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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pyrrole Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (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 (OSRAM)
JP (1) JPH07501078A (OSRAM)
CN (1) CN1073946A (OSRAM)
AU (1) AU661362B2 (OSRAM)
CA (1) CA2123128A1 (OSRAM)
CZ (1) CZ124494A3 (OSRAM)
FI (1) FI942345A0 (OSRAM)
HU (1) HUT67937A (OSRAM)
IL (1) IL103817A0 (OSRAM)
MX (1) MX9206628A (OSRAM)
NO (1) NO941905L (OSRAM)
NZ (1) NZ245207A (OSRAM)
PT (1) PT101079A (OSRAM)
SI (1) SI9200332A (OSRAM)
SK (1) SK59294A3 (OSRAM)
TW (1) TW232697B (OSRAM)
WO (1) WO1993010127A1 (OSRAM)

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
TR200000815T2 (tr) 1997-09-29 2000-12-21 Point Therapeutics Inc. In vitro hematopoietik hücrelerin stimulasyonu.
EP1075266A1 (en) 1998-05-04 2001-02-14 Point Therapeutics, Inc. Hematopoietic stimulation
BR9910907A (pt) * 1998-06-05 2002-02-13 Point Therapeutics Inc Compostos cìclicos de boroprolina
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
WO2001062266A2 (en) * 2000-02-25 2001-08-30 Novo Nordisk A/S Use of dpp-iv inhibitors for the treatment of diabetes
AU2003218969A1 (en) * 2002-02-01 2003-09-02 Probiodrug Ag Modulation of t lymphocytes using dp iv inhibitors
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
US7317109B2 (en) 2003-11-12 2008-01-08 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
BRPI0416444B8 (pt) 2003-11-12 2021-05-25 Chiesi Farm Spa composto de ácido borônico heterocíclico, composição farmacêutica, e, combinação farmacêutica compreendendo o mesmo
KR20120008093A (ko) 2003-11-17 2012-01-25 노파르티스 아게 디펩티딜 펩티다제 ⅳ 억제제의 용도
PT3738585T (pt) 2004-01-20 2023-01-30 Novartis Ag Formulação e processo de compressão direta
SV2005002092A (es) 2004-04-27 2005-12-13 Wyeth Corp " proceso de acoplamiento para la generacion de derivados reactivos de pirrol-2-carbonitrilo n-sustituidos con contenido de boro para producir biarilos " ref. am - 101481salvo.
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
AU2006246719A1 (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
US7833730B2 (en) 2006-04-11 2010-11-16 Arena Pharmaceuticals, Inc. Methods of using GPR119 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
GEP201706703B (en) 2008-06-17 2017-07-25 Millennium Pharmaceuticals Inc (A Delaware Corporation) Boronate ester compounds and pharmaceutical compositions thereof
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
US20130023494A1 (en) 2010-04-06 2013-01-24 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
CN103221410B (zh) 2010-09-22 2017-09-15 艾尼纳制药公司 Gpr119受体调节剂和对与其相关的障碍的治疗
US20140018371A1 (en) 2011-04-01 2014-01-16 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
US20140066369A1 (en) 2011-04-19 2014-03-06 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
US20140051714A1 (en) 2011-04-22 2014-02-20 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
KR102509950B1 (ko) 2014-05-20 2023-03-14 밀레니엄 파머슈티컬스 인코퍼레이티드 일차 암 치료법 후 사용하기 위한 붕소-함유 프로테아좀 저해제
WO2016144862A1 (en) 2015-03-09 2016-09-15 Intekrin Therapeutics, Inc. Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy
WO2018162722A1 (en) 2017-03-09 2018-09-13 Deutsches Institut Für Ernährungsforschung Potsdam-Rehbrücke Dpp-4 inhibitors for use in treating bone fractures
CN110996951A (zh) 2017-04-03 2020-04-10 科赫罗斯生物科学股份有限公司 治疗进行性核上性麻痹的PPARγ激动剂
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
PL3755681T3 (pl) * 2018-02-20 2022-11-28 Otsuka Pharmaceutical Co., Ltd. Sposób wytwarzania 4-boronofenyloalaniny
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
EP0528858B1 (en) * 1990-04-14 1997-01-22 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type iv
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
HUT67937A (en) 1995-05-29
AU661362B2 (en) 1995-07-20
NO941905L (no) 1994-07-14
PT101079A (pt) 1994-02-28
FI942345A7 (fi) 1994-05-20
AU3136893A (en) 1993-06-15
CZ124494A3 (en) 1995-07-12
SK59294A3 (en) 1995-02-08
JPH07501078A (ja) 1995-02-02
NO941905D0 (no) 1994-05-20
FI942345A0 (fi) 1994-05-20
TW232697B (OSRAM) 1994-10-21
EP0641347A1 (en) 1995-03-08
IL103817A0 (en) 1993-04-04
SI9200332A (en) 1993-06-30
CA2123128A1 (en) 1993-05-27
MX9206628A (es) 1993-05-01
WO1993010127A1 (en) 1993-05-27
CN1073946A (zh) 1993-07-07

Similar Documents

Publication Publication Date Title
AU661362B2 (en) Method for making a prolineboronate ester
US5384410A (en) Removal of boronic acid protecting groups by transesterification
Katz et al. Episelection: novel Ki. apprx. nanomolar inhibitors of serine proteases selected by binding or chemistry on an enzyme surface
KR100939598B1 (ko) 붕소산 에스테르와 산 화합물의 합성
US5462928A (en) Inhibitors of dipeptidyl-aminopeptidase type IV
CA2121369C (en) Inhibitors of dipeptidyl-aminopeptidase type iv
CA2080474A1 (en) Inhibitors of dipeptidyl-aminopeptidase type iv
Wityak et al. Synthesis of thrombin inhibitor DuP 714
EP0724446A1 (en) Electrophilic peptide analogs as inhibitors of trypsin-like enzymes
EP1743676A1 (en) Heterocyclic boronic acid derivatives, dipeptidyl peptidase IV inhibitors
JP2022068192A (ja) 銅およびニッケル触媒による脱炭酸ホウ素化反応
CA2174311A1 (en) Boropeptide inhibitors of thrombin which contain a substituted pyrrolidine ring
Shue et al. Novel methodology for the synthesis of trans-alkene dipeptide isosteres
AU2003299042A1 (en) Process for the synthesis of intermediates useful for the synthesis of tubulin inhibitors
Demizu et al. Convenient synthesis of an enantiomerically pure bicyclic proline and its N-oxyl derivatives
Elgendy et al. Facile routes to 1-halo-1-alkyl boronic esters as precursors for novel thrombin inhibitors
Aggarwal et al. Synthesis of new, highly hindered C2-symmetric trans-(2S, 5S)-disubstituted pyrrolidines
US5543526A (en) 1-amino-4-(1H-imidazole)- aminobutaneboronic acid derivatives, their preparation and use as synthetic intermediates
Taylor et al. The conversion of pentoses to 3, 4-dihydroxyprolines
EP0379063A2 (en) Process for preparing (trans)-4-substituted-DL-proline derivatives
Hennings et al. Synthesis of (S, S)-and (R, R)-2-amino-3-methylaminobutanoic acid (AMBA)
US5473092A (en) Synthesis of optically-active phosphono analogs of succinates
Peper et al. Utilization of industrial waste materials, 5. Synthesis of new, chiral 1, 3, 2‐oxazaphospholidine‐borane complexes and attempts to apply them in the stereoselective synthesis
US20080261923A1 (en) Alkene Mimics
HK40066099A (en) Synthesis of boronic ester and acid compounds