公开(公告)号：US20050171091A1

公开(公告)日：2005-08-04

申请号：US11090743

申请日：2005-03-25

申请人： Mladen Mercep ,  Milan Mesic ,  Dijana Pesic ,  Zeljko Zupanovic ,  Boska Hrvacic

发明人： Mladen Mercep ,  Milan Mesic ,  Dijana Pesic ,  Zeljko Zupanovic ,  Boska Hrvacic

IPC分类号： A61K31/381 ,  A61K31/55 ,  A61P1/04 ,  A61P11/06 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07B61/00 ,  C07D495/04 ,  C07D495/02 ,  C07D498/02

CPC分类号： C07D495/04

摘要： The present invention relates to the dibenzoazulene compounds represented by formula I as well as to their pharmaceutical preparations for the inhibition of tumor necrosis factor alpha (TNF-α) and interleukine 1 (IL-1) in mammals at all diseases and conditions where these mediators are excessively secreted. The compounds of the present invention also demonstrate an analgetic action and can be used to relieve pain.

摘要翻译： 本发明涉及由式I表示的二苯并薁化合物及其在所有疾病和病症中抑制哺乳动物的肿瘤坏死因子α（TNF-α）和白细胞介素1（IL-1）的药物制剂，其中这些介质 过度分泌。 本发明的化合物还表现出止痛作用，可用于缓解疼痛。

公开(公告)号：US06897211B2

公开(公告)日：2005-05-24

申请号：US10298217

申请日：2002-11-18

申请人： Mladen Mercep ,  Milan Mesic ,  Dijana Pesic ,  Zeljko Zupanovic ,  Boska Hrvacic

发明人： Mladen Mercep ,  Milan Mesic ,  Dijana Pesic ,  Zeljko Zupanovic ,  Boska Hrvacic

IPC分类号： A61K31/381 ,  A61K31/55 ,  A61P1/04 ,  A61P11/06 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07B61/00 ,  C07D495/04

CPC分类号： C07D495/04

摘要： The present invention relates to the dibenzoazulene compounds represented by formula I as well as to their pharmaceutical preparations for the inhibition of tumor necrosis factor alpha (TNF-α) and interleukine 1 (IL-1) in mammals at all diseases and conditions where these mediators are excessively secreted. The compounds of the present invention also demonstrate an analgetic action and can be used to relieve pain.

公开(公告)号：US20060241099A1

公开(公告)日：2006-10-26

申请号：US11381163

申请日：2006-05-02

申请人： Mladen Mercep ,  Milan Mesic ,  Dijana Pesic ,  Ivana Ozimec Landak ,  Boska Hrvacic ,  Barbara Stanic

发明人： Mladen Mercep ,  Milan Mesic ,  Dijana Pesic ,  Ivana Ozimec Landak ,  Boska Hrvacic ,  Barbara Stanic

IPC分类号： A61K31/55 ,  A61K31/381 ,  C07D498/02 ,  C07D495/02

CPC分类号： A61K31/00 ,  A61K31/381 ,  A61K31/55

摘要： The present invention relates to the use of compounds from the group of 2-thia-dibenzo[e,h]azulenes and of their pharmacologically acceptable salts and solvates for the manufacture of a pharmaceutical formulation for the treatment and prevention of diseases, damages and disorders of the central nervous system (CNS) caused by disorders of the neurochemical equilibrium of biogenic amines or other neurotransmitters.

摘要翻译： 本发明涉及2-硫杂 - 二苯并[e，h]薁类化合物及其药理学上可接受的盐和溶剂化物在制备用于治疗和预防疾病，损伤和障碍的药物制剂中的用途 的中枢神经系统（CNS），由生物胺或其他神经递质的神经化学平衡紊乱引起。

公开(公告)号：US20080153872A1

公开(公告)日：2008-06-26

申请号：US11813885

申请日：2006-01-13

申请人： Mladen Mercep ,  Ivica Malnar ,  Boska Hrvacic ,  Stribor Markovic ,  Anita Filipovic Sucic ,  Berislav Bosnjak ,  Andreja Cempuh Klonkay ,  Renata Rupcic ,  Antun Hutinec ,  Ivaylo Jivkov Elenkov ,  Milan Mesic

发明人： Mladen Mercep ,  Ivica Malnar ,  Boska Hrvacic ,  Stribor Markovic ,  Anita Filipovic Sucic ,  Berislav Bosnjak ,  Andreja Cempuh Klonkay ,  Renata Rupcic ,  Antun Hutinec ,  Ivaylo Jivkov Elenkov ,  Milan Mesic

IPC分类号： A61K31/4709 ,  C07D407/06 ,  A61K31/353 ,  A61K31/357 ,  C07D409/14 ,  A61K31/4406 ,  C07D493/14 ,  A61P37/00 ,  A61P29/00 ,  C07D493/04 ,  A61K31/352 ,  C07D401/14 ,  A61K31/381 ,  C07D405/14 ,  A61K31/4155

CPC分类号： C07D413/12 ,  A61K47/545 ,  C07D311/56 ,  C07D407/06 ,  C07D407/14 ,  C07D413/14 ,  C07H17/00 ,  C07H17/08

摘要： Certain bis-(coumarin) compounds as well as the products of their intramolecular cyclization including pharmaceutically acceptable salts, hydrates, solvates, clathrates, prodrugs, tautomers and stereoisomers thereof are disclosed. Certain processes and intermediates for the preparation of certain bis-(coumarin) compounds, as well as for the use of these compounds as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diseases and conditions in mammals, especially humans are also disclosed.

摘要翻译： 公开了某些双 - （香豆素）化合物及其分子内环化的产物，包括其药学上可接受的盐，水合物，溶剂化物，包合物，前药，互变异构体和立体异构体。 还公开了某些制备某些二 - （香豆素）化合物的方法和中间体，以及将这些化合物用作治疗活性剂用于预防和治疗哺乳动物，特别是人类的哮喘和其它炎性疾病和病症 。

公开(公告)号：US20060148889A1

公开(公告)日：2006-07-06

申请号：US11337274

申请日：2006-01-20

申请人： Mladen Mercep ,  Milan Mesic ,  Boska Hrvacic ,  Ivaylo Jivkov Elenkov ,  Ivica Malnar ,  Stribor Markovic ,  Lidija Simicic ,  Andreja Cempuh Klonkay ,  Anita Filipovic

发明人： Mladen Mercep ,  Milan Mesic ,  Boska Hrvacic ,  Ivaylo Jivkov Elenkov ,  Ivica Malnar ,  Stribor Markovic ,  Lidija Simicic ,  Andreja Cempuh Klonkay ,  Anita Filipovic

IPC分类号： A61K31/366 ,  C07D493/02

CPC分类号： C07D493/04

摘要： The invention relates to novel compounds of the formula (I) including all their tautomers, to pharmaceutically acceptable salts and solvates thereof, to processes and reactive intermediates for the preparation thereof, and to processes and reactive intermediates for the preparation of the compounds of the formula (II) including all their stereoisomers and tautomers to the use of the compounds of the formula (II) as suitable precursors for the preparation of the compounds of the formula (I) as well as to use of the compounds of the formula (I) and of the compounds of the formula (II) as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diesases and conditions in humans.

摘要翻译： 本发明涉及包含其所有互变异构体，其药学上可接受的盐和溶剂合物的式（I）化合物，其制备方法和反应中间体，以及制备式I化合物的方法和反应中间体 （II）包括其所有立体异构体和互变异构体以使用式（II）化合物作为制备式（I）化合物的合适前体，以及使用式（I）化合物， 和式（II）的化合物作为预防和治疗哮喘和其它炎性糖尿病和人类病症的治疗活性剂。

公开(公告)号：US07262302B2

公开(公告)日：2007-08-28

申请号：US10515700

申请日：2003-05-20

申请人： Mladen Mercep ,  Milan Mesic ,  Marina Modric ,  Dijana Pesic ,  Davor Kidemet

发明人： Mladen Mercep ,  Milan Mesic ,  Marina Modric ,  Dijana Pesic ,  Davor Kidemet

IPC分类号： C07D277/60 ,  C07D513/02 ,  C07D487/02

CPC分类号： C07D513/04

摘要： The present invention relates to derivatives of 1-thia-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-α (TNF-α) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

摘要翻译： 本发明涉及1-硫杂-3-氮杂 - 二苯并薁类衍生物，其药理学上可接受的盐和溶剂合物，其制备方法和中间体以及它们的抗炎作用，特别是抑制肿瘤坏死因子 α（TNF-α）产生和白细胞介素-1（IL-1）产生的抑制以及其镇痛作用。

公开(公告)号：US20050148576A1

公开(公告)日：2005-07-07

申请号：US10510620

申请日：2003-04-09

申请人： Mladen Mercep ,  Milan Mesic ,  Dijana Pesic ,  Iva Benko

发明人： Mladen Mercep ,  Milan Mesic ,  Dijana Pesic ,  Iva Benko

IPC分类号： C07D498/04 ,  A61K31/42 ,  A61K31/424 ,  A61P1/04 ,  A61P11/06 ,  A61P17/04 ,  A61P17/06 ,  A61P17/16 ,  A61P19/02 ,  A61P19/08 ,  A61P27/02 ,  A61P29/00 ,  A61P43/00 ,  C07D263/52 ,  A61K31/55 ,  C07D491/02

CPC分类号： C07D263/52 ,  Y02P20/55

摘要： The present invention relates to derivatives of 1-oxa-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory actions, especially to the inhibition of tumour necrosis factor-α (TNF-α) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

摘要翻译： 本发明涉及1-氧杂-3-氮杂 - 二苯并薁类衍生物，其药理学上可接受的盐和溶剂合物，其制备方法和中间体以及它们的抗炎作用，特别是抑制肿瘤坏死因子 α（TNF-α）产生和白细胞介素-1（IL-1）产生的抑制以及其镇痛作用。

公开(公告)号：US07208518B2

公开(公告)日：2007-04-24

申请号：US11338871

申请日：2006-01-23

申请人： Mladen Mercep ,  Milan Mesic ,  Boska Hrvacic ,  Ivaylo Jivkov Elenkov ,  Ivica Malnar ,  Stribor Markovic ,  Lidija Simicic ,  Andreja Cempuh Klonkay ,  Anita Filipovic

发明人： Mladen Mercep ,  Milan Mesic ,  Boska Hrvacic ,  Ivaylo Jivkov Elenkov ,  Ivica Malnar ,  Stribor Markovic ,  Lidija Simicic ,  Andreja Cempuh Klonkay ,  Anita Filipovic

IPC分类号： C07D495/14 ,  C07D495/04 ,  A61K31/352

CPC分类号： C07D493/04

摘要： The present invention relates to novel compounds of the formula (I) including all stereoisomers and tautomers thereof, to the pharmaceutically acceptable salts and solvates thereof, to the processes and reactive intermediates for their preparation and to their use in the prophylaxis and treatment of asthma and other inflammatory diseases and/or conditions in humans.

摘要翻译： 本发明涉及式（I）的新化合物，其包括其所有立体异构体和互变异构体，其药学上可接受的盐和溶剂化物，其制备方法和反应中间体及其在预防和治疗哮喘中的用途和 人类的其他炎性疾病和/或病症。

公开(公告)号：US20050080003A1

公开(公告)日：2005-04-14

申请号：US10830858

申请日：2004-04-22

申请人： Mladen Mercep ,  Milan Mesic ,  Linda Tomaskovic ,  Stribor Markovic ,  Boska Hrvacic ,  Oresta Makaruha ,  Visnja Poljak

发明人： Mladen Mercep ,  Milan Mesic ,  Linda Tomaskovic ,  Stribor Markovic ,  Boska Hrvacic ,  Oresta Makaruha ,  Visnja Poljak

IPC分类号： C07D273/00 ,  C07D413/12 ,  C07D473/04 ,  C07H17/08 ,  C07J1/00 ,  A61K38/16 ,  C07K9/00

CPC分类号： C07D273/00 ,  C07D413/12 ,  C07D473/04 ,  C07H17/08 ,  C07J1/00

摘要： The present invention relates to new compounds represented by Formula I: wherein M represents a macrolide subunit of the substructure II: L represents the chain of the substructure III: —X1—(CH2)m-Q-(CH2)n—X2—  III D represents the steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity; The present invention relates also to pharmaceutically acceptable salts and solvates of such prepared compounds, to processe and intermediates for their preparation, as well as to the improved therapeutic action and the use in the treatment of inflammatory diseases and conditions in humans and animals.

摘要翻译： 本发明涉及由式I表示的新化合物：其中M表示亚结构II的大环内酯亚单位：L表示下结构III的链：-X 1 - （CH 2）mQ-（CH 2）n X 2 - III D代表衍生自具有抗炎活性的类固醇或非甾体（NSAID）药物的类固醇或非甾体亚基; 本发明还涉及这种制备的化合物的药学上可接受的盐和溶剂化物，其制备方法和中间体，以及改进的治疗作用以及用于治疗人和动物的炎性疾病和病症的用途。

公开(公告)号：US20090221687A1

公开(公告)日：2009-09-03

申请号：US11815317

申请日：2006-02-01

申请人： Milan Mesic ,  Mladen Mercep ,  Dijana Pesic ,  Renata Rupcic ,  Barbara Stanic

发明人： Milan Mesic ,  Mladen Mercep ,  Dijana Pesic ,  Renata Rupcic ,  Barbara Stanic

IPC分类号： A61K31/381 ,  C07D495/04 ,  A61P25/00

CPC分类号： C07D495/04

摘要： Novel tetracyclic dibenzo(e,h)azulene compounds of formula I; their pharmacologically acceptable derivatives; process and intermediates for their preparation; pharmaceutical compositions containing them and their activity and use in the treatment of central nervous system (CNS) diseases and conditions in humans and animals.

摘要翻译： 式I的新型四环二苯并（e，h）薁化合物; 其药理学上可接受的衍生物; 工艺和中间体的制备; 含有它们的药物组合物及其活性和用于治疗人和动物中的中枢神经系统（CNS）疾病和病症。