HUP0203122A2 - Fab I inhibitorok, eljárás az előállításukra, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

Fab I inhibitorok, eljárás az előállításukra, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk

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Publication number
HUP0203122A2
HUP0203122A2 HU0203122A HUP0203122A HUP0203122A2 HU P0203122 A2 HUP0203122 A2 HU P0203122A2 HU 0203122 A HU0203122 A HU 0203122A HU P0203122 A HUP0203122 A HU P0203122A HU P0203122 A2 HUP0203122 A2 HU P0203122A2
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HU
Hungary
Prior art keywords
compounds
alkyl
hydrogen
fab
substituted
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Application number
HU0203122A
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English (en)
Inventor
Walter E. DeWolf
Dalia R. Jakas
William H. Miller
Kenneth A. Newlander
Mark A. Seefeld
Irene N. Uzinskas
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Smithkline Beecham Corp.
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Publication date
Application filed by Smithkline Beecham Corp. filed Critical Smithkline Beecham Corp.
Publication of HUP0203122A2 publication Critical patent/HUP0203122A2/hu
Publication of HUP0203122A3 publication Critical patent/HUP0203122A3/hu
Publication of HU230030B1 publication Critical patent/HU230030B1/hu

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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • 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
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
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    • C07D209/52—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 condensed with a ring other than six-membered
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    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
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    • 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
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    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
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    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Pyridine Compounds (AREA)
  • Indole Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

A találmány (I) általános képletű vegyületekre - amelyek képletében jelentése adott esetben szubsztituált, kondenzált heteroaromás csoport, mely heteroatomként 1-2 nitrogénatomot vagy oxigén- vagy kénatomot tartalmaz. R1 jelentése hidrogénatom vagy alkilcsoport; R2 jelentése hidrogénatom, alkil- vagy cikloalkilcsoport; R3 jelentése adott esetben kondenzált öt- vagy hattagú heterogyűrűs csoportok, melyek heteroatomként nitrogént tartalmaznak és további csoportokkal szubsztituáltak; R4 jelentése hidrogénatom vagy alkilcsoport; azt jelenti, hogy a jelzett két kötés egyike kettős kötés, és a másik egyes kötés; R5 jelentése metiléncsoport, ha R5 egy kettős kötéshez kapcsolódik; vagy R5 jelentése hidrogénatom vagy alkilcsoport, ha R5 egy egyes kötéshez kapcsolódik; és gyógyászatilag elfogadható sóikra vonatkozik. A találmány szerinti vegyületek gátolják a Fab I-et, és így felhasználhatók bakteriális fertőzések kezelésére. A találmány magában foglalja a vegyületeket tartalmazó gyógyszerkészítményeket, valamint a vegyületek előállítási eljárását és gyógyászati alkalmazását is. Ó
HU0203122A 1999-10-08 2000-10-06 Fab I inhibitorok HU230030B1 (hu)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US15870499P 1999-10-08 1999-10-08
US60/158,704 1999-10-08
PCT/US2000/027844 WO2001027103A1 (en) 1999-10-08 2000-10-06 Fab i inhibitors

Publications (3)

Publication Number Publication Date
HUP0203122A2 true HUP0203122A2 (hu) 2003-01-28
HUP0203122A3 HUP0203122A3 (en) 2004-01-28
HU230030B1 HU230030B1 (hu) 2015-05-28

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ID=22569335

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Application Number Title Priority Date Filing Date
HU0203122A HU230030B1 (hu) 1999-10-08 2000-10-06 Fab I inhibitorok

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US (5) US6846819B1 (hu)
EP (1) EP1226138B1 (hu)
JP (1) JP4803935B2 (hu)
KR (1) KR100823382B1 (hu)
CN (1) CN1197860C (hu)
AR (1) AR025976A1 (hu)
AT (1) ATE285821T1 (hu)
AU (1) AU773218B2 (hu)
BR (1) BRPI0014470B1 (hu)
CA (1) CA2387016C (hu)
CZ (1) CZ302015B6 (hu)
DE (1) DE60017180T2 (hu)
EC (1) ECSP003699A (hu)
ES (1) ES2231275T3 (hu)
HK (1) HK1049656A1 (hu)
HU (1) HU230030B1 (hu)
IL (2) IL148820A0 (hu)
NO (1) NO322708B1 (hu)
NZ (1) NZ517706A (hu)
PE (1) PE20010635A1 (hu)
PL (1) PL201627B1 (hu)
TW (1) TW534909B (hu)
UY (1) UY26380A1 (hu)
WO (1) WO2001027103A1 (hu)
ZA (1) ZA200202631B (hu)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7524843B2 (en) 1999-10-08 2009-04-28 Affinium Pharmaceuticals, Inc. Fab I inhibitors
US9862737B2 (en) 2007-02-16 2018-01-09 Debiopharm International Sa Salts, prodrugs and polymorphs of fab I inhibitors
US10751351B2 (en) 2016-02-26 2020-08-25 Debiopharm International S.A. Medicament for treatment of diabetic foot infections

Families Citing this family (50)

* Cited by examiner, † Cited by third party
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CO5180550A1 (es) 1999-04-19 2002-07-30 Smithkline Beecham Corp Inhibidores de fab i
CO5370679A1 (es) 1999-06-01 2004-02-27 Smithkline Beecham Corp Inhibidores fab 1
US6730684B1 (en) 1999-10-08 2004-05-04 Affinium Pharmaceuticals, Inc. Fab I inhibitors
US6762201B1 (en) 1999-10-08 2004-07-13 Affinium Pharmaceuticals, Inc. Fab I inhibitors
WO2001026652A1 (en) * 1999-10-08 2001-04-19 Smithkline Beecham Corporation Fab i inhibitors
JP4272338B2 (ja) 2000-09-22 2009-06-03 バイエル アクチェンゲゼルシャフト ピリジン誘導体
AU2000277557A1 (en) * 2000-10-06 2002-04-22 Smith Kline Beecham Corporation Methods of agonizing and antagonizing fabk
US7048926B2 (en) 2000-10-06 2006-05-23 Affinium Pharmaceuticals, Inc. Methods of agonizing and antagonizing FabK
AU2002367773A1 (en) * 2001-04-06 2003-11-03 Affinium Pharmaceuticals, Inc. Fab i inhibitors
US7790709B2 (en) * 2002-12-06 2010-09-07 Affinium Pharmaceuticals, Inc. Heterocyclic compounds, methods of making them and their use in therapy
WO2004082586A2 (en) * 2003-03-17 2004-09-30 Affinium Pharmaceuticals, Inc. Phamaceutical compositions comprising inhibitors of fab i and further antibiotics
PL380887A1 (pl) 2003-12-29 2007-04-02 Sepracor Inc. Pirolowe i pirazolowe inhibitory DAAO
PT1828167E (pt) * 2004-06-04 2014-10-08 Debiopharm Int Sa Derivados de acrilamida como agentes antibióticos
EP1778695B1 (en) 2004-08-21 2012-03-21 Merck Patent GmbH POLYMERS OF THIENO[2,3-b]THIOPHENE
US7973060B2 (en) 2005-10-13 2011-07-05 Crystalgenomics, Inc. Fab I inhibitor and process for preparing same
WO2007067416A2 (en) * 2005-12-05 2007-06-14 Affinium Pharmaceuticals, Inc. Heterocyclylacrylamide compounds as fabi inhibitors and antibacterial agents
ES2594156T3 (es) 2006-01-06 2016-12-16 Sunovion Pharmaceuticals Inc. Cicloalquilaminas como inhibidores de la recaptación de monoaminas
JP5438975B2 (ja) 2006-01-06 2014-03-12 サノビオン ファーマシューティカルズ インク テトラロン系モノアミン再取り込み阻害剤
WO2007086584A1 (ja) * 2006-01-30 2007-08-02 Meiji Seika Kaisha, Ltd. 新規ＦａｂＫおよびＦａｂＩ／Ｋ阻害剤
WO2007115185A2 (en) 2006-03-31 2007-10-11 Sepracor Inc. Preparation of chiral amides and amines
US7884124B2 (en) 2006-06-30 2011-02-08 Sepracor Inc. Fluoro-substituted inhibitors of D-amino acid oxidase
EP2687533B1 (en) * 2006-07-20 2017-07-19 Debiopharm International SA Acrylamide derivatives as FAB I inhibitors
US7902252B2 (en) 2007-01-18 2011-03-08 Sepracor, Inc. Inhibitors of D-amino acid oxidase
NZ580429A (en) 2007-05-31 2012-04-27 Sepracor Inc Phenyl substituted cycloalkylamines as monoamine reuptake inhibitors
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