4-(aminomethyl)-piperidine benzamides for treating...

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C546S197000, C546S205000, C546S207000, C546S214000

Reexamination Certificate

active

10353307

ABSTRACT:
The present invention of compounds of formula (I)a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, —R1—R2— is a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl or hydroxy; R3is hydrogen or halo; R4is hydrogen or C1-6alkyl; R5is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, oxoC5-6cycloalkyl, C2-6alkenyl, or L is a radical of formula -Alk-R6—, Alk-X—R7, -Alk-Y—C(═O)—R9, or -Alk-Y—C(═O)—NR11R12wherein each Alk is C1-12alkanediyl; and R6is hydrogen, amino, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, oxoC5-6cycloalkyl, aryl or a heterocyclic ringsystem; R7is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, aryl or a heterocyclic ringsystem; X is O, S, SO2or NR8; said R8being hydrogen or C1-6alkyl; R9is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy, hydroxy or aryl; Y is a direct bond or NR10; said R10being hydrogen, or C1-6alkyl; R11and R12each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, or R11and R12combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating or preventing gastrointestinal disorders.

REFERENCES:
patent: 5705509 (1998-01-01), Gaster et al.
patent: 2002/0042430 (2002-04-01), Bosmans et al.
patent: 0389037 (1995-09-01), None
patent: WO93/03725 (1993-03-01), None
patent: WO93/05038 (1993-03-01), None
patent: WO93/16072 (1993-08-01), None
patent: WO94/05654 (1994-03-01), None
patent: WO94/08994 (1994-04-01), None
patent: WO94/08995 (1994-04-01), None
patent: WO94/10174 (1994-05-01), None
patent: WO94/29298 (1994-12-01), None
patent: WO96/28424 (1996-09-01), None
patent: WO96/33186 (1996-10-01), None
D. Fancelli, et al., Serotoninergic 5-HT3and 5-ht4receptor activities of dihydrobenzofuran carboxylic acid Derivatives, Bioorg. Med. Chem Letter. vol. 6 No. 3 (1996) pp. 263-266.
R.D. Clark et al., Synthesis and Preliminary Pharmaceological Evaluation of 2-Benxyloxy-Substituted Aryl Ketones as 5HT4Receptor Antagonists, Biorg. Med. Chem Lett. vol. 4 No. 20, (1994) pp. 2481-2484.
I.M. Gaster, et al., “(1-Butyl-4-piperidinyl)methyl 8-Amino-7-chloro-1,4-benzodioxane-5-carboxylate Hydrochloride: A Highly Potent and Selective 5-HT4 Receptor Antagonist Derived from Metoclopramide”, J. Med. Chem, 36(25), (1993) PP. 4121-4123.
Y. Ben-David, et al., “Chelate-Assisted, Pd-Catalyzed Efficient Carbonylation of Aryl Chlorides”, J. Am. Chem. Soc., vol. 111, No. 23, (1989) pp. 8742-8744.
International Search Report PCT/EP99/10064 dated Mar. 23, 2000.

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