OA10956A - Phosphinate based inhibitors of matrix metalloproteases - Google Patents
Phosphinate based inhibitors of matrix metalloproteases Download PDFInfo
- Publication number
- OA10956A OA10956A OA9900007A OA9900007A OA10956A OA 10956 A OA10956 A OA 10956A OA 9900007 A OA9900007 A OA 9900007A OA 9900007 A OA9900007 A OA 9900007A OA 10956 A OA10956 A OA 10956A
- Authority
- OA
- OAPI
- Prior art keywords
- alkyl
- benzyl
- methylcarbamoyl
- dimethyl
- phosphinic acid
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title description 17
- 239000011159 matrix material Substances 0.000 title description 4
- 102000005741 Metalloproteases Human genes 0.000 title description 3
- 108010006035 Metalloproteases Proteins 0.000 title description 3
- ACVYVLVWPXVTIT-UHFFFAOYSA-M phosphinate Chemical compound [O-][PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-M 0.000 title description 3
- 150000001875 compounds Chemical class 0.000 claims abstract description 64
- -1 cis-platinim Chemical compound 0.000 claims abstract description 41
- 102000002274 Matrix Metalloproteinases Human genes 0.000 claims abstract description 12
- 108010000684 Matrix Metalloproteinases Proteins 0.000 claims abstract description 12
- 238000004519 manufacturing process Methods 0.000 claims abstract description 12
- 201000010099 disease Diseases 0.000 claims abstract description 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 11
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- 230000000694 effects Effects 0.000 claims abstract description 9
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- 238000011282 treatment Methods 0.000 claims abstract description 7
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- 206010040070 Septic Shock Diseases 0.000 claims abstract description 4
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims abstract description 4
- 230000036303 septic shock Effects 0.000 claims abstract description 4
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- 125000000217 alkyl group Chemical group 0.000 claims description 63
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- 125000003118 aryl group Chemical group 0.000 claims description 21
- 239000002253 acid Substances 0.000 claims description 19
- 230000005764 inhibitory process Effects 0.000 claims description 17
- 238000000034 method Methods 0.000 claims description 17
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- 125000003545 alkoxy group Chemical group 0.000 claims description 16
- 239000000203 mixture Substances 0.000 claims description 14
- 229910052739 hydrogen Inorganic materials 0.000 claims description 13
- 239000001257 hydrogen Substances 0.000 claims description 13
- 229910052799 carbon Inorganic materials 0.000 claims description 12
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 10
- 241000124008 Mammalia Species 0.000 claims description 9
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 8
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims description 8
- ACVYVLVWPXVTIT-UHFFFAOYSA-N phosphinic acid Chemical compound O[PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-N 0.000 claims description 8
- 125000004104 aryloxy group Chemical group 0.000 claims description 7
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 7
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 7
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 6
- 125000005843 halogen group Chemical group 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
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- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 5
- 125000001544 thienyl group Chemical group 0.000 claims description 5
- 125000006282 2-chlorobenzyl group Chemical group [H]C1=C([H])C(Cl)=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 4
- 125000004847 2-fluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 4
- 125000006284 3-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(F)=C1[H])C([H])([H])* 0.000 claims description 4
- 125000004217 4-methoxybenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1OC([H])([H])[H])C([H])([H])* 0.000 claims description 4
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 4
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- 125000001153 fluoro group Chemical group F* 0.000 claims description 3
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- 125000004414 alkyl thio group Chemical group 0.000 claims description 2
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims description 2
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims description 2
- 150000001721 carbon Chemical group 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 229910002091 carbon monoxide Inorganic materials 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 125000004850 cyclobutylmethyl group Chemical group C1(CCC1)C* 0.000 claims description 2
- 125000004210 cyclohexylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 2
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
- C07F9/655345—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a five-membered ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
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- C07F9/28—Phosphorus compounds with one or more P—C bonds
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/02—Local antiseptics
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- 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
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P35/00—Antineoplastic agents
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
- C07F9/301—Acyclic saturated acids which can have further substituents on alkyl
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
- C07F9/306—Arylalkanephosphinic acids, e.g. Ar-(CH2)n-P(=X)(R)(XH), (X = O,S, Se; n>=1)
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/58—Pyridine rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
- C07F9/65525—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a seven-(or more) membered ring
- C07F9/65527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a seven-(or more) membered ring condensed with carbocyclic rings or carbocyclic ring systems
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Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US2195996P | 1996-07-18 | 1996-07-18 |
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OA10956A true OA10956A (en) | 2001-10-30 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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OA9900007A OA10956A (en) | 1996-07-18 | 1999-01-13 | Phosphinate based inhibitors of matrix metalloproteases |
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US (1) | US6147061A (fr) |
EP (1) | EP0923585B1 (fr) |
JP (1) | JP3299975B2 (fr) |
KR (1) | KR20000067904A (fr) |
CN (1) | CN1225639A (fr) |
AP (1) | AP761A (fr) |
AR (1) | AR008260A1 (fr) |
AT (1) | ATE217315T1 (fr) |
AU (1) | AU712973B2 (fr) |
BG (1) | BG103111A (fr) |
BR (1) | BR9710381A (fr) |
CA (1) | CA2260898C (fr) |
CO (1) | CO4890852A1 (fr) |
CZ (1) | CZ11899A3 (fr) |
DE (1) | DE69712496T2 (fr) |
DK (1) | DK0923585T3 (fr) |
EA (1) | EA199900036A1 (fr) |
ES (1) | ES2175415T3 (fr) |
GT (1) | GT199700085A (fr) |
HN (1) | HN1997000099A (fr) |
HR (1) | HRP970391A2 (fr) |
HU (1) | HUP9903014A3 (fr) |
ID (1) | ID19443A (fr) |
IL (1) | IL127567A0 (fr) |
IS (1) | IS4928A (fr) |
MA (1) | MA24270A1 (fr) |
NO (1) | NO990184L (fr) |
NZ (1) | NZ333303A (fr) |
OA (1) | OA10956A (fr) |
PA (1) | PA8433701A1 (fr) |
PE (1) | PE88198A1 (fr) |
PL (1) | PL331254A1 (fr) |
PT (1) | PT923585E (fr) |
SI (1) | SI0923585T1 (fr) |
SK (1) | SK3799A3 (fr) |
TN (1) | TNSN97122A1 (fr) |
TR (1) | TR199900066T2 (fr) |
WO (1) | WO1998003516A1 (fr) |
YU (1) | YU1899A (fr) |
ZA (1) | ZA976330B (fr) |
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Publication number | Priority date | Publication date | Assignee | Title |
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ZW23187A1 (en) * | 1986-12-15 | 1988-06-29 | Hoffmann La Roche | Phosphinic acid derivatives |
CA2058797A1 (fr) * | 1991-02-01 | 1992-08-02 | Michael John Broadhurst | Derives d'aminoacide |
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UA48121C2 (uk) * | 1993-11-04 | 2002-08-15 | Сінтекс (С.Ш.А.) Інк. | Інгібітори матричних металопротеаз і фармацетична композиція на їх основі |
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1997
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- 1997-06-30 CA CA002260898A patent/CA2260898C/fr not_active Expired - Fee Related
- 1997-06-30 AU AU31042/97A patent/AU712973B2/en not_active Ceased
- 1997-06-30 WO PCT/IB1997/000800 patent/WO1998003516A1/fr active IP Right Grant
- 1997-06-30 IL IL12756797A patent/IL127567A0/xx unknown
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- 1997-06-30 CN CN97196455A patent/CN1225639A/zh active Pending
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- 1997-06-30 JP JP50673698A patent/JP3299975B2/ja not_active Expired - Fee Related
- 1997-06-30 BR BR9710381A patent/BR9710381A/pt not_active Application Discontinuation
- 1997-06-30 SK SK37-99A patent/SK3799A3/sk unknown
- 1997-06-30 EA EA199900036A patent/EA199900036A1/ru unknown
- 1997-06-30 PT PT97926182T patent/PT923585E/pt unknown
- 1997-06-30 HU HU9903014A patent/HUP9903014A3/hu unknown
- 1997-06-30 KR KR1019997000356A patent/KR20000067904A/ko not_active Application Discontinuation
- 1997-06-30 DE DE69712496T patent/DE69712496T2/de not_active Expired - Fee Related
- 1997-06-30 EP EP97926182A patent/EP0923585B1/fr not_active Expired - Lifetime
- 1997-06-30 AT AT97926182T patent/ATE217315T1/de not_active IP Right Cessation
- 1997-06-30 NZ NZ333303A patent/NZ333303A/en unknown
- 1997-06-30 SI SI9730325T patent/SI0923585T1/xx unknown
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- 1997-07-11 PE PE1997000608A patent/PE88198A1/es not_active Application Discontinuation
- 1997-07-14 HN HN1997000099A patent/HN1997000099A/es unknown
- 1997-07-14 US US08/892,417 patent/US6147061A/en not_active Expired - Fee Related
- 1997-07-15 GT GT199700085A patent/GT199700085A/es unknown
- 1997-07-16 ID IDP972461A patent/ID19443A/id unknown
- 1997-07-16 TN TNTNSN97122A patent/TNSN97122A1/fr unknown
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- 1997-07-16 AR ARP970103192A patent/AR008260A1/es not_active Application Discontinuation
- 1997-07-17 ZA ZA976330A patent/ZA976330B/xx unknown
- 1997-07-17 HR HR60/021,959A patent/HRP970391A2/hr not_active Application Discontinuation
- 1997-07-17 AP APAP/P/1997/001043A patent/AP761A/en active
- 1997-07-18 CO CO97040976A patent/CO4890852A1/es unknown
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1998
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1999
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