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Molecular Formula: C25H27N7O
Molecular Weight: 441.539 g/mol


CAS 1428445-40-2

REF Bioorganic & Medicinal Chemistry (2013), 21(7), 1749-1755.

NEXT ONE………………


CID 71553372.png

CAS 1415912-31-0

1H-Purine-2,6-dione, 8-[(3R)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-([1,2,5]thiadiazolo[3,4-b]pyridin-5-ylmethyl)-
Molecular Formula: C21H23N9O2S
Molecular Weight: 465.536 g/mol

REF CN 102807568, CN 105315301,  WO 2016019868


CAS 1874255-95-4

C21 H23 N9 O2 S . C6 H8 O7
1H-Purine-2,6-dione, 8-[(3R)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-([1,2,5]thiadiazolo[3,4-b]pyridin-5-ylmethyl)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)



Guangzhou Institutes of Biomedicine and Health

Image result for Guangzhou Institutes of Biomedicine and Health

Chia Tai Tianqing Pharmaceutical Group Co Ltd;

Image result for Chia Tai Tianqing Pharmaceutical Group Co Ltd;
Non-insulin dependent diabetes

Dipeptidyl peptidase IV inhibitor (oral, type 2 diabetes),

DPP-IV inhibitors (oral, type 2 diabetes), Guangzhou Institutes of Biomedicine and Health/Jiangsu Chia Tai Tianqing Pharmaceutical ; HWH-ZGC-2-143 ;

Novel polymorphic forms of thiadiazole derivatives, preferably aglucin, sitagliptin, saxagliptin, vildagliptin, levaratine, useful for treating type II diabetes. Guangzhou Institutes of Biomedicine and Health , in collaboration with Jiangsu Chia Tai Tianqing Pharmaceutical , is investigating tilogliptin , an oral dipeptidyl peptidase IV inhibitor and a pyrrolopyrimidine analog, for treating type 2 diabetes.

As of June 2017, Centaurus BioPharma is developing diabetes therapy, CT-1006 and CT-1005 (in preclinical development) for treating diabetes mellitus.

See WO2016019868, claiming novel citric acid salt of 8-((R)-3-amino-piperidin-1-yl)-1-([1,2,5]-thiadiazolo [3,4-b] pyridine-5methyl)-7-(2-butyn-1-yl)-3-methyl-xanthine, coassigned to Lianyungang Runzhong Pharmaceutical .




Chinese Patent Application CN102807568 discloses the use of thiadiazole derivatives DPP-IV inhibitors and their use in the treatment and / or prophylaxis of diseases susceptible to DPP-IV inhibition, particularly in the treatment of type II diabetes. There is still a need for a good thiadiazole derivative DPP-IV inhibitor and a pharmaceutically acceptable salt thereof having good pharmacological and bioavailability.
The contents of the invention
In one aspect, the present application provides 8 – ((R) -3-amino-piperidin-1-yl) -1 – ([1,2,5] thiadiazolo [3,4-b] pyridine- Methyl) -7- (2-butyn-1-yl) -3-methyl-xanthine (having the structure of the following formula I, hereinafter referred to as the compound of formula I).
In another aspect, the present application provides monocarbamates of the compounds of formula I wherein the structural formula is as follows:


WO 2017088790

Centaurus BioPharma Co Ltd; Chia Tai Tianqing Pharmaceutical Group Co Ltd

DPP-IV (dipeptidyl peptidase IV) is a serine protease that is expressed in various tissues (eg, liver, lung, intestine, kidney, etc.) in vivo, responsible for endogenous peptides (GLP-1 (7 -36)) metabolic cleavage. However, GLP-1 (7-36) has a variety of beneficial effects in the body, including stimulation of insulin secretion, inhibition of glucagon secretion, promotion of fullness and delayed gastric emptying. Thus, inhibition of DPP-IV can be used to prevent and / or treat diabetes, particularly type II diabetes. There are a variety of DPP-IV inhibitors listed, such as aglucin, sitagliptin, saxagliptin, vildagliptin, levaratine and so on.
Chinese Patent Application CN102807568 discloses a thiadiazole derivative DPP-IV inhibitor as shown in Formula I or Formula II wherein said compound of formula (especially compound 7) has a very good DPP-IV inhibitory activity. In addition, compound 7 also has a very good in vivo metabolic level and a very suitable in vivo half-life, particularly suitable as a DPP-IV inhibitor drug.
In addition to the therapeutic efficacy, the drug developer attempts to provide a suitable form of the active molecule having properties as a drug (e.g., processing, preparation, storage stability, etc.). Therefore, the discovery of the form of the desired nature of the drug development is also essential.
To a 30 L glass autoclave was added 5.5 L of ethanol, 550 g of an intermediate of 1,256 g of (R) 3-aminopiperidine dihydrochloride, 414 g of sodium bicarbonate, stirred and heated to a temperature of 75 ° C to 80 ° C ℃, stirring reaction 4h. TLC (254 nm UV light, methanol: dichloromethane: aqueous ammonia = 1: 10: 0.1, Rf intermediate 1 = 0.7, Rf product = 0.5) was monitored until intermediate 1 was complete, filtered, and ethanol washed. The filtrate 45 ± 5 ℃ under reduced pressure evaporated, add 5L of methylene chloride dissolved, 5L purified water washing; add 5L purified water, 288g citric acid extraction, 2.5L purified water extraction organic phase, combined with water; Methyl chloride and 10L ethanol; add 5L dichloromethane, the temperature control does not exceed 30 degrees, slowly adding sodium hydroxide solution, extraction and separation; organic phase washed with 5L purified water; anhydrous sodium sulfate drying organic phase. Filtered and the filtrate 30 ± 5 ° C evaporated to dryness under reduced pressure to give 372 g of the compound of formula 7 as an amorphous form

Discovery of potent dipeptidyl peptidase IV inhibitors through pharmacophore hybridization and hit-to-lead optimization

  • a Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science, 190 Kaiyuan Avenue, Guangzhou Science Park, Guangzhou 510530, China
  • b Jiangsu Chia-Tai Tianqing Pharmaceutical Co. Ltd, No. 8 Julong North Rd., Xinpu Lianyungang, Jiangsu 222006, China
  • c State Key Laboratory of Respiratory Disease, Guangzhou 510120, China





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DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK LIFE SCIENCES LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 30 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, Dr T.V. Radhakrishnan and Dr B. K. Kulkarni, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 30 PLUS year tenure till date June 2021, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 90 Lakh plus views on dozen plus blogs, 233 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 33 lakh plus views on New Drug Approvals Blog in 233 countries...... , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc

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