NO318801B1 - Hiv-replikasjonsinhiberende pyrimidiner, dens anvendelse, farmasoytiske sammensetninger inneholder dem og fremgangsmate for deres fremstilling - Google Patents

Hiv-replikasjonsinhiberende pyrimidiner, dens anvendelse, farmasoytiske sammensetninger inneholder dem og fremgangsmate for deres fremstilling Download PDF

Info

Publication number: NO318801B1
Authority: NO; Norway
Prior art keywords: amino; formula; alkyl; compound; benzonitrile
Prior art date: 1998-11-10

Application number

NO20011696A

Other languages

English (en)

Norwegian (no)

Other versions

NO20011696D0 (no

NO20011696L (no

Inventor

Jan Heeres

Michael Joseph Kukla

Paul Adriaan Jan Janssen

Bart De Corte

Marc Rene De Jonge

Chih Yung Ho

Robert W Kavash

Lucien Maria Henricus Koymans

Donald William Ludovici

Koen Jeanne Alfons Van Aken

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.)

1998-11-10

Filing date

2001-04-04

Publication date

2005-05-09

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26805159&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NO318801(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2001-04-04 Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv

2001-04-04 Publication of NO20011696D0 publication Critical patent/NO20011696D0/no

2001-04-04 Publication of NO20011696L publication Critical patent/NO20011696L/no

2005-05-09 Publication of NO318801B1 publication Critical patent/NO318801B1/no

Links

238000000034 method Methods 0.000 title claims description 21
238000002360 preparation method Methods 0.000 title claims description 18
239000008194 pharmaceutical composition Substances 0.000 title claims description 9
230000002401 inhibitory effect Effects 0.000 title description 5
150000003230 pyrimidines Chemical class 0.000 title description 4
230000010076 replication Effects 0.000 title description 4
150000001875 compounds Chemical class 0.000 claims description 133
239000002904 solvent Substances 0.000 claims description 56
-1 cyano, aminocarbonyl Chemical group 0.000 claims description 45
125000000217 alkyl group Chemical group 0.000 claims description 39
238000006243 chemical reaction Methods 0.000 claims description 39
150000003839 salts Chemical class 0.000 claims description 36
239000001257 hydrogen Substances 0.000 claims description 26
229910052739 hydrogen Inorganic materials 0.000 claims description 26
241000725303 Human immunodeficiency virus Species 0.000 claims description 23
239000002253 acid Substances 0.000 claims description 18
125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims description 17
125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 17
125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 16
150000001412 amines Chemical group 0.000 claims description 15
150000002431 hydrogen Chemical class 0.000 claims description 15
238000011282 treatment Methods 0.000 claims description 15
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229910052736 halogen Chemical group 0.000 claims description 13
150000002367 halogens Chemical group 0.000 claims description 13
239000002585 base Substances 0.000 claims description 12
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
230000000798 anti-retroviral effect Effects 0.000 claims description 9
239000012298 atmosphere Substances 0.000 claims description 9
125000001424 substituent group Chemical group 0.000 claims description 9
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125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 7
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125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 5
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238000004519 manufacturing process Methods 0.000 claims description 5
150000001204 N-oxides Chemical class 0.000 claims description 4
239000004480 active ingredient Substances 0.000 claims description 4
125000004448 alkyl carbonyl group Chemical group 0.000 claims description 4
125000005196 alkyl carbonyloxy group Chemical group 0.000 claims description 4
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VKQKEROEGYSHIY-UHFFFAOYSA-N 4-[[5-bromo-2-(4-cyanoanilino)pyrimidin-4-yl]amino]-3,5-dimethylbenzonitrile Chemical compound CC1=CC(C#N)=CC(C)=C1NC1=NC(NC=2C=CC(=CC=2)C#N)=NC=C1Br VKQKEROEGYSHIY-UHFFFAOYSA-N 0.000 claims description 3
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Classifications

- 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
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
- C07D239/80—Oxygen atoms

NO20011696A 1998-11-10 2001-04-04 Hiv-replikasjonsinhiberende pyrimidiner, dens anvendelse, farmasoytiske sammensetninger inneholder dem og fremgangsmate for deres fremstilling NO318801B1 (no)

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US10779298P	1998-11-10	1998-11-10
US14396299P	1999-07-15	1999-07-15
PCT/EP1999/007417 WO2000027825A1 (en)	1998-11-10	1999-09-24	Hiv replication inhibiting pyrimidines

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NO20011696D0 NO20011696D0 (no)	2001-04-04
NO20011696L NO20011696L (no)	2001-04-04
NO318801B1 true NO318801B1 (no)	2005-05-09

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NO20011696A NO318801B1 (no)	1998-11-10	2001-04-04	Hiv-replikasjonsinhiberende pyrimidiner, dens anvendelse, farmasoytiske sammensetninger inneholder dem og fremgangsmate for deres fremstilling
NO2009003C NO2009003I2 (no)	1998-11-10	2009-02-23	Etravirin
NO2021015C NO2021015I1 (no)	1998-11-10	2021-03-29	Etravirin - forlenget SPC

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NO2009003C NO2009003I2 (no)	1998-11-10	2009-02-23	Etravirin
NO2021015C NO2021015I1 (no)	1998-11-10	2021-03-29	Etravirin - forlenget SPC

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Publication number	Publication date
HK1048817A1 (en)	2003-04-17
HK1025330A1 (en)	2000-11-10
IL169949A (en)	2011-02-28
FR09C0004I2 (fr)	2010-06-11
AU762523B2 (en)	2003-06-26
ES2338760T3 (es)	2010-05-12
JP2002529456A (ja)	2002-09-10
AU762523C (en)	2004-02-12
DE69905683T2 (de)	2004-03-18
UA70966C2 (uk)	2004-11-15
OA11674A (en)	2005-01-12
CZ20011533A3 (cs)	2001-10-17
IL143023A0 (en)	2002-04-21
ZA200103769B (en)	2002-08-12
ATE455107T1 (de)	2010-01-15
EA004049B1 (ru)	2003-12-25
HU227453B1 (en)	2011-06-28
HRP20080359B1 (hr)	2016-01-01
JP3635238B2 (ja)	2005-04-06
NO2009003I1 (no)	2009-03-09
SK6032001A3 (en)	2002-01-07
EP1270560A1 (en)	2003-01-02
EE05086B1 (et)	2008-10-15
BR9915552A (pt)	2001-08-14
AR024227A1 (es)	2002-09-25
NL300373I1 (nl)	2009-03-02
KR20010075235A (ko)	2001-08-09
CZ301367B6 (cs)	2010-02-03
PT1002795E (pt)	2003-07-31
US8530655B2 (en)	2013-09-10
US8003789B2 (en)	2011-08-23
LTC1002795I2 (lt)	2021-06-10
EP1002795A1 (en)	2000-05-24
US20050288278A1 (en)	2005-12-29
TWI238161B (en)	2005-08-21
LTPA2008016I1 (lt)	2021-04-26
CY2008021I1 (el)	2010-07-28
CN1214013C (zh)	2005-08-10
KR100658489B1 (ko)	2006-12-18
HU230394B1 (hu)	2016-04-28
US20080176880A1 (en)	2008-07-24
NO20011696D0 (no)	2001-04-04
US20110263625A1 (en)	2011-10-27
EP1002795B1 (en)	2003-03-05
WO2000027825A1 (en)	2000-05-18
HRP20010161B9 (hr)	2014-10-24
CA2350801A1 (en)	2000-05-18
NL300373I2 (nl)	2009-04-01
HRP20010161A2 (en)	2002-02-28
EA200100536A1 (ru)	2002-02-28
BR9915552B1 (pt)	2013-11-19
SK287270B6 (sk)	2010-05-07
US20030114472A1 (en)	2003-06-19
HRP20010161B1 (en)	2009-03-31
US7037917B2 (en)	2006-05-02
BG105418A (en)	2001-11-30
ES2193664T3 (es)	2003-11-01
EE200100252A (et)	2002-10-15
BG65103B1 (bg)	2007-02-28
US6878717B2 (en)	2005-04-12
DE69905683D1 (de)	2003-04-10
DK1002795T3 (da)	2003-06-30
ID28376A (id)	2001-05-17
BRPI9915552B8 (pt)	2021-05-25
AU2011200708A1 (en)	2011-03-10
CA2350801C (en)	2008-05-20
NO2021015I1 (no)	2021-03-29
LU91528I2 (fr)	2009-04-20
PL347586A1 (en)	2002-04-08
PL204427B1 (pl)	2010-01-29
CN1322198A (zh)	2001-11-14
NO2009003I2 (no)	2010-06-07
HUP0104177A3 (en)	2003-01-28
HUP0104177A2 (hu)	2002-03-28
CY2008021I2 (el)	2010-07-28
HK1048817B (zh)	2010-04-09
AP1683A (en)	2006-11-29
DE122009000003I1 (de)	2009-05-20
SI1002795T1 (en)	2003-10-31
EP1270560B1 (en)	2010-01-13
LU91528I9 (pt)	2019-01-02
TR200101306T2 (tr)	2001-10-22
DE69941934D1 (de)	2010-03-04
AU6200899A (en)	2000-05-29
ATE233740T1 (de)	2003-03-15
FR09C0004I1 (pt)	2009-02-27
SK287269B6 (sk)	2010-05-07
NZ511116A (en)	2003-08-29
MY121108A (en)	2005-12-30
NO20011696L (no)	2001-04-04
US20040039005A1 (en)	2004-02-26
HRP20080359A2 (en)	2008-12-31

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Publication	Publication Date	Title
NO318801B1 (no)	2005-05-09	Hiv-replikasjonsinhiberende pyrimidiner, dens anvendelse, farmasoytiske sammensetninger inneholder dem og fremgangsmate for deres fremstilling
DK1282607T3 (en)	2016-02-01	Prodrugs of HIV replication inhibiting pyrimidines
NO327639B1 (no)	2009-09-07	HIV-hemmende pyrimidinderivater
AU764472B2 (en)	2003-08-21	2,4-disubstituted triazine derivatives
MXPA01003646A (en)	2001-12-04	Hiv replication inhibiting pyrimidines
MXPA01003644A (en)	2002-06-05	2,4-disubstituted triazine derivatives