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AR078536A1 - Derivados de pirazol como ligandos del receptor de estrogeno - Google Patents

Derivados de pirazol como ligandos del receptor de estrogeno

Info

Publication number
AR078536A1
AR078536A1 ARP100103629A ARP100103629A AR078536A1 AR 078536 A1 AR078536 A1 AR 078536A1 AR P100103629 A ARP100103629 A AR P100103629A AR P100103629 A ARP100103629 A AR P100103629A AR 078536 A1 AR078536 A1 AR 078536A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
benzyl
alkynyl
cycloalkyl
Prior art date
Application number
ARP100103629A
Other languages
English (en)
Original Assignee
Karobio Ab
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
Priority claimed from GB0917576A external-priority patent/GB0917576D0/en
Priority claimed from GBGB1011859.4A external-priority patent/GB201011859D0/en
Application filed by Karobio Ab filed Critical Karobio Ab
Publication of AR078536A1 publication Critical patent/AR078536A1/es

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    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/12—Heterocyclic 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/40—2,5-Pyrrolidine-diones
    • C07D207/416—2,5-Pyrrolidine-diones 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 other ring carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/14—Heterocyclic 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 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
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    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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

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Abstract

Composicion farmacéutica. Presenta además el uso de dichos compuestos en el tratamiento o profilaxis de una condicion asociada a una enfermedad o trastorno asociado a la actividad del receptor de estrogeno. Reivindicacion 1: Un compuesto de la formula (1) o un éster, amida, solvato o sal farmacéuticamente aceptable del mismo, incluyendo una sal de dicho éster o amida, y un solvato de dicho éster, amida o sal, en el cual G representa uno de los grupos: (2); R1 es seleccionado del grupo que consiste en halogeno, ciano, nitro, ORA, N(RB)2, -C(O) alquilo C1-4, -SO2alquilo C1-4, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6, trihaloalquilo C1-6, haloalquenilo C2-6, dihaloalquenilo C2-6, trihaloalquenilo C2-6, cianoalquilo C1-6, alcoxi C1-4 alquilo C1-6, cicloalquilo C3-8, cicloalquil C3-8alquilo C1-6, fenilo bencilo y heterocicliclo de 5-10 miembros, donde dicho grupo bencilo o heterociclilo está sin sustituir o dicho grupo fenilo, bencilo o heterociclilo está sustituido con 1 a 3 sustituyentes, cada uno de los cuales es independientemente seleccionado del grupo que consiste en ORA, N(RB)2, halogeno, ciano, nitro, -C(O) alquilo C1-4, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6 y trihaloalquilo C1-6; R2 es seleccionado del grupo que consiste en ciano, -CH=N-OH, -C(NH2)=N-OH, -C(O)NH2, alquil C1-6-NH2 y alquil C1-6-OH; R3 es seleccionado del grupo que consiste en hidrogeno, halogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8 , cicloalquil C3-8alquilo C1-6; haloalquilo C1-6, dihaloalquilo C1-6, trihaloalquil C1-6 o, fenilo, bencilo y heterociclilo de 5-10 miembros, donde dicho grupo bencilo o heterociclilo está sin sustituir o dicho grupo fenilo, bencilo o heterociclilo está sustituido con 1 a 3 sustituyentes, cada uno de los cuales es independientemente seleccionado del grupo que consiste en ORA, halogeno, ciano, nitro, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6 y trihaloalquilo C1-6; y donde solo uno de R1 y R3 puede ser simultáneamente un fenilo sustituido o no sustituido; cada uno de R4, R5, R6 y R7 es seleccionado, en forma independiente, del grupo constituido por hidrogeno, ORA, halogeno, ciano, nitro, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6 y trihaloalquilo C1-6; cada RA es independientemente seleccionado del grupo que consiste en hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil C3-8alquilo C1-6, fenilo, bencilo y heterociclilo de 5-10 miembros, cada uno de los cuales está opcionalmente sustituido con 1 a 3 átomos de halogeno y cada RB es independientemente seleccionado del grupo que consiste en hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil C3-8alquilo C1-6, fenilo, bencilo y heterociclilo de 5-10 miembros, cada uno de los cuales está opcionalmente sustituido con 1 a 3 átomos de halogeno.
ARP100103629A 2009-10-07 2010-10-06 Derivados de pirazol como ligandos del receptor de estrogeno AR078536A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0917576A GB0917576D0 (en) 2009-10-07 2009-10-07 Novel estrogenreceptor ligands
GBGB1011859.4A GB201011859D0 (en) 2010-07-14 2010-07-14 Novel estrogen receptor ligands

Publications (1)

Publication Number Publication Date
AR078536A1 true AR078536A1 (es) 2011-11-16

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Family Applications (2)

Application Number Title Priority Date Filing Date
ARP100103631A AR078538A1 (es) 2009-10-07 2010-10-06 Pirroles e imidazoles sustituidos como ligandos del receptor de estrogenos
ARP100103629A AR078536A1 (es) 2009-10-07 2010-10-06 Derivados de pirazol como ligandos del receptor de estrogeno

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ARP100103631A AR078538A1 (es) 2009-10-07 2010-10-06 Pirroles e imidazoles sustituidos como ligandos del receptor de estrogenos

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US (2) US8653112B2 (es)
EP (1) EP2486018B1 (es)
JP (1) JP5735518B2 (es)
CN (1) CN102648183B (es)
AR (2) AR078538A1 (es)
DK (1) DK2486018T3 (es)
ES (1) ES2737429T3 (es)
IN (1) IN2012DN02556A (es)
TW (2) TW201124409A (es)
WO (2) WO2011042477A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201113538D0 (en) 2011-08-04 2011-09-21 Karobio Ab Novel estrogen receptor ligands
EP2800745B1 (en) 2011-12-02 2020-02-12 Phenex Pharmaceuticals AG Pyrrolo carboxamides as modulators of orphan nuclear receptor rar-related orphan receptor-gamma (rory, nr1f3) activity and for the treatment of chronic inflammatory and autoimmune diseases
CN102558058B (zh) * 2012-01-19 2014-10-29 陕西理工学院 1-芳基-3-取代-5-取代氨基-4-吡唑甲酰胺类化合物及其应用
JO3215B1 (ar) 2012-08-09 2018-03-08 Phenex Pharmaceuticals Ag حلقات غير متجانسة بها 5 ذرات تحتوي على النيتروجين بها استبدال بكربوكساميد أو سلفوناميد كمعدلات لمستقبل نووي غير محمي RORy
US9944597B2 (en) 2013-09-16 2018-04-17 The Board Of Regents Of The University Of Texas System Polysubstituted pyrroles having microtubule-disrupting, cytotoxic and antitumor activities and methods of use thereof
WO2015070366A1 (en) * 2013-11-12 2015-05-21 Merck Sharp & Dohme Corp. Aryl linked imidazole and triazole derivatives and methods of use thereof for improving the pharmacokinetics of a drug
CA2932224A1 (en) 2013-12-05 2015-06-11 Karo Pharma Ab Estrogen receptor beta agonists for use in treating mesothelioma
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