AR037748A1 - Glicinamidas como inhibidores del factor xa - Google Patents

Glicinamidas como inhibidores del factor xa

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Publication number
AR037748A1
AR037748A1 ARP020104701A ARP020104701A AR037748A1 AR 037748 A1 AR037748 A1 AR 037748A1 AR P020104701 A ARP020104701 A AR P020104701A AR P020104701 A ARP020104701 A AR P020104701A AR 037748 A1 AR037748 A1 AR 037748A1
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Argentina
Prior art keywords
cr3r3a
cr3r3e
substituted
ring
alkyl
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ARP020104701A
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English (en)
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Jennifer Qiao
Donald Pinto
Wei Han
Zilun Hu
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Bristol Myers Squibb Co
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Publication of AR037748A1 publication Critical patent/AR037748A1/es

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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
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    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D401/00—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
    • C07D401/02—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
    • 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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    • 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
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    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Compuestos que son útiles como inhibidores del factor Xa y agente anticoagulante. Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula: P4-P-M-M4, o un estereoisómeros o sal aceptable para uso farmacéutico del mismo, donde: M es un carbociclo de 3-10 miembros o un heterociclo de 4-10 miembros, que consiste de: átomos de carbono y 1-3 heteroátomos seleccionados entre O, S(O)p, N, y NZ2; el anillo M está sustituido con 0-3 R1a y 0-2 grupos carbonilo, y hay 0-3 uniones dobles en el anillo; P está fusionado al anillo M y es un carbociclo de 5, 6 ó 7 miembros o un heterociclo de 5, 6 ó 7 miembros, que consiste de: átomos de carbono y 1-3 heteroátomos seleccionados entre O, S(O)p, y N; el anillo P está sustituido con 0-3 R1a y 0-2 grupos carbonilo, y hay 0-3 uniones dobles en el anillo; como alternativa, el anillo P está ausente y P4 está unido directamente al anillo M; uno de P4 y M4 es -Z-A-B y el otro -G1-G, con la condición de que P4 y M4 se unan a anillos diferentes cuando está presente el anillo P; G es un grupo de fórmula (1) ó (2); el anillo D, incluyendo los dos átomos del anillo E al cual está unido, es un anillo de 5-6 miembros que consiste de: átomos de carbono y 0-2 heteroátomos seleccionados del grupo formado por N, O, y S(O)p; el anillo D está sustituido con 0-2 R y hay 0-3 uniones dobles en el anillo; E se selecciona entre fenilo, piridilo, pirimidilo, pirazinilo, y piridazinilo, y está sustituido con 1-2 R; como alternativa, el anillo D está ausente y el anillo E se selecciona entre fenilo, piridilo, pirimidilo, pirazinilo, piridazinlo, pirrolilo, pirazolilo, imidazolilo, isoxazolilo, oxazolilo, triazolilo, tienilo, y tiazolilo, y el anillo E está sustituido con 1-2 R; como alternativa, el anillo D está ausente y el anillo E se selecciona entre fenilo, piridilo, pirimidilo, pirazinilo, piridazinilo, pirrolilo, pirazolilo, imidazolilo, isoxazolilo, oxazolilo, triazolilo, tienilo, y tiazolilo, y el anillo E está sustituido con 1R y con un heterociclo de 5-6 miembros que consiste de: átomos de carbono y 1-4 heteroátomos seleccionados del grupo formado por N, O, y S(O)p, donde el heterociclo de 5-6 miembros está sustituido con 0-1 carbonilo y 1-2 R y tiene 0-3 uniones dobles en el anillo; R se selecciona entre H, alquilo C1-4, F, Cl, Br; I, OH, OCH3, OCH2CH3, OCH(CH3)2, OCH2CH2CH3, CN, C(=NR8)NR7R9, NHC(=NR8)NR7R9, ONHC(=NR8)NR7R9, NR8CH(=NR7), NH2, NH(alquilo C1-3), N(alquil C1-3)2, C(=NH)NH2, CH2NH2, CH2NH(alquilo C1-3), CH2N(alquil C1-3)2, CH2CH2NH2, CH2CH2NH(alquilo C1-3), CH2CH2N(alquil C1-3)2, (CR8R9)tC(O)H, (CR8R9)tC(O)R2c, (CR8R9)tNR7R8, (CR8R9)tC(O)NR7R8, (CR8R9)tNR7C(O)R7, (CR8R9)tOR3, (CR8R9)tS(O)pNR7R8, (CR8R9)tNR7S(O)pR7, (CR8R9)tSR3, (CR8R9)tS(O)R3, (CR8R9)tS(O)2R3, y OCF3; como alternativa, cuando 2 grupos R están unidos a átomos adyacentes, se combinan para formar metilendioxi o etilendioxi; A se selecciona entre: carbociclo C3-10 sustituido con 0-2 R4, y heterociclo de 5-12 miembros que consiste de: átomos de carbono y 1-4 heteroátomos seleccionados del grupo formado por N, O, y S(O)p y sustituidos con 0-2 R4; B se selecciona entre N(B1)C(O)C(R3R3g)R3, N(B1)C(O)C(R3R3g)OR3, N(B1)C(O)C(R3R3g)NB2B3, N(B1)C(O) C(R3R3g)C(R3R3g)NB2B3, N(B1)C(O)C(R3R3g)C(R3R3g)C(R3R3g)NB2B3, y N(B1)C(O)C(R3R3g)C(R3R3g)C(R3R3g)C(R3R3g)NB2B3, con la condición de que Z y B se unan a diferentes átomos en A; B1 se selecciona entre H, CH3, CH2CH3, CH2CH2CH3, CH(CH3)2, CH2CH2CH2CH3, CH2CH(CH3)2, CH(CH3)CH2CH3, C(CH3)3, -(CH2)0-2-carbociclo C3-7 sustituido con 0-2 R4b, y -(CH2)0-2-heterociclo de 5-6 miembros que consiste de: átomos de carbono y 1-4 heteroátomos seleccionados del grupo formado por N, O, y S(O)p y sustituidos con 0-2 R4b; B2 se selecciona entre H, alquilo C1-6 sustituido con 0-2 R4c, C(O)R2e, C(O)OR2d, C(O)NR2dR2d, C(O)NH(CH2)2NR2dR2d, SO2NR2dR2d, C(O)NHSO2-alquilo C1-4, y S(O)pR5a; B3 se selecciona entre H, alquilo C1-6 sustituido con 0-1 R4c, -(CH2)0-1-carbociclo de 3-8 miembros sustituido con 0-2 R5, y un -(CH2)0-1-heterociclo de 3 a 8 miembros que consiste de: átomos de carbono y 1-4 heteroátomos seleccionados del grupo formado por N, O, y S(O)p y sustituidos con 0-2 R5; como alternativa, NB2B3 es un heterociclo de 3 a 8 miembros que consiste de: los N mostrados, átomos de carbono, y 0-3 heteroátomos adicionales seleccionados del grupo formado por N, O, y S(O)p y sustituidos con 0-2 R5; G1 está ausente o se selecciona entre (CR3R3a)1-5, (CR3R3a)0-2CR3=CR3(CR3R3a)0-2, (CR3R3a)0-2CsC(CR3R3a)0-2, (CR3R3a)uC(O)(CR3R3a)w, (CR3R3a)uC(O)O(CR3R3a)w, (CR3R3a)uOC(O)(CR3R3a)w, (CR3R3a)uO(CR3R3a)w, (CR3R3a)uN3b(CR3R3a)w, (CR3R3a)uC(O)N3b(CR3R3a)w, (CR3R3a)uN3bC(O)(CR3R3a)w, (CR3R3a)uOC(O)N3b(CR3R3a)w, (CR3R3a)uN3bC(O)O(CR3R3a)w, (CR3R3a)uN3bC(O)N3b(CR3R3a)w, (CR3R3a)uN3bC(S)N3b(CR3R3a)w, (CR3R3a)uS(CR3R3a)w, (CR3R3a)uS(O)(CR3R3a)w, (CR3R3a)uS(O)2(CR3R3a)w, (CR3R3a)uS(O)N3b(CR3R3a)w, (CR3R3a)uN3bS(O)2(CR3R3a)w, (CR3R3a)uS(O)2N3b(CR3R3a)w, (CR3R3a)uN3bS(O)2N3b(CR3R3a)w, (CR3R3a)uNR3e(CR3R3a)w, (CR3R3a)uC(O)(CR3R3a)uC(O)(CR3R3a)w, (CR3R3a)uNR3b(CR3R3a)uC(O)NR3b(CR3R3a)w, (CR3R3a)uNR3bC(O) (CR3R3a)uC(O)(CR3R3a)w, (CR3R3a)uC(O)(CR3R3a)uC(O)NR3b(CR3R3a)w, (CR3R3a)uNR3bC(O)(CR3R3a)uC(O)NR3b(CR3R3a)w, (CR3R3a)uS(O)NR3bC(O)(CR3R3a)w, (CR3R3a)uC(O)NR3bS(O)2(CR3R3a)w, (CR3R3a)uS(O)2NR3bC(O)NR3b(CR3R3a)w, donde u + w totalizan 0, 1, 2, 3, ó 4 , con la condición de que G1 no forme un enlace N-S, NCH2N, NCH2O, o NCH2S con ninguno de los grupos al cual está unido; Z se selecciona entre un enlace, -(CR3R3e)1-4-, (CR3R3e)qO(CR3R3e)q1, (CR3R3e)qNR3b(CR3R3e)q1, (CR3R3e)qC(O)(CR3R3e)q1, (CR3R3e)qC(O)O(CR3R3e)q1, (CR3R3e)qOC(O)(CR3R3e)q1, (CR3R3e)qC(O)NR3b(CR3R3e)q1, (CR3R3e)qNR3bC(O)(CR3R3e)q1, (CR3R3e)qOC(O)O(CR3R3e)q1, (CR3R3e)qOC(O)NR3b(CR3R3e)q1, (CR3R3e)qNR3bC(O)O(CR3R3e)q1, (CR3R3e)qNR3bC(O)NR3b(CR3R3e)q1, (CR3R3e)qC(O)(CR3R3e)qC(O) (CR3R3e)q1, (CR3R3e)qNR3b(CR3R3e)qC(O)NR3b(CR3R3e)q1, (CR3R3e)qNR3bC(O)(CR3R3e)qC(O)(CR3R3e)q1, (CR3R3e)qC(O)(CR3R3e)qC(O)NR3b(CR3R3e)q1, (CR3R3e)qNR3bC(O)(CR3R3e)qC(O)NR3b(CR3R3e)q1, (CR3R3e)qS(CR3R3e)q1, (CR3R3e)qS(O)(CR3R3e)q1, (CR3R3e)qS(O)2(CR3R3e)q1, (CR3R3e)qSO2NR3b(CR3R3e)q1, (CR3R3e)qNR3bSO2(CR3R3e)q1, (CR3R3e)qS(O)NR3bC(O)(CR3R3e)q1, (CR3R3e)qC(O)NR3bS(O)2(CR3R3e)q1, y (CR3R3e)qNR3bSO2NR3b(CR3R3e)q1, donde q + q1 totalizan 0, 1, 2, 3, ó 4, con la condición de que Z no forme un enlace N-S, NCH2N, NCH2O, o NCH2S con ninguno de los grupos al cual está unido; Z2 se selecciona entre H, S(O)2NHR3b, C(O)R3b, C(O)NHR3b, C(O)OR3f, S(O)R3f, S(O)2R3f, alquilo C1-6 sustituido con 0-2 R1a, alquenilo C2-6 sustituido con 0-2 R1a, alquinilo C2-6 sustituido con 0-2 R1a, -(alquil C0-4)-cicloalquilo sustituido con 0-3 R1a, -(alquil C0-4)-heterociclo sustituido con 0-3 R1a, -(alquil C0-4)-arilo sustituido con 0-3 R1a, y, -(alquil C0-4)-heteroarilo sustituido con 0-3 R1a; R1a, en cada caso, se selecciona entre H, -(CR3R3a)r-R1b, -(CR3R3a)r-CR3R1bR1b, -(CR3R3a)r-O-(CR3R3a)r-R1b, -(CR3R3a)r-NR2-(CR3R3a)r-R1b, -(CR3R3a)r-S(O)p-(CR3R3a)r-R1b, -(CR3R3a)r-CO2-(CR3R3a)r-R1b, -(CR3R3a)r-C(O)NR2-(CR3R3a)r-R1b, -(CR3R3a)r-C(O)-(CR3R3a)r-R1b, -alquenilen C2-6-R1b, -alquinilen C2-6-R1b, y -(CR3R3a)r-C(=NR1b)NR3R1b, con la condición de que R1a forme un enlace que no sea N-halo, N-S, O-O, o N-CN; como alternativa, cuando dos grupos R1a están unidos a átomos adyacentes o al mismo átomo de carbono, junto con los átomos a los cuales están unidos, forman un anillo de 5-7 miembros que consiste de: átomos de carbono y 0-2 heteroátomos seleccionados del grupo formado por N, O, y S(O)p, y este anillo está sustituido con 0-2 R4b y comprende: 0-3 uniones dobles; R1b se selecciona entre H, alquilo C1-3, F, Cl, Br, I, -CN, -NO2, -CHO, (CF2)rCF3, (CR3R3a)rOR2, NR2R2a, C(O)R2b, CO2R2b, OC(O)R2, CH(CH2OR2)2, (CF2)rCO2R2a, S(O)pR2b, NR2(CH2)rOR2, C(=NR2c)NR2R2a, NR2C(O)R2b, NR2C(O)NR2R2a, NR2C(O)2R2a, OC(O)NR2R2a, C(O)NR2R2a, C(O)NR2(CH2)rOR2, SO2NR2R2a, NR2SO2R2, C(O)NR2SO2R2, carbociclo C3-6 sustituido con 0-2 R4b, y heterociclo de 5-10 miembros sustituido con 0-2 R4b y que consiste de átomos de carbono y entre 1 y 4 heteroátomos seleccionados del grupo formado por N, O, y S(O)p, con la condición de que R1b forme un enlace que no sea O-O, N-halo, N-S, o N-CN y con la condición de que S(O)pR2 forme algo distinto de S(O)2H o S(O)H; R2, en cada caso, se selecciona entre H, CF3, alquilo C1-6, bencilo, -(CH2)r-carbociclo C3-10 sustituido con 0-2 R4b, y -(CH2)r-heterociclo de 5-10 miembros que consiste de: átomos de carbono y 1-4 heteroátomos seleccionados del grupo formado por N, O, y S(O)p y sustituidos con 0-2 R4b; R2a, en cada caso, se selecciona entre H, CF3, alquilo C1-6, bencilo, -(CH2)r-carbociclo C3-10 sustituido con 0-2 R4b, y -(CH2)r- heterociclo de 5-10 miembros que consiste de: átomos de carbono y 1-4 heteroátomos seleccionados del grupo formado por N, O, y S(O)p y sustituidos con 0-2 R4b; como alternativa, R2 y R2a, junto con el átomo al cual están unidos, se combinan para formar un anillo saturado, parcialmente saturado o insaturado de 5 ó 6 miembros sustituidos con 0-2 R4b y que consiste de: 0-1 heteroátomos adicionales seleccionados del grupo formado por N, O, y S(O)p; R2b, en cada caso, se selecciona entre CF3, alcoxi C1-4, alquilo C1-6 sustituido con 0-2 R4b, -(CH2)r-carbociclo C3-10 sustituido con 0-2 R4b, y -(CH2)r- heterociclo de 5-10 miembros que consiste de: átomos de carbono y 1-4 heteroátomos seleccionados del grupo formado por N, O, y S(O)p y sustituidos con 0-2 R4b; R2c, en cada caso, se selecciona entre CF3, OH, alcoxi C1-4, alquilo C1-6, -(CH2)r-carbociclo C3-10 sustituido con 0-2 R4b, y -(CH2)r-heterociclo de 5-10 miembros que contiene entre 1 y 4 heteroátomos seleccionados del grupo formado por N, O, y S(O)p y sustituidos con 0-2 R4b; R2d, en cada caso, se selecciona entre H, R4c, alquilo C1-6 sustituido con 0-2 R4c, -(CR3R3a)r-carbociclo C3-10 sustituido con 0-2 R4c, y -(CR3R3a)r-heterociclo de 5-10 miembros que consiste de: átomos de carbono y 1-4 heteroátomos seleccionados del grupo
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