IP Library Granted Patent US 8,785,647
Granted Patent B2
US 8,785,647 · App. 13/829,353 · Granted Jul 22, 2014

Pesticidal arylpyrrolidines

Inventors: Ulrich Görgens (Ratingen, DE); Jun Mihara (Tochigi, JP); Tetsuya Murata (Tochigi, JP); Daiei Yamazaki (Tochigi, JP); Yasushi Yoneta (Saitama, JP); Koichi Araki (Ibaraki, JP); Norio Sasaki (Ibaraki, JP); Kei Domon (Tochigi, JP); Mamoru Hatazawa (Ibaraki, JP); Eiichi Shimojo (Tochigi, JP); Teruyuki Ichihara (Tochigi, JP); Masashi Ataka (Ibaraki, JP); Katsuhiko Shibuya (Tochigi, JP)
Assignee: Bayer Intellectual Property GmbH
C07D401/04A01N43/40
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 8,785,647
App. No.
13/829,353
Granted
Jul 22, 2014
Kind
B2
Abstract

The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the vield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.

Claims (64)

1. An arylpyrrolidine compound having the formula

or salts thereof,

wherein

A 1 represents C—Y 2-4 or nitrogen;

X 1 , X 2-1 , X 2-2 , X 2-3 and X 2-4 each independently represents hydrogen, halogen, nitro, cyano, hydroxy, mercapto, amino, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, haloalkylsulfanyl, haloalkylsulfinyl, haloalkylsulfonyl, acylamino, alkoxycarbonylamino, haloalkoxycarbonylamino, alkoxyimino, haloalkoxyimino, alkylsulfonylamino, or pentafluorosulfur;

Y 2-1 , Y 2-3 , and Y 2-4 each independently represents hydrogen, halogen, nitro, cyano, hydroxy, mercapto, amino, alkyl, haloalkyl, cycloalkyl, cyclohaloalkyl, alkenyl, alkynyl, alkoxy, haloalkoxy, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, haloalkylsulfanyl, haloalkylsulfinyl, haloalkylsulfonyl, alkylsulfonyloxy, haloalkylsulfonyloxy, alkylaminosulfonyl, haloalkylaminosulfonyl, dialkylaminosulfonyl, di(haloalkyl)aminosulfonyl, alkylamino, dialkylamino, acylamino, alkoxycarbonylamino, haloalkoxycarbonylamino, alkylsulfonylamino, haloalkylsulfonylamino, trialkylsilyl, alkoxyimino, haloalkoxyimino, alkoxyiminoalkyl, haloalkoxyiminoalkyl, alkylsulfinylimino, alkylsulfinyliminoalkyl, alkylsulfinyliminoalkylcarbonyl, alkylsulfoxyimino, alkylsulfoxyiminoalkyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl, aminothiocarbonyl, alkylaminothiocarbonyl, dialkylaminocarbonyl, or dialkylaminothiocarbonyl;

R 3 and R 4 each independently represents hydrogen, cyano, alkyl, alkenyl, alkynyl, cycloalkyl or alkoxycarbonyl;

R 5-1 represents hydrogen, amino, hydroxy, cyano, alkyl, haloalkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, aminocarbonylalkyl, iminoalkyl, alkylcarbonyl, alkylcarbonylamino, alkylimino, aryl, aralkyl, a heterocycle, a heterocyclic ring substituted alkyl, R 7 —C(═O)—, or R 7 —C(═S)—;

R 6-1 represents C 3-6 cycloalkyl(C 1-4 )alkylcarbonyl, C 1-4 -alkoxy(C 1-4 )alkylcarbonyl, C 1-4 alkyl-S(C 1-4 )alkylcarbonyl, C 1-4 alkyl-SO(C 1-4 )alkylcarbonyl, C 1-4 alkyl-SO 2 (C 1-4 )alkylcarbonyl,

R 7 represents phenyl or a saturated or unsaturated heterocyclic ring.

2. The arylpyrrolidine compound of claim 1 , wherein

X 1 , X 2-1 , X 2-2 , X 2-3 and X 2 -4 each independently represents hydrogen, halogen or haloalkyl;

Y 2-1 , Y 2-3 , and Y 2-4 each independently represents hydrogen, halogen, alkyl, haloalkyl, alkoxy, cycloalkyl, haloalkoxy, alkylsulfonyl, or haloalkylsulfinyl;

R 3 , R 4 each independently represents hydrogen or alkyl;

R 5-1 represents hydrogen, alkyl, or haloalkyl; and

R 6-1 represents C 3-6 cycloalkyl(C 1-4 )alkylcarbonyl, C 1-4 alkoxy(C 1-4 )alkylcarbonyl, C 1-4 alkyl-S(C 1-4 )alkylcarbonyl, C 1-4 alkyl-SO(C 1-4 )alkylcarbonyl, C 1-4 alkyl-SO 2 (C 1-4 )alkylcarbonyl,

3. The arylpyrrolidine compound of claim 1 , wherein

X 1 , Y 2-1 , Y 2-2 , Y 2-3 and X 2-4 each independently represents hydrogen, halogen or C 1-4 -haloalkyl;

Y 2-1 , Y 2-3 , and Y 2-4 each independently represents hydrogen, halogen, C 1-4 -alkyl, C 1-4 -alkoxy, C 1-4 -haloalkoxy, C 3-6 -cycloalkyl, C 1-4 -haloalkyl, C 1-4 alkylsulfanyl, or C 1-4 -haloalkylsulfanyl;

R 3 or R 4 independently of each other represents hydrogen;

R 5-1 represents hydrogen, C 1-4 alkyl or C 1-4 -haloalkyl; and

R 6-1 is selected from the group consisting of

4. The arylpyrrolidine compound of claim 2 , wherein at least one of X 1 , X 2-1 , X 2-2 , X 2-3 and X 2-4 is hydrogen.

5. The arylpyrrolidine compound of claim 2 , wherein at least one of X 1 , X 2-2 , and X 2-4 is hydrogen.

6. The arylpyrrolidine compound of claim 2 , wherein X 1 and X 2-4 are hydrogen, and X 2-1 , X 2-2 , and X 2-3 each independently is selected from the group consisting of CF 3 , F, Cl, and Br.

7. An arylpyrrolidine compound having the formula

or salts thereof,

wherein

X 1 , X 2-1 , X 2-2 , X 2-3 and X 2-4 each independently represents hydrogen, halogen, nitro, cyano, hydroxy, mercapto, amino, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, haloalkylsulfanyl, haloalkylsulfinyl, haloalkylsulfonyl, acylamino, alkoxycarbonylamino, haloalkoxycarbonylamino, alkoxyimino, haloalkoxyimino, alkylsulfonylamino, or pentafluorosulfur;

Y 2-3 and Y 2-4 each independently represents hydrogen, halogen, nitro, cyano, hydroxy, mercapto, amino, alkyl, haloalkyl, cycloalkyl, cyclohaloalkyl, alkenyl, alkynyl, alkoxy, haloalkoxy, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, haloalkylsulfanyl, haloalkylsulfinyl, haloalkylsulfonyl, alkylsulfonyloxy, haloalkylsulfonyloxy, alkylaminosulfonyl, haloalkylaminosulfonyl, dialkylaminosulfonyl, di(haloalkyl)aminosulfonyl, alkylamino, dialkylamino, acylamino, alkoxycarbonylamino, haloalkoxycarbonylamino, alkylsulfonylamino, haloalkylsulfonylamino, trialkylsilyl, alkoxyimino, haloalkoxyimino, alkoxyiminoalkyl, haloalkoxyiminoalkyl, alkylsulfinylimino, alkylsulfinyliminoalkyl, alkylsulfinyliminoalkylcarbonyl, alkylsulfoxyimino, alkylsulfoxyiminoalkyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl, aminothiocarbonyl, alkylaminothiocarbonyl, dialkylaminocarbonyl, or dialkylaminothiocarbonyl;

R 3 and R 4 each independently represents hydrogen, cyano, alkyl, alkenyl, alkynyl, cycloalkyl or alkoxycarbonyl;

R 5-1 represents hydrogen, amino, hydroxy, cyano, alkyl, haloalkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, aminocarbonylalkyl, iminoalkyl, alkylcarbonyl, alkylcarbonylamino, alkylimino, aryl, aralkyl, a heterocycle, a heterocyclic ring substituted alkyl, R 7 —C(═O)—, or R 7 —C(═S)—;

R 6-1 represents C 3-6 cycloalkyl(C 1-4 )alkylcarbonyl, C 1-4 alkoxy(C 1-4 )alkylcarbonyl, C 1-4 alkyl-S(C 1-4 )alkylcarbonyl, C 1-4 alkyl-SO(C 1-4 alkylcarbonyl, C 1-4 alkyl-SO 2 (C 1-4 )alkylcarbonyl,

R 7 represents phenyl or a saturated or unsaturated heterocyclic ring.

8. The arylpyrrolidine compound of claim 7 , wherein

X 1 , X 2-1 , X 2-2 , X 2-3 and X 2-4 each independently represents hydrogen, halogen or haloalkyl;

Y 2-3 and Y 2-4 each independently represents hydrogen, halogen, alkyl, haloalkyl, alkoxy, cycloalkyl, haloalkoxy, alkylsulfonyl, or haloalkylsulfinyl;

R 3 and R 4 each independently represents hydrogen or alkyl;

R 5-1 represents hydrogen, alkyl, or haloalkyl; and

R 6-1 represents C 3-6 cycloalkyl(C 1-4 )alkylcarbonyl, C 1-4 alkoxy(C 1-4 )alkylcarbonyl, C 1-4 alkyl-S(C 1-4 )alkylcarbonyl, C 1-4 alkyl-SO(C 1-4 )alkylcarbonyl, C 1-4 alkyl-SO 2 (C 1-4 )alkylcarbonyl,

9. The arylpyrrolidine compound of claim 7 , wherein

X 1 , X 2-1 , X 2-2 , X 2-3 and X 2-4 each independently represents hydrogen, halogen or C 1-4 -haloalkyl;

Y 2-3 and Y 2-4 each independently represents hydrogen, halogen, C 1-4 -alkyl, C 1-4 -alkoxy, C 1-4 -haloalkoxy, C 3-6 -cycloalkyl, C 1-4 -haloalkyl, C 1-4 -alkylsulfanyl, or C 1-4 -haloalkylsulfanyl;

R 3 and R 4 independently of each other represents hydrogen;

R 5-1 represents hydrogen, C 1-4 alkyl or C 1-4 haloalkyl; and

R 6-1 is selected from the group consisting of

10. The arylpyrrolidine compound of claim 7 , wherein at least one of X 1 , X 2-1 , X 2-2 , X 2-3 and A 2-4 is hydrogen.

11. The arylpyrrolidine compound of claim 7 , wherein at least one of X 1 , X 2-2 , and X 2-4 is hydrogen.

12. The arylpyrrolidine compound of claim 7 , wherein X 1 and X 2-4 are hydrogen, and X 2-1 , X 2-2 , and X 2-3 each independently is selected from the group consisting of CF 3 , F, Cl, and Br.

13. A composition comprising one or more compounds selected from the compounds according to claim 1 and one or more diluents, emulsifiers, or a combination thereof.

14. A composition comprising one or more compounds selected from the compounds according to claim 3 and one or more diluents, emulsifiers, or a combination thereof.

15. A composition comprising one or more compounds selected from the compounds according to claim 7 and one or more diluents, emulsifiers, or a combination thereof.

16. A composition comprising one or more compounds selected from the compounds according to claim 9 and one or more diluents, emulsifiers, or a combination thereof.

17. A method for controlling plant damaging animal pests comprising applying the composition according to claim 13 or 14 to said pests, their habitat, or a combination thereof.

18. The method of claim 17 , wherein the composition according to claim 14 is applied to said pests, their habitat, or a combination thereof.

19. A method for controlling parasites in or on an animal comprising administering the composition according to claim 15 or 16 to said animal.

20. The method of claim 19 , wherein the composition according to claim 16 is applied to said animal.

21. A method for treating seeds of conventional or transgenic plants comprising administering the composition according to claim 13 or 14 to said seeds.

22. The method of claim 21 , wherein the composition according to claim 14 is applied to said seeds.

23. The arylpyrrolidine compound of claim 1 , wherein the compound is

24. The arylpyrrolidine compound of claim 1 , wherein the compound is

25. The arylpyrrolidine compound of claim 1 , wherein the compound is

26. The arylpyrrolidine compound of claim 1 , wherein the compound is

27. A composition comprising any of the compounds according to any of claims 23 - 26 and one or more diluents, emulsifiers, or a combination thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 18, 2014
From: BAYER CROPSCIENCE AG
To: BAYER INTELLECTUAL PROPERTY GMBH
Reel/Frame 032233/0578 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 18, 2014
From: GORGENS, ULRICH; MIHARA, JUN; MURATA, TETSUYA; YAMAZAKI, DAIEI; YONETA, YASUSHI; ARAKI, KOICHI; SASAKI, NORIO; DOMON, KEI; HATAZAWA, MAMORU; SHIMOJO, EIICHI; ICHIHARA, TERUYUKI; ATAKA, MASASHI; SHIBUYA, KATSUHIKO
To: BAYER CROPSCIENCE AG
Reel/Frame 032233/0617 →
Priority Claims (2)
JP 2008-268729 · Oct 17, 2008 · national
JP 2009-111390 · Apr 30, 2009 · national
Continuity (2)
Continuation 12588411 · Oct 14, 2009
Related Publication 20130310408A1 · Nov 21, 2013