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Preparation of 5-(arylalkynyl)pyrimidines having neurotrophic activity for the treatment of neurodegerative and other neurological disorders

Preparation of 5-(arylalkynyl)pyrimidines having neurotrophic activity for the treatment of neurodegerative and other neurological disorders. Beauchamp, Lilia; Krenitsky, Thomas A.; Kelley, James L. (Krenitsky Pharmaceuticals, Inc., USA). PCT Int. Appl. WO 2002008205 A1 31 Jan 2002, 60 pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, ZW, AM, AZ, BY, KG, KZ, MD, RU, TJ, TM; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: C07D239-34. ICS: C07D239-38; C07D239-42; C07D239-48; C07D239-46; A61K031-505; A61P025-00; A61P025-28; A61P003-10. APPLICATION: WO 2001-US23088 20 Jul 2001. PRIORITY: US 2000-PV220348 24 Jul 2000. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1 Title compds. I [wherein Z = O, NH, or S; m = 0-1; R1 = (un)substituted (alkyl)a((hetero)cycloalkyl or (hetero)aryl)b(alkyl)c; a, b, and c = independently 0-1 and a + b + c 3 1, with provisos; R2 = H, NH2, or NHCOR3; R3 = H or alkyl; X = (un)substituted aryl; and pharmaceutically acceptable esters, amides, salts, or solvates thereof] were prepd. Pharmaceutical compns. which contain I, methods for their prepn., and their use in therapy, particularly in the treatment of neurodegenerative or other neurol. disorders of the central and peripheral nervous systems, including age related cognitive disorders such as senility and Alzheimer's disease, nerve injuries, peripheral neuropathies, and seizure disorders such as epilepsy, are disclosed. For example, 4-chloro-5-(4-chlorophenylethynyl)pyrimidine (prepn. given) was coupled with (trans)-4-aminocyclohexanol·HCl using TEA and MeCN in CH2Cl2 to afford II. The latter increased the choline acetyltransferase (ChAT) activity relative to nerve growth factor (NGF) alone with EC2x of 0.2 mM. Keywords arylalkynyl pyrimidine prepn neurotrophic activity phenylethynylpyrimidine prepn nervous system agents Index Entries Nervous system degeneration, treatment; prepn. of (arylalkynyl)pyrimidines having neurotrophic activity for the treatment of neurodegenerative and other neurol. disorders Nerve, disease peripheral neuropathy, treatment; prepn. of (arylalkynyl)pyrimidines having neurotrophic activity for the treatment of neurodegenerative and other neurol. disorders Nervous system peripheral, disease, treatment; prepn. of (arylalkynyl)pyrimidines having neurotrophic activity for the treatment of neurodegenerative and other neurol. disorders Anti-Alzheimer's agents Anticonvulsants Antidiabetic agents Cognition enhancers Human Nervous system agents prepn. of (arylalkynyl)pyrimidines having neurotrophic activity for the treatment of neurodegenerative and other neurol. disorders Mental disorder senile psychosis, treatment; prepn. of (arylalkynyl)pyrimidines having neurotrophic activity for the treatment of neurodegenerative and other neurol. disorders Aging, animal senility, treatment; prepn. of (arylalkynyl)pyrimidines having neurotrophic activity for the treatment of neurodegenerative and other neurol. disorders 393856-66-1 393856-71-8 393856-87-6 393857-07-3 393857-16-4 393855-70-4 393855-73-7 393855-76-0 393855-79-3 393855-81-7 393855-83-9 393855-87-3 393855-89-5 393855-91-9 393855-93-1 393855-96-4 393855-99-7 393856-02-5 393856-04-7 393856-07-0 393856-10-5 393856-13-8 393856-17-2 393856-21-8 393856-24-1 393856-26-3 393856-29-6 393856-31-0 393856-34-3 393856-36-5 393856-39-8 393856-42-3 393856-45-6 393856-48-9 393856-51-4 393856-54-7 393856-57-0 393856-60-5 393856-63-8 393856-69-4 393856-73-0 393856-76-3 393856-79-6 393856-82-1 393856-85-4 393856-89-8 393856-91-2 393856-95-6 393857-11-9 393857-13-1 393857-18-6 393857-31-3 393857-34-6 393857-35-7 393857-41-5 393857-43-7 393857-47-1 393857-50-6 CNS agent; prepn. of (arylalkynyl)pyrimidines having neurotrophic activity for the treatment of neurodegenerative and other neurol. disorders 3993-79-1 35447-83-7 40307-11-7 62452-73-7 81631-65-4 393856-98-9 393857-01-7 393857-03-9 393857-05-1 393857-09-5 393857-14-2 393857-20-0 393857-23-3 393857-27-7 393857-29-9 393857-33-5 393857-36-8 393857-37-9 393857-39-1 intermediate; prepn. of (arylalkynyl)pyrimidines having neurotrophic activity for the treatment of neurodegenerative and other neurol. disorders 9012-78-6 9061-61-4 prepn. of (arylalkynyl)pyrimidines having neurotrophic activity for the treatment of neurodegenerative and other neurol. disorders 108-53-2 123-30-8 123-31-9, reactions 536-74-3 588-93-2 637-89-8 766-96-1 873-73-4 929-06-6 1066-54-2 6850-65-3 13889-98-0 14235-81-5 22428-87-1 25309-64-2 26912-67-4 27489-62-9 50910-54-8 63558-65-6 76445-65-3 reactant; prepn. of (arylalkynyl)pyrimidines having neurotrophic activity for the treatment of neurodegenerative and other neurol. disorders