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Alopecia - Hair Loss

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/* GSK3 inhibition by pryazole pyrimidine amine derivatives */
Pyrimidine derivative of Pyrazole Used in Alopecia
'''Patent Number''': US6989385'''Applicant''': ''Vertex Pharmaceuticals Incorporated'''''Title''': Pyrazole compounds useful as protein kinase inhibitors'''Basic Structure:''':
[[Image:pyrazol1.jpg]]
          '''Derivatives of pyrimidine-pyrazole aminedisclosed in the patent:'''
* [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-met- hyl-2H-pyrazol-3-yl)-amine
* [2-(2,6-Dichlorobenzyl)-6-methyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl- )-amine
* [2-(2,6-Dichlorobenzyl)-5,6-dimethyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-- 3-yl)-amine
----
'''Patent Number''': US7008948
'''Applicant''': Vertex Pharmaceuticals Incorporated
'''Title''': Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors
'''Basic Structure'''
[[Image:pyrazol2.jpg]]
'''Patent NumberDerivatives of pyrimidine-pyrazole amine disclosed in the patent: US7008948 Applicant: Vertex Pharmaceuticals IncorporatedBasic Structure''' 
* [2-(2-Clorophenyl)-5,6-dimethylpyrimidin-4-yl]-(5-Methyl-2H-pyrazol-3-yl)-- amine
* (1H-Indazol-3-yl)-[6-methyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine
* 1H-Indazol-3-yl)-[6-phenyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-amine
----
'''Patent Number''': US6977262
'''Assignee''': Mitsubishi Pharma Corporation
'''Title''': Dihydropyrazolopyridine compounds and pharmaceutical use thereof
'''Basic Structure''':
[[Image:pyrazol3.jpg]]
   '''Patent NumberDerivatives of pyrimidine-pyrazole amine disclosed in the patent: US6977262Assignee: Mitsubishi Pharma CorporationTitle: Dihydropyrazolopyridine compounds and pharmaceutical use thereof''' 
* Ethyl 4-(2-chlorophenyl)-4,7-dihydro-6-methyl-2H-pyrazolo[3,4-b]pyridine-5-carboxylate
* Ethyl 4,7-dihydro-6-trifluoromethyl-4-(2-trifluoromethylphenyl)-2H-pyrazolo[3,4- b]pyridine-5-carboxylate
* Ethyl 4-(3-chlorophenyl)-4,7-dihydro-6-trifluoromethyl-2H-pyrazolo[3,4-b]pyridin e-5-carboxylate
----
'''Patent Number''': US6664247
'''Assignee''': Vertex Pharmaceuticals Incorporated
'''Title''': Pyrazole compounds useful as protein kinase inhibitors'''
'''Basic Structure''':
[[Image:pyrazol4.jpg]]
'''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''
* (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphtalen-2-ylsulfanyl)-6-phenylpyrimid in-4-yl]-amine
* 5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methoxycarbonyl-phenylylsulfanyl)-6-p henylpyrimidin-4-yl]-amine
* (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl ]-amine
* (5-Cyclopropyl-2H-pyrazol-3-yl)-[5,6-dimethyl-2-(naphthalen-2-ylsulfanyl)-p yrimidin-4-yl]-amine
* (5-Cyclopropyl-2H-pyrazol-3-yl)-[5-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine
* (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine
* (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(morpholin-4-yl)-2-(naphthalen-2-ylsulfa nyl)-pyrimidin-4-yl]-amine
* (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(1-methylpiperazin-4-yl)-2-(naphthalen-2 -ylsulfanyl)-pyrimidin-4-yl]-amine
* [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine
* [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine
* [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyraz ol-3-yl)-amine
* (5-Methyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-6-phenyl-pyrimidin- 4-yl]-amine
* [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine
* [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine
* (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-py rimidin-4-yl]-amine
* [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine
* (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyls ulfanyl]-pyrimidin-4-yl}-amine
* [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine
* [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine
* [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine
* [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine
* [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-met hyl-2H-pyrazol-3-yl)-amine
* [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine
* [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine
* (2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-yl }-(5-methyl-2H-pyrazol-3-yl)-amine
* [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine
* [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine
* [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine
* [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y l)-amine
* [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine
* [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5 -methyl-2H-pyrazol-3-yl)-amine
* [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine
* 5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfan yl)-pyrimidin-4-yl]-amine
* [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine
* (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mor pholin-4-yl-pyrimidin-4-yl}-amine
* {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimid in-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine
* {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrim idin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine
* [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine
* [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine
* [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine
* [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine
* (5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-yl-methylsulf anyl)-pyrimidin-4-yl]-amine
* {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)phenyl]-pyri midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine
* [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methyl -2H-pyrazol-3-yl)-amine
* [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine
* [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl) -amine
* [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)pyrimidin-4-yl]-( 5-methyl-2H-pyrazol-3-yl)-amine
* [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine.
----
'''Patent Number''': US2004224944
'''Assignee''': VERTEX PHARMACEUTICALS INC
'''Title''': Pyrazole compounds useful as protein kinase inhibitors
'''Basic Structure''':
[[Image:pyrazol5.jpg]]
'''Derivatives of pyrimidine-pyrazole amine disclosed in the patent:'''
   '''Patent No.: US6664247Assignee: Vertex Pharmaceuticals IncorporatedTitle: Pyrazole compounds useful as protein kinase inhibitors'''            (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphtalen-2-ylsulfanyl)-6-phenylpyrimid in-4-yl]-amine (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(3-methoxycarbonyl-phenylylsulfanyl)-6-p henylpyrimidin-4-yl]-amine (5-Cyclopropyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl ]-amine (5-Cyclopropyl-2H-pyrazol-3-yl)-[5,6-dimethyl-2-(naphthalen-2-ylsulfanyl)-p yrimidin-4-yl]-amine (5-Cyclopropyl-2H-pyrazol-3-yl)-[5-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-methyl-2-(naphthalen-2-ylsulfanyl)-pyrim idin-4-yl]-amine (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(morpholin-4-yl)-2-(naphthalen-2-ylsulfa nyl)-pyrimidin-4-yl]-amine (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-(1-methylpiperazin-4-yl)-2-(naphthalen-2 -ylsulfanyl)-pyrimidin-4-yl]-amine [6-(2,6-Dimethylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine [6-(2-Methylphenyl)-2-(naphthalen-2-ylsulfanyl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine [2-(4-Acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyraz ol-3-yl)-amine (5-Methyl-2H-pyrazol-3-yl)-[2-(naphthalen-2-ylsulfanyl)-6-phenyl-pyrimidin- 4-yl]-amine [2-(4-Isobutyrylylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine [6-(4-Methylpiperazin-1-yl)-2-methylsulfanyl-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine (5-Methyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenylsulfanyl)-py rimidin-4-yl]-amine [2-(4-Cyclopropanecarbonylamino-phenylsulfanyl)-6-phenylpyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine (5-Methyl-2H-pyrazol-3-yl)-{6-phenyl-2-[4-(propane-1-sulfonylamino)-phenyls ulfanyl]-pyrimidin-4-yl}-amine [2-(4-Ethanesulfonylamino-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine [2-(4-Acetamidophenyl-sulfanyl)-6-(2-methylphenyl)-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine [2-(4-Isobutanecarbonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine [2-(4-Acetamido-phenyl-sulfanyl)-5-methyl-6-phenyl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine [2-(4-Acetamido-phenyl-sulfanyl)-6-(4-methoxyphenyl)-pyrimidin-4-yl]-(5-met hyl-2H-pyrazol-3-yl)-amine [6-(3-Acetamidophenyl)-2-(4-acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine [2-(4-Isopropanesulfonylamino-phenyl-sulfanyl)-6-phenyl-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine (2-[4-(2-Dimethylamino-acetylamino)-phenylsulfanyl]-6-phenyl-pyrimidin-4-yl }-(5-methyl-2H-pyrazol-3-yl)-amine [2-(3-Chloro-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine [2-(3-Chloro-benzylsulfanyl)-6-(2-methoxy-ethylamino)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine [2-Benzylsulfanyl-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5-methyl-2H-p yrazol-3-yl)-amine [2-Benzylsulfanyl-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-y l)-amine [2-(3-Chloro-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine [2-(4-methoxy-benzylsulfanyl)-6-(4-methylpiperazin-1-yl)-pyrimidin-4-yl]-(5 -methyl-2H-pyrazol-3-yl)-amine [2-(4-Acetamido-phenyl-sulfanyl)-6-tert-butyl-pyrimidin-4-yl]-(5-methyl-2H- pyrazol-3-yl)-amine (5-Cyclopropyl-2H-pyrazol-3-yl)-[6-phenyl-2-(4-propionylamino-phenyl-sulfan yl)-pyrimidin-4-yl]-amine [2-(3-Chloro-benzylsulfanyl)-6-(piperidin-1-yl)-pyrimidin-4-yl]-(5-methyl-2 H-pyrazol-3-yl)-amine (5-Methyl-2H-pyrazol-3-yl)-{2-[4-(morpholinesulfonyl)-benzylsulfanyl]-6-mor pholin-4-yl-pyrimidin-4-yl}-amine {6-(2-Methoxy-ethylamino)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrimid in-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine {6-(4-methylpiperazin-1-yl)-2-[4-(morpholinesulfonyl)-benzylsulfanyl]-pyrim idin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine [6-Methoxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine [2-(4-Methoxycarbonyl-phenyl-sulfanyl)-6-methoxymethyl-pyrimidin-4-yl]-(5-m ethyl-2H-pyrazol-3-yl)-amine [2-(3,5-Dimethoxy-benzylsulfanyl)-6-morpholin-4-yl-pyrimidin-4-yl]-(5-methy l-2H-pyrazol-3-yl)-amine [2-(3,5-Dimethoxy-benzylsulfanyl)-6-pyrrolidin-4-yl-pyrimidin-4-yl]-(5-meth yl-2H-pyrazol-3-yl)-amine (5-Methyl-2H-pyrazol-3-yl)-[6-morpholin-4-yl-2-(naphthalene-2-yl-methylsulf anyl)-pyrimidin-4-yl]-amine {2-(4-Acetamido-phenyl-sulfanyl)-6-[4-(3-dimethylamino-propoxy)phenyl]-pyri midin-4-yl}-(5-methyl-2H-pyrazol-3-yl)-amine [2-(4-Acetamidophenylsulfanyl)-6-(morpholin-4-yl)-pyrimidin-4-yl]-(5-methyl -2H-pyrazol-3-yl)-amine [6-Hydroxymethyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-me thyl-2H-pyrazol-3-yl)-amine [2-(4-Acetamido-phenyl-sulfanyl)-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl) -amine [6-(1-Butoxycarbonyl)-2-(4-propionylamino-phenyl-sulfanyl)pyrimidin-4-yl]-( 5-methyl-2H-pyrazol-3-yl)-amine [6-Methoxycarbonyl-2-(4-propionylamino-phenyl-sulfanyl)-pyrimidin-4-yl]-(5- methyl-2H-pyrazol-3-yl)-amine. Patent no: US2004224944Assignee: VERTEX PHARMACEUTICALS INCTitle: Pyrazole compounds useful as protein kinase inhibitors   * [2-(2-Chloro-phenyl)-6,7-dihydro-5H-cyclopentapyrimidin-4-yl]-(5,7-difluoro-1H-indazol-3-yl)-amine * (1H-Indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine * (7-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine * (5,7-Difluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-5,6,7,8,9,10-hexahydro-cyclooctapyrimidin-4-yl]-amine * [6-Cyclohexyl-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine * [6-(2-Fluoro-phenyl)-2-(2-trifluoromethyl-phenyl)-pyrimidin-4-yl]-(1H-indazol-3-yl)-amine * (6-Fluoro-1H-indazol-3-yl)-[2-(2-trifluoromethyl-phenyl)-quinazolin-4-yl]-amine * 3-[2-(2-Trifluoromethyl-phenyl)-quinazolin-4-ylamino]-1H-indazole-5-carboxylic acid methyl ster * (5-Methyl-2H-pyrazol-3-yl)-[2-(2-naphthyl-1-yl)-quinazolin-4-yl]-* [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(7-fluoro-1H-indazol-3-yl)-amine * [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(5-fluoro-1H-indazol-3-yl)-amine
== Inhibition of 5- - reductase by Finasteride ==
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