公开(公告)号：US20160207930A1

公开(公告)日：2016-07-21

申请号：US14913647

申请日：2014-08-15

Applicant: LEO PHARMA A/S

Inventor： Haakan BLADH ,  Jakob FELDING ,  Ding ZHOU ,  Zhen-wei CAI ,  Morten Dahl SØRENSEN

IPC: C07D487/04 ,  A61K9/00 ,  A61K31/4985

CPC classification number: C07D487/04 ,  A61K9/0014 ,  A61K31/4985

Abstract: The invention relates novel NK1 receptor antagonists represented in formula A, wherein R1 and R2 independently are selected from the group consisting of (C1-4)alkyl, (C1-4)haloalkyl, (C1-4)alkoxy, CD3 or halogen; R3 is selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4)haloalkyl and (C1-4)hydroxyalkyl; R4 is selected from the group consisting of phenyl, 5-membered heteroaryl and 6-membered heteroaryl; R5 and R6 are independently selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4) hydroxyalkyl and (C1-4)haloalkyl and X and Y are independently selected from the group consisting of CH and N. The invention furthermore relates to intermediates for the preparation of said compounds, to their use in therapy, and to pharmaceutical compositions comprising said compounds.

Abstract translation: 本发明涉及式A中所示的新型NK1受体拮抗剂，其中R1和R2独立地选自（C1-4）烷基，（C1-4）卤代烷基，（C1-4）烷氧基，CD3或卤素; R3选自氢，（C1-4）烷基，（C1-4）卤代烷基和（C1-4）羟基烷基; R4选自苯基，5元杂芳基和6元杂芳基; R 5和R 6独立地选自氢，（C 1-4）烷基，（C 1-4）羟基烷基和（C 1-4）卤代烷基，X和Y独立地选自CH和N。 本发明还涉及制备所述化合物的中间体，其在治疗中的用途以及包含所述化合物的药物组合物。

公开(公告)号：US20160009751A1

公开(公告)日：2016-01-14

申请号：US14330808

申请日：2014-07-14

Applicant: LEO Pharma A/S

Inventor： Michael L. SIERRA ,  Jakob FELDING ,  Qianghui ZHOU ,  Hans RENATA ,  Philippe S. BARAN

IPC: C07J7/00 ,  C07J21/00 ,  A61K31/573

CPC classification number: C07J7/0085 ,  A61K31/573 ,  A61K45/06 ,  C07J21/006

Abstract: The present invention relates to a compound according to formula I wherein R1 is selected from the group consisting of hydrogen and fluoro and R2 is selected from C1-C4 alkyl and hydrates or solvates thereof. The invention further relates to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.

Abstract translation: 本发明涉及式Ⅰ化合物，其中R 1选自氢和氟，R 2选自C 1 -C 4烷基及其水合物或溶剂合物。 本发明还涉及用于制备所述化合物的中间体，用于治疗的所述化合物，包含所述化合物的药物组合物，用所述化合物治疗疾病的方法，以及所述化合物在制备药物中的用途。