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US 2020/0270306 A1Published application
Peptides and pharmaceutical compositions for treating eye diseases
AssigneeYuyu Pharma, Inc.
InventorsTaegon Baik, Jong-Yun Choi, Gyoung-Wook Min
Life of this patent
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Abstract
The present invention relates to novel peptides and a pharmaceutical compositions comprising the same. The peptide compounds and compositions disclosed herein are useful as therapeutic agents for treating eye diseases. When administered to the eyes, the peptide compounds and compositions disclosed herein increase the amount of tear secretion and promotes recovery of a damaged cornea.
Claims36
A compound represented by Formula (I):
- or a pharmaceutically acceptable salt thereof;
- wherein:
- R1, R2, and R3 are each independently H or substituted or unsubstituted alkyl, alkoxy, haloalkyl, alkenyl, alkynyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, heteroaryl, or heteroarylalkyl;
- R4, independently for each occurrence, is selected from substituted or unsubstituted alkyl, aryl, arylalkyl, heterocycloalkyl, oxo, —ORb, —CH2ORb, halo, hydroxyl, and hydroxyalkyl;
- Rb is substituted or unsubstituted alkyl, aryl, arylalkyl, or heterocycloalkyl;
- p is 0, 1, or 2;
- R6 is hydrogen or substituted or unsubstituted alkyl;
- and
- R7, R8, and R9 are each independently hydrogen or alkyl;
- wherein the compound is not:
7 more elements
3-9. (canceled)
11-17. (canceled)
19-23. (canceled)
25-28. (canceled)
30-47. (canceled)
49-52. (canceled)
54-58. (canceled)
(canceled)
63-74. (canceled)
A compound represented by Formula (V):
- or a pharmaceutically acceptable salt thereof;
- wherein:
- R1 and R2 are each independently H or substituted or unsubstituted alkyl, alkoxy, haloalkyl, alkenyl, alkynyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, heteroaryl, or heteroarylalkyl;
- R4, independently for each occurrence, is selected from substituted or unsubstituted alkyl, aryl, arylalkyl, heterocycloalkyl, oxo, —ORb, —CH2ORb, halo, hydroxyl, and hydroxyalkyl;
- Rb is substituted or unsubstituted alkyl, aryl, arylalkyl, or heterocycloalkyl;
- p is 0, 1, or 2;
- R6 is hydrogen or substituted or unsubstituted alkyl;
- and
- R9 is hydrogen or alkyl.
6 more elements
76-91. (canceled)
(canceled)
A compound represented by Formula (VI):
- or a pharmaceutically acceptable salt thereof;
- wherein:
- R1 and R2 are each independently H or substituted or unsubstituted alkyl, alkoxy, haloalkyl, alkenyl, alkynyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, heteroaryl, or heteroarylalkyl;
- R4, independently for each occurrence, is selected from substituted or unsubstituted alkyl, aryl, arylalkyl, heterocycloalkyl, oxo, —ORb, —CH2ORb, halo, hydroxyl, and hydroxyalkyl;
- Rb is substituted or unsubstituted alkyl, aryl, arylalkyl, or heterocycloalkyl;
- p is 0, 1, or 2;
- R6 is hydrogen or substituted or unsubstituted alkyl;
- R7 is hydrogen or alkyl;
- and
- R9 is hydrogen or alkyl.
7 more elements
95-116. (canceled)
A compound represented by Formula (VII):
- or a pharmaceutically acceptable salt thereof;
- wherein:
- R1 and R2 are each independently H or substituted or unsubstituted alkyl, alkoxy, haloalkyl, alkenyl, alkynyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, heteroaryl, or heteroarylalkyl;
- R4, independently for each occurrence, is selected from substituted or unsubstituted alkyl, aryl, arylalkyl, heterocycloalkyl, oxo, —ORb, —CH2ORb, halo, hydroxyl, and hydroxyalkyl;
- Rb is substituted or unsubstituted alkyl, aryl, arylalkyl, or heterocycloalkyl;
- p is 0, 1, or 2;
- R6 is hydrogen or substituted or unsubstituted alkyl;
- R7 is hydrogen or alkyl;
- and
- R9 is hydrogen or alkyl.
7 more elements
118-142. (canceled)
A compound represented by Formula (IX):
- or a pharmaceutically acceptable salt thereof;
- wherein:
- R1 and R2 are each independently H or substituted or unsubstituted alkyl, alkoxy, haloalkyl, alkenyl, alkynyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, heteroalkyl, cycloalkyl, heterocyclyl, or heterocyclylalkyl;
- R4, independently for each occurrence, is selected from substituted or unsubstituted alkyl, aryl, arylalkyl, heterocyclyl, oxo, —ORb, —CH2ORb, halo, hydroxyl, and hydroxyalkyl;
- Rb is substituted or unsubstituted alkyl, aryl, arylalkyl, or heterocyclyl;
- p is 0, 1, or 2;
- R6 is hydrogen or substituted or unsubstituted alkyl;
- R7, R8, and R9 are each independently hydrogen or alkyl;
- J is OH or —NRxRy;
- and
- Rx and Ry are each independently selected from H, optionally substituted alkyl, optionally substituted alkoxylalkyl, or Rx and Ry taken together with the intervening nitrogen atom form a ring.
8 more elements
144-174. (canceled)
A compound represented by Formula (X-am):
- or a pharmaceutically acceptable salt thereof;
- wherein:
- R1, R2, and R3 are each independently H or substituted or unsubstituted alkyl, alkoxy, haloalkyl, alkenyl, alkynyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, heteroalkyl, cycloalkyl, heterocyclyl, or heterocyclylalkyl;
- R4, independently for each occurrence, is selected from substituted or unsubstituted alkyl, aryl, arylalkyl, heterocyclyl, oxo, —ORb, —CH2ORb, halo, hydroxyl, and hydroxyalkyl;
- Rb is substituted or unsubstituted alkyl, aryl, arylalkyl, or heterocyclyl;
- p is 0, 1, or 2;
- R6 is hydrogen or substituted or unsubstituted alkyl;
- R7, R8, and R9 are each independently hydrogen or alkyl;
- J is OH or —NRxRy;
- and
- Rx and Ry are each independently selected from H, optionally substituted alkyl, optionally substituted alkoxylalkyl, or Rx and Ry taken together with the intervening nitrogen atom form a ring.
8 more elements
176-243. (canceled)
(canceled)
247-248. (canceled)
Dependencies are inferred from the claim text.