公开(公告)号：US20180290966A1

公开(公告)日：2018-10-11

申请号：US16003385

申请日：2018-06-08

Applicant: Hoffmann-La Roche Inc.

Inventor： Olivier GAVELLE ,  Uwe GRETHER ,  Matthias NETTEKOVEN ,  Stephan ROEVER ,  Mark ROGERS-EVANS ,  Didier ROMBACH

IPC: C07C235/52 ,  C07C231/02 ,  C07D271/06 ,  C07D277/28 ,  C07D205/04 ,  C07D413/12 ,  C07D305/08 ,  C07D331/04 ,  C07D207/16 ,  C07D413/10 ,  C07D213/61 ,  C07D403/10 ,  C07D231/12 ,  C07D401/10 ,  C07D207/10 ,  C07D413/06

Abstract: The invention relates to a compound of formula (I) wherein R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

公开(公告)号：US20150307452A1

公开(公告)日：2015-10-29

申请号：US14648431

申请日：2013-12-02

Applicant: HOFFMANN-LA ROCHE INC.

Inventor： Beat FREI ,  Luca GOBBI ,  Uwe GRETHER ,  Atsushi KIMBARA ,  Matthias NETTEKOVEN ,  Stephan ROEVER ,  Mark ROGERS-EVANS ,  Tanja SCHULZ-GASCH

IPC: C07D213/81 ,  C07D401/12 ,  C07D405/14 ,  C07D405/12 ,  C07D401/14 ,  C07D401/04

CPC classification number: C07D213/81 ,  A61P3/10 ,  A61P9/00 ,  A61P27/02 ,  A61P29/00 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: The invention relates to a compound of formula (I) wherein R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract translation: 本发明涉及式（I）化合物，其中R 1至R 3如在说明书和权利要求书中所定义。 式（I）化合物可以用作药物。

公开(公告)号：US20240376073A1

公开(公告)日：2024-11-14

申请号：US18404194

申请日：2024-01-04

Applicant: Hoffmann-La Roche Inc.

Inventor： Sandra Marie Joseph GRALL-ULSEMER ,  Xingchun HAN ,  Joel Lukas KNECHT ,  Christian LERNER ,  Mingming LI ,  Yongqiang LIU ,  Patrizio MATTEI ,  Matthias NETTEKOVEN ,  Philippe PFLIEGER ,  Theodor STOLL ,  Jianhua WANG ,  Min WANG ,  Yongguang WANG ,  Song YANG ,  Chengang ZHOU

IPC: C07D401/12 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/427 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5355 ,  A61P31/04 ,  C07C53/06 ,  C07C53/10 ,  C07D233/90 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/14 ,  C07D487/04

Abstract: The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein R1 to R6 are as described herein: Frther provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.

公开(公告)号：US20230203043A1

公开(公告)日：2023-06-29

申请号：US17976651

申请日：2022-10-28

Applicant: Hoffmann-La Roche Inc.

Inventor： Jean-Baptiste BLANC ,  Christian LERNER ,  Matthias NETTEKOVEN ,  Philippe PFLIEGER ,  Bernd PUELLMANN ,  Sébastien SCHMITT ,  Theodor STOLL ,  Song YANG ,  Chengang ZHOU

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The invention provides novel imidazopyrazine derivatives having the general formula (I), or pharmaceutically acceptable salts thereof, wherein X and R3 to R9 are as described herein:




Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.

公开(公告)号：US20220396565A1

公开(公告)日：2022-12-15

申请号：US17869755

申请日：2022-07-20

Applicant: Hoffmann-La Roche Inc.

Inventor： Zhanling CHENG ,  Xingchun HAN ,  Christian KRAMER ,  Christian LERNER ,  Yongqiang LIU ,  Matthias NETTEKOVEN ,  Philippe PFLIEGER ,  Bernd PUELLMANN ,  Jianhua WANG ,  Lisha WANG ,  Min WANG ,  Yongguang WANG ,  Song YANG ,  Chengang ZHOU

IPC: C07D403/12 ,  C07D233/90 ,  C07D403/14 ,  C07D487/10 ,  C07D401/14

Abstract: Provided are novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein R1 to R4, m, n, and p are as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.

公开(公告)号：US20150344429A1

公开(公告)日：2015-12-03

申请号：US14648412

申请日：2013-12-04

Applicant: HOFFMANN-LA ROCHE INC.

Inventor： Uwe GRETHER ,  Atsushi KIMBARA ,  Matthias NETTEKOVEN ,  Fabienne RICKLIN ,  Stephan ROEVER ,  Mark ROGERS-EVANS ,  Didier ROMBACH ,  Tanja SCHULZ-GASCH ,  Matthias WESTPHAL

IPC: C07D213/81 ,  C07D413/14 ,  C07D491/107 ,  C07D417/14 ,  C07D401/04 ,  C07D405/12 ,  C07D417/12

CPC classification number: C07D213/81 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D491/10 ,  C07D491/107

Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) is a CB2 agonist and can be used as an active ingredient in a medicament.

Abstract translation: 本发明涉及式（I）化合物，其中R 1至R 4如说明书和权利要求中所定义。 式（I）化合物是CB 2激动剂，可用作药物中的活性成分。

公开(公告)号：US20230257354A1

公开(公告)日：2023-08-17

申请号：US18117966

申请日：2023-03-06

Applicant: Hoffmann-La Roche Inc.

Inventor： Zhanling CHENG ,  Christian LERNER ,  Yongqiang LIU ,  Matthias NETTEKOVEN ,  Philippe PFLIEGER ,  Bernd PUELLMANN ,  Jianhua WANG ,  Min WANG ,  Yongguang WANG ,  Song YANG ,  Chengang ZHOU

IPC: C07D233/90 ,  C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  A61P31/04

CPC classification number: C07D233/90 ,  C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  A61P31/04

Abstract: The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein R1 to R9 and p are as described herein:




Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.

公开(公告)号：US20230141403A1

公开(公告)日：2023-05-11

申请号：US18076383

申请日：2022-12-06

Applicant: Hoffmann-La Roche Inc.

Inventor： Zhanling CHENG ,  Xingchun HAN ,  Christian KRAMER ,  Holger KUEHNE ,  Christian LERNER ,  Mingming LI ,  Matthias NETTEKOVEN ,  Theodor STOLL ,  Min WANG ,  Song YANG

IPC: C07D487/04 ,  A61P31/04

CPC classification number: C07D487/04 ,  A61P31/04

Abstract: The invention provides novel imidazopyrazine derivatives having the general formula (I), or pharmaceutically acceptable salts thereof, wherein X, m, n, and R1 to R3 are as described herein:




Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.

公开(公告)号：US20230012368A1

公开(公告)日：2023-01-12

申请号：US17349832

申请日：2021-06-16

Applicant: Hoffmann-La Roche Inc.

Inventor： Jean-Baptiste BLANC ,  Zhanling CHENG ,  Xingchun HAN ,  Nawaz KHAN ,  Christian KRAMER ,  Holger KUEHNE ,  Christian LERNER ,  Matthias NETTEKOVEN ,  Philippe PFLIEGER ,  Bernd PUELLMANN ,  Sebastien SCHMITT ,  Theodor STOLL ,  Jianhua WANG ,  Yongguang WANG ,  Song YANG

IPC: C07D487/04 ,  C07F9/6561 ,  C07D519/00 ,  C07H9/06 ,  A61P31/04

Abstract: Provided are novel imidazopyrazine derivatives having the general formula (I), wherein R1 to R11 are as described herein and pharmaceutically acceptable salts thereof.
Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and related diseases.

公开(公告)号：US20150299220A1

公开(公告)日：2015-10-22

申请号：US14648399

申请日：2013-12-04

Applicant: HOFFMANN-LA ROCHE INC.

Inventor： Baledi DHURWASULU ,  Uwe GRETHER ,  Matthias NETTEKOVEN ,  Stephan ROEVER ,  Mark ROGERS-EVANS ,  Tanja SCHULZ-GASCH

IPC: C07D498/08 ,  C07D403/14 ,  C07D417/14 ,  C07D413/14 ,  C07D491/107 ,  C07D403/06 ,  C07D403/04

CPC classification number: C07D498/08 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14 ,  C07D491/107

Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) is a CB2 receptor agonist for use in the treatment of several disorders, such as pain, atherosclerosis and glaucoma.

Abstract translation: 本发明涉及式（I）化合物，其中R 1至R 4如说明书和权利要求中所定义。 式（I）化合物是用于治疗几种疾病如疼痛，动脉粥样硬化和青光眼的CB2受体激动剂。