cas 864070-44-0, Empagliflozin | Articles data

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Preparation method of SGLT-2 inhibitor and intermediate
The invention discloses a preparation method of an SGLT-2 inhibitor and an intermediate. The method comprises the following steps: (1) reacting a compound A with chlorosilane under the action of an acid-binding agent to generate a compound B; (2) mixing the compound B and a compound C to obtain a compound D; and (3) reacting the compound D with a reducing agent and a catalyst to obtain the SGLT-2 inhibitor compound.
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(2021/05/19)

Synthesis, Isolation, Characterization and Suppression of Impurities during Optimization of Empagliflozin (Jardiance)
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Liu, Xiao,Peng, Peng,Yang, Jiangtao,Yu, Jun,Zhang, Fuli,Zhao, Chuanmeng
(2022/03/14)

Synthetic method of empagliflozin
The invention discloses a synthesis method of empagliflozin. According to the method, (S)-3-(4-(5-bromo-2-chlorobenzyl) phenoxy) tetrahydrofuran is adopted as a starting raw material and is coupled with 2, 3, 4, 6-tetrabenzyl-D-glucopyranosyl-1, 5-lactone under the catalysis of Pd2 (dba) 3 and the combined action of p-toluenesulfonhydrazide, Xphos and lithium tert-butoxide to generate an intermediate I, double bonds of the intermediate I are subjected to hydrogenation reduction through raney nickel, meanwhile, debenzylation is conducted, and the empagliflozin is obtained. The method does not need butyl lithium, Grignard reagent and other dangerous materials, has the advantages of short reaction route, simple reaction and post-treatment, high safety, few side reactions, high product yield and high purity, and is especially suitable for industrial production.
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Paragraph 0039; 0041-0042; 0044

(2021/10/30)

Synthetic method of empagliflozin
The invention belongs to the technical field of raw material medicine preparation, and relates to a synthetic method of an SGLT-2 inhibitor empagliflozin, which comprises the following steps: 1) taking glucose as an initial raw material, and preparing an active intermediate 3 through full acylation, selective hydrolysis and esterification; 2) reacting the intermediate 3 with chlorobenzene under the catalysis of boron trifluoride/diethyl ether to generate an intermediate 4, and reacting the intermediate 4 with paraformaldehyde and phenoxy tetrahydrofuran to generate an intermediate 5; and 3) removing the protecting group under the action of alkali to obtain the final product empagliflozin. The method is simple to operate, low-temperature reaction in the prior art is avoided, and the purity of the obtained product is higher.
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(2021/07/24)

IMPROVED PROCESS FOR THE PREPARATION OF EMPAGLIFLOZIN AND ITS CRYSTALLINE POLYMORPH
The present invention relates to an improved method for the production of Empagliflozin formula (I). The invention further relates to the preparation of a crystalline form of Empagliflozin and its particle size having a coarser particle or a D50 equal to or greater than 60 μm and a D90 equal to or greater than 180 μm. (I)
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(2021/12/31)

Preparation method of glucopyranosyl substituted benzyl benzene derivative and intermediate thereof
The invention relates to a preparation method of a glucopyranosyl substituted benzyl benzene derivative and an intermediate thereof, and a method for preparing a compound represented by a formula (I),wherein the group R is defined in claim 1. The method is simple to operate, high in product yield, good in selectivity and suitable for industrial production. The present invention relates to theintermediate obtained in the method.
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(2020/07/02)

Synthetic method of empagliflozin
The invention provides a brand-new synthesis process of empagliflozin. According to the process, a boric acid ester is used for halogen removal, and specific reaction conditions are combined, so thatempagliflozin can be prepared with high yield and simplicity and convenience in operation. The synthesis method of empagliflozin has the advantages of mild reaction conditions, high total yield, few side reactions and convenience in operation, thereby being beneficial to industrial production and cost control.
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(2020/02/14)

Preparation method suitable for industrial production of empagliflozin
The invention belongs to the technical field of organic synthesis route design and medicine and chemical engineering, particularly relates to a synthesis method of a sodium-glucose cotransporter 2(SGLT2) inhibitor, and more particularly relates to a preparation method of empagliflozin. The empagliflozin is synthesized by taking (3S)-3-[4-[(2-chloro-5-iodophenyl) methyl] phenoxy] tetrahydrofuran and glucono delta-lactone as initial raw materials through a series of substep reactions such as protection, addition, substitution, deprotection and reduction. In the synthesis steps disclosed by the invention, a staged target product does not need to be separated and purified after each step of reaction, and the target product is finally obtained by directly subjecting a high-purity reaction intermediate to subsequent steps. The preparation method is simple in process, simple and convenient to operate and good in industrial prospect.
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(2019/08/12)

Synthesizing method suitable for industrial empagliflozin production
The invention discloses a synthesizing method suitable for industrial empagliflozin production. The synthesizing method includes: subjecting a compound as shown in formula (II) to reduction reaction to obtain a compound as shown in formula (I), and removing the protecting groups of the compound as shown in formula (I) to obtain empagliflozin. The synthesizing method has the advantages that the method is simple in process, only needs one-step reduction reaction and can effectively reduce the repeated use of high-toxicity and high-risk chemicals; in addition, the intermediate purified after derivation protection, effective process control is achieved, and product quality is increased; the method is high in practical application value and suitable for industrial production.
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(2019/10/17)

Refining method of SGLT-2 inhibitor intermediate
The invention discloses a refining method of an SGLT-2 inhibitor intermediate; the SGLT-2 inhibitor intermediate is represented by the formula (I), wherein the definition of substituent groups in theformula (I) is detailed in the specification. The refining method includes the following steps: the SGLT-2 inhibitor intermediate is dissolved in a polar organic solvent and cooled to ultra-low temperature, the non-polar organic solvent is added, and the solid SGLT-2 inhibitor intermediate is obtained. The refining method is different from a conventional recrystallization technology, and can refine materials that are not easy to solidify at room temperature. A new choice is provided for refining the materials with low melting point and high viscosity. The refining method is suitable for industrialized scale-up production.
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(2019/11/20)

Halopivalylglucopyranose and preparation method for SGLT2 inhibitor
The invention belongs to the technical field of drug synthesis. The invention relates to a novel method for preparing a compound (including Canagliflozin, Dapagliflozin, Empagliflozin and Ipragliflozin) with inhibitory activity on sodium-dependent glucose transporters (SGLT) existing in the intestines or the kidneys. The invention discloses a 1,2,3,4,6-penta-O-halopivalylglucopyranose, the generalstructural formula of which is formula I. The invention further discloses a 2,3,4,6-tetra-O-halopivalyl-Alpha-D-haloglucopyranose (haloglucose for short), the general structural formula of which is formula III. The invention further discloses a preparation method for an SGLT2 inhibitor. The SGLT2 inhibitor which is prepared by adopting the method disclosed by the invention has the technical advantages of high purity, high yield, easiness in operation, suitability for industrial production and the like.
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Paragraph 0090; 0092; 0109-0111; 0120; 0122; 0123; 0158-0160

(2019/01/14)

Processes for the Preparation of SGLT-2 Inhibitors, Intermediates Thereof
The present invention relates to novel, improved processes for the preparation of sodium glucose co-transporter 2 (SGLT-2) inhibitors and novel intermediates thereof. More particularly, the present invention relates to a novel, improved process for the preparation of gliflozin compounds such as empagliflozin and dapagliflozin, intermediates thereof. The product obtained from the processes of present invention may be amorphous or crystalline, or in the form of amorphous/crystalline solid dispersions/solutions with pharmaceutically acceptable polymers and preparation process thereof. Also, the products obtained from the present invention may be used for the preparation of medicaments for the prevention and/or treatment of diseases and conditions associated with SGLT-2 inhibition.
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(2019/01/04)

6-halogenated glucose C-glycoside as well as preparation method and application thereof
The invention discloses a 6-halogenated glucose C-glycoside as well as a preparation method and application thereof. A structure of 6-halogenated glucose C-glycoside is shown in formula I; an intermediate can be synthesized efficiently with cheap and easily available raw materials; meanwhile, when the raw material is used for synthesizing Jardiance, dapagliflozin and the like, a reaction yield ishigh, and an obtained product has high purity and relatively high industrial application prospect.
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Paragraph 0129; 0130; 0131; 0134

(2018/11/03)

Preparation method of empagliflozin
The invention relates to a preparation method of empagliflozin. The preparation method of empagliflozin comprises the following steps: taking 2-chlorobenzaldehyde as a starting material; carrying outbromination reaction, reduction reaction and halogenating reaction on the starting material, and carrying out Friedel-Crafts alkylation reaction on the starting material and (S)-3-phenoxyl tetrahydrofuran to obtain an intermediate which is (S)-3-(4-(5-bromo-2-chlorobenzyl) phenoxyl) tetrahydrofuran; and then carrying out condensation, etherification and methoxyl removal on the intermediate and 2,3,4,6-quadri-O-trimethylsilyl-D-glucolactone to obtain the empagliflozin as a hypoglycemic drug. The preparation method of the empagliflozin has the advantages that compared with an existing synthesisprocess, the preparation method of the empagliflozin takes the 2-chlorobenzaldehyde as the starting material, raw materials are cheap and easy to obtain, industrialization is easy to implement in theprocess, the synthesis route is short, and the method is easy to operate; in a preparation process, various temperature conditions are easy to control, reaction conversion rate is high, and the totalyield can be 75% or above; and moreover, by the preparation method, the product cannot be isomerized easily, impurities are fewer, the purity of the product can be improved, and the purity can be 99%or above.
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(2018/03/26)

A PROCESS FOR THE PREPARATION OF D-GLUCITOL, 1,5-ANHYDRO-1-C-[4-CHLORO-3-[[4- [[(3S)-TETRAHYDRO-3-FURANYL]OXY]PHENYL]METHYL]PHENYL]-, ( 1 S)
The present invention relates to a process for the preparation of D-glucitol, 1,5- anhydro-1-C-[4-chloro-3-[[ 4-[[(3S)-tetrahydro-3-furanyl)oxy )phenyl] methyl]phenyl]-, (IS) formula-1.
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Page/Page column 20; 22; 23

(2018/09/28)

Preparation method of SGLT2 inhibitor-empagliflozin
The invention relates to a preparation method of a SGLT2 inhibitor-empagliflozin. The preparation method includes: using 2-methylaniline as a starting raw material, subjecting the starting raw material to bromination, diazotization, chlorination and bromination, and enabling the starting raw material to be in friedel-crafts alkylation reaction with (S)-3-phenoxy tetrahydrofuran to obtain an intermediate-(S)-3-(4-(5-bromo-2-chlorobenzyl)phenoxy) tetrahydrofuran; subjecting the intermediate and 2, 3, 4, 6-tetra-O-trimethylsilyl-D-glucolactone to condensation, etherification and methoxy removal.The preparation method has the advantages that compared with existing synthetic methods, 2-methylaniline is used as the starting raw material, so that the raw material is low in cost and easy to get,the process is easy for industrialization, and a synthetic route is short and easy to operate; in the process of preparation, temperature conditions are easy to control, reaction conversion rate is high, and total yield is up to higher than 75%. In addition, through the preparation method, the inhibitor is less prone to isomerization, impurities are few, and purity of the inhibitor can be improvedto higher than 99%.
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(2018/03/26)

Synthesis process for empagliflozin
The invention relates to a synthesis process for empagliflozin. The synthesis process for empagliflozin comprises the following steps: taking 4-fluorotoluene as a starting material; carrying out radical bromo reaction, Friedel-Crafts alkylation reaction, deprotection, diazotization chlorination and alkylation reaction to obtain an intermediate which is (S)-3-(4-(5-bromo-2-chlorobenzyl) phenoxyl) tetrahydrofuran; and then carrying out condensation, etherification and methoxyl removal on the intermediate and 2,3,4,6-quadri-O-trimethylsilyl-D-glucolactone to obtain the empagliflozin as a hypoglycemic drug. The synthesis process for empagliflozin has the advantages that compared with an existing synthesis process, the synthesis process for the empagliflozin takes the 4-fluorotoluene as the starting material, raw materials are cheap and easy to obtain, industrialization is easy to implement in the process, the synthesis route is short, and the process is easy to operate; in a preparation process, various temperature conditions are easy to control, reaction conversion rate is high, and the total yield can be 70% or above; and moreover, by the synthesis process, the product cannot be isomerized easily, impurities are fewer, the purity of the product can be improved, and the purity can be 99% or above.
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(2018/03/28)

The net [...] B crystal form and its preparation
The invention relates to a B crystal form of empagliflozin and a preparation method of the B crystal form. The prepared B crystal form of empagliflozin has diffraction peaks when the diffraction angle 2 theta is equal to 8.916 degrees, 10.011 degrees, 11.239 degrees, 17.567 degrees, 18.775 degrees, 19.308 degrees, 25.353 degrees and 26.000 degrees according to characterization of a powder x-ray diffraction pattern, and the powder x-ray diffraction pattern is obtained through CuK alpha rays. The preparation technology of the crystal form is simple, the stability is better, and the medicinal requirements are met.
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Paragraph 0033; 0034; 0035; 0036

(2018/03/01)

A method for preparing empagliflozin
A method for preparing empagliflozin is provided. The method includes steps of preparing a composite organometallic reagent to promote condensation of (S)-4-halogen-1-chloro-2-(4-tetrahydrofuran-3-yloxy-benzyl) benzene and halogenated glucose, and then removing a protecting group to obtain a product, wherein the organometallic reagent is a product by mixing a Grignard reagent or a lithium chloridepromoted Grignard reagent with a lithium reagent. The organometallic reagent can allow the temperature of a coupling reaction to be increased from -78 DEG C to -10 DEG C, thus improving process reaction conditions, making operation simple and convenient, reducing byproducts and reducing the production cost. The method reduces process steps, avoids reactions at excessively low temperatures, increases the total yield and has an industrial application prospect.
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Paragraph 0045; 0047

(2018/04/01)

Empagliflozin monocrystalline and preparation method and purpose thereof
The invention relates to an Empagliflozin monocrystalline and a preparation method and a purpose thereof. A chemical structural formula of Empagliflozin is shown as a formula I, according to the Empagliflozin monocrystalline, the X-ray powder diffracting at the diffraction angles 2theta of 13.33, 14.66, 18.81, 20.33, 23.44, and 26.84 has characteristic peaks. A crystal structure of the Empagliflozin monocrystalline is a monoclinic system, the space group is C2, the number Z of molecules in crystal is 4, and the Empagliflozin monocrystalline is colorless sheet-shaped crystallization at normal temperature. The monocrystalline form is good, and the purity is as high as 99%.
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Paragraph 0053-0060

(2017/06/02)

Industrial preparation method for empagliflozin
The invention discloses an industrial preparation method for empagliflozin. Specifically, the invention relates to a preparation method for empagliflozin as shown in formula as defined in the specification, i.e., (1S)-1,5-dehydro-1-(4-chloro-3{4-[(3S)-tetrahydrofuran-3-yloxy]benzyl}pheyl)-D-glucitol, and an intermediate prepared by using the method. The preparation method for empagliflozin in the invention is stable in process, good in reproducibility and suitable for large-scale production.
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(2017/08/27)

Preparation method of Jardiance
The invention discloses a preparation method of Jardiance. The preparation method comprises the following steps: (1) performing a Grignard exchange reaction on a compound 5, then enabling the compound 5 after the Grignard exchange reaction to react with a glucose lactone derivative 6 so as to obtain a compound 7 (as shown in the description), wherein X is bromine or iodine, LG is chlorine, bromine, mesyloxy or tosyl, and PG is acetyl, tert- butanoyl or benzoyl; (2) under the action of alkali, performing deprotection on the compound 7 so as to obtain a finished product namely an Jardiance type compound 8 (as shown in the description). The preparation route is simple to operate, the reaction steps are reduced, the yield is high, the obtained product is high in purity, and the preparation method is suitable for scaled production.
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(2017/07/21)

SOLID STATE FORMS OF EMPAGLIFLOZIN
The present invention provides solid state forms of empagliflozin, complexes of empagliflozin with amino acids, processes for their preparation and their use in purification of empagliflozin and also provided pharmaceutical compositions comprising them and their use in therapy (Formula I).
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Page/Page column 32

(2017/12/29)

Method for preparing high purity Empagliflozin
The present invention provides an improved method for preparing high purity Empagliflozin, the method includes the following steps: step a. under the protection of nitrogen, performing reaction of compounds 1 and 2 to obtain a compound 3; step b. adding the compound 3 into a reactor, adding methanol, dropwise adding concentrated hydrochloric acid, stirring, dissolving, clarifying, and performing reaction at room temperatur to obtain a compound 4; step c. adding dropwise an acetonitrile and dichloromethane solution of the compound 4 to an aluminium chloride, triethyl silicane, acetonitrile and dichloromethane solution for reaction, after completion of the reaction, adding water for quenching the reaction, stirring until a solid is precipitated, filtering by suction, and collecting a filter cake to obtain a crude product of compound 5, namely Empagliflozin; and d. refining the crude product. The method is suitable for industrial production,and can be used for the preparation of the high purity Empagliflozin.
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(2017/10/13)

Method for preparing empagliflozin
The invention provides a method for preparing empagliflozin. The method comprises the following steps: by taking (S)-3-(4-(5-bromine-2-chlorobenzyl) phenoxyl) tetrahydrofuran and glucolactone as initial raw materials, performing coupling so as to obtain an intermediate compound 3, performing etherification so as to obtain an intermediate compound 4, performing reduction so as to obtain a crude empagliflozin compound 5, and performing refining, thereby obtaining a qualified empagliflozin finished product.
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(2017/08/29)

PROCESSES FOR THE PREPARATION OF EMPAGLIFLOZIN
The present invention relates to processes for the preparation of empagliflozin. In particular, the present invention relates to the preparation of empagliflozin and intermediates thereof. The present invention also relates to co-crystal of empagliflozin and amino acid and amorphous form of empagliflozin.
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(2017/09/13)

PROCESS FOR PREPARING SGLT2 INHIBITORS AND INTERMEDIATES THEREOF
The present invention provides processes for preparing SGLT2 inhibitors, such as dapagliflozin and empagliflozin.
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(2017/09/06)

COMPLEX OF SGLT2 INHIBITOR AND PROCESS FOR PREPARATION THEREOF
The present invention relates to a crystalline Form A of complex of Empagliflozin with L-Proline and process for preparation thereof. The present invention further relates to a method of preparing pure crystalline Empagliflozin via formation of the said complex.
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(2017/09/08)

THE PRESENT INVENTION RELATES TO PROCESS FOR THE PREPARATION OF D-GLUCITOL, 1,5- ANHYDRO-1-C-[4-CHLORO-3-[[4-[[(3S)-TETRAHYDRO-3-FURANYL] OXY]PHENYL] METHYL]PHENYL]-, (1S) AND ITS CRYSTALLINE FORMS THEREOF.
The present invention relates to process for the preparation of D-glucitol, 1,5- anhydro-l-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl] methyl]phenyl]-, (1S) formula- 1 and its crystalline forms thereof.
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(2017/08/22)

Pipeline synthesis process for liflozin drugs
The invention relates to a pipeline synthesis process for liflozin drugs. The synthesis process is based on a pipeline reactor, and the pipeline reactor comprises a first pipeline section used for preheating and a second pipeline section used for reacting. The synthesis process comprises the following steps: respectively dissolving raw materials in an organic solvent, respectively pumping the materials into the pipeline reactor, and enabling the materials to enter the first pipeline section to be preheated; preheating for multiple time, enabling the materials to respectively enter the second pipeline section, pumping an aqueous solution of inorganic base through a joint of the second pipeline section, remaining for multiple time and discharging, performing after-treatment, thereby obtaining the raw liflozin drugs. Compared with the prior art, the pipeline synthesis process disclosed by the invention has the beneficial effects that the equipment miniaturization and continuous production of production of the raw liflozin drugs can be realized by utilizing the pipeline reaction process, the mass transfer and heat transfer of the materials are stable, and the pipeline reaction has high synthesis efficiency compared with a batch reaction.
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Paragraph 0020; 0021

(2018/01/13)

Synthetic method of empagliflozin
The invention provides a synthetic method of empagliflozin. The synthetic method comprises the following steps of: by using 2, 3, 4, 6-tetra-O-benzyl-D-glucopyranose acid-1,5-lactone and p-chloroiodobenzene as raw materials, performing a reaction so as to obtain an intermediate as shown in a formula II; performing reduction to eliminate a hydroxyl on anomeric carbon of the intermediate as shown in the formula II, so as to obtain an intermediate as shown in a formula III; by using (S)-3-phenoxy tetrahydrofuran, the intermediate as shown in the formula III, and paraform as raw materials, performing a reaction so as to obtain an intermediate as shown in a formula IV; and removing benzyl of the intermediate as shown in the formula IV, so as to obtain the empagliflozin. According to the synthetic method disclosed by the invention, firstly 1-p-chlorophenyl-2,3,4,6-tetra-O-benzyl-D-glucopyranose is prepared, then the intermediate of the 1-p-chlorophenyl-2,3,4,6-tetra-O-benzyl-D-glucopyranose, the (S)-3-phenoxy tetrahydrofuran and the paraform are used as the raw materials, the empagliflozin protected by intermediate benzyl is prepared, and finally a benzyl protecting group is removed, so that the empagliflozin is obtained. The synthetic route of the synthetic method disclosed by the invention is short, and the total yield is high.
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(2017/01/31)

Preparation method of SGLT-2 inhibitor compound
The invention relates to a preparation method of SGLT-2 inhibitor compound. The preparation method comprises the following steps: performing hydroxyl protection, coupling reaction, hydroxyl de-protection, ketalation and the like to the compound A so as to obtain an intermediate I; and then preparing the SGLT-2 inhibitor compound by the obtained intermediate I.
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(2016/10/09)

Empagliflozin crystal forms, preparation methods and uses thereof, and pharmaceutical composition
The present invention relates to new empagliflozin crystal forms, wherein the new empagliflozin crystal forms have a variety of improved characteristics compared with the known crystal form, and are suitable for pharmaceutical preparations. The present invention further relates to preparation methods of the new crystal forms, a pharmaceutical composition of the new crystal form, and uses of the new crystal forms in preparation of drugs for treatment and/or prevention of type II diabetes.
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Paragraph 0075; 0076

(2016/11/28)

PROCESS FOR THE PREPARATION OF EMPAGLIFLOZIN
An improved process for the preparation of empagliflozin is disclosed. Novel intermediates of formulas (13) and (14) for the preparation of empagliflozin are also disclosed, wherein R1 and R2 are independently hydrogen or hydroxyl protecting groups.
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(2015/07/16)

Efficient synthesis of empagliflozin, an inhibitor of SGLT-2, utilizing an AlCl3-promoted silane reduction of a β-glycopyranoside
An efficient production synthesis of the SGLT-2 inhibitor Empagliflozin (5) from acid 1 is described. The key tactical stage involves I/Mg exchange of aryl iodide 2 followed by addition to glucono lactone 3 in THF. Subsequent in situ treatment of the resulting lactol with HCl in MeOH produces β-anomeric methyl glycopyranoside 4 which is, without isolation, directly reduced with Et3SiH mediated by AlCl3 as a Lewis acid in CH 2Cl2/MeCN to afford 5 in 50% overall yield. The process was implemented for production on a metric ton scale for commercial launch.
Wang, Xiao-Jun,Zhang, Li,Byrne, Denis,Nummy, Larry,Weber, Dirk,Krishnamurthy, Dhileep,Yee, Nathan,Senanayake, Chris H.
p. 4090 - 4093
(2014/10/15)

PROCESSES FOR PREPARING OF GLUCOPYRANOSYL-SUBSTITUTED BENZYL-BENZENE DERIVATIVES
The present invention relates to processes for preparing a glucopyranosyl-substituted benzyl-benzene derivative of general formula III, wherein R1 is defined according to claim 1.
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(2011/10/12)

METHOD FOR THE PREPARATION OF A CRYSTALLINE FORM
The invention relates to a method for the preparation for a crystalline form of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene. In addition the invention relates to a crystalline form obtainable by this method, to a pharmaceutical composition and to the use thereof for preparing medicaments.
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(2011/10/12)

METHOD FOR THE PREPARATION OF A CRYSTALLINE FORM OF 1-CHLORO-4- (BETA-D-GLUCOPYRANOS-1-YL)-2-(4-((S)-TETRAHYDROFURAN-3-YLOXY)BENZYL)BENZENE
The invention relates to a method for the preparation for a crystalline form of 1-chloro-4-(Β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene. In addition the invention relates to a crystalline form obtainable by this method, to a pharmaceutical composition and to the use thereof for preparing medicaments.
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Page/Page column 21-23

(2011/04/25)

THERAPEUTIC USES OF SGLT2 INHIBITORS
Provided are methods of using one or more SGLT2 inhibitors, independently or in combination, for treating edema or reducing fluid retention. The invention also provides methods of using one or more SGLT2 inhibitors for the preparation of a medicament for treating edema or fluid retention. Methods are also provided for treating diabetes with an amount of one or more SGLT2 inhibitors and one or more PPAR-gamma agonists.
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(2011/04/19)

Crystalline form of 1-chloro-4-(beta-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments
The invention relates to a crystalline form of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.
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Page/Page column 6

(2010/11/28)

GLUCOPYRANOSYL-SUBSTITUTED BENZONITRILE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR MANUFACTURE
Glucopyranosyl-substituted benzonitrile derivative of formula (I) are disclosed, wherein R3 denotes hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, iso-butyl, tert-butyl, 3-methyl-but-1-yl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, difluoromethyl, trifluoromethyl, pentafluoroethyl, 2-hydroxyl-ethyl, hydroxymethyl, 3-hydroxy-propyl, 2-hydroxy-2-methyl-prop-1 -yl, 3- hydroxy-3-methyl-but-1-yl, 1-hydroxy-1-methyl-ethyl, 2,2,2-trifluoro-1-hydroxy-1-methyl-ethyl, 2,2,2-trifluoro-1-hydroxy-1 -trifluoromethyl-ethyl, 2-methoxy-ethyl, 2-ethoxy-ethyl, hydroxy, methyloxy, ethyloxy, isopropyloxy, difluoromethyloxy, trifluoromethyloxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy, (S)-tetrahydrofuran-3-yloxy, (R)-tetrahydrofuran-3-yloxy, tetrahydropyran-4-yloxy, 1-acetyl-piperidin-4-yloxy, 2-methyloxy-ethyloxy, methylsulfanyl, methylsulfinyl, methylsulfonyl, ethylsulfinyl, ethylsulfonyl, trimethylsilyl and cyano, or a derivative thereof wherein one or more hydroxyl groups of the β-D-glucopyranosyl group are acylated with groups selected from (C1-18-alkyl)carbonyl, (C1-18-alkyl)oxycarbonyl, phenylcarbonyl and phenyl-(C1-3-alkyl)-carbonyl; including tautomers, stereoisomers thereof or mixtures thereof; and physiologically acceptable salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
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Page/Page column 37

(2008/06/13)

Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein
The present invention relates to processes for preparing the compounds of general formula I, wherein the groups R1 and R3 are defined according to claim 1. Furthermore this inventions relates to intermediates obtained in these processes.
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Page/Page column 29-30

(2010/11/24)

CRYSTALLINE FORM OF 1-CHLORO-4-(?-D-GLUCOPYRANOS-1-YL)-2-[4-((S)-TETRAHYDROFURAN-3-YLOXY)-BENZYL]-BENZENE, A METHOD FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS
The invention relates to a crystalline form of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((Sj-tetrahydrofuran-3-yloxy)-benzyl]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.
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Page/Page column 17

(2010/11/24)

Glucopyranosyl-substituted phenyl derivatives, medicaments containing such compounds, their use and process for their manufacture
Glucopyranosyl-substituted benzene derivatives of general formula I where the groups R1 to R6 as well as R7a, R7b, R7c are defined herein and the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
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Page/Page column 28

(2008/06/13)

GLUCOPYRANOSYL-SUBSTITUTED BENZOL DERIVATIVES, DRUGS CONTAINING SAID COMPOUNDS, THE USE THEREOF AND METHOD FOR THE PRODUCTION THEREOF
The invention relates to glucopyranosyl-substitutedted benzol derivatives of general formula (I), wherein rests R1 to R6 and R7a, R7b, R7c are such as defined in the claim 1, including the tautomers, stereoisomers, mixtures and the salts thereof. The inventive compounds are useful for treating metabolic diseases.
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Page/Page column 68

(2008/06/13)

Chemical Properties

Boiling Point: 665℃
Flash Point:356℃
Density: 1.398
Solubility:insoluble in H2O; ≥20.75 mg/mL in DMSO; ≥7.06 mg/mL in EtOH with ultrasonic
Storage Temp.:2-8°C
PKA: 13.23±0.70(Predicted)
PSA: 108.61000
LogP: 1.61340

Global suppliers and manufacturers of 864070-44-0total 230 suppliers on LookChem

Company Name
Business Type
Min Order
FOB Price
Main Products
Contact

Hangzhou Hysen Pharma co.,Ltd.
Business Type:Lab/Research institutions
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FOB Price:No Data
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Enke Pharma-tech Co.,Ltd. （Cangzhou, China ）
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Senova Technology Company Limited
Business Type:Trading Company
Min Order:100 Gram
FOB Price:No Data
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Koning Pharmchem Co., Ltd.
Business Type:Trading Company
Min Order:No Data
FOB Price:No Data
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ZHEJIANG JIUZHOU CHEM CO.,LTD
Business Type:Trading Company
Min Order:10 Gram
FOB Price:USD $ 19.0-65.0 / Gram
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Sinoway Industrial Co., Ltd.
Business Type:Trading Company
Min Order:25 Kilogram
FOB Price:USD $ 13.0-13.0 / Kilogram
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Hangzhou Dingyan Chem Co., Ltd
Business Type:Trading Company
Min Order:1 Kilogram
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Wuhan Fortuna Chemical Co.,Ltd
Business Type:Trading Company
Min Order:1 Kilogram
FOB Price:USD $ 2500.0-2727.0 / Kilogram
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Hangzhou Think Chemical Co. Ltd
Business Type:Other
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Ality Chemical Corporation
Business Type:Other
Min Order:1
FOB Price:No Data
Main Products:165
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Xi'an Xszo Chem Co., Ltd.
Business Type:Manufacturers
Min Order:1 Gram
FOB Price:USD $ 0.1-0.1 / Gram
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ANQING CHICO PHARMACEUTICAL CO.,LTD.
Business Type:Trading Company
Min Order:1 Kilogram
FOB Price:No Data
Main Products:32
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Shanghai Seasonsgreen Chemical Co.,Ltd
Business Type:Manufacturers
Min Order:1 Kilogram
FOB Price:USD $ 1.0-1.0 / Kilogram
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Dayang Chem (Hangzhou) Co.,Ltd.
Business Type:Lab/Research institutions
Min Order:1 Kilogram
FOB Price:USD $ 4.0-5.0 / Kilogram
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Chemwill Asia Co., Ltd.
Business Type:Manufacturers
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Hebei yanxi chemical co.,LTD.
Business Type:Trading Company
Min Order:1 Metric Ton
FOB Price:USD $ 1.0-2.0 / Metric Ton
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Hubei DiBo chemical co., LTD
Business Type:Other
Min Order:25 Kilogram
FOB Price:USD $ 1.0-2.0 / Kilogram
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Hebei Nengqian Chemical Import and Export Co., LTD
Business Type:Trading Company
Min Order:1 Kilogram
FOB Price:USD $ 1.0-10.0 / Kilogram
Main Products:165
Country:

Henan Tianfu Chemical Co., Ltd.
Business Type:Lab/Research institutions
Min Order:1 Metric Ton
FOB Price:USD $ 500.0-500.0 / Metric Ton
Main Products:67
Country:

Zhuozhou Wenxi import and Export Co., Ltd
Business Type:Trading Company
Min Order:1 Kilogram
FOB Price:USD $ 139.0-210.0 / Kilogram
Main Products:1
Country:

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Chemical Properties

Boiling Point: 665℃

Flash Point:356℃

Density: 1.398

Solubility:insoluble in H2O; ≥20.75 mg/mL in DMSO; ≥7.06 mg/mL in EtOH with ultrasonic

Storage Temp.:2-8°C

PKA: 13.23±0.70(Predicted)

PSA: 108.61000

LogP: 1.61340

Global suppliers and manufacturers of 864070-44-0total 230 suppliers on LookChem