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1. 发明申请

WO2022199815A1 8-CYCLO-SUBSTITUTED QUINAZOLINE DERIVATIVES AS LPA RECEPTOR 2 INHIBITORS 审中-公开
公开(公告)号：WO2022199815A1
公开(公告)日：2022-09-29
申请号：PCT/EP2021/057609
申请日：2021-03-24
申请人： CHIESI FARMACEUTICI S.P.A.
发明人： AMARI, Gabriele , ARMANI, Elisabetta , PAGANO, Mafalda , GIULIANI, Marta , RAVEGLIA, Luca , BEATO, Claudia
IPC分类号： C07D239/94 , C07D403/12 , C07D413/14 , C07D417/12 , C07D417/14 , A61K31/517 , A61P37/00
摘要： The present invention relates to compounds of general formula (I) inhibiting lysophosphatidic acid receptor 2 (LPA2), particularly the invention relates to compounds that are 8-cyclo-substituted quinazoline derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. The compounds of the invention may be useful in the treatment of diseases or conditions associated with a dysregulation of LPA receptors, in particular fibrosis.

2. 发明申请

WO2022174883A1 5-MEMBERED HETEROCYCLYL DERIVATIVES AS DUAL LPA RECEPTOR 1 AND LPA RECEPTOR 2 INHIBITORS 审中-公开
公开(公告)号：WO2022174883A1
公开(公告)日：2022-08-25
申请号：PCT/EP2021/053708
申请日：2021-02-16
申请人： CHIESI FARMACEUTICI S.P.A.
发明人： AMARI, Gabriele , ARMANI, Elisabetta
IPC分类号： C07D275/03 , C07D333/36 , C07D417/12 , A61K31/381 , A61P11/00
摘要： The present invention relates to a compounds of general formula (I) inhibiting both lysophosphatidic acid receptor 1 (LPA1) and receptor 2 (LPA2), particularly the invention relates to compounds that are 5-membered heterocyclyl derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. The compounds of the invention may be useful in the treatment of diseases or conditions associated with a dysregulation of LPA receptors, in particular fibrosis.

3. 发明申请

WO2021116259A1 AROMATIC AMIDO DERIVATIVES AS LPA RECEPTOR 2 INHIBITORS 审中-公开
公开(公告)号：WO2021116259A1
公开(公告)日：2021-06-17
申请号：PCT/EP2020/085458
申请日：2020-12-10
申请人： CHIESI FARMACEUTICI S.P.A.
发明人： AMARI, Gabriele , ARMANI, Elisabetta , PAGANO, Mafalda , RAVEGLIA, Luca , BEATO, Claudia
IPC分类号： C07D417/12 , C07D417/14 , A61P1/16 , A61P9/00 , A61P11/00 , A61P27/02 , A61K31/427 , A61K31/428
摘要： The present invention relates to compounds of general formula (I) inhibiting lysophosphatidic acid receptor 2 (LPA2), particularly the invention relates to compounds that are aromatic amido derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. The compounds of the invention may be useful in the treatment of diseases or conditions associated with a dysregulation of LPA receptors, in particular fibrosis.

4. 发明申请

WO2017108737A1 1-(3-TERT-BUTYL-PHENYL)-3-(4-([1,2,4]TRIAZOLO[4,3-A]PYRIDIN-6-YLOXY)-1,2,3,4-TETRAHYDRO- NAPHTHALEN-1-YL)-UREA DERIVATIVES AND THEIR USE AS P38 MAPK INHIBITORS 审中-公开
标题翻译： 1-（3-叔丁基 - 苯基）-3-（4 - （[1,2,4]三唑并[4,3-a]吡啶-6-基氧基）-1,2,3,4-四氢萘酚-1-基） - 脲衍生物及其作为P38 MAPK抑制剂的用途
公开(公告)号：WO2017108737A1
公开(公告)日：2017-06-29
申请号：PCT/EP2016/081837
申请日：2016-12-20
申请人： CHIESI FARMACEUTICI S.P.A.
发明人： CAPALDI, Carmelida , ARMANI, Elisabetta , JENNINGS, Andrew Stephen Robert , HURLEY, Christopher
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00 , A61P11/06
CPC分类号： C07D471/04
摘要： This invention relates to compounds of formula (I) wherein R 1 is H or selected from the group consisting of (C 1 -C 4 )alkyl-, (C 3 - C 7 )cycloalkyl-, (C 4 -C 7 )heterocycloalkyl-, R A O-, R C SO 2 (R A )N-, R C SO 2 -, (R A R B )NC(O)-, R C CO(R A )N-, R A O(C 1 -C 4 )alkylene-, (R A R B )N-, R C O(O) C-, (R A R B )NSO 2 -, R C SO 2 (C 1 -C 4 )alkylene-, R C (O)CO(C 1 -C 4 )alkylene-, R C SO 2 (R A )N(C 1 -C 4 )alkylene-, R C OC(O)(R A )N-, (R A R B )NCO(R D )N-, (R A R B ) N(C 1 -C 6 )alkylene-, wherein any of such alkyl, alkylene, cycloalkyl, heterocycloalkyl or heteroaryl may be optionally substituted by one or more groups selected from (C 1 -C 3 )alkyl, (C 3 -C 6 )cycloalkyl, (C 4 -C 7 ) heterocycloalkyl, -OR A , halo and CN; R 2 is H or selected from the group consisting of halo, (C 1 -C 6 )alkyl, R A O-, (R A R B )N(C 1 -C 6 )alkylene- and R A O(C 1 -C 4 )alkylene-; R 3 is selected from (lla)-(llf) and compositions that are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
摘要翻译：本发明涉及式（I）的化合物，其中R 1是H或选自（C 1 -C 4）烷基，（C 3 -C 7）环烷基 - ，（C 4 -C 4）烷基 - ，（C 3 -C 7）环烷基 - 7）杂环烷基 - ，R'-O-，R'C-SO 2（R'-A）（O） - ，R（= O） - ，R（R）（C1-C4）N-，R1-A（C1-C4）（R 1）R 2 B）N-，R 2 C（O）C-，（R 1）（A，B，B）NSO 2 - ，R C -SO 2（C = （O）CO（C 1 -C 4）亚烷基 - ，其中C 1 -C 4亚烷基 - （C 1 -C 2）亚烷基 - ，R 2 C（SO 2）2（R 1）N（C 1 -C 4）（O）（R A）N - ，（R A）R sup （B 1）NCO（R 2 D）N - ，（R 1 R 2 B）N（C 1） C 1-6亚烷基 - ，其中任何这样的烷基，亚烷基，环烷基，杂环基， C 1 -C 3烷基或杂芳基可任选被一个或多个选自（C 1 -C 3）烷基，（C 1 -C 3）（C 1 -C 7） - 杂环烷基，-OR A，卤素和CN; R 2是H或选自由卤素，（C 1 -C 6）烷基，R 2，（R 1 R 2 B）N（C 1 -C 6）亚烷基 - 和 [R ^{A 0（C <子> 1 -C <子> 4 ）亚烷基 - ; R31选自（IIa） - （IIf）和作为p38 MAPK抑制剂的组合物，其可用作治疗呼吸道疾病的抗炎剂。}

5. 发明申请

WO2013083606A1 KINASE INHIBITORS 审中-公开
标题翻译：激酶抑制剂
公开(公告)号：WO2013083606A1
公开(公告)日：2013-06-13
申请号：PCT/EP2012/074450
申请日：2012-12-05
申请人： CHIESI FARMACEUTICI S.P.A.
发明人： VAN NIEL, Monique Bodil , RAY, Nicholas Charles , ALCARAZ, Lilian , PANCHAL, Terry Aaron , JENNINGS, Andrew Stephen Robert , ARMANI, Elisabetta , CRIDLAND, Andrew Peter , HURLEY, Cristopher
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00
CPC分类号： C07D471/04
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R 2 , W, A, Y and R 1 are as defined in the specification, are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
摘要翻译：式（I）化合物或其药学上可接受的盐：其中R2，W，A，Y和R1如说明书中所定义，是p38MAPK抑制剂，其可用作治疗疾病的抗炎药的呼吸道。

6. 发明申请

WO2013083604A1 KINASE INHIBITORS 审中-公开
标题翻译：激酶抑制剂
公开(公告)号：WO2013083604A1
公开(公告)日：2013-06-13
申请号：PCT/EP2012/074446
申请日：2012-12-05
申请人： CHIESI FARMACEUTICI S.P.A.
发明人： VAN NIEL, Monique Bodil , RAY, Nicholas Charles , ALCARAZ, Lilian , PANCHAL, Terry Aaron , JENNINGS, Andrew Stephen Robert , ARMANI, Elisabetta , CRIDLAND, Andrew Peter , HURLEY, Cristopher
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00 , C07D401/12 , C07D403/12 , C07D519/00
CPC分类号： C07D471/04 , C07C53/06 , C07D231/40 , C07D401/12 , C07D403/12 , C07D487/08 , C07D498/08 , C07D519/00
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof: formula (I) wherein R 2 , W, A, Y and R 1 are as defined in the specification, are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia , diseases of the respiratory tract.
摘要翻译：式（I）化合物或其药学上可接受的盐：其中R 2，W，A，Y和R 1如说明书中所定义的式（I）是p38 MAPK抑制剂，其可用作抗炎剂，尤其是呼吸道疾病。

7. 发明申请

WO2017207433A1 HETETOCYCLIC COMPOUNDS FOR USE IN THE TREATMENT OF A DISEASE IN WHICH HNE IS IMPLICATED 审中-公开
标题翻译：用于治疗HNE所致疾病的杂环化合物
公开(公告)号：WO2017207433A1
公开(公告)日：2017-12-07
申请号：PCT/EP2017/062757
申请日：2017-05-26
申请人： CHIESI FARMACEUTICI S.P.A.
发明人： CAPALDI, Carmelida , ARMANI, Elisabetta , JENNINGS, Andrew Stephen Robert
IPC分类号： C07D401/14 , C07D403/04 , A61K31/4152 , A61K31/4155 , A61P11/00
摘要： This invention relates to imidazolone and pyrazolone derivatives having human neutrophil elastase inhibitory properties, and their use in therapy.
摘要翻译：本发明涉及具有人嗜中性粒细胞弹性蛋白酶抑制性质的咪唑酮和吡唑啉酮衍生物及其在治疗中的用途。

8. 发明申请

WO2017108738A1 1-(3-TERT-BUTYL-2H-PYRAZOL-5-YL OR 5-TERT-BUTYL-ISOXAOL-3-YL)-3-(4-([1,2,4]TRIAZOLO[4,3-A]PYRIDIN-6-YLOXY)-1,2,3,4-TETRAHYDRO-NAPHTHALENYL) UREA DERIVATIVES AND THEIR USE AS P38 MAPK INHIBITORS 审中-公开
标题翻译： 1-（3-叔丁基-2H-吡唑-5-基或5-叔丁基 - 异羟基-3-基）-3-（4 - （[1,2,4]三唑并[4,3-A ]吡啶-6-基氧基）-1,2,3,4-四 - 四氢萘基）脲衍生物及其作为P38 MAPK抑制剂的用途
公开(公告)号：WO2017108738A1
公开(公告)日：2017-06-29
申请号：PCT/EP2016/081839
申请日：2016-12-20
申请人： CHIESI FARMACEUTICI S.P.A.
发明人： CAPALDI, Carmelida , ARMANI, Elisabetta , JENNINGS, Andrew Stephen Robert , HURLEY, Christopher
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00 , A61P11/06
CPC分类号： C07D471/04
摘要： This invention relates to compounds of formulae (I), (II), and (III) and to compositions that are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
摘要翻译：本发明涉及式（I），（II）和（III）的化合物以及作为p38MAPK抑制剂的组合物，其用作抗炎剂尤其用于治疗呼吸道疾病。

9. 发明申请

WO2017102674A1 NOVEL TETRAHYDROTRIAZOLOPYRIMIDINE DERIVATIVES AS NHE INHIBITORS 审中-公开
标题翻译：作为NHE抑制剂的新型四氢三唑并嘧啶衍生物
公开(公告)号：WO2017102674A1
公开(公告)日：2017-06-22
申请号：PCT/EP2016/080713
申请日：2016-12-13
申请人： CHIESI FARMACEUTICI S.P.A.
发明人： ARMANI, Elisabetta , CAPALDI, Carmelida
IPC分类号： C07D487/04 , A61K31/519 , A61P11/00 , A61P11/06 , A61P37/08
CPC分类号： C07D487/04 , A61K31/519
摘要： This invention relates to triazolinone derivatives having human neutrophil elastase inhibitory properties, and their use in therapy.
摘要翻译：本发明涉及具有人嗜中性粒细胞弹性蛋白酶抑制性质的三唑啉酮衍生物及其在治疗中的用途。

10. 发明申请

WO2015082616A1 HETEROARYL DERIVATIVES FOR THE TREATMENT OF RESPIRATORY DISEASES 审中-公开
标题翻译：用于治疗呼吸道疾病的异氟烷衍生物
公开(公告)号：WO2015082616A1
公开(公告)日：2015-06-11
申请号：PCT/EP2014/076572
申请日：2014-12-04
申请人： CHIESI FARMACEUTICI S.P.A.
发明人： AMARI, Gabriele , ARMANI, Elisabetta , GHIDINI, Eleonora , BAKER-GLENN, Charles , VAN DE PÖEL, Hervé , WHITTAKER, Ben
IPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D409/14 , C07D417/14 , A61K31/444 , A61P11/00
CPC分类号： C07D453/02 , A61K31/44 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61M15/0065 , A61M16/14 , A61M2202/064 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention relates to novel compounds of formula (I) which are both phosphodiesterase 4 (PDE4) enzyme inhibitors and muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
摘要翻译：本发明涉及磷酸二酯酶4（PDE4）酶抑制剂和毒蕈碱M3受体拮抗剂二者的新型式（I）化合物，制备这些化合物的方法，含有它们的组合物及其治疗用途。

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