Patent(s) and the Corresponding Patented Drug(s) |
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World Intellectual Property Organization (WIPO) |
Patent ID |
WO2014061031 |
Title |
2-Phenyl-5-Heterocyclyl-Tetrahydro-2H-Pyran-3-Amine Compounds for Use In The Treatment of Diabetes and Its Associated Disorders. |
Abstract |
The present invention relates to novel compounds of the general formula (I) their tautomeric forms, their enantiomers, their diastereoisomers, their pharmaceutically accepted salts, or pro-drugs thereof, which are useful for the treatment or prevention of diabetes mellitus (DM), obesity and other metabolic disorders. The invention also relates to process for the manufacture of said compounds, and pharmaceutical compositions containing them and their use. |
Applicant(s) |
Cadila Healthcare Limited |
Representative Drug(s) |
D06PIP |
Drug Info
|
IC50 < 10 nM |
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[1] |
2
|
D0A6LI
|
Drug Info
|
IC50 < 10 nM
|
[1] |
Patent ID |
WO2014017474 |
Title |
Collagen Peptide Composition Production Method, Dpp-4 Inhibitor, and Antihyperglycemic Agent. |
Abstract |
Provided are a novel collagen peptide composition production method, as well as a DPP-4 inhibitor and an antihyperglycemic agent containing said collagen peptide composition. This peptide composition including a peptide represented by X-Hyp-Gly (where, X is an amino acid residue other than Gly, Hyp, and Pro) is generated by adding and dissolving ginger rhizome-derived enzymes in a collagen and/or gelatin solution. The collagen peptide composition thus obtained exhibits high DPP-4 inhibitory activity, and an excellent antihyperglycemic effect. |
Applicant(s) |
Nippi Co., Ltd |
Representative Drug(s) |
D0J4KQ |
Drug Info
|
IC50 = 0.008 mg/ml |
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[1] |
2
|
D0BY2H
|
Drug Info
|
IC50 = 0.039 mg/ml
|
[1] |
Patent ID |
WO2014000629 |
Title |
Hexahydropentaleno Derivatives, Preparation Method and Use In Medicine Thereof. |
Abstract |
The invention relates to hexahydropentaleno derivatives, the preparation method and use in medicine thereof, and in particular to hexahydropentaleno derivatives or stereo-isomers or pharmaceutically acceptable salts thereof as shown in general formula (I), and to the preparation method therefor and pharmaceutical compositions comprising the derivatives, and to the use thereof as a therapeutical agent, especially as a DPP-IV inhibitor. The definition of each substituent in formula (I) is the same as the definition in the description. |
Applicant(s) |
Sunshine Lake Pharma Co., Ltd |
Representative Drug(s) |
D0G3IL |
Drug Info
|
IC50 = 1.56 nM |
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[1] |
2
|
D0KR7R
|
Drug Info
|
IC50 = 1.73 nM
|
[1] |
Patent ID |
WO2013133031 |
Title |
Dipeptidyl Peptidase-Iv Inhibitor. |
Abstract |
Provided are a superior dipeptidyl peptidase-IV inhibitor and the like.Specifically provided are a dipeptidyl peptidase-IV inhibitor, a hypoglycemic agent and a vascular endothelial dysfunction inhibitor, each comprising, as an active ingredient, one or more peptides selected from among peptides comprising one of the amino acid sequences represented by (a)-(d): (a) Ser-Pro-Ala-Gln (SEQ ID NO: 1), (b) Gly-Pro-Val-Arg (SEQ ID NO: 2), (c) His-Pro-His-Pro-His (SEQ ID NO: 3), and (d) Ala-Pro-Lys (SEQ ID NO: 4).Also provided are new peptides comprising any one of the amino acid sequences represented by (a)-(c): (a) Ser-Pro-Ala-Gln (SEQ ID NO: 1), (b) Gly-Pro-Val-Arg (SEQ ID NO: 2), and (c) His-Pro-His-Pro-His (SEQ ID NO: 3). |
Applicant(s) |
Morinaga Milk Industry Co |
Representative Drug(s) |
D05LJQ |
Drug Info
|
Inhibitory activity = 1900 ng/ml |
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[1] |
2
|
D04XXF
|
Drug Info
|
IC50 = 10500 ng/ml
|
[1] |
Patent ID |
WO2012089127 |
Title |
Certain Dipeptidyl Peptidase Inhibitors. |
Abstract |
Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor. |
Applicant(s) |
Shanghai Fochon Pharmaceutical Co Ltd |
Representative Drug(s) |
D0PM4N |
Drug Info
|
IC50 = 0.5 nM |
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[1] |
2
|
D0O6SK
|
Drug Info
|
IC50 = 0.7 nM
|
[1] |
Patent ID |
WO2012089123 |
Title |
Certain Dipeptidyl Peptidase Inhibitors. |
Abstract |
Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor. |
Applicant(s) |
Shanghai Fochon Pharmaceutical Co Ltd |
Representative Drug(s) |
D02SUS |
Drug Info
|
IC50 = 0.9 to 1 nM |
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[1] |
2
|
D04UXC
|
Drug Info
|
IC50 = 0.9 to 1 nM
|
[1] |
3
|
D0KS8Y
|
Drug Info
|
IC50 = 0.9 to 1 nM
|
[1] |
Patent ID |
WO2012088680 |
Title |
Certain Dipeptidyl Peptidase Inhibitors. |
Abstract |
Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor. |
Applicant(s) |
Shanghai Fochon Pharmaceutical Co Ltd |
Representative Drug(s) |
D02SUS |
Drug Info
|
IC50 = 0.9 to 1 nM |
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[1] |
2
|
D04UXC
|
Drug Info
|
IC50 = 0.9 to 1 nM
|
[1] |
3
|
D0KS8Y
|
Drug Info
|
IC50 = 0.9 to 1 nM
|
[1] |
Patent ID |
WO2014018355 |
Title |
Treating Diabetes with Dipeptidyl Peptidase-Iv Inhibitors. |
Abstract |
The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-N enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase IV enzyme is involved. |
Applicant(s) |
Merck Sharp & Dohme Corp |
Representative Drug(s) |
D0XB0Q |
Drug Info
|
IC50 = 8.8 nM |
[1] |
Patent ID |
WO2013065832 |
Title |
Dpp-4 Inhibitor. |
Abstract |
A DPP-4 inhibitor containing, as an active ingredient, a peptide represented by formula (1): Xe-Pro/Ala/Hyp-Xa-Xb-Xc-Xd (wherein Xe represents an amino acid residue having an isoelectric point of 5.9-6.3; Pro/Ala/Hyp represents Pro, Ala or Hyp; Xa represents an amino acid residue other than Hyp, Pro and Arg or a deletion; Xb represents Gly, Pro or a deletion; Xc represents Pro, Ala or a deletion; and Xd represents an amino acid residue or a deletion). This inhibitor is expected to exert an activity of decreasing a blood glucose level through the potentiation of the activity of an incretin, and therefore can be used as a therapeutic agent for diabetes. In addition, this inhibitor can act on an immune system or the like, and therefore can be used for the treatment of skin diseases or the like. |
Applicant(s) |
Nippi Co., Ltd |
Representative Drug(s) |
D0WE8K |
Drug Info
|
IC50 = 60 nM |
[1] |
Patent ID |
WO2013010964 |
Title |
Substituted Quinazolines, The Preparation Thereof and The Use Thereof In Pharmaceutical Compositions. |
Abstract |
The present invention relates to substituted quinazolines of formula (I) wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV). |
Applicant(s) |
Boehringer Ingelheim International Gmbh |
Representative Drug(s) |
D05HLQ |
Drug Info
|
IC50 = 6 pM |
[1] |
Patent ID |
WO2013006526 |
Title |
Tricyclic Heterocycles Useful As Dipeptidyl Peptidase-Iv Inhibitors. |
Abstract |
The present invention is directed to novel tricyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. |
Applicant(s) |
Merck Sharp & Dohme Corp |
Representative Drug(s) |
D0E8AS |
Drug Info
|
IC50 = 1.7 nM |
[1] |
Patent ID |
WO2012147092 |
Title |
Novel Salts of Dpp-Iv Inhibitor. |
Abstract |
The present invention discloses new salts of (2R)-4-oxo-4-[3-(trifluoromethyl)- 5,6-dihydro[ l,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]- l -(2,4,5-trifluorophenyl)butan-2- amine i.e. gentisate, adipate and trifluoro acetic acid salts. The invention also describes the new. crystalline and amorphous forms of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6- dihydro[ l,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]- l -(2,4,5-triflLiorophenyl)butan-2-amine gentisate. The present invention also discloses novel crystalline salt form of (2R)-4-oxo-4-[3- (trifliioromethyl)-5,6-dihydiO[ 1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]- 1 -(2,4,5- trifluorophenyl)butan-2-amine hydrochloride and novel crystalline and amorphous salt forms of besylate and process for their preparation and isolation. |
Applicant(s) |
Cadila Healthcare Limited |
Representative Drug(s) |
D0JP6A |
Drug Info
|
IC50 = 18 nM |
[1] |
Patent ID |
WO2012089122 |
Title |
Certain Dipeptidyl Peptidase Inhibitors. |
Abstract |
Provided are compounds represented by formula (I), their pharmaceutical compositions, and their uses for preparing medicaments as inhibitors of dipepetidyl peptidase-IV enzyme, wherein each substitutuent of formula (I) is defined as the description. |
Applicant(s) |
Shanghai Fochon Pharmaceutical Co Ltd |
Representative Drug(s) |
D0UV3I |
Drug Info
|
IC50 = 0.5 nM |
[1] |
Patent ID |
WO2012088677 |
Title |
Certain Dipeptidyl Peptidase Inhibitors. |
Abstract |
Disclosed are compounds represented by formula (I) and their pharmaceutical compositions, and uses thereof in the preparation of the drugs for treating a condition responsive to inhibition of dipeptidyl peptidase-IV enzyme, wherein each substituent of formula (I) is defined as the description. |
Applicant(s) |
Shanghai Fochon Pharmaceutical Co Ltd |
Representative Drug(s) |
D0UV3I |
Drug Info
|
IC50 = 0.5 nM |
[1] |
Patent ID |
WO2012078448 |
Title |
Tricyclic Heterocycles Useful As Dipeptidyl Peptidase-Iv Inhibitors. |
Abstract |
The present invention is directed to novel tricyclic heterocycles of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. I. |
Applicant(s) |
Merck Sharp & Dohme Corp |
Representative Drug(s) |
D0K2ZQ |
Drug Info
|
IC50 = 0.38 nM |
[1] |
Patent ID |
WO2014034626 |
Title |
Crystal of N-[2-({2-[(2S)-2-Cyanopyrrolidin-1-Yl]-2- Oxoethyl}Amino)-2-Methylpropyl]-2-Methylpyrazolo[1,5-A]Pyrimidine-6-Carboxamide. |
Abstract |
[Problem] To provide: a crystal of anagliptin, which has high purity, excellent stability, low hygroscopicity and a property of being dissolved in water extremely satisfactorily; and a method for producing the crystal of anagliptin. [Solution] A crystal of anagliptin, which has peaks at points located adjacent to diffraction angles, each of which is expressed in 2, of 9.8, 17.4, 18.6, 25.3 and 25.8 and has substantially the same powder X-ray diffraction pattern as that illustrated in fig. 1. The crystal can be produced by reacting N-(2-amino-2-methylpropyl)-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide with (2S)-N-chloroacetyl- 2-cyanopyrrolidine in an organic solvent, then purifying the resultant product by column chromatography to produce an amorphous form of anagliptin, and then crystallizing the amorphous form of anagliptin from 2-propanol. |
Applicant(s) |
Sanwa Chemistry Laboratory Co., Ltd |
Representative Drug(s) |
D06GQG |
Drug Info
|
N.A. |
[1] |
Patent ID |
WO2014018350 |
Title |
Treating Diabetes with Dipeptidyl Peptidase-Iv Inhibitors. |
Abstract |
The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-N enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase IV enzyme is involved. |
Applicant(s) |
Merck Sharp & Dohme Corp |
Representative Drug(s) |
D0K5YJ |
Drug Info
|
N.A. |
[1] |
Patent ID |
WO2013111158 |
Title |
Process for The Preparation of Dpp-Iv Inhibitor. |
Abstract |
The present invention provides a process for the preparation of (l S,3S,5S)-2-[(2S)-2- amino-2-(3 -hydroxyadamantan- l-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile and its pharmaceutically acceptable salts thereof, represented by the compound of formula- 1. |
Applicant(s) |
Msn Laboratories Limited |
Representative Drug(s) |
D01MMT |
Drug Info
|
N.A. |
[1] |
United States Patent and Trademark Office (USPTO) |
Patent ID |
US20130184322 |
Title |
Novel dipeptidyl-peptidase-iv inhibitors. |
Representative Drug(s) |
D0E9MO |
Drug Info
|
IC50 = 1.5 nM |
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[1] |
2
|
D02LNB
|
Drug Info
|
IC50 = 46 nM
|
[1] |
Japan Patent Office (JPO) |
Patent ID |
JP2013184962 |
Title |
Dipeptidyl Peptidase 4 Inhibitor. |
Applicant(s) |
Morinaga Milk Industry Co |
Representative Drug(s) |
D0QE8Z |
Drug Info
|
IC50 = 12200 ng/ml |
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[1] |
2
|
D0B4CH
|
Drug Info
|
IC50 = 12500 ng/ml
|
[1] |
3
|
D0E8WW
|
Drug Info
|
IC50 = 25500 ng/ml
|
[1] |
Patent ID |
JP2013040111 |
Title |
Dipeptidyl Peptidase-4 Inhibitor and Method of Production of The Same. |
Applicant(s) |
Okayama Prefecture |
Representative Drug(s) |
D05GEY |
Drug Info
|
ID50 = 410000 nM |
[1] |
China National Intellectual Property Administration (CNIPA) |
Patent ID |
CN103848835 |
Title |
Dipeptidyl Peptidase 4 Inhibitor, Application Thereof, Intermediate Body Thereof and Preparation Method of Intermediate Body Thereof. |
Applicant(s) |
Shanghai Sun-Sail Pharmaceutical Science & Technology Co |
Representative Drug(s) |
D0P3DS |
Drug Info
|
IC50 = 2.52 nM |
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[1] |
2
|
D0EL5B
|
Drug Info
|
IC50 = 3.51 nM
|
[1] |
Patent ID |
CN103772323 |
Title |
Dipepitidyl Peptidase 4 Inhibitor Compound. |
Applicant(s) |
Nanjing Huawei Pharmaceutical Science and Technology Development Co |
Representative Drug(s) |
D02UOW |
Drug Info
|
IC50 = 0.6 to 0.8 nM |
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[1] |
2
|
D0IO0M
|
Drug Info
|
IC50 = 0.6 to 0.8 nM
|
[1] |
3
|
D0W6HL
|
Drug Info
|
IC50 = 0.6 to 0.8 nM
|
[1] |
Patent ID |
CN103626775 |
Title |
Dpp 4 Inhibitor with Diazine Structure. |
Applicant(s) |
Nanjing Huawei Pharmaceutical Science and Technology Development Co |
Representative Drug(s) |
D0XN3O |
Drug Info
|
IC50 = 6.5 nM |
Click to Show More |
[1] |
2
|
D0BJ2X
|
Drug Info
|
IC50 = 7.4 nM
|
[1] |
Patent ID |
CN103044392 |
Title |
Dpp 4 Inhibitor Preparation Method. |
Applicant(s) |
Lianyungang Runzhong Pharmaceutical Co |
Representative Drug(s) |
D04MAZ |
Drug Info
|
IC50 = 0.27 nM |
Click to Show More |
[1] |
2
|
D0CW9H
|
Drug Info
|
IC50 = 0.35 nM
|
[1] |
Patent ID |
CN103044391 |
Title |
Dpp 4 Inhibitor. |
Applicant(s) |
Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences |
Representative Drug(s) |
D04MAZ |
Drug Info
|
IC50 = 0.27 nM |
Click to Show More |
[1] |
2
|
D0CW9H
|
Drug Info
|
IC50 = 0.35 nM
|
[1] |
Patent ID |
CN102311448 |
Title |
Thieno-pyrimidone DPP-IV (dipeptidyl peptidase) inhibitor. |
Applicant(s) |
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences |
Representative Drug(s) |
D0RT1R |
Drug Info
|
IC50 = 3.1 nM |
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[1] |
2
|
D07JJT
|
Drug Info
|
IC50 = 3.6 nM
|
[1] |
Patent ID |
CN103848811 |
Title |
Uracil Derivative, Preparation Method and Application Thereof. |
Applicant(s) |
Qilu Pharmaceutical Co |
Representative Drug(s) |
D0G1CF |
Drug Info
|
N.A. |
Click to Show More |
[1] |
2
|
D0PF2W
|
Drug Info
|
N.A.
|
[1] |
3
|
D0T1WB
|
Drug Info
|
N.A.
|
[1] |
Patent ID |
CN103420981 |
Title |
Substituted Pyrrolidinyl Contained Thiomorpholine Compounds. |
Applicant(s) |
Institute of Materia Medica, Chinese Academy of Medical Sciences |
Representative Drug(s) |
D06HJX |
Drug Info
|
N.A. |
Click to Show More |
[1] |
2
|
D0D4BP
|
Drug Info
|
N.A.
|
[1] |
Patent ID |
CN102453001 |
Title |
Thiomorpholine compounds and their preparation and use. |
Abstract |
The present invention relates to a thiomorpholine compound and its preparation method and uses. Specifically, the present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt, free base, solvate, ester, prodrug, stereoisomer, geometric isomer, racemate, wherein each symbol is as described in the specification. The present invention further relates to pharmaceutical compositions comprising a compound of the invention, the compounds of the present invention is the preparation of a medicament for the treatment and / or prophylaxis of high DPP-IV activity with DPP-IV or overexpression of a disease or condition associated in uses, and methods of using the compounds of the present invention is the treatment of related diseases. Compounds of the invention have potent inhibition of DPP-IV activity. |
Applicant(s) |
Institute of Materia Medica, Chinese Academy of Medical Sciences |
Representative Drug(s) |
D06HJX |
Drug Info
|
N.A. |
Click to Show More |
[1] |
2
|
D0D4BP
|
Drug Info
|
N.A.
|
[1] |
Patent ID |
CN103373999 |
Title |
Purine compounds, intermediates, preparation method and application. |
Abstract |
The present invention discloses a xanthine compound I, R1 is hydrogen or 2-cyanophenyl; R2 is 2-cyanobenzyl group; R3 is an amino group or, where, n = 2 ~ 4, m = 2 ~ 3, D is H or NH2, E is CH2 or NH. A method for preparing xanthine compound I: compound II with the nucleophilic substitution reaction R3H; or nucleophilic compound II with R-3- tert-butyloxycarbonyl-amino-piperidine substitution reaction, de tert acyl protecting group. The present invention also discloses a xanthine compound according to any one of the intermediates I, R1, and R2 as described above. Application of a xanthine compound I in the manufacture DPP-4 inhibitor activity, or, and / or DPP-4 inhibition by drugs enzyme treatment and prevention of diseases associated therewith in. Xanthine compounds of the present invention provides a new direction for the development of DPP-4 inhibitor, is important for the development of potential DPP-4 inhibitor. |
Applicant(s) |
Shanghai Institute of Pharmaceutical Industry |
Representative Drug(s) |
D0ND5K |
Drug Info
|
89.5% inhibition = 1000 ng/ml |
[1] |
Patent ID |
CN103788070 |
Title |
Dpp 4 Inhibitor Polymer. |
Applicant(s) |
Nanjing Huawei Pharmaceutical Science and Technology Development Co |
Representative Drug(s) |
D00GNP |
Drug Info
|
IC50 = 0.6 nM |
[1] |
Patent ID |
CN103172633 |
Title |
Compound, and Preparation Method and Application Thereof. |
Applicant(s) |
Chengdu Diao Pharmaceutical Group Co |
Representative Drug(s) |
D0T6SD |
Drug Info
|
IC50 = 0.09 nM |
[1] |
Patent ID |
CN103030631 |
Title |
Dipepitidyl Peptidase 4 Inhibitor Compound. |
Applicant(s) |
Jiangsu Chia-Tai Tianqing Pharmaceutical Co |
Representative Drug(s) |
D0J5EW |
Drug Info
|
IC50 < 30 nM |
[1] |
Patent ID |
CN103664893 |
Title |
Novel Dpp 4 Inhibitor, and Preparation Method and Medicinal Application Thereof. |
Applicant(s) |
China Pharmaceutical University |
Representative Drug(s) |
D0J0UN |
Drug Info
|
N.A. |
[1] |
Patent ID |
CN102863440 |
Title |
Crystallographic form of Salt of Dipeptidyl Peptidase 4 Inhibitor. |
Applicant(s) |
Kbp Biomedical Co |
Representative Drug(s) |
D0A5QV |
Drug Info
|
N.A. |
[1] |
Intellectual Property Office in India (IP India) |
Patent ID |
IN2013254994 |
Title |
Preparation of Thienopyrimidones Derivatives As DPP-4 Inhibitors. |
Applicant(s) |
Orchid Chemicals & Pharmaceuticals |
Representative Drug(s) |
D0LG1I |
Drug Info
|
IC50 = 100 nM |
[1] |
Patent ID |
IN2012251197 |
Title |
Preparation of novel pyrrolidines as DPP-4 inhibitors. |
Applicant(s) |
Matrix Laboratories |
Representative Drug(s) |
D0N9CV |
Drug Info
|
IC50 = 8.1 nM |
[1] |
Intellectual Property Office of United Kingdom (IPOUK) |
Patent ID |
GB2497351 |
Title |
Novel compounds. |
Applicant(s) |
Prosidion Ltd |
Representative Drug(s) |
D06PDK |
Drug Info
|
IC50 < 1000 nM |
[1] |