Israel state records י"ג בשבט התשס"ח January 20, 2008

תולדות בנזאימידאזול ותכשירי רוקחות המכילים אותן	BENZIMIDAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
[54]
	17.01.2001					[22]
	JP	[33]	17.01.2000	[32]	2000/007533	[31]
	JP		25.12.2000		2000/392303
Int. Cl.8 C07D 403/00, 409/00						[51]
			TEIJIN LIMITED, JAPAN			[71]
	WO/2001/053291					[87]
וולף, ברגמן וגולר, רחוב קרן היסוד 19ב' , ת.ד. 1352, ירושלים			WOLFF, BREGMAN AND GOLLER, 19B KEREN HAYESOD ST., P.O.B. 1352, JERUSALEM 91013			[74]

[57] A benzimidazole derivative or its medically acceptable salt represented by a compound selected from the group of the following formulas:

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150710			[21][11]
תכשירי N–פיפרידינו–5–(4–כלורופניל)–1–(2,4–דיכלורופניל)–4–מתילפיראזון–3–קרבוקסאמיד לטיפול בתלות בניקוטין			N-PIPERIDINO-5-(CHLOROPHENYL)-1-(2,4-DICHLOROPHENYL)-4-METHYLPYRAZOLE-3-CARBOXAMIDE COMPOSITIONS FOR THE TREATMENT OF NICOTINE DEPENDENCE			[54]
	07.02.2001					[22]
	FR	[33]	09.02.2000	[32]	00/01682	[31]
Int. Cl.8 A61K 031/395, A61P 025/34, C07D 401/12						[51]
			SANOFI AVENTIS, FRANCE			[71]
	WO/2001/058450					[87]
סנפורד ט. קולב ושות', שער הגיא 4, מרמורק , ת.ד. 2273, רחובות			SANFORD T.COLB & CO., P.O.B. 2273, REHOVOT 76122			[74]

[57] Use of N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carboxamide, a pharmaceutically acceptable salt thereof or a solvate thereof for the preparation of medicinal products that are intended for helping to quit tobacco consumption, for the treatment of nicotine dependence and/or for the treatment of the symptoms of withdrawal from nicotine.

__________

150757			[21][11]
תולדות 2–אוקסו–1–פירולידין, תהליך הכנתן והשימוש בהן			2-OXO-1-PYRROLIDINE DERIVATIVES, PROCESS FOR PREPARING THEM AND THEIR USES			[54]
	21.02.2001					[22]
	GB	[33]	23.02.2000	[32]	0004297.8	[31]
Int. Cl.8 C07D 207/27						[51]
			UCB FARCHIM S.A., SWITZERLAND			[71]
	WO/2001/064637					[87]
ריינהולד כהן ושותפיו, רחוב אחד העם 21 , ת.ד. 4060, תל אביב			REINHOLD COHN AND PARTNERS, 21 AHAD HA'AM ST., P.O.B. 4060, TEL AVIV 61040			[74]

[57] Intermediate compounds of the formula

and pharmaceutically acceptable salt thereof wherein X is –CONR⁵R⁶ or –COOR⁷ or –CO-R⁸ or CN; R¹ is hydrogen or alkyl, aryl, heterocycloalkyl, heteroaryl, halogen, hydroxy, amino, nitro, cyano;

R² and R⁴ are the same or different and each is independently hydrogen or halogen, hydroxy, amino, nitro, cyano, acyl, acyloxy, -SO₂-alkyl, -SO₂-aryl, -SO-alkyl, -SO-aryl, alkylamino, carboxy, ester, ether, amido, sulfonic acid, sulfonamide, alkoxycarbonyl, alkylthio, arylthio, alkyl, alkoxy, oxyester, oxyamido, aryl, arylamino, aryloxy, heterocycloalkyl, heteroaryl, vinyl;

R³ is hydrogen, halogen, hydroxy, amino, nitro, cyano, acyl, acyloxy, -SO₂-alkyl, -SO₂-aryl, -SO-alkyl, -SO-aryl, alkylamino, carboxy, ester, ether, amido, sulfonic acid, sulfonamide, alkoxycarbonyl, alkylthio, arylthio, alkyl, alkoxy, oxyester, oxyamido, aryl, arylamino, aryloxy, heterocycloalkyl, heteroaryl, (C2-C5) alkenyl, (C2-C5) alkynyl, azido, phenylsulfonyloxy wherein each (C2-C5) alkenyl, (C2-C5) alkynyl may independently be optionally substituted by one or more halogen, cyano, thiocyano, azido, alkylthio, cyclopropyl, acyl, and/or phenyl;

R⁵, R⁶, R⁷ are the same or different and each is independently hydrogen, hydroxy, alkyl, aryl, heterocycloalkyl, heteroaryl, alkoxy, aryloxy;

and R⁸ is hydrogen, hydroxy, thiol, halogen, alkyl, aryl, heterocycloalkyl, heteroaryl, alkylthio, arylthio; each alkyl contains 1-20 carbon atoms and has straight, branched or cyclic moieties or combinations thereof and may be optionally substituted 1 to 5 substituents independently selected from halogen, hydroxy, thiol, amino, nitro, cyano, acyl, acyloxy, -SO₂-alkyl, -SO₂aryl, -SO-alkyl, -SO-aryl, alkylamino, carboxy, ester, ether, amido, sulfonic acid, sulfonamide, alkoxycarbonyl, alkylthio, arylthio, oxyester, oxyamido, heterocycloalkyl, heteroaryl, vinyl (C1-C5) alkoxy, (C6-C10) aryloxy, (C6-C10) aryl; each aryl may be optionally substituted by 1 to 5 substituents independently selected from halogen, hydroxy, thiol, amino, nitro, cyano, acyl, acyloxy –SO₂-alkyl, -SO₂-aryl, -SO-alkyl, -SO-aryl, alkylamino, carboxy, ester, ether, amido, sulfonic acid, sulfonamide, alkoxycarbonyl, alkylthio, oxyester, oxyamido, aryl, (C1-C6) alkoxy, (C6-C10) aryloxy, (C1-C6) alkyl; with the proviso that the compound is not methyl 2-(4R,S-isopropyl-2-oxo-pyrrolidin-1-yl) acrylate, methyl 2-(3R, S-chloro-4- R,S-isopropyl-2-oxypyrrolidin-1-yl) acrylate or methyl 2-(2-oxo-pyrrolidin-1-yl)-acrylate.

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150783			[21][11]