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    Substituted 5-phenyl pyrimidines I in therapy
    2.
    发明专利
    Substituted 5-phenyl pyrimidines I in therapy 未知

    公开(公告)号：ZA200707315B

    公开(公告)日：2008-11-26

    申请号：ZA200707315

    申请日：2007-08-29

    Applicant: BASF AG

    Inventor： JOACHIM RHEINHEIMER ,  THOMAS GROTE ,  BERND MUELLER ,  FRANK SCHIEWECK ,  ANJA SCHWOEGLER ,  THORSTEN JABS ,  CARSTEN BLETTNER ,  BARBARA NAVE

    IPC: A61K20090101 ,  C07D20090101

    Abstract: The present invention relates to substituted 5-phenyl pyrimidines I, which carry a radical X in the 4-position of the pyrimidine ring, a radical Y in the 6-position of the pyrimidine ring, the radical X denoting a group of the formula NR 1 R 2 , OR 1a or SR 1a , in which R 1 , R 2 , independently of each other, denote hydrogen, C 1 -C 10 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 10 -haloalkyl, C 3 -C 8 -cycloalkyl, C 3 -C 8 -halocycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered heterocyclyl, containing 1, 2, 3 or 4 nitrogen atoms or 1, 2 or 3 nitrogen atoms and one sulfur or oxygen atom as ring members, which radicals may be unsubstituted or may carry 1, 2, 3 or 4 radicals R a1 ; or the radical NR 1 R 2 may also form a 5- or 6-membered optionally substituted heterocyclic ring, containing 1, 2, 3 or 4 nitrogen atoms or 1, 2 or 3 nitrogen atoms and one sulfur or oxygen atom as ring members, which are non-adjacent to the nitrogen of NR 1 R 2 , in which two adjacent C atoms or one N atom and one adjacent C atom can be linked by a C 1 -C 4 -alkylene chain and wherein the heterocyclic ring may be unsubstituted or may carry 1, 2, 3 or 4 radicals R a1 as defined in claim 1 , R 1a has one of the meanings given for R 1 except for hydrogen; the radical Y being selected from the group consisting of halogen, cyano, C 1 -C 4 -alkyl, C 2 -C 4 -alkenyl, C 2 -C 4 -alkynyl, C 3 -C 6 -cycloalkyl, C 1 -C 4 -alkoxy, C 3 -C 4 -alkenyloxy, C 3 -C 4 -alkynyloxy, C 1 -C 6 -alkylthio, di-(C 1 -C 6 -alkyl)amino or C 1 -C 6 -alkylamino, where the alkyl, alkenyl and alkynyl radicals of Y may be substituted by halogen, cyano, nitro, C 1 -C 2 -alkoxy or C 1 -C 4 -alkoxycarbonyl; and wherein the pyrimidine radical may also carry a radical different from hydrogen in the 2-position and wherein the phenyl ring in the 5-position of the pyrimidine ring may be unsubstituted or carry 1, 2, 3, 4 or 5 radicals L which are different from hydrogen, and the pharmaceutically acceptable salts substituted 5-phenyl pyrimidines for use in therapy, in particular in therapy or treatment of cancerous diseases.

    2-(pyridin-2-yl)-pyrimidines and their use for controlling pathogenic fungi
    6.
    发明专利
    2-(pyridin-2-yl)-pyrimidines and their use for controlling pathogenic fungi 未知

    公开(公告)号：ZA200701518B

    公开(公告)日：2008-12-31

    申请号：ZA200701518

    申请日：2007-02-21

    Applicant: BASF AG

    Inventor： WASSILIOS GRAMMENOS ,  THOMAS GROTE ,  CARSTEN BLETTNER ,  MARKUS GEWEHR ,  UDO HUENGER ,  BERND MUELLER ,  JOACHIM RHEINHEIMER ,  PETER SCHAEFER ,  FRANK SCHIEWECK ,  ANJA SCHWOEGLER ,  ULRICH SCHOEFL ,  HARALD KOEHLE ,  SIEGFRIED STRATHMANN ,  MARIA SCHRERER ,  REINHARD STIERL ,  JAN RETHER

    IPC: A01N20090101 ,  A01N43/54 ,  C07D20090101 ,  C07D401/04

    Abstract: 2-Pyridyl pyrimidine derivatives (I) are new. 2-Pyridyl pyrimidine derivatives of formula (I) and their salts are new. k : 0-3; m : 0-5; n : 1-5; R 1>halo, OH, CN, NO 2, 1-4C (halo)alkyl, 104C (halo)alkoxy, 2-4C alkenyl, 2-4C alkynyl, 3-8C cycloalkyl, (1-4C)alkoxy(1-4C)alkyl, NH 2, phenoxy (optionally substituted with halo or 1-4C alkyl), NHR, NRR, C(Ra)=NORb, SO pA 1> or COA 2>; or R 1>+R 1>1-4C (halo)alkylenedioxy; R : 1-4C alkyl or 1-4C alkylcarbonyl; Ra : H or 1-4C alkyl; Rb : 1-4C alkyl, 3-4C alkenyl or 3-4C alkynyl; p : 0-2; A 1>1-4C alkyl, or also NH 2, 1-4C alkylamino or di(1-4C alkyl)amino when p = 2; A 2>H, OH, 1-4C alkyl, 1-4C alkylamino, di(1-4C alkyl)amino, 2-4C alkenyl or 1-4C (halo)alkoxy; R 2>1-4C haloalkyl, 1-4C (halo)alkoxy, OH, halo, CN or NO 2, or R 2> can be H or 1-4C alkyl if n = 3-5 and/or k = 1-3 and/or at least one R 1> is other than halo, 1-4C (halo)alkyl and 1-4C alkoxy; and R 3>1-4C alkyl. An independent claim is also included for controlling phytopathogenic fungi by treating the fungi, or materials, plants, soil or seeds to be protected from fungal attack, with a compound (I). [Image] ACTIVITY : Plant antifungal. In a protective test against Alternaria solani on tomato plants, plants treated with 2-(5-methyl-6-phenyl-2-pyridyl)-4,5-pentamethylene-pyrimidine (250 ppm) suffered no attack, whereas 90% of untreated plants were attacked. MECHANISM OF ACTION : None given.

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