PATENT CLAIM ANALYSIS

Application Number: 15900405
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-12
Patent Classification: ["514", "303000"]

Abstract:
Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Claim (Index 28):
A method of assaying a compound for CCR1 antagonistic activity, said method comprising\n (a) contacting the compound with cells expressing CCR1 and a radioactive CCR1 ligand to form a reaction mixture; (b) aspirating the reaction mixture onto a GF/B glass filter pre-soaked in a polyethyleneimine solution; (c) measuring the amount radioactivity remaining on the GF/B glass filter,\n wherein said method comprises performing steps (a)-(c) with a positive control sample having a formula represented by the structure \n wherein\n the subscript n is an integer of from 0 to 3; \n each R 1a  and R b  is a member independently selected from the group consisting of H, C 1-8  alkyl, C 1-8  haloalkyl, C 3-6  cycloalkyl, \u2014COR a , \u2014CO 2 R a , \u2014CONR a R b , \u2014NR a R b , \u2014NR a COR b , \u2014OR a , \u2014X 1 COR a , \u2014X 1 CO 2 R a , \u2014X 1 CONR a R b , \u2014X 1 NR a COR b , \u2014X 1 NR a R b , and \u2014X 1 OR a , wherein X 1  is a member selected from the group consisting of C 1-4  alkylene, and each R a  and R b  is independently selected from the group consisting of hydrogen, C 1-8  alkyl, C 1-8  haloalkyl, and C 3-6  cycloalkyl, and optionally two R 1a  groups on adjacent carbon atoms are joined to form a 5-, 6- or 7-membered carbocyclic or heterocyclic ring; \n each of R 2a  and R 2b  is a member independently selected from the group consisting of H, hydroxyl, C 1-8  alkyl, C 1-8  haloalkyl, C 1-8  alkoxy, C 1-4  alkoxy-C 1-4  alkyl, C 1-8  hydroxyalkyl, C 1-4  alkoxy-C 1-4  alkoxy, C 3-6  cycloalkyl, C 3-6  cycloalkyl-C 1-4  alkyl, 3- to 7-membered heterocycloalkyl, 3- to 7-membered heterocycloalkyl-C 1-4  alkyl, \u2014X 1 CO 2 R a , \u2014X 1 CONR a R b , \u2014X 1 NR a COR b , \u2014X 1 NR a R b , wherein X 1 , R a  and R b  are defined above; \n Ar 1  is a member selected from the group consisting of phenyl, naphtyl and pyridyl, each of which is substituted with from one to five substituents, R 3 , R 3a , R 3b , R 4  and R 4a  which are independently selected from the group consisting of H, halogen, \u2014OR c , \u2014OC(O)R c , \u2014NR c R d , \u2014SR c , \u2014R c , \u2014CN, \u2014NO 2 , \u2014CO 2 R c , \u2014CONR c R d , \u2014C(O)R c , \u2014OC(O)NR c R d , \u2014NR d C(O)R c , \u2014NR d C(O) 2 R, \u2014NR c \u2014C(O)NR c R d , \u2014NH\u2014C(NH 2 )\u2550NH, \u2014NR e C(NH 2 )\u2550NH, \u2014NH\u2014C(NH 2 )\u2550NR e , \u2014NH\u2014C(NHR e )\u2550NH, \u2014S(O)R, \u2014S(O) 2 R e , \u2014NR c S(O) 2 R e , \u2014S(O) 2 NR c R d , \u2014N 3 , \u2014X 2 OR c , \u2014O\u2014X 2 OR c , \u2014X 2 OC(O)R c , \u2014X 2 NR c R d , \u2014O\u2014X 2 NR c R d , \u2014X 2 SR c , \u2014X 2 CN, \u2014X 2 NO 2 , \u2014X 2 CO 2 R c , \u2014O\u2014X 2 CO 2 R c , \u2014X 2 CONR c R d , \u2014O\u2014X 2 CONR c R d , \u2014X 2 C(O)R c , \u2014X 2 OC(O)NR c R d , \u2014X 2 NR d C(O)R c , \u2014X 2 NR d C(O) 2 R e , \u2014X 2 NR c C(O)NR c R d , \u2014X 2 NH\u2014C(NH 2 )\u2550NH, \u2014X 2 NR e C(NH 2 )\u2550NH, \u2014X 2 NH\u2014C(NH 2 )\u2550NR e , \u2014X 2 NH\u2014C(NHR e )\u2550NH, \u2014X 2 S(O)R, \u2014X 2 S(O) 2 R, \u2014X 2 NR c S(O) 2 R e , \u2014X 2 S(O) 2 NR c R d , \u2014X 2 N 3 , \u2014NR d \u2014X 2 OR, \u2014NR d \u2014X 2 NR c R d , \u2014NR d \u2014X 2 CO 2 R c , and \u2014NR d \u2014X 2 CONR c R d , wherein each X 2  is a member independently selected from the group consisting of C 1-4  alkylene, and each R c  and R d  is independently selected from hydrogen, C 1-8  alkyl, C 1-8  hydroxyalkyl, C 1-8  haloalkyl and C 3-6  cycloalkyl, or optionally R and R d  when attached to the same nitrogen atom can be combined with the nitrogen atom to form a five or six-membered ring having from 0 to 2 additional heteroatoms as ring members; and each R is independently selected from the group consisting of C 1-8  is alkyl, C 1-8  hydroxyalkyl, C 1-8  haloalkyl and C 3-6  cycloalkyl; \n Ar 2  is a member selected from the group consisting of a six- or ten-membered monocyclic or fused bicyclic aryl ring, and a five- to ten-membered monocyclic or fused bicyclic heteroaryl ring; each of which is substituted with from one to five substituents, R 5 , R 6 , R 7 , R 8  and R 9 , independently selected from the group consisting of H, halogen, \u2014OR f , \u2014OC(O)R f , \u2014NR f R g , \u2014SR, \u2014R h , \u2014CN, \u2014NO 2 , \u2014CO 2 R f , \u2014CONR f R g , \u2014C(O)R f , \u2014OC(O)NR f R g , \u2014NR g C(O)R f , \u2014NR g C(O) 2 R h , \u2014NR f \u2014C(O)NR f R g , \u2014NH\u2014C(NH 2 )\u2550NH, \u2014NR h C(NH 2 )\u2550NH, \u2014NH\u2014C(NH 2 )\u2550NR h , \u2014NH\u2014C(NHR h )\u2550NH, \u2014S(O)R h , \u2014S(O) 2 R h , \u2014NR f S(O) 2 R h , \u2014S(O) 2 NR f R g , \u2014NR f S(O) 2 NR f R g , \u2014N 3 , \u2014X 3 OR, \u2014X 3 OC(O)R f , \u2014X 3 NR f R g , \u2014X 3 SR f , \u2014X 3 CN, \u2014X 3 NO 2 , \u2014X 3 CO 2 R, \u2014X 3 CONR f R g , \u2014X 3 C(O)R f , \u2014X 3 OC(O)NR f R g , \u2014X 3 NR g C(O)R f , \u2014X 3 NR g C(O) 2 R h , \u2014X 3 NR f \u2014C(O)NR f R g , \u2014X 3 NH\u2014C(NH 2 )\u2550NH, \u2014X 3 NR h C(NH 2 )\u2550NH, \u2014X 3 NH\u2014C(NH 2 )\u2550NR h , \u2014X 3 NH\u2014C(NHR h )\u2550NH, \u2014X 3 S(O)R h , \u2014X 3 S(O) 2 R h , \u2014X 3 NR f S(O) 2 R h , \u2014X 3 S(O) 2 NR f R g , \u2014Y, \u2014X 3 Y, \u2014S(O) 2 Y, \u2014C(O)Y, \u2014X 3 N 3 , \u2014O\u2014X 3 OR f , \u2014O\u2014X 3 NR f R g , \u2014O\u2014X 3 CO 2 R, \u2014O\u2014X 3 CONR f R g , \u2014NR g \u2014X 3 OR f , \u2014NR g \u2014X 3 NR f R g , \u2014NR g \u2014X 3 CO 2 R f , and \u2014NR 9 \u2014X 3 CONR f R g , wherein Y is a five or six-membered aryl, heteroaryl or heterocyclic ring, optionally substituted with from one to three substitutents selected from the group consisting of halogen, \u2014OR f , \u2014OC(O)R, \u2014NR f R g , \u2014R h , \u2014SR f , \u2014CN, \u2014NO 2 , \u2014CO 2 R f , \u2014CONR f R g , \u2014C(O)R f , \u2014NR g C(O)R f , \u2014NR g C(O) 2 R h , \u2014S(O)R h , \u2014S(O) 2 R h , \u2014NR f S(O) 2 R h , \u2014S(O) 2 NR f R g , \u2014X 3 OR f , \u2014X 3 SR f , \u2014X 3 CN, \u2014X 3 NO 2 , \u2014X 3 CO 2 R f , \u2014X 3 CONR f R g , \u2014X 3 C(O)R f , \u2014X 3 OC(O)NR f R g , \u2014X 3 NR g C(O)R f , \u2014X 3 NR g C(O) 2 R h , \u2014X 3 NR f \u2014C(O)NR f R g , \u2014X 3 OC(O)R f , \u2014X 3 S(O)R h , \u2014X 3 S(O) 2 R h , \u2014X 3 NR f R g , \u2014X 3 NR f S(O) 2 R h , \u2014X 3 S(O) 2 NR f R g , \u2014O\u2014X 3 OR f , \u2014O\u2014X 3 NR f R g , \u2014O\u2014X 3 CO 2 R, \u2014O\u2014X 3 CONR f R g , \u2014NR g \u2014X 3 OR f , \u2014NR g \u2014X 3 NR f R g , \u2014NR g \u2014X 3 CO 2 R f , and \u2014NR g \u2014X 3 CONR f R g  and wherein each X 3  is independently selected from the group consisting of C 1-4  alkylene, and each R f  and R g  is independently selected from hydrogen, C 1-8  alkyl, C 1-8  hydroxyalkyl, C 1-8  haloalkyl and C 3-6  cycloalkyl, or when attached to the same nitrogen atom can be combined with the nitrogen atom to form a five or six-membered ring having from 0 to 2 additional heteroatoms as ring members, and each R h  is independently selected from the group consisting of C 1-8  alkyl, C 2-8  alkenyl, C 2-8  alkynyl, C 1-8  hydroxyalkyl, C 1-8  haloalkyl and C 3-6  cycloalkyl;\n or when two of R 5 , R 6 , R 7 , R 8  and R 9 , are attached to adjacent ring vertices of Ar 2 , are optionally combined to form a five or six membered ring having zero, one or two heteroatoms selected from O and N as ring members; \n or a pharmaceutically acceptable salt, or rotamer thereof.

Metadata:
- Claim Count in Document: 71.0
- Percentile: 88.0
- Lexical Diversity: 1.44737
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14011174', '11491540', '10460752', '10732897', '11694935']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8147848058067959
- 35 USC 102 Novelty (BERT): 0.5449358190174688
- Combined Prediction Score: 0.7877999071278633
- Mean Citation Score: 355.22914799999984
- Max Citation Score: 430.1475
- Similarity Product: 264.741006821394

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