Benzene compounds
First Claim
Patent Images
1. A compound of formula (I-I), a pharmaceutically acceptable salt thereof, or a solvate thereof:
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Accused Products
Abstract
The present invention provides novel benzene compounds presented by the following formulas, and analogs thereof, that exert an ACC activity-inhibiting effect that is effective in the treatment of obesity, hyperlipemia, fatty liver, hyperglycemia, impaired glucose tolerance, diabetes, diabetic complications (diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, and diabetic macroangiopathy, hypertension, arteriosclerosis), hypertension, and arteriosclerosis.
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Citations
40 Claims
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1. A compound of formula (I-I), a pharmaceutically acceptable salt thereof, or a solvate thereof:
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 15)
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2. A method for preventing and/or treating hyperlipemia, comprising administering to a subject in need thereof an effective amount of a compound according to claim 1, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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3. A method for preventing and/or treating fatty liver, comprising administering to a subject in need thereof an effective amount of a compound according to claim 1, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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4. A method for preventing and/or treating hyperglycemia, comprising administering to a subject in need thereof an effective amount of a compound according to claim 1, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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5. A method for preventing and/or treating, impaired glucose tolerance or diabetes, comprising administering to a subject in need thereof an effective amount of a compound according to claim 1, a pharmaceutically acceptable salt thereof or a solvate thereof.
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6. A method for preventing and/or treating diabetic complications, comprising administering to a subject in need thereof an effective amount of a compound according to claim 1, a pharmaceutically acceptable salt thereof, or a solvate thereof;
wherein said diabetic complications represent diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, hypertension, or arteriosclerosis.
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7. A method for preventing and/or treating hypertension or arteriosclerosis, comprising administering to a subject in need thereof an effective amount of a compound according to claim 1, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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8. A method for preventing and/or treating obesity, hyperlipemia, fatty liver, impaired glucose tolerance, diabetes, diabetic complications, hypertension, arteriosclerosis, or hyperglycemia, comprising administering to a subject in need thereof an effective amount of i) a compound according to claim 1, a pharmaceutically acceptable salt thereof, or a solvate thereof, and ii) any one or two of drugs which is selected from the group consisting of insulin, sulfonylurea agents, α
- -glucosidase inhibitors, biguanide agents, PPAR-γ
agonists, PPAR-γ
antagonists, PPAR-α
agonists, SGLT inhibitors, GLP-1 receptor agonists, DPP-IV inhibitors, aldose reductase inhibitors, anti-diabetic neuropathy drugs, HMG-CoA reductase inhibitors, antioxidants, calcium antagonists, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, beta blockers, α
1 blockers, diuretics, anti-obesity drugs, and low energy foods;
wherein said diabetic complications represent diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, hypertension, or arteriosclerosis.
- -glucosidase inhibitors, biguanide agents, PPAR-γ
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9. A pharmaceutical composition comprising i) a compound according to claim 1, a pharmaceutically acceptable salt thereof, or a solvate thereof, and ii) a pharmaceutical acceptable carrier.
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10. A pharmaceutical composition comprising i) a compound according to claim 1, a pharmaceutically acceptable salt thereof, or a solvate thereof, and ii) any one or two of drugs which is selected from the group consisting of insulin, sulfonylurea agents, α
- -glucosidase inhibitors, biguanide agents, PPAR-γ
agonists, PPAR-γ
antagonists, PPAR-α
agonists, SGLT inhibitors, GLP-1 receptor agonists, DPP-IV inhibitors, aldose reductase inhibitors, anti-diabetic neuropathy drugs, HMG-CoA reductase inhibitors, antioxidants, calcium antagonists, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, beta blockers, α
1 blockers, diuretics, anti-obesity drugs, and low energy foods.
- -glucosidase inhibitors, biguanide agents, PPAR-γ
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15. A method for preventing and/or treating impaired glucose tolerance or diabetes, comprising administering to a subject in need thereof an effective amount of a compound according to claim 1, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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2. A method for preventing and/or treating hyperlipemia, comprising administering to a subject in need thereof an effective amount of a compound according to claim 1, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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11. A compound of formula (I-II), a pharmaceutically acceptable salt thereof, or a solvate thereof:
- View Dependent Claims (12, 13, 14, 16, 17, 18, 19, 20)
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12. A method for preventing and/or treating hyperlipemia, comprising administering to a subject in need thereof an effective amount of a compound according to claim 11, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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13. A method for preventing and/or treating fatty liver, comprising administering to a subject in need thereof an effective amount of a compound according to claim 11, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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14. A method for, preventing and/or treating hyperglycemia, comprising administering to a subject in need thereof an effective amount of a compound according to claim 11, a pharmaceutically acceptable salt thereof;
- or a solvate thereof.
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16. A method for preventing and/or treating diabetic complications, comprising administering to a subject in need thereof an effective amount of a compound according to claim 11, a pharmaceutically acceptable salt thereof, or a solvate thereof;
wherein said diabetic complications represent diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, hypertension, or arteriosclerosis.
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17. A method for preventing and/or treating hypertension or arteriosclerosis, comprising administering to a subject in need thereof an effective amount of a compound according to claim 11, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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18. A method for preventing and/or treating obesity, hyperlipemia, fatty liver, impaired glucose tolerance, diabetes, diabetic complications, hypertension, arteriosclerosis, or hyperglycemia, comprising administering to a subject in need thereof an effective amount of i) a compound according to claim 11, a pharmaceutically acceptable salt thereof, or a solvate thereof, and ii) any one or two of drugs which is selected from the group consisting of insulin, sulfonylurea agents, α
- -glucosidase inhibitors, biguanide agents, PPAR-γ
agonists, PPAR-γ
antagonists, PPAR-α
agonists, SGLT inhibitors, GLP-1 receptor agonists, DPP-IV inhibitors, aldose reductase inhibitors, anti-diabetic neuropathy drugs, HMG-CoA reductase inhibitors, antioxidants, calcium antagonists, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, beta blockers, α
1 blockers, diuretics, anti-obesity drugs, and low energy foods;
wherein said diabetic complications represent diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, hypertension, or arteriosclerosis.
- -glucosidase inhibitors, biguanide agents, PPAR-γ
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19. A pharmaceutical composition comprising i) a compound according to claim 11, a pharmaceutically acceptable salt thereof, or a solvate thereof, and ii) a pharmaceutical acceptable carrier.
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20. A pharmaceutical composition comprising i) a compound according to claim 11, a pharmaceutically acceptable salt thereof, or a solvate thereof, and ii) any one or two of drugs which is selected from the group consisting of insulin, sulfonylurea agents, α
- -glucosidase inhibitors, biguanide agents, PPAR-γ
agonists, PPAR-γ
antagonists, PPAR-α
agonists, SGLT inhibitors, GLP-1 receptor agonists, DPP-IV inhibitors, aldose reductase inhibitors, anti-diabetic neuropathy drugs, HMG-CoA reductase inhibitors, antioxidants, calcium antagonists, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, beta blockers, α
1 blockers, diuretics, anti-obesity drugs, and low energy foods.
- -glucosidase inhibitors, biguanide agents, PPAR-γ
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12. A method for preventing and/or treating hyperlipemia, comprising administering to a subject in need thereof an effective amount of a compound according to claim 11, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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21. A compound of formula (1A-III), (1B-III), (1C-III), or (1D-III), a pharmaceutically acceptable salt thereof, or a solvate thereof:
- View Dependent Claims (22, 23, 24, 25, 26, 27, 28, 29, 30)
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22. A method for preventing and/or treating hyperlipemia, comprising administering to a subject in need thereof an effective amount of a compound according to claim 21, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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23. A method for preventing and/or treating fatty liver, comprising administering to a subject in need thereof an effective amount of a compound according to claim 21, a pharmaceutically acceptable salt thereof or a solvate thereof.
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24. A method for preventing and/or treating hyperglycemia, comprising administering to a subject in need thereof an effective amount of a compound according to claim 21, a pharmaceutically acceptable salt thereof or a solvate thereof.
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25. A method for preventing and/or treating impaired glucose tolerance or diabetes, comprising administering to a subject in need thereof an effective amount of a compound according to claim 21, a pharmaceutically acceptable salt thereof or a solvate thereof.
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26. A method for preventing and/or treating diabetic complications, comprising administering to a subject in need thereof an effective amount of a compound according to claim 21, a pharmaceutically acceptable salt thereof, or a solvate thereof;
wherein said diabetic complications represent diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, hypertension, or arteriosclerosis.
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27. A method for preventing and/or, treating hypertension or arteriosclerosis, comprising administering to a subject in need thereof an effective amount of a compound according to claim 21, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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28. A method for preventing and/or treating obesity, hyperlipemia, fatty liver, impaired glucose tolerance, diabetes, diabetic complications, hypertension, arteriosclerosis, or hyperglycemia, comprising administering to a subject in need thereof an effective amount of i) a compound according to claim 21, a pharmaceutically acceptable salt thereof, or a solvate thereof, and ii) any one or two of drugs which is selected from the group consisting of insulin, sulfonylurea agents, α
- -glucosidase inhibitors, biguanide agents, PPAR-γ
agonists, PPAR-γ
antagonists, PPAR-α
agonists, SGLT inhibitors, GLP-1 receptor agonists, DPP-IV inhibitors, aldose reductase inhibitors, anti-diabetic neuropathy drugs, HMG-CoA reductase inhibitors, antioxidants, calcium antagonists, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, beta blockers, α
1 blockers, diuretics, anti-obesity drugs, and low energy foods;
wherein said diabetic complications represent diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, hypertension, or arteriosclerosis.
- -glucosidase inhibitors, biguanide agents, PPAR-γ
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29. A pharmaceutical composition comprising i) a compound according to claim 21, a pharmaceutically acceptable salt thereof, or a solvate thereof, and ii) a pharmaceutical acceptable carrier.
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30. A pharmaceutical composition comprising i) a compound according to claim 21, a pharmaceutically acceptable salt thereof, or a solvate thereof, and ii) any one or two of drugs which is selected from the group consisting, of insulin, sulfonylurea agents, α
- -glucosidase inhibitors, biguanide agents, PPAR-γ
agonists, PPAR-γ
antagonists, PPAR-α
agonists, SGLT inhibitors, GLP-1 receptor agonists, DPP-IV inhibitors, aldose reductase inhibitors, anti-diabetic neuropathy drugs, HMG-CoA reductase inhibitors, antioxidants, calcium antagonists, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, beta blockers, α
1 blockers, diuretics, anti-obesity drugs, and low energy foods.
- -glucosidase inhibitors, biguanide agents, PPAR-γ
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22. A method for preventing and/or treating hyperlipemia, comprising administering to a subject in need thereof an effective amount of a compound according to claim 21, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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31. A compound of formula (1A-IV), a pharmaceutically acceptable salt thereof, or a solvate thereof:
- View Dependent Claims (32, 33, 34, 35, 36, 37, 38, 39, 40)
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32. A method for preventing and/or treating hyperlipemia, comprising administering to a subject in need thereof an effective amount of a compound according to claim 31, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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33. A method for preventing and/or treating fatty liver, comprising administering to a subject in need thereof an effective amount of a compound according to claim 31, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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34. A method for preventing and/or treating hyperglycemia, comprising administering to a subject in need thereof an effective amount of a compound according to claim 31, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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35. A method for preventing and/or treating impaired glucose tolerance or diabetes, comprising administering to a subject in need thereof an effective amount of a compound according to claim 31, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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36. A method for preventing and/or treating diabetic complications, comprising administering to a subject in need thereof an effective amount of a compound according to claim 31, a pharmaceutically acceptable salt thereof, or a solvate thereof,
wherein said diabetic complications represent diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, hypertension, or arteriosclerosis. -
37. A method for preventing and/or treating hypertension or arteriosclerosis, comprising administering to a subject in need thereof an effective amount of a compound according to claim 31, a pharmaceutically acceptable salt thereof, or a solvate thereof.
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38. A method for preventing and/or treating obesity, hyperlipemia, fatty liver, impaired glucose tolerance, diabetes, diabetic complications, hypertension, arteriosclerosis, or hyperglycemia, comprising administering to a subject in need thereof an effective amount of i) a compound according to claim 31, a pharmaceutically acceptable salt thereof, or a solvate thereof, and ii) any one or two of drugs which is selected from the group consisting of insulin, sulfonylurea agents, α
- -glucosidase inhibitors, biguanide agents, PPAR-γ
agonists, PPAR-γ
antagonists, PPAR-α
agonists, SGLT inhibitors, GLP-1 receptor agonists, DPP-IV inhibitors, aldose reductase inhibitors, anti-diabetic neuropathy drugs, HMG-CoA reductase inhibitors, antioxidants, calcium antagonists, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, beta blockers, α
1 blockers, diuretics, anti-obesity drugs, and low energy foods;
wherein said diabetic complications represent diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, hypertension, or arteriosclerosis.
- -glucosidase inhibitors, biguanide agents, PPAR-γ
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39. A pharmaceutical composition comprising i) a compound according to claim 31, a pharmaceutically acceptable salt thereof, or a solvate thereof;
- and ii) a pharmaceutical acceptable carrier.
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40. A pharmaceutical composition comprising a combination of i) a compound according to claim 31, a pharmaceutically acceptable salt thereof, or a solvate thereof, and ii) any one or two of drugs which is selected from the group consisting of insulin, sulfonylurea agents, α
- -glucosidase inhibitors, biguanide agents, PPAR-γ
agonists, PPAR-γ
antagonists, PPAR-α
agonists, SGLT inhibitors, GLP-1 receptor agonists, DPP-IV inhibitors, aldose reductase inhibitors, anti-diabetic neuropathy drugs, HMG-CoA reductase inhibitors, antioxidants, calcium antagonists, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, beta blockers, α
1 blockers, diuretics, anti-obesity drugs, and low energy foods.
- -glucosidase inhibitors, biguanide agents, PPAR-γ
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32. A method for preventing and/or treating hyperlipemia, comprising administering to a subject in need thereof an effective amount of a compound according to claim 31, a pharmaceutically acceptable salt thereof, or a solvate thereof.
Specification
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Current AssigneeAjinomoto Co., Inc.
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Original AssigneeAjinomoto Co., Inc.
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InventorsNakanishi, Eiji, Kondo, Nobuo, Tanaka, Hideyuki, Hatanaka, Toshihiro, Masuzawa, Yoko, Nihei, Yukio, SUZUKI, Nobuyasu, Yasa, Noriko, Ichinose, Hidehiro
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Granted Patent
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Time in Patent OfficeDays
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Field of Search
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US Class Current514/312
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CPC Class CodesA61K 31/167 having the nitrogen of a ca...A61K 31/18 Sulfonamides compounds cont...A61K 31/192 having aromatic groups, e.g...A61K 31/194 having two or more carboxyl...A61K 31/198 Alpha-amino acids, e.g. ala...A61K 31/216 of acids having aromatic ri...A61K 31/341 not condensed with another ...A61K 31/381 having five-membered ringsA61K 31/402 1-aryl substituted, e.g. pi...A61K 31/4035 Isoindoles, e.g. phthalimideA61K 31/4245 OxadiazolesA61K 31/4402 only substituted in positio...A61K 31/4409 only substituted in positio...A61K 31/4439 containing a five-membered ...A61K 31/445 Non condensed piperidines, ...A61K 31/455 Nicotinic acids, e.g. niaci...A61K 31/47 Quinolines; IsoquinolinesA61K 31/4709 Non-condensed quinolines an...A61K 31/473 ortho- or peri-condensed wi...A61K 31/496 Non-condensed piperazines c...A61K 31/501 : not condensed and containin...A61K 31/502 : ortho- or peri-condensed wi...A61K 31/5377 : not condensed and containin...A61K 31/551 : having two nitrogen atoms, ...A61P 1/16 : for liver or gallbladder di...A61P 13/12 : of the kidneysA61P 25/02 : for peripheral neuropathiesA61P 27/02 : Ophthalmic agentsA61P 3/06 : AntihyperlipidemicsA61P 3/10 : for hyperglycaemia, e.g. an...A61P 43/00 : Drugs for specific purposes...A61P 9/00 : Drugs for disorders of the ...A61P 9/10 : for treating ischaemic or a...A61P 9/12 : AntihypertensivesA61P 9/14 : Vasoprotectives; Antihaemor...C07C 233/66 : having the nitrogen atom of...C07C 2601/02 : with a three-membered ringC07C 2601/04 : with a four-membered ringC07C 2601/08 : the ring being saturatedC07C 2601/14 : The ring being saturatedC07C 2603/24 : Anthracenes; Hydrogenated a...C07C 275/30 : being further substituted b...C07C 311/16 : having the nitrogen atom of...C07C 311/21 : having the nitrogen atom of...C07C 311/51 : Y being a hydrogen or a car...C07D 207/452 : with hydrocarbon radicals, ...C07D 209/48 : with oxygen atoms in positi...C07D 215/48 : Carbon atoms having three b...C07D 235/18 : with aryl radicals directly...C07D 271/06 : 1,2,4-Oxadiazoles; Hydrogen...C07D 277/28 : Radicals substituted by nit...C07D 277/30 : Radicals substituted by car...C07D 413/04 : directly linked by a ring-m...C07D 413/14 : containing three or more he...C07D 417/04 : directly linked by a ring-m...C07D 417/10 : linked by a carbon chain co...C07F 9/65318 : having the two nitrogen ato...