公开(公告)号：US5986129A

公开(公告)日：1999-11-16

申请号：US903663

申请日：1997-07-31

Applicant: Guido Di Napoli

Inventor： Guido Di Napoli

IPC: A61K8/30 ,  A61K8/00 ,  A61K8/35 ,  A61K8/36 ,  A61K8/368 ,  A61K8/41 ,  A61K31/19 ,  A61P43/00 ,  A61Q19/00 ,  C07C51/06 ,  C07C51/09 ,  C07C51/353 ,  C07C51/367 ,  C07C51/373 ,  C07C66/02 ,  C07C67/00 ,  C07C69/02 ,  C07C69/16 ,  C07C69/95 ,  C07C227/20 ,  C07C229/66 ,  C07C229/74 ,  C07C237/30 ,  C07C237/40 ,  C07C327/16 ,  C07C327/26 ,  C07C59/76 ,  C07C67/02

CPC classification number: C07C66/02 ,  C07C229/66 ,  Y02P20/55

Abstract: The following description sets forth a process for producing rhein, diacerhein and other diacyl derivatives thereof, which comprises the following steps: treatment of a diphenylketone ##STR1## in which R.sub.1 is --OR', --NR'R", --SR', where R' and R" are H, an alkyl or aromatic group; R.sub.2 is H or a protective group, R.sub.3 is --OH or C.sub.1 -C.sub.4 alkyl, with an acid or superacid to give a 1-aminoanthraquinone derivative, diazotisation, replacement of the --NH.sub.2 group by --OH, optional removal of the protective group, and acylation.

Abstract translation: 下面的描述阐述了生产大黄酸，二烯酰亚胺和其它二酰基衍生物的方法，其包括以下步骤：处理其中R 1是-OR'， - NR'R“，-SR'的二苯基酮，其中R' 和R“是H，烷基或芳基; R2是H或保护基团，R3是-OH或C1-C4烷基，与酸或超酸反应得到1-氨基蒽醌衍生物，重氮化，-NH 2基团被-OH取代，任选地除去保护基团， 和酰化。

公开(公告)号：US07453004B2

公开(公告)日：2008-11-18

申请号：US11667087

申请日：2005-11-11

Applicant: Stefano Carlino ,  Guido Di Napoli

Inventor： Stefano Carlino ,  Guido Di Napoli

IPC: C07C45/27 ,  C07C45/00 ,  C09B1/00

CPC classification number: C07C66/02

Abstract: A process for preparing aloe-emodin from aloin by oxidizing aloin by treatment with an oxygen-containing gas in the presence of an acid. The aloe-emodin may be used for the production of rhein and diacerein by oxidizing aloe-emodin by treatment with a chromium-free oxidizing medium to obtain rhein and purifying the rhein obtained. The rhein may be acetylated to obtain diacerein.

Abstract translation: 一种通过在酸存在下用含氧气体处理氧化芦荟来从芦荟中制备芦荟大黄素的方法。 芦荟大黄素可用于通过用无铬氧化介质处理氧化芦荟大黄素来生产大黄酸和双醋瑞因，以获得大黄酸并纯化获得的大黄酸。 可以将大黄酸乙酰化以获得双醋瑞因。

公开(公告)号：US06844365B2

公开(公告)日：2005-01-18

申请号：US09798355

申请日：2001-03-02

Applicant: Guido Di Napoli

Inventor： Guido Di Napoli

IPC: A61P17/06 ,  A61K31/192 ,  A61K31/222 ,  A61K31/235 ,  A61P37/02 ,  A61K31/19

CPC classification number: A61K31/192 ,  A61K31/222

Abstract: It is disclosed the use of diacerein or a pharmaceutically acceptable derivative thereof for the manufacture of a pharmaceutical composition for the treatment of psoriasis or diseases associated therewith, such as psoriatic arthritis.

Abstract translation: 公开了双醋瑞因或其药学上可接受的衍生物在制备用于治疗牛皮癣或其相关疾病的药物组合物如牛皮癣关节炎中的用途。

公开(公告)号：US5670695A

公开(公告)日：1997-09-23

申请号：US376722

申请日：1995-01-23

Applicant: Guido Di Napoli

Inventor： Guido Di Napoli

IPC: A61K31/235 ,  A61P29/00 ,  C07C67/08 ,  C07C67/40 ,  C07C67/52 ,  C07C69/00 ,  C07C69/16 ,  C07C69/95 ,  C07F9/02 ,  C07C49/593 ,  C07C333/00

CPC classification number: C07C67/293 ,  C07C2103/24

Abstract: The present invention relates to a process for the preparation of 1,8-diacetoxy-3-carboxyanthraquinone, also known as diacerein, via aloin acetylation, oxidation of the acetylated product, and purification of the raw diacerein obtained by means of crystallization from 2-methoxyethanol or N,N-dimethylacetamide and optionally by dissolution of the corresponding salt with triethylamine in methylene chloride, followed by removal of the insoluble residue.

Abstract translation: 本发明涉及通过芦荟乙酰化，乙酰化产物的氧化，以及通过2-甲基-2-吡咯烷酮的结晶得到的生成的双醋瑞因的纯化制备1,8-二乙酰氧基-3-羧基蒽醌（也称为双醋瑞因）的方法， 甲氧基乙醇或N，N-二甲基乙酰胺，任选地通过将相应的盐与三乙胺在二氯甲烷中溶解，然后除去不溶性残余物。

公开(公告)号：US06953776B2

公开(公告)日：2005-10-11

申请号：US10721007

申请日：2003-11-21

Applicant: Guido Di Napoli

Inventor： Guido Di Napoli

IPC: A61K9/08 ,  A61K9/00 ,  A61K31/728 ,  A61K38/00 ,  A61K38/13 ,  A61K47/26 ,  A61K47/34 ,  A61K47/36 ,  A61P27/02 ,  A61P29/00 ,  A61P37/06

CPC classification number: A61K38/13 ,  A61K9/0048 ,  A61K47/26 ,  A61K47/36

Abstract: A topical ophthalmic formulation in the form of an aqueous solution comprising a cyclosporin, hyaluronic acid or one of its salts, and polysorbate 80 is described.

Abstract translation: 描述了包含环孢菌素，透明质酸或其一种盐的水溶液形式的局部眼用制剂和聚山梨醇酯80。

公开(公告)号：US20050004045A1

公开(公告)日：2005-01-06

申请号：US10900740

申请日：2004-07-28

Applicant: Guido Di Napoli

Inventor： Guido Di Napoli

IPC: A61P17/06 ,  A61K31/192 ,  A61K31/222 ,  A61K31/235 ,  A61P37/02 ,  A61K31/19

CPC classification number: A61K31/192 ,  A61K31/222

Abstract: It is disclosed the use of diacerein or a pharmaceutically acceptable derivative thereof for the manufacture of a pharmaceutical composition for the treatment of psoriasis or diseases associated therewith, such as psoriatic arthritis.

公开(公告)号：US20080125611A1

公开(公告)日：2008-05-29

申请号：US11667087

申请日：2005-11-11

Applicant: Stefano Carlino ,  Guido Di Napoli

Inventor： Stefano Carlino ,  Guido Di Napoli

IPC: C07C45/32

CPC classification number: C07C66/02

Abstract: A process for preparing aloe-emodin from aloin by oxidizing aloin by treatment with an oxygen-containing gas in the presence of an acid. The aloe-emodin may be used for the production of rhein and diacerein by oxidizing aloe-emodin by treatment with a chromium-free oxidizing medium to obtain rhein and purifying the rhein obtained. The rhein may be acetylated to obtain diacerein.

Abstract translation: 一种通过在酸存在下用含氧气体处理氧化芦荟来从芦荟中制备芦荟大黄素的方法。 芦荟大黄素可用于通过用无铬氧化介质处理氧化芦荟大黄素来生产大黄酸和双醋瑞因，以获得大黄酸并纯化获得的大黄酸。 可以将大黄酸乙酰化以获得双醋瑞因。

公开(公告)号：US06455578B1

公开(公告)日：2002-09-24

申请号：US09830800

申请日：2001-04-30

Applicant: Guido Di Napoli

Inventor： Guido Di Napoli

IPC: A01N4316

CPC classification number: C07D311/22 ,  C07C49/82

Abstract: The present invention is directed to aromatic derivatives of formula (I), wherein: R1 is (a), wherein R3 and R4 are selected from between H and OH, provided that R3 and R4 are not simultaneously H, and R2 is H; or R1 and R2 taken together, are (b), wherein R5 is selected from between CH3 and (CH2)5OH, to the iron complexes thereof, and to their use for the preparation of pharmaceutical compositions for the normalization of iron level.

Abstract translation: 本发明涉及式（I）的芳族衍生物，其中：R1是（a），其中R3和R4选自H和OH之间，条件是R3和R4不同时为H，R2为H; 或R 1和R 2一起是（b），其中R 5选自CH 3和（CH 2）5 OH，其铁络合物，以及它们在制备用于铁含量标准化的药物组合物中的用途。

公开(公告)号：US5864048A

公开(公告)日：1999-01-26

申请号：US903660

申请日：1997-07-31

Applicant: Guido Di Napoli

Inventor： Guido Di Napoli

IPC: A61K20060101 ,  A61K31/165 ,  A61K31/22 ,  A61K31/235 ,  C07C20060101 ,  C07C50/26 ,  C07C65/40 ,  C07C67/31 ,  C07C67/313 ,  C07C69/017 ,  C07C69/90 ,  C07C69/95 ,  C07C205/25 ,  C07C205/42 ,  C07C229/52 ,  C07C229/66 ,  C07C229/74 ,  C07C233/54 ,  C07C235/84 ,  C07C245/20

CPC classification number: C07C69/95 ,  A61K8/355 ,  A61Q19/00 ,  C07C229/66 ,  C07C229/74 ,  C07C233/33 ,  C07C235/84 ,  C07C69/18 ,  C07C2103/24

Abstract: The present description relates to new anthraquinone-derivatives endowed with inhibitory activity of the serine proteinase enzymes, useful for the treatment of rheumatoid arthritis, acute respiratory syndrome of adult, and pulmonary emphysema, and to new processes for the preparation of rhein derivatives.

Abstract translation: 本说明书涉及可用于治疗类风湿性关节炎，成人急性呼吸综合征和肺气肿的丝氨酸蛋白酶抑制活性的新型蒽醌衍生物以及制备大黄酸衍生物的新方法。

公开(公告)号：US06677304B2

公开(公告)日：2004-01-13

申请号：US09818213

申请日：2001-03-27

Applicant: Guido Di Napoli

Inventor： Guido Di Napoli

IPC: A61K3800

CPC classification number: A61K38/13 ,  A61K9/0048 ,  A61K47/26 ,  A61K47/36

Abstract: A topical ophthalmic formulation in the form of an aqueous solution comprising a cyclosporin, hyaluronic acid or one of its salts, and polysorbate 80 is described.