PATENT CLAIM ANALYSIS

Application Number: 16157333
Application Type: Utility
Filing Date: 2018-10
Publication Date: 2019-03
Patent Classification: ["514", "232200"]

Abstract:
The present invention relates to a pharmaceutical combination which comprises (a) a phosphatidylinositol 3-kinase inhibitor or pharmaceutically acceptable salt thereof, and (b) at least one c-Met receptor tyrosine kinase inhibitor or pharmaceutically acceptable salt thereof, for simultaneous, separate or sequential administration for the treatment of a proliferative disease, particularly a c-Met dependent proliferative disease; a pharmaceutical composition comprising such combination; a method of treating a subject having a proliferative disease comprising administration of said combination to a subject in need thereof; use of such combination for the treatment of proliferative disease; and a commercial package comprising such combination.

Claim (Index 9):
A method of treating a proliferative disease which comprises administering to a subject in need thereof a pharmaceutical combination comprising (a) a phosphatidylinositol 3-kinase inhibitor selected from the group consisting of a compound of formula (I), wherein R 1  is naphthyl or phenyl wherein said phenyl is substituted by one or two substituents independently selected from the group consisting of Halogen; lower alkyl unsubstituted or substituted by halogen, cyano, imidazolyl or triazolyl; cycloalkyl; amino substituted by one or two substituents independently selected from the group consisting of lower alkyl, lower alkyl sulfonyl, lower alkoxy and lower alkoxy lower alkylamino; piperazinyl unsubstituted or substituted by one or two substituents independently selected from the group consisting of lower alkyl and lower alkyl sulfonyl; 2-oxo-pyrrolidinyl; lower alkoxy lower alkyl; imidazolyl; pyrazolyl; and triazolyl; R 2  is O or S; R 3  is lower alkyl; R 4  is pyridyl unsubstituted or substituted by halogen, cyano, lower alkyl lower alkoxy or piperazinyl unsubstituted or substituted by lower alkyl; pyrimidinyl unsubstituted or substituted by lower alkoxy; quinolinyl unsubstituted or substituted by halogen; quinoxalinyl; or phenyl substituted with alkoxy R 5  is hydrogen or halogen; n is 0 or 1; R 6  is oxido; with the proviso that if n=1, the N-atom bearing the radical R 6  has a positive charge; R 7  is hydrogen or amino; or a compound of formula (II), wherein W is CR w  or N, wherein\n R w  is selected from the group consisting of:\n (1) hydrogen, \n (2) cyano, \n (3) halogen, \n (4) methyl, \n 5) trifluoromethyl, \n (6) sulfonamide; \n \n R 1  is selected from the group consisting of:\n (1) hydrogen, \n (2) cyano, \n (3) nitro, \n (4) halogen, \n (5) substituted and unsubstituted alkyl, \n (6) substituted and unsubstituted alkenyl, \n (7) substituted and unsubstituted alkynyl, \n (8) substituted and unsubstituted aryl, \n (9) substituted and unsubstituted heteroaryl, \n (10) substituted and unsubstituted heterocyclyl, \n (11) substituted and unsubstituted cycloalkyl, \n (12) \u2014COR 1a , \n (13) \u2014CO 2 R 1a , \n (14) \u2014CONR 1a R 1b , \n (15) \u2014NR 1a R 1b , \n (16) \u2014NR 1a COR 1b , \n (17) \u2014NR 1a SO 2 R 1b , \n (18) \u2014OCOR 1a , \n (19) \u2014OR 1a , \n (20) \u2014SR 1a , \n (21) \u2014SOR 1a , \n (23) \u2014SO 2 NR 1a R 1b  wherein \n \n R 1a , and R 1b  are independently selected from the group consisting of:\n (a) hydrogen, \n (b) substituted or unsubstituted alkyl, \n (c) substituted and unsubstituted aryl, \n (d) substituted and unsubstituted heteroaryl, \n (e) substituted and unsubstituted heterocyclyl, and \n (f) substituted and unsubstituted cycloalkyl; \n \n R 2  is selected from the group consisting of:\n (1) hydrogen, \n (2) cyano, \n (3) nitro, \n (4) halogen, \n (5) hydroxy, \n (6) amino, \n (7) substituted and unsubstituted alkyl, \n (8) \u2014COR 2a , and \n (9) \u2014NR 2a COR 2b , wherein \n \n R 2a , and R 2b  are independently selected from the group consisting of:\n (a) hydrogen, and \n (b) substituted or unsubstituted alkyl; \n \n R 3  is selected from the group consisting of:\n (1) hydrogen, \n (2) cyano, \n (3) nitro, \n (4) halogen, \n (5) substituted and unsubstituted alkyl, \n (6) substituted and unsubstituted alkenyl, \n (7) substituted and unsubstituted alkenyl, \n (8) substituted and unsubstituted aryl, \n (9) substituted and unsubstituted heteroaryl, \n (10) substituted and unsubstituted heterocyclyl, \n (11) substituted and unsubstituted cycloalkyl, \n (12) \u2014COR 3a , \n (14) \u2014NR 3a R 3b  \n (13) \u2014NR 3a COR 3b , \n (15) \u2014NR 3a SO 2 R 3b , \n (16) \u2014OR 3a , \n (17) \u2014SR 3a , \n (18) \u2014SOR 3a , \n (19) \u2014SO 2 R 3a , wherein \n \n R 3a , and R 3b  are independently selected from the group consisting of:\n (a) hydrogen, \n (b) substituted or unsubstituted alkyl, \n (c) substituted and unsubstituted aryl, \n (d) substituted and unsubstituted heteroaryl, \n (e) substituted and unsubstituted heterocyclyl, and \n (f) substituted and unsubstituted cycloalkyl; and \n \n R 4  is selected from the group consisting of\n (1) hydrogen, and \n (2) halogen, \n \n and a compound of formula (III) wherein A represents a heteroaryl selected from the group consisting of: R 1  represents one of the following substituents: (1) unsubstituted or substituted, preferably substituted C 1 -C 7 -alkyl, wherein said substituents are independently selected from one or more, preferably one to nine of the following moieties: deuterium, fluoro, or one to two of the following moieties C 3 -C 5 -cycloalkyl; (2) optionally substituted C 3 -C 5 -cycloalkyl wherein said substituents are independently selected from one or more, preferably one to four of the following moieties: deuterium, C 1 -C 4 -alkyl (preferably methyl), fluoro, cyano, aminocarbonyl; (3) optionally substituted phenyl wherein said substituents are independently selected from one or more preferably one to two of the following moieties: deuterium, halo, cyano, C 1 -C 7 -alkyl, C 1 -C 7 -alkylamino, di(C 1 -C 7 -alkyl)amino, C 1 -C 7 -alkylaminocarbonyl, di(C 1 -C 7 -alkyl)aminocarbonyl, C 1 -C 7 -alkoxy; (4) optionally mono- or di-substituted amine; wherein said substituents are independently selected from the following moieties: deuterium, C 1 -C 7 -alkyl (which is unsubstituted or substituted by one or more substituents selected from the group of deuterium, fluoro, chloro, hydroxy), phenylsulfonyl (which is unsubstituted or substituted by one or more, preferably one, C 1 -C 7 -alkyl, C 1 -C 7 -alkoxy, di(C 1 -C 7 -alkylamino-C 1 -C 7 -alkoxy); (5) substituted sulfonyl; wherein said substituent is selected from the following moieties: C 1 -C 7 -alkyl (which is unsubstituted or substituted by one or more substituents selected from the group of deuterium, fluoro), pyrrolidino, (which is unsubstituted or substituted by one or more substituents selected from the group of deuterium, hydroxy, oxo; particularly one oxo); (6) fluoro, chloro; R 2  represents hydrogen; R 3  represents (1) hydrogen, (2) fluoro, chloro, (3) optionally substituted methyl, wherein said substituents are independently selected from one or more, preferably one to three of the following moieties: deuterium, fluoro, chloro, dimethylamino, or a pharmaceutically acceptable salt thereof, and (b) at least one c-Met receptor tyrosine kinase inhibitor or pharmaceutically acceptable salt thereof, in a quantity which is jointly therapeutically effective against said proliferative disease.

Metadata:
- Claim Count in Document: 39.0
- Percentile: 97.0
- Lexical Diversity: 1.94737
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['12072269', '15328661', '16134162', '15535405', '13471111']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.783917875966514
- 35 USC 102 Novelty (BERT): 0.53524825230137
- Combined Prediction Score: 0.7590509135999997
- Mean Citation Score: 347.658454
- Max Citation Score: 371.75415
- Similarity Product: 246.32081381487248

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 0
- Claim Label 112: 1
- Combined Label: 1
- Label 101 Adjusted: 1

Dataset: test