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Indazole compounds for use in tendon and/or ligament injuries

A compound, indazole technology, applied in drug combination, organic chemistry, drug delivery, etc., can solve problems such as tendinopathy in its infancy

Active Publication Date: 2022-08-05
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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  • Indazole compounds for use in tendon and/or ligament injuries
  • Indazole compounds for use in tendon and/or ligament injuries
  • Indazole compounds for use in tendon and/or ligament injuries

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Embodiment 1. A compound of formula (I) in free form or in the form of a pharmaceutically acceptable salt

[0078]

[0079] in,

[0080] R 1 from C 1 -C 3 Alkyl, halogen and C 1 -C 3 alkoxy;

[0081] R 2 independently selected from C 1 -C 3 Alkyl and halogen;

[0082] n is 1 or 2;

[0083] R 3 selected from H and C 1 -C 3 alkyl; and

[0084] R 4 is selected optionally by R 5 replace C one or more times 4 -C 6 Cycloalkyl, containing at least one heteroatom selected from N, O or S, optionally substituted by hydroxy, C 1 -C 3 Alkyl, C 1 -C 3 A 5- or 6-membered heterocyclic non-aromatic ring independently substituted one or more times by alkoxy; wherein R 4 not 4-hydroxycyclohexyl or tetrahydrofuran;

[0085] or

[0086] R 3 and R 4 Together with the N atom to which they are attached form a 4-, 5- or 6-membered heterocyclic non-aromatic ring optionally containing one additional heteroatom selected from N, O or S, the ring being surrounded by R ...

Embodiment 2

[0089]Embodiment 2. The compound of Embodiment 1, having formula (I-1), in free form or in the form of a pharmaceutically acceptable salt

[0090]

Embodiment 3

[0091] Embodiment 3. The compound of embodiment 1 or 2, having formula (II), in free form or in the form of a pharmaceutically acceptable salt

[0092]

[0093] where m is 0, 1 or 2 and x is 1 or 2.

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Abstract

The present invention provides compounds of formula (I) in free form or in pharmaceutically acceptable salt form (I), methods for making the compounds of the present invention, and therapeutic uses thereof. The present invention further provides combinations of pharmacologically active agents and pharmaceutical compositions.

Description

technical field [0001] The present invention provides indazole compounds for their use in the treatment of tendon and / or ligament injuries, and methods of using the compounds for the treatment of 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 many specific growth factors and transcription factors have been identified to be involved in tendinogenesis 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 highlights that there remains a need for effective treatments for tendon injuries. [0004] To d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D231/56A61P19/04A61K31/416
CPCA61K31/416A61K31/454C07D231/56C07D401/12C07D403/12C07D405/12A61P19/00A61P19/02A61P19/04A61P21/00A61P43/00A61K2300/00A61K9/0019A61K9/1647C07D405/04
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
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