AR108671A1 - IMIDODICARBONIMIDIC DIAMIDE ANALOGS - Google Patents

IMIDODICARBONIMIDIC DIAMIDE ANALOGS

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Publication number
AR108671A1
AR108671A1 ARP170101515A ARP170101515A AR108671A1 AR 108671 A1 AR108671 A1 AR 108671A1 AR P170101515 A ARP170101515 A AR P170101515A AR P170101515 A ARP170101515 A AR P170101515A AR 108671 A1 AR108671 A1 AR 108671A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
independently
alkyl
heterocycloalkyl
nr5r6
Prior art date
Application number
ARP170101515A
Other languages
Spanish (es)
Original Assignee
Enlibrium 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 Enlibrium Inc filed Critical Enlibrium Inc
Publication of AR108671A1 publication Critical patent/AR108671A1/en

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    • 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
    • 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
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms

Abstract

La presente solicitud está dirigida a compuestos de diamida imidodicarbonimidica, y sus sales, solvatos o estereoisómeros farmacéuticamente aceptables. También proporciona composiciones y el uso de tales composiciones en métodos para tratar el cáncer, la diabetes o el síndrome de ovario poliquístico. Reivindicación 1: Un compuesto que tiene la estructura de fórmula (1) donde: cada R¹ es independientemente halógeno, -CN, -NO₂, -OR⁴, -NR⁴R⁴, alquilo C₁₋₆, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, heterocicloalquilo C₁₋₆ opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, -C(O)R³, -OC(O)R³, -CO₂R⁴, -N(R⁴)C(O)R³, -C(O)NR⁵R⁶, -N(R⁴)C(O)NR⁵R⁶, -S(O)₂R³, -N(R⁴)S(O)₂R³, o -S(O)₂NR⁵R⁶; cada R² es independientemente alquilo C₁₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, heterocicloalquilo C₁₋₆ opcionalmente sustituido, arilo opcionalmente sustituido, o heteroarilo opcionalmente sustituido; cada R³ es independientemente alquilo C₁₋₆; cada R⁴ es independientemente H o alquilo C₁₋₆; cada R⁵ y cada R⁶ son independientemente H o alquilo C₁₋₆; o R⁵ y R⁶ junto con el átomo de nitrógeno al cual están unidos forman un heterocicloalquilo C₁₋₆ opcionalmente sustituido; p es 0, 1, 2, 3, 4 ó 5; y q es 0, 1, 2, 3 ó 4; o una sal, un solvato o un estereoisómero farmacéuticamente aceptable de este. Reivindicación 18: Un compuesto de fórmula (2) donde: cada R¹ es independientemente halógeno, -CN, -NO₂, -OR⁴, -NR⁴R⁴, alquilo C₁₋₆, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, heterocicloalquilo C₁₋₆ opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, -C(O)R³, -OC(O)R³, -CO₂R⁴, -N(R⁴)C(O)R³, -C(O)NR⁵R⁶, -N(R⁴)C(O)NR⁵R⁶, -S(O)₂R³, -N(R⁴)S(O)₂R³, o -S(O)₂NR⁵R⁶; cada R² es independientemente alquilo C₁₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, heterocicloalquilo C₁₋₆ opcionalmente sustituido, arilo opcionalmente sustituido, o heteroarilo opcionalmente sustituido; cada R³ es independientemente alquilo C₁₋₆; cada R⁴ es independientemente H o alquilo C₁₋₆; cada R⁵ y cada R⁶ son independientemente H o alquilo C₁₋₆; o R⁵ y R⁶ junto con el átomo de nitrógeno al cual están unidos forman un heterocicloalquilo C₁₋₆ opcionalmente sustituido; p es 1, 2, 3, 4 ó 5; y q es 0, 1, 2, 3 ó 4; o una sal, un solvato o un estereoisómero farmacéuticamente aceptable de este. Reivindicación 34: Un compuesto de fórmula (3) donde: cada R¹ es independientemente halógeno, -CN, -NO₂, -NR⁴R⁴, alquilo C₁₋₆, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, heterocicloalquilo C₁₋₆ opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, -C(O)R³, -OC(O)R³, -CO₂R⁴, -N(R⁴)C(O)R³, -C(O)NR⁵R⁶, -N(R⁴)C(O)NR⁵R⁶, -S(O)₂R³, -N(R⁴)S(O)₂R³, o -S(O)₂NR⁵R⁶; cada R² es independientemente alquilo C₁₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, heterocicloalquilo C₁₋₆ opcionalmente sustituido, arilo opcionalmente sustituido, o heteroarilo opcionalmente sustituido; cada R³ es independientemente alquilo C₁₋₆; cada R⁴ es independientemente H o alquilo C₁₋₆; cada R⁵ y cada R⁶ son independientemente H o alquilo C₁₋₆; o R⁵ y R⁶ junto con el átomo de nitrógeno al cual están unidos forman un heterocicloalquilo C₁₋₆ opcionalmente sustituido; n es 0 ó 1; p es 1, 2, 3 ó 4; y q es 0, 1, 2, 3 ó 4; o una sal, un solvato o un estereoisómero farmacéuticamente aceptable de este. Reivindicación 51: Un compuesto de fórmula (4) donde: cada R¹ es independientemente -CN, -NR⁴R⁴, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, heterocicloalquilo C₁₋₆ opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, -C(O)R³, -OC(O)R³, -CO₂R⁴, -N(R⁴)C(O)R³, -C(O)NR⁵R⁶, -N(R⁴)C(O)NR⁵R⁶, -S(O)₂R³, -N(R⁴)S(O)₂R³, o -S(O)₂NR⁵R⁶; cada R² es independientemente alquilo C₁₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, heterocicloalquilo C₁₋₆ opcionalmente sustituido, arilo opcionalmente sustituido, o heteroarilo opcionalmente sustituido; cada R³ es independientemente alquilo C₁₋₆; cada R⁴ es independientemente H o alquilo C₁₋₆; cada R⁵ y cada R⁶ son independientemente H o alquilo C₁₋₆; o R⁵ y R⁶ junto con el átomo de nitrógeno al cual están unidos forman un heterocicloalquilo C₁₋₆ opcionalmente sustituido; p es 1, 2, 3, 4 ó 5; y q es 0, 1, 2, 3 ó 4; o una sal, un solvato o un estereoisómero farmacéuticamente aceptable de este.The present application is directed to imidodicarbonimidic diamide compounds, and their pharmaceutically acceptable salts, solvates or stereoisomers. It also provides compositions and the use of such compositions in methods for treating cancer, diabetes or polycystic ovarian syndrome. Claim 1: A compound having the structure of formula (1) wherein: each R¹ is independently halogen, -CN, -NO₂, -OR⁴, -NR⁴R⁴, C alquilo alkyl, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy, heterocycloalkyl Optionally substituted C₁₋₆, optionally substituted aryl, optionally substituted heteroaryl, -C (O) R³, -OC (O) R³, -CO₂R⁴, -N (R⁴) C (O) R³, -C (O) NR⁵R⁶, - N (R⁴) C (O) NR⁵R⁶, -S (O) ₂R³, -N (R⁴) S (O) ₂R³, or -S (O) ₂NR⁵R⁶; each R² is independently C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy, optionally substituted C₁₋₆ heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; each R³ is independently C₁₋₆ alkyl; each R⁴ is independently H or C₁₋₆ alkyl; each R⁵ and each R⁶ are independently H or C₁₋₆ alkyl; or R⁵ and R⁶ together with the nitrogen atom to which they are attached form an optionally substituted C₁₋₆ heterocycloalkyl; p is 0, 1, 2, 3, 4 or 5; and q is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt, solvate or stereoisomer thereof. Claim 18: A compound of formula (2) wherein: each R¹ is independently halogen, -CN, -NO₂, -OR⁴, -NR⁴R⁴, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy, C₁₋₆ heterocycloalkyl optionally substituted, optionally substituted aryl, optionally substituted heteroaryl, -C (O) R³, -OC (O) R³, -CO₂R⁴, -N (R⁴) C (O) R³, -C (O) NR⁵R⁶, -N (R⁴) C (O) NR⁵R⁶, -S (O) ₂R³, -N (R⁴) S (O) ₂R³, or -S (O) ₂NR⁵R⁶; each R² is independently C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy, optionally substituted C₁₋₆ heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; each R³ is independently C₁₋₆ alkyl; each R⁴ is independently H or C₁₋₆ alkyl; each R⁵ and each R⁶ are independently H or C₁₋₆ alkyl; or R⁵ and R⁶ together with the nitrogen atom to which they are attached form an optionally substituted C₁₋₆ heterocycloalkyl; p is 1, 2, 3, 4 or 5; and q is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt, solvate or stereoisomer thereof. Claim 34: A compound of formula (3) wherein: each R¹ is independently halogen, -CN, -NO₂, -NR⁴R⁴, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy, optionally substituted C₁₋₆ heterocycloalkyl, aryl optionally substituted, optionally substituted heteroaryl, -C (O) R³, -OC (O) R³, -CO₂R⁴, -N (R⁴) C (O) R³, -C (O) NR⁵R⁶, -N (R⁴) C (O ) NR⁵R⁶, -S (O) ₂R³, -N (R⁴) S (O) ₂R³, or -S (O) ₂NR⁵R⁶; each R² is independently C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy, optionally substituted C₁₋₆ heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; each R³ is independently C₁₋₆ alkyl; each R⁴ is independently H or C₁₋₆ alkyl; each R⁵ and each R⁶ are independently H or C₁₋₆ alkyl; or R⁵ and R⁶ together with the nitrogen atom to which they are attached form an optionally substituted C₁₋₆ heterocycloalkyl; n is 0 or 1; p is 1, 2, 3 or 4; and q is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt, solvate or stereoisomer thereof. Claim 51: A compound of formula (4) wherein: each R¹ is independently -CN, -NR⁴R⁴, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy, optionally substituted C₁₋₆ heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, -C ( O) R³, -OC (O) R³, -CO₂R⁴, -N (R⁴) C (O) R³, -C (O) NR⁵R⁶, -N (R⁴) C (O) NR⁵R⁶, -S (O) ₂R³, -N (R⁴) S (O) ₂R³, or -S (O) ₂NR⁵R⁶; each R² is independently C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy, optionally substituted C₁₋₆ heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; each R³ is independently C₁₋₆ alkyl; each R⁴ is independently H or C₁₋₆ alkyl; each R⁵ and each R⁶ are independently H or C₁₋₆ alkyl; or R⁵ and R⁶ together with the nitrogen atom to which they are attached form an optionally substituted C₁₋₆ heterocycloalkyl; p is 1, 2, 3, 4 or 5; and q is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt, solvate or stereoisomer thereof.

ARP170101515A 2016-06-03 2017-06-02 IMIDODICARBONIMIDIC DIAMIDE ANALOGS AR108671A1 (en)

Applications Claiming Priority (1)

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US201662345708P 2016-06-03 2016-06-03

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AR (1) AR108671A1 (en)
WO (1) WO2017210580A1 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3049926A1 (en) 2017-01-17 2018-07-26 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
WO2023209611A1 (en) * 2022-04-26 2023-11-02 Beigene Switzerland Gmbh Methods of treating cancer with a b-raf inhibitor, in particular lifirafenib

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5254593A (en) * 1984-03-19 1993-10-19 The Rockefeller University Compositions containing biguanides and derivatives thereof as inhibitors of nonenzymatic cross-linking
MXPA01010489A (en) * 1999-04-15 2002-05-06 Fox Chase Cancer Ct Method for reducing a susceptibility to tumor formation induced by 3-deoxyglucosone and precursors thereof.
US7622117B2 (en) * 2002-04-17 2009-11-24 Dynamis Therapeutics, Inc. 3-deoxyglucosone and skin
US7256218B2 (en) * 2002-11-22 2007-08-14 Jacobus Pharmaceutical Company, Inc. Biguanide and dihydrotriazine derivatives
US8058312B2 (en) * 2007-01-29 2011-11-15 Hanall Biopharma Co., Ltd. N, N-dimethyl imidodicarbonimidic diamide acetate, method for producing the same and pharmaceutical compositions comprising the same
US8796338B2 (en) * 2011-01-07 2014-08-05 Elcelyx Therapeutics, Inc Biguanide compositions and methods of treating metabolic disorders
US9480663B2 (en) * 2011-01-07 2016-11-01 Elcelyx Therapeutics, Inc. Biguanide compositions and methods of treating metabolic disorders
KR101424667B1 (en) * 2011-08-08 2014-08-04 한올바이오파마주식회사 N1-cyclic amine-n2-substituted biguanide derivatives, methods of preparing the same and pharmaceutical composition comprising the same

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