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1. 发明授权

US5073568A Antipsoriatic agents 失效
标题翻译：抗菌药物
公开(公告)号：US5073568A
公开(公告)日：1991-12-17
申请号：US270980
申请日：1988-11-14
申请人： Peter M. Wovkulich , Milan R. Uskokovic , Ann Goldstein , John A. McLane
发明人： Peter M. Wovkulich , Milan R. Uskokovic , Ann Goldstein , John A. McLane
IPC分类号： A61K31/22 , A61K31/365 , A61P3/06 , A61P17/00 , C07C53/21 , C07C69/63 , C07C69/708 , C07D309/30
CPC分类号： C07C53/21 , C07D309/30 , Y10S514/824 , Y10S514/863
摘要： The invention relates to compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl; A is ##STR2## or A is ##STR3## wherein R.sub.2 is lower alkyl; R.sub.3 is phenyl, or phenyl substituted by 1 to 3 substituents selected from the group consisting of halo, lower alkyl, and lower alkoxy; and R.sub.4 is hydrogen or methyl or the corresponding hydroxy acid of formula ##STR4## wherein A is ##STR5## or A is ##STR6## and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as described above; or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid, an acetylamino-substituted-C.sub.1-4 alkyl ester of said acid, a phenyl-dimethylamino ester of said acid or a .alpha.-monoglyceride of said acid.The compounds of formulas I and II are useful as agents for the treatment of hyperproliferative skin diseases such as psoriasis.
摘要翻译：本发明涉及式Ⅰ化合物，其中R 1是氢或甲基; A是或A是，其中R2是低级烷基; 或者被1至3个选自卤代，低级烷基和低级烷氧基的取代基取代的苯基; 并且R 4是氢或甲基或相应的式II的羟基酸，其中A是A或A是R 1，R 2，R 3和R 4如上所述; 或所述酸的药学上可接受的盐，所述酸的C 1-4烷基酯，所述酸的乙酰氨基取代的C 1-4烷基酯，所述酸的苯基二甲基氨基酯或所述酸的α-单酸甘油酯。式I和II的化合物可用作治疗过度增生性皮肤疾病如牛皮癣的药剂。

2. 发明授权

US5401733A Stable and active metabolites of 1,25-dihydroxy-16-ene-cholecalciferol 失效
标题翻译： 1,25-二羟基-16-烯 - 胆钙化甾醇的稳定和活性代谢物
公开(公告)号：US5401733A
公开(公告)日：1995-03-28
申请号：US131264
申请日：1993-10-01
申请人： John A. McLane , Satyanarayama G. Reddy , Milan R. Uskokovic
发明人： John A. McLane , Satyanarayama G. Reddy , Milan R. Uskokovic
IPC分类号： A61K31/59 , A61K31/593 , A61P17/00 , A61P17/06 , A61P35/00 , A61P35/02 , C07C401/00
CPC分类号： C07C401/00
摘要： The invention relates to the compounds 1,25-dihydroxy-16-ene-24-oxo-cholecalciferol and 1,24,25-trihydroxy-16-ene-cholecalciferol which stimulate differentiation of HL-60 cells, rendering them useful as an agent for the treatment of neoplastic diseases such as leukemia, and also decrease proliferation of human keratinocytes, rendering them useful as an agent for the treatment of hyperproliferative disorders of the skin such as psoriasis.
摘要翻译：本发明涉及刺激HL-60细胞分化的化合物1,25-二羟基-16-烯-24-氧代 - 胆钙化甾醇和1,24,25-三羟基-16-烯 - 胆钙化甾醇，使其可用作试剂用于治疗诸如白血病的肿瘤性疾病，并且还减少人角质形成细胞的增殖，使其可用作治疗皮肤过度增生性疾病如银屑病的药剂。

3. 发明授权

US5393900A Steroid intermediates for the formation of vitamin D.sub.3 analogues 失效
标题翻译：类固醇中间体形成维生素D3类似物
公开(公告)号：US5393900A
公开(公告)日：1995-02-28
申请号：US255012
申请日：1994-06-07
申请人： Thomas I. Doran , John A. McLane , Masami Okabe , Michelangelo Scalone , Milan R. Uskokovic
发明人： Thomas I. Doran , John A. McLane , Masami Okabe , Michelangelo Scalone , Milan R. Uskokovic
IPC分类号： A61K31/59 , A61K31/593 , A61K31/695 , A61P3/02 , A61P17/00 , C07C401/00 , C07F7/18 , C07J9/00 , C07J13/00 , C07J51/00
CPC分类号： C07F7/1856 , C07C401/00 , C07J51/00
摘要： The invention comprises compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or acyl; provided that only one of R.sup.1 or R.sup.2 is hydrogen, useful in the treatment of hyperproliferative skin diseases and sebaceous gland diseases. The invention also includes a process for making these compounds and steroid intermediates of the process.
摘要翻译：本发明包括式I的化合物，其中R 1和R 2是氢或酰基; 只要R1或R2中只有一个是氢，可用于治疗过度增生性皮肤病和皮脂腺疾病。本发明还包括制备该方法的这些化合物和类固醇中间体的方法。

4. 发明授权

US5200549A Antipsoriatic agents 失效
标题翻译：抗牛皮癣药
公开(公告)号：US5200549A
公开(公告)日：1993-04-06
申请号：US764641
申请日：1991-09-24
申请人： Peter M. Wovkulich , Milan R. Uskokovic , Ann Goldstein , John A. McLane
发明人： Peter M. Wovkulich , Milan R. Uskokovic , Ann Goldstein , John A. McLane
IPC分类号： C07C53/21 , C07D309/30
CPC分类号： C07C53/21 , C07D309/30
摘要： The invention relates to compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl; ##STR2## wherein R.sub.2 is lower alkyl; R.sub.3 is phenyl, or phenyl substituted by 1 to 3 substituents selected from the group consisting of halo, lower alkyl, and lower alkoxy; and R.sub.4 is hydrogen or methyl or the corresponding hydroxy acid of formula ##STR3## and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as described above; or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid, an acetylamino-substituted-C.sub.1-4 alkyl ester of said acid, a phenyl-dimethylamino ester of said acid or a .alpha.-monoglyceride of said acid.The compounds of formulas I and II are useful as agents for the treatment of hyperproliferative skin diseases such as psoriasis.
摘要翻译：本发明涉及式Ⅰ化合物，其中R 1是氢或甲基; 其中R2是低级烷基; 或者被1至3个选自卤代，低级烷基和低级烷氧基的取代基取代的苯基; 并且R 4是氢或甲基，或者相应的式II的羟基酸，R 1，R 2，R 3和R 4如上所述; 或所述酸的药学上可接受的盐，所述酸的C 1-4烷基酯，所述酸的乙酰氨基取代的C 1-4烷基酯，所述酸的苯基二甲基氨基酯或所述酸的α-单酸甘油酯。式I和II的化合物可用作治疗过度增生性皮肤疾病如牛皮癣的药剂。

5. 发明申请

US20110112010A1 OCTANOIC ACID FORMULATIONS AND METHODS OF TREATMENT USING THE SAME 审中-公开
标题翻译：十八酸制剂及其使用方法
公开(公告)号：US20110112010A1
公开(公告)日：2011-05-12
申请号：US12867702
申请日：2009-02-12
申请人： Mark Hallett , John A. McLane , Fatta B. Nahab
发明人： Mark Hallett , John A. McLane , Fatta B. Nahab
IPC分类号： A61K38/16 , A61K31/20 , A61K31/5513 , A61K31/23 , A61K31/7028 , A61P25/16 , A61P5/16 , A61P25/08 , A61P1/16
CPC分类号： A61K31/23 , A61K31/201 , A61K45/06 , A61K2300/00
摘要： The invention features pharmaceutical formulations containing octanoic acid or a salt or ester thereof. The pharmaceutical formulations are useful for the treatment of involuntary tremors.
摘要翻译：本发明的特征在于含有辛酸或其盐或酯的药物制剂。药物制剂可用于治疗不自主的震颤。

6. 发明授权

US5428029A Vitamin D3 fluorinated analogs 失效
标题翻译：维生素D3氟化类似物
公开(公告)号：US5428029A
公开(公告)日：1995-06-27
申请号：US158068
申请日：1993-11-24
申请人： Thomas I. Doran , Bernard M. Hennessy , John A. McLane , Giacomo Pizzolato , Farhad Sedarati , Milan R. Uskokovic
发明人： Thomas I. Doran , Bernard M. Hennessy , John A. McLane , Giacomo Pizzolato , Farhad Sedarati , Milan R. Uskokovic
IPC分类号： A61K31/59 , A61K31/593 , A61P17/00 , A61P35/00 , A61P35/02 , C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： Compounds of the formula ##STR1## wherein R is hydrogen, hydroxy, or fluorine, X is H.sub.2 or .dbd.CH.sub.2, and the 23,24-double bond is E or Z, are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of tumors such as breast cancer, as agents for the treatment of neoplastic diseases such as leukemia, and as agents for the treatment of sebaceous gland diseases such as acne and seborrheic dermatitis.
摘要翻译：其中R是氢，羟基或氟，X是H 2或= CH 2，并且23,24-双键是E或Z的式的化合物可用作治疗过度增殖性疾病的药剂皮肤如牛皮癣，作为治疗诸如乳腺癌的肿瘤的药剂，作为用于治疗诸如白血病的肿瘤疾病的药剂，以及用于治疗皮脂腺疾病如痤疮和脂溢性皮炎的药剂。

7. 发明授权

US5021451A Method for inhibiting hyperproliferative diseases 失效
标题翻译：抑制过度增殖性疾病的方法
公开(公告)号：US5021451A
公开(公告)日：1991-06-04
申请号：US270983
申请日：1988-11-14
申请人： John A. McLane , Milan R. Uskokovic
发明人： John A. McLane , Milan R. Uskokovic
IPC分类号： A61K31/22 , A61K31/365 , A61P17/00 , A61P43/00 , C07C69/03 , C07D309/30
CPC分类号： A61K31/365 , A61K31/22 , Y10S514/863
摘要： A method of treating hyperproliferative skin diseases, such as psoriasis, using a compound of formula ##STR1## wherein R.sub.1 is hydrogen when R.sub.2 is hydroxy, and R.sub.1 is methyl when R.sub.2 is hydrogen; and A is alkyl; cycloalkyl; alkenyl; alkyl substituted with trifluoromethyl; phenyl; halophenyl; phenyl-C.sub.1-3 alkyl; phenyl-C.sub.1-3 alkyl substituted on the phenyl with 1 to 3 substituents selected from the group consisting of halo, C.sub.1-3 alkyl, and C.sub.1-3 alkoxy; orA is ##STR2## wherein R.sub.3 is hydrogen or ##STR3## R.sub.4 is hydrogen or methyl, and n is 1 to 5, or the corresponding hydroxy acid of formula ##STR4## or a pharmaceutically acceptable salt of said acid, an alkyl ester of said acid, an acetylamino-substituted-C.sub.1-4 alkyl ester of said acid, a phenyl-dimethylamino ester of said acid or a .alpha.-monoglyceride of said acid.
摘要翻译：一种治疗过度增生性皮肤病的方法，例如银屑病，其中当R 2为羟基时，其中R 1为氢，R 2为氢时R 1为甲基; A是烷基; 环烷基烯基; 被三氟甲基取代的烷基; 苯基; 卤代苯基; 苯基-C 1-3烷基; 在苯基上被1至3个选自卤素，C 1-3烷基和C 1-3烷氧基的取代基取代的苯基-C 1-3烷基; 或A是其中R 3是氢或者R 4是氢或甲基，n是1至5，或相应的式II的羟基酸或所述酸的药学上可接受的盐，烷基酯的所述酸，所述酸的乙酰氨基取代的C 1-4烷基酯，所述酸的苯基二甲基氨基酯或所述酸的α-单酸甘油酯。

8. 发明申请

US20090215892A1 Octanol Formulations and Methods of Treatment Using the Same 审中-公开
标题翻译：辛醇制剂及其使用方法
公开(公告)号：US20090215892A1
公开(公告)日：2009-08-27
申请号：US12083141
申请日：2006-10-05
申请人： Fatta B. Nahab , Mark Hallett , Jeff Serbin , John A. McLane
发明人： Fatta B. Nahab , Mark Hallett , Jeff Serbin , John A. McLane
IPC分类号： A61K31/045 , A61K31/23
CPC分类号： A61K31/045 , A61K9/2846 , A61K9/2866 , A61K9/4825 , A61K9/4858
摘要： The invention features pharmaceutical formulations containing octanol and esters thereof. The pharmaceutical formulations are useful for the treatment of involuntary tremors.
摘要翻译：本发明的特征在于含有辛醇及其酯的药物制剂。药物制剂可用于治疗不自主的震颤。

9. 发明授权

US5342833A Vitamin D3 analogs 失效
标题翻译：维生素D3类似物
公开(公告)号：US5342833A
公开(公告)日：1994-08-30
申请号：US155663
申请日：1993-11-22
申请人： Thomas I. Doran , John A. McLane , Masami Okabe , Michelangelo Scalone , Milan R. Uskokovic
发明人： Thomas I. Doran , John A. McLane , Masami Okabe , Michelangelo Scalone , Milan R. Uskokovic
IPC分类号： A61K31/59 , A61K31/593 , A61K31/695 , A61P3/02 , A61P17/00 , C07C401/00 , C07F7/18 , C07J9/00 , C07J13/00 , C07J51/00
CPC分类号： C07F7/1856 , C07C401/00 , C07J51/00
摘要： The invention is drawn to compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or acyl; provided that only one of R.sup.1 or R.sup.2 is hydrogen, useful in the treatment of hyperproliferative skin diseases and sebaceous gland diseases.
摘要翻译：本发明涉及下式的化合物，其中R 1和R 2是氢或酰基; 只要R1或R2中只有一个是氢，可用于治疗过度增生性皮肤病和皮脂腺疾病。

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