PE115699A1 - PROTEASE CO-INHIBITORS - Google Patents
PROTEASE CO-INHIBITORSInfo
- Publication number
- PE115699A1 PE115699A1 PE1998000830A PE00083098A PE115699A1 PE 115699 A1 PE115699 A1 PE 115699A1 PE 1998000830 A PE1998000830 A PE 1998000830A PE 00083098 A PE00083098 A PE 00083098A PE 115699 A1 PE115699 A1 PE 115699A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- protease
- ch2cf3
- compound
- treat
- Prior art date
Links
- 108091005804 Peptidases Proteins 0.000 title abstract 2
- 239000004365 Protease Substances 0.000 title abstract 2
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 102000005927 Cysteine Proteases Human genes 0.000 abstract 1
- 108010005843 Cysteine Proteases Proteins 0.000 abstract 1
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 102000012479 Serine Proteases Human genes 0.000 abstract 1
- 108010022999 Serine Proteases Proteins 0.000 abstract 1
- ZRALSGWEFCBTJO-UHFFFAOYSA-N anhydrous guanidine Natural products NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 abstract 1
- 210000000988 bone and bone Anatomy 0.000 abstract 1
- 210000000845 cartilage Anatomy 0.000 abstract 1
- 230000015556 catabolic process Effects 0.000 abstract 1
- 238000006731 degradation reaction Methods 0.000 abstract 1
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 abstract 1
- 208000007565 gingivitis Diseases 0.000 abstract 1
- 239000011159 matrix material Substances 0.000 abstract 1
- 201000001245 periodontitis Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—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
- 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
- C07D277/38—Nitrogen atoms
- C07D277/44—Acylated amino or imino radicals
- C07D277/48—Acylated amino or imino radicals by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof, e.g. carbonylguanidines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- 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
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Thiazole And Isothizaole Compounds (AREA)
Abstract
SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE X, X1, X2 Y X3 SON H, ALQUILO C1-C6 OPCIONALMENTE SUSTITUIDO CON F, CICLOALQUILO C3-C7, CN, C(O)R1, C(NCN)SR3, O(CH2)qC(O)NR1R2, S(O)mR3, ENTRE OTROS; m ES 0-2; q ES 1-2; n ES 0-2; R1 ES H, ALQUILO C1-C6, CF3, CH2CF3; O R1 Y R2 JUNTO CON N FORMAN UN ANILLO DE 5-7 MIEMBROS; R2 ES H, ALQUILO C1-C6, CF3, CH2CF3; R3 ES ALQUILO C1-C6, CF3, CH2CF3 Y X4 ES H, ALQUILO C1-C6, CICLOALQUILO C3-C7, COAr, COO-ALQUILO C1-C6, COOAr. UN COMPUESTO PREFERIDO ES N-BENCIL-N`-{4-{3-[4-(N-METIL-N-FENIL)AMINO-BUTOXI]-FENIL}TIAZOL-2-IL}GUANIDINA, ENTRE OTROS. EL COMPUESTO I INHIBE A UNA PROTEASA, DE PREFERENCIA A UNA CISTEINA-PROTEASA O UNA SERINA-PROTEASA; POR LO QUE PUEDE SER UTIL PARA TRATAR UNA ENFERMEDAD CARACTERIZADA POR PERDIDA DE HUESO COMO OSTEOPOROSIS, PERIODONTITIS, GINGIVITIS O TRATAR UNA ENFERMEDAD CARACTERIZADA POR LA EXCESIVA DEGRADACION DEL CARTILAGO DE LA MATRIZ COMO OSTEOARTRITIS, ARTRITIS REUMATOIDEREFERS TO A COMPOUND OF FORMULA I, WHERE X, X1, X2 AND X3 ARE H, ALKYL C1-C6 OPTIONALLY REPLACED WITH F, CYCLLOALKYL C3-C7, CN, C (O) R1, C (NCN) SR3, O ( CH2) qC (O) NR1R2, S (O) mR3, AMONG OTHERS; m IS 0-2; q IS 1-2; n ES 0-2; R1 IS H, C1-C6-ALKYL, CF3, CH2CF3; OR R1 AND R2 TOGETHER WITH N FORM A RING OF 5-7 MEMBERS; R2 IS H, C1-C6-ALKYL, CF3, CH2CF3; R3 IS C1-C6 ALKYL, CF3, CH2CF3 AND X4 IS H, C1-C6 ALKYL, CYCLOALKYL C3-C7, COAr, COO-C1-C6 ALKYL, COOAr. A PREFERRED COMPOUND IS N-BENCIL-N`- {4- {3- [4- (N-METHYL-N-PHENYL) AMINO-BUTOXI] -FENYL} THIAZOL-2-IL} GUANIDINE, AMONG OTHERS. COMPOUND I INHIBITS A PROTEASE, PREFERRED TO A CYSTEINE-PROTEASE OR SERINE-PROTEASE; SO IT MAY BE USEFUL TO TREAT A DISEASE CHARACTERIZED BY LOSS OF BONE LIKE OSTEOPOROSIS, PERIODONTITIS, GINGIVITIS OR TREAT A DISEASE CHARACTERIZED BY THE EXCESSIVE DEGRADATION OF THE CARTILAGE OF THE MATRIX, OSTEOARTRITIS,
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US5752797P | 1997-09-04 | 1997-09-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE115699A1 true PE115699A1 (en) | 2000-01-13 |
Family
ID=22011125
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE1998000830A PE115699A1 (en) | 1997-09-04 | 1998-09-04 | PROTEASE CO-INHIBITORS |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP1015438A4 (en) |
| JP (1) | JP2001514257A (en) |
| AU (1) | AU9300298A (en) |
| CA (1) | CA2302361A1 (en) |
| CO (1) | CO4970736A1 (en) |
| MA (1) | MA26540A1 (en) |
| PE (1) | PE115699A1 (en) |
| SA (1) | SA98190653A (en) |
| WO (1) | WO1999011637A1 (en) |
| ZA (1) | ZA988064B (en) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030144175A1 (en) | 1998-12-23 | 2003-07-31 | Smithkline Beecham Corporation | Protease inhibitors |
| US6583137B1 (en) | 1999-11-10 | 2003-06-24 | Smithkline Beecham Corporation | Protease inhibitors |
| WO2001034599A1 (en) | 1999-11-10 | 2001-05-17 | Smithkline Beecham Corporation | Protease inhibitors |
| JP2003513924A (en) | 1999-11-10 | 2003-04-15 | スミスクライン・ビーチャム・コーポレイション | Protease inhibitor |
| NZ520588A (en) | 2000-03-21 | 2004-06-25 | Smithkline Beecham Corp | Protease inhibitors |
| WO2002083863A2 (en) | 2001-04-17 | 2002-10-24 | Sepracor, Inc. | Thiazole and other heterocyclic ligands and use thereof |
| US7282512B2 (en) | 2002-01-17 | 2007-10-16 | Smithkline Beecham Corporation | Cycloalkyl ketoamides derivatives useful as cathepsin K inhibitors |
| KR100962972B1 (en) | 2002-07-26 | 2010-06-09 | 주식회사유한양행 | 1-phenylpiperidin-3-one derivatives and preparation method thereof |
| DE102004008141A1 (en) | 2004-02-19 | 2005-09-01 | Abbott Gmbh & Co. Kg | Guanidine compounds and their use as binding partners for 5-HT5 receptors |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS59225172A (en) * | 1983-06-03 | 1984-12-18 | Yamanouchi Pharmaceut Co Ltd | Novel guanidinothiazole derivative and its preparation |
-
1998
- 1998-09-01 MA MA25238A patent/MA26540A1/en unknown
- 1998-09-03 CO CO98050517A patent/CO4970736A1/en unknown
- 1998-09-03 JP JP2000508676A patent/JP2001514257A/en not_active Withdrawn
- 1998-09-03 ZA ZA988064A patent/ZA988064B/en unknown
- 1998-09-03 WO PCT/US1998/018289 patent/WO1999011637A1/en not_active Ceased
- 1998-09-03 CA CA002302361A patent/CA2302361A1/en not_active Abandoned
- 1998-09-03 EP EP98945850A patent/EP1015438A4/en not_active Withdrawn
- 1998-09-03 AU AU93002/98A patent/AU9300298A/en not_active Abandoned
- 1998-09-04 PE PE1998000830A patent/PE115699A1/en not_active Application Discontinuation
- 1998-10-17 SA SA98190653A patent/SA98190653A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MA26540A1 (en) | 2004-12-20 |
| ZA988064B (en) | 1999-05-28 |
| WO1999011637A1 (en) | 1999-03-11 |
| EP1015438A1 (en) | 2000-07-05 |
| SA98190653A (en) | 2005-12-03 |
| CO4970736A1 (en) | 2000-11-07 |
| CA2302361A1 (en) | 1999-03-11 |
| JP2001514257A (en) | 2001-09-11 |
| EP1015438A4 (en) | 2000-11-08 |
| AU9300298A (en) | 1999-03-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |