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1. 发明公开

EP4263504A1 MODIFIED INDOLE ALKALOIDS FOR THERAPEUTIC USES 审中-实审
公开(公告)号：EP4263504A1
公开(公告)日：2023-10-25
申请号：EP21907956.3
申请日：2021-12-17
申请人： COMPASS Pathfinder Limited
发明人： PROTZKO, Ryan
IPC分类号： C07D209/32 , C07D471/04 , C07D471/14 , C07D487/22 , C07H17/02 , C07H17/08 , C07B45/04 , C07B41/12 , C07B41/06 , A61P25/30 , A61P25/28 , A61P25/24 , A61P25/22 , A61P25/06

2. 发明授权

EP2170826B1 PRO-DRUGS OF NSAIAS WITH VERY HIGH SKIN AND MEMBRANES PENETRATION RATES AND THEIR NEW MEDICINAL USES 有权
公开(公告)号：EP2170826B1
公开(公告)日：2022-04-27
申请号：EP07825791.2
申请日：2007-06-04
发明人： YU, Chongxi , XU, Lina
IPC分类号： C07D209/32 , C07D231/12 , C07D471/08 , C07D487/08 , C07D213/74 , C07D215/10 , C07D217/12 , A61K31/44 , A61P29/00 , A61P3/00

3. 发明公开

EP2170826A4 PRO-DRUGS OF NSAIAS WITH VERY HIGH SKIN AND MEMBRANES PENETRATION RATES AND THEIR NEW MEDICINAL USES 有权
标题翻译： NSAIDs的前体药物具有很高的皮肤和膜的普及率及新医疗用途
公开(公告)号：EP2170826A4
公开(公告)日：2012-11-07
申请号：EP07825791
申请日：2007-06-04
申请人： TECHFIELDS INC , YU CHONGXI
发明人： YU CHONGXI , XU LINA
IPC分类号： C07D209/32 , A61K31/44 , A61P3/00 , A61P29/00 , C07D213/74 , C07D215/10 , C07D217/12 , C07D231/12 , C07D471/08 , C07D487/08
CPC分类号： C07D513/04 , C07D205/04 , C07D211/22 , C07D295/088 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07D491/052
摘要： The novel positively charged pro-drugs of NSAIAs in the general formulas (1, 2a, 2b, 2c, or 2d) “Structure 1, 2a, 2b, 2c, or 2d” were designed and synthesized. The compounds of the general formulas (1, 2a, 2b, 2c, or 2d) “Structure 1, 2a, 2b, 2c, or 2d” indicated above can be prepared from metal salts, organic base salts, or immobilized base salts of NSAIAs with suitable halide compounds. The positively charged amino groups in the pro-drugs in this invention largely increase the solubility of the drugs in water and will bond to the negative charge on the phosphate head group of membrane. Thus, the local concentration of the outside of the membrane or skin will be very high and will facilitate the passage of these pro-drugs from a region of high concentration to a region of low concentration. This bonding will disturb the membrane a little bit and may make some room for the lipophilic portion of the pro-drug. When the molecules of membrane move, the membrane may “crack” a little bit due to the bonding of the pro-drug. This will let the pro-drug insert into the membrane. At pH 7.4, only about 99% of the amino group is protonated. When the amino group is not protonated, the bonding between the amino group of the pro-drug and the phosphate head group of the membrane will disassociate, and the pro-drug will enter the membrane completely. When the amino group of the pro-drug flips to the other side of the membrane and thus becomes protonated, then the pro-drug is pulled into the cytosol, a semi-liquid concentrated aqueous solution or suspension. These pro-drugs can be used for treating and preventing diabetes (type I or/and type II), abnormal blood glucose and lipid levels, stroke, heart attack, and other heart and vascular diseases Alzheimer's diseases, Parkinson's diseases and other neurodegenerative diseases, psoriasis, discoid lupus erythematosus, systemic lupus erythematosus (SLE), autoimmune hepatitis, multiple sclerosis (MS), and other autoimmune diseases, amyotrophic lateral sclerosis (ALS), oculopharyngeal muscular dystrophy (OPMD), and other muscle disorders, inflamed hemorrhoids, cryptitis, other inflammatory conditions of the anorectum, and pruritus ani, prostatitis, prostatocystitis, varicose veins, autoimmune liver inflammation, autoimmune kidney inflammation, vein inflammation and other inflammations, skin cancers, breast cancer, colon-rectum cancer, oral cancer, and other cancers, scars, abnormal vascular skin lesions, birthmarks, moles (nevi), skin tags, aging spots (liver spots), and other skin disorders. These pro-drugs can be administered transdermally without the help of skin penetration enhancers.

4. 发明公开

EP1848704A4 NOVEL TUBULIN POLYMERISATION INHIBITORS 审中-公开
标题翻译：新的抑制剂微管蛋白聚合
公开(公告)号：EP1848704A4
公开(公告)日：2011-05-11
申请号：EP06704869
申请日：2006-02-14
申请人： BIONOMICS LTD
发明人： CHAPLIN JASON HUGH , GILL GURMIT SINGH , GROBELNY DAMIAN WOJCIECH , FLYNN BERNARD LUKE
IPC分类号： C07D307/83 , A61K31/04 , A61K31/33 , A61K31/343 , A61K31/381 , A61P29/00 , A61P35/00 , C07D209/32 , C07D333/64 , C07D345/00
CPC分类号： C07D403/04 , C07D307/80 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07F9/65517 , C07F9/65586

5. 发明公开

EP1948604A1 INDOLE COMPOUNDS HAVING C4-ACIDIC SUBSTITUENTS AND USE THEREOF AS PHOSPHOLIPASE-A2 INHIBITORS 审中-公开
标题翻译：具有酸性C4取代基和它们作为抑制剂的磷脂酶A2吲哚化合物
公开(公告)号：EP1948604A1
公开(公告)日：2008-07-30
申请号：EP06836969.3
申请日：2006-11-03
申请人： Ilypsa, Inc.
发明人： CHANG, Han-Ting , CHARMOT, Dominique , GLINKA, Tomasz , COPE, Michael, James , GOKA, Elizabeth , SHAO, Jun , CHEN, Shiah-yun , BUYSSE, Jerry, M.
IPC分类号： C07D209/32 , A61K31/405 , A61P3/04
CPC分类号： C07D209/32
摘要： Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject.

6. 发明公开

EP1793816A2 COMPOSITIONS FOR TREATING AMYLOID ASSOCIATED DISEASES 有权
标题翻译：组合物治疗淀粉样蛋白相关疾病
公开(公告)号：EP1793816A2
公开(公告)日：2007-06-13
申请号：EP05774727.1
申请日：2005-08-18
申请人： Tel Aviv University Future Technology Development L.P.
发明人： GAZIT, Ehud , COHEN, Tomer
IPC分类号： A61K31/403 , A61K31/415 , A61K31/4164 , A61K31/404 , A61P25/28 , A61P5/50 , C07D209/32 , C07D209/12
CPC分类号： C07D209/12 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4164 , C07D209/32
摘要： Indole derivatives, compositions including same, and methods utilizing same for the treatment of amyloid associated diseases, such as type II diabetes mellitus, Alzheimer's dementia or diseases, systemic and localized amyloidosis, and prion-related encephalopathies are provided.

7. 发明公开

EP1447400A4 BICYCLIC COMPOUND 有权
标题翻译： BICYCLISCHE VERBINDUNG
公开(公告)号：EP1447400A4
公开(公告)日：2005-11-09
申请号：EP02770271
申请日：2002-10-25
申请人： ASAHI KASEI PHARMA CORP
发明人： MIYOSHI SHIRO , OGAWA KOHEI
IPC分类号： A61K31/343 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/422 , A61K31/4439 , A61K31/454 , A61P1/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P13/02 , A61P25/24 , A61P43/00 , C07D209/04 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/32 , C07D209/42 , C07D231/56 , C07D307/79 , C07D307/83 , C07D307/84 , C07D307/85 , C07D333/64 , C07D401/04 , C07D405/06 , C07D413/04 , C07D413/06
CPC分类号： C07D413/06 , A61K31/343 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/422 , A61K31/4439 , A61K31/454 , C07D209/04 , C07D209/12 , C07D209/14 , C07D209/16 , C07D209/18 , C07D209/22 , C07D209/32 , C07D209/42 , C07D231/56 , C07D307/79 , C07D307/83 , C07D307/84 , C07D307/85 , C07D333/64 , C07D401/04 , C07D405/06
摘要： A compound represented by the general formula (I): (I) (wherein R1 represents hydrogen, etc.; R2 represents NHSO2R3, etc., provided that R3 represents C1-6 alkyl, etc.; R5 represents hydrogen, etc.; R6 and R7 may be the same or different and each independently represents hydrogen, etc.; X represents oxygen, etc.; Y represents oxygen, etc.; Z1 to Z6 each represents carbon, etc.; n is an integer of 0 to 6; and *1 indicates that the carbon atom is asymmetric, and *2, in the case where R5 is not hydrogen, indicates that the carbon atom is asymmetric) or a salt of the compound.
摘要翻译：通式（I）表示的化合物：（I）（式中，R1表示氢等; R2表示NHSO2R3等，条件是R3表示C1-6烷基等; R5表示氢等; R6 R 7可以相同或不同，各自独立地表示氢等; X表示氧等; Y表示氧等; Z 1至Z 6各自表示碳等; n是0至6的整数; 和1表示碳原子是不对称的，并且2在R5不是氢的情况下表示碳原子是不对称的）或该化合物的盐。

8. 发明授权

EP0959881B1 SYNTHETIC METHODS FOR THE PREPARATION OF INDOLYLQUINONES AND MONO- AND BIS-INDOLYLQUINONES PREPARED THEREFROM 失效
标题翻译： SYSNTHESEVERFAHREN准备和INDOLYLQUINONEN单和双INDOLYLQUINONE BY THE程序制备。
公开(公告)号：EP0959881B1
公开(公告)日：2005-09-21
申请号：EP97946641.4
申请日：1997-11-12
申请人： Sugen, Inc.
发明人： TANG, Peng, C. , HARRIS, G., David
IPC分类号： C07D209/12 , A61K31/40 , C07D209/42 , C07D209/40 , C07D209/32 , C07D209/30
CPC分类号： A61K31/4045 , A61K31/404 , C07D209/12 , C07D209/42
摘要： The present invention relates to novel synthetic methods for the preparation of indolylquinones. The methods of the present invention are directed to synthetic reactions involving indoles and halo-quinones in solvent and in the presence of a metal carbonate. The invention also relates to bis- and mono- indolylquinones of high purity and pharmaceutical compositions containing the same.

9. 发明公开

EP1554243A1 BICYCLIC BENZAMIDE COMPOUNDS AS HISTAMINE H3 RECEPTOR LIGAND USEFUL IN THE TREATMENT OF NEUROLOGICAL DISEASES 有权
标题翻译：双环苯甲酰胺用于治疗神经系统疾病SUITABLE组胺H3受体配体
公开(公告)号：EP1554243A1
公开(公告)日：2005-07-20
申请号：EP03769430.4
申请日：2003-10-20
申请人： GLAXO GROUP LIMITED
发明人： BEST, Desmond, JohnGlaxoSmithKline , ORLEK, Barry, SidneyGlaxoSmithKline
IPC分类号： C07D209/26 , C07D217/06 , C07D209/44 , C07D209/32 , C07D215/08 , C07D403/04 , C07D223/16 , C07D409/04 , C07D491/04 , C07D403/12 , A61K31/4035 , A61K31/404 , A61K31/47 , A61K31/55 , A61P25/00
CPC分类号： C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D491/04
摘要： The present invention relates to novel bicyclic benzamide derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.

10. 发明授权

EP1315739B1 PROCEDE DE COUPLAGE, EN SOLUTION, ENTRE UN PEPTIDE ET UN VECTEUR LIPOPHILE ET SES APPLICATIONS 有权
标题翻译： PROCESS FOR IN之间的肽和亲脂性化合物溶液的离合器，及其用途
公开(公告)号：EP1315739B1
公开(公告)日：2004-08-18
申请号：EP01967454.8
申请日：2001-09-07
申请人： INSTITUT PASTEUR DE LILLE Etablissement Public , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
发明人： BONNET, Dominique , BOUREL, Line , MELNYK, Oleg , GRAS-MASSE, Hélène
IPC分类号： C07K1/107 , A61K47/48 , C07C233/03 , C07D209/32 , A61K39/395
CPC分类号： C07D263/04 , A61K38/00 , A61K47/54 , C07C235/74 , C07K1/1077

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