NZ245207A - Preparation of prolineboronate esters; peptides with a prolineboronic acid ester at the c-terminus - Google Patents

Preparation of prolineboronate esters; peptides with a prolineboronic acid ester at the c-terminus

Info

Publication number
NZ245207A
NZ245207A NZ24520792A NZ24520792A NZ245207A NZ 245207 A NZ245207 A NZ 245207A NZ 24520792 A NZ24520792 A NZ 24520792A NZ 24520792 A NZ24520792 A NZ 24520792A NZ 245207 A NZ245207 A NZ 245207A
Authority
NZ
New Zealand
Prior art keywords
pyrrolidine
boronic acid
formula
protected
pinanediol
Prior art date
Application number
NZ24520792A
Other languages
English (en)
Inventor
Roger Snow
Terence A Kelly
Julian Adams
Simon Coutts
Clark Perry
Original Assignee
Boehringer Ingelheim Pharma
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
Application filed by Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma
Publication of NZ245207A publication Critical patent/NZ245207A/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrrole Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
NZ24520792A 1991-11-22 1992-11-20 Preparation of prolineboronate esters; peptides with a prolineboronic acid ester at the c-terminus NZ245207A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US79614891A 1991-11-22 1991-11-22
US93619892A 1992-08-26 1992-08-26

Publications (1)

Publication Number Publication Date
NZ245207A true NZ245207A (en) 1994-07-26

Family

ID=27121696

Family Applications (1)

Application Number Title Priority Date Filing Date
NZ24520792A NZ245207A (en) 1991-11-22 1992-11-20 Preparation of prolineboronate esters; peptides with a prolineboronic acid ester at the c-terminus

Country Status (17)

Country Link
EP (1) EP0641347A1 (enrdf_load_html_response)
JP (1) JPH07501078A (enrdf_load_html_response)
CN (1) CN1073946A (enrdf_load_html_response)
AU (1) AU661362B2 (enrdf_load_html_response)
CA (1) CA2123128A1 (enrdf_load_html_response)
CZ (1) CZ124494A3 (enrdf_load_html_response)
FI (1) FI942345A7 (enrdf_load_html_response)
HU (1) HUT67937A (enrdf_load_html_response)
IL (1) IL103817A0 (enrdf_load_html_response)
MX (1) MX9206628A (enrdf_load_html_response)
NO (1) NO941905L (enrdf_load_html_response)
NZ (1) NZ245207A (enrdf_load_html_response)
PT (1) PT101079A (enrdf_load_html_response)
SI (1) SI9200332A (enrdf_load_html_response)
SK (1) SK59294A3 (enrdf_load_html_response)
TW (1) TW232697B (enrdf_load_html_response)
WO (1) WO1993010127A1 (enrdf_load_html_response)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6825169B1 (en) 1991-10-22 2004-11-30 Trustees Of Tufts College Inhibitors of dipeptidyl-aminopeptidase type IV
US5965532A (en) * 1996-06-28 1999-10-12 Trustees Of Tufts College Multivalent compounds for crosslinking receptors and uses thereof
US6040145A (en) 1997-05-07 2000-03-21 Tufts University Potentiation of the immune response
US6100234A (en) 1997-05-07 2000-08-08 Tufts University Treatment of HIV
NZ503359A (en) 1997-09-29 2002-02-01 Point Therapeutics Inc Method for proliferating haematopoietic cells in vitro in the absence of exogenous cytokines
CA2331122A1 (en) 1998-05-04 1999-11-11 Point Therapeutics, Inc. Hematopoietic stimulation
US6355614B1 (en) * 1998-06-05 2002-03-12 Point Therapeutics Cyclic boroproline compounds
US6979697B1 (en) 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
US6890904B1 (en) 1999-05-25 2005-05-10 Point Therapeutics, Inc. Anti-tumor agents
JP2003523396A (ja) * 2000-02-25 2003-08-05 ノボ ノルディスク アクティーゼルスカブ ベータ細胞変性の抑制
WO2003063903A2 (en) * 2002-02-01 2003-08-07 Probiodrug Ag Modulation of t lymphocytes using dp iv inhibitors
US7317109B2 (en) 2003-11-12 2008-01-08 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
WO2005047297A1 (en) 2003-11-12 2005-05-26 Phenomix Corporation Heterocyclic boronic acid compounds
US7576121B2 (en) 2003-11-12 2009-08-18 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
US7767828B2 (en) 2003-11-12 2010-08-03 Phenomix Corporation Methyl and ethyl substituted pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
KR20140089408A (ko) 2003-11-17 2014-07-14 노파르티스 아게 디펩티딜 펩티다제 ⅳ 억제제의 용도
US20080038341A1 (en) 2004-01-20 2008-02-14 James Kowalski Direct Compression Formulation And Process
WO2005105817A2 (en) * 2004-04-27 2005-11-10 Wyeth Coupling process for generating reactive boron­ containing derivatives of n-substituted pyrrole-2­ carbonitriles to produce biaryls
DOP2006000008A (es) 2005-01-10 2006-08-31 Arena Pharm Inc Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1
CA2606785A1 (en) 2005-05-19 2006-11-23 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods
US7825139B2 (en) 2005-05-25 2010-11-02 Forest Laboratories Holdings Limited (BM) Compounds and methods for selective inhibition of dipeptidyl peptidase-IV
CN1331835C (zh) * 2005-10-18 2007-08-15 武汉大学 光活性β-羟基酮的制备方法
CN101379069A (zh) * 2005-12-19 2009-03-04 塔夫茨大学信托人 软蛋白酶抑制剂及其前软形式
PE20071221A1 (es) 2006-04-11 2007-12-14 Arena Pharm Inc Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas
MEP27308A (en) 2006-04-11 2010-06-10 Arena Pharm Inc Methods of using gpr119 receptor to identify compounds useful for increasing bone mass in an individual
EP2146210A1 (en) 2008-04-07 2010-01-20 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY
MX358222B (es) * 2008-06-17 2018-08-10 Millennium Pharm Inc Compuestos de ester boronato y composiciones farmaceuticas de los mismos.
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
CN102918027A (zh) 2010-04-06 2013-02-06 艾尼纳制药公司 Gpr119受体调节剂和对与所述受体有关的障碍的治疗
BR112013008100A2 (pt) 2010-09-22 2016-08-09 Arena Pharm Inc "moduladores do receptor de gpr19 e o tratamento de distúrbios relacionados a eles."
WO2012135570A1 (en) 2011-04-01 2012-10-04 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145361A1 (en) 2011-04-19 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145604A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145603A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
US9523687B2 (en) 2014-02-28 2016-12-20 Institut Pasteur Levels of CXCL 10/IP-10 forms and soluble CD26/DPPIV activity as early predictive biomarkers for HIV/SIV associated mucosal inflammation and progression towards AIDS
EA201692332A1 (ru) 2014-05-20 2017-04-28 Милленниум Фармасьютикалз, Инк. Борсодержащие ингибиторы протеасом для применения после первичной противораковой терапии
MA42450A (fr) 2015-03-09 2018-05-23 Intekrin Therapeutics Inc Méthodes de traitement de la stéatose hépatique non alcoolique et/ou de la lipodystrophie
WO2018162722A1 (en) 2017-03-09 2018-09-13 Deutsches Institut Für Ernährungsforschung Potsdam-Rehbrücke Dpp-4 inhibitors for use in treating bone fractures
JP2020515639A (ja) 2017-04-03 2020-05-28 コヒラス・バイオサイエンシズ・インコーポレイテッド 進行性核上性麻痺の処置のためのPPARγアゴニスト
CN108047257B (zh) * 2017-12-17 2020-03-13 沧州普瑞东方科技有限公司 一种手性n-boc-吡咯烷-2-硼酸的制备工艺
JP7273854B2 (ja) * 2018-02-20 2023-05-15 大塚製薬株式会社 4-ボロノフェニルアラニンの製造方法
CN110452258B (zh) * 2019-09-03 2021-01-01 上海馨远医药科技有限公司 一种二肽缬氨酸硼脯氨酸盐的制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4935493A (en) * 1987-10-06 1990-06-19 E. I. Du Pont De Nemours And Company Protease inhibitors
ATE148130T1 (de) * 1990-04-14 1997-02-15 New England Medical Center Inc Typ-iv-dipeptidyl-aminopeptidase-inhibitoren
GB9017694D0 (en) * 1990-08-13 1990-09-26 Sandoz Ltd Improvements in or relating to organic chemistry

Also Published As

Publication number Publication date
HU9401350D0 (en) 1994-08-29
CZ124494A3 (en) 1995-07-12
AU3136893A (en) 1993-06-15
FI942345A0 (fi) 1994-05-20
IL103817A0 (en) 1993-04-04
SI9200332A (en) 1993-06-30
JPH07501078A (ja) 1995-02-02
CA2123128A1 (en) 1993-05-27
NO941905D0 (no) 1994-05-20
NO941905L (no) 1994-07-14
HUT67937A (en) 1995-05-29
WO1993010127A1 (en) 1993-05-27
TW232697B (enrdf_load_html_response) 1994-10-21
SK59294A3 (en) 1995-02-08
AU661362B2 (en) 1995-07-20
MX9206628A (es) 1993-05-01
EP0641347A1 (en) 1995-03-08
PT101079A (pt) 1994-02-28
FI942345A7 (fi) 1994-05-20
CN1073946A (zh) 1993-07-07

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