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1. 发明授权

US5827883A Dermatological use of vitamin D derivatives 失效
标题翻译：维生素D衍生物的皮肤病学用途
公开(公告)号：US5827883A
公开(公告)日：1998-10-27
申请号：US875187
申请日：1997-07-21
申请人： Pierre Barbier , Marc Muller , Josef Stadlwieser
发明人： Pierre Barbier , Marc Muller , Josef Stadlwieser
IPC分类号： A61K31/59 , A61K31/00 , A61P3/00 , A61P3/02 , A61P17/00 , A61P17/02 , A61P17/06 , A61P35/00 , C07C401/00 , A01N37/02 , A01N37/08 , C07C69/66 , C07C69/74
CPC分类号： A61K31/593 , C07C401/00
摘要： A method of using vitamin D derivatives of the formula ##STR1## wherein X is .dbd.CH.sub.2 or H,H; Y is a moiety --CH(CH.sub.3)--(A).sub.n --C(O)--OR.sup.1 (a) --CH(CH.sub.3)--CH.sub.2 --O--C(O)--R.sup.2 (b) or --C(O)--OR.sup.1 (c); A is --CH.dbd.CH-- or CH.sub.2 --CH.sub.2 -- R.sup.1 is lower alkyl, cycloalkyl, cycloalkylmethyl, --CH.sub.2 R.sup.3 or --CH.sub.2 --CH.sub.2 R.sup.3 ; R.sup.2 is lower alkyl, cycloalkyl or R.sup.3 ; R.sup.3 is hydroxy-lower alkyl, hydroxy-cycloalkyl or trifluoromethyl-hydroxy-lower-alkyl; n is 0 or 1; and the dotted bond in the five membered ring is optional; in the treatment of dermatological conditions, in particular keratinization disorders such as psoriasis, as well as acne and photodamaged skin, is described. Vitamin D derivatives of the formula I above, wherein X, Y, A, R.sup.1, R.sup.2, R.sup.3 and n are as set forth above; with the proviso that X is H,H when Y is --CH(CH.sub.3)--CH.sub.2 --OC(O)--C(OH)(CH.sub.3).sub.2 and the dotted bond in the five-membered ring is not present; as well as a process for the preparation of the compounds of formula I, and pharmaceutical compositions containing a compound of the formula I wherein X, Y, A, R.sup.1, R.sup.2, R.sup.3 and n are set forth above; with the proviso that X is H,H when Y is --CH(CH.sub.3)--CH.sub.2 --OC(O)--C(OH)(CH.sub.3).sub.2 and the dotted bond in the five-membered ring is not present, are also described.
摘要翻译： PCT No.PCT / EP96 / 00176 Sec。 371日期1997年7月21日 102（e）日期1997年7月21日PCT 1996年1月17日PCT公布。公开号WO96 / 22776 日期：1996年8月1日使用式（I）所示维生素D衍生物的方法，其中X为= CH2或H，H; Y是部分-CH（CH 3） - （A）n C（O）-OR 1（a）-CH（CH 3）-CH 2 -O（O）-R 2（b）或-C（O） ; A是-CH = CH-或CH 2 -CH 2 -R 1是低级烷基，环烷基，环烷基甲基，-CH 2 R 3或-CH 2 -CH 2 R 3; R2是低级烷基，环烷基或R3; R3是羟基 - 低级烷基，羟基 - 环烷基或三氟甲基 - 羟基 - 低级 - 烷基; n为0或1; 五元环中的虚线键是任选的; 在治疗皮肤病的情况下，特别是角质化障碍如牛皮癣，以及痤疮和光损伤的皮肤。上述式I的维生素D衍生物，其中X，Y，A，R 1，R 2，R 3和n如上所述; 条件是当Y是-CH（CH 3）-CH 2 OC（O）-C（OH）（CH 3）2时，X是H，H，五元环中的虚数键不存在; 以及制备式I化合物的方法，以及含有式I化合物的药物组合物，其中X，Y，A，R 1，R 2，R 3和n如上所述; 条件是当Y是-CH（CH 3）-CH 2 OC（O）-C（OH）（CH 3）2时X是H，H，并且五元环中的虚线键不存在）。

2. 发明授权

US5914406A Azepanes and their ring homologues having protein kinase inhibiting activity 失效
标题翻译： Azepanes及其具有蛋白激酶抑制活性的环同系物
公开(公告)号：US5914406A
公开(公告)日：1999-06-22
申请号：US19876
申请日：1998-02-06
申请人： Pierre Barbier , Isabelle Huber , Fernand Schneider , Josef Stadlwieser , Sven Taylor
发明人： Pierre Barbier , Isabelle Huber , Fernand Schneider , Josef Stadlwieser , Sven Taylor
IPC分类号： A61K31/00 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4468 , A61K31/55 , A61P17/00 , A61P17/06 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D207/12 , C07D207/14 , C07D211/44 , C07D211/56 , C07D223/08 , C07D223/12 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/12
CPC分类号： C07D401/12 , C07D207/12 , C07D207/14 , C07D223/08 , C07D223/12 , C07D405/12 , C07D417/12
摘要： The compounds of formula I: wherein R.sup.1 --R.sup.9, R.sup.15, A, X, Y, and Z have the meaning given in the specification are active as protein kinase inhibitors and can be used as medicaments, particularly for the treatment of inflammatory skin disorders and alopecia.
摘要翻译：式I化合物：其中R1-R9，R15，A，X，Y和Z具有说明书中给出的含义，作为蛋白激酶抑制剂是有活性的，可用作药物，特别是用于治疗炎性皮肤病和脱发

3. 发明授权

US5583222A Azepanes and their ring homologues having protein kinase inhibiting activity 失效
标题翻译： Azepanes及其具有蛋白激酶抑制活性的环同系物
公开(公告)号：US5583222A
公开(公告)日：1996-12-10
申请号：US368690
申请日：1995-01-04
申请人： Pierre Barbier , Isabelle Huber , Fernand Schneider , Josef Stadlwieser , Sven Taylor
发明人： Pierre Barbier , Isabelle Huber , Fernand Schneider , Josef Stadlwieser , Sven Taylor
IPC分类号： A61K31/00 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4468 , A61K31/55 , A61P17/00 , A61P17/06 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D207/12 , C07D207/14 , C07D211/44 , C07D211/56 , C07D223/08 , C07D223/12 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/12 , C07D401/06 , C07D403/06 , C07D413/06
CPC分类号： C07D401/12 , C07D207/12 , C07D207/14 , C07D223/08 , C07D223/12 , C07D405/12 , C07D417/12
摘要： The compounds of formula I ##STR1## wherein R.sup.1 -R.sup.9, R.sup.15, A, X, Y, Z and n have the meaning given in the specification are active as protein kinase inhibitors and can be used as medicaments, particularly for the treatment of inflammatory skin disorders and alopecia.
摘要翻译：式I的化合物其中R1-R9，R15，A，X，Y，Z和n具有本说明书中给出的含义，作为蛋白激酶抑制剂是有活性的，可用作药物，特别是用于治疗炎症性皮肤病和脱发。

4. 发明授权

US5907038A Azepanes 失效
公开(公告)号：US5907038A
公开(公告)日：1999-05-25
申请号：US831269
申请日：1997-03-31
申请人： Pierre Barbier , Josef Stadlwieser , Sven Taylor
发明人： Pierre Barbier , Josef Stadlwieser , Sven Taylor
IPC分类号： A61K31/40 , A61K31/445 , A61K31/55 , A61P29/00 , A61P37/00 , A61P37/04 , A61P43/00 , C07D207/14 , C07D211/56 , C07D223/12 , C07D405/14 , C12P21/08 , C07D223/08
CPC分类号： C07D211/56 , C07D207/14 , C07D223/12
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is phenyl or alpha- or beta-naphthyl, which groups can be substituted by hydroxy, lower-alkyl, lower-alkoxy, lower alkoxycarbonyl, phenoxy, acyloxy, hydroxyphenoxy-sulfonyl, halogen, nitro, amino, acylamino or N-lower-alkyl-acylamino;R.sup.2 is phenyl or phenyl substituted by hydroxy or acyloxy;Y is a carbon-carbon bond or is vinylene; andn is 1,2 or 3;and pharmaceutically acceptable acid addition salts thereof are protein kinase inhibitors and can be used for the treatment of disorders mediated by such enzymes, for example, inflammatory diseases.
摘要翻译：低级烷基，低级烷氧基，低级烷氧基羰基，苯氧基，酰氧基，羟基苯氧基 - 磺酰基，卤素，硝基，氨基，酰基氨基的取代基，其中R 1为苯基或α-或β-萘基，或N-低级 - 烷基 - 酰基氨基; R2是苯基或被羟基或酰氧基取代的苯基; Y是碳 - 碳键或是亚乙烯基; n为1,2或3; 和其药学上可接受的酸加成盐是蛋白激酶抑制剂，可用于治疗由这些酶介导的病症，例如炎性疾病。

5. 发明授权

US5750706A Azepanes and their ring homologues having protein kinase inhibiting activity 失效
公开(公告)号：US5750706A
公开(公告)日：1998-05-12
申请号：US706896
申请日：1996-09-03
申请人： Pierre Barbier , Isabelle Huber , Fernand Schneider , Josef Stadlwieser , Sven Taylor
发明人： Pierre Barbier , Isabelle Huber , Fernand Schneider , Josef Stadlwieser , Sven Taylor
IPC分类号： A61K31/00 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4468 , A61K31/55 , A61P17/00 , A61P17/06 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D207/12 , C07D207/14 , C07D211/44 , C07D211/56 , C07D223/08 , C07D223/12 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/12
CPC分类号： C07D401/12 , C07D207/12 , C07D207/14 , C07D223/08 , C07D223/12 , C07D405/12 , C07D417/12
摘要： The compounds of formula I ##STR1## wherein R.sup.1 -R.sup.9, R.sup.15, A, X, Y, Z and n have the meaning given in the specification are active as protein kinase inhibitors and can be used as medicaments, particularly for the treatment of inflammatory skin disorders and alopecia.

6. 发明授权

US6136969A Azepanes 失效
公开(公告)号：US6136969A
公开(公告)日：2000-10-24
申请号：US215611
申请日：1998-12-17
申请人： Pierre Barbier , Josef Stadlwieser , Sven Taylor
发明人： Pierre Barbier , Josef Stadlwieser , Sven Taylor
IPC分类号： A61K31/40 , A61K31/445 , A61K31/55 , A61P29/00 , A61P37/00 , A61P37/04 , A61P43/00 , C07D207/14 , C07D211/56 , C07D223/12 , C07D405/14 , C12P21/08 , C07D223/08
CPC分类号： C07D211/56 , C07D207/14 , C07D223/12
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is phenyl or alpha- or beta-naphthyl, which groups can be substituted by hydroxy, lower-alkyl, lower-alkoxy, lower alkoxy-carbonyl, phenoxy, acyloxy, hydroxyphenoxy-sulfonyl, halogen, nitro, amino, acylamino or N-lower-alkyl-acylamino;R.sup.2 is phenyl or phenyl substituted by hydroxy or acyloxy;Y is a carbon-carbon bond or is vinylene; andn is 1,2 or 3;and pharmaceutically acceptable acid addition salts thereof are protein kinase inhibitors and can be used for the treatment of disorders mediated by such enzymes, for example, inflammatory diseases.
摘要翻译：低级烷基，低级烷氧基，低级烷氧基 - 羰基，苯氧基，酰氧基，羟基苯氧基 - 磺酰基，卤素，硝基，氨基，，酰基氨基或N-低级 - 烷基 - 酰基氨基; R2是苯基或被羟基或酰氧基取代的苯基; Y是碳 - 碳键或是亚乙烯基; n为1,2或3; 和其药学上可接受的酸加成盐是蛋白激酶抑制剂，可用于治疗由这些酶介导的病症，例如炎性疾病。

7. 发明授权

US06184422B2 Cyclohexanediol derivatives 有权
标题翻译：环己二醇衍生物
公开(公告)号：US06184422B2
公开(公告)日：2001-02-06
申请号：US09252508
申请日：1999-02-18
申请人： Pierre Barbier , Franz Bauer , Peter Mohr , Marc Muller , Wolfgang Pirson
发明人： Pierre Barbier , Franz Bauer , Peter Mohr , Marc Muller , Wolfgang Pirson
IPC分类号： C07C3518
CPC分类号： C07C17/00 , C07B2200/07 , C07B2200/09 , C07C45/29 , C07C45/292 , C07C47/19 , C07C47/263 , C07C47/273 , C07C403/08 , C07C2601/14 , C07F7/1804 , C07C21/14 , C07C47/21 , C07C47/195
摘要： Compounds of formula I wherein X is C═CH2 or CH2; Y and Z are independently of each other hydrogen, fluorine or hydroxy; A is —C≡C—, —CH═CH— or —CH2—CH2—, R1 and R2 are independently of each other alkyl or perfluoroalkyl; and R3 is lower alkyl are useful in the treatment or prevention of hyperproliferative skin diseases, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis; or for reversing the conditions associated with photodamage.
摘要翻译：式I的化合物，其中X为C = CH 2或CH 2; Y和Z彼此独立地为氢，氟或羟基; A为-C = C - ， - CH = CH-或-CH 2 -CH 2 - ，R 1和R 2独立地为的其它烷基或全氟烷基; R 3为低级烷基，可用于治疗或预防过度增生性皮肤病，特别是牛皮癣，基底细胞癌，角质化和角化病症; 或用于逆转与光损伤相关的条件。

8. 发明授权

US06043385A Vitamin D derivatives 有权
标题翻译：维生素D衍生物
公开(公告)号：US06043385A
公开(公告)日：2000-03-28
申请号：US203088
申请日：1998-12-01
申请人： Pierre Barbier , Franz Bauer , Peter Mohr , Marc Muller , Wolfgang Pirson
发明人： Pierre Barbier , Franz Bauer , Peter Mohr , Marc Muller , Wolfgang Pirson
IPC分类号： C07C401/00 , A61N45/00
CPC分类号： C07C401/00
摘要： The present invention relates to vitamin D derivatives of the formula I ##STR1## wherein X is C.dbd.CH.sub.2 or CH.sub.2 ;Y is hydrogen, fluorine or hydroxyZ is hydroxyn is 1 or 2R.sup.1 is lower alkyl,R.sup.2 is a branched alkyl having 3 to 8 carbon atoms which is unsubstituted or substituted with one or more halogen or OH substituents, or is a phenyl group which is unsubstituted or substituted with a branched alkyl having 3 to 8 carbon atoms which is unsubstituted or substituted with one or more halogen or OH substituents;and the dotted carbon-carbon bond in ring D is --C--C-- or --C.dbd.C--; or a pharmaceutically usable salt thereof.
摘要翻译：本发明涉及式I的维生素D衍生物，其中X为C = CH 2或CH 2; Y是氢，氟或羟基，Z是羟基，n是1或2，R 1是低级烷基，R 2是未取代或被一个或多个卤素或OH取代基取代的具有3-8个碳原子的支链烷基，或是苯基其未取代或被未取代或被一个或多个卤素或OH取代基取代的具有3-8个碳原子的支链烷基取代; 环D中的点状碳 - 碳键为-C-C-或-C = C-; 或其药学上可用的盐。

9. 发明授权

US6153605A Arylsecocholadiene derivatives 失效
标题翻译：芳基二环戊二烯衍生物
公开(公告)号：US6153605A
公开(公告)日：2000-11-28
申请号：US61381
申请日：1998-04-16
申请人： Pierre Barbier , Franz Bauer , Peter Mohr , Marc Muller , Wolfgang Pirson
发明人： Pierre Barbier , Franz Bauer , Peter Mohr , Marc Muller , Wolfgang Pirson
IPC分类号： A61K31/59 , A61P3/02 , A61P17/00 , A61P19/10 , A61P37/06 , C07C35/23 , C07C35/32 , C07C49/403 , C07C49/497 , C07C69/88 , C07C401/00 , C07F7/18 , A61K3/59
CPC分类号： C07C69/88 , C07C35/32 , C07C401/00 , C07F7/1856
摘要： Compounds of formula (I) ##STR1## as defined by the specification. The compounds are useful in the treatment or prevention of vitamin D dependent disorders, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis, leukemia, osteoporosis, hyperparathyroidism accompanying renal failure, transplant rejection and graft vs. host disease.
摘要翻译：式（I）化合物，如本说明书所定义。该化合物可用于治疗或预防维生素D依赖性疾病，特别是牛皮癣，基底细胞癌，角质化和角化病，白血病，骨质疏松症，伴随肾衰竭的甲状旁腺功能亢进，移植排斥反应和移植物抗宿主病。

10. 发明授权

US5994569A Dihomo-seco-cholestanes 失效
公开(公告)号：US5994569A
公开(公告)日：1999-11-30
申请号：US115188
申请日：1998-07-14
申请人： Pierre Barbier , Peter Mohr , Marc Muller , Christopher Self
发明人： Pierre Barbier , Peter Mohr , Marc Muller , Christopher Self
IPC分类号： A61K31/59 , A61P3/02 , A61P3/10 , A61P19/10 , A61P29/00 , A61P35/00 , A61P37/00 , C07C401/00
CPC分类号： C07C401/00
摘要： Polyunsaturated 24a,24b-dihomo-9,10-secocholestane derivatives of formula ##STR1## wherein A is a single or double bond,B.sup.1 and B.sup.2 are each independently CH.dbd.CH or C.tbd.C,T is CH.sub.2 or CH.sub.2 CH.sub.2,X is --CH.sub.2 -- or >C.dbd.CH.sub.2,R.sup.1 is H, F or OH,R.sup.2 and R.sup.3 are each independently lower alkyl or CF.sub.3, orC(R.sup.2,R.sup.3) is C.sub.3-6 -cycloalkyl,are useful in the treatment or prevention of vitamin D dependent disorders and of IL-12-dependent autoimmune diseases, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis, leukemia, osteoporosis, hyperparathyroidism accompanying renal failure, multiple sclerosis, transplant rejection, graft vs. host disease, rheumatoid arthritis, insulin-dependent diabetes mellitus, inflammatory bowel disease, septic shock and allergic encephalomyelitis.
摘要翻译：多不饱和的24a，24b-二氢-9,10-断氧胆甾烷衍生物，其中A为单键或双键，B1和B2各自独立地为CH = CH或C，3BOND C，T为CH2或CH2CH2，X为-CH2-或 > C = CH 2，R 1为H，F或OH，R 2和R 3各自独立地为低级烷基或CF 3，或C（R 2，R 3）为C 3-6环烷基，可用于治疗或预防维生素D依赖性疾病和IL-12依赖性自身免疫性疾病，特别是牛皮癣，基底细胞癌，角质化和角化病，白血病，骨质疏松症，伴随肾衰竭的甲状旁腺功能亢进，多发性硬化，移植排斥，移植物抗宿主病，类风湿性关节炎，胰岛素依赖性糖尿病，炎性肠病，败血性休克和过敏性脑脊髓炎。

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