Claims for Patent: 7,456,190

Summary for Patent: 7,456,190

Title:	Compositions useful as protein kinase inhibitors
Abstract:	The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Inventor(s):	Maltais; Francois (Tewksbury, MA), Aronov; Alex (Watertown, MA), Hale; Michael R. (Bedford, MA), Moon; Young-Choon (Belle Meade, NJ)
Assignee:	Vertex Pharmaceuticals Incorporated (Cambridge, MA)
Application Number:	10/798,766
Patent Claims:	1. A compound of formula I: ##STR00082## or a pharmaceutically acceptable salt thereof, wherein: R.sup.z is hydrogen R; each R.sup.y is an optionally substituted C.sub.1-4 aliphatic group Z.sup.1 is N; Z.sup.2 is CH; T.sub.(m)R.sup.1 is hydrogen; U is NH; Q is --C(O)N(R)-- or --C(O)O--; R.sup.2 is selected from (CH.sub.2).sub.yR.sup.5, (CH.sub.2).sub.yCH(R.sup.5).sub.2, or (CH.sub.2).sub.yCH(R.sup.7)CH(R.sup.5).sub.2; y is 0-6; each Ar is independently selected from an optionally substituted 3-7 membered saturated, partially unsaturated, or fully unsaturated monocyclic ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an optionally substituted 8-10 membered saturated, partially unsaturated, or fully unsaturated bicyclic ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R.sup.3 is selected from hydrogen, CH(R.sup.7)R.sup.5, a 3-7 membered carbocyclyl, or an optionally substituted group selected from C.sub.1-4 aliphatic, a 3-6 membered heterocyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5-6 membered aryl or heteroaryl ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each R is independently selected from hydrogen or an optionally substituted C.sub.1-6 aliphatic group, or: two R on the same nitrogen atom are taken together with the nitrogen atom attached thereto to form a 4-8 membered saturated, partially unsaturated, or fully unsaturated ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each R.sup.4 is independently selected from R.sup.6, C(O)R.sup.6, CO.sub.2R.sup.6, CON(R.sup.6).sub.2, SO.sub.2R.sup.6; each R.sup.5 is independently selected from R.sup.6, OR.sup.6, CO.sub.2R.sup.6, (CH.sub.2).sub.yN(R.sup.4).sub.2, N(R.sup.4).sub.2, N(R)C(O)R.sup.6, N(R)CON(R.sup.6).sub.2, CON(R.sup.6).sub.2, SO.sub.2R.sup.6, N(R)SO.sub.2R.sup.6, C(O)R.sup.6, CN, or SO.sub.2N(R.sup.6).sub.2; each R.sup.6 is independently selected from R or Ar; R.sup.7 is selected from R.sup.6, (CH.sub.2).sub.wOR.sup.6, (CH.sub.2).sub.wN(R.sup.4).sub.2, or (CH.sub.2).sub.wSR.sup.6; and each w is independently selected from 0-4. 2. The compound according to claim 1, wherein R.sup.3 is CH(R.sup.7)R.sup.5. 3. The compound according to claim 1, wherein R.sup.3 is a 3-6 membered heterocyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur. 4. The compound according to claim 1, wherein said compound has the formula III: ##STR00083## or a pharmaceutically acceptable salt thereof. 5. The compound according to claim 1, wherein said compound has the formula IV: ##STR00084## or a pharmaceutically acceptable salt thereof. 6. The compound according to claim 1, wherein said compound is selected from the group consisting of: ##STR00085## ##STR00086## ##STR00087## ##STR00088## ##STR00089## ##STR00090## ##STR00091## ##STR00092## ##STR00093## ##STR00094## ##STR00095## ##STR00096## ##STR00097## ##STR00098## 7. A composition comprising an effective amount of a compound according to claim 1, and a pharmaceutically acceptable carrier, adjuvant, or vehicle. 8. The composition of claim 7, additionally comprising a therapeutic agent selected from a chemotherapeutic or anti-proliferative agent selected from mechlorethamine, chlorambucil, cyclophosphamide, melphalan, ifosfamide, methotrexate, 6-mercaptopurine, 5-fluorouracil, cytarabile, gemcitabine, vinblastine, vincristine, vinorelbine, paclitaxel, etoposide, irinotecan, topotecan, doxorubicin, bleomycin, mitomycin, carmustine, lomustine, cisplatin, carboplatin, asparaginase, tamoxifen, leuprolide, flutamide, megestrol, imatinib, adriamycin, dexamethasone, or cyclophosphamide. 9. A method of inhibiting ERK2, JNK3, SRC, Aurora2, or GSK3 protein kinase activity in a biological sample selected from a cell culture, saliva, urine, feces, semen, tears, or an extract thereof, which method comprises contacting said biological sample in vitro with: a) a composition according to claim 7; or b) a compound according to claim 1.

Details for Patent 7,456,190

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Recordati Rare Diseases, Inc.	ELSPAR	asparaginase	For Injection	101063	01/10/1978		2023-03-13