A61K31/428

PHARMACEUTICAL COMPOSITION, COMPLEMENTARY KIT AND APPLICATION THEREOF
20230028539 · 2023-01-26 ·

A pharmaceutical composition, a complementary kit and an application thereof; the pharmaceutical composition comprises pramipexole and safinamide, the mass ratio of pramipexole to safinamide being 1:300-1:30; and the pharmaceutical composition has a good curative effect and has few side effects, and effectively improve the condition of a patient. The capabilities thereof in restoring dopamine levels are better than those from using pramipexole or safinamide alone. In addition, the composition has better neuroprotective activity, and therefore damage to the dopaminergic system and the normal sensitivity of the dopamine system to dopamine agonists are reduced. The composition can restore or balance a potential unbalanced response to “increasing dopaminergic treatment” that is caused by the use of a dopamine agonist alone; the composition can reduce the amount of pramipexole when used alone so as to reduce the risk of side effects and drug resistance.

PHARMACEUTICAL COMPOSITION, COMPLEMENTARY KIT AND APPLICATION THEREOF
20230028539 · 2023-01-26 ·

A pharmaceutical composition, a complementary kit and an application thereof; the pharmaceutical composition comprises pramipexole and safinamide, the mass ratio of pramipexole to safinamide being 1:300-1:30; and the pharmaceutical composition has a good curative effect and has few side effects, and effectively improve the condition of a patient. The capabilities thereof in restoring dopamine levels are better than those from using pramipexole or safinamide alone. In addition, the composition has better neuroprotective activity, and therefore damage to the dopaminergic system and the normal sensitivity of the dopamine system to dopamine agonists are reduced. The composition can restore or balance a potential unbalanced response to “increasing dopaminergic treatment” that is caused by the use of a dopamine agonist alone; the composition can reduce the amount of pramipexole when used alone so as to reduce the risk of side effects and drug resistance.

Treatment of unipolar depressive disorder

The invention relates to the treatment or control of unipolar depressive disorder by administering a compound of Formula I or a salt thereof to a subject; ##STR00001##
wherein:
E is S or Se;
R.sup.1 and R.sup.2 are optional substituents, and are at each occurrence independently selected from:
(1) a halogen, which is preferably selected from F, Cl and Br;
(2) C.sub.1-C.sub.4 alkyl, such as C.sub.1-C.sub.2 alkyl or C.sub.1 alkyl, optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br; and
(3) C.sub.1-C.sub.4 alkoxy, such as C.sub.1-C.sub.2 alkoxy or C.sub.1 alkoxy; optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br;
m is an integer in the range of from 0 to 5; and
n is an integer in the range of from 0 to 4.

Treatment of unipolar depressive disorder

The invention relates to the treatment or control of unipolar depressive disorder by administering a compound of Formula I or a salt thereof to a subject; ##STR00001##
wherein:
E is S or Se;
R.sup.1 and R.sup.2 are optional substituents, and are at each occurrence independently selected from:
(1) a halogen, which is preferably selected from F, Cl and Br;
(2) C.sub.1-C.sub.4 alkyl, such as C.sub.1-C.sub.2 alkyl or C.sub.1 alkyl, optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br; and
(3) C.sub.1-C.sub.4 alkoxy, such as C.sub.1-C.sub.2 alkoxy or C.sub.1 alkoxy; optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br;
m is an integer in the range of from 0 to 5; and
n is an integer in the range of from 0 to 4.

Treatment of unipolar depressive disorder

The invention relates to the treatment or control of unipolar depressive disorder by administering a compound of Formula I or a salt thereof to a subject; ##STR00001##
wherein:
E is S or Se;
R.sup.1 and R.sup.2 are optional substituents, and are at each occurrence independently selected from:
(1) a halogen, which is preferably selected from F, Cl and Br;
(2) C.sub.1-C.sub.4 alkyl, such as C.sub.1-C.sub.2 alkyl or C.sub.1 alkyl, optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br; and
(3) C.sub.1-C.sub.4 alkoxy, such as C.sub.1-C.sub.2 alkoxy or C.sub.1 alkoxy; optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br;
m is an integer in the range of from 0 to 5; and
n is an integer in the range of from 0 to 4.

Antibacterial compounds

The present invention relates to certain compounds of formula (I) wherein—Ar is (Ar1) or (Ar2) and to their uses as antibacterial agents. The invention further relates to methods of treatment of bacterial infection with such compounds, optionally in combination with other antimicrobials and to compositions and pharmaceutical formulations containing such compounds. The invention additionally relates to coatings containing such compounds and to items having such coatings. ##STR00001##

Antibacterial compounds

The present invention relates to certain compounds of formula (I) wherein—Ar is (Ar1) or (Ar2) and to their uses as antibacterial agents. The invention further relates to methods of treatment of bacterial infection with such compounds, optionally in combination with other antimicrobials and to compositions and pharmaceutical formulations containing such compounds. The invention additionally relates to coatings containing such compounds and to items having such coatings. ##STR00001##

Combination of low dose IL-2 and an inhibitor of Treg IL-2R desensitization to treat autoimmune and allergic inflammatory diseases

Provided herein are methods and compositions for treating inflammatory disease by the administration, to a patient in need thereof, of an inhibitor of IL-2R desensitization in combination with a low dose of IL-2. A low dose of interleukin-2 (IL-2) is sufficient to stimulate regulatory T lymphocytes (Tregs) without substantially inducing effector T lymphocytes (Teffs). In some embodiments, the inhibitor of IL-2R desensitization is a small molecule or drug. Is some embodiments the inhibitor is a NEDD8 activating enzyme (NAE) inhibitor. In some embodiments a combination therapy provides for a synergistic effect, where the combination of the inhibitor of IL-2R desensitization and low dose IL-2 provides an effect that is greater than the sum of either the inhibitor or low dose IL-2 administered as a single agent.

Combination of low dose IL-2 and an inhibitor of Treg IL-2R desensitization to treat autoimmune and allergic inflammatory diseases

Provided herein are methods and compositions for treating inflammatory disease by the administration, to a patient in need thereof, of an inhibitor of IL-2R desensitization in combination with a low dose of IL-2. A low dose of interleukin-2 (IL-2) is sufficient to stimulate regulatory T lymphocytes (Tregs) without substantially inducing effector T lymphocytes (Teffs). In some embodiments, the inhibitor of IL-2R desensitization is a small molecule or drug. Is some embodiments the inhibitor is a NEDD8 activating enzyme (NAE) inhibitor. In some embodiments a combination therapy provides for a synergistic effect, where the combination of the inhibitor of IL-2R desensitization and low dose IL-2 provides an effect that is greater than the sum of either the inhibitor or low dose IL-2 administered as a single agent.

Combination of low dose IL-2 and an inhibitor of Treg IL-2R desensitization to treat autoimmune and allergic inflammatory diseases

Provided herein are methods and compositions for treating inflammatory disease by the administration, to a patient in need thereof, of an inhibitor of IL-2R desensitization in combination with a low dose of IL-2. A low dose of interleukin-2 (IL-2) is sufficient to stimulate regulatory T lymphocytes (Tregs) without substantially inducing effector T lymphocytes (Teffs). In some embodiments, the inhibitor of IL-2R desensitization is a small molecule or drug. Is some embodiments the inhibitor is a NEDD8 activating enzyme (NAE) inhibitor. In some embodiments a combination therapy provides for a synergistic effect, where the combination of the inhibitor of IL-2R desensitization and low dose IL-2 provides an effect that is greater than the sum of either the inhibitor or low dose IL-2 administered as a single agent.