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Last Updated: September 22, 2020

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Claims for Patent: 9,782,406

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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.

Summary for Patent:   Start Trial

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
China2011 1 0327240Oct 25, 2011

Details for Patent 9,782,406

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Genentech RITUXAN rituximab SOLUTION;INTRAVENOUS 103705 001 1997-11-26   Start Trial Peking University Shenzhen Graduate School (Shenzhen, CN) Beijing Reciprocapharmaceuticals Co., Ltd. (Beijing, CN) 2031-10-25 RX search
Genentech RITUXAN rituximab SOLUTION;INTRAVENOUS 103705 002 1997-11-26   Start Trial Peking University Shenzhen Graduate School (Shenzhen, CN) Beijing Reciprocapharmaceuticals Co., Ltd. (Beijing, CN) 2031-10-25 RX search
Bristol Myers Squibb ORENCIA abatacept INJECTABLE; IV (INFUSION) 125118 001 2005-12-23   Start Trial Peking University Shenzhen Graduate School (Shenzhen, CN) Beijing Reciprocapharmaceuticals Co., Ltd. (Beijing, CN) 2031-10-25 RX search
Bristol Myers Squibb NULOJIX belatacept INJECTABLE; INJECTION 125288 001 2011-06-15   Start Trial Peking University Shenzhen Graduate School (Shenzhen, CN) Beijing Reciprocapharmaceuticals Co., Ltd. (Beijing, CN) 2031-10-25 RX search
Novartis ARZERRA ofatumumab INJECTABLE; INJECTION 125326 001 2009-10-26   Start Trial Peking University Shenzhen Graduate School (Shenzhen, CN) Beijing Reciprocapharmaceuticals Co., Ltd. (Beijing, CN) 2031-10-25 RX search
Novartis KESIMPTA ofatumumab SOLUTION;SUBCUTANEOUS 125326 002 2009-10-26   Start Trial Peking University Shenzhen Graduate School (Shenzhen, CN) Beijing Reciprocapharmaceuticals Co., Ltd. (Beijing, CN) 2031-10-25 RX search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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