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Aza-indazole compounds for use in tendon and/or ligament injuries

A compound and heterocyclic technology, applied in the fields of drug combination, organic chemistry, drug delivery, etc., can solve problems such as tendinopathy in its infancy

Active Publication Date: 2019-05-03
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although many specific growth factors and transcription factors have been identified to be involved in tenogenesis during development and repair, a detailed understanding of tendinopathy is still in its infancy

Method used

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  • Aza-indazole compounds for use in tendon and/or ligament injuries
  • Aza-indazole compounds for use in tendon and/or ligament injuries
  • Aza-indazole compounds for use in tendon and/or ligament injuries

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Embodiment 1. A compound having formula (I), which is in free form or in the form of a pharmaceutically acceptable salt

[0073]

[0074] in,

[0075] R 1 from C 1 -C 3 Alkyl and halogen;

[0076] R 2 Selected from NHSO 2 (CH 2 ) n R 3 or SO 2 NR 5 R 6 ;

[0077] n is 0 or 1;

[0078] R 3 selected from optionally by R 4 Phenyl substituted one or more times, C optionally substituted by hydroxy 3 -C 6 Cycloalkyl, fused bicyclic aromatic ring systems;

[0079] R 4 independently selected from halogen, C 1 -C 3 Alkoxy, cyano, C 1 -C 3 Alkyl, hydroxyl, halogenated C 1 -C 3 Alkyl, NHC(O)CH 3 , Halogenated C 1 -C 3 Alkoxy, SO 2 NH(CH 3 );and / or

[0080] Two R's at adjacent carbon atoms 4 Forming a 5-membered or 6-membered heterocyclic non-aromatic ring comprising at least one heteroatom selected from N, O or S, which is fused to a benzene ring and optionally surrounded by C(O)CH 3 replace;

[0081] R 5 Choose from H, C 1 -C 3 alkyl;

[...

Embodiment 2

[0087] Embodiment 2. The compound according to embodiment 1, which has formula (II), which is in free form or in the form of a pharmaceutically acceptable salt

[0088]

Embodiment 3

[0089] Embodiment 3. The compound according to embodiment 1 or 2, which compound has formula (IIa), which is in free form or in the form of a pharmaceutically acceptable salt

[0090]

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Abstract

The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form, a method for manufacturing the compounds of the invention, and its therapeutic uses.The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Description

technical field [0001] The present invention provides aza-indazole compounds, their use for treating tendon and / or ligament injuries, and methods of using said compounds for treating tendon and / or ligament injuries. Background technique [0002] Tendons and ligaments form an important part of the musculoskeletal system by connecting muscles to bones and bones to bones, respectively. Both tendons and ligaments arise through the same differentiation process (Schweitzer, R. et al. Development, 2001 Oct;128(19):3855-66). Although a number of specific growth factors and transcription factors have been identified to be involved in tenogenesis during development and repair, a detailed understanding of tendinopathy is still in its infancy. [0003] A review of tendon biology (Duprez D. et al., Nature, 2015, 11, 223-233) summarizes the progress made so far in tendon biology and emphasizes that there is still a need for effective treatments for tendon injuries. [0004] To date, the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61K31/437A61P19/02
CPCC07D471/04A61P19/02A61P19/04A61P21/00A61P43/00A61K9/0019A61K9/1647A61K9/5031A61K31/437A61K31/496A61K31/538
Inventor B·布尔苏拉亚A·菲施J·P·拉伊内斯R·马绍尔S·马莱卡H·M·J·彼得拉西F·拉马扎尼A-C·雷蒙德T·乌尔里奇P·于塞尔曼E·范格莱维灵格
Owner NOVARTIS AG