公开(公告)号：US20230022724A1

公开(公告)日：2023-01-26

申请号：US17349760

申请日：2021-06-16

Applicant: Hoffmann-La Roche Inc.

Inventor： Zhanling CHENG ,  Nawaz KHAN ,  Christian KRAMER ,  Christian LERNER ,  Philippe PFLIEGER ,  Theodor STOLL ,  Jianhua WANG ,  Yongguang WANG ,  Song YANG

IPC: C07D487/04 ,  A61P31/04

Abstract: Provided are novel imidazopyrazine derivatives having the general formula (I), wherein A and 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 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：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：US20230013602A1

公开(公告)日：2023-01-19

申请号：US17349888

申请日：2021-06-16

Applicant: Hoffmann-La Roche Inc.

Inventor： Jean-Baptiste BLANC ,  Nawaz KHAN ,  Christian KRAMER ,  Christian LERNER ,  Philippe PFLIEGER ,  Theodor STOLL ,  Song YANG

IPC: C07D487/04 ,  A61P31/04 ,  B01J31/12

Abstract: Provided are novel imidazopyrazine derivatives having the general formula (I), wherein A and R1 to R14 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 resulting diseases.

公开(公告)号：US20240050516A1

公开(公告)日：2024-02-15

申请号：US18379626

申请日：2023-10-12

Applicant: Hoffmann-La Roche Inc.

Inventor： Konrad BLEICHER ,  Daniella CHEANG ,  Patrick DI GIORGIO ,  Taishan HU ,  Christian JENNY ,  Patrizio MATTEI ,  Petra SCHMITZ ,  Theodor STOLL

IPC: A61K38/12 ,  A61P31/04

CPC classification number: A61K38/12 ,  A61P31/04

Abstract: The present invention provides compounds of formula (I)






wherein X1, X2, R1 to R6 and A are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by bacteria.

公开(公告)号：US20230391778A1

公开(公告)日：2023-12-07

申请号：US18451702

申请日：2023-08-17

Applicant: Hoffmann-La Roche Inc.

Inventor： Hans HILPERT ,  Sabine KOLCZEWSKI ,  Roland HUMM ,  Theodor STOLL ,  Thorsten MUSER ,  Jean-Marc PLANCHER ,  Delphine GAUFRETEAU

IPC: C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  A61K31/4439 ,  A61K31/506 ,  A61K45/06 ,  C07D403/04

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  A61K31/4439 ,  A61K31/506 ,  A61K45/06 ,  C07D403/04

Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula






wherein
Ar1 is phenyl or a five or six membered heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O−);
R1 is lower alkyl, halogen, cyano or cycloalkyl;
Ar2 is a five or six membered heteroaryl group, containing one, two, three or four heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O−), or is benzo[b]thiophenyl;
R2 is hydrogen, lower alkyl, halogen, cyano, lower alkyl substituted by hydroxyl, lower alkyl substituted by halogen, lower alkyl substituted by amino, lower alkyl substituted by alkoxy, lower alkyl substituted by amide, or is cycloalkyl;
X is CH or N;
n is 1 or 2;
m is 1 or 2;
as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof




The compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, epilepsy, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems.

公开(公告)号：US20230141600A1

公开(公告)日：2023-05-11

申请号：US18076274

申请日：2022-12-06

Applicant: Hoffmann-La Roche Inc.

Inventor： Zhanling CHENG ,  Christian KRAMER ,  Christian LERNER ,  Yongqiang LIU ,  Matthias NETTEKOVEN ,  Philippe PFLIEGER ,  Sébastien SCHMITT ,  Theodor STOLL ,  Jianhua WANG ,  Yongguang WANG ,  Song YANG ,  Chengang ZHOU

IPC: C07D487/04 ,  C07D519/00 ,  A61P31/04 ,  A61K9/20 ,  A61K9/48 ,  A61K9/08 ,  A61K47/12 ,  A61K47/40

CPC classification number: C07D487/04 ,  C07D519/00 ,  A61P31/04 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2009 ,  A61K9/4866 ,  A61K9/4858 ,  A61K9/485 ,  A61K9/08 ,  A61K47/12 ,  A61K47/40

Abstract: The invention provides novel imidazopyrazine derivatives having the general formula (I), wherein Rx and R3 to R5 are as described herein:




or 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 resulting diseases.

公开(公告)号：US20230017532A1

公开(公告)日：2023-01-19

申请号：US17349862

申请日：2021-06-16

Applicant: Hoffmann-La Roche Inc.

Inventor： Zhanling CHENG ,  Nawaz KHAN ,  Christian KRAMER ,  Christian LERNER ,  Matthias NETTEKOVEN ,  Philippe PFLIEGER ,  Bernd PUELLMANN ,  Sebastien SCHMITT ,  Theodor STOLL ,  Jianhua WANG ,  Song YANG

IPC: C07D487/04 ,  C07D519/00

Abstract: Provided are novel imidazopyrazine derivatives having the general formula (I), wherein A and 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.