Use of anthelmintic agents against dirofilaria immitis
A kind of canine heartworm, selected technology, applied in the application field of anti-helminth agent against canine heartworm
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[0240] In some embodiments, Z 1 is N. Such an embodiment consists of the following structures:
[0241] .
[0242] In some embodiments, Z 1 is selected from halogen, nitro, cyano, C 1 -C 6 -alkoxy and C 1 -C 6 - CH substituted by a substituent of alkylsulfanyl. The C 1 -C 6 -alkoxy and C 1 -C 6 -Alkylsulfanyl is optionally substituted with one or more independently selected halogen.
[0243] In some embodiments, Z 1 is CH substituted with an electron-withdrawing substituent. Such substituents include, for example, halo, nitro, cyano, halo-C 1 -C 6 -Alkyl, halo-C 1 -C 6 -alkoxy and halo-C 1 -C 6 - Alkylsulfanyl.
[0244] In some embodiments, Z 1 is CH substituted with halogen. For example, in some such embodiments, Z 1 is CH substituted by chlorine. These embodiments are comprised of the following structures:
[0245] .
[0246] In some embodiments, Z 1 is CH substituted by nitro. Such an embodiment consists of the following structures:
[0247]...
Embodiment 1
[0398] Example 1. Preparation of Analytical Protocols for Compounds of the Invention
[0399] Applicants have prepared a number of compounds for use in the present invention. Identity and purity were characterized and verified using various analytical high performance liquid chromatography ("HPLC") and mass spectrometry ("MS") protocols. These schemes are discussed below.
[0400] System I
[0401] In some cases, compound analysis was performed using a binary pump (G1312A) with a degasser (G1379A), a well plate autosampler (G1367A), a column oven (G1316A), a diode array detector (G1315B), a ESI-source mass spectrometer detector (G1946D SL) and evaporative light detector (Sedex 75) HPLC / MSD 1100 (Agilent, Santa Clara, CA, USA) were performed. The system uses four different columns and detection methods:
[0402] Plan I-A
[0403] The column used for this protocol was a Zorbax SB-C18 (Agilent) with 4.6 mm diameter, 30 mm length and 3.5 μm packing. The column was operat...
Embodiment 266
[0442] Further examples of compounds useful in the invention are described below. The first novel compound (Example 266) was prepared as follows:
[0443]
[0444] 4-[4-(Trifluoromethoxy)phenoxy]piperidine (2 g; 7.7 mmol) was suspended in dichloromethane (25 mL), and chloroacetic anhydride (1.35 g; 7.7 mmol) was slowly added with stirring ) in dichloromethane (5 mL). After 140 min reaction time, additional chloroacetic anhydride (575 mg; 3.3 mmol) was added and the reaction mixture was stirred overnight. The reaction mixture was washed with aq. 0.2M hydrochloric acid (2×30 mL) and aq. 1M sodium hydroxide (50 mL). The organic phase was dried over sodium sulfate, filtered and concentrated under reduced pressure to give the desired crude product (2.1 g; 6.2 mmol), which was used as such in the next step.
[0445]
[0446] 2-Chloro-1-[4-[4-(trifluoromethoxy)phenoxy]-1-piperidinyl]ethanone (23 g; 68 mmol) and 4-[4-nitro-3-( Trifluoromethyl)anilino]cyclohexanol (20.7 g; 68...
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