HRP20040936B1 - Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors - Google Patents
Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitorsInfo
- Publication number
- HRP20040936B1 HRP20040936B1 HRP20040936AA HRP20040936A HRP20040936B1 HR P20040936 B1 HRP20040936 B1 HR P20040936B1 HR P20040936A A HRP20040936A A HR P20040936AA HR P20040936 A HRP20040936 A HR P20040936A HR P20040936 B1 HRP20040936 B1 HR P20040936B1
- Authority
- HR
- Croatia
- Prior art keywords
- 4alkyl
- protease inhibitors
- hiv protease
- amino
- substituted benzimidazole
- Prior art date
Links
- XRGHQBXKSHAQRB-UHFFFAOYSA-N 1h-benzimidazole-2-sulfonamide Chemical class C1=CC=C2NC(S(=O)(=O)N)=NC2=C1 XRGHQBXKSHAQRB-UHFFFAOYSA-N 0.000 title 1
- 239000004030 hiv protease inhibitor Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- -1 oxycarbonyloxy Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/08—Radicals containing only hydrogen and carbon atoms
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
- C07D235/30—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
- C07D235/30—Nitrogen atoms not forming part of a nitro radical
- C07D235/32—Benzimidazole-2-carbamic acids, unsubstituted or substituted; Esters thereof; Thio-analogues thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
- C07D413/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D417/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP02075999 | 2002-03-12 | ||
PCT/EP2003/050057 WO2003076413A1 (en) | 2002-03-12 | 2003-03-12 | Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
HRP20040936A2 HRP20040936A2 (en) | 2005-10-31 |
HRP20040936B1 true HRP20040936B1 (en) | 2012-09-30 |
Family
ID=27798870
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20040936AA HRP20040936B1 (en) | 2002-03-12 | 2004-10-07 | Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors |
Country Status (26)
Country | Link |
---|---|
US (2) | US20050171175A1 (es) |
EP (1) | EP1485358B1 (es) |
JP (1) | JP4557552B2 (es) |
KR (3) | KR20040093119A (es) |
CN (2) | CN101935303B (es) |
AP (1) | AP2111A (es) |
AR (1) | AR038928A1 (es) |
AT (1) | ATE497494T1 (es) |
AU (1) | AU2003219159B2 (es) |
BR (1) | BR0303373A (es) |
CA (1) | CA2479012C (es) |
DE (1) | DE60335939D1 (es) |
DK (1) | DK1485358T3 (es) |
EA (1) | EA011946B1 (es) |
HK (1) | HK1072053A1 (es) |
HR (1) | HRP20040936B1 (es) |
IL (1) | IL163960A0 (es) |
MX (1) | MXPA04008929A (es) |
MY (1) | MY142238A (es) |
NO (1) | NO326702B1 (es) |
NZ (1) | NZ535439A (es) |
PL (1) | PL213645B1 (es) |
SI (1) | SI1485358T1 (es) |
TW (1) | TWI329639B (es) |
WO (1) | WO2003076413A1 (es) |
ZA (1) | ZA200407242B (es) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EA011891B1 (ru) * | 2003-09-30 | 2009-06-30 | Тиботек Фармасьютикалз Лтд. | Способы получения соединений бензоксазолсульфонамида и их промежуточные соединения |
AU2005244121B2 (en) * | 2004-05-07 | 2012-01-19 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
KR101333627B1 (ko) | 2005-02-25 | 2013-11-27 | 얀센 알 앤드 디 아일랜드 | 프로테아제 저해제 전구체 합성 |
UA103013C2 (uk) | 2007-12-06 | 2013-09-10 | Тиботек Фармасьютикелз | Амідні сполуки як активатори противірусних препаратів |
WO2011061590A1 (en) | 2009-11-17 | 2011-05-26 | Hetero Research Foundation | Novel carboxamide derivatives as hiv inhibitors |
WO2013011485A1 (en) * | 2011-07-20 | 2013-01-24 | Ranbaxy Laboratories Limited | Process for the preparation of sulfonamides useful as retroviral protease inhibitors |
Citations (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1996022287A1 (en) * | 1995-01-20 | 1996-07-25 | G.D. Searle & Co. | Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors |
WO1996028465A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
WO1996028464A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
WO1996028463A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
WO1996028418A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
WO1999059989A1 (en) * | 1998-05-19 | 1999-11-25 | G.D. Searle & Co. | Process for the preparation of a benzo fused heterocyclo sulfonyl halide intermediate |
WO1999065870A2 (en) * | 1998-06-19 | 1999-12-23 | Vertex Pharmaceuticals Incorporated | Sulfonamide inhibitors of aspartyl protease |
WO1999067254A2 (en) * | 1998-06-23 | 1999-12-29 | The United States Of America Represented By The Secretary, Department Of Health And Human Services | Multi-drug resistant retroviral protease inhibitors and use thereof |
WO2000076961A1 (en) * | 1999-06-11 | 2000-12-21 | Vertex Pharmaceuticals Incorporated | Inhibitors of aspartyl protease |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
KR100336699B1 (ko) * | 1992-08-25 | 2002-05-13 | 윌리암스 로저 에이 | 레트로바이러스 프로테아제 저해제로서 유용한히드록시에틸아미노 술폰아미드 |
PH30929A (en) | 1992-09-03 | 1997-12-23 | Janssen Pharmaceutica Nv | Beads having a core coated with an antifungal and a polymer. |
US5723490A (en) * | 1992-09-08 | 1998-03-03 | Vertex Pharmaceuticals Incorporated | THF-containing sulfonamide inhibitors of aspartyl protease |
EP0715618B1 (en) | 1993-08-24 | 1998-12-16 | G.D. Searle & Co. | Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors |
DE69429357T2 (de) | 1993-10-01 | 2002-08-14 | Astrazeneca Ab, Soedertaelje | Verfahren i |
US5776971A (en) * | 1995-03-10 | 1998-07-07 | G.D. Searle & Co. | Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
AU7722296A (en) | 1995-11-15 | 1997-06-05 | G.D. Searle & Co. | Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
HU227745B1 (en) | 1996-05-20 | 2012-02-28 | Janssen Pharmaceutica Nv | Antifungal compositions containing itraconazole |
BR9806174A (pt) | 1997-03-26 | 1999-10-19 | Janssen Pharmaceutica Nv | Péletes tendo um núcleo revestido com um antifúngico e um polìmero |
EP1005569A2 (en) * | 1997-08-01 | 2000-06-07 | MorphoSys AG | Novel method and phage for the identification of nucleic acid sequences encoding members of a multimeric (poly)peptide complex |
TR200002402T2 (tr) | 1997-12-24 | 2001-01-22 | Vertex Pharmaceuticals Incorporated | Aspartil proteaz inhibitörü ön-ilaçlar. |
WO1999033795A1 (en) | 1997-12-24 | 1999-07-08 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
US6436989B1 (en) | 1997-12-24 | 2002-08-20 | Vertex Pharmaceuticals, Incorporated | Prodrugs of aspartyl protease inhibitors |
AU2010299A (en) | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs os aspartyl protease inhibitors |
-
2003
- 2003-03-10 MY MYPI20030825A patent/MY142238A/en unknown
- 2003-03-11 TW TW092105142A patent/TWI329639B/zh not_active IP Right Cessation
- 2003-03-11 AR ARP030100829A patent/AR038928A1/es not_active Application Discontinuation
- 2003-03-12 CN CN201010251011.9A patent/CN101935303B/zh not_active Expired - Fee Related
- 2003-03-12 NZ NZ535439A patent/NZ535439A/en not_active IP Right Cessation
- 2003-03-12 AP APAP/P/2004/003151A patent/AP2111A/en active
- 2003-03-12 AT AT03714954T patent/ATE497494T1/de not_active IP Right Cessation
- 2003-03-12 KR KR10-2004-7014171A patent/KR20040093119A/ko not_active Application Discontinuation
- 2003-03-12 JP JP2003574633A patent/JP4557552B2/ja not_active Expired - Fee Related
- 2003-03-12 PL PL374152A patent/PL213645B1/pl unknown
- 2003-03-12 KR KR1020107018927A patent/KR101302421B1/ko not_active IP Right Cessation
- 2003-03-12 EA EA200401188A patent/EA011946B1/ru not_active IP Right Cessation
- 2003-03-12 IL IL16396003A patent/IL163960A0/xx unknown
- 2003-03-12 DK DK03714954.9T patent/DK1485358T3/da active
- 2003-03-12 BR BR0303373-2A patent/BR0303373A/pt not_active IP Right Cessation
- 2003-03-12 US US10/508,561 patent/US20050171175A1/en not_active Abandoned
- 2003-03-12 CN CNA038104725A patent/CN1653053A/zh active Pending
- 2003-03-12 WO PCT/EP2003/050057 patent/WO2003076413A1/en active Application Filing
- 2003-03-12 DE DE60335939T patent/DE60335939D1/de not_active Expired - Lifetime
- 2003-03-12 EP EP03714954A patent/EP1485358B1/en not_active Expired - Lifetime
- 2003-03-12 AU AU2003219159A patent/AU2003219159B2/en not_active Ceased
- 2003-03-12 SI SI200331984T patent/SI1485358T1/sl unknown
- 2003-03-12 MX MXPA04008929A patent/MXPA04008929A/es active IP Right Grant
- 2003-03-12 CA CA2479012A patent/CA2479012C/en not_active Expired - Fee Related
- 2003-03-12 KR KR1020127028481A patent/KR20120136411A/ko not_active Application Discontinuation
- 2003-11-12 NO NO20035023A patent/NO326702B1/no not_active IP Right Cessation
-
2004
- 2004-09-09 ZA ZA2004/07242A patent/ZA200407242B/en unknown
- 2004-10-07 HR HRP20040936AA patent/HRP20040936B1/xx not_active IP Right Cessation
-
2005
- 2005-06-10 HK HK05104907.9A patent/HK1072053A1/xx not_active IP Right Cessation
-
2009
- 2009-04-27 US US12/430,547 patent/US8143421B2/en not_active Expired - Fee Related
Patent Citations (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1996022287A1 (en) * | 1995-01-20 | 1996-07-25 | G.D. Searle & Co. | Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors |
WO1996028465A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
WO1996028464A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
WO1996028463A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
WO1996028418A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
WO1999059989A1 (en) * | 1998-05-19 | 1999-11-25 | G.D. Searle & Co. | Process for the preparation of a benzo fused heterocyclo sulfonyl halide intermediate |
WO1999065870A2 (en) * | 1998-06-19 | 1999-12-23 | Vertex Pharmaceuticals Incorporated | Sulfonamide inhibitors of aspartyl protease |
WO1999067254A2 (en) * | 1998-06-23 | 1999-12-29 | The United States Of America Represented By The Secretary, Department Of Health And Human Services | Multi-drug resistant retroviral protease inhibitors and use thereof |
WO2000076961A1 (en) * | 1999-06-11 | 2000-12-21 | Vertex Pharmaceuticals Incorporated | Inhibitors of aspartyl protease |
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