NO324503B1 - Tripeptidylpeptidaseinhibitorforbindelser, farmasoytisk sammensetning inneholdende dem og fremgangsmate for deres fremstilling. - Google Patents

Tripeptidylpeptidaseinhibitorforbindelser, farmasoytisk sammensetning inneholdende dem og fremgangsmate for deres fremstilling. Download PDF

Info

Publication number: NO324503B1
Authority: NO; Norway
Prior art keywords: formula; mol; compound; alkyl; amino
Prior art date: 2000-10-30

Application number

NO20031930A

Other languages

English (en)

Norwegian (no)

Other versions

NO20031930L (no

NO20031930D0 (no

Inventor

Michael Joseph Kukla

Henry Joseph Breslin

Hans Louis Jos De Winter

Original Assignee

Janssen Pharmaceutica Nv

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.)

2000-10-30

Filing date

2003-04-29

Publication date

2007-11-05

2003-04-29 Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv

2003-04-29 Publication of NO20031930L publication Critical patent/NO20031930L/no

2003-04-29 Publication of NO20031930D0 publication Critical patent/NO20031930D0/no

2007-11-05 Publication of NO324503B1 publication Critical patent/NO324503B1/no

Links

238000000034 method Methods 0.000 title claims description 13
238000002360 preparation method Methods 0.000 title claims description 13
239000008194 pharmaceutical composition Substances 0.000 title claims description 8
230000008569 process Effects 0.000 title claims description 3
BBKRCKQWYZACFI-SQRKDXEHSA-N (2s)-2-amino-n-[(2s)-2-[[(2s)-4-chloro-3-oxo-1-phenylbutan-2-yl]amino]propanoyl]propanamide;2,2,2-trifluoroacetic acid Chemical class OC(=O)C(F)(F)F.C[C@H](N)C(=O)NC(=O)[C@H](C)N[C@H](C(=O)CCl)CC1=CC=CC=C1 BBKRCKQWYZACFI-SQRKDXEHSA-N 0.000 title 1
150000001875 compounds Chemical class 0.000 claims abstract description 113
238000006243 chemical reaction Methods 0.000 claims description 40
-1 phenylalaninyl Chemical group 0.000 claims description 25
150000003839 salts Chemical class 0.000 claims description 20
125000000217 alkyl group Chemical group 0.000 claims description 18
125000001475 halogen functional group Chemical group 0.000 claims description 14
150000003254 radicals Chemical class 0.000 claims description 14
239000002253 acid Substances 0.000 claims description 13
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 12
125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 11
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 8
125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 8
239000002585 base Substances 0.000 claims description 8
125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 8
239000001257 hydrogen Substances 0.000 claims description 8
229910052739 hydrogen Inorganic materials 0.000 claims description 8
125000004448 alkyl carbonyl group Chemical group 0.000 claims description 7
125000001424 substituent group Chemical group 0.000 claims description 7
125000000539 amino acid group Chemical group 0.000 claims description 6
125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 6
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
JIDDDPVQQUHACU-YFKPBYRVSA-N (2s)-pyrrolidine-2-carbaldehyde Chemical group O=C[C@@H]1CCCN1 JIDDDPVQQUHACU-YFKPBYRVSA-N 0.000 claims description 5
125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims description 5
239000003814 drug Substances 0.000 claims description 5
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ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims description 5
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125000004457 alkyl amino carbonyl group Chemical group 0.000 claims description 2
125000005196 alkyl carbonyloxy group Chemical group 0.000 claims description 2
125000003277 amino group Chemical group 0.000 claims description 2
125000005129 aryl carbonyl group Chemical group 0.000 claims description 2
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239000012458 free base Substances 0.000 claims description 2
125000000623 heterocyclic group Chemical group 0.000 claims description 2
238000004519 manufacturing process Methods 0.000 claims description 2
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239000007983 Tris buffer Substances 0.000 description 6
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LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 6
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NPZTUJOABDZTLV-UHFFFAOYSA-N hydroxybenzotriazole Substances O=C1C=CC=C2NNN=C12 NPZTUJOABDZTLV-UHFFFAOYSA-N 0.000 description 4
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ORCYVNAGTAUIEH-UHFFFAOYSA-N methyl n-(9h-fluoren-9-yl)-n-(2-fluoro-2-oxoethyl)carbamate Chemical compound C1=CC=C2C(N(CC(F)=O)C(=O)OC)C3=CC=CC=C3C2=C1 ORCYVNAGTAUIEH-UHFFFAOYSA-N 0.000 description 3
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Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- 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
- A61P3/04—Anorexiants; Antiobesity agents
- 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
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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Chemical Kinetics & Catalysis (AREA)
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Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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Pharmacology & Pharmacy (AREA)
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NO20031930A 2000-10-30 2003-04-29 Tripeptidylpeptidaseinhibitorforbindelser, farmasoytisk sammensetning inneholdende dem og fremgangsmate for deres fremstilling. NO324503B1 (no)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US24422300P	2000-10-30	2000-10-30
PCT/EP2001/012388 WO2002036116A2 (fr)	2000-10-30	2001-10-24	Inhibiteurs de tripeptidyl peptidase

Publications (3)

Publication Number	Publication Date
NO20031930L NO20031930L (no)	2003-04-29
NO20031930D0 NO20031930D0 (no)	2003-04-29
NO324503B1 true NO324503B1 (no)	2007-11-05

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ID=22921880

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
NO20031930A NO324503B1 (no)	2000-10-30	2003-04-29	Tripeptidylpeptidaseinhibitorforbindelser, farmasoytisk sammensetning inneholdende dem og fremgangsmate for deres fremstilling.

Country Status (25)

Country	Link
US (4)	US7125891B2 (fr)
EP (1)	EP1392291B1 (fr)
JP (1)	JP2004512365A (fr)
KR (1)	KR100820598B1 (fr)
CN (2)	CN100400040C (fr)
AT (1)	ATE363276T1 (fr)
AU (2)	AU2002224797B2 (fr)
BG (1)	BG107729A (fr)
CA (1)	CA2422617C (fr)
CZ (1)	CZ20031422A3 (fr)
DE (1)	DE60128731T2 (fr)
DK (1)	DK1392291T3 (fr)
EA (1)	EA006443B1 (fr)
EE (1)	EE200300168A (fr)
ES (1)	ES2287185T3 (fr)
HU (1)	HU230376B1 (fr)
IL (2)	IL155604A0 (fr)
MX (1)	MXPA03003868A (fr)
NO (1)	NO324503B1 (fr)
NZ (1)	NZ525928A (fr)
PL (1)	PL205536B1 (fr)
PT (1)	PT1392291E (fr)
SK (1)	SK6282003A3 (fr)
WO (1)	WO2002036116A2 (fr)
ZA (1)	ZA200303302B (fr)

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US8017168B2 (en)	2006-11-02	2011-09-13	The Coca-Cola Company	High-potency sweetener composition with rubisco protein, rubiscolin, rubiscolin derivatives, ace inhibitory peptides, and combinations thereof, and compositions sweetened therewith
GB0709031D0 (en) *	2007-05-10	2007-06-20	Sareum Ltd	Pharmaceutical compounds
GB201202027D0 (en)	2012-02-06	2012-03-21	Sareum Ltd	Pharmaceutical compounds
EP3040336B1 (fr)	2012-03-02	2020-04-08	Sareum Limited	Composés pour l'utilisation des conditions liées à la tyk2 kinase
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EP2961403A4 (fr) *	2013-03-01	2016-11-30	Zalicus Pharmaceuticals Ltd	Inhibiteurs hétérocycliques du canal sodique
US9675587B2 (en)	2013-03-14	2017-06-13	Allergan Holdings Unlimited Company	Opioid receptor modulator dosage formulations
GB201617871D0 (en)	2016-10-21	2016-12-07	Sareum Limited	Pharmaceutical compounds
US10716306B2 (en)	2016-11-01	2020-07-21	Nihon Nohyaku Co., Ltd.	N-alkylsulfonyl indoline compound, agricultural and horticultural insecticide comprising the compound, and method for using the insecticide
GB201816369D0 (en)	2018-10-08	2018-11-28	Sareum Ltd	Pharmaceutical compounds
EP4045491A1 (fr) *	2019-10-17	2022-08-24	Givaudan SA	Azacyles substitués en tant que modulateurs de trpm8
GB202005114D0 (en)	2020-04-07	2020-05-20	Sareum Ltd	Crystalline Forms of a Pharmaceutical Compound

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2001
- 2001-10-24 DE DE60128731T patent/DE60128731T2/de not_active Expired - Lifetime
- 2001-10-24 CZ CZ20031422A patent/CZ20031422A3/cs unknown
- 2001-10-24 HU HU0302770A patent/HU230376B1/hu unknown
- 2001-10-24 EE EEP200300168A patent/EE200300168A/xx unknown
- 2001-10-24 AU AU2002224797A patent/AU2002224797B2/en not_active Expired
- 2001-10-24 SK SK628-2003A patent/SK6282003A3/sk unknown
- 2001-10-24 ES ES01992570T patent/ES2287185T3/es not_active Expired - Lifetime
- 2001-10-24 AU AU2479702A patent/AU2479702A/xx active Pending
- 2001-10-24 KR KR1020037004180A patent/KR100820598B1/ko not_active Expired - Lifetime
- 2001-10-24 EP EP01992570A patent/EP1392291B1/fr not_active Expired - Lifetime
- 2001-10-24 MX MXPA03003868A patent/MXPA03003868A/es active IP Right Grant
- 2001-10-24 PL PL361064A patent/PL205536B1/pl unknown
- 2001-10-24 WO PCT/EP2001/012388 patent/WO2002036116A2/fr not_active Ceased
- 2001-10-24 IL IL15560401A patent/IL155604A0/xx unknown
- 2001-10-24 CA CA2422617A patent/CA2422617C/fr not_active Expired - Lifetime
- 2001-10-24 CN CNB018181015A patent/CN100400040C/zh not_active Expired - Lifetime
- 2001-10-24 AT AT01992570T patent/ATE363276T1/de active
- 2001-10-24 PT PT01992570T patent/PT1392291E/pt unknown
- 2001-10-24 EA EA200300523A patent/EA006443B1/ru not_active IP Right Cessation
- 2001-10-24 NZ NZ525928A patent/NZ525928A/en not_active IP Right Cessation
- 2001-10-24 CN CN2008101078402A patent/CN101307046B/zh not_active Expired - Lifetime
- 2001-10-24 JP JP2002538928A patent/JP2004512365A/ja active Pending
- 2001-10-24 US US10/415,623 patent/US7125891B2/en not_active Expired - Lifetime
- 2001-10-24 DK DK01992570T patent/DK1392291T3/da active
2003
- 2003-04-16 BG BG107729A patent/BG107729A/bg unknown
- 2003-04-28 IL IL155604A patent/IL155604A/en unknown
- 2003-04-29 NO NO20031930A patent/NO324503B1/no not_active IP Right Cessation
- 2003-04-29 ZA ZA200303302A patent/ZA200303302B/en unknown
2006
- 2006-08-07 US US11/499,937 patent/US20060276509A1/en not_active Abandoned
2007
- 2007-10-30 US US11/928,273 patent/US7947713B2/en not_active Expired - Fee Related
2011
- 2011-05-19 US US13/111,010 patent/US8247432B2/en not_active Expired - Fee Related

Also Published As

Publication number	Publication date
WO2002036116A3 (fr)	2002-09-26
BG107729A (bg)	2004-01-30
CN100400040C (zh)	2008-07-09
US20040034089A1 (en)	2004-02-19
CN101307046A (zh)	2008-11-19
WO2002036116A9 (fr)	2003-05-30
HUP0302770A2 (hu)	2003-12-29
EA200300523A1 (ru)	2003-08-28
KR20030046465A (ko)	2003-06-12
CZ20031422A3 (cs)	2004-01-14
NO20031930L (no)	2003-04-29
ES2287185T3 (es)	2007-12-16
PT1392291E (pt)	2007-08-24
ZA200303302B (en)	2004-07-29
AU2479702A (en)	2002-05-15
US20060276509A1 (en)	2006-12-07
WO2002036116A2 (fr)	2002-05-10
US20110224255A1 (en)	2011-09-15
DE60128731D1 (de)	2007-07-12
AU2002224797B2 (en)	2006-10-26
NZ525928A (en)	2005-06-24
IL155604A0 (en)	2003-11-23
CA2422617A1 (fr)	2002-05-10
DE60128731T2 (de)	2008-02-07
CA2422617C (fr)	2011-07-12
EE200300168A (et)	2003-06-16
PL361064A1 (en)	2004-09-20
JP2004512365A (ja)	2004-04-22
US8247432B2 (en)	2012-08-21
EP1392291A2 (fr)	2004-03-03
SK6282003A3 (en)	2004-02-03
HUP0302770A3 (en)	2009-03-30
US20080108653A1 (en)	2008-05-08
KR100820598B1 (ko)	2008-04-08
CN1471394A (zh)	2004-01-28
US7947713B2 (en)	2011-05-24
ATE363276T1 (de)	2007-06-15
DK1392291T3 (da)	2007-10-08
EP1392291B1 (fr)	2007-05-30
PL205536B1 (pl)	2010-04-30
CN101307046B (zh)	2012-08-15
US7125891B2 (en)	2006-10-24
MXPA03003868A (es)	2003-07-28
NO20031930D0 (no)	2003-04-29
HU230376B1 (hu)	2016-03-29
EA006443B1 (ru)	2005-12-29
IL155604A (en)	2009-07-20

Legal Events

Date	Code	Title	Description
2021-11-08	MK1K	Patent expired

Publication	Publication Date	Title
NO324503B1 (no)	2007-11-05	Tripeptidylpeptidaseinhibitorforbindelser, farmasoytisk sammensetning inneholdende dem og fremgangsmate for deres fremstilling.
AU2002224797A1 (en)	2002-07-18	Tripeptidyl peptidase inhibitors
DE60132017T2 (de)	2008-12-04	Neue benzazepine und ähnliche heterocyclische derivate,die als orexin rezeptor antagonisten geeignet sind
DE60102710T2 (de)	2005-04-14	Bizyklische pyrrolyl-amide als glukogen-phosphorylase-hemmer
CA2545644C (fr)	2011-11-01	Agonistes du recepteur de la melanocortine
HUE033243T2 (hu)	2017-11-28	Benzilamin-származékok
CN101663301A (zh)	2010-03-03	作为黑皮质素-4受体拮抗剂的取代的咪唑并吡啶衍生物
US7166603B2 (en)	2007-01-23	Dihydropyrimidone inhibitors of calcium channel function
CN101918361B (zh)	2014-05-28	哌啶磺酰胺衍生物
ES2257168B1 (es)	2007-06-01	Ligandos del receptor 5-ht7.
WO2018041563A1 (fr)	2018-03-08	N-[2-(4-phénoxypipéridin-1-yl)-2-(1,3-thiazol-5-yl)éthyl]benzamide substitué et dérivés de n-[2-(4-benzyloxypipéridin-1-yl)-2-(1,3-thiazol-5-yl)éthyl]benzamide en tant qu'antagonistes du récepteur p2x7
TW201038562A (en)	2010-11-01	Azetidines as histamine H3 receptor antagonists
JPH11512710A (ja)	1999-11-02	アルファ１ｂアドレナリンレセプターアンタゴニスト
ES2257167B1 (es)	2007-06-01	Inhibidores del receptor 5-ht7.
HK1062526A (en)	2004-11-12	Tripeptidyl peptidase inhibitors