ATE523195T1 - Neue thiophen-derivate als sphingosin-1-phosphat- 1-rezeptorantagonisten - Google Patents

Neue thiophen-derivate als sphingosin-1-phosphat- 1-rezeptorantagonisten

Info

Publication number
ATE523195T1
ATE523195T1 AT06727686T AT06727686T ATE523195T1 AT E523195 T1 ATE523195 T1 AT E523195T1 AT 06727686 T AT06727686 T AT 06727686T AT 06727686 T AT06727686 T AT 06727686T AT E523195 T1 ATE523195 T1 AT E523195T1
Authority
AT
Austria
Prior art keywords
sphingosine
phosphate
receptor antagonists
thiophene derivatives
new thiophene
Prior art date
Application number
AT06727686T
Other languages
English (en)
Inventor
Martin Bolli
David Lehmann
Boris Mathys
Claus Mueller
Oliver Nayler
Joerg Velker
Thomas Weller
Original Assignee
Actelion Pharmaceuticals Ltd
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 Actelion Pharmaceuticals Ltd filed Critical Actelion Pharmaceuticals Ltd
Application granted granted Critical
Publication of ATE523195T1 publication Critical patent/ATE523195T1/de

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
    • C07D333/68Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D333/70Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/04Heterocyclic 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
    • C07D295/14Heterocyclic 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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155Heterocyclic 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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/78Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10Heterocyclic 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 carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AT06727686T 2005-03-23 2006-03-20 Neue thiophen-derivate als sphingosin-1-phosphat- 1-rezeptorantagonisten ATE523195T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP2005003072 2005-03-23
PCT/IB2006/050853 WO2006100635A2 (en) 2005-03-23 2006-03-20 Novel thiophene derivatives as sphingosine-1-phosphate-1 receptor agonists

Publications (1)

Publication Number Publication Date
ATE523195T1 true ATE523195T1 (de) 2011-09-15

Family

ID=37024211

Family Applications (1)

Application Number Title Priority Date Filing Date
AT06727686T ATE523195T1 (de) 2005-03-23 2006-03-20 Neue thiophen-derivate als sphingosin-1-phosphat- 1-rezeptorantagonisten

Country Status (18)

Country Link
US (1) US7846964B2 (de)
EP (1) EP1863475B1 (de)
JP (1) JP5063581B2 (de)
KR (1) KR20080002850A (de)
CN (1) CN101180050B (de)
AR (1) AR053449A1 (de)
AT (1) ATE523195T1 (de)
AU (1) AU2006226022A1 (de)
BR (1) BRPI0609665A2 (de)
CA (1) CA2602478A1 (de)
ES (1) ES2370791T3 (de)
IL (1) IL186149A0 (de)
MX (1) MX2007011669A (de)
NO (1) NO20075297L (de)
RU (1) RU2007138878A (de)
TW (1) TW200716552A (de)
WO (1) WO2006100635A2 (de)
ZA (1) ZA200709086B (de)

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US7605269B2 (en) * 2005-03-23 2009-10-20 Actelion Pharmaceuticals Ltd. Thiophene derivatives as Sphingosine-1-phosphate-1 receptor agonists
US7951794B2 (en) * 2005-06-24 2011-05-31 Actelion Pharmaceuticals Ltd. Thiophene derivatives
AR057894A1 (es) * 2005-11-23 2007-12-26 Actelion Pharmaceuticals Ltd Derivados de tiofeno
TWI404706B (zh) * 2006-01-11 2013-08-11 Actelion Pharmaceuticals Ltd 新穎噻吩衍生物
AU2007209051A1 (en) * 2006-01-24 2007-08-02 Actelion Pharmaceuticals Ltd Novel pyridine derivatives
PT2069336E (pt) * 2006-09-07 2013-03-07 Actelion Pharmaceuticals Ltd Derivados de piridin-4-ilo como agentes imunomoduladores
AR061841A1 (es) * 2006-09-07 2008-09-24 Actelion Pharmaceuticals Ltd Derivados de tiofen-oxadiazoles, agonistas del receptor s1p1/edg1, composiciones farmaceuticas que los contienen y usos como agentes inmunomoduladores.
PL2069335T3 (pl) * 2006-09-08 2013-05-31 Actelion Pharmaceuticals Ltd Pochodne pirydyn-3-ylu jako środki immunomodulujące
BRPI0808789A2 (pt) * 2007-03-16 2014-08-12 Actelion Pharmaceuticals Ltd Compostos e composição farmacêutica de derivados aminopiridina e uso destes
MX2010005889A (es) * 2007-12-10 2010-06-22 Actelion Pharmaceuticals Ltd Derivados de tiofeno como agonistas de s1p1/edg1.
EP2262799B1 (de) * 2008-03-06 2012-07-04 Actelion Pharmaceuticals Ltd. Pyridinverbindungen
WO2009109872A1 (en) * 2008-03-07 2009-09-11 Actelion Pharmaceuticals Ltd Pyridin-2-yl derivatives as immunomodulating agents
PL2278960T5 (pl) 2008-03-17 2020-06-29 Actelion Pharmaceuticals Ltd. Schemat dawkowania dla selektywnego agonisty receptora sip1
US8580841B2 (en) 2008-07-23 2013-11-12 Arena Pharmaceuticals, Inc. Substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives useful in the treatment of autoimmune and inflammatory disorders
HRP20160890T1 (hr) 2008-08-27 2016-09-23 Arena Pharmaceuticals, Inc. Derivati supstituirane tricikličke kiseline kao agonisti s1p1-receptora korisni u liječenju autoimunih i upalnih poremećaja
CA2767585C (en) 2009-07-16 2017-09-26 Actelion Pharmaceuticals Ltd Pyridin-4-yl derivatives
JP5856980B2 (ja) 2010-01-27 2016-02-10 アリーナ ファーマシューティカルズ, インコーポレイテッド (R)−2−(7−(4−シクロペンチル−3−(トリフルオロメチル)ベンジルオキシ)−1,2,3,4−テトラヒドロシクロペンタ[b]インドール−3−イル)酢酸およびその塩の調製のためのプロセス
CN105503882B (zh) 2010-03-03 2019-07-05 艾尼纳制药公司 制备s1p1受体调节剂及其晶体形式的方法
MA34910B1 (fr) 2011-01-19 2014-02-01 Actelion Pharmaceuticals Ltd Dérivés de 2-methoxy-pyridin-4-yl
SMT202000298T1 (it) 2012-08-17 2020-07-08 Actelion Pharmaceuticals Ltd Processo per la produzione di (2z,5z)-5-(3-cloro-4((r)-2,3-diidrossipropossi) benziliden)-2-(propilimmino)-3-(o-tolil)tiazolidin-4-one e intermedio usato in detto processo
US20140235613A1 (en) * 2013-02-20 2014-08-21 Allergan, Inc. Substituted diaryl azetidine derivatives as sphingosine receptor modulators
PL3242666T3 (pl) 2015-01-06 2025-02-17 Arena Pharmaceuticals, Inc. Związek do zastosowania w leczeniu dolegliwości związanych z receptorem s1p1
PH12017502097B1 (en) 2015-05-20 2023-05-05 Idorsia Pharmaceuticals Ltd Crystalline form of the compound (s)-3-{4-[5-(2-cyclopentyl-6-methoxy-pyridin-4-yl)-[1,2,4]oxadiazol-3-yl]-2-ethyl-6-methyl-phenoxy}-propane-1,2-diol
US10111841B2 (en) 2015-06-19 2018-10-30 University Of South Florida Stabilization of alcohol intoxication-induced cardiovascular instability
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MX2019009841A (es) 2017-02-16 2020-01-30 Arena Pharm Inc Compuestos y metodos para el tratamiento de la colangitis biliar primaria.
MX2019009843A (es) 2017-02-16 2020-01-30 Arena Pharm Inc Compuestos y metodos para el tratamiento de la enfermedad inflamatoria intestinal con manifestaciones extraintestinales.
CA3102136A1 (en) 2018-06-06 2019-12-12 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
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WO2006010379A1 (en) * 2004-07-29 2006-02-02 Actelion Pharmaceuticals Ltd. Novel thiophene derivatives as immunosuppressive agents
CA2602474C (en) * 2005-03-23 2014-06-10 Actelion Pharmaceuticals Ltd Hydrogenated benzo (c) thiophene derivatives as immunomodulators
US7605269B2 (en) * 2005-03-23 2009-10-20 Actelion Pharmaceuticals Ltd. Thiophene derivatives as Sphingosine-1-phosphate-1 receptor agonists
US7951794B2 (en) 2005-06-24 2011-05-31 Actelion Pharmaceuticals Ltd. Thiophene derivatives
AR057894A1 (es) 2005-11-23 2007-12-26 Actelion Pharmaceuticals Ltd Derivados de tiofeno
AU2007209051A1 (en) 2006-01-24 2007-08-02 Actelion Pharmaceuticals Ltd Novel pyridine derivatives

Also Published As

Publication number Publication date
TW200716552A (en) 2007-05-01
ES2370791T3 (es) 2011-12-22
WO2006100635A2 (en) 2006-09-28
JP5063581B2 (ja) 2012-10-31
JP2008535815A (ja) 2008-09-04
US20080194670A1 (en) 2008-08-14
CN101180050A (zh) 2008-05-14
US7846964B2 (en) 2010-12-07
MX2007011669A (es) 2007-11-15
ZA200709086B (en) 2008-12-31
EP1863475B1 (de) 2011-09-07
CA2602478A1 (en) 2006-09-28
NO20075297L (no) 2007-12-27
AR053449A1 (es) 2007-05-09
WO2006100635A3 (en) 2007-01-18
AU2006226022A1 (en) 2006-09-28
RU2007138878A (ru) 2009-04-27
IL186149A0 (en) 2008-01-20
KR20080002850A (ko) 2008-01-04
EP1863475A2 (de) 2007-12-12
BRPI0609665A2 (pt) 2010-04-20
CN101180050B (zh) 2011-07-27

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