Sulfonylureas and method of controlling undesirable vegetation

 

(57) Abstract:

Usage: in agriculture, in particular as a herbicide funds. The inventive product is substituted sulfonylureas f-ly 1, where Q is the group CH CH or S; R group; C1-C3alkyl group and X; OCH3or CH3or its applicable agricultural salt. The method of controlling undesirable vegetation are using the specified connection f-crystals of 1 in the amount of 0.25 to 1 g/ar. The compound of the formula I 2 s and 12 C. p. F.-ly, 10 PL.

The invention relates to new compounds useful as herbicides, and to their use in weed control in the cultivation of fine-grained cereals.

More specifically the invention relates to herbicide compounds having selectively regulating action in the presence of many valuable fine-grained cereals, such as wheat, barley, oats and rye.

Compounds according to the invention can be used to control undesirable vegetation, such as grass weeds such as Alopecurus myservername (Alopecurus myosuroides), or fire roofing (Bromus tectorum 1).

Derivative sulfonyl the vegetation in the presence of many valuable fine-grained cereals, such as wheat, barley, oats and rye.

Various synthetic compounds sulfonylureas, have a weed-killing activity described in patent applications laid Japan N 162587/1983 and 45572/1985, and in tiled applications Europatent 96003, 152286 and 238070. Some compounds used as herbicides in the cultivation of grain crops, are commercially available (for example, Cleantn, AllyTMHarmonyTM, AmbetTMand so on).

Although such connections sulfonylation have a strong herbicide effect on broadleaf weeds in extremely low concentrations, however, they are still not satisfactory in practice because they do not have or have only a very weak herbicide activity against grass weeds in terms of their selective use in crops of wheat.

So currently, however, there is still the development of a new herbicide with sufficient herbicide activity against cereal weeds, and at the same time not adversely impact on fine-grained culture.

One aspect of the invention is to develop a new herbicide with preferred instrument is the object of the invention is to provide a new herbicide, with a strong herbicide activity against cereal weeds, in particular, against Alopecurus myservicename and fire the roof, as well as a wide range of other weeds, without adverse effects on many valuable fine-grain crops such as wheat, oats, barley and rye. These herbicides are designed for use in combating unwanted vegetation when growing fine crops such as wheat, barley, oats and rye, and especially wheat.

As a result of extensive studies, it was found that the compounds of formula I and their agricultural acceptable salts possess unexpectedly strong herbicide activity against a wide range of noxious weeds, which includes not only broad-leaved weeds, such as cleaver (Garium aparine), chamomile pharmaceutical. (Matricaria chamomilla), wild Pansy (Viola tricolor), starwort common (Stellaria media), wild mustard (Sihapis arevensis I.) and Highlander vjunkovye (Polygonum convolvulus I. ), but also cereal weeds such as Alopecurus myservername, wild oat (Avenatata I. ), roofing and fire spickle green (Setaria viridis); and mainly do not have a toxic effect on fine-grained cult of the new weeds (e.g. Alopecurus myservername, the fire roofing, chamomile, white mustard, and starwort), and especially against Alopecurus myservicename and fire the roof.

The invention relates to compounds of the formula I

CH3where Q is-CH= CH - or-S-; R C1-C3-alkyl; and X co3or CH3or agricultural acceptable salts of its agronomically acceptable salts.

Additionally, the invention relates to a method of controlling undesirable vegetation when growing fine crops, namely, that on these plants put herbicide effective amount of the compounds of formula I or its selskohozjajstvenno acceptable salt.

In the above formula WITH1-C3the alkyl in the definition of R means alkyl straight or branched chain such as methyl, ethyl, n-propyl, isopropyl, etc., Preferred examples of alkyl are methyl and ethyl, and more preferred is ethyl.

X represents methoxy or methyl, more preferably methoxy;

Q is-C=CH= or-S-, more preferably-CH=CH-.

Compound I has an acid group-SOCO Connection I can form a salt with neorganicheskoy salts with inorganic bases, such as alkali metals (e.g. magnesium, calcium, etc), and ammonia, organic bases, such as diethylamine, triethylamine, pyrrolidine, piperidine, piperazine, morpholine, benzylamine, ethanolamine and diethanolamine.

The compounds I or their agricultural acceptable salts can be used as herbicides in the form of any of the forms suitable for conventional agricultural chemicals. For these purposes may be prepared herbicide composition containing an effective amount of compound I or its agricultural acceptable salt and agricultural acceptable filler, by mixing the compounds or salts thereof with a filler comprising a solid carriers, liquid, etc., for Example one or more of the above compounds I and their agricultural acceptable salts can dissolve or dispergirujutsja in the relevant agricultural acceptable liquid or solid carrier, or mixed or adsorbed on a suitable agricultural acceptable carrier, for example, hard copy, depending on the purpose of their use, with the formation of a suitable finished formulation or preparation, such as emulge is prone to drift with the wind), suspension concentrate, granules, microspheres F, granules, for example, water-dispersible granules, tablets, liquids, sprays (compositions for spray or aerosols. Among them, preferred are wettable powder, emulsifiable concentrate, flowable dusty and granules. More preferred are wettable powder and emulsifiable concentrate. These forms can be obtained by standard methods known in themselves. These forms, if necessary, may contain an emulsifier, suspendisse agent, spray tool, agent, penetration, wetting agent, thickener, sliseobrazutee agent, stabilizer, etc.

Suitable examples of liquid fillers or carriers (solvents are water, alcohols (e.g. methanol, ethanol, n-propanol, isopropanol, ethylene glycol, etc.,), ketones (e.g. acetone, methyl ethyl ketone, etc.), ethers (e.g. dioxane, tetrahydrofuran, onomatology ether of ethylene glycol, onomatology ether of diethylene glycol, onomatology ether of propylene glycol, etc.,), aliphatic hydrocarbons (e.g. kerosene, snow oil, fuel oil, machine oil, etc., aromatic hydrocarbons (e.g. benzene, toluene, K, carbon tetrachloride, etc.), acid amides (e.g. dimethylformamide, dimethylacetamide, etc.), esters (e.g. ethyl acetate, butyl acetate, an ester of glycerin fatty acid), and NITRILES (e.g. acetonitrile, propionitrile, and so on ). These solvents can be used singly or in mixture of two or more ingredients in the appropriate proportions.

Examples of the solid carrier (diluent/filler) are vegetable powders (e.g. soybean meal, tobacco powder, wheat flour, sawdust, etc.), mineral powders (e.g. clays such as kaolin, bentonite, high-grade gypsum, talcum powder, such as powdered talc and agalmatolite powder; and silicas, such as diatomaceous earth and mica powder), alumina, sulfur powder and activated carbon. These solid carriers may be used alone or in mixture of two or more ingredients in the appropriate proportions.

Listed liquid or solid excipients (or carriers) can be used independently or in combination. The amount of filler may comprise up to 100 wt. with respect to the whole composition.

Surface-active substances (surfactants), which can apply the th agent, represent different Soaps and nonionic or anionic surfactants, such as alkylacrylate esters of polyoxyethylene [(for example, NoigenTMand E. A. 142TM, Dai-ichi Kogyo Seiyaku K. K.)] formaldehyde condensates alienologo ether of polyoxyethylene [(for example, Newcalgen E-300TM)]0 sulfates phenylphenolate ether of polyoxyethylene [(for example, Agrizol FL-2017TM)] special polyhydric polymers [for example, Agrizol FL-GATM)] akrilovye esters of polyoxyethylene [(e.g., NonalTM, The Toho Kadaki K. K.)] alkyl sulphates [(for example, Enal 10TMand Emal 40TM, Kao K. K.)] alkyl sulphonates [(for example, Neogenm and Neogen TTM, Dai-ichi Kogyo Seiyaku K. K. Neopellex, Kao K. K.)] esters of polyoxyethyleneglycol [(e.g., Nonipol 85TM, Nonipol 100TMand Nonipol 160TM, Sanyo Kasei K. K.)] esters of a polyhydric alcohol [(e.g., tween-20TMand tween-80TM, Kao K. K.)] the Amount of surfactant ranges from 0 to 50 wt% and preferably from 1 to 25 wt. from the whole composition.

The ratio of active ingredients in the herbicide composition depends on the purpose of its use. For example, in the case when used in emulsifiable concentrate, wettable powder, suspension concentrate, water soluble granules, it is okoe of microgranules, the microgranules F, etc., this concentration is about 0.05-10 wt. This concentration of active ingredients may vary depending on the application. Emulsifiable concentrate, wettable powder and flowable dusty spraying after dilution with water or another diluent (for example, in 100-100 000 times).

The exact dose of herbicide depends not only on the specific active ingredient, but also from the desired action (total or selective) of the season, place and method of application, grain crops, plant species, stage of growth, as well as parts of plants, which directly contacts the active ingredient. Preferably herbicide compound of the present invention is used in a quantity in the range of 0.05 to 20 g, and more preferably 0.1 to 5 g per 1 ar.

The connection according to the invention and containing herbicide composition, preferably, applied to plants by mixing them into the soil or spreading on the fields before sowing, by treating soils or fields to the germination of seeds by spraying the leaves and stems directly crops, etc. in areas planted with cereals.

Depending on the circumstances of the what michigami (for example, organochlorine fungicides, organic sulfur fungicides, azole fungicides, antibiotics, etc ), pesticides (for example, PYRETHROID insecticides, organophosphorus insecticides, urethane insecticides, etc.,), acaricides, nematicides, plant hormones, synergists, attractants, repellents, pigments, fertilizers and composts.

The compounds I and salts thereof can be obtained by methods known in themselves, for example, using the method described below according to the posted application Europatent N 238070 (published patent application Japan N 38091-1989).

O

where each group has the values defined above.

Compound II or its salt is usually subjected to interaction with the compound III or its salt in the presence of a base (for example, 1,8-diazabicyclo (5,4,0)undecene-7 (hereinafter referred DBU), triethylamine, and so on) in an inert solvent, such as acetonitrile and chloroform.

Or compound IV or its salt is subjected to interaction with the compound V or its salt in the same solvent.

Compounds II, IV and their salts can be obtained by methods described in Japanese laid patent 316370/1979.

< / BR>connections VII, VIII, IX, II or their salts can be used in the subsequent reaction without isolation and purification.

The original VI compounds and their salts can be obtained by or in accordance with the method described in laid a European patent application N 238070 (Japanese laid patent N 38091/1989).

< / BR>
where each group has the values defined above.

Compounds according to the invention have a high herbicide activity in extremely low concentrations against a wide range of weeds when exposed to grain crops. They do not have adverse effects on mammals, birds, fish and other organisms living in water, and can be used safely without polluting the environment.

Presents examples, working examples, and examples of tests are given to illustrate the invention and in no way limit its scope.

In comparative examples and examples of the preparation, as well as in the tables the following abbreviations are used:

with singlet; D. doublet; T. triplet; q Quartet; DD, double doublet; m, multiplet; Shir. wide; J: constant interaction; D dimethyl sulfoxide; ph is phenyl, wt. unless otherwise requested.

The ASS="ptx2">

6 Atitikimas (2,1-b)thiazole.

(a) To a suspension of sodium hydride (34.3 g, 60% in mineral oil) in dimethylformamide (1 l) was added drop by drop with 44.8 g of ethyl mercaptan during cooling, and the mixture was stirred 30 min at room temperature. To the resulting mixture in small amounts slowly added ethyl 6-methylimidazo (2,1-b)thiazole-5-carboxylate (197,8 g). After stirring for 3 hours at room temperature, the reaction mixture was poured into ice water (3 l), and precipitated crystals were separated by filtration, washed with water and dried, 161,3 g ethyl-6-atitikimas[(2,1-b) thiazole-5-carboxylate.

< / BR>
(b) To a solution of sodium hydroxide (414 g) in water (1.2 g) and ethanol (800 ml) was added 161,3 ethyl 6-atitikimas [2,1-b]thiazole-5-carboxylate, and the resulting mixture was heated at the temperature of reflux distilled for 1.5 hours and Then the ethanol is kept off, and the residue was diluted with water (2 l) and neutralized with hydrochloric acid (to pH 1). Precipitated crystals were separated by filtration and washed with water. The wet crystals were heated at 150aboutC for 30 minutes while heating the crystals formed of foamed oil. The oil was dissolved in chloroform (500 ml), washed with aqueous sodium bicarbonate solution and su is CLASS="ptx2">

NMR (CDCl3) of 1.28 (t, 3H); 2,92 (sq. 2H); 6,83 (d, 1H); 7,38 (d, 1H); of 7.48 (s, 1H).

Comparative example 2.

6-(n-Propylthio)imidazo[2,1-b]thiazole.

In accordance with the procedure described in comparative example 1, ethyl 6-methylimidazo(2,1-b)thiazole-5-carboxyla - one and n-propylmercaptan got oily target connection

NMR (CDCl3) : and 1.00 (t, 3H); 1,43-1,90 (m, 2H); is 2.88 (t, 2H); 6,83 (d, 1H); 7,38 (s, 1H); 7,47 (s,1H).

Comparative example 3.

6 Isopropylimidazole(2,1-b)thiazole.

In accordance with the procedure described in comparative example 1 was obtained oily target compound from ethyl 6-methylimidazo(2,1-b)thiazole-5-carboxyla - TA and isopropylparaben.

NMR (CDCl3): 1,30 (C, 6N); 3,15-the 3.65 (m, 1H); 6,85 (d, 1H); 7,38 (d, 1H); a 7.62 (s, 1H).

Comparative example 4.

2 Isopropylimidazole(1,2-a)Piri - DIN.

In accordance with the procedure described in comparative example 1 was obtained oily target compound from ethyl 2-methylimidazo(2,1-a)pyridine-3-carboxy - Lata and isopropylparaben.

< / BR>
Comparative example 5.

2 Atitikimas(1,2-a)pyridine-3-su - ltname

To a solution of 2-atitikimas(1,2-a)pyridine (36,0 g, tiled application patane (300 ml) at a temperature below the 50aboutC. After addition the mixture was heated under conditions of reflux distilled under stirring for 7 h, and then cooled, followed by adding triethylamine (27,0 g). The resulting mixture was stirred at room temperature for 30 min, and then heated. Under conditions of reflux distilled was added dropwise phosphorus oxychloride (37,2 g). The resulting mixture was continued to stir for 1.5 hours After cooling, the reaction mixture was washed with water, and a layer of dichloroethane was concentrated in vacuum. The residue was dissolved in acetonitrile (300 ml), and after adding aqueous ammonia (50 ml), cooled to 10-20aboutWith was stirred at room temperature for 1 h

The reaction mixture was concentrated in vacuo to approximately half volume, and the precipitated crystals were collected by filtration, washed with water and dried, 29,1 g (yield of 56.4%) of target compound as white crystals.

so pl. 169-171aboutC.

NMR (DMCO-d6) : of 1.35 (t, 3H); 3,20 (sq. 2H); 7,05-7,25 (m, 1H); 7,39-of 7.60 (m, 1H); 7,66 (d, 1H); of 7.75 (s, 2H); at 8.60 (d, 1H).

According to the method similar to that described in comparative example 5 were obtained sulfonamidnuyu compounds are presented in table.1 and 2.

Comparative example 6.

2-Ethylal is 0 g) in dimethylformamide (300 ml) was added 45,0 g of m-chloroperbenzoic acid at 5-20aboutWith cooling, and the mixture was stirred at the same temperature for 3 hours

Then the mixture was poured into ice water (1.5 l) and the precipitated crystals were collected by filtration. The wet crystals were added to aqueous solution of sodium bisulfate (500 ml, NaHSO3, 1.0 g), was stirred at room temperature for 30 min, separated by filtration, washed with aqueous sodium carbonate and then water, and dried, obtaining of 20.8 g (yield of 68.6%) of target compound as white crystals.

so pl. 190-192aboutWITH

NMR (DMCO-d6) : of 1.23 (t, 3H); 3,62 (sq. 2H); 7,30-7,58 (m, 1H); 7,60 is 7.85 (m, 1H); to 7.95 (d, 1H); 7,98 (s, 2H); 9,0 (d, 1H).

In the manner similar to that described in comparative example 6, were obtained sulfonamide compounds are presented in table.3 and 4.

An example of retrieving I.

N-(2-Ethylsulfonyl [1,2-a] pyridine-3-ylsulphonyl)-N- (4,6-dimethoxy-2-pyrimidyl)urea (compound 2).

To a suspension of 2-ethylsulfonyl[1,2-a]pyridine-3-sulfonamida (20.5 g) and phenyl N-(4,6-dimethoxypyrimidine-2-yl)carbamate (20,0 g) in 250 ml of acetonitrile under ice cooling was added (11,0 g), and the resulting mixture was stirred 3 h at room temperature.

Then the mixture was poured into water (2 l), neutral is, receiving 28.6 g (yield of 91.3%) of target compound as white crystals.

so pl. 197-199aboutWITH

NMR (DMCO-d6) : of 1.29 (t, 3H); 3,23 (sq. 2H); 3,95 (C, 6N); 5,96 (s, 1H); 7,11-7,31 (m, 1H); 7,47-7,81 (m, 2H); of 8.92 (d, 1H); 10,51 (s, 1H); 12,91 (C. 1H).

In accordance with the procedure described in Example receipt I received connection sulfonylureas, are presented in table.5 and 6.

Example test I.

Selectivity for wheat (pre-emergence treatment).

Pots with a diameter of 10 cm was filled with soil (about 300 g, sterilized by steam) and the corresponding individual pots were planted 20 seeds of weeds (including 10 seeds of white mustard) and 10 wheat seeds, and then covered by soil layer thickness of about 1 cm Then on the soil surface of each pot was sprayed diluted compositions containing the compound (1), in quantities of 1 or 0.25 g on ar (0.01 ha).

Each connection (1 or 0.25 g) used in the test series, was dissolved in a solution of acetone (500 ml) containing 2 wt./about. Tween-20TM(SAS) and was diluted with water to a final volume of 5 l

4 weeks after herbicide treatment and the toxic effect of the relevant subjects of the ingredients in the appropriate groups of plants assessing bodily in the greenhouse. The degree of growth inhibition and adverse effects were evaluated according to the following scale (this scale was also used in the example test 2). The data are given in table.7 and 8

Example of test 2.

Selectivity for wheat (post-harvest processing).

In separate pots (10 cm in diameter) filled with soil (about 300 g, steam sterilized) were planted 20 seeds of weeds (including 10 seeds of white mustard) and 10 wheat seeds, and covered the top soil layer thickness of about 1 cm Then, when cereal weeds have reached the stage of development of 1-1,5 leaf and broadleaf weeds have reached the stage from 2 to 6 leaves in each pot was left 10 of the same seedlings, and the rest were removed (except mustard wild, where he left 5 seedlings). When the wheat has reached the stage of 2-3 leaves, each pot was left on 5 plants. Then the seedlings in each pot was sprayed compositions with test compounds (1) when the consumption rate in an amount of from 1 to 0.25 g on ar.

Each connection (1 or 0.25 g) used in the test series, was dissolved in acetone (500 ml) containing 2 wt./about. Tween-20TM(SAS), and was diluted with water to 5 l 4 weeks after treatment, herbicide and harmful damage to cnym described in example test 1. The results are presented in table.10. The tests were carried out in a greenhouse with controlled temperature.

1. Sulfonylureas of the General formula

< / BR>
where Q is-CH=CH - or S -;

R1WITH3-alkyl;

X group-och3or-CH3,

or agricultural acceptable salt.

2. Connection on p. 1 of General formula

< / BR>
where R1WITH3-alkyl;

X CO3or CH3,

or agricultural acceptable salt.

3. Connection on p. 2, where X och3.

4. Connection on p. 2, where R is methyl or ethyl, X och3.

5. Connection on p. 1 of General formula

< / BR>
where R1WITH3-alkyl;

X CO3or CH3,

or agricultural acceptable salt.

6. Connection on p. 5, where X is methoxy.

7. Connection on p. 5, where R is methyl or ethyl, X is methoxy.

8. Connection on p. 1 formula

< / BR>
or agricultural acceptable salt.

9. Connection on p. 1 formula

< / BR>
or agricultural acceptable salt.

10. The compound according to any one of paragraphs.1 9, useful as a herbicide.

11. The method of controlling undesirable vegetation by cobraboy used as a compound of General formula

< / BR>
where Q CH=CH - or S -;

R1WITH3-alkyl;

X is methoxy or methyl,

or agricultural acceptable salt at the rate of 0.25 to 1.0 g/ar.

12. The method according to p. 11, characterized in that is used as a compound of the formula

< / BR>
or agricultural acceptable salt.

13. The method according to p. 11, characterized in that is used as a compound of the formula

< / BR>
or agricultural acceptable salt.

14. The method according to p. 11, wherein the treatment is carried out in the wheat fields.

 

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FIELD: organic chemistry, chemical technology, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of piperazinylalkylthiopyrimidine of the formula (I): wherein R1 represents hydrogen atom, (C1-C4)-alkyl, (C1-C4)-alkanoyl or di-(C1-C4-alkyl)-amino-(C1-C4-alkyl); R2 means hydrogen atom or benzyl substituted with 1-3 substitutes taken among the group consisting of (C1-C4)-alkyl, (C1-C4)-alkoxy-group, di-(C1-C4-alkyl)-amino-group, hydroxyl group and halogen atom; n = 2, 3 or 4, and to its pharmaceutically acceptable acid addition salt. Also, invention describes a method for preparing compounds and pharmaceutical composition based on thereof. Compounds are useful for treatment of diseases arising as result of the central nervous system injury.

EFFECT: improved preparing method, valuable medicinal properties of compounds.

14 cl, 3 tbl, 26 ex

FIELD: organic chemistry, heterocyclic compounds, medicine, pharmacy.

SUBSTANCE: invention relates to nitrogen-containing heterocyclic derivatives of the formula (I): A-B-D-E (I) wherein A means 5- or 6-membered heteroaryl comprising one or two nitrogen atoms in ring; B means ethenylene; D mean phenylene; E means group -N(COR)-SO2-G wherein G means phenyl; R means 5- or 6-membered heteroaryl or heteroarylmethyl comprising one or two nitrogen atoms in ring, or group -(CH2)n-N(R5)R6 wherein n means a whole number from 1 to 5; R5 and R6 are similar or different and mean: hydrogen atom, (C1-C6)-alkyl, hydroxyalkyl, aminoalkyl; or R5 and R6 in common with nitrogen atom can form 5-7-membered cyclic amino-group -N(R5)R6 that can comprise, except for nitrogen atom, also oxygen, sulfur or nitrogen atom as a component forming the ring, or their N-oxides. Compounds of the formula (I) elicit anticancer activity and can be used in medicine.

EFFECT: valuable medicinal properties of compounds.

10 cl, 1 tbl, 24 ex

FIELD: organic chemistry, biochemistry, pharmacy.

SUBSTANCE: invention relates to new compounds of the formula (I):

eliciting inhibitory activity with respect to metalloproteinases and wherein R1 means phenoxy-group wherein phenyl residue can be substituted with one or some halogen atoms, hydroxy-, (C1-C6)-alkoxy-group, (C1-C6)-alkyl, cyano- or nitro-group; R2 means pyrimidine, pyrazine or its N-oxide or phenyl substituted with -SO2NR3R4 wherein R3 and R4 can be similar or different and mean hydrogen atom, direct-chain or branch-chain (C1-C6)-alkyl that can be substituted once or some times with the group OH, N(CH3)2, or it can be broken by oxygen atom, or it represents COR5 wherein R5 means (C1-C)-alkyl group that can be substituted with NH2. Also, invention relates to a pharmaceutical composition comprising above said compounds.

EFFECT: valuable biochemical properties of compounds and composition.

5 cl, 1 sch, 1 tbl, 10 ex

FIELD: organic chemistry, pharmaceutical composition.

SUBSTANCE: new isoindoline-1-on-glucokinase activators of general formula I , as well as pharmaceutically acceptable salts or N-oxide thereof are disclosed. In formula A is phenyl optionally substituted with one or two halogen or one (law alkyl)sulfonyl group, or nitro group; R1 is C3-C9cycloalkyl; R2 is optionally monosubstituted five- or six-membered heterocyclic ring bonded via carbon atom in cycle to amino group, wherein five- or six-membered heteroaromatic ring contains one or two heteroatoms selected form sulfur, oxygen or nitrogen, one of which is nitrogen atom adjacent to carbon atom bonded to said amino group; said cycle is monocyclic or condensed with phenyl via two carbon atoms in cycle; said monosubstituted with halogen or law alkyl heteroaromatic ring has monosubstituted carbon atom in cycle which in not adjacent to carbon atom bonded to amino group; * is asymmetric carbon atom. Claimed compounds have glucokinase inhibitor activity and useful in pharmaceutical composition for treatment of type II diabetes.

EFFECT: new isoindoline-1-on-glucokinase activators useful in treatment of type II diabetes.

23 cl, 3 dwg, 43 ex

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