SG43862A1 - Novel sulfonamide inhibitors of aspartyl protease - Google Patents

Novel sulfonamide inhibitors of aspartyl protease

Info

Publication number
SG43862A1
SG43862A1 SG1996003219A SG1996003219A SG43862A1 SG 43862 A1 SG43862 A1 SG 43862A1 SG 1996003219 A SG1996003219 A SG 1996003219A SG 1996003219 A SG1996003219 A SG 1996003219A SG 43862 A1 SG43862 A1 SG 43862A1
Authority
SG
Singapore
Prior art keywords
aspartyl protease
novel sulfonamide
sulfonamide inhibitors
inhibitors
novel
Prior art date
Application number
SG1996003219A
Other languages
English (en)
Inventor
Roger D Tung
Mark A Murcko
Govinda Rao Bhisetti
Original Assignee
Vertex Pharma
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.)
Filing date
Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of SG43862A1 publication Critical patent/SG43862A1/en

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    • 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
    • C07D207/18—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—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 one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C307/00—Amides of sulfuric acids, i.e. compounds having singly-bound oxygen atoms of sulfate groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
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    • C07C307/06—Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
    • C07C311/13—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/18—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
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    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C07C311/38—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
    • C07C311/39—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
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    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
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    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
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    • C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
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    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
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    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
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SG1996003219A 1992-09-08 1993-09-07 Novel sulfonamide inhibitors of aspartyl protease SG43862A1 (en)

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DE10199024I2 (de) 2006-04-06
NZ314376A (en) 1998-10-28
NO303444B1 (no) 1998-07-13
AU691160B2 (en) 1998-05-14
GEP20012579B (en) 2001-11-26
US5585397A (en) 1996-12-17
US20100210603A1 (en) 2010-08-19
PL185635B1 (pl) 2003-06-30
CN1061339C (zh) 2001-01-31
US20080293727A1 (en) 2008-11-27
CZ58795A3 (en) 1995-12-13
HU9500685D0 (en) 1995-04-28
FI120685B (fi) 2010-01-29
RO118747B1 (ro) 2003-10-30
SK281360B6 (sk) 2001-02-12
IL106927A0 (en) 1993-12-28
CO4870779A1 (es) 1999-12-27
NZ256238A (en) 1997-04-24
DK0659181T3 (da) 1999-10-18
WO1994005639A1 (fr) 1994-03-17
HK1012631A1 (en) 1999-08-06
MY142901A (en) 2011-01-31
CY2164B1 (en) 2002-08-23
MXPA03010538A (es) 2011-12-16
GR3030719T3 (en) 1999-11-30
FI951059A0 (fi) 1995-03-07
IL106927A (en) 2001-01-11
AP390A (en) 1995-08-02
JP3012002B2 (ja) 2000-02-21
NL300039I2 (nl) 2001-09-03
NO950876D0 (no) 1995-03-07
UA44694C2 (uk) 2002-03-15
AU4852093A (en) 1994-03-29
NO950876L (no) 1995-05-08
HU228198B1 (en) 2013-01-28
AP9300572A0 (en) 1993-10-31
SK29395A3 (en) 1995-09-13
US7608632B2 (en) 2009-10-27
CA2143208C (fr) 2003-01-07
EP0659181A1 (fr) 1995-06-28
RU95109928A (ru) 1997-03-20
LT3302B (en) 1995-06-26
EP0885887A2 (fr) 1998-12-23
EP0885887B1 (fr) 2003-05-28
BG62488B1 (bg) 1999-12-30
BG99540A (bg) 1995-11-30
HUT71892A (en) 1996-02-28
ATE241602T1 (de) 2003-06-15
IS4068A (is) 1994-03-09
IS2334B (is) 2008-02-15
BR1100824A (pt) 1999-08-31
PT885887E (pt) 2003-10-31
TW254927B (fr) 1995-08-21
RU2135496C1 (ru) 1999-08-27
US20060189810A1 (en) 2006-08-24
CZ289475B6 (cs) 2002-01-16
US5856353A (en) 1999-01-05
NO2001012I1 (no) 2001-07-23
DE69324369T2 (de) 1999-08-26
EP0885887A3 (fr) 1999-02-03
DE69324369D1 (de) 1999-05-12
LU90736I2 (fr) 2001-05-07
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HK1023561A1 (en) 2000-09-15
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JPH08501299A (ja) 1996-02-13
US20030069222A1 (en) 2003-04-10
ES2131589T3 (es) 1999-08-01
KR100262056B1 (ko) 2000-07-15
PL307858A1 (en) 1995-06-26
ATE178598T1 (de) 1999-04-15
US6372778B1 (en) 2002-04-16
PH31251A (en) 1998-05-05
DE10199024I1 (de) 2001-07-12
DE69333012D1 (de) 2003-07-03
DK0885887T3 (da) 2003-09-22
DE69333012T2 (de) 2004-04-01
CN1087347A (zh) 1994-06-01
LTIP917A (en) 1994-11-25
EP0659181B1 (fr) 1999-04-07
FI951059L (fi) 1995-04-18

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