WO2001068603A3 - Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl iv, processes for their preparation, and their use - Google Patents

Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl iv, processes for their preparation, and their use Download PDF

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Publication number
WO2001068603A3
WO2001068603A3 PCT/US2001/007151 US0107151W WO0168603A3 WO 2001068603 A3 WO2001068603 A3 WO 2001068603A3 US 0107151 W US0107151 W US 0107151W WO 0168603 A3 WO0168603 A3 WO 0168603A3
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WO
WIPO (PCT)
Prior art keywords
dipeptidyl
cyclopropyl
processes
preparation
based inhibitors
Prior art date
Application number
PCT/US2001/007151
Other languages
French (fr)
Other versions
WO2001068603A2 (en
Inventor
Jeffrey A Robl
Richard B Sulsky
David J Augeri
David R Magnin
Lawrence G Hamann
David A Betebenner
Original Assignee
Bristol Myers Squibb Co
Jeffrey A Robl
Richard B Sulsky
David J Augeri
David R Magnin
Lawrence G Hamann
David A Betebenner
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22693638&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2001068603(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to ES01918383T priority Critical patent/ES2305062T3/en
Application filed by Bristol Myers Squibb Co, Jeffrey A Robl, Richard B Sulsky, David J Augeri, David R Magnin, Lawrence G Hamann, David A Betebenner filed Critical Bristol Myers Squibb Co
Priority to MXPA02008837A priority patent/MXPA02008837A/en
Priority to CA2402894A priority patent/CA2402894C/en
Priority to KR1020067004515A priority patent/KR100758407B1/en
Priority to JP2001567699A priority patent/JP4460205B2/en
Priority to DE122010000008C priority patent/DE122010000008I1/en
Priority to PL365520A priority patent/PL207041B1/en
Priority to DE60134122T priority patent/DE60134122D1/en
Priority to AU4546601A priority patent/AU4546601A/en
Priority to HU1200546A priority patent/HU230380B1/en
Priority to HU0302792A priority patent/HU228110B1/en
Priority to CZ2015493A priority patent/CZ307821B6/cs
Priority to BRPI0109115A priority patent/BRPI0109115B8/en
Priority to NZ520821A priority patent/NZ520821A/en
Priority to KR1020027011806A priority patent/KR100754089B1/en
Priority to HU1200545A priority patent/HU230347B1/en
Priority to EP01918383A priority patent/EP1261586B1/en
Priority to IL15137201A priority patent/IL151372A0/en
Priority to EP15186007.9A priority patent/EP2995615B1/en
Priority to AU2001245466A priority patent/AU2001245466B2/en
Priority to DK01918383T priority patent/DK1261586T3/en
Publication of WO2001068603A2 publication Critical patent/WO2001068603A2/en
Publication of WO2001068603A3 publication Critical patent/WO2001068603A3/en
Priority to IL151372A priority patent/IL151372A/en
Priority to NO20024295A priority patent/NO324227B1/en
Priority to HK03101079.9A priority patent/HK1049330B/en
Priority to IL177018A priority patent/IL177018A0/en
Priority to IL177019A priority patent/IL177019A/en
Priority to CY20081100885T priority patent/CY1108273T1/en
Priority to BE2010C008C priority patent/BE2010C008I2/fr
Priority to LU91650C priority patent/LU91650I2/en
Priority to NL300436C priority patent/NL300436I1/en
Priority to FR10C0010C priority patent/FR10C0010I2/en
Priority to NO2010006C priority patent/NO2010006I2/en
Priority to CY2010005C priority patent/CY2010005I1/en
Priority to BE2012C016C priority patent/BE2012C016I2/fr
Priority to DE201212000023 priority patent/DE122012000023I1/en
Priority to CY2012009C priority patent/CY2012009I2/en
Priority to LU91985C priority patent/LU91985I2/en
Priority to NO2012009C priority patent/NO2012009I2/en
Priority to HUS1200031C priority patent/HUS1200031I1/en
Priority to HUS1200030C priority patent/HUS1200030I1/en

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Abstract

Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula (I) where x is 0 or 1 and y is 0 or 1 (provided that x = 1 when y = 0 and x = 0 when y = 1); n is 0 or 1; X is H or CN; and wherein R?1, R2, R3 and R4¿ are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.
PCT/US2001/007151 2000-03-10 2001-03-05 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl iv, processes for their preparation, and their use WO2001068603A2 (en)

Priority Applications (40)

Application Number Priority Date Filing Date Title
DK01918383T DK1261586T3 (en) 2000-03-10 2001-03-05 Cyclopropyl Condensed Dipeptidyl Peptidase IV Inhibitors Based on Pyrrolidine, Methods for their Preparation and Use
HU0302792A HU228110B1 (en) 2000-03-10 2001-03-05 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase iv and method for their preparation and pharmaceutical compositions containing the compounds
MXPA02008837A MXPA02008837A (en) 2000-03-10 2001-03-05 Cyclopropyl fused pyrrolidine based inhibitors of dipeptidyl peptidase iv and method.
CA2402894A CA2402894C (en) 2000-03-10 2001-03-05 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase iv and method
KR1020067004515A KR100758407B1 (en) 2000-03-10 2001-03-05 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl iv, processes for their preparation, and their use
JP2001567699A JP4460205B2 (en) 2000-03-10 2001-03-05 Inhibitors and methods for dipeptidyl peptidase IV having a cyclopropyl-fused pyrrolidine skeleton
DE122010000008C DE122010000008I1 (en) 2000-03-10 2001-03-05 CYCLOPROPYL-CONDENSED DIPEPTIDYL-PEPTIDASE IV HEMMER BASED ON PYRROLIDINE, PROCESS FOR THEIR PREPARATION AND THEIR USE
PL365520A PL207041B1 (en) 2000-03-10 2001-03-05 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl iv, processes for their preparation, and their use
DE60134122T DE60134122D1 (en) 2000-03-10 2001-03-05 CYCLOPROPYL-CONDENSED DIPEPTIDYL-PEPTIDASE IV HEMMER BASED ON PYRROLIDINE, PROCESS FOR THEIR PREPARATION AND THEIR USE
AU4546601A AU4546601A (en) 2000-03-10 2001-03-05 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase iv and method
HU1200546A HU230380B1 (en) 2000-03-10 2001-03-05 N-protected amino hydroxy adamantane carboxylic acid and process for producing the same
ES01918383T ES2305062T3 (en) 2000-03-10 2001-03-05 INHIBITORS BASED ON PIROLIDINE CONDENSED WITH CYCLOPROPYL OF PIPEPTIDIL PEPTIDASE IV, PROCEDURES FOR THEIR PREPARATION, AND THEIR USE.
NZ520821A NZ520821A (en) 2000-03-10 2001-03-05 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV, method ofr preparation, and their use
BRPI0109115A BRPI0109115B8 (en) 2000-03-10 2001-03-05 fused cyclopropyl pyrrolidine-based dipeptidyl peptidase inhibitors iv and method
CZ2015493A CZ307821B6 (en) 2000-03-10 2001-03-05
KR1020027011806A KR100754089B1 (en) 2000-03-10 2001-03-05 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl iv, processes for their preparation, and their use
HU1200545A HU230347B1 (en) 2000-03-10 2001-03-05 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase iv, process for their preparation and their use
EP01918383A EP1261586B1 (en) 2000-03-10 2001-03-05 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase iv, processes for their preparation, and their use
IL15137201A IL151372A0 (en) 2000-03-10 2001-03-05 Cyclopropyl-fused pyrrolidine derivatives and pharmaceutical compositions containing the same
EP15186007.9A EP2995615B1 (en) 2000-03-10 2001-03-05 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase iv and their pharmaceutical use
AU2001245466A AU2001245466B2 (en) 2000-03-10 2001-03-05 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl IV, processes for their preparation, and their use
IL151372A IL151372A (en) 2000-03-10 2002-08-21 Cyclopropyl-fused pyrrolidine derivatives and pharmaceutical compositions containing the same
NO20024295A NO324227B1 (en) 2000-03-10 2002-09-09 Cyclopropyl-fused pyrrolidine-based compounds, pharmaceutical compositions and combinations containing them as well as the use thereof for the manufacture of medicaments for the treatment of diseases
HK03101079.9A HK1049330B (en) 2000-03-10 2003-02-14 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase iv, processes for their preparation, and their use
IL177018A IL177018A0 (en) 2000-03-10 2006-07-23 Cyclopropyl-fused pyrrolidine derivatives and pharmaceutical compositions containing the same
IL177019A IL177019A (en) 2000-03-10 2006-07-23 Protected amino hydroxyl adamantane carboxylic acid and methods for the preparation thereof
CY20081100885T CY1108273T1 (en) 2000-03-10 2008-08-20 PYRROLIDINE-BASED INHIBITORS OF CYCLOPROPYL-FUSED DIPEPTYLPEPTIDASE 4 AND METHODS OF THEIR PREPARATION AND USE
BE2010C008C BE2010C008I2 (en) 2000-03-10 2010-02-11
LU91650C LU91650I2 (en) 2000-03-10 2010-02-17 Saxagliptin and pharmaceutically acceptable salts thereof, including saxagliptin hydrochloride - Onglyza-saxagliptin
NL300436C NL300436I1 (en) 2000-03-10 2010-02-17 Cyclopropyl-condensed pyrrolidine-based dipeptidyl peptidase IV inhibitors, methods for their preparation, and their use.
FR10C0010C FR10C0010I2 (en) 2000-03-10 2010-02-22 DIPEPTIDYL-PEPTIDASE IV INHIBITORS COMPRISING A FUSED PYRROLIDINE AND CYCLOPROPYL, PROCESSES FOR THEIR PREPARATION AND USE OF THESE COMPOUNDS
NO2010006C NO2010006I2 (en) 2000-03-10 2010-03-16 Saxagliptin and its pharmaceutically acceptable salts, including Saxagliptin hydrochloride
CY2010005C CY2010005I1 (en) 2000-03-10 2010-03-30 PYRROLIDINE-BASED INHIBITORS OF CYCLOPROPYL-FUSED DIPEPTYLPEPTIDASE 4 AND METHODS OF THEIR PREPARATION AND USE
BE2012C016C BE2012C016I2 (en) 2000-03-10 2012-04-18
DE201212000023 DE122012000023I1 (en) 2000-03-10 2012-04-23 Cyclopropyl-fused dipeptidyl-peptidase-IV inhibitors based on pyrrolidine, process for their preparation and their use.
CY2012009C CY2012009I2 (en) 2000-03-10 2012-04-24 PYRROLIDINE-BASED INHIBITORS OF CYCLOPROPYL-FUSED DIPEPTYLPEPTIDASE 4 AND METHODS OF THEIR PREPARATION AND USE
LU91985C LU91985I2 (en) 2000-03-10 2012-04-25 A combination product of Saxagliptin and metformin and pharmaceutically acceptable salts thereof, including the salts of Saxgliptin hydrochloride and metformin
NO2012009C NO2012009I2 (en) 2000-03-10 2012-05-21 Combination product of saxaglipin and metformin and pharmaceutically acceptable salts thereof, including the HCI salts of saxaglipin and metformin
HUS1200031C HUS1200031I1 (en) 2000-03-10 2012-12-14 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase iv and method for their preparation and pharmaceutical compositions containing the compounds
HUS1200030C HUS1200030I1 (en) 2000-03-10 2012-12-14 Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase iv and method for their preparation and pharmaceutical compositions containing the compounds

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US18855500P 2000-03-10 2000-03-10
US60/188,555 2000-03-10

Publications (2)

Publication Number Publication Date
WO2001068603A2 WO2001068603A2 (en) 2001-09-20
WO2001068603A3 true WO2001068603A3 (en) 2002-02-14

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US8883714B2 (en) 2008-04-07 2014-11-11 Arena Pharmaceuticals, Inc. Pharmaceutical compositions comprising GPR119 agonists which act as peptide YY (PYY) secretagogues
US9457029B2 (en) 2009-11-27 2016-10-04 Boehringer Ingelheim International Gmbh Treatment of genotyped diabetic patients with DPP-IV inhibitors such as linagliptin
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof

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