C07D317/68

DOPAMINE D3 RECEPTOR SELECTIVE ANTAGONISTS/PARTIAL AGONISTS AND USES THEREOF
20220265643 · 2022-08-25 ·

Disclosed herein are novel methods of treating pain in a patient in need thereof by providing to the patient a selective dopamine D3 receptor antagonist/partial agonist which when used with an opioid analgesic, can mitigate the development of opioid dependence, by preventing the need for dose escalation while either maintaining the opioid analgesic effect or providing analgesia with a lower dose of the opioid. In addition, the D3 antagonists/partial agonists described herein may be used to augment the effectiveness of current Medication Assisted Treatment regimens (e.g. methadone or buprenorphine) for the treatment of opioid use disorders.

Benzamide derivatives for inhibiting endoplasmic reticulum (ER) stress

Novel 3-(N-piperidinyl)methyl benzamide derivatives are disclosed. The compounds can be used in treating diseases and conditions which are associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic β-cell dysfunction and death, for example in the treatment of diabetes.

Benzamide derivatives for inhibiting endoplasmic reticulum (ER) stress

Novel 3-(N-piperidinyl)methyl benzamide derivatives are disclosed. The compounds can be used in treating diseases and conditions which are associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic β-cell dysfunction and death, for example in the treatment of diabetes.

NOVEL COMPOUND HAVING ANTICANCER ACTIVITY, AND METHOD FOR PRODUCING SAME
20220204497 · 2022-06-30 ·

The present invention pertains to a novel compound having anticancer activity, and a method for producing same, and more specifically, to a novel compound that exhibits excellent anticancer activity by inhibiting the expression of AIMP2-DX2, and a method for producing same. The compound represented by chemical formula 1 according to the present invention is highly effective in inhibiting the expression of AIMP2-DX2, and thus can be very advantageously used for the development of agents for treating various diseases, in particular cancer, caused by AIMP2-DX2.

NOVEL COMPOUND HAVING ANTICANCER ACTIVITY, AND METHOD FOR PRODUCING SAME
20220204497 · 2022-06-30 ·

The present invention pertains to a novel compound having anticancer activity, and a method for producing same, and more specifically, to a novel compound that exhibits excellent anticancer activity by inhibiting the expression of AIMP2-DX2, and a method for producing same. The compound represented by chemical formula 1 according to the present invention is highly effective in inhibiting the expression of AIMP2-DX2, and thus can be very advantageously used for the development of agents for treating various diseases, in particular cancer, caused by AIMP2-DX2.

Dopamine D3 receptor selective antagonists/partial agonists and uses thereof

Disclosed herein are novel methods of treating pain in a patient in need thereof by providing to the patient a selective dopamine D3 receptor antagonist/partial agonist which when used with an opioid analgesic, can mitigate the development of opioid dependence, by preventing the need for dose escalation while either maintaining the opioid analgesic effect or providing analgesia with a lower dose of the opioid. In addition, the D3 antagonists/partial agonists described herein may be used to augment the effectiveness of current Medication Assisted Treatment regimens (e.g. methadone or buprenorphine) for the treatment of opioid use disorders.

NERVE DAMAGE PREVENTING AND NERVE PROTECTING COMPOUNDS, PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION THEREOF, AND THEIR USE

The present invention provides a novel compound for effectively preventing nerve damage and protecting nerves, and a preparation method thereof. Besides, the present invention also provides a pharmaceutical composition comprising the novel compound, and a use of the novel compound for preventing nerve damage and protecting nerves.

NERVE DAMAGE PREVENTING AND NERVE PROTECTING COMPOUNDS, PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION THEREOF, AND THEIR USE

The present invention provides a novel compound for effectively preventing nerve damage and protecting nerves, and a preparation method thereof. Besides, the present invention also provides a pharmaceutical composition comprising the novel compound, and a use of the novel compound for preventing nerve damage and protecting nerves.

PROCESS FOR THE PREPARATION OF 2,2-DIFLUORO-1,3-BENZODIOXOLE AND INTERMEDIATES THEREOF

A process for preparing 2,2-difluoro-1,3-benzodioxole is provided that comprises a step of reacting 1,3-benzodioxole with chlorine in benzotrifluoride in the presence of a radical initiator. Additional processes are provided for preparing 2,2-dichloro-1,3-benzodioxole, which is used as an intermediate in preparation of 2,2-difluoro-1,3-benzodioxole.

PROCESS FOR THE PREPARATION OF 2,2-DIFLUORO-1,3-BENZODIOXOLE AND INTERMEDIATES THEREOF

A process for preparing 2,2-difluoro-1,3-benzodioxole is provided that comprises a step of reacting 1,3-benzodioxole with chlorine in benzotrifluoride in the presence of a radical initiator. Additional processes are provided for preparing 2,2-dichloro-1,3-benzodioxole, which is used as an intermediate in preparation of 2,2-difluoro-1,3-benzodioxole.