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US 2009/0156599 A1Published application
Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of TRPV1
AssigneeJanssen Pharmaceutica NV
InventorsBryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
Life of this patent
Estimating the term…
Abstract
Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
Claims27
A composition of matter selected from the group consisting of:
- (a) compounds of Formula (I):
- wherein:
- R1 is —H;
- —NRaRb;
- a —C1-6alkyl, —OC1-6alkyl, —S—C1-6alkyl, or —SO2—C1-6alkyl group unsubstituted or substituted with an —OH, —OC1-4alkyl, or —NRcRd substituent;
- where Ra and Rb are each independently —H;
- —C1-6alkyl;
- a —C2-4alkyl group substituted with a —OH, —OC1-4alkyl, or —NReRf substituent;
- or a saturated monocyclic cycloalkyl, —C1alkyl-(saturated monocyclic cycloalkyl), —C1alkyl-(carbon-linked, saturated monocyclic heterocycloalkyl), benzyl, or —C1alkyl-(monocyclic heteroaryl) group, each unsubstituted or substituted with a —C1-6alkyl, —OH, —OC1-4alkyl, —NRpRq, or fluoro substituent;
- or, Ra and Rb taken together with the nitrogen of attachment in —NRaRb form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with one, two, or three moieties independently selected from the group consisting of —C1-6alkyl, —C1-2alkyl-OH, —C1-2alkyl-OC1-2alkyl, —OH, —OC1-4alkyl, —NRpRq, fluoro, —CO2H, and monocyclic cycloalkyl substituents;
- where Rc and Rd are each independently —H or —C1-6alkyl;
- or Rc and Rd taken together with the nitrogen of attachment in —NRcRd form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- Re and Rf are each independently —H or —C1-6alkyl;
- or Re and Rf taken together with their nitrogen of attachment in —NReRf form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- and
- Rp and Rq are each independently —H or —C1-6alkyl;
- or Rp and Rq taken together with the nitrogen of attachment in —NRpRq form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- R2 is:
- 1) a phenyl group unsubstituted or substituted with one, two, or three Rg substituents;
- where each Rg substituent is —C1-6alkyl, —OH, —OC1-6alkyl, —CN, —NO2, —N(Rh)Ri, —C(O)N(Rh)Ri, —C(O)C1-6alkyl, —S(O)0-2—C1-6alkyl, —SO2CF3, —SO2N(Rh)Ri, —SCF3, halo, —CF3, —OCF3, —CO2H, —CO2C1-6alkyl, —C(Rj)2—CN, —C(Rj)2—CO2C1-4alkyl, —C(Rj)2—CO2H, —C(Rj)2—CON(Rh)Ri, —C(Rj)2—CH2N(Rh)Ri, or —C(Rj)2—OH;
- or two adjacent Rg substituents taken together form —OC1-2alkylO—, —C2-6alkylO—, or —C2-6alkylN(Rh)—;
- where Rh and Ri are each independently —H or —C1-6alkyl;
- or Rh and Ri taken together with their nitrogen of attachment in —NRhRi form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- where each Rj is independently —H, —C1-6alkyl, or —CF3;
- or both Rj substituents taken together with the carbon to which they are attached form a monocyclic cycloalkyl ring;
- or
- 2) a thiadiazolyl or six-membered monocyclic heteroaryl ring, each substituted with —CF3 or tert-butyl;
- R3 is —H, —CH3, —CF3, halo, —CN, —COC1-6alkyl, —CO2H, —CO2C1-6alkyl, —C(O)N(Rk)Rl, —CH2N(Rk)Rl, —S(O)0-2—C1-6alkyl, —S—Si(C1-6alkyl)3, —SO2CF3, or —SO2N(Rk)Rl;
- or phenyl or 6-membered heteroaryl ring, each unsubstituted or substituted with —OH, —CH2N(Rk)Rl, —C(O)N(Rk)Rl, —SO2N(Rk)Rl, or —CO2H;
- where Rk and Rl are each independently —H or —C1-6alkyl;
- or Rk and Rl taken together with their nitrogen of attachment in —NRkRl form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- R4 is —H, —CF3, halo, —CN, —CO2H, —CO2C1-6alkyl, —C(O)N(Rn)Ro, —C1-4alkyl-OH, —C1-4alkyl-N(Rn)Ro, —S(O)0-2—C1-6alkyl, —SO2CF3, or -SO2N(Rn)Ro;
- where Rn and Ro are each independently —H or —C1-6alkyl;
- X is S, O, or NH;
- R5 is —H, —CH3, halo, or —CF3;
- and
- R6 and R7 are each independently —H or methyl;
- or R6 and R7 taken together with the carbon to which they are attached form a monocyclic cycloalkyl ring;
- and (b) pharmaceutically acceptable salts of the compounds of Formula (I),
- pharmaceutically acceptable prodrugs of the compounds of Formula (I), and
- pharmaceutically active metabolites of the compounds of Formula (I).
38 more elements
A pharmaceutical composition for treating a disease, disorder, or medical condition mediated by TRPV1 activity, comprising:
- (a) an effective amount of at least one agent selected from compounds of Formula (I) and pharmaceutically acceptable salts, pharmaceutically acceptable prodrugs, and pharmaceutically active metabolites of said compounds of Formula (I):
- wherein:
- R1 is —H;
- —NRaRb;
- a —C1-6alkyl, —OC1-6alkyl, —S—C1-6alkyl, or —SO2—C1-6alkyl group unsubstituted or substituted with an —OH, —OC1-4alkyl, or —NRcRd substituent;
- where Ra and Rb are each independently —H;
- —C1-6alkyl;
- a —C2-4alkyl group substituted with a —OH, —OC1-4alkyl, or —NReRf substituent;
- or a saturated monocyclic cycloalkyl, —C1alkyl-(saturated monocyclic cycloalkyl), —C1alkyl-(carbon-linked, saturated monocyclic heterocycloalkyl), benzyl, or —C1alkyl-(monocyclic heteroaryl) group, each unsubstituted or substituted with a —C1-6alkyl, —OH, —OC1-4alkyl, —NRpRq, or fluoro substituent;
- or, Ra and Rb taken together with the nitrogen of attachment in —NRaRb form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with one, two, or three moieties independently selected from the group consisting of —C1-6alkyl, —C1-2alkyl-OH, —C1-2alkyl-OC1-2alkyl, —OH, —OC1-4alkyl, —NRpRq, fluoro, —CO2H, and monocyclic cycloalkyl substituents;
- where Rc and Rd are each independently —H or —C1-6alkyl;
- or Rc and Rd taken together with the nitrogen of attachment in —NRcRd form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- Re and Rf are each independently —H or —C1-6alkyl;
- or Re and Rf taken together with their nitrogen of attachment in —NReRf form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- and
- Rp and Rq are each independently —H or —C1-6alkyl;
- Rp and Rq taken together with the nitrogen of attachment in —NRpRq form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- R2 is:
- 1) a phenyl group unsubstituted or substituted with one, two, or three Rg substituents;
- where each Rg substituent is —C1-6alkyl, —OH, —OC1-6alkyl, —CN, —NO2, —N(Rh)Ri, —C(O)N(Rh)Ri, —C(O)C1-6alkyl, —S(O)0-2—C1-6alkyl, —SO2CF3, —SO2N(Rh)Ri, —SCF3, halo, —CF3, —OCF3, —CO2H, —CO2C1-6alkyl, —C(Rj)2—CN, —C(Rj)2—CO2C1-4alkyl, —C(Rj)2—CO2H, —C(Rj)2—CON(Rh)Ri, —C(Rj)2—CH2N(Rh)Ri, or —C(Rj)2—OH;
- or two adjacent Rg substituents taken together form —OC1-2alkylO—, —C2-6alkylO—, or —C2-6alkylN(Rh)—;
- where Rh and Ri are each independently —H or —C1-6alkyl;
- or Rh and Ri taken together with their nitrogen of attachment in —NRhRi form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- where each Rj is independently —H, —C1-6alkyl, or —CF3;
- or both Rj substituents taken together with the carbon to which they are attached form a monocyclic cycloalkyl ring;
- or
- 2) a thiadiazolyl or six-membered monocyclic heteroaryl ring, each substituted with —CF3 or tert-butyl;
- R3 is —H, —CH3, —CF3, halo, —CN, —COC1-6alkyl, —CO2H, —CO2C1-6alkyl, —C(O)N(Rk)Rl, —CH2N(Rk)Rl, —S(O)0-2—C1-6alkyl, —S—Si(C1-6alkyl)3, —SO2CF3, or —SO2N(Rk)Rl;
- or a phenyl or 6-membered heteroaryl ring, each unsubstituted or substituted with —OH, —CH2N(Rk)Rl, —C(O)N(Rk)Rl, —SO2N(Rk)Rl, or —CO2H;
- where Rk and Rl are each independently —H or —C1-6alkyl;
- or Rk and Rl taken together with their nitrogen of attachment in —NRkRl form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- R4 is —H, —CF3, halo, —CN, —CO2H, —CO2C1-6alkyl, —C(O)N(Rn)Ro, —C1-4alkyl-OH, —C1-4alkyl N(Rn)Ro, —S(O)0-2—C1-6alkyl, —SO2CF3, or —SO2N(Rn)Ro;
- where Rn and Ro are each independently —H or —C1-6alkyl;
- X is S, O, or NH;
- R5 is —H, —CH3, halo, or —CF3;
- and
- R6 and R7 are each independently —H or methyl;
- or R6 and R7 taken together with the carbon to which they are attached form a monocyclic cycloalkyl ring;
- and (b) a pharmaceutically acceptable excipient.
36 more elements
A method of treating a subject suffering from or diagnosed with a disease, disorder, or condition mediated by TRPV1 activity, comprising administering to the subject an effective-amount of at least one agent selected from compounds of Formula (I) and pharmaceutically acceptable salts, pharmaceutically acceptable prodrugs, and pharmaceutically active metabolites of said compounds of Formula (I):
- wherein:
- R1is —H;
- —NRaRb;
- a —C1-6alkyl, —OC1-6alkyl, —S—C1-6alkyl, or —SO2—C1-6alkyl group;
- unsubstituted or substituted with an —OH, —OC1-4alkyl, or —NRcRd substituent;
- where Ra and Rb are each independently —H;
- —C1-6alkyl;
- a —C2-4alkyl group substituted with a —OH, —OC1-4alkyl, or —NReRf substituent;
- or a saturated monocyclic cycloalkyl, —C1alkyl-(saturated monocyclic cycloalkyl), —C1alkyl-(carbon-linked, saturated monocyclic heterocycloalkyl), benzyl, or —C1alkyl-(monocyclic heteroaryl) group, each unsubstituted or substituted with a —C1-6alkyl, —OH, —OC1-4alkyl, —NRpRq, or fluoro substituent;
- or, Ra and Rb taken together with the nitrogen of attachment in —NRaRb form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with one, two, or three moieties independently selected from the group consisting of —C1-6alkyl, —C1-2alkyl-OH, —C1-2alkyl-OC1-2alkyl, —OH, —OC1-4alkyl, —NRpRq, fluoro, —CO2H, and monocyclic cycloalkyl substituents;
- where Rc and Rd are each independently —H or —C1-6alkyl;
- or Rc and Rd taken together with the nitrogen of attachment in —NRcRd form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- Re and Rf are each independently —H or —C1-6alkyl;
- or Re and Rf taken together with their nitrogen of attachment in —NReRf form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- and
- Rp and Rq are each independently —H or —C1-6alkyl;
- or Rp and Rq taken together with the nitrogen of attachment in —NRpRq form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- R2 is:
- 1) a phenyl group unsubstituted or substituted with one, two, or three Rg substituents;
- where each Rg substituent is —C1-6alkyl, —OH, —OC1-6alkyl, —CN, —NO2, —N(Rh)Ri, —C(O)N(Rh)Ri, —C(O)C1-6alkyl, —S(O)0-2—C1-6alkyl, —SO2CF3, —SO2N(Rh)Ri, —SCF3, halo, —CF3, —OCF3, —CO2H, —CO2C1-6alkyl, —C(Rj)2—CN, —C(Rj)2—CO2C1-4alkyl, —C(Rj)2—CO2H, —C(Rj)2—CON(Rh)Ri, —C(Rj)2—CH2N(Rh)Ri, or —C(Rj)2—OH;
- or two adjacent Rg substituents taken together form —OC1-2alkylO-, —C2-6alkylO—, or —C2-6alkylN(Rh)—;
- where Rh and Ri are each independently —H or —C1-6alkyl;
- or Rh and Ri taken together with their nitrogen of attachment in —NRhRi form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- where each Rj is independently —H, —C1-6alkyl, or —CF3;
- or both Rj substituents taken together with the carbon to which they are attached form a monocyclic cycloalkyl ring;
- or
- 2) a thiadiazolyl or six-membered monocyclic heteroaryl ring, each substituted with —CF3 or tert-butyl;
- R3 is —H, —CH3, —CF3, halo, —CN, —COC1-6alkyl, —CO2H, —CO2C1-6alkyl, —C(O)N(Rk)Rl, —CH2N(Rk)Rl, —S(O)0-2—C1-6alkyl, —S—Si(C1-6alkyl)3, —SO2CF3, or —SO2N(Rk)Rl;
- or a phenyl or 6-membered heteroaryl ring, each unsubstituted or substituted with —OH, —CH2N(Rk)Rl, —C(O)N(Rk)Rl, —SO2N(Rk)Rl, or —CO2H;
- where Rk and Rl are each independently —H or —C1-6alkyl;
- or Rk and Rl taken together with their nitrogen of attachment in —NRkRl form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- R4 is —H, —CF3, halo, —CN, —CO2H, —CO2C1-6alkyl, —C(O)N(Rn)Ro, —C1-4alkyl-OH, —C1-4alkyl-N(Rn)Ro, —S(O)0-2—C1-6alkyl, —SO2CF3, or —SO2N(Rn)Ro;
- where Rn and Ro are each independently —H or —C1-6alkyl;
- X is S, O, or NH;
- R5 is —H, —CH3, halo, or —CF3;
- and
- R6 and R7 are each independently —H or methyl;
- or R6 and R7 taken together with the carbon to which they are attached form a monocyclic cycloalkyl ring.
35 more elements
A process for the preparation of a compound of Formula (I) or a pharmaceutically acceptable salt thereof:
- comprising reacting a compound of formula (XVI):
- with thiourea, to give a compound of Formula (I);
- wherein:
- R1 is —H;
- —NRaRb;
- a —C1-6alkyl, —OC1-6alkyl, —S—C1-6alkyl, or —SO2—C1-6alkyl group unsubstituted or substituted with an —OH, —OC1-4alkyl, or —NRcRd substituent;
- where Ra and Rb are each independently —H;
- —C1-6alkyl;
- a —C2-4alkyl group substituted with a —OH, —OC1-4alkyl, or —NReRf substituent;
- or a saturated monocyclic cycloalkyl, —C1alkyl-(saturated monocyclic cycloalkyl), —C1alkyl-(carbon-linked, saturated monocyclic heterocycloalkyl), benzyl, or —C1alkyl-(monocyclic heteroaryl) group, each unsubstituted or substituted with a —C1-6alkyl, —OH, —OC1-4alkyl, —NRpRq, or fluoro substituent;
- or, Ra and Rb taken together with the nitrogen of attachment in —NRaRb form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with one, two, or three moieties independently selected from the group consisting of —C1-6alkyl, —C1-2alkyl-OH, —C1-2alkyl-OC1-2alkyl, —OH, —OC1-4alkyl, —NRpRq, fluoro, —CO2H, and monocyclic cycloalkyl substituents;
- where Rc and Rd are each independently —H or —C1-6alkyl;
- or Rc and Rd taken together with the nitrogen of attachment in —NRcRd form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- Re and Rf are each independently —H or —C1-6alkyl;
- or Re and Rf taken together with their nitrogen of attachment in —NReRf form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- and
- Rp and Rq are each independently —H or —C1-6alkyl;
- or Rp and Rq taken together with the nitrogen of attachment in —NRpRq form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- R2 is:
- 1) a phenyl group unsubstituted or substituted with one, two, or three Rg substituents;
- where each Rg substituent is —C1-6alkyl, —OH, —OC1-6alkyl, —CN, —NO2, —N(Rh)Ri, —C(O)N(Rh)Ri, —C(O)C1-6alkyl, —S(O)0-2—C1-6alkyl, —SO2CF3, —SO2N(Rh)Ri, —SCF3, halo, —CF3, —OCF3, —CO2H, —CO2C1-6alkyl, —C(Rj)2—CN, —C(Rj)2—CO2—C1-4alkyl, —C(Rj)2—CO2H, —C(Rj)2—CON(Rh)Ri, —C(Rj)2—CH2N(Rh)Ri, or —C(Rj)2—OH;
- or two adjacent Rg substituents taken together form —OC1-2alkylO—, —C2-6alkylO—, or —C2-6alkylN(Rh—;
- where Rh and Ri are each independently —H or —C1-6alkyl;
- or Rh and Ri taken together with their nitrogen of attachment in —NRhRi form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- where each Rj is independently —H, —C1-6alkyl, or —CF3;
- or both Rj substituents taken together with the carbon to which they are attached form a monocyclic cycloalkyl ring;
- or
- 2) a thiadiazolyl or six-membered monocyclic heteroaryl ring, each substituted with —CF3 or tert-butyl;
- R3 is —H, —CH3, —CF3, halo, —CN, —COC1-6alkyl, —CO2H, —CO2C1-6alkyl, —C(O)N(Rk)Rl, —CH2N(Rk)Rl, —S(O)0-2—C1-6alkyl, —S—Si(C1-6alkyl)3, —SO2CF3, or —SO2N(Rk)Rl;
- or a phenyl or 6-membered heteroaryl ring, each unsubstituted or substituted with —OH, —CH2N(Rk)Rl, —C(O)N(Rk)Rl, —SO2N(Rk)Rl, or —CO2H;
- where Rk and Rl are each independently —H or —C1-6alkyl;
- or Rk and Rl taken together with their nitrogen of attachment in —NRkRl form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- R4 is —H, —CF3, halo, —CN, —CO2H, —CO2C1-6alkyl, —C(O)N(Rn)Ro, —C1-4alkyl-OH, —C1-4alkyl-N(Rn)Ro, —S(O)0-2—C1-6alkyl, —SO2CF3, or —SO2N(Rn)Ro;
- where Rn and Ro are each independently —H or —C1-6alkyl;
- X is S;
- R5 is —H, —CH3, halo, or —CF3;
- and
- R6 and R7 are each independently —H or methyl;
- or R6 and R7 taken together with the carbon to which they are attached form a monocyclic cycloalkyl ring.
36 more elements
A compound of formula (XVI):
- wherein:
- R1 is —H;
- —NRaRb;
- a —C1-6alkyl, —OC1-6alkyl, —S—C1-6alkyl, or —SO2—C1-6alkyl group unsubstituted or substituted with an —OH, —OC1-4alkyl, or —NRcRd substituent;
- where Ra and Rb are each independently —H;
- —C1-6alkyl;
- a —C2-4alkyl group substituted with a —OH, —OC1-4alkyl, or —NReRf substituent;
- or a saturated monocyclic cycloalkyl, -C1alkyl-(saturated monocyclic cycloalkyl), —C1alkyl-(carbon-linked, saturated monocyclic heterocycloalkyl), benzyl, or —C1alkyl-(monocyclic heteroaryl) group, each unsubstituted or substituted with a —C1-6alkyl, —OH, —OC1-4alkyl, —NRpRq, or fluoro substituent;
- or, Ra and Rb taken together with the nitrogen of attachment in —NRaRb form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with one, two, or three moieties independently selected from the group consisting of —C1-6alkyl, —C1-2alkyl-OH, —C1-2alkyl-OC1-2alkyl, —OH, —OC1-4alkyl, NRpRq, fluoro, —CO2H, and monocyclic cycloalkyl substituents;
- where Rc and Rd are each independently —H or —C1-6alkyl;
- or Rc and Rd taken together with the nitrogen of attachment in —NRcRd form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- Re and Rf are each independently —H or —C1-6alkyl;
- or Re and Rf taken together with their nitrogen of attachment in —NReRf form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- and
- Rp and Rq are each independently —H or —C1-6alkyl;
- or Rp and Rq taken together with the nitrogen of attachment in —NRpRq form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- R2 is:
- 1) a phenyl group unsubstituted or substituted with one, two, or three Rg substituents;
- where each Rg substituent is —C1-6alkyl, —OH, —OC1-6alkyl, —CN, —NO2, —N(Rh)Ri, —C(O)N(Rh)Ri, —C(O)C1-6alkyl, —S(O)0-2—C1-6alkyl, —SO2CF3, —SO2N(Rh)Ri, —SCF3, halo, —CF3, —OCF3, —CO2H, —CO2C1-6alkyl, —C(Rj)2—CN, —C(Rj)2—CO2C1-4alkyl, —C(Rj)2—CO2H, —C(Rj)2—CON(Rh)Ri, —C(Rj)2—CH2N(Rh)Ri, or —C(Rj)2—OH;
- or two adjacent Rg substituents taken together form —OC1-2alkylO—, —C2-6alkylO—, or —C2-6alkylN(Rh)—;
- where Rh and Ri are each independently —H or —C1-6alkyl;
- or Rh and Ri taken together with their nitrogen of attachment in —NRhRi form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- where each Rj is independently —H, —C1-6alkyl, or —CF3;
- or both Rj substituents taken together with the carbon to which they are attached form a monocyclic cycloalkyl ring;
- or
- 2) a thiadiazolyl or six-membered monocyclic heteroaryl ring, each substituted with —CF3 or tert-butyl;
- R3 is —H, —CH3, —CF3, halo, —CN, —COC1-6alkyl, —CO2H, —CO2C1-6alkyl, —C(O)N(Rk)Rl, —CH2N(Rk)Rl, —S(O)0-2—C1-6alkyl, —S—Si(C1-6alkyl)3, —SO2CF3, or —SO2N(Rk)Rl;
- or a phenyl or 6-membered heteroaryl ring, each unsubstituted or substituted with —OH, —CH2N(Rk)Rl, —C(O)N(Rk)Rl, —SO2N(Rk)Rl, or —CO2H;
- where Rk and Rl are each independently —H or —C1-6alkyl;
- or Rk and Rl taken together with their nitrogen of attachment in —NRkRl form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with methyl;
- R4 is —H, —CF3, halo, —CN, —CO2H, —CO2C1-6alkyl, —C(O)N(Rn)Ro, —C1-4alkyl-OH, —C1-4alkyl-N(Rn)Ro, —S(O)0-2—C1-6alkyl, —SO2CF3, or —SO2N(Rn)Ro;
- where Rn and Ro are each independently —H or —C1-6alkyl;
- R5 is —H, —CH3, halo, or —CF3;
- and
- R6 and R7 are each independently —H or methyl;
- or R6 and R7 taken together with the carbon to which they are attached form a monocyclic cycloalkyl ring.
33 more elements
Dependencies are inferred from the claim text.