公开(公告)号：WO2005028425A3

公开(公告)日：2005-06-09

申请号：PCT/EP2004052201

申请日：2004-09-16

Applicant: DOMPE SPA ,  ALLEGRETTI MARCELLO ,  CESTA MARIA CANDIDA ,  NANO GIUSEPPE ,  BERTINI RICCARDO ,  BIZZARRI CINZIA ,  COLOTTA FRANCESCO

Inventor： ALLEGRETTI MARCELLO ,  CESTA MARIA CANDIDA ,  NANO GIUSEPPE ,  BERTINI RICCARDO ,  BIZZARRI CINZIA ,  COLOTTA FRANCESCO

IPC: C07C257/14 ,  C07C309/65 ,  C07C309/66 ,  C07D211/26 ,  C07D233/10 ,  C07D273/04 ,  C07D333/24 ,  A61K31/155 ,  A61K31/255 ,  A61K31/381 ,  A61K31/4164 ,  A61K31/4453 ,  A61K31/5395 ,  A61P17/06

CPC classification number: C07C309/65 ,  C07C257/14 ,  C07D211/26 ,  C07D233/10 ,  C07D273/04 ,  C07D333/24

Abstract: Amidines and derivatives thereof of formula (I) are described. The process for their preparation and pharmaceutical compositions thereof are also described. The amidines of the invention are useful in the inhibition of chemotaxis of neutrophils induced by IL- 8. The compounds of the invention are used in the treatement of psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.

Abstract translation: 描述了式（I）的脒及其衍生物。 还描述了它们的制备方法及其药物组合物。 本发明的脒类可用于抑制由IL-8诱导的嗜中性粒细胞的趋化性。本发明的化合物用于治疗银屑病，溃疡性结肠炎，黑素瘤，慢性阻塞性肺病（COPD），大疱性白斑，类风湿 关节炎，特发性纤维化，肾小球肾炎以及预防和治疗由缺血和再灌注引起的损伤。

公开(公告)号：WO2004080951A2

公开(公告)日：2004-09-23

申请号：PCT/EP2004050293

申请日：2004-03-11

Applicant: DOMPE SPA ,  ALLEGRETTI MARCELLO ,  ARAMINI ANDREA ,  CESTA MARIA CANDIDA ,  BERTINI RICCARDO ,  BIZZARRI CINZIA ,  COLOTTA FRANCESCO

Inventor： ALLEGRETTI MARCELLO ,  ARAMINI ANDREA ,  CESTA MARIA CANDIDA ,  BERTINI RICCARDO ,  BIZZARRI CINZIA ,  COLOTTA FRANCESCO

IPC: A61K31/10 ,  A61K31/18 ,  A61P29/00 ,  C07C309/24 ,  C07C309/29 ,  C07C309/65 ,  C07C309/73 ,  C07C311/08 ,  C07C311/13 ,  C07C311/16 ,  C07C311/21 ,  C07C311/27 ,  C07C311/35 ,  C07C311/51 ,  C07D207/26 ,  C07D207/263 ,  C07D207/27 ,  C07D207/32 ,  C07D207/333

CPC classification number: C07D207/333 ,  C07C309/24 ,  C07C309/65 ,  C07C309/73 ,  C07C311/08 ,  C07C311/13 ,  C07C311/27 ,  C07C311/35 ,  C07C311/51 ,  C07D207/27

Abstract: Selected sulfonic acids, their derivatives and pharmaceutical compositions containing such compounds are useful in inhibiting the chernotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCRI and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, the selected sulfonic acids and their derivativas are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrofil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.

Abstract translation: 选择的磺酸，其衍生物和含有这些化合物的药物组合物可用于抑制由白细胞介素-8（IL-8）与CXCR1和CXCR2膜受体相互作用诱导的嗜中性粒细胞（PMN白细胞）的切割型活化。 所述化合物用于预防和治疗由所述活化引起的病理学。 值得注意的是，选择的磺酸及其衍生物没有环加氧酶抑制活性，并且特别可用于治疗中性粒细胞依赖性病理如牛皮癣，溃疡性结肠炎，黑素瘤，慢性阻塞性肺病（COPD），大疱性类天疱疮，类风湿 关节炎，特发性纤维化，肾小球性肾炎，以及预防和治疗由缺血和再灌注引起的损伤。

公开(公告)号：WO02062330A3

公开(公告)日：2003-04-03

申请号：PCT/EP0200946

申请日：2002-01-30

Applicant: DOMPE SPA ,  BERTINI RICCARDO ,  COLOTTA FRANCESCO ,  NOVELLINI ROBERTO

Inventor： BERTINI RICCARDO ,  COLOTTA FRANCESCO ,  NOVELLINI ROBERTO

IPC: A61K47/18 ,  A61K31/18 ,  A61K31/216 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P37/06

CPC classification number: A61K31/216

Abstract: The use of (R).-ibuprofen methanesulfonamide is described for the preparation of medicaments for the treatment and prevention of functional injury resulting from rejection reactions of transplanted organs. In particular, the use of non-toxic salts of (R)-ibuprofen methanesulfonamide, such as the (L)-lysine salt, is described for the prevention and the treatment of rejection reactions of transplanted kidneys.

Abstract translation: 描述了（R） - 布洛芬甲磺酰胺的用途，用于制备用于治疗和预防由移植器官的排斥反应引起的功能性损伤的药物。 特别地，描述了（R） - 布洛芬甲磺酰胺的无毒盐（例如（L） - 赖氨酸盐）的用途，用于预防和治疗移植肾的排斥反应。

公开(公告)号：WO2010031835A3

公开(公告)日：2010-06-24

申请号：PCT/EP2009062109

申请日：2009-09-18

Applicant: DOMPE SPA ,  ALLEGRETTI MARCELLO ,  ARAMINI ANDREA ,  BIANCHINI GIANLUCA ,  CESTA MARIA CANDIDA

Inventor： ALLEGRETTI MARCELLO ,  ARAMINI ANDREA ,  BIANCHINI GIANLUCA ,  CESTA MARIA CANDIDA

IPC: C07D263/48 ,  A61K31/421 ,  A61K31/427 ,  A61P29/00 ,  C07D277/42

CPC classification number: C07D263/48 ,  C07D277/42

Abstract: The present invention relates to (R,S) 2-aryl-propionic acids and derivatives, their single cnantiomcr (S) and to pharmaceutical compositions containing them, which arc used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonuclcated neutrophils (PIvTN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of transient cerebral ischemia, bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and damages caused by ischemia and reperfusion. (Formula (I)

Abstract translation: 本发明涉及（R，S）2-芳基 - 丙酸及其衍生物，它们的单一抗坏血酸（S）和含有它们的药物组合物，其用于预防和治疗组织损伤，这是由于多形核酸 中性粒细胞（PIvTN白细胞）在炎症部位。 本发明提供了用于治疗短暂性脑缺血，大疱性肺炎，类风湿性关节炎，特发性纤维化，肾小球肾炎和由缺血和再灌注引起的损伤的化合物。 （式（I）

公开(公告)号：WO2004069782A3

公开(公告)日：2004-09-16

申请号：PCT/EP2004001021

申请日：2004-02-04

Applicant: DOMPE SPA ,  MORICONI ALESSIO ,  ALLEGRETTI MARCELLO ,  BERTINI RICCARDO ,  CESTA MARIA CANDIDA ,  BIZZARRI CINZIA ,  COLOTTA FRANCESCO

Inventor： MORICONI ALESSIO ,  ALLEGRETTI MARCELLO ,  BERTINI RICCARDO ,  CESTA MARIA CANDIDA ,  BIZZARRI CINZIA ,  COLOTTA FRANCESCO

IPC: C07C59/205 ,  C07C63/04 ,  C07C65/32 ,  C07C311/02 ,  C07C311/09 ,  C07C311/21 ,  C07C311/29 ,  C07C311/51 ,  C07D207/32 ,  C07D207/337 ,  C07D209/26 ,  C07D209/42 ,  C07D295/12 ,  C07D295/13 ,  C07D471/04

CPC classification number: C07D207/337 ,  C07C57/30 ,  C07C57/58 ,  C07C311/09 ,  C07C311/21 ,  C07C311/51 ,  C07D209/26 ,  C07D209/42 ,  C07D295/13 ,  C07D471/04

Abstract: Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.

Abstract translation: 所选的2-芳基乙酸，其衍生物和含有这些化合物的药物组合物可用于抑制由白细胞介素-8（IL-8）与CXCR1和CXCR2膜受体相互作用诱导的嗜中性粒细胞（PMN白细胞）的趋化性活化。 这些化合物用于预防和治疗源自所述活化的病变。 具体而言，2（邻位） - 取代的芳基乙酸或其衍生物，例如酰胺和磺酰胺，缺乏环加氧酶抑制活性，并且特别可用于治疗嗜中性粒细胞依赖性病变，例如牛皮癣，溃疡性结肠炎，黑素瘤，慢性阻塞 肺部疾病（COPD），大疱性类天疱疮，类风湿性关节炎，特发性纤维化，肾小球肾炎以及预防和治疗由缺血和再灌注引起的损伤。

公开(公告)号：WO0179189A3

公开(公告)日：2003-10-09

申请号：PCT/EP0104137

申请日：2001-04-11

Applicant: DOMPE SPA ,  ALLEGRETTI MARCELLO ,  BERTINI RICCARDO ,  BIZZARRI CINZIA ,  SABBATINI VILMA ,  CASELLI GIANFRANCO ,  CESTA MARIA CANDIDA ,  GANDOLFI CARMELO ,  COLOTTA FRANCESCO

Inventor： ALLEGRETTI MARCELLO ,  BERTINI RICCARDO ,  BIZZARRI CINZIA ,  SABBATINI VILMA ,  CASELLI GIANFRANCO ,  CESTA MARIA CANDIDA ,  GANDOLFI CARMELO ,  COLOTTA FRANCESCO

IPC: A61P17/06 ,  C07D207/20 ,  C07D209/18 ,  C07D213/75 ,  C07D215/12 ,  C07D239/42 ,  C07D241/20 ,  C07D277/46 ,  C07D295/155 ,  C07D401/12 ,  C07D403/12 ,  C07D521/00 ,  A61K31/47 ,  C07D215/38

CPC classification number: C07D213/75 ,  C07D207/20 ,  C07D209/18 ,  C07D215/12 ,  C07D231/12 ,  C07D233/56 ,  C07D239/42 ,  C07D241/20 ,  C07D249/08 ,  C07D277/46 ,  C07D295/155 ,  C07D401/12 ,  C07D403/12

Abstract: N-(2-aminoaryl-propionyl)-amides of formula (1) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The amides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear neutrophils (leukocytes PMN) at the inflammatory sites. In particular, the invention relates to the R enantiomers of 2-(aminoaryl)-propionyl amides of formula (1) for use in the inhibition of the chemotaxis of neutrophils induced by IL-8. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, and rheumatoid arthritis.

Abstract translation: 描述了式（1）的N-（2-氨基芳基 - 丙酰基） - 酰胺。 还描述了其制备方法及其制备药物。 本发明的酰胺可用于预防和治疗由于炎性部位多形核嗜中性粒细胞（白细胞PMN）的加剧引起的组织损伤。 特别地，本发明涉及用于抑制IL-8诱导的嗜中性粒细胞趋化性的式（1）的2-（氨基芳基） - 丙酰基酰胺的R对映异构体。 本发明的化合物用于治疗牛皮癣，溃疡性胆管炎，肾小球性肾炎，急性呼吸功能不全，特发性纤维化和类风湿性关节炎。

公开(公告)号：WO0158852A3

公开(公告)日：2002-03-14

申请号：PCT/EP0101285

申请日：2001-02-06

Applicant: DOMPE SPA ,  ALLEGRETTI MARCELLO ,  BERTINI RICCARDO ,  CINZIA BIZZARRI ,  SABBATINI VILMA ,  CASELLI GIANFRANCO ,  CESTA MARIA CANDIDA ,  GANDOLFI CARMELO ,  COLOTTA FRANCESCO

Inventor： ALLEGRETTI MARCELLO ,  BERTINI RICCARDO ,  CINZIA BIZZARRI ,  SABBATINI VILMA ,  CASELLI GIANFRANCO ,  CESTA MARIA CANDIDA ,  GANDOLFI CARMELO ,  COLOTTA FRANCESCO

IPC: A61K31/12 ,  A61K31/16 ,  A61K31/165 ,  A61K31/197 ,  A61K31/221 ,  A61K31/223 ,  A61K31/4035 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/495 ,  A61K31/4965 ,  A61K31/505 ,  A61K38/00 ,  A61P1/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P17/06 ,  A61P19/02 ,  A61P21/02 ,  A61P29/00 ,  C07C51/353 ,  C07C57/42 ,  C07C59/52 ,  C07C69/157 ,  C07C233/11 ,  C07C233/22 ,  C07C233/51 ,  C07C233/52 ,  C07C235/34 ,  C07C235/78 ,  C07C237/20 ,  C07C259/06 ,  C07C271/64 ,  C07D209/46 ,  C07D213/75 ,  C07D233/61 ,  C07D239/42 ,  C07D241/28 ,  C07D409/12 ,  C07K5/06 ,  A61K31/395 ,  C07D241/20 ,  C07K5/062

CPC classification number: C07D213/75 ,  A61K38/00 ,  C07B2200/07 ,  C07C233/11 ,  C07C233/22 ,  C07C233/51 ,  C07C233/52 ,  C07C235/34 ,  C07C235/78 ,  C07C237/20 ,  C07C271/64 ,  C07C2601/14 ,  C07D239/42 ,  C07K5/06026

Abstract: N-(2-aryl-propionyl)-amides of formula (I) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The amides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear neutrophils (leukocytes PMN) at the inflammatory sites. In particular, the invention relates to the R enantiomers of N-(2-aryl-propionyl)amides of formula (I) for use in the inhibition of the chemotaxis of neutrophils induced by IL-8. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, and rheumatoid arthritis.

Abstract translation: 描述了式（I）的N-（2-芳基 - 丙酰基） - 酰胺。 还描述了其制备方法及其制备药物。 本发明的酰胺可用于预防和治疗由于炎性部位多形核嗜中性粒细胞（白细胞PMN）的加剧引起的组织损伤。 特别地，本发明涉及用于抑制IL-8诱导的嗜中性粒细胞趋化性的式（I）的N-（2-芳基 - 丙酰基）酰胺的R对映异构体。 本发明的化合物用于治疗牛皮癣，溃疡性胆管炎，肾小球性肾炎，急性呼吸功能不全，特发性纤维化和类风湿性关节炎。

公开(公告)号：WO1994020449A1

公开(公告)日：1994-09-15

申请号：PCT/IT1994000020

申请日：1994-03-07

Applicant: DOMPE'FARMACEUTICI SPA ,  DOMPE' SPA ,  BOSONE, Enrico ,  CLAVENNA, Gaetano ,  GANDOLFI, Carmelo ,  MANTOVANINI, Marco ,  CURTI, Roberto

Inventor： DOMPE'FARMACEUTICI SPA ,  DOMPE' SPA

IPC: C07C59/84

CPC classification number: C07D295/088 ,  A61K31/19 ,  C07C59/84 ,  C07C229/26 ,  C07C279/14

Abstract: The salts of S(+) 2-(3-benzoylphenyl)propionic acid and of R(-) 2-(3-benzoylphenyl)propionic acid with an achiral, organic base such as tris-(hydroxymethyl)aminomethane or a chiral organic base such as D-lysine, L-lysine, L-arginine, (R) 3-(4-phenylpiperazin-1-yl)propane-1,2-diol and (S) 3-(4-phenylpiperazin-1-yl)propane-1,2-diol, the process for their preparation and the corresponding pharmaceutical compositions containing said salts are described.

Abstract translation: S（+）2-（3-苯甲酰基苯基）丙酸和R（ - ）2-（3-苯甲酰基苯基）丙酸与非手性有机碱如三 - （羟甲基）氨基甲烷或手性有机碱 例如D-赖氨酸，L-赖氨酸，L-精氨酸，（R）3-（4-苯基哌嗪-1-基）丙烷-1,2-二醇和（S）3-（4-苯基哌嗪-1-基） 丙烷-1,2-二醇，其制备方法和含有所述盐的相应药物组合物。