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公开(公告)号：US11724979B2
公开(公告)日：2023-08-15
申请号：US17377125
申请日：2021-07-15
发明人： Imre Juhász , Irén Hortobágyi , Tamás Altsach , István Lászlófi , Ágnes Nagyné Borkó , Imre Rozsumberszki , Gábor Havasi , Zsuzsanna Kardos , Péter Buzder-Lantos
IPC分类号： C07C51/347 , C07C41/26 , C07C45/30 , C07C45/65 , C07C51/09 , C07C51/41 , C07C67/14 , C07C67/29 , C07C67/293 , C07C69/76 , C07C41/30 , C07C41/48 , C07C43/315 , C07C13/547 , C07C35/37 , C07C59/72
CPC分类号： C07C51/347 , C07C13/547 , C07C35/37 , C07C41/26 , C07C41/30 , C07C41/48 , C07C43/315 , C07C45/30 , C07C45/305 , C07C45/65 , C07C51/09 , C07C51/412 , C07C59/72 , C07C67/14 , C07C67/29 , C07C67/293 , C07C69/76 , C07C2603/14 , C07C45/305 , C07C49/84 , C07C45/30 , C07C49/84 , C07C45/65 , C07C49/755 , C07C51/09 , C07C59/70 , C07C41/48 , C07C43/315 , C07C67/14 , C07C69/76 , C07C67/29 , C07C69/76 , C07C67/293 , C07C69/76 , C07C51/412 , C07C59/70
摘要： Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates.
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公开(公告)号：US20180230143A1
公开(公告)日：2018-08-16
申请号：US15837235
申请日：2017-12-11
IPC分类号： C07D471/04 , C07D209/42 , C07D317/60 , C07D239/22 , C07C59/68 , C07D493/04 , C07D207/337 , C07D307/68 , G01N27/447 , C07C59/70 , G01N33/50 , C07D235/28
CPC分类号： C07D471/04 , C07C59/68 , C07C59/70 , C07D207/337 , C07D209/42 , C07D235/28 , C07D239/22 , C07D307/68 , C07D317/60 , C07D493/04 , G01N27/447 , G01N33/5011 , G01N2333/47
摘要： The invention relates to inhibitors of the NHR2 tetramerization and their use as tumor therapeutics (e.g. against acute myeloid leukemia (AML)), cytostatics, and diagnostic agents.
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公开(公告)号：US20180179139A1
公开(公告)日：2018-06-28
申请号：US15892317
申请日：2018-02-08
申请人： FibroStatin, S.L.
发明人： Juan Saus , Santos Fustero , Juan F. Sanz-Cervera , Enrique Pérez-Payá , Raül Blasco , Francisco Revert-Ros , Fernando Revert
IPC分类号： C07C59/52 , C07D213/58 , C07D213/55 , C07D213/48 , C07D213/34 , C07D213/26 , C07C309/65 , C07C45/68 , C07C69/734 , C07C69/732 , C07C67/313 , C07C59/70 , C07C59/64 , C07C59/56 , C07C69/738
CPC分类号： C07C59/52 , C07C45/68 , C07C47/565 , C07C59/56 , C07C59/64 , C07C59/70 , C07C67/313 , C07C69/732 , C07C69/734 , C07C69/738 , C07C309/65 , C07D213/26 , C07D213/34 , C07D213/48 , C07D213/55 , C07D213/58
摘要： Disclosed are compounds of formula: that inhibiting GPBP activity, making them useful as therapeutics in antibody-mediated disorders, drug-resistant cancer, inflammation, protein misfolding and ER stress-mediated disorders, and aberrant apoptosis.
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4.发明申请公开(公告)号：US20160108031A1
公开(公告)日：2016-04-21
申请号：US14787151
申请日：2014-04-25
IPC分类号： C07D471/04 , C07D307/68 , C07D493/04 , G01N27/447 , C07C59/68 , C07D317/60 , C07D239/22 , G01N33/50 , C07D207/337 , C07D209/42
CPC分类号： C07D471/04 , C07C59/68 , C07C59/70 , C07D207/337 , C07D209/42 , C07D235/28 , C07D239/22 , C07D307/68 , C07D317/60 , C07D493/04 , G01N27/447 , G01N33/5011 , G01N2333/47
摘要： The invention relates to inhibitors of the NHR2 tetramerization and their use as tumor therapeutics (e.g. against acute myeloid leukemia (AML)), cytostatics, and diagnostic agents.
摘要翻译： 本发明涉及NHR2四聚化的抑制剂及其作为肿瘤治疗剂（例如针对急性骨髓性白血病（AML）），细胞抑制剂和诊断剂的用途。
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公开(公告)号：US09199936B2
公开(公告)日：2015-12-01
申请号：US14063709
申请日：2013-10-25
申请人： FibroStatin, S.L.
发明人： Juan Saus , Santos Fustero , Juan F Sanz-Cervera , Enrique Pérez-Payá , Raül Blasco , Francisco Revert-Ros , Fernando Revert
IPC分类号： C07C43/23 , C07C59/90 , C07C43/225 , C07D213/58 , C07C45/68 , C07C47/565 , C07C59/52 , C07C59/56 , C07C59/64 , C07C59/70 , C07C69/732 , C07C69/734 , C07C69/738 , C07C309/65 , C07D213/26 , C07D213/34 , C07D213/48 , C07D213/55
CPC分类号： C07C59/52 , C07C45/68 , C07C47/565 , C07C59/56 , C07C59/64 , C07C59/70 , C07C67/313 , C07C69/732 , C07C69/734 , C07C69/738 , C07C309/65 , C07D213/26 , C07D213/34 , C07D213/48 , C07D213/55 , C07D213/58
摘要： Disclosed are compounds of formula: that inhibiting GPBP activity, making them useful as therapeutics in antibody-mediated disorders, drug-resistant cancer, inflammation, protein misfolding and ER stress-mediated disorders, and aberrant apoptosis.
摘要翻译： 公开的是下式的化合物：抑制GPBP活性，使其可用作抗体介导的病症，耐药性癌症，炎症，蛋白质错误折叠和ER应激介导的病症以及异常凋亡中的治疗剂。
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公开(公告)号：US09063416B2
公开(公告)日：2015-06-23
申请号：US13706771
申请日：2012-12-06
IPC分类号： G03F7/004 , C07C59/125 , G03F7/027 , G03F7/039 , C07D313/10 , C07D327/04 , C07D333/46 , C07D333/54 , C07D333/76 , C07D335/02 , C07D335/16 , C07C323/52 , C07C381/12 , C07D493/18 , C07D307/00 , C07D307/33 , C07C25/18 , C07C69/14 , C07C69/63 , C07C69/753 , C07C69/78 , C07C59/13 , C07C59/66 , C07C59/70 , C07C62/04 , C07D493/08
CPC分类号： G03F7/027 , C07C25/18 , C07C59/125 , C07C59/13 , C07C59/66 , C07C59/70 , C07C62/04 , C07C69/14 , C07C69/63 , C07C69/753 , C07C69/78 , C07C323/52 , C07C381/12 , C07C2601/08 , C07C2603/74 , C07D307/00 , C07D307/33 , C07D313/10 , C07D327/04 , C07D333/46 , C07D333/54 , C07D333/76 , C07D335/02 , C07D335/16 , C07D493/08 , C07D493/18 , G03F7/0045 , G03F7/0397
摘要： A resist composition comprising: a base component (A) that exhibits changed solubility in a developing solution by the action of acid; a photoreactive quencher (C); and an acid-generator component (B) that generates acid upon exposure, wherein the photoreactive quencher (C) contains a compound represented by general formula (c1) shown below. In the formula, R1 represents a hydrogen atom or a hydrocarbon group of 1 to 20 carbon atoms which may have a substituent; each of R2 and R3 independently represents a hydrogen atom or a hydrocarbon group of 1 to 20 carbon atoms which may have a substituent; at least two of R1 to R3 may be mutually bonded to form a ring; X represents an oxygen atom or a sulfur atom; n represents 0 or 1; and Z+ represents an organic cation.
摘要翻译： 一种抗蚀剂组合物，其包含：通过酸作用而在显影液中显示改变的溶解度的碱成分（A） 光反应猝灭剂（C）; 以及曝光时产生酸的酸发生剂成分（B），其中，所述光反应性猝灭剂（C）含有下述通式（c1）表示的化合物。 在该式中，R 1表示氢原子或可以具有取代基的1〜20个碳原子的烃基; R 2和R 3各自独立地表示氢原子或可以具有取代基的1〜20个碳原子的烃基; R 1至R 3中的至少两个可以相互键合形成环; X表示氧原子或硫原子; n表示0或1; Z +表示有机阳离子。
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公开(公告)号：US20130331453A1
公开(公告)日：2013-12-12
申请号：US13966493
申请日：2013-08-14
发明人： Gee-Hong Kuo , Rui Zhang , Aihua Wang , Alan R. DeAngelis
IPC分类号： C07C323/20
CPC分类号： A61K31/277 , A61K31/192 , C07C59/68 , C07C59/70 , C07C317/22 , C07C323/20 , C07C323/60 , C07C323/62 , C07D333/16 , C07D333/28
摘要： The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.
摘要翻译： 本发明具有4 - （（苯氧基烷基）硫基） - 苯氧基乙酸及其类似物，含有它们的组合物，以及使用它们作为PPARδ调节剂治疗或抑制例如血脂异常进展的方法。
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公开(公告)号：US20120295980A1
公开(公告)日：2012-11-22
申请号：US13558757
申请日：2012-07-26
申请人： Ken Phares , David Mottola
发明人： Ken Phares , David Mottola
CPC分类号： C07C59/13 , A61K9/0019 , A61K9/0053 , A61K31/192 , A61K31/216 , A61K31/223 , A61K31/235 , C07C51/412 , C07C59/70 , C07C69/712 , C07C229/08 , C07C235/06 , C07C235/08 , C07C259/06 , C07C2103/10 , C07C2603/10 , C07F9/091 , C07F9/117
摘要： This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally. Compounds of the present invention have the following formula:
摘要翻译： 本发明一般涉及前列环素类似物及其用于促进血管舒张，抑制血小板聚集和血栓形成，刺激溶栓，抑制细胞增殖（包括血管重构），提供细胞保护，预防动脉粥样硬化和诱导血管生成的方法。 通常，本发明的化合物和方法在口服给药时增加了曲前列素的口服生物利用度和循环浓度。 本发明化合物具有下式：
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公开(公告)号：US08232316B2
公开(公告)日：2012-07-31
申请号：US13013155
申请日：2011-01-25
申请人： Ken Phares , David Mottola
发明人： Ken Phares , David Mottola
IPC分类号： A61K31/216 , C07C69/716
CPC分类号： C07C59/13 , A61K9/0019 , A61K9/0053 , A61K31/192 , A61K31/216 , A61K31/223 , A61K31/235 , C07C51/412 , C07C59/70 , C07C69/712 , C07C229/08 , C07C235/06 , C07C235/08 , C07C259/06 , C07C2103/10 , C07C2603/10 , C07F9/091 , C07F9/117
摘要： This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally. Compounds of the present invention have the following formula:
摘要翻译： 本发明一般涉及前列环素类似物及其用于促进血管舒张，抑制血小板聚集和血栓形成，刺激溶栓，抑制细胞增殖（包括血管重构），提供细胞保护，预防动脉粥样硬化和诱导血管生成的方法。 通常，本发明的化合物和方法在口服给药时增加了曲前列素的口服生物利用度和循环浓度。 本发明化合物具有下式：
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公开(公告)号：US20120122988A1
公开(公告)日：2012-05-17
申请号：US13332453
申请日：2011-12-21
申请人： Gee-Hong Kuo , Rui Zhang , Aihua Wang , Alan R. DeAngelis
发明人： Gee-Hong Kuo , Rui Zhang , Aihua Wang , Alan R. DeAngelis
IPC分类号： A61K31/192 , A61P3/10 , A61P9/00 , A61P3/04 , A61P7/00 , A61P3/06 , A61P9/10 , C07C321/28 , A61P3/00
CPC分类号： A61K31/277 , A61K31/192 , C07C59/68 , C07C59/70 , C07C317/22 , C07C323/20 , C07C323/60 , C07C323/62 , C07D333/16 , C07D333/28
摘要： The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.
摘要翻译： 本发明具有4 - （（苯氧基烷基）硫基） - 苯氧基乙酸及其类似物，含有它们的组合物，以及使用它们作为PPARδ调节剂治疗或抑制例如血脂异常进展的方法。
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