HUP0105282A2 - A TNF-alfa-konvertáló enzimet gátló acetilénes szulfonamid-tiol vegyületek, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények - Google Patents
A TNF-alfa-konvertáló enzimet gátló acetilénes szulfonamid-tiol vegyületek, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0105282A2 HUP0105282A2 HU0105282A HUP0105282A HUP0105282A2 HU P0105282 A2 HUP0105282 A2 HU P0105282A2 HU 0105282 A HU0105282 A HU 0105282A HU P0105282 A HUP0105282 A HU P0105282A HU P0105282 A2 HUP0105282 A2 HU P0105282A2
- Authority
- HU
- Hungary
- Prior art keywords
- alkyl
- aryl
- hydrogen
- heteroaryl
- alkynyl
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 229940124530 sulfonamide Drugs 0.000 title 1
- -1 sulfonamide thiol Chemical class 0.000 title 1
- 239000002447 tumor necrosis factor alpha converting enzyme inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 102000004190 Enzymes Human genes 0.000 abstract 2
- 108090000790 Enzymes Proteins 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 208000030507 AIDS Diseases 0.000 abstract 1
- 206010009900 Colitis ulcerative Diseases 0.000 abstract 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 abstract 1
- 102000002274 Matrix Metalloproteinases Human genes 0.000 abstract 1
- 108010000684 Matrix Metalloproteinases Proteins 0.000 abstract 1
- 206010040047 Sepsis Diseases 0.000 abstract 1
- 206010054094 Tumour necrosis Diseases 0.000 abstract 1
- 201000006704 Ulcerative Colitis Diseases 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 201000008482 osteoarthritis Diseases 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
Classifications
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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
- C07F9/50—Organo-phosphines
- C07F9/53—Organo-phosphine oxides; Organo-phosphine thioxides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P31/04—Antibacterial agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B53/00—Asymmetric syntheses
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Neurosurgery (AREA)
- Virology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Emergency Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Transplantation (AREA)
- Physical Education & Sports Medicine (AREA)
- Biochemistry (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Hematology (AREA)
Abstract
A találmány a (B) általános képletű vegyületekre vonatkozik. A (B)vegyület (1a), (1b) vagy (1c) szerkezetű lehet. E képletekben abetűszimbólumok főbb jelentései: W jelentése oxigén- vagy kénatom; Xjelentése SO2 vagy -P(O)- R10 csoport; Y jelentése aril- vagyheteroarilcsoport; Z jelentése O, NH, CH2 vagy S; R1 jelentésehidrogénatom, aril-, alkil-, alkenil- vagy alkinilcsoport; R2jelentése hidrogénatom, aril-, cikloalkil-, alkil-, alkenil- vagyalkinilcsoport; R3 jelentése hidrogénatom vagy alkilcsoport; R4 és R5jelentése hidrogénatom, alkil- vagy cianocsoport; R6 jelentésehidrogénatom, aril-, heteroarilcsoport, alkil-, alkenil-, alkinil-vagy heterocikloalkilcsoport; R10 jelentése alkil- vagycikloalkilcsoport, aril- vagy heteroarilcsoport; és R14 jelentésehidroxil-, alkoxi-, amino-, alkil-, cikloalkil-, aril- vagyheteroarilcsoport. A találmány szerinti vegyületek gátolják atumornekrózis-a-faktor konvertáló enzimet (TACE) vagy a mátrix-metalloproteináz enzimet, és ennek alapján várhatóan alkalmasaklesznek ezen enzimekkel közvetített kóros állapotok - például reumásízületi gyulladás, csontízületi gyulladás, szepszis, AIDS, és fekélyesvastagbélgyulladás - kezelésére. A találmány kiterjed a vegyületekelőállítására és ezeket tartalmazó gyógyszerkészítményekre. Ó
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23839399A | 1999-01-27 | 1999-01-27 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0105282A2 true HUP0105282A2 (hu) | 2002-05-29 |
| HUP0105282A3 HUP0105282A3 (en) | 2005-04-28 |
Family
ID=22897697
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0105282A HUP0105282A3 (en) | 1999-01-27 | 2000-01-27 | Acetylenic sulfonamide thiol tace inhibitors process for their preparation and pharmaceutical compositions containing the same |
Country Status (21)
| Country | Link |
|---|---|
| EP (1) | EP1149074B1 (hu) |
| JP (1) | JP2002535386A (hu) |
| KR (1) | KR20010101691A (hu) |
| CN (1) | CN1224612C (hu) |
| AT (1) | ATE280152T1 (hu) |
| AU (1) | AU766192B2 (hu) |
| BR (1) | BR0007727A (hu) |
| CA (1) | CA2356480A1 (hu) |
| CZ (1) | CZ20012545A3 (hu) |
| DE (1) | DE60015079T2 (hu) |
| DK (1) | DK1149074T3 (hu) |
| EA (1) | EA200100811A1 (hu) |
| ES (1) | ES2230064T3 (hu) |
| HK (1) | HK1038915A1 (hu) |
| HU (1) | HUP0105282A3 (hu) |
| IL (1) | IL144347A0 (hu) |
| NO (1) | NO20013638L (hu) |
| NZ (1) | NZ512306A (hu) |
| PL (1) | PL350420A1 (hu) |
| WO (1) | WO2000044716A1 (hu) |
| ZA (1) | ZA200105069B (hu) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003033477A1 (en) * | 2001-10-12 | 2003-04-24 | Warner-Lambert Company Llc | Alkynlated fused ring pyrimidine compounds as matrix metalloprotease-13 inhibitor |
| US6962922B2 (en) | 2001-10-12 | 2005-11-08 | Warner-Lambert Company Llc | Alkynylated quinazoline compounds |
| DE60232276D1 (de) | 2001-12-20 | 2009-06-18 | Bristol Myers Squibb Co | Alpha-(n-sulfonamid)acetamidderivate als beta-amyloidinhibitoren |
| US6747147B2 (en) | 2002-03-08 | 2004-06-08 | Warner-Lambert Company | Oxo-azabicyclic compounds |
| US6894057B2 (en) | 2002-03-08 | 2005-05-17 | Warner-Lambert Company | Oxo-azabicyclic compounds |
| US7199155B2 (en) | 2002-12-23 | 2007-04-03 | Wyeth Holdings Corporation | Acetylenic aryl sulfonate hydroxamic acid TACE and matrix metalloproteinase inhibitors |
| US8084477B2 (en) | 2007-10-31 | 2011-12-27 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production |
| US8093276B2 (en) | 2007-10-31 | 2012-01-10 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production |
| US8044077B2 (en) | 2009-03-19 | 2011-10-25 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compounds incorporating deuterium as inhibitors of beta amyloid peptide production |
| US7977362B2 (en) | 2009-03-20 | 2011-07-12 | Bristol-Myers Squibb Company | Alpha-(N-benzenesulfonamido)cycloalkyl derivatives |
| US8252821B2 (en) | 2009-04-14 | 2012-08-28 | Bristol-Myers Squibb Company | Bioavailable capsule compositions of amorphous alpha-(N-sulfonamido)acetamide compound |
| US20210393632A1 (en) | 2018-10-04 | 2021-12-23 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Egfr inhibitors for treating keratodermas |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2194209T3 (es) * | 1996-07-22 | 2003-11-16 | Monsanto Co | Inhibidores de metaloproteasa de tiol sulfona. |
| NZ333825A (en) * | 1996-07-22 | 2000-10-27 | Monsanto Co | Metalloprotease inhibitors particularly MMP-13 |
-
2000
- 2000-01-27 CZ CZ20012545A patent/CZ20012545A3/cs unknown
- 2000-01-27 AU AU27417/00A patent/AU766192B2/en not_active Ceased
- 2000-01-27 NZ NZ512306A patent/NZ512306A/en unknown
- 2000-01-27 JP JP2000595972A patent/JP2002535386A/ja active Pending
- 2000-01-27 HU HU0105282A patent/HUP0105282A3/hu unknown
- 2000-01-27 EA EA200100811A patent/EA200100811A1/ru unknown
- 2000-01-27 EP EP00905787A patent/EP1149074B1/en not_active Expired - Lifetime
- 2000-01-27 PL PL00350420A patent/PL350420A1/xx not_active Application Discontinuation
- 2000-01-27 KR KR1020017009365A patent/KR20010101691A/ko not_active Application Discontinuation
- 2000-01-27 DE DE60015079T patent/DE60015079T2/de not_active Expired - Fee Related
- 2000-01-27 CA CA002356480A patent/CA2356480A1/en not_active Abandoned
- 2000-01-27 DK DK00905787T patent/DK1149074T3/da active
- 2000-01-27 ES ES00905787T patent/ES2230064T3/es not_active Expired - Lifetime
- 2000-01-27 AT AT00905787T patent/ATE280152T1/de not_active IP Right Cessation
- 2000-01-27 WO PCT/US2000/002143 patent/WO2000044716A1/en not_active Application Discontinuation
- 2000-01-27 CN CNB008030286A patent/CN1224612C/zh not_active Expired - Fee Related
- 2000-01-27 BR BR0007727-5A patent/BR0007727A/pt not_active IP Right Cessation
- 2000-01-27 IL IL14434700A patent/IL144347A0/xx unknown
-
2001
- 2001-06-20 ZA ZA200105069A patent/ZA200105069B/en unknown
- 2001-07-24 NO NO20013638A patent/NO20013638L/no not_active Application Discontinuation
-
2002
- 2002-01-18 HK HK02100417.3A patent/HK1038915A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| HUP0105282A3 (en) | 2005-04-28 |
| HK1038915A1 (zh) | 2002-04-04 |
| EP1149074A1 (en) | 2001-10-31 |
| BR0007727A (pt) | 2001-10-30 |
| AU766192B2 (en) | 2003-10-09 |
| CA2356480A1 (en) | 2000-08-03 |
| DK1149074T3 (da) | 2005-01-10 |
| NZ512306A (en) | 2003-10-31 |
| WO2000044716A1 (en) | 2000-08-03 |
| NO20013638D0 (no) | 2001-07-24 |
| KR20010101691A (ko) | 2001-11-14 |
| DE60015079T2 (de) | 2005-03-03 |
| AU2741700A (en) | 2000-08-18 |
| NO20013638L (no) | 2001-07-24 |
| CN1337947A (zh) | 2002-02-27 |
| PL350420A1 (en) | 2002-12-16 |
| CZ20012545A3 (cs) | 2002-04-17 |
| ZA200105069B (en) | 2002-09-20 |
| ES2230064T3 (es) | 2005-05-01 |
| EA200100811A1 (ru) | 2002-12-26 |
| EP1149074B1 (en) | 2004-10-20 |
| JP2002535386A (ja) | 2002-10-22 |
| IL144347A0 (en) | 2002-05-23 |
| ATE280152T1 (de) | 2004-11-15 |
| DE60015079D1 (de) | 2004-11-25 |
| CN1224612C (zh) | 2005-10-26 |
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