UA79285C2 - Non-nucleoside reverse transcriptase inhibitors and use thereof - Google Patents

Non-nucleoside reverse transcriptase inhibitors and use thereof Download PDF

Info

Publication number: UA79285C2
Authority: UA; Ukraine
Prior art keywords: cooh; optionally substituted; svalkyl; substituted; methyl
Prior art date: 2002-05-16

Application number

UA20041210291A

Other languages

English (en)

Ukrainian (uk)

Inventor

Bruno Simoneau

Serge Landry

Eric Malenfant

Julie Naud

Meara Jeffrey O'

Bounkham Thavonekham

Christiane Yoakim

Original Assignee

Boehringer Ingelheim Int

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.)

2002-05-16

Filing date

2003-05-14

Publication date

2007-06-11

2003-05-14 Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int

2007-06-11 Publication of UA79285C2 publication Critical patent/UA79285C2/uk

Links

229940042402 non-nucleoside reverse transcriptase inhibitor Drugs 0.000 title description 2
239000002726 nonnucleoside reverse transcriptase inhibitor Substances 0.000 title description 2
150000001875 compounds Chemical class 0.000 claims abstract description 157
125000001424 substituent group Chemical group 0.000 claims abstract description 39
125000000623 heterocyclic group Chemical group 0.000 claims abstract description 31
229910052739 hydrogen Inorganic materials 0.000 claims abstract description 26
229910052717 sulfur Inorganic materials 0.000 claims abstract description 15
150000003839 salts Chemical class 0.000 claims abstract description 13
125000005842 heteroatom Chemical group 0.000 claims abstract description 8
229910052757 nitrogen Inorganic materials 0.000 claims abstract description 8
125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract description 4
125000000896 monocarboxylic acid group Chemical group 0.000 claims description 61
229910052736 halogen Inorganic materials 0.000 claims description 34
150000002367 halogens Chemical class 0.000 claims description 34
-1 substituted Chemical class 0.000 claims description 28
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 26
RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 25
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 23
JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 22
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230000003000 nontoxic effect Effects 0.000 description 1
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239000001301 oxygen Chemical group 0.000 description 1
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238000007911 parenteral administration Methods 0.000 description 1
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239000000546 pharmaceutical excipient Substances 0.000 description 1
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239000002574 poison Substances 0.000 description 1
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229920002401 polyacrylamide Polymers 0.000 description 1
229920001515 polyalkylene glycol Polymers 0.000 description 1
229920000573 polyethylene Polymers 0.000 description 1
229920000136 polysorbate Polymers 0.000 description 1
229940068965 polysorbates Drugs 0.000 description 1
229920002451 polyvinyl alcohol Polymers 0.000 description 1
229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
239000001267 polyvinylpyrrolidone Substances 0.000 description 1
235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
239000012256 powdered iron Substances 0.000 description 1
239000002244 precipitate Substances 0.000 description 1
239000002243 precursor Substances 0.000 description 1
238000012545 processing Methods 0.000 description 1
239000000047 product Substances 0.000 description 1
VVWRJUBEIPHGQF-UHFFFAOYSA-N propan-2-yl n-propan-2-yloxycarbonyliminocarbamate Chemical compound CC(C)OC(=O)N=NC(=O)OC(C)C VVWRJUBEIPHGQF-UHFFFAOYSA-N 0.000 description 1
125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
229960003415 propylparaben Drugs 0.000 description 1
238000000746 purification Methods 0.000 description 1
125000003226 pyrazolyl group Chemical group 0.000 description 1
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239000011347 resin Substances 0.000 description 1
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239000000523 sample Substances 0.000 description 1
238000007127 saponification reaction Methods 0.000 description 1
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125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
239000000377 silicon dioxide Substances 0.000 description 1
235000012239 silicon dioxide Nutrition 0.000 description 1
229910052708 sodium Inorganic materials 0.000 description 1
229940001607 sodium bisulfite Drugs 0.000 description 1
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HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 1
235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
229940001584 sodium metabisulfite Drugs 0.000 description 1
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239000007909 solid dosage form Substances 0.000 description 1
239000003381 stabilizer Substances 0.000 description 1
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238000004659 sterilization and disinfection Methods 0.000 description 1
239000011593 sulfur Chemical group 0.000 description 1
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229940095064 tartrate Drugs 0.000 description 1
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VCMJCVGFSROFHV-WZGZYPNHSA-N tenofovir disoproxil fumarate Chemical compound OC(=O)\C=C\C(O)=O.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N VCMJCVGFSROFHV-WZGZYPNHSA-N 0.000 description 1
238000002560 therapeutic procedure Methods 0.000 description 1
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RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 description 1
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JBWKIWSBJXDJDT-UHFFFAOYSA-N triphenylmethyl chloride Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(Cl)C1=CC=CC=C1 JBWKIWSBJXDJDT-UHFFFAOYSA-N 0.000 description 1
125000001493 tyrosinyl group Chemical group [H]OC1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 description 1
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Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
- 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
- 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)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Veterinary Medicine (AREA)
Animal Behavior & Ethology (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Virology (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Pharmacology & Pharmacy (AREA)
Tropical Medicine & Parasitology (AREA)
Molecular Biology (AREA)
Oncology (AREA)
Communicable Diseases (AREA)
AIDS & HIV (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Saccharide Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

UA20041210291A 2002-05-16 2003-05-14 Non-nucleoside reverse transcriptase inhibitors and use thereof UA79285C2 (en)

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US38088602P	2002-05-16	2002-05-16
PCT/CA2003/000718 WO2003097644A2 (en)	2002-05-16	2003-05-14	Non-nucleoside reverse transcriptase inhibitors

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US (1)	US6806265B2 (de)
EP (1)	EP1506195B1 (de)
JP (1)	JP4230448B2 (de)
KR (1)	KR20050008716A (de)
CN (1)	CN1318421C (de)
AR (1)	AR040027A1 (de)
AT (1)	ATE412653T1 (de)
AU (1)	AU2003229186A1 (de)
BR (1)	BR0310033A (de)
CA (1)	CA2485916C (de)
DE (1)	DE60324418D1 (de)
EA (1)	EA009178B1 (de)
EC (1)	ECSP045432A (de)
ES (1)	ES2315492T3 (de)
HR (1)	HRP20041065A2 (de)
IL (1)	IL163753A0 (de)
MX (1)	MXPA04010409A (de)
MY (1)	MY134646A (de)
NO (1)	NO20044104L (de)
NZ (1)	NZ536736A (de)
PE (1)	PE20040365A1 (de)
PL (1)	PL371663A1 (de)
RS (1)	RS98004A (de)
TW (1)	TW200404071A (de)
UA (1)	UA79285C2 (de)
UY (1)	UY27809A1 (de)
WO (1)	WO2003097644A2 (de)
ZA (1)	ZA200406912B (de)

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GB0302094D0 (en)	2003-01-29	2003-02-26	Pharmagene Lab Ltd	EP4 receptor antagonists
WO2004087169A1 (en) *	2003-03-27	2004-10-14	Boehringer Ingelheim International Gmbh	Antiviral combination of nevirapine and a further antiretroviral compound
US7348338B2 (en)	2003-07-17	2008-03-25	Plexxikon, Inc.	PPAR active compounds
CA2532403A1 (en) *	2003-07-17	2005-02-03	James Arnold	Ppar active compounds
GB0324269D0 (en)	2003-10-16	2003-11-19	Pharmagene Lab Ltd	EP4 receptor antagonists
DE102004051277A1 (de) *	2004-10-21	2006-04-27	Merck Patent Gmbh	Heterocyclische Carbonylverbindungen
JP2008521829A (ja) *	2004-11-30	2008-06-26	プレキシコン，インコーポレーテッド	Ｐｐａｒ活性化合物
JP2009509932A (ja) *	2005-09-07	2009-03-12	プレキシコン，インコーポレーテッド	Ｐｐａｒ活性化合物
WO2007030559A2 (en) *	2005-09-07	2007-03-15	Plexxikon, Inc.	1, 3-disubstituted indole derivatives for use as ppar modulators
BRPI0615948A2 (pt) *	2005-09-07	2011-05-31	Plexxikon Inc	composto ativo de ppar, sua composição, seu kit e seu uso
US8492428B2 (en)	2005-09-20	2013-07-23	Mayo Foundation For Medical Education And Research	Small-molecule botulinum toxin inhibitors
PE20090159A1 (es) *	2007-03-08	2009-02-21	Plexxikon Inc	COMPUESTOS DERIVADOS DE ACIDO INDOL-PROPIONICO COMO MODULADORES PPARs
CN107428747A (zh)	2014-11-25	2017-12-01	拜耳制药股份公司	取代的吡啶并苯并二氮杂*酮衍生物及其用途
ES2946917T3 (es)	2017-07-21	2023-07-27	Antabio Sas	Compuestos químicos
BR112020018094A2 (pt)	2018-03-08	2020-12-22	Incyte Corporation	Compostos de aminopirazina diol como inibidores de pi3k-¿
US11046658B2 (en)	2018-07-02	2021-06-29	Incyte Corporation	Aminopyrazine derivatives as PI3K-γ inhibitors
CN118103038A (zh) *	2021-08-20	2024-05-28	英安塔制药有限公司	17β-羟基类固醇脱氢酶13型抑制剂及其使用方法

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US5366972A (en)	1989-04-20	1994-11-22	Boehringer Ingelheim Pharmaceuticals, Inc.	5,11-dihydro-6H-dipyrido(3,2-B:2',3'-E)(1,4)diazepines and their use in the prevention or treatment of HIV infection
US5705499A (en) *	1995-10-06	1998-01-06	Boehringer Ingelheim Pharmaceuticals, Inc.	8-arylalkyl- and 8-arylheteroalkyl-5,11-dihydro-6H-dipyrido 3,2-B:2',3'-e! 1!diazepines and their use in the treatment of HIV-1 infection
TWI270547B (en)	2000-06-16	2007-01-11	Boehringer Ingelheim Ca Ltd	Non-nucleoside reverse transcriptase inhibitors
US6716836B2 (en)	2001-03-22	2004-04-06	Boehringer Ingelheim (Canada) Ltd.	Non-nucleoside reverse transcriptase inhibitors
US6673791B2 (en)	2001-07-30	2004-01-06	Boehringer Ingelheim (Canada) Ltd.	Non-nucleoside reverse transcriptase inhibitors

2003
- 2003-05-06 US US10/430,116 patent/US6806265B2/en not_active Expired - Lifetime
- 2003-05-13 MY MYPI20031796A patent/MY134646A/en unknown
- 2003-05-14 AU AU2003229186A patent/AU2003229186A1/en not_active Abandoned
- 2003-05-14 EA EA200401482A patent/EA009178B1/ru not_active IP Right Cessation
- 2003-05-14 PL PL03371663A patent/PL371663A1/xx not_active Application Discontinuation
- 2003-05-14 JP JP2004505376A patent/JP4230448B2/ja not_active Expired - Fee Related
- 2003-05-14 MX MXPA04010409A patent/MXPA04010409A/es active IP Right Grant
- 2003-05-14 NZ NZ536736A patent/NZ536736A/en unknown
- 2003-05-14 WO PCT/CA2003/000718 patent/WO2003097644A2/en not_active Ceased
- 2003-05-14 BR BR0310033-2A patent/BR0310033A/pt not_active IP Right Cessation
- 2003-05-14 AT AT03724719T patent/ATE412653T1/de active
- 2003-05-14 DE DE60324418T patent/DE60324418D1/de not_active Expired - Lifetime
- 2003-05-14 CA CA002485916A patent/CA2485916C/en not_active Expired - Fee Related
- 2003-05-14 HR HR20041065A patent/HRP20041065A2/hr not_active Application Discontinuation
- 2003-05-14 EP EP03724719A patent/EP1506195B1/de not_active Expired - Lifetime
- 2003-05-14 PE PE2003000461A patent/PE20040365A1/es not_active Application Discontinuation
- 2003-05-14 UA UA20041210291A patent/UA79285C2/uk unknown
- 2003-05-14 CN CNB038111187A patent/CN1318421C/zh not_active Expired - Fee Related
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- 2003-05-14 ES ES03724719T patent/ES2315492T3/es not_active Expired - Lifetime
- 2003-05-14 KR KR10-2004-7018428A patent/KR20050008716A/ko not_active Withdrawn
- 2003-05-14 RS YU98004A patent/RS98004A/sr unknown
- 2003-05-15 UY UY27809A patent/UY27809A1/es not_active Application Discontinuation
- 2003-05-15 TW TW092113234A patent/TW200404071A/zh unknown
- 2003-05-16 AR ARP030101708A patent/AR040027A1/es unknown
2004
- 2004-08-31 ZA ZA200406912A patent/ZA200406912B/xx unknown
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Also Published As

Publication number	Publication date
CA2485916C (en)	2009-12-08
CN1653066A (zh)	2005-08-10
IL163753A0 (en)	2005-12-18
MXPA04010409A (es)	2005-02-17
DE60324418D1 (de)	2008-12-11
UY27809A1 (es)	2003-12-31
NZ536736A (en)	2006-11-30
TW200404071A (en)	2004-03-16
HRP20041065A2 (en)	2005-04-30
ATE412653T1 (de)	2008-11-15
MY134646A (en)	2007-12-31
JP4230448B2 (ja)	2009-02-25
ES2315492T3 (es)	2009-04-01
EA200401482A1 (ru)	2005-06-30
HK1080849A1 (en)	2006-05-04
EP1506195B1 (de)	2008-10-29
EP1506195A2 (de)	2005-02-16
BR0310033A (pt)	2005-02-15
US6806265B2 (en)	2004-10-19
CA2485916A1 (en)	2003-11-27
WO2003097644A2 (en)	2003-11-27
PL371663A1 (en)	2005-06-27
AU2003229186A1 (en)	2003-12-02
KR20050008716A (ko)	2005-01-21
PE20040365A1 (es)	2004-07-22
ECSP045432A (es)	2005-01-03
RS98004A (sr)	2006-12-15
AR040027A1 (es)	2005-03-09
CN1318421C (zh)	2007-05-30
WO2003097644A3 (en)	2004-02-05
EA009178B1 (ru)	2007-12-28
US20040006071A1 (en)	2004-01-08
NO20044104L (no)	2004-12-01
JP2005526851A (ja)	2005-09-08
ZA200406912B (en)	2006-06-28

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