Claims for Patent: 12,077,533
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Summary for Patent: 12,077,533
| Title: | Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides |
| Abstract: | The present invention provides a method for treating alopecia using certain pharmaceutically active pyrrolo[2,3-d]pyrimidinyl acrylamides having the structure: or a pharmaceutically acceptable salt thereof, as set forth in the Description. |
| Inventor(s): | Atli Thorarensen, Matthew Frank Brown, Agustin Casimiro-Garcia, Ye CHE, Jotham Wadsworth Coe, Mark Edward Flanagan, Adam Matthew Gilbert, Matthew Merrill Hayward, Jonathan David Langille, Justin Ian Montgomery, Jean-Baptiste Telliez, Rayomand Jal Unwalla, John I Trujillo |
| Assignee: | Pfizer Corp SRL |
| Application Number: | US17/393,463 |
| Patent Claims: |
1. A method for treating alopecia by administering to a mammal in need a therapeutically effective amount of a compound having the structure: or a pharmaceutically acceptable salt or solvate thereof, or an enantiomer or diastereomer thereof, and wherein R2 is selected from the group consisting of hydrogen, deuterium, C1-C6 linear or branched chain alkyl, C3-C6 cycloalkyl, C6-C10 aryl, monocyclic or bicyclic heteroaryl, comprising 5- and/or 6-membered rings, (aryl)C1-C6 linear or branched chain alkyl, (heteroaryl)C1-C6 linear or branched chain alkyl, (heterocyclic)C1-C6 linear or branched chain alkyl, (C1-C6 linear or branched chain alkyl)aryl, (C1-C6 linear or branched chain alkyl)heteroaryl, (C1-C6 linear or branched chain alkyl)heterocyclic, C1-C6 linear or branched chain perfluoroalkyl, C1-C6 linear or branched chain alkoxy, C1-C6 linear or branched chain perfluoroalkoxy, halogen, cyano, hydroxyl, amino, carboxy, aminocarbonyl, (C1-C6 linear or branched chain alkyl)aminocarbonylamino, (C1-C6 linear or branched chain alkyl)aminocarbonyl, —SOR12, —SO2R12, —NR13SO2R12, —SO2NR13R14, and —NR13SO2NR14R15; where said alkyl, aryl and heteroaryl is independently optionally substituted with one or more substituents selected from the group consisting of halo, hydroxy, methoxy, amino, cyano, alkylamino, dialkylamino, CF3, aminocarbonyl, (C1-C6 linear or branched chain alkyl)aminocarbonyl, and C3-C6 cycloalkyl; R3 is selected from the group consisting of hydrogen, deuterium, C1-C6 linear or branched chain alkyl, C1-C6 linear or branched chain perfluoroalkyl, halogen, and cyano; Ra, Rb, Rc and Rd are independently selected from hydrogen, C1-C6 linear or branched chain alkyl, C1-C6 linear or branched chain perfluoroalkyl, aryl, alkylaryl, (aryl)C1-C6 linear or branched chain alkyl, (heteroaryl)C1-C6 linear or branched chain alkyl, heteroaryl, halogen, cyano, hydroxyl, C1-C6 linear or branched chain alkoxy, amino, carboxy, aminocarbonyl, (heterocyclic)C1-C6 linear or branched chain alkyl, (C1-C6 linear or branched chain alkyl)aryl, (C1-C6 linear or branched chain alkyl)heteroaryl, and (C1-C6 linear or branched chain alkyl)heterocyclic, where said alkyl is further optionally substituted with one or more substituents selected from the group consisting of halo, hydroxy, methoxy, amino, alkylamino, dialkylamino, CF3, and C3-C6 cycloalkyl; R0, R1, R4, R6, R8, R9 and R10 are independently selected from hydrogen, C1-C6 linear or branched chain alkyl, C1-C6 linear or branched chain perfluoroalkyl, C6-C10 aryl, monocyclic or bicyclic heteroaryl, comprising 5- and/or 6-membered rings, (aryl)C1-C6 linear or branched chain alkyl, (heteroaryl)C1-C6 linear or branched chain alkyl, heteroaryl, halogen, cyano, hydroxyl, C1-C6 linear or branched chain alkoxy, amino, carboxy, aminocarbonyl, (heterocyclic)C1-C6 linear or branched chain alkyl, (C1-C6 linear or branched chain alkyl)aryl, (C1-C6 linear or branched chain alkyl)heteroaryl, and (C1-C6 linear or branched chain alkyl)heterocyclic, where said alkyl is further optionally substituted with one or more substituents selected from the group consisting of halo, hydroxy, methoxy, amino, alkylamino, dialkylamino, CF3, and C3-C6 cycloalkyl; where, alternatively, R0 or R1, and/or R6, respectively together with either of R4, Ra, Rb, Rc or Rd, may independently form a bond or a C1-C6 linear alkyl chain; and/or, alternatively, R4, respectively together with either of Ra, Rb, Rc or Rd, may independently form a bond or a C1-C6 linear alkyl chain; and/or, alternatively, R8 and R9 may together form a 3-6-membered ring optionally containing one or two O or N atoms; R11 is hydrogen or deuterium; and, R12, R13, R14 and R15 are independently selected from hydrogen, C1-C6 linear or branched chain alkyl, C1-C6 linear or branched chain perfluoroalkyl, C6-C10 aryl, alkylaryl, and (aryl)C1-C6 linear or branched chain alkyl. 2. A method for treating alopecia by administering to a mammal in need a therapeutically effective amount of the compound 1-((2S,5R)-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-2-methylpiperidin-1-yl)prop-2-en-1-one, or a pharmaceutically acceptable salt thereof. |
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