatment of dermatological or mucosal diseases such as atopic or contact dermatitis or dry skin, asteatotic eczema or xerosis.
摘要翻译： 提供大环内酯类T细胞免疫调节剂或免疫抑制剂如33-表氯-3-脱氧菌丝霉素和神经酰胺如神经酰胺3，LPC-9S或亚油酸的综合组合，其特别用于治疗皮肤病学或粘膜疾病 如特应性或接触性皮炎或干性皮肤，硬皮病湿疹或干性病。
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5.发明申请Synergistic combinations of macrolide t-cell modulator or immunosuppressant and a retinoid 审中-公开大环内酯类T细胞调节剂或免疫抑制剂和类视色素的协同组合公开(公告)号：US20060100187A1
公开(公告)日：2006-05-11
申请号：US10550358
申请日：2004-04-02
申请人： Maximilian Grassberger , Stefan Hirsch , Friedrich Mayer , Josef Meingassner , Carle Paul , Nabila Sekkat , Anton Stutz
发明人： Maximilian Grassberger , Stefan Hirsch , Friedrich Mayer , Josef Meingassner , Carle Paul , Nabila Sekkat , Anton Stutz
IPC分类号： A61K31/203 , A61K31/33
CPC分类号： A61K31/05 , A61K31/07 , A61K31/436 , A61K2300/00
摘要： Additive or synergistic combinations of a macrolide T-cell immunomodulator or immunosuppressant such as 33-epichloro-33-desoxyascomycin and a retinoid, such as etretinate, isotretinoin or tazarotene, optionally with a further pharmaceutically active agent, especially an antibacterial, are provided, which are useful in particular in the treatment of dermatological diseases such as eczema, atopic dermatitis, acne, psoriasis, skin aging, sun damage, post-peel erythema and stretch marks.
摘要翻译： 提供了大环内酯类T细胞免疫调节剂或免疫抑制剂如33-表氯-3-脱氧菌丝霉素和类视黄醇如维A酸，异维A酸或他扎罗汀，任选另外的药物活性剂，特别是抗菌剂的添加剂或协同组合，其中 特别适用于治疗皮肤病，如湿疹，特应性皮炎，痤疮，牛皮癣，皮肤老化，阳光损伤，皮后红斑和妊娠纹。
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公开(公告)号：US06423722B1
公开(公告)日：2002-07-23
申请号：US09690404
申请日：2000-10-17
申请人： Cornelia Dosenbach , Maximilian Grassberger , Otto Hartmann , Amarylla Horvath , Jean-Paul Mutz , Gerhard Penn , Sabine Pfeffer , Dierk Wieckhusen
发明人： Cornelia Dosenbach , Maximilian Grassberger , Otto Hartmann , Amarylla Horvath , Jean-Paul Mutz , Gerhard Penn , Sabine Pfeffer , Dierk Wieckhusen
IPC分类号： A61K31695
CPC分类号： C07D498/18 , C30B7/00
摘要： 33-Epichloro-33-desoxyascomycin of formula I and various tautomeric or forms thereof, in crystalline form, such as Form A and Form B. Their preparation involves appropriately converting amorphous compound of formula I, or compound of formula I in other than Form A, or compound of formula I in other than Form B, respectively, from a solution thereof under crystallization-inducing conditions or conditions inducing preferential crystallization of Form A or B, respectively. Such crystals are particularly indicated for use in the preparation of topical galenical forms of the compound for pharmaceutical use, e.g. creams, emulsions and ointments.
摘要翻译： 式I的33-表氯-3-脱氧菌丝霉素及其各种互变异构体或其形式，其结晶形式如形式A和形式B.它们的制备包括适当地转化式I的无定形化合物或除形式A之外的式I化合物， 或分别由结晶诱导条件或诱导A型或B型优先结晶的条件的方法从其溶液中分离得到式I化合物。此类晶体特别用于制备局部盖仑制剂形式 用于药物用途的化合物，例如 霜，乳剂和软膏。
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7.发明授权Pipecolic acid-containing peptolides, their preparation and pharmaceutical compositions containing them 失效含有胆酸的培哚尔酮，其制备方法和含有它们的药物组合物
公开(公告)号：US5643869A
公开(公告)日：1997-07-01
申请号：US446983
申请日：1995-05-22
申请人： Michael Morris Dreyfuss , Gerhard Emmer , Maximilian Grassberger , Klaus Ruedi , Hans Tscherter
发明人： Michael Morris Dreyfuss , Gerhard Emmer , Maximilian Grassberger , Klaus Ruedi , Hans Tscherter
IPC分类号： C12N1/14 , A61K38/00 , A61P31/00 , A61P31/04 , A61P35/00 , C07K1/02 , C07K1/113 , C07K7/64 , C07K11/02 , C07K14/195 , C07K14/41 , C12P21/02 , C12P21/04 , C12R1/645 , C07K5/12 , C07K7/06
摘要： Pipecolic acid-containing peptolides wherein the peptidic backbone is of at least 9 .alpha.-amino acid residues joined together by peptide bonds, particularly the compounds of formula I ##STR1## wherein the substituents have various significances, are disclosed. They can be prepared by isolation or derivation from an appropriate microorganism strain such as S 42508/F (NRRL 15761).They have interesting pharmacological, e.g. antifungal, chemotherapeutic drug resistance reversing and to some extent immunosuppressant and antiinflammatory properties.
摘要翻译： 其中肽主链是通过肽键连接在一起的至少9个α-氨基酸残基，特别是其中取代基具有各种含义的式I的化合物。 它们可以通过从合适的微生物菌株如S 42508 / F（NRRL 15761）的分离或衍生来制备。 它们具有有趣的药理学，例如 抗真菌药，化疗药物耐药性逆转和一定程度的免疫抑制剂和抗炎性质。
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8.发明授权
公开(公告)号：US4382951A
公开(公告)日：1983-05-10
申请号：US329171
申请日：1981-12-10
IPC分类号： A61K31/35 , A61K31/352 , A61K31/38 , A61K31/382 , A61P31/04 , A61P31/10 , C07C29/14 , C07C43/225 , C07C45/51 , C07D311/58 , C07D311/70 , C07D311/72 , C07D335/06 , C07D311/04
CPC分类号： C07D335/06 , C07C29/14 , C07C43/225 , C07C45/513 , C07D311/58
摘要： Benzopyrane and benzothiopyrane derivatives which possess pharmaceutical in particular anti-mycotic activity.
摘要翻译： 具有药物特异性抗真菌活性的苯并吡喃和苯并噻喃衍生物。
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公开(公告)号：US07514554B2
公开(公告)日：2009-04-07
申请号：US11575757
申请日：2005-10-10
IPC分类号： C07D498/18
CPC分类号： C07D498/18 , C07H19/01 , Y02P20/55
摘要： A process for the production of 33-Epi-33-chloro-FR 520 in one step from FR520 wherein protecting groups are avoided.
摘要翻译： 从FR520一步制备33-Epi-33-氯-FR 520的方法，其中避免了保护基团。
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公开(公告)号：US20080071082A1
公开(公告)日：2008-03-20
申请号：US11575757
申请日：2005-10-10
IPC分类号： C07D498/12
CPC分类号： C07D498/18 , C07H19/01 , Y02P20/55
摘要： A process for the production of 33-Epi-33-chloro-FR 520 in one step from FR520 wherein protecting groups are avoided.
摘要翻译： 从FR520一步制备33-Epi-33-氯-FR 520的方法，其中避免了保护基团。
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