NO333251B1 - Fremgangsmate for fremstilling av N-substituerte 2-cyanopyrrolidoner - Google Patents

Fremgangsmate for fremstilling av N-substituerte 2-cyanopyrrolidoner

Info

Publication number: NO333251B1
Authority: NO; Norway
Prior art keywords: reaction; preparation; resulting compound; substituted; cyanopyrrolidones
Prior art date: 2003-04-16

Application number

NO20055226A

Other languages

English (en)

Norwegian (no)

Other versions

NO20055226L (no

Inventor

Gottfried Sedelmeier

Frank Schafer

Original Assignee

Novartis Ag

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.)

2003-04-16

Filing date

2005-11-07

Publication date

2013-04-22

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33301223&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NO333251(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2003-04-16 Priority claimed from GB0308854A external-priority patent/GB0308854D0/en

2003-05-22 Priority claimed from GB0311836A external-priority patent/GB0311836D0/en

2005-11-07 Application filed by Novartis Ag filed Critical Novartis Ag

2005-11-07 Publication of NO20055226L publication Critical patent/NO20055226L/no

2013-04-22 Publication of NO333251B1 publication Critical patent/NO333251B1/no

Links

238000000034 method Methods 0.000 title abstract 2
238000002360 preparation method Methods 0.000 title abstract 2
150000001875 compounds Chemical class 0.000 abstract 4
ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 abstract 3
229910052736 halogen Inorganic materials 0.000 abstract 2
238000002955 isolation Methods 0.000 abstract 2
VLJNHYLEOZPXFW-BYPYZUCNSA-N L-prolinamide Chemical compound NC(=O)[C@@H]1CCCN1 VLJNHYLEOZPXFW-BYPYZUCNSA-N 0.000 abstract 1
-1 N- (N'-substituted glycyl) -2-cyanopyrrolidine Chemical class 0.000 abstract 1
239000002253 acid Substances 0.000 abstract 1
125000000217 alkyl group Chemical group 0.000 abstract 1
150000001412 amines Chemical class 0.000 abstract 1
125000003118 aryl group Chemical group 0.000 abstract 1
239000012024 dehydrating agents‎ Substances 0.000 abstract 1
125000005843 halogen group Chemical group 0.000 abstract 1
150000002367 halogens Chemical class 0.000 abstract 1
238000011084 recovery Methods 0.000 abstract 1
150000003839 salts Chemical group 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/401—Proline; Derivatives thereof, e.g. captopril
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
General Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
Diabetes (AREA)
Medicinal Chemistry (AREA)
Public Health (AREA)
Animal Behavior & Ethology (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Obesity (AREA)
Hematology (AREA)
Endocrinology (AREA)
Emergency Medicine (AREA)
Epidemiology (AREA)
Pyrrole Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Plural Heterocyclic Compounds (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

NO20055226A 2003-04-16 2005-11-07 Fremgangsmate for fremstilling av N-substituerte 2-cyanopyrrolidoner NO333251B1 (no)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
GB0308854A GB0308854D0 (en)	2003-04-16	2003-04-16	Organic compounds
GB0311836A GB0311836D0 (en)	2003-05-22	2003-05-22	Process for the manufacture of organic compounds
PCT/EP2004/003980 WO2004092127A1 (en)	2003-04-16	2004-04-15	Process for the preparation of n-substituted 2-cyanopyrrolidines

Publications (2)

Publication Number	Publication Date
NO20055226L NO20055226L (no)	2005-11-07
NO333251B1 true NO333251B1 (no)	2013-04-22

Family

ID=33301223

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
NO20055226A NO333251B1 (no)	2003-04-16	2005-11-07	Fremgangsmate for fremstilling av N-substituerte 2-cyanopyrrolidoner

Country Status (30)

Country	Link
US (1)	US7375238B2 (pt)
EP (1)	EP1620396B1 (pt)
JP (1)	JP4672647B2 (pt)
KR (1)	KR101192538B1 (pt)
AR (1)	AR044019A1 (pt)
AU (2)	AU2004230245B2 (pt)
BR (1)	BRPI0409471B8 (pt)
CA (1)	CA2520128C (pt)
CL (1)	CL2004000804A1 (pt)
CO (1)	CO5700735A2 (pt)
CY (1)	CY1116008T1 (pt)
DK (1)	DK1620396T3 (pt)
EC (1)	ECSP056093A (pt)
ES (1)	ES2531084T3 (pt)
HR (1)	HRP20150163T1 (pt)
IL (1)	IL170887A (pt)
IS (1)	IS2979B (pt)
MA (1)	MA27765A1 (pt)
MX (1)	MXPA05011073A (pt)
MY (1)	MY139476A (pt)
NO (1)	NO333251B1 (pt)
NZ (1)	NZ542899A (pt)
PE (2)	PE20081293A1 (pt)
PL (1)	PL1620396T3 (pt)
PT (1)	PT1620396E (pt)
RU (1)	RU2369598C2 (pt)
SG (1)	SG160212A1 (pt)
SI (1)	SI1620396T1 (pt)
TW (1)	TWI359135B (pt)
WO (1)	WO2004092127A1 (pt)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
PE20081293A1 (es)	2003-04-16	2008-11-04	Novartis Ag	Procedimiento de preparacion de compuestos 2(s)-cianopirrolidina n-(n'-glicilo sustituida)
EP3366283B1 (en)	2004-01-20	2021-09-01	Novartis AG	Direct compression formulation and process
GT200600008A (es)	2005-01-18	2006-08-09		Formulacion de compresion directa y proceso
CN101277949A (zh)	2005-04-22	2008-10-01	阿兰托斯制药控股公司	二肽基肽酶-ⅳ抑制剂
WO2007019255A2 (en) *	2005-08-04	2007-02-15	Novartis Ag	Salts of vildagliptin
WO2008066083A1 (fr) *	2006-11-29	2008-06-05	Mitsubishi Tanabe Pharma Corporation	Procédé de production d'un dérivé de n-(n'-glycyle substitué)-2-cyanopyrrolidine
WO2008084383A2 (en) *	2007-01-10	2008-07-17	Medichem, S.A.	Process for preparing vildagliptin
CZ2008512A3 (cs)	2008-08-26	2010-03-10	Zentiva, A. S	Zpusob prípravy vysoce cistého vildagliptinu
SI2459531T1 (sl)	2009-07-31	2020-02-28	Krka, D.D., Novo Mesto	Granulat, ki obsega vildagliptin, in postopek njegove priprave
HUP0900638A2 (en) *	2009-10-07	2011-05-30	Egyt Gyogyszervegyeszeti Gyar	Adducts of inorganic salts basea on vildaelitpin applicable for preparation of pharmaceutical compositions
IT1400714B1 (it)	2010-07-06	2013-06-28	Chemelectiva S R L	Processo ed intermedi per la preparazione di un principio attivo.
HU231050B1 (hu)	2010-08-19	2020-02-28	Egis Gyógyszergyár Nyrt.	Eljárás gyógyszerhatóanyag előállítására
ITMI20112224A1 (it) *	2011-12-06	2013-06-07	Chemelectiva S R L	Nuovo processo ed intermedi per la sintesi di vildagliptin
WO2013179300A2 (en) *	2012-05-04	2013-12-05	Megafine Pharma (P) Ltd.	A process for the preparation of vildagliptin and its intermediate thereof
CN103922986B (zh) *	2013-01-16	2017-02-15	上海彩迩文生化科技有限公司	维大列汀及其类似物、中间体及其制备方法和应用
WO2015145467A1 (en) *	2014-03-28	2015-10-01	Laurus Labs Private Limited	An improved process for preparing vildagliptin
WO2021234430A1 (en)	2020-05-17	2021-11-25	Lotus International Pte. Ltd.	Modified release dosage form comprising vildagliptin and process for manufacturing the same
WO2022003405A1 (en)	2020-07-03	2022-01-06	Savoi Guilherme	One-pot process to obtain a pyrrolidine-2-carbonitrile intermediate compound and industrial scale telescopic process to prepare (2s)-1-[n-(3-hydroxyadamantan-1-yl)glycyl]-2-pyrrolidinecarbonitrile (vildagliptin) using same

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5510369A (en) *	1994-07-22	1996-04-23	Merck & Co., Inc.	Pyrrolidine thrombin inhibitors
TW492957B (en) *	1996-11-07	2002-07-01	Novartis Ag	N-substituted 2-cyanopyrrolidnes
CO5150173A1 (es) *	1998-12-10	2002-04-29	Novartis Ag	Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv
US6380398B2 (en) *	2000-01-04	2002-04-30	Novo Nordisk A/S	Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
AU2001228309A1 (en) *	2000-01-24	2001-08-07	Novo-Nordisk A/S	N-substituted 2-cyanopyroles and -pyrrolines which are inhibitors of the enzyme dpp-iv
TW583185B (en) *	2000-06-13	2004-04-11	Novartis Ag	N-(substituted glycyl)-2-cyanopyrrolidines and pharmaceutical composition for inhibiting dipeptidyl peptidase-IV (DPP-IV) or for the prevention or treatment of diseases or conditions associated with elevated levels of DPP-IV comprising the same
JP2002265439A (ja) *	2001-03-08	2002-09-18	Mitsubishi Pharma Corp	シアノピロリジン誘導体およびその医薬用途
PE20081293A1 (es)	2003-04-16	2008-11-04	Novartis Ag	Procedimiento de preparacion de compuestos 2(s)-cianopirrolidina n-(n'-glicilo sustituida)

2004
- 2004-04-14 PE PE2007000421A patent/PE20081293A1/es not_active Application Discontinuation
- 2004-04-14 AR ARP040101251A patent/AR044019A1/es not_active Application Discontinuation
- 2004-04-14 PE PE2004000370A patent/PE20050021A1/es not_active Application Discontinuation
- 2004-04-15 WO PCT/EP2004/003980 patent/WO2004092127A1/en not_active Ceased
- 2004-04-15 SI SI200432220T patent/SI1620396T1/sl unknown
- 2004-04-15 DK DK04727557.3T patent/DK1620396T3/en active
- 2004-04-15 RU RU2005135331/04A patent/RU2369598C2/ru active
- 2004-04-15 BR BRPI0409471A patent/BRPI0409471B8/pt not_active IP Right Cessation
- 2004-04-15 TW TW093110566A patent/TWI359135B/zh not_active IP Right Cessation
- 2004-04-15 MY MYPI20041383A patent/MY139476A/en unknown
- 2004-04-15 EP EP04727557.3A patent/EP1620396B1/en not_active Expired - Lifetime
- 2004-04-15 SG SG200716949-3A patent/SG160212A1/en unknown
- 2004-04-15 CA CA2520128A patent/CA2520128C/en not_active Expired - Fee Related
- 2004-04-15 PL PL04727557T patent/PL1620396T3/pl unknown
- 2004-04-15 HR HRP20150163TT patent/HRP20150163T1/hr unknown
- 2004-04-15 KR KR1020057019568A patent/KR101192538B1/ko not_active Expired - Fee Related
- 2004-04-15 AU AU2004230245A patent/AU2004230245B2/en not_active Ceased
- 2004-04-15 CL CL200400804A patent/CL2004000804A1/es unknown
- 2004-04-15 US US10/552,835 patent/US7375238B2/en not_active Expired - Fee Related
- 2004-04-15 NZ NZ542899A patent/NZ542899A/en not_active IP Right Cessation
- 2004-04-15 ES ES04727557T patent/ES2531084T3/es not_active Expired - Lifetime
- 2004-04-15 PT PT04727557T patent/PT1620396E/pt unknown
- 2004-04-15 JP JP2006505132A patent/JP4672647B2/ja not_active Expired - Lifetime
- 2004-04-15 MX MXPA05011073A patent/MXPA05011073A/es active IP Right Grant
2005
- 2005-09-15 IL IL170887A patent/IL170887A/en active IP Right Grant
- 2005-10-12 EC EC2005006093A patent/ECSP056093A/es unknown
- 2005-10-19 MA MA28559A patent/MA27765A1/fr unknown
- 2005-11-03 CO CO05112189A patent/CO5700735A2/es not_active Application Discontinuation
- 2005-11-07 NO NO20055226A patent/NO333251B1/no not_active IP Right Cessation
- 2005-11-10 IS IS8122A patent/IS2979B/is unknown
2008
- 2008-05-22 AU AU2008202278A patent/AU2008202278A1/en not_active Abandoned
2015
- 2015-02-18 CY CY20151100168T patent/CY1116008T1/el unknown

Also Published As

Publication number	Publication date
PT1620396E (pt)	2015-03-05
SG160212A1 (en)	2010-04-29
KR101192538B1 (ko)	2012-10-17
NO20055226L (no)	2005-11-07
ES2531084T3 (es)	2015-03-10
NZ542899A (en)	2009-02-28
CA2520128C (en)	2012-02-07
MA27765A1 (fr)	2006-02-01
DK1620396T3 (en)	2015-02-23
RU2369598C2 (ru)	2009-10-10
BRPI0409471A (pt)	2006-05-02
MXPA05011073A (es)	2005-12-12
AR044019A1 (es)	2005-08-24
TW200510299A (en)	2005-03-16
PL1620396T3 (pl)	2015-05-29
WO2004092127A1 (en)	2004-10-28
CY1116008T1 (el)	2017-01-25
PE20050021A1 (es)	2005-03-15
IS2979B (is)	2017-09-15
HK1087695A1 (en)	2006-10-20
PE20081293A1 (es)	2008-11-04
IL170887A (en)	2013-06-27
AU2004230245B2 (en)	2008-02-21
RU2005135331A (ru)	2006-06-27
JP2006523645A (ja)	2006-10-19
IS8122A (is)	2005-11-10
BRPI0409471B8 (pt)	2021-05-25
BRPI0409471B1 (pt)	2015-11-03
EP1620396B1 (en)	2014-12-03
SI1620396T1 (sl)	2015-03-31
CO5700735A2 (es)	2006-11-30
ECSP056093A (es)	2006-03-01
KR20060003878A (ko)	2006-01-11
JP4672647B2 (ja)	2011-04-20
AU2008202278A1 (en)	2008-11-20
CA2520128A1 (en)	2004-10-28
AU2004230245A1 (en)	2004-10-28
TWI359135B (en)	2012-03-01
US7375238B2 (en)	2008-05-20
EP1620396A1 (en)	2006-02-01
US20060199854A1 (en)	2006-09-07
CL2004000804A1 (es)	2005-02-11
HRP20150163T1 (xx)	2015-03-27
MY139476A (en)	2009-10-30

Legal Events

Date	Code	Title	Description
2023-11-20	MM1K	Lapsed by not paying the annual fees

Publication	Publication Date	Title
NO20055226L (no)	2005-11-07	Fremgangsmate for fremstilling av N-substituerte 2-cyanopyrrolidoner
EA200970171A1 (ru)	2009-06-30	Производные n-(аминогетероарил)-1н-индол-2-карбоксамидов, их получение и их применение в терапии
TR200103497T2 (tr)	2002-05-21	Beta2-adrenoseptör agonistler.
IS6257A (is)	2002-01-31	Frumuviðloðunartálmar
NO20050650L (no)	2005-03-04	Fremgangsmate for selektiv fremstilling av aryl-5-tio- -D-aldoheksopyranosider
NO20053890L (no)	2005-10-20	Syntese av 4-amino-2-butenolklorider og anvendelse derav for fremstilling av 3-cyanokinoliner
NO20031561L (no)	2003-06-14	Kjemiske forbindelser
DK0944617T3 (da)	2003-09-01	Krystaller af benzimidazolderivater og deres fremstilling
NO20053246L (no)	2005-08-30	Kondensert 1,3-dihydroimidazol-ringforbindelse.
NO331165B1 (no)	2011-10-24	Derivater av dioksan-2-alkylkarbamater, fremgangsmate for fremstilling derav og anvendelse av de samme for fremstilling av medikamenter
BRPI0414738A (pt)	2006-11-21	derivados de ácido acético substituìdos
NO20022558L (no)	2002-05-29	4-karboksyamino-2-etyl-1,2,3,4-tetrahydrokinolinkrystall som CETP inhibitor
BR0014199A (pt)	2002-05-21	Derivados de bifenila como inibidores de nhe-3
NO20082077L (no)	2008-06-04	Spirosykliske quinazolinderivater som PDE7-inhibitorer
TR200201168T2 (tr)	2002-08-21	CGRP-Antagonistleri-yeni siklopropanlar içeren ilaçlar ve üretim yöntemleri.
GB1046506A (en)	1966-10-26	Guanidine compounds and process for their manufacture
NO20060703L (no)	2006-03-13	Fremgangsmate for fremstilling av cis-4-fluor-1-prolinderivater
NO985335L (no)	1999-01-15	2,4-Diaminopyrimidinderivater
NO20054787L (no)	2005-11-14	Indenderivater som farmasotiske midler
MY138051A (en)	2009-04-30	Compounds and processes
HUP0201475A2 (hu)	2003-10-28	Heteroarilamidin-, metilamidin- és guanidinszármazékok, előállításuk és alkalmazásuk, valamint e vegyületeket tartalmazó gyógyászati készítmények
EA200100825A1 (ru)	2002-02-28	Новые 1-арил-4-тиотриазины
BG48932A3 (bg)	1991-06-14	Метод за получаване на амидни съединения
NO20016267L (no)	2002-01-30	Nye kvatern¶re ammoniumforbindelser, en fremgangsmåte for fremstilling av dem og den farmasöytiske anvendelse derav
SE0003186D0 (sv)	2000-09-07	New process