AR093339A1 - Analogos de spliceostatina y metodos para su preparacion - Google Patents
Analogos de spliceostatina y metodos para su preparacionInfo
- Publication number
- AR093339A1 AR093339A1 ARP130104017A ARP130104017A AR093339A1 AR 093339 A1 AR093339 A1 AR 093339A1 AR P130104017 A ARP130104017 A AR P130104017A AR P130104017 A ARP130104017 A AR P130104017A AR 093339 A1 AR093339 A1 AR 093339A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- independently selected
- nrr
- group
- hydrogen
- Prior art date
Links
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 4
- 150000002431 hydrogen Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 125000005915 C6-C14 aryl group Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000001118 alkylidene group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 231100000433 cytotoxic Toxicity 0.000 abstract 1
- 230000001472 cytotoxic effect Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 229940127121 immunoconjugate Drugs 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
Classifications
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- A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
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- A61K47/6835—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6851—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
- A61K47/6855—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from breast cancer cell
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- A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
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- 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
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/453—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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- A61K47/68—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
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- A61K47/6835—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
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- A61K47/68—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no 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
- C07D309/10—Oxygen atoms
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no 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
- C07D309/14—Nitrogen atoms not forming part of a nitro radical
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/14—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 three or more hetero rings
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- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/10—Spiro-condensed systems
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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
- C07D405/12—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 linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
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- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
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- Engineering & Computer Science (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Mycology (AREA)
- Microbiology (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pyrane Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
La presente se refiere a análogos de spliceostatina citotóxicos y derivados, a sus conjugados farmacológicos de anticuerpos y a métodos para usarlos para tratar enfermedades médicas que incluyen cáncer. Reivindicación 1: Un compuesto de la fórmula (1), en donde: una línea de puntos representa un enlace opcional; cada X¹ está seleccionado, de modo independiente, del grupo que consiste en: -O-, -S- y -NR-; cada X² está seleccionado, de modo independiente, del grupo que consiste en: -O-, -S- y -NR-; R¹ está seleccionado del grupo que consiste en: -R, -OR, -OCOR¹³, -OCONR¹⁴R¹⁵, -OCON(R¹⁴)NR(R¹⁵), =O (doble enlace con oxígeno) y -NR¹⁴R¹⁵; R² y R³ están seleccionados, de modo independiente, del grupo que consiste en: hidrógeno y alquilo C₁₋₆; R⁴ y R⁵ están seleccionados, de modo independiente, del grupo que consiste en: hidrógeno, -OR, -NR¹⁴R¹⁵ y oxo; R⁶ y R⁷ están seleccionados, de modo independiente, del grupo que consiste en: hidrógeno, halógeno, hidroxilo y alquilo C₁₋₆ opcionalmente sustituido con 1 - 3 sustituyentes seleccionados, de modo independiente, de hidroxilo y halógeno, R⁶ y R⁷ forman, junto con el átomo de carbono al que están ligados, un alquilideno C₂₋₅ opcionalmente sustituido con 1 - 3 sustituyentes seleccionados, de modo independiente, de R, R⁶ y R⁷ son juntos oxo o R⁶ y R⁷ forman, junto con el átomo de carbono al que están ligados, un resto de heterocicloalquilo de 3 a 5 miembros que comprende 1 ó 2 heteroátomos seleccionados, de modo independiente, del grupo que consiste en oxígeno, nitrógeno y azufre, en donde dicho resto de heterocicloalquilo puede estar opcionalmente sustituido con uno a tres sustituyentes seleccionados, de modo independiente, de R; R⁸ es hidrógeno, alquilo C₁₋₆ u -OR; R⁹ está seleccionado, de modo independiente, de hidrógeno, -alquilo C₁₋₆, -(C(R)₂)ₘ-C(O)OR, -(C(R)₂)ₘ-C(O)NR¹⁴R¹⁵, -(C(R)₂)ₘ-NR¹⁴R¹⁵, -(C(R)₂)ₘ-N(R)COR¹³, -(C(R)₂)ₘ-C(O)-SR, -(C(R)₂)ₘ-C(O)NR¹⁴N(R)R¹⁵, -(C(R)₂)ₘ-NR-C(O)-NR¹⁴R¹⁵ y -(C(R)₂)ₘ-NR¹⁴N(R)R¹⁵; R¹³ está seleccionado del grupo que consiste en hidrógeno, alquilo C₁₋₆, carbociclilo C₃₋₈, heterociclilo C₃₋₈, alquil C₁₋₆-arilo C₆₋₁₄, alquil C₁₋₆-heteroarilo C₅₋₁₄, en donde R¹³ está opcionalmente sustituido con -NRR o -SO₂NRR; cada R¹⁴ y R¹⁵ está seleccionado, de modo independiente, del grupo que consiste en: hidrógeno, hidroxilo, -NRR, -NRNR₂, -carbociclilo C₃₋₁₀, -alquilen C₁₋₆-carbociclilo C₃₋₁₀, -heterociclilo C₃₋₁₀, -alquilen C₁₋₆-heterociclilo C₃₋₁₀, -(CH₂CH₂O)₁₋₆CH₂CH₂C(O)OR, -(CH₂CH₂O)₁₋₆CH₂CH₂NRR, -alquilo C₁₋₆, arilo C₆₋₁₄, -alquilen C₁₋₆-arilo C₆₋₁₄ y -heteroarilo C₅₋₁₄; o R¹⁴ y R¹⁵, junto con el átomo o los átomos a los que están unidos, forman un anillo heterociclilo C₃₋₁₀, en donde R¹⁴, R¹⁵ o ambos o un anillo formado con R¹⁴ y R¹⁵, están opcionalmente sustituidos con -(C(R)₂)ₘ-R¹⁸ donde cada R¹⁸ está seleccionado, de modo independiente, de (i) -NRR, (ii) -C(NRR)(C(O)OR), (iii) -S-R, (iv) arilo o heteroarilo opcionalmente sustituido con uno o varios de halógeno, -CF₃, -C(R)₂)ₘ-NRR o -(C(R)₂)ₘ-SO₂NRR, (v) -SO₂R, (vi) -S-S-alquil C₁₋₆-C(O)OR, (vii) -SO₂NRR, (viii) -C(O)NRR, (ix) -C(O)OR, (x) -cicloalquilo C₄₋₆ opcionalmente sustituido con -NRR, -SO₂NRR o -NR-C(O)(CH₂)₀₋₆NRR, (xi) -R, (xii) -OR, (xiii) -N(R)NRR, (xiv) -C(O)N(R)NRR, -(C(R)₂)ₘ-O-NRR y -S-S-alquil C₁₋₆-NRR; cada R está seleccionado, de modo independiente, del grupo que consiste en: hidrógeno y -alquilo C₁₋₆; y cada m es, de modo independiente, 0, 1, 2 ó 3; o una de sus sales farmacéuticamente aceptables.
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