AU2006262275A1 - HIV-1 protease inhibitors, and methods of making and using them - Google Patents

HIV-1 protease inhibitors, and methods of making and using them Download PDF

Info

Publication number: AU2006262275A1
Authority: AU; Australia
Prior art keywords: alkyl; compound; heterocyclyl; aryl; aralkyl
Prior art date: 2005-06-22
Legal status (The legal status 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 status listed.): Abandoned

Application number

AU2006262275A

Other languages

English (en)

Inventor

Akbar Ali

Michael D. Altman

Saima Ghafoor Anjum

Hong Cao

Sripriya Chellappan

Miguel X. Fernandes

Kiran Kumar Reddy Garudammagari Sai

Michael Gilson

Visvaldas Kairys

Nancy King

Madhavi Nagga Laxmi Nalam

Ellen Nalivaika

Moses Prabu

Tariq M. Rana

Celia A. Schiffer

Bruce Tidor

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Massachusetts Institute of Technology

University of Maryland College Park

University of Massachusetts Amherst

Original Assignee

Massachusetts Institute of Technology

University of Maryland College Park

University of Massachusetts Amherst

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.)

2005-06-22

Filing date

2006-06-21

Publication date

2007-01-04

2006-06-21 Application filed by Massachusetts Institute of Technology, University of Maryland College Park, University of Massachusetts Amherst filed Critical Massachusetts Institute of Technology

2007-01-04 Publication of AU2006262275A1 publication Critical patent/AU2006262275A1/en

2009-04-02 Assigned to UNIVERSITY OF MASSACHUSETTS, THE MASSACHUSETTS INSTITUTE OF TECHNOLOGY, THE UNIVERSITY OF MARYLAND BIOTECHNOLOGY INSTITUTE reassignment UNIVERSITY OF MASSACHUSETTS Alteration of Name(s) of Applicant(s) under S113 Assignors: UNIVERSITY OF MASSACHUSETTS

2011-04-21 Assigned to UNIVERSITY OF MASSACHUSETTS, UNIVERSITY OF MARYLAND, COLLEGE PARK, THE MASSACHUSETTS INSTITUTE OF TECHNOLOGY reassignment UNIVERSITY OF MASSACHUSETTS Request for Assignment Assignors: THE MASSACHUSETTS INSTITUTE OF TECHNOLOGY, THE UNIVERSITY OF MARYLAND BIOTECHNOLOGY INSTITUTE, UNIVERSITY OF MASSACHUSETTS

Status Abandoned legal-status Critical Current

Links

238000000034 method Methods 0.000 title claims description 67
239000000137 peptide hydrolase inhibitor Substances 0.000 title claims description 52
229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title description 43
108010016183 Human immunodeficiency virus 1 p16 protease Proteins 0.000 title description 35
125000000217 alkyl group Chemical group 0.000 claims description 740
150000001875 compounds Chemical class 0.000 claims description 550
125000000623 heterocyclic group Chemical group 0.000 claims description 383
125000003118 aryl group Chemical group 0.000 claims description 371
125000003710 aryl alkyl group Chemical group 0.000 claims description 315
125000001072 heteroaryl group Chemical group 0.000 claims description 290
125000000753 cycloalkyl group Chemical group 0.000 claims description 244
229910052739 hydrogen Inorganic materials 0.000 claims description 219
239000001257 hydrogen Substances 0.000 claims description 215
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150000002431 hydrogen Chemical group 0.000 claims description 157
125000003342 alkenyl group Chemical group 0.000 claims description 126
-1 cycloalklyl Chemical group 0.000 claims description 120
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 120
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125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 90
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RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 72
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229910052736 halogen Inorganic materials 0.000 claims description 70
150000002367 halogens Chemical class 0.000 claims description 70
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125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 24
KJHKTHWMRKYKJE-SUGCFTRWSA-N Kaletra Chemical compound N1([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=2C=CC=CC=2)NC(=O)COC=2C(=CC=CC=2C)C)CC=2C=CC=CC=2)CCCNC1=O KJHKTHWMRKYKJE-SUGCFTRWSA-N 0.000 claims description 23
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HBOMLICNUCNMMY-XLPZGREQSA-N zidovudine Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](N=[N+]=[N-])C1 HBOMLICNUCNMMY-XLPZGREQSA-N 0.000 claims description 16
PEASPLKKXBYDKL-FXEVSJAOSA-N enfuvirtide Chemical compound C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(C)=O)[C@@H](C)O)[C@@H](C)CC)C1=CN=CN1 PEASPLKKXBYDKL-FXEVSJAOSA-N 0.000 claims description 15
WREGKURFCTUGRC-POYBYMJQSA-N Zalcitabine Chemical compound O=C1N=C(N)C=CN1[C@@H]1O[C@H](CO)CC1 WREGKURFCTUGRC-POYBYMJQSA-N 0.000 claims description 14
NQDJXKOVJZTUJA-UHFFFAOYSA-N nevirapine Chemical compound C12=NC=CC=C2C(=O)NC=2C(C)=CC=NC=2N1C1CC1 NQDJXKOVJZTUJA-UHFFFAOYSA-N 0.000 claims description 14
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239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims description 14
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BXZVVICBKDXVGW-NKWVEPMBSA-N Didanosine Chemical compound O1[C@H](CO)CC[C@@H]1N1C(NC=NC2=O)=C2N=C1 BXZVVICBKDXVGW-NKWVEPMBSA-N 0.000 claims description 11
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108010032976 Enfuvirtide Proteins 0.000 claims description 10
229910052760 oxygen Inorganic materials 0.000 claims description 10
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108090000790 Enzymes Proteins 0.000 claims description 9
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NCDNCNXCDXHOMX-XGKFQTDJSA-N ritonavir Chemical compound N([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1SC=NC=1)CC=1C=CC=CC=1)C(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-XGKFQTDJSA-N 0.000 claims description 9
SUJUHGSWHZTSEU-FYBSXPHGSA-N tipranavir Chemical compound C([C@@]1(CCC)OC(=O)C([C@H](CC)C=2C=C(NS(=O)(=O)C=3N=CC(=CC=3)C(F)(F)F)C=CC=2)=C(O)C1)CC1=CC=CC=C1 SUJUHGSWHZTSEU-FYBSXPHGSA-N 0.000 claims description 9
229960000523 zalcitabine Drugs 0.000 claims description 9
XPOQHMRABVBWPR-ZDUSSCGKSA-N efavirenz Chemical compound C([C@]1(C2=CC(Cl)=CC=C2NC(=O)O1)C(F)(F)F)#CC1CC1 XPOQHMRABVBWPR-ZDUSSCGKSA-N 0.000 claims description 8
JTEGQNOMFQHVDC-NKWVEPMBSA-N lamivudine Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1 JTEGQNOMFQHVDC-NKWVEPMBSA-N 0.000 claims description 8
QAGYKUNXZHXKMR-HKWSIXNMSA-N nelfinavir Chemical compound CC1=C(O)C=CC=C1C(=O)N[C@H]([C@H](O)CN1[C@@H](C[C@@H]2CCCC[C@@H]2C1)C(=O)NC(C)(C)C)CSC1=CC=CC=C1 QAGYKUNXZHXKMR-HKWSIXNMSA-N 0.000 claims description 8
QWAXKHKRTORLEM-UGJKXSETSA-N saquinavir Chemical compound C([C@@H]([C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)C=1N=C2C=CC=CC2=CC=1)C1=CC=CC=C1 QWAXKHKRTORLEM-UGJKXSETSA-N 0.000 claims description 8
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AXRYRYVKAWYZBR-GASGPIRDSA-N atazanavir Chemical compound C([C@H](NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)[C@@H](O)CN(CC=1C=CC(=CC=1)C=1N=CC=CC=1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C1=CC=CC=C1 AXRYRYVKAWYZBR-GASGPIRDSA-N 0.000 claims description 7
CJBJHOAVZSMMDJ-HEXNFIEUSA-N darunavir Chemical compound C([C@@H]([C@H](O)CN(CC(C)C)S(=O)(=O)C=1C=CC(N)=CC=1)NC(=O)O[C@@H]1[C@@H]2CCO[C@@H]2OC1)C1=CC=CC=C1 CJBJHOAVZSMMDJ-HEXNFIEUSA-N 0.000 claims description 7
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229910052757 nitrogen Inorganic materials 0.000 claims description 7
LHCOVOKZWQYODM-CPEOKENHSA-N 4-amino-1-[(2r,5s)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one;1-[(2r,4s,5s)-4-azido-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1.O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](N=[N+]=[N-])C1 LHCOVOKZWQYODM-CPEOKENHSA-N 0.000 claims description 6
238000011225 antiretroviral therapy Methods 0.000 claims description 6
CBVCZFGXHXORBI-PXQQMZJSSA-N indinavir Chemical compound C([C@H](N(CC1)C[C@@H](O)C[C@@H](CC=2C=CC=CC=2)C(=O)N[C@H]2C3=CC=CC=C3C[C@H]2O)C(=O)NC(C)(C)C)N1CC1=CC=CN=C1 CBVCZFGXHXORBI-PXQQMZJSSA-N 0.000 claims description 6
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239000003937 drug carrier Substances 0.000 claims description 5
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WMHSRBZIJNQHKT-FFKFEZPRSA-N abacavir sulfate Chemical compound OS(O)(=O)=O.C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1.C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1 WMHSRBZIJNQHKT-FFKFEZPRSA-N 0.000 claims description 4
MLBVMOWEQCZNCC-OEMFJLHTSA-N fosamprenavir Chemical compound C([C@@H]([C@H](OP(O)(O)=O)CN(CC(C)C)S(=O)(=O)C=1C=CC(N)=CC=1)NC(=O)O[C@@H]1COCC1)C1=CC=CC=C1 MLBVMOWEQCZNCC-OEMFJLHTSA-N 0.000 claims description 4
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ASOMNDIOOKDVDC-UHFFFAOYSA-N 1h-indol-2-yl-[4-[3-(propan-2-ylamino)pyridin-2-yl]piperazin-1-yl]methanone Chemical compound CC(C)NC1=CC=CN=C1N1CCN(C(=O)C=2NC3=CC=CC=C3C=2)CC1 ASOMNDIOOKDVDC-UHFFFAOYSA-N 0.000 claims description 2
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CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
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235000019204 saccharin Nutrition 0.000 description 1
239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
238000012216 screening Methods 0.000 description 1
150000003335 secondary amines Chemical class 0.000 description 1
229910052711 selenium Inorganic materials 0.000 description 1
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238000010561 standard procedure Methods 0.000 description 1
239000008107 starch Substances 0.000 description 1
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238000004659 sterilization and disinfection Methods 0.000 description 1
238000003756 stirring Methods 0.000 description 1
238000003860 storage Methods 0.000 description 1
238000010254 subcutaneous injection Methods 0.000 description 1
239000007929 subcutaneous injection Substances 0.000 description 1
125000000547 substituted alkyl group Chemical group 0.000 description 1
125000005346 substituted cycloalkyl group Chemical group 0.000 description 1
239000001384 succinic acid Substances 0.000 description 1
239000005720 sucrose Substances 0.000 description 1
235000000346 sugar Nutrition 0.000 description 1
150000005846 sugar alcohols Polymers 0.000 description 1
150000008163 sugars Chemical class 0.000 description 1
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150000008053 sultones Chemical class 0.000 description 1
239000000829 suppository Substances 0.000 description 1
239000002511 suppository base Substances 0.000 description 1
FIAFUQMPZJWCLV-UHFFFAOYSA-N suramin Chemical compound OS(=O)(=O)C1=CC(S(O)(=O)=O)=C2C(NC(=O)C3=CC=C(C(=C3)NC(=O)C=3C=C(NC(=O)NC=4C=C(C=CC=4)C(=O)NC=4C(=CC=C(C=4)C(=O)NC=4C5=C(C=C(C=C5C(=CC=4)S(O)(=O)=O)S(O)(=O)=O)S(O)(=O)=O)C)C=CC=3)C)=CC=C(S(O)(=O)=O)C2=C1 FIAFUQMPZJWCLV-UHFFFAOYSA-N 0.000 description 1
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NVPOUMXZERMIJK-QWHCGFSZSA-N tert-butyl n-[(1s)-1-[(2s)-oxiran-2-yl]-2-phenylethyl]carbamate Chemical compound C([C@H](NC(=O)OC(C)(C)C)[C@@H]1OC1)C1=CC=CC=C1 NVPOUMXZERMIJK-QWHCGFSZSA-N 0.000 description 1
YOWOIMCOCHUFEO-PZUNEJSGSA-N tert-butyl n-[(2s,3r)-3-hydroxy-4-[(3-methoxyphenyl)sulfonyl-[[(2r)-oxolan-2-yl]methyl]amino]-1-phenylbutan-2-yl]carbamate Chemical compound COC1=CC=CC(S(=O)(=O)N(C[C@@H](O)[C@H](CC=2C=CC=CC=2)NC(=O)OC(C)(C)C)C[C@@H]2OCCC2)=C1 YOWOIMCOCHUFEO-PZUNEJSGSA-N 0.000 description 1
NVPOUMXZERMIJK-UHFFFAOYSA-N tert-butyl n-[1-(oxiran-2-yl)-2-phenylethyl]carbamate Chemical compound C1OC1C(NC(=O)OC(C)(C)C)CC1=CC=CC=C1 NVPOUMXZERMIJK-UHFFFAOYSA-N 0.000 description 1
RAOIDOHSFRTOEL-UHFFFAOYSA-N tetrahydrothiophene Chemical compound C1CCSC1 RAOIDOHSFRTOEL-UHFFFAOYSA-N 0.000 description 1
ALPKFOALTCELEH-UHFFFAOYSA-J tetrasodium 4-[[4-[[4-anilino-6-[[5-hydroxy-6-[(2-methoxy-5-sulfonatophenyl)diazenyl]-7-sulfonatonaphthalen-2-yl]amino]-1,3,5-triazin-2-yl]amino]-5-methoxy-2-methylphenyl]diazenyl]-5-hydroxynaphthalene-2,7-disulfonate Chemical compound CC1=CC(=C(C=C1N=NC2=C3C(=CC(=C2)S(=O)(=O)[O-])C=C(C=C3[O-])S(=O)(=O)O)OC)NC4=NC(=NC(=N4)NC5=CC6=CC(=C(C(=C6C=C5)[O-])N=NC7=C(C=CC(=C7)S(=O)(=O)[O-])OC)S(=O)(=O)O)NC8=CC=CC=C8.[Na+].[Na+].[Na+].[Na+] ALPKFOALTCELEH-UHFFFAOYSA-J 0.000 description 1
231100001274 therapeutic index Toxicity 0.000 description 1
GVIJJXMXTUZIOD-UHFFFAOYSA-N thianthrene Chemical compound C1=CC=C2SC3=CC=CC=C3SC2=C1 GVIJJXMXTUZIOD-UHFFFAOYSA-N 0.000 description 1
RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 description 1
229940033663 thimerosal Drugs 0.000 description 1
150000007970 thio esters Chemical class 0.000 description 1
QERYCTSHXKAMIS-UHFFFAOYSA-N thiophene-2-carboxylic acid Chemical compound OC(=O)C1=CC=CS1 QERYCTSHXKAMIS-UHFFFAOYSA-N 0.000 description 1
230000036964 tight binding Effects 0.000 description 1
HPGGPRDJHPYFRM-UHFFFAOYSA-J tin(iv) chloride Chemical compound Cl[Sn](Cl)(Cl)Cl HPGGPRDJHPYFRM-UHFFFAOYSA-J 0.000 description 1
KJAMZCVTJDTESW-UHFFFAOYSA-N tiracizine Chemical compound C1CC2=CC=CC=C2N(C(=O)CN(C)C)C2=CC(NC(=O)OCC)=CC=C21 KJAMZCVTJDTESW-UHFFFAOYSA-N 0.000 description 1
229950011282 tivirapine Drugs 0.000 description 1
JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
230000009466 transformation Effects 0.000 description 1
150000003852 triazoles Chemical class 0.000 description 1
125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
125000004360 trifluorophenyl group Chemical group 0.000 description 1
125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 description 1
ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
238000001291 vacuum drying Methods 0.000 description 1
238000009777 vacuum freeze-drying Methods 0.000 description 1
NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical class CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 1
239000003981 vehicle Substances 0.000 description 1
239000008215 water for injection Substances 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/08—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
- 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
- C07D263/18—Oxygen atoms
- C07D263/20—Oxygen atoms attached in position 2
- C07D263/24—Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
- 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
- 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

Landscapes

Organic Chemistry (AREA)
Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Virology (AREA)
General Chemical & Material Sciences (AREA)
Veterinary Medicine (AREA)
Oncology (AREA)
Communicable Diseases (AREA)
Chemical Kinetics & Catalysis (AREA)
Public Health (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
AIDS & HIV (AREA)
Tropical Medicine & Parasitology (AREA)
Molecular Biology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Plural Heterocyclic Compounds (AREA)

AU2006262275A 2005-06-22 2006-06-21 HIV-1 protease inhibitors, and methods of making and using them Abandoned AU2006262275A1 (en)

Applications Claiming Priority (7)

Application Number	Priority Date	Filing Date	Title
US69313405P	2005-06-22	2005-06-22
US60/693,134		2005-06-22
US74990205P	2005-12-12	2005-12-12
US60/749,902		2005-12-12
US81023406P	2006-06-02	2006-06-02
US60/810,234		2006-06-02
PCT/US2006/024109 WO2007002173A1 (fr)	2005-06-22	2006-06-21	Inhibiteurs de la protease du vih-1, et leurs procedes de fabrication et d'utilisation

Publications (1)

Publication Number	Publication Date
AU2006262275A1 true AU2006262275A1 (en)	2007-01-04

Family

ID=37441408

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
AU2006262275A Abandoned AU2006262275A1 (en)	2005-06-22	2006-06-21	HIV-1 protease inhibitors, and methods of making and using them

Country Status (5)

Country	Link
EP (1)	EP1937655A1 (fr)
JP (1)	JP2008546790A (fr)
AU (1)	AU2006262275A1 (fr)
CA (1)	CA2667449A1 (fr)
WO (1)	WO2007002173A1 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
BR112013010774A2 (pt) *	2010-10-31	2017-03-21	Napo Pharmaceuticals Inc	"usos de crofelemer no tratamento de diarreia associada ao hiv"

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US6046190A (en) *	1992-08-25	2000-04-04	G.D. Searle & Co.	Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors

2006
- 2006-06-21 JP JP2008518348A patent/JP2008546790A/ja not_active Withdrawn
- 2006-06-21 CA CA002667449A patent/CA2667449A1/fr not_active Abandoned
- 2006-06-21 WO PCT/US2006/024109 patent/WO2007002173A1/fr not_active Ceased
- 2006-06-21 AU AU2006262275A patent/AU2006262275A1/en not_active Abandoned
- 2006-06-21 EP EP06785253A patent/EP1937655A1/fr not_active Withdrawn

Also Published As

Publication number	Publication date
WO2007002173A1 (fr)	2007-01-04
CA2667449A1 (fr)	2007-01-04
EP1937655A1 (fr)	2008-07-02
JP2008546790A (ja)	2008-12-25

Publication	Publication Date	Title
EP2139883A2 (fr)	2010-01-06	Inhibiteurs de la protéase du vih-1
US20110178092A1 (en)	2011-07-21	HIV-1 Protease Inhibitors
JP4808380B2 (ja)	2011-11-02	Ｈｉｖプロテアーゼ阻害剤としてのカルバミン酸エステル
CA2658545A1 (fr)	2008-01-31	Inhibiteurs de bisfuranyl protease
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2009-03-05	DA3	Amendments made section 104	Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE CO-INVENTOR NAMES TO READ SCHIFFER, CELIA A.; KAIRYS, VISVALDAS; PRABU, MOSES; RANA, TARIQ M.; CAO, HONG; TIDOR, BRUCE; KING, NANCY; FERNANDES, MIGUEL X.; NALAM, MADHAVI NAGGA LAXMI; ALI, AKBAR; GARUDAMMAGARI SAI, KIRAN KUMAR REDDY; CHELLAPPAN, SRIPRIYA; GILSON, MICHAEL; NALIVAIKA, ELLEN; ANJUM, SAIMA GHAFOOR AND ALTMAN, MICHAEL D.
2011-04-21	PC1	Assignment before grant (sect. 113)	Owner name: UNIVERSITY OF MASSACHUSETTS; THE MASSACHUSETTS INS Free format text: FORMER APPLICANT(S): THE MASSACHUSETTS INSTITUTE OF TECHNOLOGY; UNIVERSITY OF MASSACHUSETTS; THE UNIVERSITY OF MARYLAND BIOTECHNOLOGY INSTITUTE
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Date

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Title

Description

2009-03-05

DA3

Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE CO-INVENTOR NAMES TO READ SCHIFFER, CELIA A.; KAIRYS, VISVALDAS; PRABU, MOSES; RANA, TARIQ M.; CAO, HONG; TIDOR, BRUCE; KING, NANCY; FERNANDES, MIGUEL X.; NALAM, MADHAVI NAGGA LAXMI; ALI, AKBAR; GARUDAMMAGARI SAI, KIRAN KUMAR REDDY; CHELLAPPAN, SRIPRIYA; GILSON, MICHAEL; NALIVAIKA, ELLEN; ANJUM, SAIMA GHAFOOR AND ALTMAN, MICHAEL D.

2011-04-21

PC1

Assignment before grant (sect. 113)

Owner name: UNIVERSITY OF MASSACHUSETTS; THE MASSACHUSETTS INS

Free format text: FORMER APPLICANT(S): THE MASSACHUSETTS INSTITUTE OF TECHNOLOGY; UNIVERSITY OF MASSACHUSETTS; THE UNIVERSITY OF MARYLAND BIOTECHNOLOGY INSTITUTE

2012-01-19

MK4

Application lapsed section 142(2)(d) - no continuation fee paid for the application