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    • 2. 发明授权
    • Method of treating human skin and a skin care composition for use in such a method
    • 治疗人类皮肤的方法和用于这种方法的护肤组合物
    • US09040509B2
    • 2015-05-26
    • US13017858
    • 2011-01-31
    • Herman Jan Tijmen Coelingh BenninkEvert Johannes BunschotenChristian Franz Holinka
    • Herman Jan Tijmen Coelingh BenninkEvert Johannes BunschotenChristian Franz Holinka
    • A61K31/565A61K8/63A61Q19/00A61K9/00A61Q19/08A61K47/22A61K47/26
    • A61Q19/004A61K8/63A61K9/0014A61K31/565A61K47/22A61K47/26A61Q19/00A61Q19/08
    • One aspect of the invention concerns a cosmetic method of treating human skin by delivering an estrogenic component to said skin. The method comprises applying to the skin a composition containing: (i) at least 5 μg/g of an estrogenic component selected from the group consisting of substances represented by the following formula (I) in which formula R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; each of R5, R6, R7 is a hydroxyl group; no more than 3 of R1, R2, R3, R4 are hydrogen atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors; and (ii) a cosmetically acceptable vehicle. Other aspects of the invention relate to therapeutic methods of treating or preventing vaginal dryness or acne and a therapeutic method of promoting wound healing. Yet another aspect of the invention relates to a skin care composition comprising the aforementioned estrogenic component and a cosmetically acceptable vehicle.
    • 本发明的一个方面涉及通过将雌激素成分递送至所述皮肤来治疗人皮肤的美容方法。 该方法包括向皮肤施用组合物,其含有:(i)至少5μg/ g的雌激素成分,其选自下式(I)表示的物质,其中式R1,R2,R3,R4独立地表示 是氢原子,羟基或具有1-5个碳原子的烷氧基; R5,R6,R7各自为羟基; 不超过3个R 1,R 2,R 3,R 4为氢原子; 在本方法中使用时能够释放根据上述式的物质的前体; 和一种或多种上述物质和/或前体的混合物; 和(ii)美容上可接受的载体。 本发明的其它方面涉及治疗或预防阴道干燥或痤疮的治疗方法以及促进伤口愈合的治疗方法。 本发明的另一方面涉及包含上述雌激素成分和美容上可接受的载体的护肤组合物。
    • 5. 发明授权
    • Estrogenic compounds in combination with progestogenic compounds in hormone-replacement therapy
    • 雌激素化合物与激素替代疗法中孕激素化合物的组合
    • US08026228B2
    • 2011-09-27
    • US10495707
    • 2002-05-23
    • Herman Jan Tijmen Coelingh BenninkEvert Johannes BunschotenChristian Franz Holinka
    • Herman Jan Tijmen Coelingh BenninkEvert Johannes BunschotenChristian Franz Holinka
    • A01N45/00A61K31/56
    • A61K31/565A61K31/56Y10S514/874
    • One aspect of the present invention relates to a method of hormone replacement in mammals, which method comprises the oral administration of an estrogenic component and a progestogenic component to a mammal in an effective amount to prevent or treat symptoms of hypoestrogenism, wherein the estrogenic component is selected from the group consisting of substances represented by the above formula in which formula R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; each of R5, R6, R7 is a hydroxyl group; and no more than 3 of R1, R2, R3, R4 are hydrogen atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors. Another aspect of the invention concerns a pharmaceutical kit comprising oral dosage units that contain the aforementioned estrogenic component and a progestogenic component as well as an androgenic component.
    • 本发明的一个方面涉及哺乳动物中激素替代的方法,该方法包括有效量地向哺乳动物口服施用雌激素成分和孕激素成分以预防或治疗低雌激素分泌的症状,其中雌激素成分为 选自由上式表示的物质,其中式R1,R2,R3,R4独立地是氢原子,羟基或具有1-5个碳原子的烷氧基; R5,R6,R7各自为羟基; 并且不大于3的R 1,R 2,R 3,R 4为氢原子; 在本方法中使用时能够释放根据上述式的物质的前体; 和一种或多种上述物质和/或前体的混合物。 本发明的另一方面涉及包含含有上述雌激素成分和孕激素成分以及雄激素成分的口服剂量单位的药物试剂盒。
    • 6. 发明授权
    • Drug delivery system comprising a tetrahydroxylated estrogen for use in hormonal contraception
    • 包含用于激素避孕的四羟甲基化雌激素的药物递送系统
    • US07871995B2
    • 2011-01-18
    • US10478357
    • 2002-05-23
    • Evert Johannes BunschotenHerman Jan Tijmen Coelingh BenninkChristian Franz Holinka
    • Evert Johannes BunschotenHerman Jan Tijmen Coelingh BenninkChristian Franz Holinka
    • A61K31/56
    • A61K31/00A61K9/0034A61K31/56A61K31/565A61K45/06A61K2300/00
    • A method of contraception in mammalian females, which method comprises the parenteral or rectal administration of an estrogenic component and a progestogenic component to a female of childbearing capability in an amount effective to inhibit ovulation, wherein the estrogenic component is selected from the group consisting of substances represented by the following formula (1) in which R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; each of R5, R6, R7 is a hydroxyl group; and no more than 3 of R1, R2, R3, R4 are hydrogen atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors. Another aspect of the invention concerns a drug delivery system for parenteral or rectal administration that contains the aforementioned estrogenic component and a progestogenic component, said drug delivery system being selected from the group consisting of suppositories, systems for intravaginal delivery, inhalers, nasal sprays and transdermal delivery systems.
    • 一种哺乳动物雌性避孕方法,该方法包括以有效抑制排卵量的雌激素成分和孕激素成分向生育能力女性肠胃外或直肠给药,其中雌激素成分选自物质 由下式(1)表示,其中R 1,R 2,R 3,R 4独立地为氢原子,羟基或具有1-5个碳原子的烷氧基; R5,R6,R7各自为羟基; 并且不大于3的R 1,R 2,R 3,R 4为氢原子; 在本方法中使用时能够释放根据上述式的物质的前体; 和一种或多种上述物质和/或前体的混合物。 本发明的另一方面涉及一种用于肠胃外或直肠给药的药物递送系统,其包含上述雌激素成分和孕激素成分,所述药物递送系统选自栓剂,阴道内递送系统,吸入器,鼻喷雾剂和透皮 送货系统。
    • 10. 发明授权
    • Pharmaceutical composition comprising estetrol derivatives for use in cancer therapy
    • 包含用于癌症治疗的雌酮衍生物的药物组合物
    • US09034854B2
    • 2015-05-19
    • US10521040
    • 2003-07-11
    • Herman Jan Tijmen Coelingh BenninkEvert Johannes Bunschoten
    • Herman Jan Tijmen Coelingh BenninkEvert Johannes Bunschoten
    • A01N45/00A61K31/56A61K45/06A61K31/565
    • A61K45/06A61K31/4196A61K31/565A61K2300/00
    • The present invention relates to a method of treating or preventing estrogen-sensitive tumors in a mammal, said method comprising the administration of a therapeutically effective amount of an estrogenic component to said mammal, wherein the estrogenic component is selected from the group consisting of:substances represented by the following formula in which formula R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors. The estrogenic component according to the invention does not have undesirable proliferative effects on breast and/or endometrial tissue and displays sufficient estrogenicity to prevent that its administration will lead to hypoestrogenism and/or climacteric complaints.
    • 本发明涉及治疗或预防哺乳动物中雌激素敏感性肿瘤的方法,所述方法包括向所述哺乳动物施用治疗有效量的雌激素成分,其中雌激素成分选自:物质 由式R1,R2,R3,R4独立地为氢原子,羟基或具有1-5个碳原子的烷氧基的下式表示; 在本方法中使用时能够释放根据上述式的物质的前体; 和一种或多种上述物质和/或前体的混合物。 根据本发明的雌激素成分对乳房和/或子宫内膜组织不具有不期望的增殖作用,并显示出足够的雌激素作用,以防止其施用将导致低雌激素过敏和/或更年期症状。