Claims for Patent: 9,782,406

Summary for Patent: 9,782,406

Title:	Kinase inhibitor and method for treatment of related diseases
Abstract:	Disclosed is a compound of (aminophenylamino) pyrimidyl benzamides and a synthesis method thereof. The compound has Btk-inhibition activity and can be used to treat autoimmune diseases, heteroimmune diseases, cancers or thromboembolic diseases.
Inventor(s):	Pan; Zhengying (Shenzhen, CN), Li; Xitao (Shenzhen, CN)
Assignee:	Peking University Shenzhen Graduate School (Shenzhen, CN) Beijing Reciprocapharmaceuticals Co., Ltd. (Beijing, CN)
Application Number:	14/830,128
Patent Claims:	1. A method for treating diffuse large B cell lymphoma, chronic lymphocytic leukemia, mantle cell lymphoma, follicular lymphoma, graft versus host disease, comprising administering to a subject in need thereof an effective amount of a compound of formula (I) ##STR00064## or a pharmaceutically acceptable salt thereof, wherein: W is selected from H, C.sub.1-6 alkyl, --(NH--CO).sub.n-L-L.sub.3, --(CO--NH).sub.n-L-L.sub.3, and --(NH--CO).sub.n--NH-L-L.sub.3; wherein: L is a bond, C.sub.1-3 alkylene or C.sub.2-3 alkenylene; L.sub.3 is C.sub.3-8 cycloalkyl, aryl or heteroaryl, each optionally substituted with 1, 2 or 3 substituents selected from the group consisting of halogen, amino, C.sub.1-6 alkyl, C.sub.1-6 alkoxyl, halo-C.sub.1-6 alkyl; n is an integer of 0 or 1; X is selected from H, halogen, and C.sub.1-6 alkyl; R.sub.1 and R.sub.2, same or different from each other, are each independently selected from H, C(O) and S(O).sub.2; L.sub.1 and L.sub.2, same or different from each other, are each independently selected from C.sub.2-3 alkenyl optionally substituted with C.sub.1-3 alkyl, and C.sub.1-3 alkyl-NHC(O)--C.sub.2-3 alkenyl; with the provisos that when R.sub.1 is H, L.sub.1 is not present; and when R.sub.2 is H, L.sub.2 is not present. 2. The method of claim 1, wherein W is selected from H, ethyl, --(NH--CO).sub.n-L-L.sub.3, --(CO--NH).sub.n-L-L.sub.3, and --(NH--CO).sub.n--NH-L-L.sub.3, wherein: L is a bond or vinylene; L.sub.3 is cyclopropyl, phenyl, naphthyl, isoxazolyl or benzo-[d][1,3]-dioxole group optionally substituted with 1 or 2 substituents selected from F, Cl, amino, methoxyl and CF.sub.3; n is an integer of 1. 3. The method of claim 1, wherein X is selected from H, F, Cl, and methyl. 4. The method of claim 1, wherein R.sub.1 and R.sub.2, same or different from each other, are each independently selected from H, C(O) and S(O).sub.2; L.sub.1 and L.sub.2, same or different from each other, are each independently selected form C.sub.2-3 alkenyl, and methyl-NHC(O)-ethenyl; with the provisos that when R.sub.1 is H, L.sub.1 is not present; and when R.sub.2 is H, L.sub.2 is not present. 5. The method of claim 1, wherein W is selected from H, ethyl, --(NH--CO).sub.n-L-L.sub.3, --(CO--NH).sub.n-L-L.sub.3, and --(NH--CO).sub.n--NH-L-L.sub.3, wherein: L is a bond or vinylene; L.sub.3 is cyclopropyl, phenyl, naphthyl, isoxazolyl or benzo-[d][1,3]-dioxole group optionally substituted with 1 or 2 substituents selected from F, Cl, amino, methoxyl and CF.sub.3; n is an integer of 1; X is selected from H, F, Cl, and methyl; R.sub.1 and R.sub.2, same or different from each other, are each independently selected from H, C(O) and S(O).sub.2; L.sub.1 and L.sub.2, same or different from each other, are each independently selected form C.sub.2-3 alkenyl, and methyl-NHC(O)-ethenyl; with the provisos that when R.sub.1 is H, L.sub.1 is not present; and when R.sub.2 is H, L.sub.2 is not present. 6. The method of claim 1, wherein the compound is selected from: ##STR00065## ##STR00066## ##STR00067## ##STR00068## ##STR00069## ##STR00070## ##STR00071## ##STR00072## ##STR00073## ##STR00074## 7. The method of claim 1, wherein the subject is a human. 8. The method of claim 1, wherein the compound is administered in combination with one or more therapeutic agents. 9. The method of claim 8, wherein the therapeutic agent modulates a protein kinase, targets an anti-cancer therapeutic target, induces or boosts immune response against cancer, or is a chemotherapeutic agent. 10. The method of claim 9, wherein the therapeutic agent is selected from the group consisting of a PI3K inhibitor, a CDK inhibitor, an anti-CD20 antibody, a BCL-2 inhibitor, a CTLA-4 derivative, a PD-1 antibody, a PD-L1 antibody, and an alkylating agent. 11. The method of claim 10, wherein the PI3K inhibitor is idelalisib, the CDK inhibitor is palbociclib or abemaciclib, the anti-CD20 antibody is rituximab, obinutuzumab or ofatumumab, the BCL-2 inhibitor is venetoclax, the CTLA-4 derivative is abatacept or belatacept, the PD-1 antibody is nivolumab, the PD-L1 antibody is pembrolizumab, and the alkylating agent is bendamustine.

Details for Patent 9,782,406

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	RITUXAN	rituximab	Injection	103705	11/26/1997		2031-10-25
Idec Pharmaceuticals Corp.	RITUXAN	rituximab	Injection	103737	02/19/2002		2031-10-25
Bristol-myers Squibb Company	ORENCIA	abatacept	For Injection	125118	12/23/2005		2031-10-25
Bristol-myers Squibb Company	ORENCIA	abatacept	Injection	125118	07/29/2011		2031-10-25