US2023374027A1PendingUtilityA1

PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF

86
Assignee: ABBVIE INCPriority: Oct 16, 2015Filed: Jul 28, 2023Published: Nov 23, 2023
Est. expiryOct 16, 2035(~9.2 yrs left)· nominal 20-yr term from priority
Inventors:Ayman AllianJayanthy JayanthMohamed-Eslam F. MohamedMathew M. MulhernFredrik Lars NordstromAhmed A. OthmanMichael J. RozemaLakshmi BhagavatulaPatrick J. MarroumPeter T. MayerAhmad Y. SheikhThomas B. BorchardtBen KlünderHeidi S. CampRobert J. PadleyJeffrey W. Voss
C07B 2200/13A61P 29/00A61P 37/00A61P 17/14A61P 17/06A61P 1/00A61P 19/02A61K 9/2013A61K 9/2054C07D 487/04A61K 47/12A61K 31/4985C07D 487/14A61K 9/0053A61K 47/38A61P 1/04A61P 17/00A61P 35/00A61P 37/02A61P 37/08A61P 43/00A61P 7/00A61K 47/02
86
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Claims

Abstract

The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.

Claims

exact text as granted — not AI-modified
1 - 116 . (canceled) 
     
     
         117 . A safe and effective method of treating a human patient suffering from an inflammatory disease, comprising once daily oral administration to the patient of 15 mg of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide (Compound 1), wherein the method safely achieves a clinically significant reduction in inflammation in the patient. 
     
     
         118 . The method of  claim 117 , wherein the inflammatory disease is selected from the group consisting of inflammatory bowel disease, rheumatoid arthritis, juvenile idiopathic arthritis, a spondyloarthropathy, a skin condition, and vasculitis. 
     
     
         119 . The method of  claim 117 , wherein the inflammatory disease has symptoms comprising skin inflammation, bowel inflammation, joint inflammation, or vascular inflammation. 
     
     
         120 . The method of  claim 117 , wherein the inflammatory disease has symptoms comprising skin inflammation. 
     
     
         121 . The method of  claim 120 , wherein the inflammatory disease is selected from the group consisting of atopic dermatitis, vitiligo, hidradenitis suppurativa, and alopecia areata. 
     
     
         122 . The method of  claim 117 , wherein the inflammatory disease has symptoms comprising bowel inflammation. 
     
     
         123 . The method of  claim 122 , wherein the inflammatory disease is selected from the group consisting of ulcerative colitis and Crohn's disease. 
     
     
         124 . The method of  claim 117 , wherein the inflammatory disease has symptoms comprising joint inflammation. 
     
     
         125 . The method of  claim 124 , wherein the inflammatory disease is selected from the group consisting of rheumatoid arthritis, juvenile idiopathic arthritis, a spondyloarthropathy, and systemic lupus erythematosus. 
     
     
         126 . The method of  claim 117 , wherein the inflammatory disease has symptoms comprising vascular inflammation. 
     
     
         127 . The method of  claim 126 , wherein the inflammatory disease is vasculitis. 
     
     
         128 . The method of  claim 117 , wherein the inflammatory disease is selected from the group consisting of rheumatoid arthritis, juvenile idiopathic arthritis, a spondyloarthopathy, vasculitis, systemic lupus erythematosus, atopic dermatitis, vitiligo, hidradenitis suppurativa, alopecia areata, ulcerative colitis and Crohn's disease. 
     
     
         129 . The method of  claim 117 , wherein the method results in a C-reactive protein (CRP) plasma concentration in the patient of less than the upper limit of normal (>5 mg/L). 
     
     
         130 . The method of  claim 117 , wherein the patient has had an inadequate response or intolerance to one or more systemic disease-modifying antirheumatic drugs (DMARDS). 
     
     
         131 . The method of  claim 130 , wherein the DMARD is an anti-TNF biologic. 
     
     
         132 . The method of  claim 117 , wherein the 15 mg of Compound 1 is administered to the patient as 15.4 mg of crystalline hemihydrate Freebase Hydrate Form C. 
     
     
         133 . A safe and effective method of treating a human patient suffering from an inflammatory disease, comprising once daily oral administration to the patient of 30 mg of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide (Compound 1), wherein the method safely achieves a clinically significant reduction in inflammation in the patient. 
     
     
         134 . The method of  claim 133 , wherein the inflammatory disease is selected from the group consisting of inflammatory bowel disease, rheumatoid arthritis, juvenile idiopathic arthritis, a spondyloarthropathy, a skin condition, and vasculitis. 
     
     
         135 . The method of  claim 133 , wherein the inflammatory disease has symptoms comprising skin inflammation, bowel inflammation, joint inflammation, or vascular inflammation. 
     
     
         136 . The method of  claim 133 , wherein the inflammatory disease has symptoms comprising skin inflammation. 
     
     
         137 . The method of  claim 136 , wherein the inflammatory disease is selected from the group consisting of atopic dermatitis, vitiligo, hidradenitis suppurativa, and alopecia areata. 
     
     
         138 . The method of  claim 133 , wherein the inflammatory disease has symptoms comprising bowel inflammation. 
     
     
         139 . The method of  claim 138 , wherein the inflammatory disease is selected from the group consisting of ulcerative colitis and Crohn's disease. 
     
     
         140 . The method of  claim 133 , wherein the inflammatory disease has symptoms comprising joint inflammation. 
     
     
         141 . The method of  claim 140 , wherein the inflammatory disease is selected from the group consisting of rheumatoid arthritis, juvenile idiopathic arthritis, a spondyloarthropathy, and systemic lupus erythematosus. 
     
     
         142 . The method of  claim 133 , wherein the inflammatory disease is selected from the group consisting of rheumatoid arthritis, juvenile idiopathic arthritis, a spondyloarthopathy, vasculitis, systemic lupus erythematosus, atopic dermatitis, vitiligo, hidradenitis suppurativa, alopecia areata, ulcerative colitis and Crohn's disease. 
     
     
         143 . The method of  claim 133 , wherein the method results in a C-reactive protein (CRP) plasma concentration in the patient of less than the upper limit of normal (>5 mg/L). 
     
     
         144 . The method of  claim 133 , wherein the patient has had an inadequate response or intolerance to one or more systemic disease-modifying antirheumatic drugs (DMARDS). 
     
     
         145 . The method of  claim 144 , wherein the DMARD is an anti-TNF biologic. 
     
     
         146 . The method of  claim 133 , wherein the 30 mg of Compound 1 is administered to the patient as 30.7 mg of crystalline hemihydrate Freebase Hydrate Form C.

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