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1. 发明申请

US20070155836A1 Steroids having a mixed androgenic and progestagenic profile 失效
标题翻译：具有混合雄激素和孕激素特征的类固醇
公开(公告)号：US20070155836A1
公开(公告)日：2007-07-05
申请号：US10584006
申请日：2004-12-15
申请人： Jaap Van Der Louw , Dirk Leysen , Arii Grootenhuis , Marcel De Gooijer
发明人： Jaap Van Der Louw , Dirk Leysen , Arii Grootenhuis , Marcel De Gooijer
IPC分类号： A61K31/22 , A61K31/15 , A61K31/12 , C07C67/02
CPC分类号： C07J63/008
摘要： This invention provides 19-nor-D-homos-teroids, having a mixed androgenic/progestagenic profile, which are orally active, prevent trabecular bone mineral density (BMD) loss, and which lack liver toxicity, having a structure according to the formula (I) wherein, R1 is O, or NOR, with R being hydrogen, (C1-6)alkyl or (C1-6)acyl, R2 is methyl or ethyl, and R3 is hydrogen or (C1-15)acyl.
摘要翻译：本发明提供具有口服活性的混合雄激素/孕激素分布的19-去甲基-D-同系物，预防小梁骨矿物质密度（BMD）损失，并且其缺乏肝毒性，具有根据式 I）其中R 1是O或NOR，其中R是氢，（C 1-6 - ）烷基或（C 1-6）烷基或 >）酰基，R 2是甲基或乙基，R 3是氢或（C 1-15）酰基。

2. 发明申请

US20090291929A1 STEROIDS HAVING A MIXED ANDROGENIC AND PROGESTAGENIC PROFILE 审中-公开
标题翻译：具有混合原始和原始性状的STEROIDS
公开(公告)号：US20090291929A1
公开(公告)日：2009-11-26
申请号：US11917464
申请日：2006-06-16
申请人： Jaap Van Der Louw , Dirk Leysen , Marcel Evert De Gooijer , Joseph Maria Gerardus Barbara Cals
发明人： Jaap Van Der Louw , Dirk Leysen , Marcel Evert De Gooijer , Joseph Maria Gerardus Barbara Cals
IPC分类号： A61K31/566 , C07J1/00
CPC分类号： C07J63/008
摘要： The invention provides for compounds having formula (1) wherein; R1 is O, (H,H), (H,OH), or NOR, with R being hydrogen, (C1-6) alkyl or (C1-6) acyl; R2 is hydrogen, methyl, ethyl, or ethenyl; R3 is hydrogen, methyl, ethyl, ethenyl, fluoro, or chloro; R4 is methyl, or ethyl; R5 is hydrogen, methyl, or ethyl; R6 is hydrogen, methyl, ethyl, (C1-3) alkenyl, or (C1-3) alkynyl; R7 is hydrogen or (C1-15) acyl; and at least one of R5 or R6 is hydrogen; or a pharmaceutically acceptable salt thereof, for use as medicine for a treatment to increase androgen levels, for androgen supplementation, for testosterone replacement and for benign prostate hypertrophy and in a method of male contraception, preferably as sole means to achieve both progestagenic sterilitant effect and androgen supplementation.
摘要翻译：本发明提供具有式（1）的化合物，其中： R 1是O，（H，H），（H，OH）或NOR，其中R是氢，（C 1-6）烷基或（C 1-6）酰基; R2是氢，甲基，乙基或乙烯基; R3是氢，甲基，乙基，乙烯基，氟或氯; R4是甲基或乙基; R5是氢，甲基或乙基; R6是氢，甲基，乙基，（C1-3）烯基或（C1-3）炔基; R7是氢或（C1-15）酰基; 并且R 5或R 6中的至少一个是氢; 用作治疗用于增加雄激素水平，用于雄激素补充，用于睾酮替代和良性前列腺肥大的药物的药物，以及用于男性避孕的方法中，优选作为实现孕激素相关性效应的唯一手段雄激素补充。

3. 发明授权

US06313108B1 Orally active androgens 失效
标题翻译：口服活性雄激素
公开(公告)号：US06313108B1
公开(公告)日：2001-11-06
申请号：US09613350
申请日：2000-07-11
申请人： Hubert Jan Jozef Loozen , Dirk Leysen , Jaap van der Louw
发明人： Hubert Jan Jozef Loozen , Dirk Leysen , Jaap van der Louw
IPC分类号： A61K3156
CPC分类号： C07J1/0074 , C07J1/007
摘要： Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.
摘要翻译：新型口服活性雄激素为7α-取代的DELTA14-诺酮类衍生物。化合物满足通式：其中R 1为O，（H，H），（H，OR），NOR，R为氢，（C 1-6）烷基或（C 1-6）酰基; R 2选自由（C2-4）烷基，（C2-4）烯基或（C2-4）炔基组成的基团，各自任选被卤素取代; 或者R 2是环丙基或环丙烯基，其各自任选地被（C 1-2）烷基或卤素取代; R 3是氢，（C 1-2）烷基或乙烯基; R 4是（C 1-2）烷基; R 5是氢或（ C1-15）酰基;虚线表示任选的键。

4. 发明授权

US06552011B1 (Androst-5-en-17beta -yl)alkyl sulfoxides and sulfones and their use for control of fertility 失效
标题翻译：（雄甾-5-en-17β-基）烷基亚砜和砜及其用于控制生育力的用途
公开(公告)号：US06552011B1
公开(公告)日：2003-04-22
申请号：US09913932
申请日：2001-08-20
申请人： Dirk Leysen , Jaap van der Louw , Anja Wiersma
发明人： Dirk Leysen , Jaap van der Louw , Anja Wiersma
IPC分类号： A61K3156
CPC分类号： A61K31/573 , Y10S514/841 , Y10S514/843
摘要： The invention relates to (androst-5-en-17beta-yl)alkylsulfoxides and sulfones having general formula (I), wherein R1, R2, R3, X and Y are defined in the specification. The compounds of the invention have meiosis inhibiting activity and can be used for the control of fertility.
摘要翻译：本发明涉及具有通式（I）的（雄甾-5-烯-17β-基）烷基亚砜和砜，其中R1，R2，R3，X和Y在本说明书中定义。本发明的化合物具有减数分裂抑制活性，可用于控制生育力。

5. 发明授权

US07582622B2 Steroids having a mixed androgenic and progestagenic profile 失效
标题翻译：具有混合雄激素和孕激素特征的类固醇
公开(公告)号：US07582622B2
公开(公告)日：2009-09-01
申请号：US10584006
申请日：2004-12-15
申请人： Jaap Van Der Louw , Dirk Leysen , Arij Jan Grootenhuis , Marcel Evert De Gooijer
发明人： Jaap Van Der Louw , Dirk Leysen , Arij Jan Grootenhuis , Marcel Evert De Gooijer
IPC分类号： A61K31/56 , A01N37/02 , A61K31/22 , A01N33/24 , A61K31/15 , C07C49/00
CPC分类号： C07J63/008
摘要： The invention provides 19-nor-D-homosteroids, having a mixed androgenic/progestagenic profile, which are orally active, prevent trabecular bone mineral density (BMD) loss, and which lack liver toxicity, having a structure according to the formula (I) wherein, R1 is O, or NOR, with R being hydrogen, (C1-6)alkyl, or (C1-6)acyl, R2 is methyl or ethyl, and R3 is hydrogen or (C1-15)acyl.
摘要翻译：本发明提供具有口服活性的混合雄激素/孕激素分布的19-去甲D-类固醇，预防小梁骨矿物质密度（BMD）损失，并且其缺乏肝毒性，具有根据式（I）的结构，其中R1是O或NOR，其中R是氢，（C1-6）烷基或（C1-6）酰基，R2是甲基或乙基，R3是氢或（C1-15）酰基。

6. 发明授权

US07037916B2 Pyrimidine derivatives as IL-8 receptor antagonists 失效
标题翻译：嘧啶衍生物作为IL-8受体拮抗剂
公开(公告)号：US07037916B2
公开(公告)日：2006-05-02
申请号：US10340398
申请日：2003-01-10
申请人： Shawn David Erickson , John J. Baldwin , Roland Ellwood Dolle, III , James Inglese , Michael H. J. Ohlmeyer , Koc-Kan Ho , Adolph C Bohnstedt , Steven G. Kultgen , Paolo Giovanni Martino Conti , Dirk Leysen , Jaap van der Louw
发明人： Shawn David Erickson , John J. Baldwin , Roland Ellwood Dolle, III , James Inglese , Michael H. J. Ohlmeyer , Koc-Kan Ho , Adolph C Bohnstedt , Steven G. Kultgen , Paolo Giovanni Martino Conti , Dirk Leysen , Jaap van der Louw
IPC分类号： A61K31/52 , C07D413/00 , C07D239/02 , C70D473/00
CPC分类号： C07D239/42 , C07D231/12 , C07D233/56 , C07D239/47 , C07D249/08 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/12
摘要： Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula I In these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, —O—alkyl or —S-alkyl. A representative example is:
摘要翻译：公开了含有嘧啶核的化合物及其用于治疗与不适当的白细胞介素-8受体活性有关的疾病和病症的用途。化合物具有式I化合物。在这些化合物中，Q优选为未取代的和取代的杂环基; U通常是氢或氟; 且V优选为氢，卤素，烷基，-O-烷基或-S-烷基。一个代表性的例子是：

7. 发明授权

US06949531B2 14 β, 16, 17-methylene steroids as novel androgens 有权
标题翻译： 14β，16,17-亚甲基类固醇作为新型雄激素
公开(公告)号：US06949531B2
公开(公告)日：2005-09-27
申请号：US10450278
申请日：2001-12-05
申请人： Jaap Van Der Louw , Dirk Leysen , Marcel Evert De Gooijer
发明人： Jaap Van Der Louw , Dirk Leysen , Marcel Evert De Gooijer
IPC分类号： A61K45/00 , A61K31/56 , A61K31/567 , A61P5/26 , A61P5/36 , A61P15/16 , C07J53/00
CPC分类号： C07J53/004
摘要： Disclosed are androgenic steroids of the (14β,17α)-17-(hydroxymethyl) type. The invention relates to an improvement thereof, which is based on the presence of a β-oriented, annellated cyclopropyl group which includes carbon atoms 16 and 17 of the steroid skeleton, i.e. a 16,17β-methylene moiety. These steroids show an unexpectedly high androgenic potency.
摘要翻译：公开了（14beta，17α）-17-（羟甲基）型的雄激素类固醇。本发明涉及其改进，其基于存在包含类固醇骨架的碳原子16和17的β取向的环状环丙基，即16,17β-亚甲基部分。这些类固醇表现出意想不到的高雄激素效力。

8. 发明授权

US06706700B2 14&bgr;,15&bgr;-methylene-17&agr;-hydroxymethyl-androgens 失效
标题翻译： 14beta，15beta-亚甲基-17α-羟甲基雄激素
公开(公告)号：US06706700B2
公开(公告)日：2004-03-16
申请号：US10148820
申请日：2002-09-11
申请人： Dirk Leysen , Jaap Van der Louw , Roberta Buma Bursi , Marcel Evert De Gooyer
发明人： Dirk Leysen , Jaap Van der Louw , Roberta Buma Bursi , Marcel Evert De Gooyer
IPC分类号： A61K3156
CPC分类号： C07J53/004
摘要： The disclosed invention relates to the unexpected finding of novel steroids which are characterized by a 14&bgr;,15&bgr;-cyclopropane ring and a 17&agr; hydroxymethyl group. These steroids according to the invention are found to have in common an androgenic activity. They can be used for the preparation of an agent for male contraception, as well as for the preparation of a medicament for the treatment of androgen insufficiency.
摘要翻译：所公开的发明涉及新颖类固醇的意想不到的发现，其特征在于14beta，15beta-环丙烷环和17α羟甲基。发现根据本发明的这些类固醇具有共同的雄激素活性。它们可以用于制备男性避孕药物，以及用于制备用于治疗雄激素不足的药物。

9. 发明授权

US06780854B2 Orally active androgens 失效
标题翻译：口服活性雄激素
公开(公告)号：US06780854B2
公开(公告)日：2004-08-24
申请号：US10280038
申请日：2002-10-24
申请人： Hubert Jan Jozef Loozen , Dirk Leysen , Jaap van der Louw
发明人： Hubert Jan Jozef Loozen , Dirk Leysen , Jaap van der Louw
IPC分类号： A61K3156
CPC分类号： C07J1/0074 , C07J1/007
摘要： Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C,1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.
摘要翻译：新型口服活性雄激素为7α-取代的Delta 14-去甲内酯衍生物。化合物满足通式：其中R 1是O，（H，H），（H，OR），NOR，其中R是氢，（C 1-6）烷基或（C 1-6）酰基; 由（C2-4）烷基，（C2-4）烯基或（C2-4）炔基组成的基团，各自任选被卤素取代; 或者R 2是环丙基或环丙烯基，其各自任选地被（C 1-2）烷基或卤素取代; R 3是氢，（C 1-2）烷基或乙烯基; R 4是（C 1-2）烷基; R 5是氢或（ C1-15）酰基;虚线表示任选的键。

10. 发明授权

US06756366B1 Orally active androgens 失效
标题翻译：口服活性雄激素
公开(公告)号：US06756366B1
公开(公告)日：2004-06-29
申请号：US09937274
申请日：2001-09-24
申请人： Jaap van der Louw , Dirk Leysen , Roberta Burma Bursi
发明人： Jaap van der Louw , Dirk Leysen , Roberta Burma Bursi
IPC分类号： A61K3156
CPC分类号： C07J1/007 , C07J1/0074
摘要： Orally Active androgens are derivative of 7&agr;-methyl-19-nortestosterone. The compounds satisfy formula (I) wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6)alkyl, or (C1-6)acyl; R2 is selected from the group consisting of (C2-3)alkyl, isopropyl, (C2-3)1-alkenyl, isopropenyl, 1,2-proandienyl, or (C2-3)1-alynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2)alkyl, or halogen; R3 is hydrogen, (C1-2)alkyl, or ethenyl; R4 is (C1-2)alkyl; R5 is hydrogen, or (C1-15)acyl; and the dotted lines indicate optional bonds.
摘要翻译：口服活性雄激素是7α-甲基-19-去睾酮的衍生物。化合物满足式（I）其中R 1为O，（H，H），（H，OR），NOR，其中R为氢，（C 1-6）烷基或（C 1-6）酰基; R2选自（C2-3）烷基，异丙基，（C2-3）-1-链烯基，异丙烯基，1,2-环戊二烯基或（C2-3）-1-亚苄基，各自任选被卤素取代; 或R 2为环丙基或环丙烯基，各自任选被（C 1-2）烷基或卤素取代; R3是氢，（C1-2）烷基或乙烯基; R4是（C1-2）烷基; R5是氢，或（C1-15）酰基; 虚线表示可选的债券。

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