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1. (EP0964849) SULFONYL UREA DERIVATIVES AND THEIR USE IN THE CONTROL OF INTERLEUKIN-1 ACTIVITY

Office : European Patent Office
Application Number: 97947201 Application Date: 29.12.1997
Publication Number: 0964849 Publication Date: 22.12.1999
Publication Kind : B1
Designated States: AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LI, LU, NL, PT, SE
Prior PCT appl.: Application Number:IB1997001603 ; Publication Number: Click to see the data
IPC:
C07D 233/20
A61K 31/357
A61K 31/4164
A61K 31/64
A61P 1/00
A61P 9/10
A61P 19/10
A61P 25/00
A61P 29/00
A61P 37/00
C07C 311/54
C07C 311/60
C07C 317/14
C07C 323/67
C07D 209/08
C07D 235/08
C07D 307/64
C07D 317/18
C07D 333/20
C07D 333/34
C07D 335/06
C07D 407/04
C07D 409/04
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
233
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
04
having one double bond between ring members or between a ring member and a non-ring member
20
with substituted hydrocarbon radicals, directly attached to ring carbon atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
335
having oxygen as the only ring hetero atom, e.g. fungichromin
357
having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4164
1,3-Diazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
64
Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1
Drugs for disorders of the alimentary tract or the digestive system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
10
for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19
Drugs for skeletal disorders
08
for bone diseases, e.g. rachitism, Paget's disease
10
for osteoporosis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29
Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
311
Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
50
Compounds containing any of the groups X being a hetero atom, Y being any atom
52
Y being a hetero atom
54
either X or Y, but not both, being nitrogen atoms, e.g. N-sulfonylurea
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
311
Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
50
Compounds containing any of the groups X being a hetero atom, Y being any atom
52
Y being a hetero atom
54
either X or Y, but not both, being nitrogen atoms, e.g. N-sulfonylurea
57
having sulfur atoms of the sulfonylurea groups bound to carbon atoms of six-membered aromatic rings
60
having nitrogen atoms of the sulfonylurea groups bound to carbon atoms of six-membered aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
317
Sulfones; Sulfoxides
14
having sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
323
Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
64
containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton
67
containing sulfur atoms of sulfonamide groups, bound to the carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
08
with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
235
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02
condensed with carbocyclic rings or ring systems
04
Benzimidazoles; Hydrogenated benzimidazoles
06
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
08
Radicals containing only hydrogen and carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02
not condensed with other rings
34
having two or three double bonds between ring members or between ring members and non-ring members
56
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
64
Sulfur atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
317
Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
08
having the hetero atoms in positions 1 and 3
10
not condensed with other rings
14
with substituted hydrocarbon radicals attached to ring carbon atoms
18
Radicals substituted by singly bound oxygen or sulfur atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
333
Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
02
not condensed with other rings
04
not substituted on the ring sulfur atom
06
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
14
Radicals substituted by singly bound hetero atoms other than halogen
20
by nitrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
333
Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
02
not condensed with other rings
04
not substituted on the ring sulfur atom
26
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
30
Hetero atoms other than halogen
34
Sulfur atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
335
Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
04
condensed with carbocyclic rings or ring systems
06
Benzothiopyrans; Hydrogenated benzothiopyrans
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
407
Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/183
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
CPC:
C07D 307/64
C07C 311/60
C07C 317/14
C07C 323/67
C07C 2601/02
C07C 2601/04
C07C 2601/08
C07C 2601/14
C07C 2602/10
C07D 209/08
C07D 317/18
C07D 333/34
Applicants: PFIZER
Inventors: DOMBROSKI MARK ANTHONY
EGGLER JAMES FREDERICK
Priority Data: 9701603 29.12.1997 IB
3697997 29.01.1997 US
Title: (DE) SULFONYLHARNSTOFF-DERIVATE UND IHRE VERWENDUNG IN DER KONTROLLE DER INTERLEUKIN-1-AKTIVITÄT
(EN) SULFONYL UREA DERIVATIVES AND THEIR USE IN THE CONTROL OF INTERLEUKIN-1 ACTIVITY
(FR) DERIVES DE SULFONYLUREE ET LEUR APPLICATION EN MATIERE DE REGULATION DE L'ACTIVITE DE L'INTERLEUKINE-1
Abstract:
(EN) A compound of formula (I) wherein R1 and R2 are as defined in the description, R2 being an aromatic group, useful in the treatment and condition selected from the group consisting of the group meningitis and salpingitis, septic shock, disseminated intravascular coagulation, and/or adult respiratory distress syndrome, acute or chronic inflammation, arthritis, cholangitis, colitis, encephalitis, endocarditis, glomerulonephritis, hepatitis, myocarditis, pancreatitis, pericarditis, reperfusion injury, vasculitis, acute and delayed hypersensitivity, graft rejection, and graft-versus-host disease, auto-immune diseases including Type 1 diabetes mellitus and multiple sclerosis, periodonate diseases, interstitial pulmonary fibrosis, cirrhosis, systemic sclerosis, keloid formation tumors which produce IL-1 as an autocrine growth factor, cachexia, Alzeimer's disease, percussion injury, depression, atherosclerosis, osteoporosis in a mammal, including a human.
(FR) L'invention a trait à un composé de la formule (I) dans laquelle R1 et R2 sont tels que définis dans le descriptif. R2 représente un groupe aromatique, des plus utile en matière de traitement de troubles faisant partie de l'ensemble représenté par les méningite et salpingite, le choc septique, la coagulation intravasculaire disséminée et/ou le syndrome de détresse respiratoire de l'adulte, les inflammations aiguës ou chroniques, l'arthrite, l'angiocholite, la colite, l'encéphalite, l'endocardite, la glomérulonéphrite, l'hépatite, la myocardite, la pancréatite, la péricardite, les troubles associés à la reperfusion, les lésions, l'angéite, la réaction immunitaire aiguë ou retardée, le rejet de transplant, la maladie homologue, les affections auto-immunes, notamment le diabète sucré insulino-dépendant et la sclérose en plaques, les paradontolyses, la fibrose interstitielle pulmonaire, la cirrhose, la sclérodermie systémique, les tumeurs de formation de type chéloïde produisant IL-1 comme facteur de croissance autocrine, la cachexie, la maladie d'Alzheimer, la dépression, l'athérosclérose et l'ostéoporose chez le mammifère, race humaine comprise.
Also published as:
CZPV1999-2575IS5099NO19993658SK98299TR1999/01816YUP-337/99
MXPA/a/1999/007030KR1020000070541SG65991VN4111IL130855MA26468
AR011093EP1270554EP1270565US6166064JP2000511200 CN1245490
CA2279186EA199900603DE000069722663DE000069729762PT964849PT1270565
NZ336248AU1998052340VN4111MYPI 98000291BG103597WO/1998/032733