WO2005014525A3 - Bi-aryl compound having immunosuppressive activity - Google Patents

Bi-aryl compound having immunosuppressive activity Download PDF

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Publication number
WO2005014525A3
WO2005014525A3 PCT/JP2004/011860 JP2004011860W WO2005014525A3 WO 2005014525 A3 WO2005014525 A3 WO 2005014525A3 JP 2004011860 W JP2004011860 W JP 2004011860W WO 2005014525 A3 WO2005014525 A3 WO 2005014525A3
Authority
WO
WIPO (PCT)
Prior art keywords
aryl compound
immunosuppressive activity
compound
aryl
lymphocytes
Prior art date
Application number
PCT/JP2004/011860
Other languages
French (fr)
Other versions
WO2005014525A2 (en
Inventor
Toshiyuki Kohara
Kunitomo Adachi
Yoshihito Tanaka
Kunio Sugahara
Ayumi Tomatsu
Masatoshi Kiuchi
Original Assignee
Mitsubishi Pharma Corp
Toshiyuki Kohara
Kunitomo Adachi
Yoshihito Tanaka
Kunio Sugahara
Ayumi Tomatsu
Masatoshi Kiuchi
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 Mitsubishi Pharma Corp, Toshiyuki Kohara, Kunitomo Adachi, Yoshihito Tanaka, Kunio Sugahara, Ayumi Tomatsu, Masatoshi Kiuchi filed Critical Mitsubishi Pharma Corp
Publication of WO2005014525A2 publication Critical patent/WO2005014525A2/en
Publication of WO2005014525A3 publication Critical patent/WO2005014525A3/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/22Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
    • C07C215/28Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/54Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C217/64Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C225/00Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
    • C07C225/02Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C225/14Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being unsaturated
    • C07C225/16Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D257/00Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04Five-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/36Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/22Radicals substituted by doubly bound hetero atoms, or by two hetero atoms other than halogen singly bound to the same carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/06Phosphorus compounds without P—C bonds
    • C07F9/08Esters of oxyacids of phosphorus
    • C07F9/09Esters of phosphoric acids
    • C07F9/094Esters of phosphoric acids with arylalkanols
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
    • C07F9/655345Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a five-membered ring

Abstract

The invention is directed to a bi-aryl compound having a unique immunomodulating activity, a process for a preparation thereof, a pharmaceutical composition containing the same, and a method of preventing or treating disorders or diseases mediated by T lymphocytes by administering the compound to a subject in need of treatment.
PCT/JP2004/011860 2003-08-12 2004-08-12 Bi-aryl compound having immunosuppressive activity WO2005014525A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US49453003P 2003-08-12 2003-08-12
US60/494,530 2003-08-12

Publications (2)

Publication Number Publication Date
WO2005014525A2 WO2005014525A2 (en) 2005-02-17
WO2005014525A3 true WO2005014525A3 (en) 2005-04-21

Family

ID=34135346

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2004/011860 WO2005014525A2 (en) 2003-08-12 2004-08-12 Bi-aryl compound having immunosuppressive activity

Country Status (2)

Country Link
TW (1) TW200505416A (en)
WO (1) WO2005014525A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8476305B2 (en) 2008-02-07 2013-07-02 Kyorin Pharmaceutical Co., Ltd. Therapeutic agent or prophylactic agent for inflammatory bowel disease comprising amino alcohol derivative as active ingredient

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CN101905023B (en) 2004-07-16 2012-07-11 杏林制药株式会社 Method of effectively using medicine and method concerning prevention of side effect
WO2006010379A1 (en) 2004-07-29 2006-02-02 Actelion Pharmaceuticals Ltd. Novel thiophene derivatives as immunosuppressive agents
JP4792400B2 (en) 2004-10-12 2011-10-12 杏林製薬株式会社 Process for producing 2-amino-2- [2- [4- (3-benzyloxyphenylthio) -2-chlorophenyl] ethyl] -1,3-propanediol hydrochloride or a hydrate thereof and production intermediate thereof
GB0504544D0 (en) * 2005-03-04 2005-04-13 Novartis Ag Organic compounds
EP1863475B1 (en) 2005-03-23 2011-09-07 Actelion Pharmaceuticals Ltd. Novel thiophene derivatives as sphingosine-1-phosphate-1 receptor agonists
JP2008546758A (en) 2005-06-24 2008-12-25 アクテリオン ファーマシューティカルズ リミテッド New thiophene derivatives
PT1926483E (en) * 2005-09-09 2011-03-03 Novartis Ag Treatment of autoimmune diseases
BRPI0617077A2 (en) 2005-10-07 2015-01-06 Kyorin Seiyaku Kk THERAPEUTIC AGENT FOR TREATMENT OF LIVER DISEASES CONTAINING 2-AMINE-1, 3-PROPANEDIOL DERIVATIVE AS ACTIVE INGREDIENT, AND METHOD FOR TREATMENT OF LIVER DISEASES
AR057894A1 (en) 2005-11-23 2007-12-26 Actelion Pharmaceuticals Ltd THIOPHEN DERIVATIVES
TWI404706B (en) * 2006-01-11 2013-08-11 Actelion Pharmaceuticals Ltd Novel thiophene derivatives
BRPI0706725A2 (en) 2006-01-24 2011-04-05 Actelion Pharmaceuticals Ltda SALT COMPOSITION OF THE SAME, PHARMACEUTICAL COMPOSITION, AND USE OF A COMPOUND
TWI389683B (en) 2006-02-06 2013-03-21 Kyorin Seiyaku Kk A therapeutic agent for an inflammatory bowel disease or an inflammatory bowel disease treatment using a 2-amino-1,3-propanediol derivative as an active ingredient
EP2058317B1 (en) 2006-08-08 2013-10-16 Kyorin Pharmaceutical Co., Ltd. Aminophosphoric acid ester derivative and s1p receptor modulator containing the same as active ingredient
CN101506145B (en) 2006-08-08 2013-05-29 杏林制药株式会社 Aminoalcohol derivative and immunosuppressant containing the same as active ingredient
AR061841A1 (en) 2006-09-07 2008-09-24 Actelion Pharmaceuticals Ltd DERIVATIVES OF THIOFEN-OXADIAZOLS, AGONISTS OF THE S1P1 / EDG1 RECEPTOR, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USES AS IMMUNOMODULATING AGENTS.
PL2069336T3 (en) 2006-09-07 2013-05-31 Idorsia Pharmaceuticals Ltd Pyridin-4-yl derivatives as immunomodulating agents
PL2069335T3 (en) 2006-09-08 2013-05-31 Actelion Pharmaceuticals Ltd Pyridin-3-yl derivatives as immunomodulating agents
JP5250556B2 (en) 2006-09-21 2013-07-31 アクテリオン ファーマシューティカルズ リミテッド Phenyl derivatives and their use as immunomodulators
JP2010521450A (en) 2007-03-16 2010-06-24 アクテリオン ファーマシューティカルズ リミテッド Amino-pyridine derivatives as S1P1 / EDG1 receptor agonists
WO2009053481A1 (en) * 2007-10-25 2009-04-30 Institut National De La Sante Et De La Recherche Medicale (Inserm) Compositions and methods for modulating nk and t cell trafficking
AU2009220893A1 (en) 2008-03-07 2009-09-11 Actelion Pharmaceuticals Ltd Novel aminomethyl benzene derivatives
PT2454255E (en) 2009-07-16 2014-01-14 Actelion Pharmaceuticals Ltd Pyridin-4-yl derivatives as s1p1/edg1 agonists
ES2548683T3 (en) 2010-04-23 2015-10-20 Bristol-Myers Squibb Company 4- (5-Isoxazolyl or 5-pyrrazolyl-1,2,4-oxadiazol-3-yl) -mandelic acid amides as sphingosine-1-phosphate receptor agonists 1
ES2548258T3 (en) 2010-09-24 2015-10-15 Bristol-Myers Squibb Company Oxadiazole compounds substituted and their use as S1P1 agonists
US8653270B2 (en) 2010-11-22 2014-02-18 Allergan, Inc. Compounds as receptor modulators with therapeutic utility
BR112013017923B1 (en) 2011-01-19 2021-08-10 Idorsia Pharmaceuticals Ltd 2-METOXY-PYRIDIN-4-IL DERIVATIVES
CN102863345A (en) * 2011-07-06 2013-01-09 中国医学科学院药物研究所 Amino propylene glycol derivative, preparation method of amino propylene glycol derivative, medicine composition of amino propylene glycol derivative and application of amino propylene glycol derivative
BR112014003878A2 (en) 2011-08-19 2017-03-21 Dsm Fine Chemicals Austria Nfg Gmbh & Co Kg synthesis of r-biphenylalaninol
CN102976989A (en) * 2012-11-26 2013-03-20 盛世泰科生物医药技术(苏州)有限公司 Method for synthesizing 2-amino-2-{2-[4-(3-benzyloxy-phenyl)-2-chloro-phenyl]-ethyl}-propane-1,3-diol hydrochloride
CN104844533B (en) * 2014-02-17 2019-04-09 中国医学科学院药物研究所 Amino-propanediol class compound, preparation method and its medical usage containing five yuan of heteroaromatics
CN104844486B (en) * 2014-02-17 2018-10-30 中国医学科学院药物研究所 Amido propylene glycol derivative, preparation method and its pharmaceutical composition and purposes
MY192358A (en) 2015-05-20 2022-08-17 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

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8476305B2 (en) 2008-02-07 2013-07-02 Kyorin Pharmaceutical Co., Ltd. Therapeutic agent or prophylactic agent for inflammatory bowel disease comprising amino alcohol derivative as active ingredient

Also Published As

Publication number Publication date
TW200505416A (en) 2005-02-16
WO2005014525A2 (en) 2005-02-17

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