HUP9902092A2 - Metalloproteináz gátló benzolszulfonamidszármazékok, intermedierjeik, előállításuk és alkalmazásuk, a vegyületeket tartalmazó gyógyászati készítmények - Google Patents
Metalloproteináz gátló benzolszulfonamidszármazékok, intermedierjeik, előállításuk és alkalmazásuk, a vegyületeket tartalmazó gyógyászati készítményekInfo
- Publication number
- HUP9902092A2 HUP9902092A2 HU9902092A HUP9902092A HUP9902092A2 HU P9902092 A2 HUP9902092 A2 HU P9902092A2 HU 9902092 A HU9902092 A HU 9902092A HU P9902092 A HUP9902092 A HU P9902092A HU P9902092 A2 HUP9902092 A2 HU P9902092A2
- Authority
- HU
- Hungary
- Prior art keywords
- atom
- compounds
- ring atoms
- prodrugs
- intermediates
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 101710170181 Metalloproteinase inhibitor Proteins 0.000 title 1
- 150000008331 benzenesulfonamides Chemical class 0.000 title 1
- 239000000543 intermediate Substances 0.000 title 1
- 229940126170 metalloproteinase inhibitor Drugs 0.000 title 1
- 239000003475 metalloproteinase inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000006413 ring segment Chemical group 0.000 abstract 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 abstract 2
- 102000002274 Matrix Metalloproteinases Human genes 0.000 abstract 2
- 108010000684 Matrix Metalloproteinases Proteins 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000004434 sulfur atom Chemical group 0.000 abstract 2
- FHYFLMZUZUUPDY-UHFFFAOYSA-N 2h-thiazine-3-carboxamide Chemical compound NC(=O)C1=CC=CSN1 FHYFLMZUZUUPDY-UHFFFAOYSA-N 0.000 abstract 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 abstract 1
- 108060005980 Collagenase Proteins 0.000 abstract 1
- 102000029816 Collagenase Human genes 0.000 abstract 1
- 102000004318 Matrilysin Human genes 0.000 abstract 1
- 108090000855 Matrilysin Proteins 0.000 abstract 1
- 102000000422 Matrix Metalloproteinase 3 Human genes 0.000 abstract 1
- 206010027476 Metastases Diseases 0.000 abstract 1
- 206010003246 arthritis Diseases 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 210000000988 bone and bone Anatomy 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229960002424 collagenase Drugs 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000004151 fermentation Effects 0.000 abstract 1
- 238000000855 fermentation Methods 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 208000018937 joint inflammation Diseases 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 230000035515 penetration Effects 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 108091007196 stromelysin Proteins 0.000 abstract 1
- 210000001519 tissue Anatomy 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/04—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
- C07D279/12—1,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
-
- 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
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Pyridine Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
A cím szerinti vegyületek (I) általánős képletében Z jelentése őxigén- vagy kénatőm; V két vegyértékű csőpőrt, C* atőmmal és nitrőgénatőmmal hattagú gyűrűtalkőt, ahől a C*-tól és N-től különböző gyűrűatőmők egymástólfüggetlenül szűbsztitűálatlanők vagy megfelelő szűbsztitűensselszűbsztitűáltak, és a többi gyűrűatőmők közül legalább egyheterőatőmként őxigén-, nitrőgén- vagy kénatőm, míg a több gyűrűatőmszénatőm; Ar jelentése aril- vagy heterőarilcsőpőrt. A találmány kiterjedtővábbá azőknak a vegyületeknek gyógyászati szempőntból elfőgadhatósóira, prődrőgjaira és szőlvátjaira is. A találmány szerintivegyületek őlyan betegségek (kórős állapőtők) kezelésébenalkalmazhatók, amelyek lefőlyását mátrix-metallőprőteinázenzimek(kőllagenáz, mátrix-metallőprőteináz, matrilizin, sztrőmelizin)közvetítik, ilyenek: rákbetegség, illetve rákős daganat behatőlásaszövetekbe, rákős áttételek és ízületi gyűlladás. Kiemelten előnyöstalálmány szerinti vegyület a 3(S)-N-hidrőxi-4-{4-[(piridin-4-il)őxi]-benzőlszűlfőnil}-2,2-dimetil-tetrahidrő-2H-1,4-<%0 tia-zin-3-karbőxamid, valamint annak gyógyászati szempőntból elfőgadhatóprődrőgjai és sói. ŕ
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US56976695A | 1995-12-08 | 1995-12-08 |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP9902092A2 true HUP9902092A2 (hu) | 1999-09-28 |
HUP9902092A3 HUP9902092A3 (en) | 2000-12-28 |
Family
ID=24276764
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU9902092A HUP9902092A3 (en) | 1995-12-08 | 1996-12-05 | Metalloproteinase inhibitor benzenesulfonamide derivatives, intermediates, preparation and use thereof, pharmaceutical compositions containing these compounds |
Country Status (39)
Country | Link |
---|---|
US (1) | US6153757A (hu) |
EP (2) | EP1095936B1 (hu) |
JP (1) | JP2000502330A (hu) |
KR (1) | KR19990072009A (hu) |
CN (2) | CN1207289C (hu) |
AP (2) | AP1368A (hu) |
AT (2) | ATE283264T1 (hu) |
AU (1) | AU725831C (hu) |
BG (1) | BG64279B1 (hu) |
BR (1) | BR9611929A (hu) |
CA (1) | CA2238306A1 (hu) |
CO (1) | CO4790150A1 (hu) |
CZ (1) | CZ292942B6 (hu) |
DE (2) | DE69633947T2 (hu) |
DK (1) | DK0874830T3 (hu) |
EA (1) | EA003294B1 (hu) |
ES (2) | ES2195034T3 (hu) |
GE (1) | GEP20012388B (hu) |
GT (2) | GT199700015AA (hu) |
HR (1) | HRP970031A2 (hu) |
HU (1) | HUP9902092A3 (hu) |
ID (1) | ID17624A (hu) |
IL (6) | IL124559A (hu) |
MX (1) | MX9804457A (hu) |
MY (1) | MY117290A (hu) |
NO (1) | NO311360B1 (hu) |
NZ (1) | NZ325559A (hu) |
OA (1) | OA10794A (hu) |
PA (1) | PA8431301A1 (hu) |
PE (1) | PE69298A1 (hu) |
PL (1) | PL327275A1 (hu) |
PT (1) | PT874830E (hu) |
SI (1) | SI0874830T1 (hu) |
SK (1) | SK73898A3 (hu) |
SV (1) | SV1997000008A (hu) |
TR (1) | TR199800990T2 (hu) |
TW (1) | TW546293B (hu) |
WO (1) | WO1997020824A1 (hu) |
YU (1) | YU21597A (hu) |
Families Citing this family (114)
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SI0874830T1 (en) * | 1995-12-08 | 2003-08-31 | Agouron Pharmaceuticals, Inc. | A metalloproteinase inhibitor, a pharmaceutical composition containing it and the pharmaceutical use and method useful for the preparation thereof |
US6500948B1 (en) | 1995-12-08 | 2002-12-31 | Agouron Pharmaceuticals, Inc. | Metalloproteinase inhibitors-compositions, uses preparation and intermediates thereof |
US6747027B1 (en) | 1996-07-22 | 2004-06-08 | Pharmacia Corporation | Thiol sulfonamide metalloprotease inhibitors |
AU714687B2 (en) * | 1996-07-22 | 2000-01-06 | Monsanto Company | Thiol sulfone metalloprotease inhibitors |
BR9712085A (pt) | 1996-08-28 | 2000-10-24 | Procter & Gamble | Inibidores de metaloprotease heterocìclicos |
DE69716934T2 (de) * | 1996-08-28 | 2003-07-31 | The Procter & Gamble Company, Cincinnati | 1,3-diheterozyklische metalloprotease inhibitoren |
BR9713465A (pt) | 1996-08-28 | 2000-03-28 | Procter & Gamble | Inibidores metalotprotease de amina cìclica sibstituìda |
BR9712792A (pt) * | 1996-08-28 | 1999-12-14 | Procter & Gamble | Inibidores de metaloprotease bidentada. |
AU731319B2 (en) * | 1996-08-28 | 2001-03-29 | Procter & Gamble Company, The | Heterocyclic metalloprotease inhibitors |
US6872742B2 (en) | 1996-08-28 | 2005-03-29 | The Procter & Gamble Company | Substituted cyclic amine metalloprotease inhibitors |
US5977408A (en) * | 1996-10-16 | 1999-11-02 | American Cyanamid Company | Preparation and use of β-sulfonamido hydroxamic acids as matrix metalloproteinase and TACE inhibitors |
US5962481A (en) * | 1996-10-16 | 1999-10-05 | American Cyanamid Company | Preparation and use of ortho-sulfonamido heteroaryl hydroxamic acids as matrix metalloproteinase and tace inhibitors |
JP2001503037A (ja) * | 1996-10-16 | 2001-03-06 | アメリカン・サイアナミド・カンパニー | マトリクス金属プロテナイーゼおよびtaceに対する阻害薬としてのオルト―スルホンアミドヘテロアリールヒドロキサム酸の製造および使用 |
US6548524B2 (en) | 1996-10-16 | 2003-04-15 | American Cyanamid Company | Preparation and use of ortho-sulfonamido bicyclic heteroaryl hydroxamic acids as matrix metalloproteinase and TACE inhibitors |
US5929097A (en) * | 1996-10-16 | 1999-07-27 | American Cyanamid Company | Preparation and use of ortho-sulfonamido aryl hydroxamic acids as matrix metalloproteinase and tace inhibitors |
US6228869B1 (en) | 1996-10-16 | 2001-05-08 | American Cyanamid Company | Ortho-sulfonamido bicyclic hydroxamic acids as matrix metalloproteinase and TACE inhibitors |
US6008243A (en) * | 1996-10-24 | 1999-12-28 | Agouron Pharmaceuticals, Inc. | Metalloproteinase inhibitors, pharmaceutical compositions containing them, and their use |
US6174915B1 (en) | 1997-03-25 | 2001-01-16 | Agouron Pharmaceuticals, Inc. | Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses |
JP2001506257A (ja) | 1996-12-17 | 2001-05-15 | 藤沢薬品工業株式会社 | Mmpまたはtnf阻害剤としてのピペラジン化合物 |
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US6794511B2 (en) | 1997-03-04 | 2004-09-21 | G. D. Searle | Sulfonyl aryl or heteroaryl hydroxamic acid compounds |
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WO1998039316A1 (en) | 1997-03-04 | 1998-09-11 | Monsanto Company | N-hydroxy 4-sulfonyl butanamide compounds |
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KR20000075955A (ko) | 1997-03-04 | 2000-12-26 | 죤 에이치. 뷰센 | 방향족 술포닐 알파-히드록시 히드록삼산 화합물 |
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DK1357109T3 (da) | 1998-06-18 | 2008-09-08 | Hoffmann La Roche | Fremgangsmåde til arylalkylsulfid |
FR2780402B1 (fr) * | 1998-06-30 | 2001-04-27 | Adir | Nouveaux composes acides carboxyliques et hydroxamiques inhibiteurs de metalloproteases, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
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