HUP0402577A2 - Citoszol foszfolipáz A2 inhibitor hatású indolszármazékok, eljárás előállításukra - Google Patents

Citoszol foszfolipáz A2 inhibitor hatású indolszármazékok, eljárás előállításukra

Info

Publication number
HUP0402577A2
HUP0402577A2 HU0402577A HUP0402577A HUP0402577A2 HU P0402577 A2 HUP0402577 A2 HU P0402577A2 HU 0402577 A HU0402577 A HU 0402577A HU P0402577 A HUP0402577 A HU P0402577A HU P0402577 A2 HUP0402577 A2 HU P0402577A2
Authority
HU
Hungary
Prior art keywords
inhibitors
producing
pharmaceutical compositions
compositions containing
indole derivatives
Prior art date
Application number
HU0402577A
Other languages
English (en)
Inventor
John Caedmon Mckew
Steve Yik-Kai Tam
James Donald Clark
Katherine Lin Lee
Lihren Chen
Paresh Thakker
Fuk-Wah Sum
Mark Leo Behnke
Baihua Hu
Original Assignee
Wyeth
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
Application filed by Wyeth filed Critical Wyeth
Publication of HUP0402577A2 publication Critical patent/HUP0402577A2/hu
Publication of HUP0402577A3 publication Critical patent/HUP0402577A3/hu

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    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C07D209/16—Tryptamines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

Abstract

A találmány tárgyát az (I) általános képletű helyettesítettindolszármazékok és gyógyászati szempontból elfogadható sóik képezik,valamint ezen vegyületek alkalmazása olyan betegségek kezeléséreszolgáló gyógyászati készítmények előállítására, amelyeknél különfélefoszfolipáz enzimek, különösen foszfolipáz A2 enzimek gátlásaszükséges, különösen gyulladás és fájdalom kezelésére, megelőzésérevagy gátlására szolgáló gyógyszerek előállítására. Ó
HU0402577A 2001-12-03 2002-12-02 Indole derivatives as inhibitors of cytosolic phospholipase a2, process for producing them and pharmaceutical compositions containing them HUP0402577A3 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US33460501P 2001-12-03 2001-12-03
US33458801P 2001-12-03 2001-12-03
US33459101P 2001-12-03 2001-12-03
US41966402P 2002-10-18 2002-10-18
PCT/US2002/038311 WO2003048122A2 (en) 2001-12-03 2002-12-02 Inhibitors of cytosolic phospholipase a2

Publications (2)

Publication Number Publication Date
HUP0402577A2 true HUP0402577A2 (hu) 2005-03-29
HUP0402577A3 HUP0402577A3 (en) 2011-05-30

Family

ID=27502498

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0402577A HUP0402577A3 (en) 2001-12-03 2002-12-02 Indole derivatives as inhibitors of cytosolic phospholipase a2, process for producing them and pharmaceutical compositions containing them

Country Status (25)

Country Link
EP (1) EP1451154B1 (hu)
JP (1) JP4657605B2 (hu)
KR (1) KR100973665B1 (hu)
CN (1) CN100503566C (hu)
AR (1) AR037684A1 (hu)
AT (1) ATE384045T1 (hu)
AU (1) AU2002351182B2 (hu)
BR (1) BR0214672A (hu)
CA (1) CA2469138C (hu)
CO (1) CO5580763A2 (hu)
CY (1) CY1107383T1 (hu)
DE (1) DE60224707T2 (hu)
DK (2) DK1451154T3 (hu)
EC (1) ECSP045131A (hu)
ES (2) ES2300490T3 (hu)
HK (2) HK1065799A1 (hu)
HU (1) HUP0402577A3 (hu)
IL (2) IL162052A0 (hu)
IN (1) IN2005KO00312A (hu)
NO (1) NO327256B1 (hu)
NZ (1) NZ533269A (hu)
PL (1) PL370445A1 (hu)
PT (1) PT1451154E (hu)
TW (1) TWI334778B (hu)
WO (1) WO2003048122A2 (hu)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7713964B2 (en) 2001-12-03 2010-05-11 Wyeth Llc Methods for treating asthmatic conditions
US7605156B2 (en) 2001-12-03 2009-10-20 Wyeth Methods for the use of inhibitors of cytosolic phospholipase A2
TW200510305A (en) 2003-07-25 2005-03-16 Wyeth Corp Process for the preparation of CPLA2 inhibitors
DK1685104T3 (da) 2003-11-17 2008-04-14 Wyeth Corp Fremgangsmåde til fremstilling af N-substituerede phthalomider
HN2004000536A (es) * 2003-12-16 2009-02-18 Wyeth Corp Un procediemiento de sintesis para la alquilacion reductiva de la posicon c-3 de indoles
AR048239A1 (es) 2004-02-25 2006-04-12 Wyeth Corp Procesos para la preparacion de haluros de aril- y heteroaril-alquilsulfonilo e intermediarios de sintesis de los mismos
US20050244367A1 (en) * 2004-05-03 2005-11-03 Ilypsa, Inc. Phospholipase inhibitors localized in the gastrointestinal lumen
AR053410A1 (es) * 2004-08-19 2007-05-09 Wyeth Corp Proceso para la sintesis de indoles n-alquilados c-2, c-3 sustituidos. compuestos intermediarios
AU2006233502B2 (en) 2005-04-13 2011-07-28 Astion Pharma A/S Beta-2 adrenoceptor agonists for treating connective tissue diseases of the skin
GT200600228A (es) 2005-05-27 2006-12-26 Inhibidores de la fosfolipasa a2 citosolica
US7842834B2 (en) * 2005-07-21 2010-11-30 Wyeth Llc Process for the synthesis of sulfonyl halides and sulfonamides from sulfonic acid salts
MX2008005666A (es) 2005-11-03 2009-03-02 Ilypsa Inc Compuestos multivalentes de indol y uso de los mismos como inhibidores de fosfolipasa-a2.
FR2899471A1 (fr) * 2006-04-06 2007-10-12 Pasteur Institut Utilisation d'au moins un inhibiteur de la phospholipase a2 cytosolique comme medicament pour le traitement des maladies respiratoires
WO2007140317A2 (en) * 2006-05-26 2007-12-06 Wyeth Use of inhibitors of cytosolic ph0sph0lipase a2 in the treatment of thrombosis
BRPI0718066A2 (pt) * 2006-10-31 2013-11-05 Wyeth Corp Composição farmacêutica; forma de dosagem farmacêutica; processo para preparar uma composição farmacêutica;e produto.
MX2009004611A (es) * 2006-10-31 2009-05-22 Wyeth Corp Formulaciones de inhibidores de enzimas de fosfolipasa.
WO2008120818A1 (ja) * 2007-03-29 2008-10-09 Asubio Pharma Co., Ltd. ｃＰＬＡ２阻害活性を有するインドール誘導体およびその用途並びに製造方法
CN104710365A (zh) 2008-04-28 2015-06-17 旭化成制药株式会社 苯丙酸衍生物及其用途
WO2011047156A1 (en) * 2009-10-15 2011-04-21 Hercules Technology Management Co V, Inc. Sepiapterin reductase inhibitors for the treatment of pain
US20130209403A1 (en) 2010-09-08 2013-08-15 Ruprecht-Karls-Universitaet Use of inhibitors of phospholipase a2 for the treatment or prevention of flavivirus infection

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2079374C (en) * 1991-09-30 2003-08-05 Merck Frosst Canada Incorporated (bicyclic-azaarylmethoxy)indoles as inhibitors of leukotriene biosynthesis
US5994398A (en) * 1996-12-11 1999-11-30 Elan Pharmaceuticals, Inc. Arylsulfonamides as phospholipase A2 inhibitors
CN1299347A (zh) * 1998-02-25 2001-06-13 遗传研究所有限公司 磷脂酶抑制剂
KR20010041344A (ko) * 1998-02-25 2001-05-15 브루스 엠. 에이센, 토마스 제이 데스로저 포스포리파제 효소의 억제제

Also Published As

Publication number Publication date
ES2300490T3 (es) 2008-06-16
IN2005KO00312A (hu) 2015-08-14
AU2002351182A1 (en) 2003-06-17
WO2003048122A3 (en) 2003-09-18
TW200301695A (en) 2003-07-16
BR0214672A (pt) 2004-10-19
JP4657605B2 (ja) 2011-03-23
PL370445A1 (en) 2005-05-30
ES2401454T3 (es) 2013-04-19
EP1451154B1 (en) 2008-01-16
JP2005515997A (ja) 2005-06-02
CO5580763A2 (es) 2005-11-30
PT1451154E (pt) 2008-04-21
KR100973665B1 (ko) 2010-08-04
NO20042679L (no) 2004-06-25
ATE384045T1 (de) 2008-02-15
NO327256B1 (no) 2009-05-25
CA2469138A1 (en) 2003-06-12
HK1065799A1 (en) 2005-03-04
HK1113798A1 (en) 2008-10-17
CN100503566C (zh) 2009-06-24
IL162052A0 (en) 2005-11-20
EP1451154A2 (en) 2004-09-01
TWI334778B (en) 2010-12-21
DK1451154T3 (da) 2008-05-19
CA2469138C (en) 2012-04-17
KR20050044661A (ko) 2005-05-12
HUP0402577A3 (en) 2011-05-30
CN1617855A (zh) 2005-05-18
ECSP045131A (es) 2004-07-23
WO2003048122A2 (en) 2003-06-12
CY1107383T1 (el) 2012-12-19
DE60224707D1 (de) 2008-03-06
IL162052A (en) 2013-04-30
DK1892239T3 (da) 2013-03-25
NZ533269A (en) 2006-03-31
AU2002351182B2 (en) 2009-01-15
AR037684A1 (es) 2004-12-01
DE60224707T2 (de) 2009-02-26

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