RU2320643C2 - Acylsulfonamides as steroid sulfatase inhibitors - Google Patents

Acylsulfonamides as steroid sulfatase inhibitors Download PDF

Info

Publication number
RU2320643C2
RU2320643C2 RU2004114244/04A RU2004114244A RU2320643C2 RU 2320643 C2 RU2320643 C2 RU 2320643C2 RU 2004114244/04 A RU2004114244/04 A RU 2004114244/04A RU 2004114244 A RU2004114244 A RU 2004114244A RU 2320643 C2 RU2320643 C2 RU 2320643C2
Authority
RU
Russia
Prior art keywords
substituted
alkyl
phenyl
bound
unsubstituted
Prior art date
Application number
RU2004114244/04A
Other languages
Russian (ru)
Other versions
RU2004114244A (en
Inventor
Амарилла ХОРВАТ (AT)
Амарилла ХОРВАТ
Филипп ЛЕР (AT)
Филипп Лер
Петер НУССБАУМЕР (AT)
Петер Нуссбаумер
Эрвин Пауль ШРАЙНЕР (AT)
Эрвин Пауль ШРАЙНЕР
Original Assignee
Новартис Аг
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB0124028A external-priority patent/GB0124028D0/en
Priority claimed from GB0124027A external-priority patent/GB0124027D0/en
Priority claimed from GB0127173A external-priority patent/GB0127173D0/en
Priority claimed from GB0127343A external-priority patent/GB0127343D0/en
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of RU2004114244A publication Critical patent/RU2004114244A/en
Application granted granted Critical
Publication of RU2320643C2 publication Critical patent/RU2320643C2/en

Links

Landscapes

  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

FIELD: organic chemistry, biochemistry, medicine, pharmacy.
SUBSTANCE: invention relates to novel compounds of formulas (Ip3)
Figure 00000003
or (Ip4)
Figure 00000004
wherein R1P3 means unsubstituted or substituted phenyl or thienyl wherein substitutes represent halogen atom, (C1-C6)-alkyl, (C1-C4)-halogenalkyl, nitro group, (C1-C4)-alkoxy group; R16P3 and R17P3 in common with carbon atom to which they are bound mean a bridge-bound saturated (C5-C12)-ring system that is substituted with (C4-C12)-alkyl, (C1-C6)-alkoxycarbonylamino group, for example, tert.-butoxycarbonylamino group; R18P3 means hydrogen atom; R1P4 means unsubstituted or substituted phenyl or thienyl wherein substitutes represent halogen atom, (C1-C6)-alkyl, (C1-C4)-halogenalkyl, nitro group, (C1-C4)-alkoxy group; R16P4 and R17P4 in common with carbon atom to which they are bound mean a substituted bridge-bound saturated (C5-C12)-cycloalkyl ring system, substituted piperidine or substituted bridge-bound piperidine wherein substitutes mean (C1-C6)-alkoxyoxycarbonyl, (C1-C6)-alkyl, unsubstituted phenyl or phenyl substituted with (C4-C12)-alkyl, (C1-C4)-halogenalkyl, nitro group, aminocarbonyl; R18P4 means hydrogen atom or hydroxyl but hydrogen atom preferably; mP4 means 1. Compounds of formulas (Ip3) and (Ip4) inhibit activity of steroid sulfatase that allows their using as components of pharmaceutical composition.
EFFECT: valuable biochemical and medicinal properties of compounds and pharmaceutical composition.
7 cl, 13 tbl, 386 ex

Description

Текст описания приведен в факсимильном виде.

Figure 00000005
Figure 00000006
Figure 00000007
Figure 00000008
Figure 00000009
Figure 00000010
Figure 00000011
Figure 00000012
Figure 00000013
Figure 00000014
Figure 00000015
Figure 00000016
Figure 00000017
Figure 00000018
Figure 00000019
Figure 00000020
Figure 00000021
Figure 00000022
Figure 00000023
Figure 00000024
Figure 00000025
Figure 00000026
Figure 00000027
Figure 00000028
Figure 00000029
Figure 00000030
Figure 00000031
Figure 00000032
Figure 00000033
Figure 00000034
Figure 00000035
Figure 00000036
Figure 00000037
Figure 00000038
Figure 00000039
Figure 00000040
Figure 00000041
Figure 00000042
Figure 00000043
Figure 00000044
Figure 00000045
Figure 00000046
Figure 00000047
Figure 00000048
Figure 00000049
Figure 00000050
Figure 00000051
Figure 00000052
Figure 00000053
Figure 00000054
Figure 00000055
Figure 00000056
Figure 00000057
Figure 00000058
Figure 00000059
Figure 00000060
Figure 00000061
Figure 00000062
Figure 00000063
Figure 00000064
Figure 00000065
Figure 00000066
Figure 00000067
Figure 00000068
Figure 00000069
Figure 00000070
Figure 00000071
Figure 00000072
Figure 00000073
Figure 00000074
Figure 00000075
Figure 00000076
Figure 00000077
Figure 00000078
Figure 00000079
Figure 00000080
Figure 00000081
Figure 00000082
Figure 00000083
Figure 00000084
Figure 00000085
Figure 00000086
Figure 00000087
Figure 00000088
Figure 00000089
Figure 00000090
Figure 00000091
Figure 00000092
Figure 00000093
Figure 00000094
Figure 00000095
Figure 00000096
Figure 00000097
Figure 00000098
Figure 00000099
Figure 00000100
Figure 00000101
Figure 00000102
Figure 00000103
Figure 00000104
Figure 00000105
Figure 00000106
Figure 00000107
Figure 00000108
Figure 00000109
Figure 00000110
Figure 00000111
Figure 00000112
Figure 00000113
Figure 00000114
Figure 00000115
Figure 00000116
Figure 00000117
Figure 00000118
The text of the description is given in facsimile form.
Figure 00000005
Figure 00000006
Figure 00000007
Figure 00000008
Figure 00000009
Figure 00000010
Figure 00000011
Figure 00000012
Figure 00000013
Figure 00000014
Figure 00000015
Figure 00000016
Figure 00000017
Figure 00000018
Figure 00000019
Figure 00000020
Figure 00000021
Figure 00000022
Figure 00000023
Figure 00000024
Figure 00000025
Figure 00000026
Figure 00000027
Figure 00000028
Figure 00000029
Figure 00000030
Figure 00000031
Figure 00000032
Figure 00000033
Figure 00000034
Figure 00000035
Figure 00000036
Figure 00000037
Figure 00000038
Figure 00000039
Figure 00000040
Figure 00000041
Figure 00000042
Figure 00000043
Figure 00000044
Figure 00000045
Figure 00000046
Figure 00000047
Figure 00000048
Figure 00000049
Figure 00000050
Figure 00000051
Figure 00000052
Figure 00000053
Figure 00000054
Figure 00000055
Figure 00000056
Figure 00000057
Figure 00000058
Figure 00000059
Figure 00000060
Figure 00000061
Figure 00000062
Figure 00000063
Figure 00000064
Figure 00000065
Figure 00000066
Figure 00000067
Figure 00000068
Figure 00000069
Figure 00000070
Figure 00000071
Figure 00000072
Figure 00000073
Figure 00000074
Figure 00000075
Figure 00000076
Figure 00000077
Figure 00000078
Figure 00000079
Figure 00000080
Figure 00000081
Figure 00000082
Figure 00000083
Figure 00000084
Figure 00000085
Figure 00000086
Figure 00000087
Figure 00000088
Figure 00000089
Figure 00000090
Figure 00000091
Figure 00000092
Figure 00000093
Figure 00000094
Figure 00000095
Figure 00000096
Figure 00000097
Figure 00000098
Figure 00000099
Figure 00000100
Figure 00000101
Figure 00000102
Figure 00000103
Figure 00000104
Figure 00000105
Figure 00000106
Figure 00000107
Figure 00000108
Figure 00000109
Figure 00000110
Figure 00000111
Figure 00000112
Figure 00000113
Figure 00000114
Figure 00000115
Figure 00000116
Figure 00000117
Figure 00000118

Claims (7)

1. Соединение формулы IР3 или IР4 1. The compound of formula I P3 or I P4
Figure 00000119
Figure 00000119
Figure 00000120
Figure 00000120
 где R1P3 обозначает незамещенный или замещенный фенил или тиенил, где заместители представляют собой галоген, C1-С6алкил, C1-C4 галоалкил, нитро, С1-С4алкокси;where R 1P3 is unsubstituted or substituted phenyl or thienyl, where the substituents are halogen, C 1 -C 6 alkyl, C 1 -C 4 haloalkyl, nitro, C 1 -C 4 alkoxy; R16P3 и R17P3 совместно с углеродным атомом, с которым они связаны, обозначают связанную мостиком насыщенную C5-C12 кольцевую систему, которая является замещенной С4-С12алкилом, C1-С6алкоксикарбониламино, например, трет-бутоксикарбониламино;R 16P3 and R 17P3 together with the carbon atom to which they are attached represent a bridged saturated C 5 -C 12 ring system that is substituted with C 4 -C 12 alkyl, C 1 -C 6 alkoxycarbonylamino, for example tert-butoxycarbonylamino; R18P3 обозначает водород;R 18P3 is hydrogen; R1P4 обозначает незамещенный или замещенный фенил или тиенил, где заместители представляют собой галоген, C1-С6алкил, C1-C4 галоалкил, нитро, С1-С4алкокси;R 1P4 is unsubstituted or substituted phenyl or thienyl, where the substituents are halogen, C 1 -C 6 alkyl, C 1 -C 4 haloalkyl, nitro, C 1 -C 4 alkoxy; R16P4 и R17P4 совместно с углеродным атомом, с которым они связаны, обозначают замещенную связанную мостиком насыщенную С5-С12циклоалкильную кольцевую систему, замещенный пиперидин или замещенный связанный мостиком пиперидин, где заместители означают C1-С6алкоксиоксикарбонил, C1-С6алкил, незамещенный фенил или фенил, замещенный С4-С12алкилом, С1-С4 галоалкилом, нитро, аминокарбонилом;R 16P4 and R 17P4 together with the carbon atom to which they are attached represent a substituted C 5 -C 12 cycloalkyl ring-linked bridge system, substituted piperidine or substituted piperidine bridged where the substituents are C 1 -C 6 alkoxyoxycarbonyl, C 1 - C 6 alkyl, unsubstituted phenyl or phenyl substituted with C 4 -C 12 alkyl, C 1 -C 4 haloalkyl, nitro, aminocarbonyl; R18P4 обозначает водород или гидроксил, более предпочтительно водород, mP4 обозначает 1.R 18P4 is hydrogen or hydroxyl, more preferably hydrogen, m P4 is 1. 2. Соединение по п.1, которое представляет собой соединение формулы2. The compound according to claim 1, which is a compound of the formula
Figure 00000121
Figure 00000121
 3. Соединение по одному из пп.1 или 2 в виде соли.3. The compound according to one of claims 1 or 2 in the form of a salt. 4. Соединение по одному из пп.1-3 для применения в качестве фармацевтического препарата, ингибирующего стероидсульфатазу.4. The compound according to one of claims 1 to 3 for use as a pharmaceutical preparation that inhibits steroid sulfatase. 5. Соединение по одному из пп.1-3 для применения для приготовления лекарственного средства, ингибирующего стероидсульфатазу.5. The compound according to one of claims 1 to 3 for use in the preparation of a medicament that inhibits steroid sulfatase. 6. Фармацевтическая композиция, ингибирующая стероидсульфатазу, включающая фармацевтически эффективное количество по меньшей мере одного соединения по одному из пп.1-3 в сочетании с по меньшей мере одним фармацевтически приемлемым наполнителем.6. A pharmaceutical composition that inhibits steroid sulfatase, comprising a pharmaceutically effective amount of at least one compound according to one of claims 1 to 3 in combination with at least one pharmaceutically acceptable excipient. 7. Соединение по одному из пп.1-3 для применения для приготовления фармацевтического препарата, ингибирующего стероидсульфатазу.7. The compound according to one of claims 1 to 3 for use in the preparation of a pharmaceutical preparation that inhibits steroid sulfatase.
RU2004114244/04A 2001-10-05 2002-10-04 Acylsulfonamides as steroid sulfatase inhibitors RU2320643C2 (en)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
GB0124028.2 2001-10-05
GB0124028A GB0124028D0 (en) 2001-10-05 2001-10-05 Organic compounds
GB0124027A GB0124027D0 (en) 2001-10-05 2001-10-05 Organic compounds
GB0124027.4 2001-10-05
GB0124839.2 2001-10-16
GB0127174.1 2001-11-12
GB0127173A GB0127173D0 (en) 2001-11-12 2001-11-12 Organic compounds
GB0127173.3 2001-11-12
GB0127343A GB0127343D0 (en) 2001-11-14 2001-11-14 Organic compounds
GB0127343.2 2001-11-14
GB0211524.4 2002-05-20

Publications (2)

Publication Number Publication Date
RU2004114244A RU2004114244A (en) 2005-10-27
RU2320643C2 true RU2320643C2 (en) 2008-03-27

Family

ID=35863786

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2004114244/04A RU2320643C2 (en) 2001-10-05 2002-10-04 Acylsulfonamides as steroid sulfatase inhibitors

Country Status (1)

Country Link
RU (1) RU2320643C2 (en)

Also Published As

Publication number Publication date
RU2004114244A (en) 2005-10-27

Similar Documents

Publication Publication Date Title
RU2342367C2 (en) Non-nucleozide inhibitors i of reverse transcriptase, intended for treatment of hiv-mediated diseases
RU2394031C2 (en) Quaternary ammonium salts as m3 antagonists
AR033525A1 (en) REPLACED ARILMETILAMINS, PHARMACEUTICAL COMPOSITIONS, USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT
MA27596A1 (en) BENZOCONDENSED HETEROARYLAMIDE DERIVATIVES OF THIENOPYRIDINES USEFUL AS THERAPEUTIC AGENTS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND METHODS FOR THEIR USE
SE0302760D0 (en) New compounds
NO20064933L (en) Macrocyclic compounds as inhibitors of viral replication
NO20050741L (en) New Process for the Synthesis and New Crystalline Form of Agomelatine and Pharmaceutical Compositions Containing the
ECSP055815A (en) COMPOSITION FOR THE TREATMENT OF INFECTION BY VIRUS FLAVIVIRIDAE
NO20062339L (en) Hepatitis C virus inhibitors
NO20056192L (en) Capase inhibitors and their use
BR0307409A (en) 2-Furanecarboxylic acid hydrazide compounds, pharmaceutical compositions containing them and use thereof for the preparation of a preventive or therapeutic agent
MXPA03011638A (en) 4-piperazinylindole derivatives with 5-ht6 receptor affinity.
NO20075749L (en) 1H-Quinazoline-2,4-diones and their use as ampa receptor ligands
NO20071314L (en) Peptidic vasopressin receptor agonists
TW200616979A (en) Non-nucleoside reverse transcriptase inhibitors
MA29213B1 (en) QUINOLONES WITH MACROLONES SUBSTITUTION - AMINO
EA200601194A1 (en) NEW DERIVATIVES OF BENZOFURANE USED FOR THE PREVENTION OR TREATMENT OF DISTURBANCES ASSOCIATED WITH 5-HT-RECEPTOR
NO20040881L (en) Oral antidiabetic agents.
RU2010154417A (en) COMBINATION OF A PARTIAL AGONIST OF NICOTINE RECEPTORS AND ACETYL CHOLINETERASE INHIBITOR CONTAINING ITS PHARMACEUTICAL COMPOSITION, AND ITS APPLICATION FOR TREATMENT OF COGNITIVE DISORDERS
DE602004029355D1 (en) SULFOPYRROLDERIVATE
SE0303480D0 (en) Benzofuranes
NO20053825L (en) Thienopyridazinones and their use in modulating autoimmune diseases.
RU2006104024A (en) KAPPA-AGONISTS, ESPECIALLY FOR TREATMENT AND / OR PREVENTION OF AN IRRITATED FATIGUE SYNDROME
KR960706476A (en) Novel benzen-esulfonylimine derivatives as inhibitors of lL-1 action as interleukin-1 activity inhibitors
RU2320643C2 (en) Acylsulfonamides as steroid sulfatase inhibitors

Legal Events

Date Code Title Description
MM4A The patent is invalid due to non-payment of fees

Effective date: 20111005