Claims for Patent: 9,421,205

Summary for Patent: 9,421,205

Title:	FAK inhibitors
Abstract:	A compound of the formula (I): ##STR00001## where R.sup.1 or R.sup.2 is a cyclic amine group and R.sup.5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
Inventor(s):	Holmes; Ian Peter (Bundoora, AU), Bergman; Yiva (Parkville, AU), Lunnis; Gillian Elizabeth (Parkville, AU), Nikac; Marica (Parkville, AU), Choi; Neil (Parkville, AU), Hemley; Catherine Fae (Parkville, AU), Walker; Scott Raymond (Parkville, AU), Foitzik; Richard Charles (Parkville, AU), Ganame; Danny (Bundoora, AU), Lessene; Romina (Bundoora, AU)
Assignee:	Cancer Therapeutics CRC PTY LTD. (Bundoora, AU)
Application Number:	14/619,674
Patent Claims:	1. A method of treating breast cancer comprising administering a therapeutically-effective amount of a compound of formula (I) in combination with a VEGF receptor tyrosine kinase inhibitor or a therapeutic antibody against vascular endothelial growth factors, wherein the compound of the formula (I) is: ##STR00117## wherein: R.sup.1 is selected from: H and ##STR00118## wherein: R.sup.N1 is selected from H, C.sub.1-3 alkyl and C(.dbd.O)Me; R.sup.N2 is selected from H, C.sub.1-3 alkyl and C(.dbd.O)Me; R.sup.N3 is selected from H, C.sub.1-3 alkyl and C(.dbd.O)Me; R.sup.N4 is selected from H and CH.sub.3, R.sup.N7 and R.sup.N8 are independently selected from H and CH.sub.3; R.sup.N9 is selected from H, C.sub.1-3 alkyl and C(.dbd.O)Me; R.sup.N10 is selected from H, C.sub.1-3 alkyl and C(.dbd.O)Me; R.sup.N11 is selected from H, C.sub.1-3 alkyl and C(.dbd.O)Me; R.sup.2 is selected from H and ##STR00119## wherein: R.sup.N5 is selected from H, C.sub.1-3 alkyl and C(.dbd.O)Me; R.sup.N6 is selected from H, C.sub.1-3 alkyl and C(.dbd.O)Me; and wherein only one of R.sup.1 and R.sup.2 is H; or R.sup.1 and R.sup.2 together form the group --CH.sub.2--N(R.sup.N12)--C.sub.2H.sub.4--, where R.sup.N12 is selected from H, C.sub.1-3 alkyl and C(.dbd.O)Me; R.sup.4 is selected from CF.sub.3, halo, CF.sub.2H and CN; and R.sup.5 is selected from groups of the following formulae: ##STR00120## wherein: R.sup.6 is selected from H, (CHR.sup.C1).sub.n1C(O)N(R.sup.N13)Z.sup.1 and (CH.sub.2).sub.n2C(O)OZ.sup.2; wherein: n1 is 1; R.sup.C1 is H or Me; R.sup.N13 is H or CH.sub.3; Z.sup.1 is H, CH.sub.3 or OCH.sub.3; n2 is 1; and Z.sup.2 is CH.sub.3; and where only one of (R.sup.N13) and Z.sup.1 can be CH.sub.3, R.sup.7, if present, is selected from H, and (CH.sub.2).sub.m1C(O)N(R.sup.M1)Y.sup.1, wherein: m1 is 0 or 1; R.sup.M1 is H; and Y.sup.1 is H, Me or OCH.sub.3; and one of R.sup.6 and R.sup.7 is not H; and R.sup.8, if present, is H or, when R.sup.7 is C(.dbd.O)NH.sub.2, R.sup.8 is selected from H and C.sub.1-2 alkyl. 2. A method according to claim 1, wherein the compound of formula (I) is: ##STR00121## 3. A method according to claim 1, wherein the VEGF receptor tyrosine kinase inhibitor or a therapeutic antibody against vascular endothelial growth factors is bevacizumab. 4. A method according to claim 2, wherein the VEGF receptor tyrosine kinase inhibitor or a therapeutic antibody against vascular endothelial growth factors is bevacizumab.

Details for Patent 9,421,205

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	AVASTIN	bevacizumab	Injection	125085	02/26/2004		2031-02-17