公开(公告)号：US20240307415A1

公开(公告)日：2024-09-19

申请号：US18573968

申请日：2022-06-23

申请人： JIANGSU SIMCERE PHARMACEUTICAL CO., LTD.

发明人： Lifeng LIU ,  Zhen LI ,  Xiaoqing LIU ,  Xiaofeng ZHAO ,  Xiaojuan CHA ,  Feng TANG ,  Yayuan FU ,  Zhuoxiao CAO ,  Renhong TANG ,  Jinsheng REN

IPC分类号： A61K31/58 ,  A61P5/46 ,  C07J71/00

CPC分类号： A61K31/58 ,  A61P5/46 ,  C07J71/0031

摘要： A compound as represented by formula (I) or a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof, a preparation method therefor, and the use thereof in the treatment of tumors, inflammatory diseases or autoimmune diseases.

公开(公告)号：US11787834B2

公开(公告)日：2023-10-17

申请号：US17700943

申请日：2022-03-22

申请人： Eli Lilly and Company

发明人： Adel Ahmed Rashad Ahmed ,  Joshua Ryan Clayton ,  Jose Eduardo Lopez ,  William Thomas McMillen ,  Ryan Edward Stites ,  Takako Wilson ,  Jacqueline Mary Wurst

IPC分类号： C07J71/00

CPC分类号： C07J71/0031

摘要： The present invention provides a compound of Formula I:




wherein R is H or





R1 is H, halogen, C1-C3 alkyl, C3-C6 cycloalkyl, C1-C3 alkoxy, C2-C3 alkenyl, OCF3,





R2 is H, halogen, C1-C3 alkyl, C1-C3 alkoxy, or C2-C4 alkenyl;

R3 is NH2, or CH2NH2; and

X is O, OCH2, OCH2CH2, OCH(CH3), CH2O, SCH2, CH2S, CH2, NHCH2, CH2NH, N(CH3)CH2, CH2CH2, C≡C, or a bond, wherein X is connected to phenyl ring A at the ortho or the meta position, or a pharmaceutically acceptable salt thereof, wherein the compound of Formula I, or pharmaceutically acceptable salt thereof is useful for treating autoimmune and inflammatory diseases, such as atopic dermatitis and rheumatoid arthritis.

公开(公告)号：US20190209702A1

公开(公告)日：2019-07-11

申请号：US16243020

申请日：2019-01-08

申请人： Regeneron Pharmaceuticals, Inc.

发明人： Amy HAN

IPC分类号： A61K47/68 ,  A61K31/58 ,  A61K31/7048 ,  A61K31/685 ,  A61K47/54 ,  C07K16/28 ,  C07K16/32

CPC分类号： A61K47/6803 ,  A61K31/58 ,  A61K31/685 ,  A61K31/7048 ,  A61K47/542 ,  A61K47/545 ,  A61K47/549 ,  A61K47/6849 ,  A61K47/6855 ,  A61K47/6889 ,  C07J71/0031 ,  C07K16/2866 ,  C07K16/2896 ,  C07K16/32 ,  C07K2317/41

摘要： Described herein protein steroid conjugates that are useful, for example, for the target-specific delivery of glucocorticoids (GCs) to cells.

公开(公告)号：US20150141390A1

公开(公告)日：2015-05-21

申请号：US14345028

申请日：2012-09-14

申请人： Michael Davidson ,  John F. Arnett ,  Sadik Elshani ,  Roelof Rongen

发明人： Michael Davidson ,  John F. Arnett ,  Sadik Elshani ,  Roelof Rongen

IPC分类号： A61K47/48 ,  A61K31/573 ,  A61K31/575

CPC分类号： A61K47/48123 ,  A61K31/573 ,  A61K31/575 ,  A61K47/554 ,  C07J9/00 ,  C07J31/006 ,  C07J41/0055 ,  C07J71/0031

摘要： The invention relates to a drug conjugate including a drug and a plant steroid. The drug conjugate may target the drug for intestinal cell delivery, and thus may be used to treat diseases, including intestinal diseases, or to affect intestinal metabolism. The invention therefore also relates to treating intestinal diseases and affecting intestinal metabolism with the drug conjugate.

摘要翻译： 本发明涉及包含药物和植物类固醇的药物缀合物。 药物缀合物可以靶向用于肠细胞递送的药物，因此可用于治疗包括肠道疾病在内的疾病或影响肠代谢。 因此，本发明还涉及用药物缀合物治疗肠道疾病和影响肠代谢。

公开(公告)号：US20150126483A1

公开(公告)日：2015-05-07

申请号：US14399780

申请日：2013-05-06

申请人： Aciex Therapeutics, Inc.

发明人： Thomas Cavanagh ,  Shikha P. Barman ,  Tian Hao ,  Thomas B. Leland ,  Ritesh V. Thekkedath

IPC分类号： C07J7/00

CPC分类号： C07J7/009 ,  C07B2200/13 ,  C07J3/005 ,  C07J31/006 ,  C07J71/0005 ,  C07J71/0031 ,  Y10T428/2982

摘要： The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).

摘要翻译： 本发明进一步提供制备疏水性治疗剂如氟替卡松或曲安奈德的纳米晶体的方法，药物组合物（例如，局部或鼻内组合物）以及用于治疗和/或预防诸如睑炎的疾病的体征和/或症状的方法 ，睑板腺功能障碍或皮肤炎症或呼吸系统疾病（如哮喘）。

公开(公告)号：US08754205B2

公开(公告)日：2014-06-17

申请号：US13474594

申请日：2012-05-17

申请人： Pawan Kumar Goel

发明人： Pawan Kumar Goel

IPC分类号： C07H1/06 ,  C07H1/08

CPC分类号： C07J71/0031 ,  A61K36/48

摘要： Disclosed is an extract obtained by a commercially viable process for the extraction of furostanolic saponins from fenugreek seeds, in which one of the compounds in the extract is protodioscin. The process includes providing plurality of fenugreek seeds and crushing the same by milling and grinding; performing a primary extraction on the prepared fenugreek seeds using a first hydrophilic polar solvent which is a lower primary aliphatic alcohol followed by ion-exchange chromatography; performing a secondary extraction after ion-exchange chromatography using a composite solvent; and decolorizing the final extract by use of activated charcoal concentration of the extract by heating and vacuum drying sieving the final powdered product.

摘要翻译： 公开了通过商业上可行的从葫芦巴种子提取呋喃维生素皂苷的提取物，其中提取物中的一种化合物是原二糖蛋白。 该方法包括提供多个葫芦巴种子并通过研磨和研磨将其破碎; 使用第一亲水极性溶剂（其为低级伯脂肪醇，然后进行离子交换色谱法）对所制备的葫芦巴种子进行初次提取; 使用复合溶剂进行离子交换层析后的二次萃取; 并通过加热和真空干燥筛分最终粉末产品，通过使用提取物的活性炭浓度使最终提取物脱色。

公开(公告)号：US08518920B2

公开(公告)日：2013-08-27

申请号：US13056921

申请日：2009-07-07

申请人： Francesca Benedini ,  Annalisa Bonfanti ,  Valerio Chiroli ,  Rebecca Steele ,  Ennio Ongini ,  Stefano Biondi

发明人： Francesca Benedini ,  Annalisa Bonfanti ,  Valerio Chiroli ,  Rebecca Steele ,  Ennio Ongini ,  Stefano Biondi

IPC分类号： A61K31/58 ,  A61K31/573 ,  C07J5/00 ,  C07J71/00

CPC分类号： C07J71/0031 ,  C07J41/005

摘要： The invention relates to nitrooxy derivatives of fluocinolone acetonide, triamcinolone acetonide, betamethasone and beclomethasone, methods for their preparation, pharmaceutical compositions containing these compounds, and methods of using these compounds and compositions for treating diabetic macular edema, diabetic retinopathy, macular degeneration, age-related macular degeneration and other diseases of retina and macula lutea.

公开(公告)号：US20120295857A1

公开(公告)日：2012-11-22

申请号：US13474594

申请日：2012-05-17

申请人： Pawan Kumar GOEL

发明人： Pawan Kumar GOEL

IPC分类号： A61K31/7048

CPC分类号： C07J71/0031 ,  A61K36/48

摘要： Disclosed is an extract obtained by a commercially viable process for the extraction of furostanolic saponins from fenugreek seeds, in which one of the compounds in the extract is protodioscin. The process includes providing plurality of fenugreek seeds and crushing the same by milling and grinding; performing a primary extraction on the prepared fenugreek seeds using a first hydrophilic polar solvent which is a lower primary aliphatic alcohol followed by ion-exchange chromatography; performing a secondary extraction after ion-exchange chromatography using a composite solvent; and decolorizing the final extract by use of activated charcoal concentration of the extract by heating and vacuum drying sieving the final powdered product.

摘要翻译： 公开了通过商业上可行的从葫芦巴种子提取呋喃维生素皂苷的提取物，其中提取物中的一种化合物是原二糖蛋白。 该方法包括提供多个葫芦巴种子并通过研磨和研磨将其破碎; 使用第一亲水极性溶剂（其为低级伯脂肪醇，然后进行离子交换色谱法）对所制备的葫芦巴种子进行初次提取; 使用复合溶剂进行离子交换层析后的二次萃取; 并通过加热和真空干燥筛分最终粉末产品，通过使用提取物的活性炭浓度使最终提取物脱色。

公开(公告)号：US20110262368A1

公开(公告)日：2011-10-27

申请号：US12736064

申请日：2008-12-18

申请人： John C. Anthes ,  Kevin D. McCormick ,  John A. Hey ,  Robert G. Aslanian ,  Purakkattle J. Biju ,  Michael Y. Berlin ,  Daniel M. Solomon ,  Philippa H. Solomon ,  Hongwu Yang ,  Yeon-Hee Lim ,  Yoon Joo Lee ,  Rema Danielle Bitar

发明人： John C. Anthes ,  Kevin D. McCormick ,  John A. Hey ,  Robert G. Aslanian ,  Purakkattle J. Biju ,  Michael Y. Berlin ,  Daniel M. Solomon ,  Philippa H. Solomon ,  Hongwu Yang ,  Yeon-Hee Lim ,  Yoon Joo Lee ,  Rema Danielle Bitar

IPC分类号： A61K31/58 ,  C07J31/00 ,  A61K31/573 ,  A61P25/00 ,  A61P27/02 ,  A61P27/14 ,  A61P29/00 ,  A61P11/06 ,  A61P11/00 ,  A61P17/00 ,  A61P17/06 ,  A61P17/04 ,  A61P31/12 ,  A61P31/00 ,  A61P11/02 ,  A61P37/06 ,  A61P37/08 ,  A61P11/10 ,  C07J43/00

CPC分类号： C07J43/003 ,  C07J31/006 ,  C07J71/0031

摘要： The present invention provides compounds of Formula (VII) and 11-keto analogs thereof, and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds and said 11-keto analogs, having the general structure formula (VII): wherein L, R1, R2, R3, R4, and R5 are selected independently of each other and as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions. The novel compounds of the present invention possess useful pharmacological activity while having unexpectedly low systemic activity. Thus, the compounds of the invention represent a safer alternative to those known glucocorticoids which have poor side-effect profiles.

摘要翻译： 本发明提供了具有通式（Ⅶ）的所述化合物和所述11-酮类似物的式（Ⅶ）化合物及其11-酮类似物及其可药用盐，溶剂合物，酯，前体药物，互变异构体和异构体， ：其中L，R 1，R 2，R 3，R 4和R 5彼此独立地选择并如本文所定义。 还提供了药物组合物，制备方法和使用这些化合物在治疗和预防广泛范围的免疫，自身免疫和炎性疾病和病症中的方法。 本发明的新型化合物具有有用的药理活性，同时具有意想不到的全身活性。 因此，本发明的化合物代表具有差的副作用特征的已知糖皮质激素的更安全的替代方案。

公开(公告)号：US20100099654A1

公开(公告)日：2010-04-22

申请号：US12531214

申请日：2008-03-13

申请人： Myhren Finn ,  Marit Liland Sandvold ,  Ole Henrik Eriksen ,  Steinar Hagen

发明人： Myhren Finn ,  Marit Liland Sandvold ,  Ole Henrik Eriksen ,  Steinar Hagen

IPC分类号： A61K31/56 ,  C07J3/00 ,  C07J71/00 ,  A61P11/00 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07J31/006 ,  C07J71/0031

摘要： The present invention relates to certain unsaturated fatty acid derivatives of therapeutically active glucocorticoides-fatty acid esters of glucocorticoids as anti-inflammatory and anti-cancer agents and pharmaceutical formulations containing them.

摘要翻译： 本发明涉及作为抗炎剂和抗癌剂的糖皮质激素的治疗​​活性的糖皮质激素 - 脂肪酸酯的某些不饱和脂肪酸衍生物和含有它们的药物制剂。