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公开(公告)号：US20100279936A1
公开(公告)日：2010-11-04
申请号：US12376417
申请日：2007-08-16
IPC分类号： A61K38/23
CPC分类号： C07D213/40 , C07B2200/07 , C07C211/29 , C07C211/30 , C07C211/49 , C07C215/24 , C07C215/28 , C07C215/30 , C07C215/50 , C07C215/54 , C07C217/46 , C07C217/58 , C07C217/62 , C07C229/30 , C07C229/34 , C07C229/38 , C07C233/36 , C07C233/38 , C07C233/62 , C07C235/10 , C07C235/60 , C07C237/16 , C07C255/30 , C07C255/58 , C07C271/20 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C311/05 , C07C311/18 , C07C311/29 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07D207/12 , C07D209/08 , C07D211/46 , C07D211/58 , C07D211/62 , C07D231/12 , C07D263/32 , C07D295/13 , C07D295/182 , C07D309/08 , C07D309/10 , C07D317/28 , C07D317/58 , C07D333/20 , C07D333/58 , C07F7/081 , C07F7/1804
摘要： The invention relates to novel compounds according to formula Ia and Ib; (Formula Ia and Ib) wherein A represents substituted or unsubstituted C1-10heteroaryl, C6-14aryl or C6-10heterocycloalkylaryl; R1 is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6hydroxyalkyl, C1-6haloalkyl, C1-6amino, C3-6 cycloalkyl, or C1-6heterocycloalkyl, each of which are optionally substituted; X represents —CR3R4—(CR5R6)n—(CR7═CR8)m—(C6-14aryl)r-(C1-10heteroaryl)s-(CR9R10)p—(CR11═CR12)q, R2 represents C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6hydroxyalkyl, C1-6haloalkyl, C1-6amino, C1-12alkylsilyl, C6-30alkylarylsilyl, C1-10heteroaryl, C6-14aryl, C1-10heterocycloalkyl, C1-10heterocycloalkenyl, C1-8cycloalkyl, C1-18cycloalkenyl, each of which is optionally substituted, or R2 represents hydrogen, carboxy, or hydroxy; or a pharmaceutically acceptable salt, solvate, or ester thereof; to processes for the preparation thereof, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, wherein said compounds being useful, e.g. in the treatment of diseases associated with disturbances of CaSR activity, such as hyperparathyroidism.
摘要翻译： 本发明涉及根据式Ia和Ib的新化合物; （式Ia和Ib）其中A表示取代或未取代的C1-10杂芳基，C6-14芳基或C6-10杂环烷基芳基; R 1是C 1-6烷基，C 2-6烯基，C 2-6炔基，C 1-6羟基烷基，C 1-6卤代烷基，C 1-6氨基，C 3-6环烷基或C 1-6杂环烷基，其各自任选被取代; X表示-CR3R4-（CR5R6）n-（CR7 = CR8）m-（C6-14芳基）r-（C1-10杂芳基）s-（CR9R10）p-（CR11 = CR12）q，R2表示C1-6烷基，C2 6-烯基，C 2-6炔基，C 1-6羟基烷基，C 1-6卤代烷基，C 1-6氨基，C 1-12烷基甲硅烷基，C 6-30烷基芳基甲硅烷基，C 1-10杂芳基，C 6-14芳基，C 1-10杂环烷基，C 1-10杂环烯基，C 1-8环烷基， ，其各自任选被取代，或R 2表示氢，羧基或羟基; 或其药学上可接受的盐，溶剂化物或酯; 涉及用于制备其的所述化合物，用于治疗的所述化合物，包含所述化合物的药物组合物，其中所述化合物是有用的。 治疗与CaSR活动相关的疾病，如甲状旁腺功能亢进。
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公开(公告)号：US20120101039A1
公开(公告)日：2012-04-26
申请号：US13322189
申请日：2010-05-26
IPC分类号： A61K38/23 , A61K31/24 , C07C63/36 , A61K31/195 , C07D295/10 , A61K31/5375 , C07D211/62 , A61K31/445 , C07D315/00 , A61K31/351 , A61K31/59 , A61P25/28 , A61P3/00 , A61P19/00 , A61P5/00 , A61P19/10 , A61P1/00 , C07C69/76
CPC分类号： C07D295/088 , C07C217/62 , C07C229/34 , C07C229/38 , C07C237/20 , C07C237/36 , C07D205/04 , C07D211/66 , C07D307/33 , C07D309/06 , C07D309/08 , C07D405/06
摘要： A compound of general formula I their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, methods of treating diseases with said compounds, and the use of said compounds in the manufacture of medicaments.
摘要翻译： 通式I的化合物，其用作钙受体活性化合物用于预防，治疗或改善与CaSR活性紊乱相关的生理障碍或疾病，例如甲状旁腺功能亢进，包含所述化合物的药物组合物，用所述化合物治疗疾病的方法 ，以及所述化合物在制备药物中的用途。
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公开(公告)号：US07977387B2
公开(公告)日：2011-07-12
申请号：US10563474
申请日：2004-07-09
申请人： Erik Rytter Ottosen , Anne Marie Horneman , Xifu Liang , Søren Christian Schou , Sophie Elisabeth Havez , Thomas Peter Sabroe
发明人： Erik Rytter Ottosen , Anne Marie Horneman , Xifu Liang , Søren Christian Schou , Sophie Elisabeth Havez , Thomas Peter Sabroe
IPC分类号： A61K31/136 , A61K31/12 , C07C211/56 , C07C49/303
CPC分类号： C07C225/22 , C07C233/43 , C07C235/16 , C07C235/20 , C07C235/64 , C07C237/30 , C07C237/32 , C07C237/34 , C07C237/36 , C07C237/38 , C07C237/40 , C07C243/38 , C07C245/24 , C07C247/04 , C07C255/58 , C07C259/10 , C07C271/20 , C07C271/28 , C07C271/38 , C07C275/40 , C07C275/42 , C07C311/08 , C07C311/13 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/21 , C07C311/29 , C07C311/39 , C07C311/40 , C07C311/41 , C07C311/46 , C07C317/44 , C07C323/60 , C07C337/06 , C07C2601/08 , C07C2601/14 , C07D207/27 , C07D213/40 , C07D233/76 , C07D239/22 , C07D249/06 , C07D257/04 , C07D263/14 , C07D277/24 , C07D277/54 , C07D285/12 , C07D285/135 , C07D307/14 , C07D307/52 , C07D307/54 , C07D309/12 , C07D317/22 , C07D333/38 , C07D405/12
摘要： The invention provides novel compounds according to formula I relates to compounds with the general formula I said compounds being useful, e.g. in the treatment of inflammatory, ophthalmic diseases or cancer.
摘要翻译： 本发明提供了根据式I的新化合物涉及具有通式I的化合物，所述化合物是有用的，例如， 在治疗炎症，眼科疾病或癌症。
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公开(公告)号：US20070167488A1
公开(公告)日：2007-07-19
申请号：US10582935
申请日：2004-12-16
申请人： Laetitia Bouerat Duvold , Jef Fensholdt , Simon Nielsen , Xifu Liang , Sophie Havez , Ellen Anderson , Lene Jensen , Jens Hansen
发明人： Laetitia Bouerat Duvold , Jef Fensholdt , Simon Nielsen , Xifu Liang , Sophie Havez , Ellen Anderson , Lene Jensen , Jens Hansen
IPC分类号： A61K31/454 , A61K31/4439 , A61K31/404
CPC分类号： A61K31/4439 , A61K31/404 , A61K31/454
摘要： Certain oxindole compounds have been found to be effective in experimentally induced autoimmune encephalitis and are therefore suggested for the preparation of a medicament for the prevention, treatment or amelioration of multiple sclerosis, or to delay the onset of or reduce the relapse rate in multiple sclerosis.
摘要翻译： 已经发现某些羟吲哚化合物在实验诱导的自身免疫性脑炎中是有效的，因此建议用于制备用于预防，治疗或改善多发性硬化的药物，或延迟多发性硬化症中的复发率或降低复发率。
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公开(公告)号：US09102687B2
公开(公告)日：2015-08-11
申请号：US13996989
申请日：2011-12-22
申请人： Gunnar Grue-Sørensen , Xifu Liang , Thomas Högberg , Kristoffer Månsson , Per Vedsø , Thomas Vifian
发明人： Gunnar Grue-Sørensen , Xifu Liang , Thomas Högberg , Kristoffer Månsson , Per Vedsø , Thomas Vifian
IPC分类号： C07D405/06 , C07D513/04 , C07C271/34 , C07C271/36 , C07C271/38 , C07D249/06 , C07D261/18 , C07D277/32 , C07D295/21 , C07D309/08 , C07D333/38 , C07D401/04 , C07D471/04 , C07D495/04 , C07D265/36 , C07D271/08 , C07D277/587 , C07D295/205 , C07D307/00 , C07D307/94
CPC分类号： C07D261/18 , A61K31/365 , A61K31/381 , A61K31/404 , A61K31/415 , A61K31/416 , A61K31/4192 , A61K31/42 , A61K31/472 , A61K31/502 , A61K31/5375 , A61K31/538 , C07C271/34 , C07C271/36 , C07C271/38 , C07C2603/86 , C07D209/08 , C07D209/42 , C07D213/79 , C07D215/50 , C07D217/26 , C07D231/14 , C07D231/56 , C07D233/90 , C07D237/28 , C07D239/28 , C07D249/04 , C07D249/06 , C07D261/20 , C07D263/34 , C07D265/36 , C07D271/08 , C07D277/32 , C07D277/56 , C07D277/587 , C07D295/182 , C07D295/205 , C07D295/21 , C07D307/00 , C07D307/68 , C07D307/94 , C07D309/08 , C07D333/38 , C07D333/40 , C07D401/04 , C07D405/06 , C07D471/04 , C07D493/08 , C07D495/04 , C07D513/04
摘要： The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
摘要翻译： 本发明涉及通式I的化合物，其中R是任选被R 7取代的杂芳基; 或R是任选被R 8取代的杂环烷基或杂环烯基; 或R为X，其中X为-NR 11 R 12; 其药学上可接受的盐，水合物或溶剂合物，用于单独或与一种或多种其它药学活性化合物组合用于治疗，用于预防，治疗或改善响应刺激的中性粒细胞氧化性突发的反应的疾病或病症 的角质形成细胞IL-8释放或响应于坏死的诱导。
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公开(公告)号：US20130324600A1
公开(公告)日：2013-12-05
申请号：US13996549
申请日：2011-12-22
申请人： Gunnar Grue-Sørensen , Xifu Liang , Thomas Högberg
发明人： Gunnar Grue-Sørensen , Xifu Liang , Thomas Högberg
IPC分类号： C07C255/41 , C07C251/44 , C07C69/533
CPC分类号： C07C255/41 , C07C69/013 , C07C69/24 , C07C69/533 , C07C69/54 , C07C69/60 , C07C69/608 , C07C69/614 , C07C69/616 , C07C69/618 , C07C233/56 , C07C251/44 , C07C251/48 , C07C255/23 , C07C2601/14 , C07C2603/86
摘要： The invention relates to compounds of general formula (I) wherein R is (C1-C7)alkyl, (C2-C7)alkenyl or (C2-C7)alkynyl; wherein R is substituted with R1; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
摘要翻译： 本发明涉及通式（I）的化合物，其中R是（C 1 -C 7）烷基，（C 2 -C 7）烯基或（C 2 -C 7）炔基; 其中R被R 1取代; 其药学上可接受的盐，水合物或溶剂合物，用于单独或与一种或多种其它药学活性化合物组合用于治疗，用于预防，治疗或改善响应刺激的中性粒细胞氧化性突发的反应的疾病或病症 的角质形成细胞IL-8释放或响应于坏死的诱导。
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公开(公告)号：US08901356B2
公开(公告)日：2014-12-02
申请号：US13811207
申请日：2011-07-08
申请人： Thomas Högberg , Gunnar Grue-Sørensen , Xifu Liang , Anne Marie Horneman , Anders Klarskov Petersen
发明人： Thomas Högberg , Gunnar Grue-Sørensen , Xifu Liang , Anne Marie Horneman , Anders Klarskov Petersen
IPC分类号： C07C49/753 , C07C59/90 , C07C67/08 , C07D319/08 , C07F7/18 , C07C67/297
CPC分类号： C07C67/08 , C07C49/753 , C07C59/90 , C07C67/14 , C07C67/297 , C07C2603/86 , C07C2603/98 , C07D317/70 , C07D319/08 , C07D493/08 , C07F7/1804 , Y02P20/55 , C07C69/533
摘要： The present invention relates to methods of producing ingenol-3-angelate (I) from ingenol (II). Furthermore, the invention relates to intermediates useful for the synthesis of ingenol-3-angelate (I) from ingenol (II) and to methods of producing said intermediates.
摘要翻译： 本发明涉及从烯醇（II）生产西内醇-3-天竺葵酸（I）的方法。 此外，本发明涉及可用于合成来自烯醇（II）的内酯-3-通配物（I）的中间体以及制备所述中间体的方法。
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公开(公告)号：US20060166990A1
公开(公告)日：2006-07-27
申请号：US10563474
申请日：2004-07-09
申请人： Erik Ottosen , Anne Horneman , Xifu Liang , Soren Schou , Sophie Havez , Thoma Sabroe
发明人： Erik Ottosen , Anne Horneman , Xifu Liang , Soren Schou , Sophie Havez , Thoma Sabroe
IPC分类号： A61K31/537 , A61K31/495 , A61K31/165
CPC分类号： C07C225/22 , C07C233/43 , C07C235/16 , C07C235/20 , C07C235/64 , C07C237/30 , C07C237/32 , C07C237/34 , C07C237/36 , C07C237/38 , C07C237/40 , C07C243/38 , C07C245/24 , C07C247/04 , C07C255/58 , C07C259/10 , C07C271/20 , C07C271/28 , C07C271/38 , C07C275/40 , C07C275/42 , C07C311/08 , C07C311/13 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/21 , C07C311/29 , C07C311/39 , C07C311/40 , C07C311/41 , C07C311/46 , C07C317/44 , C07C323/60 , C07C337/06 , C07C2601/08 , C07C2601/14 , C07D207/27 , C07D213/40 , C07D233/76 , C07D239/22 , C07D249/06 , C07D257/04 , C07D263/14 , C07D277/24 , C07D277/54 , C07D285/12 , C07D285/135 , C07D307/14 , C07D307/52 , C07D307/54 , C07D309/12 , C07D317/22 , C07D333/38 , C07D405/12
摘要： The invention provides novel compounds according to formula I relates to compounds with the general formula I said compounds being useful, e.g. in the treatment of inflammatory, ophthalmic diseases or cancer.
摘要翻译： 本发明提供了根据式I的新化合物涉及具有通式I的化合物，所述化合物是有用的，例如， 在治疗炎症，眼科疾病或癌症。
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公开(公告)号：US09656945B2
公开(公告)日：2017-05-23
申请号：US13997011
申请日：2011-12-22
IPC分类号： C07C69/013 , C07C69/74 , C07C69/75 , C07C69/753 , C07C69/76 , C07C69/78 , C07C69/92 , A61K31/215 , A61K31/235 , A61K31/245 , C07C229/56 , C07C229/58 , C07C229/64 , C07C233/54 , C07C255/46 , A61K31/277 , A61K45/06
CPC分类号： C07C69/74 , A61K31/215 , A61K31/235 , A61K31/245 , A61K31/277 , A61K45/06 , C07C69/013 , C07C69/75 , C07C69/753 , C07C69/76 , C07C69/78 , C07C69/92 , C07C229/56 , C07C229/58 , C07C229/64 , C07C233/54 , C07C255/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2603/86
摘要： The invention relates to compounds of general formula I, (I), wherein R is wherein R is aryl substituted by R3; or R is (C3-Ci3)-cycloalkyl, (C3-Ci3)-cycloalkenyl or (C7-Ci3)-cycloalkynyl optionally substituted by R4; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
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公开(公告)号：US20130177952A1
公开(公告)日：2013-07-11
申请号：US13811207
申请日：2011-07-08
申请人： Thomas Högberg , Gunnar Grue-Sørensen , Xifu Liang , Anne Marie Horneman , Anders Klarskov Petersen
发明人： Thomas Högberg , Gunnar Grue-Sørensen , Xifu Liang , Anne Marie Horneman , Anders Klarskov Petersen
IPC分类号： C07C49/753 , C07C59/90 , C07C67/08 , C07D319/08 , C07F7/18
CPC分类号： C07C67/08 , C07C49/753 , C07C59/90 , C07C67/14 , C07C67/297 , C07C2603/86 , C07C2603/98 , C07D317/70 , C07D319/08 , C07D493/08 , C07F7/1804 , Y02P20/55 , C07C69/533
摘要： The present invention relates to methods of producing ingenol-3-angelate (I) from ingenol (II). Furthermore, the invention relates to intermediates useful for the synthesis of ingenol-3-angelate (I) from ingenol (II) and to methods of producing said intermediates.
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