AR075781A1 - Derivados de oxadiazol piridina como agonistas del receptor s1p1/edg1 y un metodo para su preparacion. - Google Patents

Derivados de oxadiazol piridina como agonistas del receptor s1p1/edg1 y un metodo para su preparacion.

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Publication number
AR075781A1
AR075781A1 ARP100100623A ARP100100623A AR075781A1 AR 075781 A1 AR075781 A1 AR 075781A1 AR P100100623 A ARP100100623 A AR P100100623A AR P100100623 A ARP100100623 A AR P100100623A AR 075781 A1 AR075781 A1 AR 075781A1
Authority
AR
Argentina
Prior art keywords
hal
denotes
nco2r3
ocf3
atoms
Prior art date
Application number
ARP100100623A
Other languages
English (en)
Original Assignee
Merck Serono Sa
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 Merck Serono Sa filed Critical Merck Serono Sa
Publication of AR075781A1 publication Critical patent/AR075781A1/es

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    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2063—Proteins, e.g. gelatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • 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

Abstract

Derivados de oxadiazol piridina, su uso como medicamentos y su uso para el tratamiento de la esclerosis multiple y otras enfermedades. Reivindicacion 1: Un compuesto de formula (1): donde: R1 denota -CO2R3, -CON(H)2-p(A)p, -N(H)(CH2)nCO2R3, -N(R3)(CH2)nCO2R3, -NH-CO-A, Hal, -CF3, -OCF3, -OH, -OA, -CN, o -NO2, -(CH2)nHet, -(CH2)sN(H)2-p(A)p, -CH(CH3)(CH2)nN(H)2-p(A)p, -CH(R3)(CH2)nN(H)2-p(A)p, -(CH2)sN(R3)(CH2)nCO2R3, -(CH2)sNH-CO-A, - (CH2)nN(R3)2, -CH(CH3)(CH2)nN(R3)CH(CH3)(CH2)nCO2R3, -CH(R3)(CH2)nN(R3)CH(R3)(CH2)nCO2R3, o cuando se halla en la posicion meta o para respecto del anillo de oxadiazol, R1 también denota -N(H)2-p(A)p o A, R2 es H, Hal, -CN, -NO2, -OH, OA, -CO2R3, -CON(H)2-p(A)p, -N(H)(CH2)nCO2R3, -NH-CO-A, -CF3, -OCF3, o cuando se halla en la posicion meta o para respecto del anillo de oxadiazol, R2 también denota -N(H)2-p(A)p o A, Ra Rb son independientemente uno del otro A, -CF3, Hal, -CH2-OR3, OR3, -OCF3, alquilo (C1-7), -(CH2)nO(CH2)nOMe o CH(CH3)OCH3. W, Y son independientemente uno del otro CH o N, Z denota Ar o Het, A es alquilo ramificado o lineal que posee 1 a 12 átomos de C, donde uno o más, con preferencia 1 a 7 átomos de H pueden estar reemplazados por Hal, OR3, CN, CO2R3 o N(R3)2 y donde uno o más, con preferencia 1 a 7 grupos CH2 no adyacentes pueden estar reemplazados por O, NR3 o S y/o por grupos -CH=CH- o -C:::C-, o denota cicloalquilo o cicloalquilalquileno que posee 3-7 átomos de C de anillo, Ar denota un anillo carbocíclico aromático, monocíclico o bicíclico que posee 6 a 14 átomos de carbono, que no está substituído o está monosustituido, disustituido o trisustituido por Hal, -CF3, -OCF3, -NO2, -CN, perfluoralquilo, A, OA, -OH, -NH2, -COH, -COOR3, -CONH2, CON(H)2-qAq, NR3(CH2)nCOA, NR3(CH2)nCOOA, - NR3(CH2)nCOR3, -N(H)2-qAq, -NHSO2A, -NHSO2-N(H)2-m(A)m, -N(H)1-qAqCOA, -N(H)1-qAqSO2-N(H)2-m(A)m, -N(H)1-qAqCON(H)2-m(A)m, -COOA, -SO2A, -SO2N(H)2-m(A)m, -SO2Het, -(CH2)nOR3, Het denota un anillo monocíclico o bicíclico, saturado, insaturado o aromático que posee 1 a 4 átomos de N, O y/o S, que no está sustituido o está monosustituido, disustituido o trisustituido por alquilo que posee 1 a 8 átomos de carbono, alcoxi que posee 1 a 8 átomos de carbono, Hal, -CF3, -OCF3, -NO2, -CN, perfluoralquilo, A, OA, -OH, -NH2, -COH, -COOR3, -CONH2, -CON(H)2-qAq, -NR3(CH2)nCOA, -NR3(CH2)nCOOA, -NR3(CH2)nCOR3, -N(H)2-qAq, -NHSO2A, -NHSO2-N(H)2-m(A)m, -N(H)1-qAqCOA, -N(H)1-qAqSO2-N(H)2-m(A)m, -N(H)1-qAqCON(H)2-m(A)m, -COOA, -SO2A, -SO2N(H)2-m(A)m, -SO2Het, -(CH2)nOR3, Hal es F, Cl, Br o I, R3 es H o A, m es 0, 1 o 2, p es 0, 1 o 2, q es 0 o 1, s es 1, 2, 3, 4 o 5, y n es 0, 1, 2, 3, 4 o 5, y sus derivados, solvatos, tautomeros, sales y estereoisomeros farmacéuticamente aceptables, que incluyen sus mezclas en todas las relaciones.
ARP100100623A 2009-03-03 2010-03-02 Derivados de oxadiazol piridina como agonistas del receptor s1p1/edg1 y un metodo para su preparacion. AR075781A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15698509P 2009-03-03 2009-03-03
EP09154174 2009-03-03

Publications (1)

Publication Number Publication Date
AR075781A1 true AR075781A1 (es) 2011-04-27

Family

ID=40886975

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100100623A AR075781A1 (es) 2009-03-03 2010-03-02 Derivados de oxadiazol piridina como agonistas del receptor s1p1/edg1 y un metodo para su preparacion.

Country Status (9)

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US (1) US8791142B2 (es)
EP (1) EP2403849B1 (es)
JP (1) JP5753104B2 (es)
AR (1) AR075781A1 (es)
AU (1) AU2010220338B2 (es)
CA (1) CA2752804C (es)
ES (1) ES2517265T3 (es)
IL (1) IL214704A (es)
WO (1) WO2010100142A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102007014224A1 (de) 2007-03-24 2008-09-25 Abiomed Europe Gmbh Blutpumpe mit Mikromotor
EP2643333B1 (en) * 2010-11-23 2016-10-12 Allergan, Inc. Novel phosphonic acids as s1p receptor modulators
EP2970236B1 (en) 2013-03-15 2017-08-30 Idorsia Pharmaceuticals Ltd Pyridin-4-yl derivatives
BR112020008457A2 (pt) 2017-11-01 2020-10-20 Bristol-Myers Squibb Company compostos bicíclicos em ponte como moduladores de receptor de farnesoide x

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR9915968A (pt) 1998-09-16 2001-08-28 Dow Agrosciences Llc Acetamidas de 2-metoxiimino- 2-(piridiniloximetil)fenila com anéis heterocìclicos de 5 elementos no anel de piridina como fungicidas
GB0108102D0 (en) 2001-03-30 2001-05-23 Pfizer Ltd Compounds
WO2004103279A2 (en) * 2003-05-15 2004-12-02 Merck & Co., Inc. 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists
US7605171B2 (en) * 2003-12-17 2009-10-20 Merck & Co., Inc. (3,4-disubstituted)propanoic carboxylates as S1P (Edg) receptor agonists
WO2006131336A1 (en) * 2005-06-08 2006-12-14 Novartis Ag POLYCYCLIC OXADIAZOLES OR I SOXAZOLES AND THEIR USE AS SlP RECEPTOR LIGANDS
CN101282936B (zh) * 2005-10-07 2012-05-16 橘生药品工业株式会社 氮化杂环化合物及包含其的药物组合物
JP4383525B2 (ja) * 2006-05-09 2009-12-16 ファイザー・プロダクツ・インク シクロアルキルアミノ酸誘導体およびその医薬組成物
JP2009269819A (ja) 2006-08-25 2009-11-19 Asahi Kasei Pharma Kk アミン化合物
PT2069336E (pt) * 2006-09-07 2013-03-07 Actelion Pharmaceuticals Ltd Derivados de piridin-4-ilo como agentes imunomoduladores
AR062684A1 (es) * 2006-09-08 2008-11-26 Actelion Pharmaceuticals Ltd Compuestos derivados de piridin-3- ilo, composicion farmaceutica que los contiene, y uso de los mismos en la preparacion de medicamentos
CN101627034B (zh) * 2007-03-16 2013-05-15 埃科特莱茵药品有限公司 氨基-吡啶衍生物作为s1p1/edg1受体激动剂

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Publication number Publication date
US8791142B2 (en) 2014-07-29
CA2752804C (en) 2017-04-04
IL214704A (en) 2017-11-30
WO2010100142A1 (en) 2010-09-10
IL214704A0 (en) 2011-11-30
EP2403849B1 (en) 2014-07-16
AU2010220338A1 (en) 2011-09-08
JP2012519204A (ja) 2012-08-23
AU2010220338B2 (en) 2016-07-21
CA2752804A1 (en) 2010-09-10
US20110306636A1 (en) 2011-12-15
ES2517265T3 (es) 2014-11-03
JP5753104B2 (ja) 2015-07-22
EP2403849A1 (en) 2012-01-11

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