WO2003004498A1 - Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes - Google Patents
Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes Download PDFInfo
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- WO2003004498A1 WO2003004498A1 PCT/US2002/021349 US0221349W WO03004498A1 WO 2003004498 A1 WO2003004498 A1 WO 2003004498A1 US 0221349 W US0221349 W US 0221349W WO 03004498 A1 WO03004498 A1 WO 03004498A1
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- 0 *CC(CC(*1CC2=**=C(*)*2CC1)=O)** Chemical compound *CC(CC(*1CC2=**=C(*)*2CC1)=O)** 0.000 description 2
- GGHTUIHJRLJIDT-GOSISDBHSA-N N[C@@H](CC(N1Cc2ncc(-c3ccccc3)[n]2CC1)=O)Cc1ccccc1F Chemical compound N[C@@H](CC(N1Cc2ncc(-c3ccccc3)[n]2CC1)=O)Cc1ccccc1F GGHTUIHJRLJIDT-GOSISDBHSA-N 0.000 description 1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
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- A61K38/28—Insulins
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- Medicinal Chemistry (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
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- Endocrinology (AREA)
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- Urology & Nephrology (AREA)
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- Neurology (AREA)
- Neurosurgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
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Abstract
Description
Claims
Priority Applications (42)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
UA2004020837A UA74912C2 (en) | 2001-07-06 | 2002-05-07 | Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes |
EP02749813A EP1412357B1 (en) | 2001-07-06 | 2002-07-05 | Beta-amino tetrahydroimidazo(1,2-a)pyrazines and tetrahydrotriazolo(4,3-a)pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
BRPI0210866A BRPI0210866B8 (en) | 2001-07-06 | 2002-07-05 | beta-amino tetrahydroimidazo (1,2-a) pyrazine and tetrahydrotriazole (4.3-a) pyrazine compounds, uses thereof and pharmaceutical composition |
IL15910902A IL159109A0 (en) | 2001-07-06 | 2002-07-05 | Beta-amino tetrahydroimidazo (1,2-a) pyrazines and tetrahydrotriazolo (4,3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
CA002450740A CA2450740C (en) | 2001-07-06 | 2002-07-05 | Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
NZ529833A NZ529833A (en) | 2001-07-06 | 2002-07-05 | Beta-amino tetrahydroimidazo (1, 2-A) pyrazines and tetrahydrotrioazolo (4, 3-A) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
HU0401104A HU225695B1 (en) | 2001-07-06 | 2002-07-05 | Beta-aminoacyl tetrahydroimidazo[1,2-a]pyrazines and tetrahydrotriazolo[4,3-a]pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes and pharmaceutical compositions containing them |
KR1020047000166A KR100606871B1 (en) | 2001-07-06 | 2002-07-05 | Beta-amino tetrahydroimidazo 1,2-a pyrazines and tetrahydrotriazolo 4, 3-a pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
MEP-2008-667A ME00439B (en) | 2001-07-06 | 2002-07-05 | Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
DE200712000056 DE122007000056I1 (en) | 2001-07-06 | 2002-07-05 | Beta-amino-tetrahydroimidazo (1,2-A) pyrazines and -tetrahydrotriazolo (4,3-A) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
DE122008000046C DE122008000046I1 (en) | 2001-07-06 | 2002-07-05 | BETA-AMINO-TETRAHYDROIMIDAZO (1,2-A) PYRAZINE AND -ETRAHYDROTRIAZOLO (4,3-A) PYRAZINE AS DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES |
SI200230301T SI1412357T1 (en) | 2001-07-06 | 2002-07-05 | Beta-amino tetrahydroimidazo(1,2-a)pyrazines and tetrahydrotriazolo(4,3-a)pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
AU2002320303A AU2002320303B2 (en) | 2001-07-06 | 2002-07-05 | Beta-amino tetrahydroimidazo (1, 2-A) pyrazines and tetrahydrotrioazolo (4, 3-A) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
DE60210093T DE60210093T2 (en) | 2001-07-06 | 2002-07-05 | BETA-AMINO-TETRAHYDROIMIDAZO (1,2-A) PYRAZINE AND -ETRAHYDROTRIAZOLO (4,3-A) PYRAZINE AS DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES |
JP2003510665A JP3762407B2 (en) | 2001-07-06 | 2002-07-05 | Β-aminotetrahydroimidazo (1,2-A) pyrazines and tetrahydrotriazolo (4,3-A) pyrazines as dipeptidyl peptidase inhibitors for treating or preventing diabetes |
PL367279A PL196278B6 (en) | 2001-07-06 | 2002-07-05 | Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
US10/481,353 US7125873B2 (en) | 2001-07-06 | 2002-07-05 | Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
MXPA04000018A MXPA04000018A (en) | 2001-07-06 | 2002-07-05 | Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes. |
EA200400153A EA006845B1 (en) | 2001-07-06 | 2002-07-05 | Beta-amino tetrahydroimidazo(1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
IL159109A IL159109A (en) | 2001-07-06 | 2003-11-27 | Dipeptidyl peptidase inhibiting 7-(3-amino-4-arylbutanoyl)tetrahydroimidazo (1,2-a) pyrazine and tetrahydrotriazolo (4,3-a) pyrazine derivatives and pharmaceutical compositions containing them |
IS7062A IS2218B (en) | 2001-07-06 | 2003-11-28 | Beta-amino tetrahydroimidazo (1,2-a) pyrazine and tetrahydrotriazolo (4,3-a) pyrazine which dipeptidylpeptidase inhibits the treatment or prevention of diabetes. |
HR20031098A HRP20031098B1 (en) | 2001-07-06 | 2003-12-30 | Beta-amino tetrahydroimidazo (1,2-a) pyrazines and tetrahydrotrioazolo (4,3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
NO20040021A NO321999B1 (en) | 2001-07-06 | 2004-01-05 | Beta-amino-tetrahydroimidaz (1,2-a) pyrazines and tetrahydrotriazolo (4,3-a) pyrazines, pharmaceutical compositions comprising the compounds, and use of the compounds in the manufacture of medicaments for use in the treatment of type II diabetes. |
HK05101300A HK1068882A1 (en) | 2001-07-06 | 2005-02-16 | Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4,3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
US11/500,252 US20060270679A1 (en) | 2001-07-06 | 2006-08-07 | Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
IL178307A IL178307A (en) | 2001-07-06 | 2006-09-26 | PHARMACEUTICAL COMPOSITION COMPRISING A TETRAHYDROTRIAZOLO[4,3-a]PYRAZINE |
IS8617A IS2964B (en) | 2001-07-06 | 2007-03-06 | Beta-amino tetrahydroimidazo (1,2-a) pyrazine and tetrahydrotiazolo (4,3-a) pyrazine for use in the treatment of type II diabetes |
NL300287C NL300287I2 (en) | 2001-07-06 | 2007-08-16 | Beta-amino tetrahydroimidazo (1,2-A) pyrazines and tetrehydrotriazolo (4,3-A) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
CY2007019C CY2007019I2 (en) | 2001-07-06 | 2007-08-23 | B-AMINO-TETRAHYDROIMIDAZO-(1,2-A)-PYRASINES AND TETRAHYDROTRIAZOLE-(4,3-A)-PYRASINES AS DIPEPTIDYLPEPTIDASE INHIBITORS FOR THE INDUCTION OR PREVENTION OF DIABETES |
FR07C0041C FR07C0041I2 (en) | 2001-07-06 | 2007-08-27 | BETA-AMINO-TETRAHYDROIMIDAZO(1, 2-A)PYRAZINES AND BETA-AMINO-TETRAHYDROTRIOAZOLO(4, 3-A)PYRAZINES USED AS DIPEPTIDYL PEPTIDASE INHIBITORS IN THE TREATMENT OR PREVENTION OF DIABETES |
LU91360C LUC91360I2 (en) | 2001-07-06 | 2007-09-05 | |
NO2007010C NO2007010I2 (en) | 2001-07-06 | 2007-09-06 | Sitagliptin, optionally in the form of a pharmaceutically acceptable salt |
LTPA2007006C LTC1412357I2 (en) | 2001-07-06 | 2007-09-12 | Beta-amino tetrahydroimidazo (1,2-a) pyrazines and tetrahydrotrazole (4,3-A) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
BE2007C047C BE2007C047I2 (en) | 2001-07-06 | 2007-09-13 | |
NL300357C NL300357I2 (en) | 2001-07-06 | 2008-08-15 | Beta-amino tetrahydroimidazo (1,2-A) pyrazines and |
LU91470C LU91470I2 (en) | 2001-07-06 | 2008-08-18 | Beta-amino-tetrahydroimidazo (1,2-A) pyrazines and betaamino-tetrahydrotrioazolo (4,3-A) pyrazines used as inhibitors of dipeptidyl peptibase in the treatment or prevention of diabetes |
FR08C0033C FR08C0033I2 (en) | 2001-07-06 | 2008-08-21 | BETA-AMINO-TETRAHYDROIMIDAZO(1, 2-A)PYRAZINES AND BETA-AMINO-TETRAHYDROTRIOAZOLO(4, 3-A)PYRAZINES USED AS DIPEPTIDYL PEPTIDASE INHIBITORS IN THE TREATMENT OR PREVENTION OF DIABETES |
NO2008013C NO2008013I2 (en) | 2001-07-06 | 2008-08-22 | Sitagliptin, optionally in the form of a pharmaceutically acceptable salt, especially the monophosphate, plus metformin hydrochloride. |
CY200800014C CY2008014I2 (en) | 2001-07-06 | 2008-09-09 | B-AMINO-TETRAHYDROIMIDAZO-(1,2-A)-PYRASINES AND TETRAHYDROTRIAZOLE-(4,3-A)-PYRASINES AS DIPEPTIDYLPEPTIDASE INHIBITORS FOR THE INDUCTION OR PREVENTION OF DIABETES |
US12/694,758 US8168637B2 (en) | 2001-07-06 | 2010-01-27 | Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment of diabetes |
US13/086,563 US8440668B2 (en) | 2001-07-06 | 2011-04-14 | Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment of type 2 diabetes |
NO2020007C NO2020007I1 (en) | 2001-07-06 | 2020-03-19 | Sitagliptin, optionally in the form of a pharmaceutically acceptable salt |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US30347401P | 2001-07-06 | 2001-07-06 | |
US60/303,474 | 2001-07-06 |
Related Child Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US10481353 A-371-Of-International | 2002-07-05 | ||
US11/500,252 Continuation US20060270679A1 (en) | 2001-07-06 | 2006-08-07 | Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2003004498A1 true WO2003004498A1 (en) | 2003-01-16 |
Family
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Family Applications (1)
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PCT/US2002/021349 WO2003004498A1 (en) | 2001-07-06 | 2002-07-05 | Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
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