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1. 发明申请

US20110160173A1 Method Of Treating Human Skin And A Skin Care Composition For Use In Such A Method 有权
标题翻译：治疗人类皮肤的方法和用于这种方法的护肤组合物
公开(公告)号：US20110160173A1
公开(公告)日：2011-06-30
申请号：US13017858
申请日：2011-01-31
申请人： Herman Jan Tijmen Coelingh Bennink , Evert Johannes Bunschoten , Christian Franz Holinka
发明人： Herman Jan Tijmen Coelingh Bennink , Evert Johannes Bunschoten , Christian Franz Holinka
IPC分类号： A61K8/63 , A61K31/566 , A61P17/02 , A61P17/10 , A61Q19/08
CPC分类号： A61Q19/004 , A61K8/63 , A61K9/0014 , A61K31/565 , A61K47/22 , A61K47/26 , A61Q19/00 , A61Q19/08
摘要： 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.
摘要翻译：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。

2. 发明授权

US07923440B2 Method of treating or preventing immune mediated disorders and pharmaceutical formulation for use therein 有权
标题翻译：治疗或预防免疫介导的病症的方法及其中使用的药物制剂
公开(公告)号：US07923440B2
公开(公告)日：2011-04-12
申请号：US10517686
申请日：2003-06-11
申请人： Evert Johannes Bunschoten , Herman Jan Tijmen Coelingh Bennink , Christian Franz Holinka
发明人： Evert Johannes Bunschoten , Herman Jan Tijmen Coelingh Bennink , Christian Franz Holinka
IPC分类号： A01N45/00 , A61K31/56
CPC分类号： A61K31/565 , Y10S514/874 , Y10S514/903
摘要： A method of treating or preventing an immune mediated disorder 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; 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. Another aspect of the invention relates to a pharmaceutical formulation comprising the aforementioned estrogenic component, an immunotherapeutic agent and a pharmaceutically acceptable excipient.
摘要翻译：一种治疗或预防哺乳动物免疫介导的病症的方法，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：由下式表示的物质式中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; 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。本发明的另一方面涉及包含上述雌激素成分，免疫治疗剂和药学上可接受的赋形剂的药物制剂。

3. 发明授权

US07732430B2 Drug delivery system comprising a tetrahydroxilated estrogen for use in hormonal contraception 有权
标题翻译：包含用于激素避孕的四氧化雌激素的药物递送系统
公开(公告)号：US07732430B2
公开(公告)日：2010-06-08
申请号：US10478365
申请日：2002-05-23
申请人： Evert Johannes Bunschoten , Herman Jan Tijmen Coelingh Bennink , Christian Franz Holinka
发明人： Evert Johannes Bunschoten , Herman Jan Tijmen Coelingh Bennink , Christian Franz Holinka
IPC分类号： A61K31/56
CPC分类号： A61K31/56 , A61K31/565 , Y10S514/841 , Y10S514/843
摘要： A method of contraception in mammalian females, which method comprises the oral 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 pharmaceutical kit comprising oral dosage units that contain the aforementioned estrogenic component and/or a progestogenic component.
摘要翻译：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口服给予生育能力的雌激素成分，其中雌激素成分选自由其中R1，R2，R3，R4独立地是氢原子，羟基或具有1-5个碳原子的烷氧基的下式（1） 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/或孕激素成分的口服剂量单位的药物试剂盒。

4. 发明授权

US07723320B2 Use of estrogen compounds to increase libido in women 有权
标题翻译：使用雌激素化合物来增加女性的性欲
公开(公告)号：US07723320B2
公开(公告)日：2010-05-25
申请号：US10478264
申请日：2002-05-17
申请人： Evert Johannes Bunschoten , Herman Jan Tijmen Coelingh Bennink , Christian Franz Holinka
发明人： Evert Johannes Bunschoten , Herman Jan Tijmen Coelingh Bennink , Christian Franz Holinka
IPC分类号： A61K31/56
CPC分类号： A61K9/0034 , A61K31/00 , A61K31/56 , A61K31/565 , A61K45/06 , A61K2300/00
摘要： Disclosed is a method of increasing libido in a woman, said method comprising administering to said woman an effective amount 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.
摘要翻译：公开了一种增加女性性欲的方法，所述方法包括向所述妇女施用有效量的选自以下的雌激素成分：由下式（I）表示的物质，其中式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; 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。

5. 发明授权

US07943604B2 Method of treating human skin and a skin care composition for use in such a method 有权
标题翻译：治疗人类皮肤的方法和用于这种方法的护肤组合物
公开(公告)号：US07943604B2
公开(公告)日：2011-05-17
申请号：US10517509
申请日：2003-06-11
申请人： Herman Jan Tijmen Coelingh Bennink , Evert Johannes Bunschoten , Christian Franz Holinka
发明人： Herman Jan Tijmen Coelingh Bennink , Evert Johannes Bunschoten , Christian Franz Holinka
IPC分类号： A61K31/56 , A61K8/02
CPC分类号： A61Q19/004 , A61K8/63 , A61K9/0014 , A61K31/565 , A61K47/22 , A61K47/26 , A61Q19/00 , A61Q19/08
摘要： The invention relates to cosmetic methods of treating human skin. The method includes applying to the skin a composition containing an estrogenic component and 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. Another aspect relates to a skin care composition comprising the aforementioned estrogenic component and a cosmetically acceptable vehicle.
摘要翻译：本发明涉及治疗人类皮肤的美容方法。该方法包括向皮肤施用含有雌激素成分和美容上可接受的载体的组合物。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。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。

6. 发明授权

US09040509B2 Method of treating human skin and a skin care composition for use in such a method 有权
标题翻译：治疗人类皮肤的方法和用于这种方法的护肤组合物
公开(公告)号：US09040509B2
公开(公告)日：2015-05-26
申请号：US13017858
申请日：2011-01-31
申请人： Herman Jan Tijmen Coelingh Bennink , Evert Johannes Bunschoten , Christian Franz Holinka
发明人： Herman Jan Tijmen Coelingh Bennink , Evert Johannes Bunschoten , Christian Franz Holinka
IPC分类号： A61K31/565 , A61K8/63 , A61Q19/00 , A61K9/00 , A61Q19/08 , A61K47/22 , A61K47/26
CPC分类号： A61Q19/004 , A61K8/63 , A61K9/0014 , A61K31/565 , A61K47/22 , A61K47/26 , A61Q19/00 , A61Q19/08
摘要： 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.
摘要翻译：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。

7. 发明授权

US09034854B2 Pharmaceutical composition comprising estetrol derivatives for use in cancer therapy 有权
标题翻译：包含用于癌症治疗的雌酮衍生物的药物组合物
公开(公告)号：US09034854B2
公开(公告)日：2015-05-19
申请号：US10521040
申请日：2003-07-11
申请人： Herman Jan Tijmen Coelingh Bennink , Evert Johannes Bunschoten
发明人： Herman Jan Tijmen Coelingh Bennink , Evert Johannes Bunschoten
IPC分类号： A01N45/00 , A61K31/56 , A61K45/06 , A61K31/565
CPC分类号： A61K45/06 , A61K31/4196 , A61K31/565 , A61K2300/00
摘要： 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.
摘要翻译：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。

8. 发明授权

US07815912B2 Method of controlled ovarian hyperstimulation and pharmaceutical kit for use in such method 有权
标题翻译：控制卵巢过度刺激的方法和用于此类方法的药物试剂盒
公开(公告)号：US07815912B2
公开(公告)日：2010-10-19
申请号：US10517028
申请日：2003-06-06
申请人： Evert Johannes Bunschoten , Herman Jan Tijmen Coelingh Bennink
发明人： Evert Johannes Bunschoten , Herman Jan Tijmen Coelingh Bennink
IPC分类号： C07K14/59 , A61K38/24
CPC分类号： A61K38/24 , A61K2300/00
摘要： One aspect of the present invention is concerned with a method of controlled ovarian hyperstimulation in a mammalian female, said method comprising the co-administration to said female of —a substance having follicle stimulating hormone activity (FSH substance) in an amount effective to stimulate multiple follicular development; —gonadotropin releasing hormone (GnRH) antagonist in an amount equivalent to a daily subcutaneous dose of at least 0.5 mg ganirelix to prevent a premature LH-surge; and —a LH substance in an amount effective to prevent or suppress symptoms of luteinising hormone (LH) deficiency resulting from the administration of the GnRH antagonist; followed by administering a meiosis and luteinisation inducing substance (ML substance) in an amount effective to stimulate resumption of meiosis and luteinisation, and wherein the LH substance is not obtained from the urine of human females. Another aspect of the to invention relates to a pharmaceutical kit for use in a method of controlled hyperstimulation, which kit comprises: —at least one parenteral or oral dosage unit containing one or more FSH substances in an amount equivalent to a subcutaneous dose of 50-1500 I.U. FSH; —at least one parenteral dosage unit containing one or more GnRH antagonists in an amount equivalent to a subcutaneous dose of 0.5-25 mg ganirelix; —at least one parenteral dosage unit containing one or more LH substances in an amount equivalent to a subcutaneous dose of 50-3000 I.U. recombinant LH; wherein the LH substance is not obtained from the urine of human females.
摘要翻译：本发明的一个方面涉及一种在哺乳动物雌性中控制卵巢过度刺激的方法，所述方法包括向所述女性共同施用具有促卵泡激素活性的物质（FSH物质），其量有效刺激多发性滤泡发育; - 促性腺激素释放激素（GnRH）拮抗剂，其剂量相当于至少0.5mg ganirelix的每日皮下剂量，以防止LH过度升高; 和一种有效预防或抑制由施用GnRH拮抗剂引起的促黄体激素（LH）缺乏症状的LH物质; 随后施用有效刺激减数分裂和黄体生成恢复的量的减数分裂和黄体生成诱导物质（ML物质），并且其中LH物质不是从人类女性的尿中获得的。本发明的另一方面涉及用于受控超刺激方法的药物试剂盒，该试剂盒包含： - 至少一种胃肠外或口服剂量单位，其含有相当于50-剂量皮下剂量的一种或多种FSH物质， 1500 IU FSH; - 至少一个含有一种或多种GnRH拮抗剂的胃肠外剂量单位，其剂量相当于皮下剂量为0.5-25mg ganirelix; - 至少一个含有一种或多种LH物质的肠胃外剂量单位，其量相当于皮下剂量为50-3000IU。重组LH; 其中LH物质不是从人类女性的尿中获得的。

9. 发明授权

US08987240B2 Pharmaceutical compositions comprising estetrol derivatives for use in cancer therapy 有权
标题翻译：包含用于癌症治疗的雌酮衍生物的药物组合物
公开(公告)号：US08987240B2
公开(公告)日：2015-03-24
申请号：US10532320
申请日：2003-10-23
申请人： Herman Jan Tijmen Coelingh Bennink , Evert Johannes Bunschoten
发明人： Herman Jan Tijmen Coelingh Bennink , Evert Johannes Bunschoten
IPC分类号： A61K31/565
CPC分类号： A61K31/565 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a method of treating or preventing estrogen-suppressed 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 (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; 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 is particularly useful in the treatment or prevention of colorectal and prostate cancer and, unlike commonly used estrogens, does not simultaneously enhance the risk of estrogen-stimulated cancers such as breast cancer.
摘要翻译：本发明涉及治疗或预防哺乳动物中雌激素抑制肿瘤的方法，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（I）表示，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; 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特别可用于治疗或预防结肠直肠癌和前列腺癌，并且与常用的雌激素不同，不同时增强雌激素刺激的癌症如乳腺癌的风险。

10. 发明授权

US08048869B2 Pharmaceutical composition for use in hormone replacement therapy 有权
标题翻译：用于激素替代疗法的药物组合物
公开(公告)号：US08048869B2
公开(公告)日：2011-11-01
申请号：US10478262
申请日：2002-05-17
申请人： Evert Johannes Bunschoten , Herman Jan Tijmen Coelingh Bennink , Christian Franz Holinka
发明人： Evert Johannes Bunschoten , Herman Jan Tijmen Coelingh Bennink , Christian Franz Holinka
IPC分类号： A61K31/56
CPC分类号： A61K45/06 , A61K9/0034 , A61K31/00 , A61K31/56 , A61K31/565 , A61K2300/00
摘要： One aspect of the invention is concerned with a method of hormone replacement therapy, which method comprises administering to a person in need of such a therapy an effective amount of an estrogenic component selected from the group consisting of: substances represented by the formula in which formula R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alokxy 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 thereof; said composition containing virtually no progestogen or anti-progestin. Another aspect of the invention relates to a drug delivery system for enteral or parenteral administration that contains at least 1 μg of the aforementioned estrogenic component and virtually no progestogen or anti-progestin.
摘要翻译：本发明的一个方面涉及激素替代疗法的方法，该方法包括向需要这种治疗的人施用有效量的选自以下的雌激素成分：由下式表示的物质，其中式 R 1，R 2，R 3，R 4独立地为氢原子，羟基或具有1-5个碳原子的羟基; 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; 当本方法使用时能够释放根据上述式的物质的前体及其混合物; 所述组合物几乎不含孕激素或抗孕激素。本发明的另一方面涉及一种用于肠内或肠胃外给药的药物递送系统，其包含至少1μg上述雌激素成分，实质上不含孕激素或抗孕激素。

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