AR096645A1 - COMBINATIONS OF BENZOPIRANO COMPOUNDS, COMPOSITIONS AND USES OF THESE - Google Patents

COMBINATIONS OF BENZOPIRANO COMPOUNDS, COMPOSITIONS AND USES OF THESE

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Publication number
AR096645A1
AR096645A1 ARP140102308A ARP140102308A AR096645A1 AR 096645 A1 AR096645 A1 AR 096645A1 AR P140102308 A ARP140102308 A AR P140102308A AR P140102308 A ARP140102308 A AR P140102308A AR 096645 A1 AR096645 A1 AR 096645A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
orc1
inhibitor
administration
Prior art date
Application number
ARP140102308A
Other languages
Spanish (es)
Original Assignee
Olema Pharmaceuticals Inc
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 Olema Pharmaceuticals Inc filed Critical Olema Pharmaceuticals Inc
Publication of AR096645A1 publication Critical patent/AR096645A1/en

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Classifications

    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • A61K31/495—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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535—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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Reivindicación 1: Un método para tratar un trastorno modulado, mediado o afectado por el receptor estrogénico en un sujeto, caracterizado porque comprende la administración al sujeto de un compuesto, que es seleccionado del grupo de fórmulas (1), en donde R¹ y R² son independientemente: (i) OH u OR⁹, (ii) en donde R⁹ se selecciona independientemente de H, halógeno (Cl, Br, I o F), aminoácido natural o no natural (ligado mediante OC(O)- o C(O)O- (un éster) o amino (mediante -C(O)-N- o -N-C(O)- (una ligadura de amida)), R¹⁰, -OR¹⁰ o -SR¹⁰ en donde R¹⁰ es -C(=O)RC¹, -C(=O)ORC¹, -C(=O)SRC¹, -C(=O)N(RC¹)₂; o polietilenglicol, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, carbociclilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, arilo sustituido o no sustituido o heteroarilo sustituido o no sustituido; -S(=O)₂RC¹, -S(=O)₂ORC¹, -S(=O)RC¹,-S(=O)ORC¹, -P(=O)₂RC¹, -P(=O)₂ORC¹, -P(=O)(ORC¹)₂, -P(=O)(RC¹)₂ o -P(Rᶜ¹)(ORC¹); u oxígeno unido a un grupo protector de oxígeno (para producir OH en la administración), azufre unido a un grupo protector de azufre (para producir SH o un disulfuro en la administración) o nitrógeno unido a un grupo protector de nitrógeno (para producir -NH- en la administración) y RC¹ se puede seleccionar independientemente de hidrógeno, polietilenglicol, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, carbociclilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, arilo sustituido o no sustituido o heteroarilo sustituido o no sustituido, o dos grupos RC¹ que se unen para formar un anillo heterocíclico sustituido o no sustituido; o una sal aceptable desde el punto de vista farmacéutico, un solvato, un hidrato, un profármaco, un estereoisómero, un tautómero o un óxido N de aquel, en combinación con un agente seleccionado del grupo que consiste en un inhibidor de mTOR, un inhibidor de CDK 4/6, un inhibidor de la quinasa PI3, un taxano, un antimetabolito y un antibiótico antineoplásico. Reivindicación 15: El método de acuerdo con la reivindicación 14, caracterizado porque el inhibidor de CDK 4/6 es PD-0332991, LY2835219 o LEE011. Reivindicación 20: El método de acuerdo con la reivindicación 18, caracterizado porque el inhibidor de mTOR es rapamycin, everolimus, temsirolimus, AP23573, AZD8055, WYE-354, WYE-600, WYE-687 o Pp121. Reivindicación 22: El método de acuerdo con la reivindicación 21, caracterizado porque el inhibidor de la quinasa PI3 es BKM-120, XL-147, RG-7321, CH-5132799 y BAY-80-6946. Reivindicación 25: El método de acuerdo con la reivindicación 24, caracterizado porque el taxano es paclitaxel o docetaxel. Reivindicación 27: El método de acuerdo con la reivindicación 26, caracterizado porque el antimetabolito es 5-flúorouracilo. Reivindicación 29: El método de acuerdo con la reivindicación 28, caracterizado porque el antibiótico antineoplásico es doxorubicina.Claim 1: A method for treating a disorder modulated, mediated or affected by the estrogenic receptor in a subject, characterized in that it comprises administration to the subject of a compound, which is selected from the group of formulas (1), wherein R¹ and R² are independently: (i) OH or OR⁹, (ii) wherein R⁹ is independently selected from H, halogen (Cl, Br, I or F), natural or unnatural amino acid (linked by OC (O) - or C (O) O- (an ester) or amino (by -C (O) -N- or -NC (O) - (an amide ligation)), R¹⁰, -OR¹⁰ or -SR¹⁰ where R¹⁰ is -C (= O) RC¹, -C (= O) ORC¹, -C (= O) SRC¹, -C (= O) N (RC¹) ₂; or polyethylene glycol, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl , substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl; -S (= O) ₂RC¹, -S (= O) ₂ORC¹, -S (= O) RC¹, - S (= O) ORC¹, -P (= O) ₂RC¹, -P (= O) ₂ORC¹, -P (= O) (ORC¹) ₂, -P (= O) (RC¹) ₂ or -P (Rᶜ¹) (ORC¹); or oxygen attached to an oxygen protecting group (to produce OH in administration), sulfur attached to a sulfur protecting group (to produce SH or a disulfide in administration) or nitrogen attached to a nitrogen protecting group (to produce - NH- in the administration) and RC¹ can be independently selected from hydrogen, polyethylene glycol, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted aryl or unsubstituted or substituted or unsubstituted heteroaryl, or two RC¹ groups that join to form a substituted or unsubstituted heterocyclic ring; or a pharmaceutically acceptable salt, a solvate, a hydrate, a prodrug, a stereoisomer, a tautomer or an N oxide thereof, in combination with an agent selected from the group consisting of an mTOR inhibitor, an inhibitor of CDK 4/6, a PI3 kinase inhibitor, a taxane, an antimetabolite and an antineoplastic antibiotic. Claim 15: The method according to claim 14, characterized in that the CDK 4/6 inhibitor is PD-0332991, LY2835219 or LEE011. Claim 20: The method according to claim 18, characterized in that the mTOR inhibitor is rapamycin, everolimus, temsirolimus, AP23573, AZD8055, WYE-354, WYE-600, WYE-687 or Pp121. Claim 22: The method according to claim 21, characterized in that the PI3 kinase inhibitor is BKM-120, XL-147, RG-7321, CH-5132799 and BAY-80-6946. Claim 25: The method according to claim 24, characterized in that the taxane is paclitaxel or docetaxel. Claim 27: The method according to claim 26, characterized in that the antimetabolite is 5-fluorouracil. Claim 29: The method according to claim 28, characterized in that the antineoplastic antibiotic is doxorubicin.

ARP140102308A 2013-06-19 2014-06-18 COMBINATIONS OF BENZOPIRANO COMPOUNDS, COMPOSITIONS AND USES OF THESE AR096645A1 (en)

Applications Claiming Priority (1)

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US201361837130P 2013-06-19 2013-06-19

Publications (1)

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AR096645A1 true AR096645A1 (en) 2016-01-20

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JP (1) JP2015003909A (en)
AR (1) AR096645A1 (en)
TW (1) TW201511755A (en)
WO (1) WO2014203129A1 (en)

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