NOVEL COMPOUNDS

The present invention relates to compounds of formula (I) wherein Q is selected from O or S; Ris a saturated or unsaturated, optionally substituted hydrocarbyl group optionally including one or more heteroatoms N, O or S; Ris a cyclic group substituted at the a and a′ positions, wherein the substituent at the α-position is a monovalent heterocyclic group or a monovalent aromatic group, wherein the heterocyclic or aromatic group may optionally be substituted, and wherein the cyclic group may optionally be further substituted; Rand Rare each independently hydrogen, halogen, —OH, —NH, —CN, —R, —OR, —NHRor —N(R); or Rand Rtogether with the carbon atom to which they are attached may form a 3- to 7-membered saturated or unsaturated, optionally substituted cyclic group; and Ris independently optionally substituted C-Calkyl. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3. 2. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof as claimed in claim 1 , wherein Ris a 4- to 10-membered cyclic group claim 1 , wherein the cyclic group may optionally be substituted.3. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof as claimed in claim 1 , wherein Ris a C-Calkyl claim 1 , C-Calkenyl claim 1 , C-Calkynyl or C-Ccycloalkyl group claim 1 , all of which may optionally be substituted claim 1 , and all of which may optionally include one claim 1 , two or three heteroatoms N claim 1 , O or S in their carbon skeleton.4. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof as claimed in claim 1 , wherein Ris an optionally substituted phenyl group or an optionally substituted benzyl group.5. The compound or a pharmaceutically acceptable salt ...

Sulfonylureas and sulfonylthioureas as nlrp3 inhibitors

The present invention relates to sulfonylureas and sulfonylthioureas comprising a monocyclic imidazolyl group. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS

The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered heteroaryl group substituted with an amide-containing group. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP. 2. A compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein Ris monovalent claim 1 , and optionally wherein —Ris any saturated hydrocarbyl group claim 1 , wherein the hydrocarbyl group may be straight-chained or branched claim 1 , or be or include cyclic groups claim 1 , wherein the hydrocarbyl group may optionally be substituted with one or more groups selected from halo claim 1 , —CN claim 1 , —OH claim 1 , —NH claim 1 , oxo (═O) and ═NH claim 1 , wherein the hydrocarbyl group includes at least one amide group in its carbon skeleton claim 1 , and wherein the hydrocarbyl group may optionally include one claim 1 , two or three further heteroatoms N and/or O in its carbon skeleton.3. (canceled)4. A compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein the 5-membered heteroaryl group of Ris monocyclic.5. A compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein Ris divalent claim 1 , and optionally wherein —R— is any saturated or unsaturated hydrocarbylene group claim 1 , wherein the hydrocarbylene group may be straight-chained or branched claim 1 , or be or include cyclic groups claim 1 , wherein the hydrocarbylene group may optionally be substituted with one or more groups selected from halo claim 1 , —CN claim 1 , —OH claim 1 , —NH claim 1 , oxo (═O) and ═NH claim 1 , wherein the hydrocarbylene group includes at least ...

MACROCYCLIC SULFONYLUREA DERIVATIVES USEFUL AS NLRP3 INHIBITORS

The present invention relates to macrocyclic compounds, such as macrocyclic sulfonyl ureas. The present invention further relates to associated salts, solvates, prodrugs and pharmaceutical compositions and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRPinhibition. 2. The compound or pharmaceutically acceptable salt or solvate thereof claim 1 , as claimed in claim 1 , wherein:{'sub': '2', '(i) J is —SO—; and/or'}(ii) Q is O; and/or{'sup': '1', '(iii) Ris hydrogen and X is —NH—; and/or'}(iv) L is a saturated or unsaturated hydrocarbylene group, wherein the hydrocarbylene group may be straight-chained or branched, wherein the hydrocarbylene group includes an aromatic cyclic group directly attached to X, wherein the ring atom of the aromatic cyclic group that is directly attached to X is a carbon atom, wherein the hydrocarbylene group may optionally include one or more further cyclic groups, wherein the hydrocarbylene group may optionally be substituted, and wherein the hydrocarbylene group may optionally include one or more heteroatoms independently selected from N, O and S in its carbon skeleton; and or{'sup': '1', '(v) the minimum single ring size that encompasses all or part of each of -J-, —N(R)—, —C(=Q)-, —X— and -L- is from 12 to 24 atoms, or from 14 to 20 atoms.'}3. (canceled)4. (canceled)5. (canceled)7. The compound or pharmaceutically acceptable salt or solvate thereof claim 6 , as claimed in claim 6 , wherein:{'sup': '1', '(i) Lis a bond, or'}{'sup': '1', '(ii) Lis a divalent 3- to 7-membered monocyclic group, or a divalent 7- to 11-membered bicyclic group, either of which may optionally be substituted with one or more monovalent substituents and/or π-bonded substituents.'}8. (canceled)9. The compound or pharmaceutically acceptable salt or solvate thereof claim 6 , as claimed claim 6 , wherein:{'sup': '2', 'i) Lis an alkylene or alkenylene group, wherein the alkylene or alkenylene group ...

NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS

The present invention relates to compounds of formula (I): wherein Q is selected from O or S; Ris a saturated or unsaturated, optionally substituted C-Chydrocarbyl group, wherein the atom of Rwhich is attached to the sulfur atom of the sulfonylurea group is not a ring atom of a cyclic group; and Ris a cyclic group substituted at the α-position, wherein R may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP. 2. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof as claimed in claim 1 , wherein Ris substituted with one or more substituents independently selected from halo claim 1 , C-Chaloalkyl claim 1 , —CN claim 1 , —N claim 1 , —NO claim 1 , —OH claim 1 , —SR claim 1 , —SOR claim 1 , —SOR claim 1 , —SON(R) claim 1 , —NH claim 1 , —COR claim 1 , —COORor —OCOR; wherein each —R is independently selected from hydrogen or a C-Calkyl claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , C-Chaloalkyl or C-Ccycloalkyl group.3. The compound or a pharmaceutically acceptable salt claim 2 , solvate or prodrug thereof as claimed in claim 2 , wherein Ris substituted with one or more substituents independently selected from halo claim 2 , C-Chaloalkyl claim 2 , —CN claim 2 , —N claim 2 , —SR claim 2 , —SOR claim 2 , —SOR or —SON(R); wherein each —Ris independently selected from hydrogen or a C-Calkyl claim 2 , C-Calkenyl claim 2 , C-Calkynyl claim 2 , C-Chaloalkyl or C-Ccycloalkyl group.4. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof as claimed in claim 1 , wherein Ris a cyclic group substituted at the α and α′ positions claim 1 , wherein Rmay optionally be further substituted.5. The compound or a pharmaceutically acceptable salt ...

SULFONYLUREAS AND SULFONYLTHIOUREAS AS NLRP3 INHIBITORS

The present invention relates to compounds of formula (I): 2. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein Ris a 6-membered heteroaryl group containing at least two nitrogen atoms in the 6-membered ring structure claim 1 , wherein Rmay optionally be substituted claim 1 , and wherein optionally:(i) at least one of the two nitrogen atoms is located at the 3, 4 or 5-position of the 6-membered ring structure; or(ii) a first nitrogen atom is located at the 2-position and a second nitrogen atom is located at the 6-position of the 6-membered ring structure, and wherein the 6-membered heteroaryl group is substituted with one or more monovalent groups at the 3- and/or 5-positions of the 6-membered ring structure.34-. (canceled)5. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein the 6-membered heteroaryl group of Ris substituted with at least one monovalent group X claim 1 , wherein X is at each occurrence any group that can mesomerically donate a lone pair of electrons from a nitrogen claim 1 , oxygen or sulphur atom onto at least one nitrogen atom in the 6-membered ring structure claim 1 , and wherein the 6-membered heteroaryl group may optionally be further substituted.6. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein:{'sup': '1', 'the 6-membered heteroaryl group of Ris substituted with at least one monovalent group X′ at a position ortho- or para- to at least one nitrogen atom in the 6-membered ring structure;'}{'sup': '1', 'the 6-membered heteroaryl group of Rmay optionally be further substituted;'}{'sup': '1', 'Xis at each occurrence independently selected from a'}{'sup': 3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3, 'sub': 2', '2', '2', '2, '—OR, —SR, —N(R), —O-L-OR, —O-L-SR, —O-L-N(R), —S-L-OR, —S ...

NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS

The present invention relates to compounds of formula (I):

NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS

The present invention relates to sulfonylureas and sulfonylthioureas comprising as-membered nitrogen-containing heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is substituted with at least one group containing an oxygen atom, and wherein said oxygen atom is attached to the heteroaryl ring via at least two other atoms. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3. 2. A compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein ring A is monocyclic.3. A compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein:(i) W, X, Y and Z are each independently N, NH or CH; and/or(ii) at least two of W, X, Y and Z are N or NH.4. (canceled)5. A compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein R—O-L- is directly attached to a ring nitrogen atom of ring A.6. A compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein{'sup': '1', '(i) the group R—O-L-, including any optional substituents, contains only atoms selected from the group consisting of carbon, hydrogen, oxygen and halogen atoms; and/or'}{'sup': 1', '2, '(ii) the oxygen atom of R—O-L- is not directly attached to a sphybridised atom.'}7. (canceled)9. A compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein [{'sup': 3', 'β', 'β', 'α', 'α', 'α', 'α', 'α', 'β', 'α', 'α', 'β', 'β', 'β', 'β', 'β', 'β', 'α', 'α', 'β', 'α', 'β', 'α', 'α', 'β', 'α', 'α', 'β', 'α', 'β', 'β', 'β', 'α', 'α', 'β', 'α', 'β', 'β', 'β', 'β', ...

NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS

The present invention relates to compounds of formula (I): Formula (I) wherein Q is selected from O or S; L is a saturated or unsaturated, optionally substituted C-Chydrocarbylene group optionally including one or more heteroatoms N, O or S; Ris —NRR, —OR, —(C═NR)R, —(CO)R, —CN, —N, a quaternary ammonium group or an optionally substituted heterocycle; R, R, R, R, Rand Rare each independently hydrogen or a saturated or unsaturated, optionally substituted C-Chydrocarbyl group optionally including one or more heteroatoms N, O or S; wherein optionally L and R, or L and R, or Rand R, or L and R, or L and R, or L and R, or Rand R, or L and Rtogether with the atom(s) to which they are attached may form a 3- to 12-membered, saturated or unsaturated, optionally substituted cyclic group; and Ris a cyclic group substituted at the a-position, wherein Rmay optionally be further substituted; provided that the atom of L which is attached to the sulfur atom of the sulfonylurea group is a carbon atom and is not a ring atom of a heterocyclic or aromatic group. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP. 2. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof as claimed in claim 1 , wherein L is a saturated or unsaturated C-Chydrocarbylene group claim 1 , wherein the hydrocarbylene group may be straight-chained or branched claim 1 , or be or include cyclic groups claim 1 , and wherein the hydrocarbylene group may optionally be substituted with one or more substituents independently selected from halo claim 1 , —CN claim 1 , —N(R) claim 1 , —ORor oxo (═O) groups claim 1 , wherein Ris independently selected from a hydrogen atom or a C-Calkyl group.3. The compound or a pharmaceutically acceptable salt claim 1 , ...

NOVEL COMPOUNDS

The present invention relates to compounds of formula (I): wherein Q is selected from O or S; Ris a saturated or unsaturated hydrocarbyl group, wherein the hydrocarbyl group may be straight-chained or branched, or be or include cyclic groups, wherein the hydrocarbyl group may optionally be substituted, and wherein the hydrocarbyl group may optionally include one or more heteroatoms N, O or S in its carbon skeleton; and Ris a cyclic group substituted at the α-position, wherein Rmay optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP. 2. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof as claimed in claim 1 , wherein Ris a saturated or unsaturated C-Chydrocarbyl group claim 1 , wherein the hydrocarbyl group may be straight-chained or branched claim 1 , or be or include cyclic groups claim 1 , wherein the hydrocarbyl group may optionally be substituted claim 1 , and wherein the hydrocarbyl group may optionally include one or more heteroatoms N claim 1 , O or S in its carbon skeleton.3. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof as claimed in claim 1 , wherein Ris a 4- to 10-membered cyclic group claim 1 , wherein the cyclic group may optionally be substituted.4. The compound or a pharmaceutically acceptable salt claim 3 , solvate or prodrug thereof as claimed in claim 3 , wherein Ris a cycloalkyl claim 3 , cycloalkenyl claim 3 , non-aromatic heterocyclic claim 3 , aryl or heteroaryl group claim 3 , all of which may optionally be substituted.5. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof as claimed in claim 1 , wherein Ris a C-Calkyl claim 1 , C-Calkenyl or C-Calkynyl group ...

Novel sulfonamide carboxamide compounds

The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

SULFONAMIDE DERIVATES AS NLRP3 INHIBITORS

The present invention relates to compounds of formula (I): (I) wherein Q is selected from O or S; Ris an optionally substituted hydrocarbyl group which may optionally include one or more heteroatoms N, O or S in its carbon skeleton, provided that the hydrocarbyl group includes at least one heteroatom N, O or S in its carbon skeleton or is substituted with a substituent comprising at least one heteroatom N, O or S, and provided that the atom of Rwhich is attached to the sulfur atom of the remainder of the molecule is not a ring atom of a cyclic group; Ris an α,α′-substituted cyclic group which may optionally be further substituted; Rand Rare each independently hydrogen, halogen, —OH, —NH, —CN, —R, —OR, —NHRs or —N(R); or Rand Rtogether with the carbon atom to which they are attached may form a 3- to 7-membered saturated or unsaturated, optionally substituted cyclic group; and Ris independently optionally substituted C-Calkyl. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP. 2. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof as claimed in claim 1 , wherein R— is R-L- claim 1 , wherein:{'sub': 1', '12, 'L is a saturated or unsaturated C-Chydrocarbylene group, wherein the hydrocarbylene group may be straight-chained or branched, or be or include cyclic groups, wherein the hydrocarbylene group may optionally be substituted, and wherein the hydrocarbylene group may optionally include one or more heteroatoms N, O or S in its carbon skeleton;'}{'sup': 21', '22', '23', '24', '25', '26', '27', '28', '29, 'sub': '3', 'Ris —NRR, —OR, —SR, —(C═NR)R, —(CO)R, —(CS)R, —CN or —N;'}{'sup': 22', '23', '24', '25', '26', '27', '28', '29, 'sub': 1', '10, 'R, R, R, R, R, R, Rand Rare each independently hydrogen ...

Novel sulfonamide carboxamide compounds

The present invention relates to compounds of formula (I) wherein Q is selected from O or S; R1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R1 may optionally be substituted; and R2 is a cyclic group substituted at the α-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

sulfonylureas and sulfonylthioureas as inhibitors of vnlrp3

A presente invenção refere-se a sulfonilureias e sulfoniltioureias compreendendo um anel heteroaril de 5 membros contendo nitrogênio ligado ao grupo sulfonil, em que o anel heteroaril é substituído por um grupo R1 contendo nitrogênio, em que R1 contém de 1 a 7 átomos que não sejam hidrogênio ou halogênio. A presente invenção refere-se adicionalmente a sais, solvatos e pró-fármacos de tais compostos, a composições farmacêuticas compreendendo tais compostos e ao uso de tais compostos no tratamento e prevenção de distúrbios e doenças médicas, principalmente pela inibição de NLRP3. The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered heteroaryl ring containing nitrogen attached to the sulfonyl group, wherein the heteroaryl ring is replaced by a nitrogen-containing group R1, where R1 contains from 1 to 7 atoms that are not hydrogen or halogen. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds and to the use of such compounds in the treatment and prevention of medical disorders and diseases, mainly by inhibiting NLRP3.

Novel compounds

The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R1 is a saturated or unsaturated hydrocarbyl group, wherein the hydrocarbyl group may be straight-chained or branched, or be or include cyclic groups, wherein the hydrocarbyl group may optionally be substituted, and wherein the hydrocarbyl group may optionally include one or more heteroatoms N, O or S in its carbon skeleton; and R2 is a cyclic group substituted at the a-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Kinase inhibitors as therapeutic agents

The present invention is directed to a compound of Formula (I) as defined herein which are useful as kinase inhibitors.

Novel sulfonamide carboxamide compounds

NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS Abstract 0 0 Q R N N' H H The present invention relates to compounds of formula (I) wherein Q is selected from 0 or S; R is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R1 may optionally be substituted; and R2 is a cyclic group substituted at the a-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Isoquinolinone derivatives

The present invention relates to isoquinolinone derivatives of formula (I): wherein are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Novel sulfonamide carboxamide compounds

The present invention relates to compounds of formula (I): Formula (I) wherein Q is selected from O or S; L is a saturated or unsaturated, optionally substituted C1-C12 hydrocarbylene group optionally including one or more heteroatoms N, O or S; R1 is -NR3R4, -OR5, -(C=NR6)R7, -(CO)R8, -CN, -N3, a quaternary ammonium group or an optionally substituted heterocycle; R3, R4, R5, R6, R7 and R8 are each independently hydrogen or a saturated or unsaturated, optionally substituted C1- C10 hydrocarbyl group optionally including one or more heteroatoms N, O or S; wherein optionally L and R3, or L and R4, or R3 and R4, or L and R5, or L and R6, or L and R7, or R6 and R7, or L and R8 together with the atom(s) to which they are attached may form a 3- to 12-membered, saturated or unsaturated, optionally substituted cyclic group; and R2 is a cyclic group substituted at the a-position, wherein R2 may optionally be further substituted; provided that the atom of L which is attached to the sulfur atom of the sulfonylurea group is a carbon atom and is not a ring atom of a heterocyclic or aromatic group. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Sulfonylureas and sulfonylthioureas as NLRP3 inhibitors

The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered nitrogen-containing heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is substituted with a nitrogen-containing group R1′ wherein R1 contains from 1 to 7 atoms other than hydrogen or halogen. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Kinase inhibitors as therapeutic agents

The present invention is directed to a compound of Formula (I) as defined herein which are useful as kinase inhibitors.

Novel sulfonamide carboxamide compounds

The present invention relates to compounds of formula (I): Formula (I) wherein Q is selected from O or S; L is a saturated or unsaturated, optionally substituted C1-C12 hydrocarbylene group optionally including one or more heteroatoms N, O or S; R1 is -NR3R4, -OR5, -(C=NR6)R7, -(CO)R8, -CN, -N3, a quaternary ammonium group or an optionally substituted heterocycle; R3, R4, R5, R6, R7 and R8 are each independently hydrogen or a saturated or unsaturated, optionally substituted C1- C10 hydrocarbyl group optionally including one or more heteroatoms N, O or S; wherein optionally L and R3, or L and R4, or R3 and R4, or L and R5, or L and R6, or L and R7, or R6 and R7, or L and R8 together with the atom(s) to which they are attached may form a 3- to 12-membered, saturated or unsaturated, optionally substituted cyclic group; and R2 is a cyclic group substituted at the a-position, wherein R2 may optionally be further substituted; provided that the atom of L which is attached to the sulfur atom of the sulfonylurea group is a carbon atom and is not a ring atom of a heterocyclic or aromatic group. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Novel sulfonamide carboxamide compounds

The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered nitrogen-containing heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is substituted with at least one monovalent group comprising a non- aromatic cyclic group, and wherein the group attached to the terminal nitrogen atom of the urea group is a 6-membered cyclic group substituted at the2- and4-positions. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLF^inhibition.

Kinase inhibitors as therapeutic agents

New compounds and their uses 707.

La presente invención se refiere a derivados de isoquinolinona de fórmula (I): donde R1, R2, R3, R4, R5, R6 y R7 son los definidos aquí; a procesos para su preparación, a composiciones farmacéuticas que los contienen y a su uso en terapia.

new sulfonamide-carboxamide compounds

A presente invenção refere-se aos compostos da fórmula (I): Fórmula (I) em que Q é selecionado dentre O ou S; R1 é um grupo heterocíclico não aromático compreendendo pelo menos um átomo de nitrogênio no anel, em que R1 é ligado ao átomo de enxofre do grupo sulfonilureia por um átomo de carbono no anel, e em que R1 pode opcionalmente ser substituído; e R2 é um grupo cíclico substituído na posição a, em que R2 pode opcionalmente ser adicionalmente substituído. A presente invenção refere-se adicionalmente a sais, solvatos e pró-fármacos de tais compostos, a composições farmacêuticas compreendendo tais compostos e ao uso de tais compostos no tratamento e prevenção de distúrbios e doenças médicas, principalmente pela inibição de NLRP3. The present invention relates to the compounds of the formula (I): Formula (I) in which Q is selected from O or S; R1 is a non-aromatic heterocyclic group comprising at least one nitrogen atom in the ring, where R1 is attached to the sulfonyl sulfur group by a carbon atom in the ring, and where R1 can optionally be substituted; and R2 is a cyclic group substituted at position a, where R2 can optionally be additionally substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds and to the use of such compounds in the treatment and prevention of medical disorders and diseases, mainly by inhibiting NLRP3.

Sulfonylureas and sulfonylthioureas as nlrp3 inhibitors

The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is di-substituted at the 3- and 4-positions relative to the point of attachment of the sulfonyl group, wherein at least one of the di-substituents contains a nitrogen atom. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP 3 .

Novel sulfonamide carboxamide compounds

The present invention relates to compounds of formula (I): Formula (I) wherein Q is selected from O or S; L is a saturated or unsaturated, optionally substituted C

Isoquinolinone derivatives

The present invention relates to isoquinolinone derivatives of formula (I): wherein are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

New compounds and their uses 707

NEW SULFONAMIDE CARBOXAMIDE COMPOUNDS

Referida a compuestos derivados de sulfonilurea o sulfoniltiourea de formula (I), donde Q es O o S; W, X, Y y Z son N, O, S, NH o CH; L es un grupo hidrocarbileno; R1 es H o un grupo hidrocarbilo; R2 es un grupo ciclico sustituido en la posicion alfa; R3 es halo, OH, NO2; N3, entre otros; m es 0, 1, 2 o 3. Tambien esta referida a una composicion farmaceutica. Dichos compuestos inhiben los inflamosomas NLRP3 y son utiles en el tratamiento de esclerosis multiple, diabetes tipo 2, enfermedad de Alzheimer, entre otras. Referring to compounds derived from sulfonylurea or sulfonylthiourea of formula (I), where Q is O or S; W, X, Y, and Z are N, O, S, NH, or CH; L is a hydrocarbylene group; R1 is H or a hydrocarbyl group; R2 is a cyclic group substituted in the alpha position; R3 is halo, OH, NO2; N3, among others; m is 0, 1, 2 or 3. It also refers to a pharmaceutical composition. Said compounds inhibit NLRP3 inflammosomes and are useful in the treatment of multiple sclerosis, type 2 diabetes, Alzheimer's disease, among others.

Novel sulfonamide carboxamide compounds

Novel sulfonamide carboxamide compounds

The present invention relates to compounds of formula (I) wherein Q is selected from O or S; R1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R1 may optionally be substituted; and R2 is a cyclic group substituted at the a-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Kinase inhibitors as therapeutic agents.

Macrocyclic sulfonylurea derivatives useful as nlrp3 inhibitors

The present invention relates to macrocyclic compounds, such as macrocyclic sulfonyl ureas. The present invention further relates to associated salts, solvates, prodrugs and pharmaceutical compositions and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP 3 inhibition.

Sulfonylureas and sulfonylthioureas as NLRP3 inhibitors

The present invention relates to sulfonylureas and sulfonylthioureas comprising a monocyclic imidazolyl group of formula (I):wherein Q is selected from O or S, R1 is an imidazolyl group, wherein the imidazolyl group is unsubstituted or substituted with one or more monovalent substituents, and R2 is a cyclic group substituted at the α-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Cyclic cyanoenone derivatives as modulators of keap1

The present invention relates to cyclic cyanoenone derivatives of Formula (I) or pharmaceutically acceptable salts or solvates thereof, wherein R 1 , R 2 , R 3 , R 4 and m are as defined herein. The present invention also relates to pharmaceutical compositions comprising the cyclic cyanoenone derivatives of Formula (I) and to their use in therapy.

Derivados de cianoenona ciclicos como moduladores de keap1.

La presente invención se refiere a derivados de cianoenona cíclicos de la Fórmula (I) (ver Fórmula) (I) o sales o solvatos farmacéuticamente aceptables de los mismos, en donde R1, R2, R3, R4 y m son como defined en el presente documento. La presente invención también se refiere a composiciones farmacéuticas que comprenden los derivados de cianoenona cíclicos de la Fórmula (I) y a su uso en la terapia.

Kinaseinhibitoren als arzneimittel

Cyclic cyanoenone derivatives as modulators of KEAP1

CYCLIC CYANOENONE DERIVATIVES AS MODULATORS OF KEAPI Abstract NC R4 R R1 R2 (I) The present invention relates to cyclic cyanoenone derivatives of Formula (I) or pharmaceutically acceptable salts or solvates thereof, wherein R, R2, R3, R4 and mare as defined herein. The present invention also relates to pharmaceutical compositions comprising the cyclic cyanoenone derivatives of Formula (I) and to their use in therapy.

Sulfonamide carboxamide compounds

The present invention relates to compounds of formula (I): Formula (I) wherein Q is selected from O or S; L is a saturated or unsaturated, optionally substituted C 1 -C 12 hydrocarbylene group optionally including one or more heteroatoms N, O or S; R 1 is —NR 3 R 4 , —OR 5 , —(C═NR 6 )R 7 , —(CO)R 8 , —CN, —N 3 , a quaternary ammonium group or an optionally substituted heterocycle; R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are each independently hydrogen or a saturated or unsaturated, optionally substituted C 1 -C 10 hydrocarbyl group optionally including one or more heteroatoms N, O or S; wherein optionally L and R 3 , or L and R 4 , or R 3 and R 4 , or L and R 5 , or L and R 6 , or L and R 7 , or R 6 and R 7 , or L and R 8 together with the atom(s) to which they are attached may form a 3- to 12-membered, saturated or unsaturated, optionally substituted cyclic group; and R 2 is a cyclic group substituted at the a-position, wherein R 2 may optionally be further substituted; provided that the atom of L which is attached to the sulfur atom of the sulfonylurea group is a carbon atom and is not a ring atom of a heterocyclic or aromatic group. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP 3 .

Sulfonamide carboxamide compounds

The present invention relates to compounds of formula (I) wherein Q is selected from O or S; R1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R1 may optionally be substituted; and R2 is a cyclic group substituted at the α-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Cyclic cyanoenone derivatives as modulators of KEAP1

The present invention relates to cyclic cyanoenone derivatives of Formula (I) or pharmaceutically acceptable salts or solvates thereof, wherein R

Cyclic cyanoenone derivatives as modulators of KEAP1

The present invention relates to cyclic cyanoenone derivatives of Formula (I) or pharmaceutically acceptable salts or solvates thereof, wherein R

Cyclic cyanoenone derivatives as modulators of keap1

The present invention relates to cyclic cyanoenone derivatives of Formula (I) or pharmaceutically acceptable salts or solvates thereof, wherein R1, R2, R3, R4 and m are as defined herein. The present invention also relates to pharmaceutical compositions comprising the cyclic cyanoenone derivatives of Formula (I) and to their use in therapy.

Sulfonamide carboxamide compounds

The present invention relates to sulfonylureas and sulfonylthioureas comprising as-membered nitrogen-containing heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is substituted with at least one group containing an oxygen atom, and wherein said oxygen atom is attached to the heteroaryl ring via at least two other atoms. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Novel sulfonamide carboxamide compounds

NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS Abstract 0 0 Q R N N' H H The present invention relates to compounds of formula (I) wherein Q is selected from 0 or S; R is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R1 may optionally be substituted; and R2 is a cyclic group substituted at the a-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Sulfonyl acetamides as NLRP3 inhibitors

The present invention relates to compounds of formula (I) wherein Q is selected from O or S; R1 is a saturated or unsaturated, optionally substituted hydrocarbyl group optionally including one or more heteroatoms N, O or S; R2 is a cyclic group substituted at the a and a′ positions, wherein the substituent at the α-position is a monovalent heterocyclic group or a monovalent aromatic group, wherein the heterocyclic or aromatic group may optionally be substituted, and wherein the cyclic group may optionally be further substituted; R3 and R4 are each independently hydrogen, halogen, —OH, —NH2, —CN, —R5, —OR5, —NHR5 or —N(R5)2; or R3 and R4 together with the carbon atom to which they are attached may form a 3- to 7-membered saturated or unsaturated, optionally substituted cyclic group; and R5 is independently optionally substituted C1-C4 alkyl. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Compuestos de sulfonamida carboxamida

Reivindicación 1: Un compuesto de fórmula (1), donde: Q se selecciona de O ó S; R¹ es un grupo hidrocarbilo saturado o insaturado, donde el grupo hidrocarbilo puede ser de cadena lineal o ramificada, o puede ser o incluir grupos cíclicos, donde el grupo hidrocarbilo puede sustituirse opcionalmente, y donde el grupo hidrocarbilo puede incluir, opcionalmente, uno o mas heteroátomos de N, O ó S en su esqueleto de carbono; y R² es un grupo cíclico sustituido en la posición a con un grupo heterocíclico monovalente o un grupo aromático monovalente, donde un átomo anular del grupo heterocíclico o aromático se acopla directamente a un átomo anular del grupo cíclico, donde el grupo heterocíclico o aromático puede sustituirse opcionalmente, y donde el grupo cíclico puede sustituirse adicionalmente de forma opcional.

Derivados de carboxamida sulfonamidas

Reivindicación 1: Un compuesto de fórmula (1), donde: Q se selecciona de O ó S; cada uno de V, X e Y se selecciona independientemente de C y N, y cada uno de W y Z se selecciona independientemente N, O, S, NH y CH, siempre que al menos uno de V, W, X, Y y Z sea N, O, S o NH; cada uno de RX y RY es independientemente cualquier grupo hidrocarbilo saturado o insaturado, donde el grupo hidrocarbilo puede ser de cadena recta o ramificado, o puede ser o incluir grupos cíclicos, donde el grupo hidrocarbilo puede sustituirse opcionalmente y donde el grupo hidrocarbilo puede incluir opcionalmente uno o más heteroátomos N, O ó S en su esqueleto de carbono; opcionalmente, RX y RY junto con los átomos X e Y a los cuales están unidos pueden formar un grupo cíclico saturado o insaturado de 3 a 12 miembros, donde el grupo cíclico puede sustituirse opcionalmente; R¹ es un grupo cíclico sustituido en la posición a, donde R¹ puede sustituirse opcionalmente de manera adicional; m es 0, 1 ó 2, cada R² es independientemente halo, -OH, -NO₂, -NH₂, -N₃,-SH, o un grupo hidrocarbilo saturado o insaturado, donde el grupo hidrocarbilo puede ser de cadena recta o ramificado, o puede ser o incluir grupos cíclicos, donde el grupo hidrocarbilo puede sustituirse opcionalmente y donde el grupo hidrocarbilo puede incluir opcionalmente uno o más heteroátomos N, O ó S en su esqueleto de carbono; opcionalmente, RX y cualquier R² unido a W junto con los átomos X e Y a los cuales están unidos pueden formar un grupo cíclico saturado o insaturado de 3 a 12 miembros, donde el grupo cíclico puede sustituirse opcionalmente; y opcionalmente, RY y cualquier R² unido a Z junto con los átomos Y y Z a los cuales están unidos pueden formar un grupo cíclico saturado o insaturado de 3 a 12 miembros, donde el grupo cíclico puede sustituirse opcionalmente; siempre que al menos uno de RX y RY comprenda un átomo de nitrógeno; y siempre que el compuesto no sea seleccionado del grupo de fórmulas (2).

Sulfonilureas y sulfoniltioureas inhibidores de nlrp3

Reivindicación 1: Un compuesto de fórmula (1), en donde: Q se selecciona de O ó S; cada uno de W, X, Y y Z es independientemente N, O, S, NH o CH, en donde al menos uno de W, X, Y y Z es N o NH; R¹ es un grupo monovalente que comprende al menos un átomo de nitrógeno, en donde -R¹- contiene de 1 a 7 átomos diferentes de hidrógeno o halógeno, o R¹ es un grupo divalente que comprende al menos un átomo de nitrógeno, en donde -R¹- contiene de 1 a 7 átomos diferentes de hidrógeno o halógeno, y en donde -R¹- se une directamente a dos W, X, Y o Z adyacentes; R² es un grupo cíclico sustituido en la posición a, en donde R² puede estar opcionalmente sustituido de forma adicional; m es 0, 1, 2 ó 3; cada R³ es independientemente un halo, -OH, -NO₂, -NH₂, -N₃, -SH, o un grupo hidrocarbilo saturado o insaturado, en donde el grupo hidrocarbilo puede ser de cadena lineal o ramificada, o puede ser o incluir grupos cíclicos, en donde el grupo hidrocarbilo se puede sustituir opcionalmente, y en donde el grupo hidrocarbilo puede incluir opcionalmente uno o mas heteroátomos N, O ó S en su estructura de carbono, y en donde, opcionalmente, cualquier R³ y cualesquiera dos W, X, Y o Z adyacentes pueden formar en conjunto un grupo cíclico saturado o insaturado de 3 a 12 miembros fusionado al anillo A, en donde el grupo cíclico fusionado al anillo A se puede sustituir opcionalmente.