PATENT CLAIM ANALYSIS

Application Number: 16120170
Application Type: Utility
Filing Date: 2018-08
Publication Date: 2019-01
Patent Classification: ["544", "324000"]

Abstract:
A compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in the treatment of autoimmune diseases and inflammatory conditions.

Claim (Index 32):
A method of treatment of autoimmune diseases and inflammatory conditions, wherein the method comprises administering a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof, to a patient in need of such treatment, wherein:\n R 1  represents \n (i) \n or\n (ii) a 6-membered heteroaryl substituted by one or more groups selected from Y 5 , or \n (iii) a 5- to 10-membered monocyclic or bicyclic heteroaryl connected to the pyrimidine ring of the compound of formula I via a carbon atom of the heteroaryl, which heteroaryl is optionally substituted by one or more groups selected from Y 5 , or \n R 2  represents hydrogen; and \n R 3  represents \u2014X-L-J, -C 1-12 alkyl optionally substituted by one or more Z 1  or heterocycloalkyl optionally substituted by one or more groups selected from Z 2 ; \n X represents -C 1-6 alkylene-, optionally substituted by one or more T 1 , or \u2014(C(R A ) 2 ) p \u2014C 2-5 heterocycloalkylene-(C(R A ) 2 ) q \u2014, where the heterocycloalkylene is optionally substituted by one or more T 2 ; \n L represents a single bond or -L 1 -L 2 -; \n L 1  represents \u2014N(R B )\u2014, \u2014O\u2014, \u2014S(O) m \u2014, \u2014C(O)N(R C )\u2014, \u2014N(R D )C(O)\u2014, \u2014S(O)\u2014N(R E )\u2014, \u2014N(R F )S(O) n \u2014 or \u2014N(R G )C(O)N(R H )\u2014; \n L 2  represents a single bond or -C 1-6 alkylene-; \n J represents \n (i) a 6- to 10-membered aryl optionally substituted by D 1  and optionally substituted by one or more groups selected from R X , or \n (ii) a 5- to 11-membered monocyclic or bicyclic heteroaryl ring, which heteroaryl contains 1 to 3 nitrogen atoms, and/or one oxygen atom and/or one or two sulfur atoms and which heteroaryl is optionally substituted by D 2  and optionally substituted by one or more groups selected from R Y ; \n Y 1  represents hydrogen, halogen, \u2014CN, R a , -A-C(Q)R b , -A-C(Q)N(R c )R d , -A-C(Q)OR e , -A-S(O) n R f , -A-S(NR g )(O)R h , -A-S(O) n N(R i )R j , -A-S(O) n OR k , \u2014B(OR l ) 2 , \u2014N 3 , \u2014NO 2 , \u2014OR\u2032 or \u2014SR n ; \n Y 2 , Y 3  and Y 4  each independently represents hydrogen, halogen, R a , -A-C(Q)R b , -A-C(Q)N(R c )R d , -A-C(Q)OR e , -A-S(O) n R f , -A-S(NR g )(O)R h , -A-S(O) n N(R i )R j , -A-S(O) n OR k , \u2014B(OR l ) 2 , \u2014N 3 , \u2014NO 2 , \u2014OH, \u2014OR m  or \u2014Sr n ; \n Y 5  represents halogen, R a , -A-C(Q)R b , -A-C(Q)N(R c )R d , -A-C(Q)OR e , -A-S(O) n R f , -A-S(NR g )(O)R h , -A-S(O) n N(R i )R j , -A-S(O) n OR k , \u2014B(OR l ) 2 , \u2014N 3 , \u2014NO 2 , \u2014OH, \u2014OR m  or \u2014SR n ; \n Q represents \u2550O, \u2550S, \u2550NR o , \u2550NN(R p )R q , \u2550N(OR r ), \u2550NS(O) 2 N(R s )R t  or \u2550C(H)NO 2 ; \n A represents a single bond, \u2014N(R I )\u2014, \u2014C(Q)N(R J )\u2014 or \u2014O\u2014; \n each R a , R f , R h  and R m  independently represents C 1-6  alkyl optionally substituted by one or more groups selected from W 1 , heterocycloalkyl optionally substituted by one or more groups selected from W 2  or aryl or heteroaryl both optionally substituted by one or more groups selected from W 3 , \n each R b , R c , R d , R e , R g , R i , R j , R k , R l , R o , R p , R q , R r , R s  and R t  independently represents hydrogen, C 1-6  alkyl optionally substituted by one or more groups selected from W 1 , heterocycloalkyl optionally substituted by one or more groups selected from W 2  or aryl or heteroaryl both optionally substituted by one or more groups selected from W 3 ; or \n any two R c  and R d , R i  and R j , R p  and R q  and/or R s  and R t  are linked together to form, along with the nitrogen atom to which they are attached, a 3- to 8-membered monocyclic or bicyclic ring, which ring optionally contains one or two further heteroatoms and which ring optionally is substituted by one or more groups selected from W 2 , C 1-3 alkyl optionally substituted by one or more groups selected from W 1 , and \u2550O; or \n two R 1  are linked together to form, along with the boron, and the oxygen atoms to which they are attached, a 5- to 8-membered heterocyclic ring, which ring optionally contains one or more further heteroatoms and which ring optionally is substituted by one or more groups independently selected from halogen, C 1-3 alkyl optionally substituted by one or more halogens, and \u2550O; \n W 1  represents halogen, \u2014CN, -A 1 -C(O)R b1 , -A 1 -C(O)N(R c1 )R d1 , -A 1 -C(O)OR e1 , -A 1 -S(O) n R f1 , -A 1 -S(O) n OR g1 , \u2014N(R h1 )R i1 , \u2014OR j1  or \u2550O; \n W 2  represents halogen, \u2014CN, R a1 , -A 1 -C(O)R b1 , -A 1 -C(O)N(R c1 )R d1 , -A 1 -C(O)OR e1 , -A 1 -S(O) n R f1 , -A 1 -S(O) n OR g1 , \u2014N(R h1 )R i1 , \u2014OR j1  or \u2550O; \n W 3  represents halogen, \u2014CN, R a1 , -A 1 -C(O)R b1 , -A 1 -C(O)N(R c1 )R d1 , -A 1 -C(O)OR e1 , -A 1 -S(O) n R f1 , -A 1 -S(O) n OR g1 ; \u2014OR j1 , -A 1 -S(NR k1 )(O)R l1 , -A 1 -S(O) n N(R m1 )R n1 , \u2014N 3 , \u2014NO 2 , \u2014SR o1  or \u2550O; \n A 1  represents a single bond, \u2014N(R K )\u2014 or \u2014O\u2014; \n each R a1 , R f1  and R l1  independently represents C 1-6  alkyl optionally substituted by one or more fluoro; \n each R b1 , R c1 , R d1 , R e1 , R g1 , R h1 , R i1 , R j1 , R k1 , R m1 , R n1 , and R o1  independently represents hydrogen or C 1-6  alkyl optionally substituted by one or more fluoro; or \n any two R c1  and R d1 , R h1  and R i1  and R m1  and R n1  are linked together to form, along with the nitrogen atom to which they are attached, a 3- to 6-membered ring, which ring optionally contains one further heteroatom and which ring optionally is substituted by one or more groups selected from fluoro, C 1-3 alkyl optionally substituted by one or more fluoro, and \u2550O; \n Z 1  represents halogen, \u2014CN, -A 2 -C(Q 1 )R b2 , -A 2 -C(Q 1 )N(R c2 )R d2 , -A 2 -C(Q 1 )OR e2 , -A 2 -S(O) n R f2 , -A 2 -S(O) n OR g2 , -A 2 -S(NR h2 )(O)R i2 , -A 2 -S(O) n N(R j2 )R k2 , \u2014N(R l2 )R m2 , \u2014OR n2 , \u2014SR o2  or heterocycloalkyl optionally substituted by one or more groups selected from W 5 ; \n Z 2  represents halogen, \u2014CN, R a2 , -A 2 -C(Q 1 )R b2 , -A 2 -C(Q 1 )N(R c2 )R d2 , -A 2 -C(Q 1 )OR e2 , -A 2 -S(O) n R f2 , -A 2 -S(O) n OR g2 , -A 2 -S(NR h2 )(O)R i2 , -A 2 -S(O) n N(R j2 )R k2 , \u2014N(R l2 )R m2 , \u2014OR n2  or =Q 1 ; \n Q 1  represents \u2550O, \u2550S, \u2550NR p2 , \u2550NN(R q2 )R r2 , \u2550N(OR s2 ), \u2550NS(O) 2 N(R t2 )R u2  or \u2550C(H)NO 2 ; \n A 2  represents a single bond, \u2014N(R L )\u2014, \u2014C(Q 1 )N(R M )\u2014 or \u2014O\u2014; \n each R a2 , R f2 , R i2 , R n2  and R o2  independently represents C 1-6 alkyl optionally substituted by one or more groups selected from W 4  or heterocycloalkyl optionally substituted by one or more groups selected from W 5 ; \n R m2  represents C 2-6 alkyl optionally substituted by one or more groups selected from W 4 ; \n each R b2 , R c2 , R d2 , R e2 , R g2 , R h2 , R j2 , R k2 , R l2 , R p2 , R q2 , R r2 , R s2 , R t2  and R u2  independently represents hydrogen, C 1-6 alkyl optionally substituted by one or more groups selected from W 4 , heterocycloalkyl optionally substituted by one or more groups selected from W 5 ; or \n any two R c2  and R d2 , R j2  and R k2 , R l2  and R m2 , R q2  and R r2  and/or R t2  and R u2  are linked together to form, along with the nitrogen atom to which they are attached, a 3- to 8-membered monocyclic or bicyclic ring, which ring optionally contains one or two further heteroatoms and which ring optionally is substituted by one or more groups selected from W 5 , C 1-3 alkyl optionally substituted by one or more groups selected from W 4 , and \u2550O; \n W 4  represents halogen, \u2014CN, -A 3 -C(O)R b3 , -A 3 -C(O)N(R c3 )R d3 , -A 3 -C(O)OR e3 , -A 3 -S(O) n R f3 , -A 3 -S(O) n OR g3 , \u2014OR h3 , \u2550O or W 6 ; \n W 5  represents halogen, \u2014CN, R a3 , -A 3 -C(O)R b3 , -A 3 -C(O)N(R c3 )R d3 , -A 3 -C(O)OR e3 , -A 3 -S(O) n R f3 , -A 3 -S(O) n OR g3 , \u2014OR h3 , \u2550O or W 6 ; \n W 6  represents phenyl or heteroaryl, both optionally substituted by one or more groups selected from halogen and R a3 ; \n A 3  represents a single bond, \u2014N(R L )\u2014 or \u2014O\u2014; \n each R a3  and R f3  independently represents C 1-6  alkyl optionally substituted by one or more fluoro; \n each R b3 , R c3 , R d3 , R e3 , R g3  and R h3  independently represents hydrogen or C 1-6 alkyl optionally substituted by one or more fluoro; or \n R c3  and R d3  are linked together to form, along with the nitrogen atom to which they are attached, a 3- to 6-membered ring, which ring optionally contains one further heteroatoms and which ring optionally is substituted by one or more groups selected from fluoro, C 1-3 alkyl optionally substituted by one or more fluoro, and \u2550O; \n D 1  and D 2  represent R a4 , -A 4 -C(Q 2 )R b4 , -A 4 -C(Q 2 )N(R c4 )R d4 , -A 4 -C(Q 2 )OR e4 , -A 4 -S(O) n R f4 , -A 4 -S(O) n C(O)R g4 , -A 4 -S(NR h4 )(O)R i4 , -A 4 -S(O) n N(R j4 )R k4 , -A 4 -S(O) n OR l4 , \u2014B(OR m4 ) 2 , \u2014N 3 , \u2014N(R n4 )R o4 , \u2014N(H)CN, \u2014NO 2 , \u2014ONO 2 , \u2014OR p4 , \u2014SR q4  or, when J is partly aromatic, =Q 2 ; \n Q 2  represents \u2550O, \u2550S, \u2550NR r4 , \u2550NN(R s4 )R t4 , \u2550N(OR u4 ), \u2550NS(O) 2 N(R v4 )R w4  or \u2550C(H)NO 2 ; \n A 4  represents a single bond, \u2014N(R M )\u2014, \u2014C(Q)N(R N )\u2014 or \u2014O\u2014; \n each R X  and R Y  independently represent halogen, \u2014CN, R a4 , \u2014N(R n4 )R o4 , \u2014NO 2 , \u2014OR p4  or \u2550O; \n R c4  represents hydrogen, R a4 , \u2014C(O)OR e4 , \u2014S(O) n R f4 , \u2014S(O) n N(R j4 )R k4 , \u2014N(R n4 )R o4  or \u2014OR p4 ; \n each R a4 , R f4  and R i4  independently represent C 1-6 alkyl optionally substituted by one or more groups selected from G 1 , heterocycloalkyl optionally substituted by one or more groups selected from G 2 , aryl optionally substituted by one or more groups selected from G 3  or heteroaryl optionally substituted by one or more groups selected from G 4 ; \n each R b4 , R d4 , R e4 , R g4 , R h4 , R j4 , R k4 , R l4 , R m4 , R n4 , R o4 , R p4 , R q4 , R r4 , R s4 , R t4 , R u4 , R v4  and R w4  independently represent hydrogen, C 1-6 alkyl optionally substituted by one or more groups selected from G 1 , heterocycloalkyl optionally substituted by one or more groups selected from G 2 , aryl optionally substituted by one or more groups selected from G 3  or heteroaryl optionally substituted by one or more groups selected from G 4 ; or \n any two R c4  and R d4 , R j4  and R k4 , R n4  and R o4 , R s4  and R t4  and/or R v4  and R w4  are linked together to form, along with the nitrogen atom to which they are attached, a 3- to 6-membered ring, which ring optionally contains one heteroatom and which ring optionally is substituted by one or more groups selected from fluoro, C 1-3 alkyl optionally substituted by one or more fluoro, and \u2550O; or \n two R m4  are linked together to form, along with the boron, and the oxygen atoms to which they are attached, a 5- to 8-membered heterocyclic ring, which ring optionally contains one or more further heteroatoms and which ring optionally is substituted by one or more groups independently selected from halogen, C 1-3 alkyl optionally substituted by one or more halogens, and \u2550O; \n each G 1  is independently selected from halogen, \u2014CN, \u2014N(R b5 )R c5 , \u2014N(H)C(O)R d5 , \u2014N(H)S(O) n R h5 , \u2014OR k5 , \u2014S(O) m R l2  or \u2550O; \n each G 2  is independently selected from halogen, R a5 , \u2014CN, \u2014N(R b5 )R c5 , \u2014N(H)C(O)R d5 , \u2014N(H)S(O) n R h5 , \u2014OR k5 , \u2014S(O) m R l2  or \u2550O; \n each G 3  and G 4  are independently selected from halogen, \u2014CN, R a5 , \u2014N(R b5 )R c5 , -A 5 -C(O)R d5 , -A 5 -C(O)N(R e5 )R f5 , -A 5 -C(O)OR g5 , -A 5 -S(O) n R h5 , -A 5 -S(O) n N(R i5 )R j5 , \u2014OR k5  or \u2550O; \n A 5  represents a single bond or \u2014N(H)\u2014; \n R a5  represents C 1-6  alkyl optionally substituted by one or more halogens; \n each R b5 , R c5 , R d5 , R e5 , R f5 , R g5 , R h5 , R i5 , R j5 , R k5  and R l5  independently represents hydrogen or C 1-6  alkyl optionally substituted by one or more halogens; or \n any two R b5  and R c5 , R e5  and R f5  and/or R i5  and R j5  are linked together to form, along with the nitrogen atom to which they are attached, a 3- to 6-membered ring, which ring optionally contains one further heteroatom and which ring optionally is substituted by one or more groups selected from halogen, C 1-3 alkyl optionally substituted by one or more halogens, and \u2550O; \n each R A , R B , R C , R D , R E , R F , R G , R H , R I , R J , R K , R L , R M  and R N  independently represents hydrogen or C 1-3  alkyl optionally substituted by one or more fluoro; \n T 1  represents halogen, \u2014CN, \u2014N(R b6 )R c6  or \u2014OR d6 ; \n T 2  represents halogen, \u2014CN, R a6 , \u2014OR d6  or \u2550O; \n each R a6  independently represents C 1-6 alkyl optionally substituted by one or more halogens; \n each R b6 , R c6  and R d6  independently represents hydrogen or C 1-6 alkyl optionally substituted by one or more halogens; or \n R b6  and R c6  are linked together to form, along with the nitrogen atom to which they are attached, a 3- to 6-membered ring; \n each p and q independently represents 0, 1 or 2, provided that the sum of p and q is 0, 1 or 2; \n each m independently represents 0, 1 or 2; \n each n independently represents 1 or 2; \n provided that when X represents \u2014CH 2 CH 2 \u2014, L represents L 1  represents \u2014N(H)\u2014 or \u2014N(Me)-, L 2  represents a single bond and J represents 4-pyrimidinyl, and said 4-pyrimidinyl is unsubstituted or substituted with \u2014CH 3 , \u2014NH 2  or \u2014N(H)CH 2 CH(CH 3 ) 2 , then R 1  does not represent phenyl, 3-chlorophenyl, 3,5-dichlorophenyl or 5-chloro-2-methoxyphenyl, and \n provided that formula I does not represent (S)\u2014N 4 -(1-(2,4-difluorophenyl)ethyl)-6-(pyrazolo[1,5-a]pyrimidin-3-yl)pyrimidine-2,4-diamine.

Metadata:
- Claim Count in Document: 5.0
- Percentile: 96.0
- Lexical Diversity: 1.08
- Patent Class: 544.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15447818', '14647400', '15899061', '15315461', '15315478']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8152093741264276
- 35 USC 102 Novelty (BERT): 0.5960434275391409
- Combined Prediction Score: 0.7932927794676989
- Mean Citation Score: 477.80761600000005
- Max Citation Score: 496.26343
- Similarity Product: 484.71099676911

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 1
- Label 101 Adjusted: 1

Dataset: test