OA12907A - Use of IKB-kinase inhibitors for the treatment of pain. - Google Patents

Use of IKB-kinase inhibitors for the treatment of pain. Download PDF

Info

Publication number: OA12907A
Authority: OA; OAPI
Prior art keywords: alkyl; radical; unsubstituted; substituted; hydrogen atom
Prior art date: 2002-08-17

Application number

OA1200500046A

Other languages

English (en)

Inventor

Martin Michaelis

Olaf Ritzeler

Gerhard Jaehne

Karl Rudolphi

Gerd Geisslinger

Hans-Georg Schaible

Original Assignee

Aventis Pharma Gmbh

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.)

2002-08-17

Filing date

2003-08-05

Publication date

2006-10-13

2003-08-05 Application filed by Aventis Pharma Gmbh filed Critical Aventis Pharma Gmbh

2006-10-13 Publication of OA12907A publication Critical patent/OA12907A/en

Links

208000002193 Pain Diseases 0.000 title claims abstract description 42
230000036407 pain Effects 0.000 title claims abstract description 40
229940043355 kinase inhibitor Drugs 0.000 title abstract description 9
239000003757 phosphotransferase inhibitor Substances 0.000 title abstract description 9
150000001875 compounds Chemical class 0.000 claims abstract description 41
239000003814 drug Substances 0.000 claims abstract description 8
-1 1,4-diazine radical Chemical class 0.000 claims description 217
150000003254 radicals Chemical class 0.000 claims description 84
125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 78
RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 62
125000003118 aryl group Chemical group 0.000 claims description 52
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 52
229910052736 halogen Inorganic materials 0.000 claims description 49
150000002367 halogens Chemical class 0.000 claims description 49
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 47
JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 46
KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Natural products C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims description 44
125000001072 heteroaryl group Chemical group 0.000 claims description 44
125000004433 nitrogen atom Chemical group N* 0.000 claims description 34
125000000623 heterocyclic group Chemical group 0.000 claims description 33
CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 32
XSCHRSMBECNVNS-UHFFFAOYSA-N benzopyrazine Natural products N1=CC=NC2=CC=CC=C21 XSCHRSMBECNVNS-UHFFFAOYSA-N 0.000 claims description 31
YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 30
KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims description 30
RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 30
SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims description 28
CIISBYKBBMFLEZ-UHFFFAOYSA-N 1,2-oxazolidine Chemical compound C1CNOC1 CIISBYKBBMFLEZ-UHFFFAOYSA-N 0.000 claims description 27
229910052757 nitrogen Inorganic materials 0.000 claims description 27
GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 26
229910052717 sulfur Inorganic materials 0.000 claims description 26
150000003852 triazoles Chemical class 0.000 claims description 26
125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 25
125000004093 cyano group Chemical group *C#N 0.000 claims description 25
125000000217 alkyl group Chemical group 0.000 claims description 24
UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 23
SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims description 22
FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims description 22
AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims description 22
CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims description 22
125000004430 oxygen atom Chemical group O* 0.000 claims description 22
125000001424 substituent group Chemical group 0.000 claims description 22
125000004434 sulfur atom Chemical group 0.000 claims description 22
ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims description 21
125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 21
125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 21
ZLTPDFXIESTBQG-UHFFFAOYSA-N isothiazole Chemical compound C=1C=NSC=1 ZLTPDFXIESTBQG-UHFFFAOYSA-N 0.000 claims description 21
PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims description 20
NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 20
YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims description 20
229940024606 amino acid Drugs 0.000 claims description 19
235000001014 amino acid Nutrition 0.000 claims description 19
150000001413 amino acids Chemical class 0.000 claims description 19
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 19
PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims description 19
WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims description 18
125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 18
150000003536 tetrazoles Chemical class 0.000 claims description 18
125000004432 carbon atom Chemical group C* 0.000 claims description 17
ZVTQYRVARPYRRE-UHFFFAOYSA-N oxadiazol-4-one Chemical compound O=C1CON=N1 ZVTQYRVARPYRRE-UHFFFAOYSA-N 0.000 claims description 16
YDCVQGAUCOROHB-UHFFFAOYSA-N oxadiazolidine-4,5-dione Chemical compound O=C1NNOC1=O YDCVQGAUCOROHB-UHFFFAOYSA-N 0.000 claims description 16
FKASFBLJDCHBNZ-UHFFFAOYSA-N 1,3,4-oxadiazole Chemical compound C1=NN=CO1 FKASFBLJDCHBNZ-UHFFFAOYSA-N 0.000 claims description 15
BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 claims description 15
BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 claims description 15
IGAVZWMNOPFOCW-UHFFFAOYSA-N 2h-1,2,4-thiadiazol-5-one Chemical compound O=C1NC=NS1 IGAVZWMNOPFOCW-UHFFFAOYSA-N 0.000 claims description 14
AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims description 14
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RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims description 14
FUOSTELFLYZQCW-UHFFFAOYSA-N 1,2-oxazol-3-one Chemical compound OC=1C=CON=1 FUOSTELFLYZQCW-UHFFFAOYSA-N 0.000 claims description 13
CZSRXHJVZUBEGW-UHFFFAOYSA-N 1,2-thiazolidine Chemical compound C1CNSC1 CZSRXHJVZUBEGW-UHFFFAOYSA-N 0.000 claims description 13
WRYCSMQKUKOKBP-UHFFFAOYSA-N Imidazolidine Chemical compound C1CNCN1 WRYCSMQKUKOKBP-UHFFFAOYSA-N 0.000 claims description 13
125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims description 13
DNXIASIHZYFFRO-UHFFFAOYSA-N pyrazoline Chemical compound C1CN=NC1 DNXIASIHZYFFRO-UHFFFAOYSA-N 0.000 claims description 13
125000003831 tetrazolyl group Chemical group 0.000 claims description 13
VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 claims description 13
125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 claims description 12
HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims description 12
KDCGOANMDULRCW-UHFFFAOYSA-N 7H-purine Chemical compound N1=CNC2=NC=NC2=C1 KDCGOANMDULRCW-UHFFFAOYSA-N 0.000 claims description 12
YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 12
MTNDZQHUAFNZQY-UHFFFAOYSA-N imidazoline Chemical compound C1CN=CN1 MTNDZQHUAFNZQY-UHFFFAOYSA-N 0.000 claims description 12
USPWKWBDZOARPV-UHFFFAOYSA-N pyrazolidine Chemical compound C1CNNC1 USPWKWBDZOARPV-UHFFFAOYSA-N 0.000 claims description 12
WTSXVIMLKCKWIW-UHFFFAOYSA-N 3h-1,3,4-oxadiazol-2-one Chemical compound O=C1NN=CO1 WTSXVIMLKCKWIW-UHFFFAOYSA-N 0.000 claims description 11
YSVFAMDLJASIGW-UHFFFAOYSA-N 5h-1,2,3,5-oxathiadiazole 2-oxide Chemical compound O=S1NC=NO1 YSVFAMDLJASIGW-UHFFFAOYSA-N 0.000 claims description 11
LFSXCDWNBUNEEM-UHFFFAOYSA-N phthalazine Chemical compound C1=NN=CC2=CC=CC=C21 LFSXCDWNBUNEEM-UHFFFAOYSA-N 0.000 claims description 11
JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 claims description 11
UWYZHKAOTLEWKK-UHFFFAOYSA-N 1,2,3,4-tetrahydroisoquinoline Chemical compound C1=CC=C2CNCCC2=C1 UWYZHKAOTLEWKK-UHFFFAOYSA-N 0.000 claims description 10
LBUJPTNKIBCYBY-UHFFFAOYSA-N 1,2,3,4-tetrahydroquinoline Chemical compound C1=CC=C2CCCNC2=C1 LBUJPTNKIBCYBY-UHFFFAOYSA-N 0.000 claims description 10
125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 10
RSEBUVRVKCANEP-UHFFFAOYSA-N 2-pyrroline Chemical compound C1CC=CN1 RSEBUVRVKCANEP-UHFFFAOYSA-N 0.000 claims description 10
206010061218 Inflammation Diseases 0.000 claims description 10
MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims description 10
125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 10
230000004054 inflammatory process Effects 0.000 claims description 10
ZVJHJDDKYZXRJI-UHFFFAOYSA-N pyrroline Natural products C1CC=NC1 ZVJHJDDKYZXRJI-UHFFFAOYSA-N 0.000 claims description 10
229960001153 serine Drugs 0.000 claims description 10
229930192474 thiophene Natural products 0.000 claims description 10
MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims description 9
229910052799 carbon Inorganic materials 0.000 claims description 9
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 9
229910052731 fluorine Inorganic materials 0.000 claims description 9
125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 9
FFSJPOPLSWBGQY-UHFFFAOYSA-N triazol-4-one Chemical compound O=C1C=NN=N1 FFSJPOPLSWBGQY-UHFFFAOYSA-N 0.000 claims description 9
FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 claims description 8
239000004475 Arginine Substances 0.000 claims description 8
DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims description 8
XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims description 8
ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims description 8
DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims description 8
ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims description 8
KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims description 8
AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims description 8
QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 claims description 8
KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims description 8
239000004472 Lysine Substances 0.000 claims description 8
239000004473 Threonine Substances 0.000 claims description 8
QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims description 8
235000009697 arginine Nutrition 0.000 claims description 8
ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims description 8
229960003121 arginine Drugs 0.000 claims description 8
235000009582 asparagine Nutrition 0.000 claims description 8
229960001230 asparagine Drugs 0.000 claims description 8
IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical compound C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 claims description 8
125000004122 cyclic group Chemical group 0.000 claims description 8
XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims description 8
235000018417 cysteine Nutrition 0.000 claims description 8
235000004554 glutamine Nutrition 0.000 claims description 8
ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 claims description 8
235000018977 lysine Nutrition 0.000 claims description 8
125000001624 naphthyl group Chemical group 0.000 claims description 8
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 8
AIFRHYZBTHREPW-UHFFFAOYSA-N β-carboline Chemical compound N1=CC=C2C3=CC=CC=C3NC2=C1 AIFRHYZBTHREPW-UHFFFAOYSA-N 0.000 claims description 8
WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims description 7
WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims description 7
AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims description 7
208000005298 acute pain Diseases 0.000 claims description 7
150000005840 aryl radicals Chemical class 0.000 claims description 7
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 7
235000013922 glutamic acid Nutrition 0.000 claims description 7
239000004220 glutamic acid Substances 0.000 claims description 7
150000002460 imidazoles Chemical class 0.000 claims description 7
229920006395 saturated elastomer Polymers 0.000 claims description 7
OYIFNHCXNCRBQI-UHFFFAOYSA-N 2-aminoadipic acid Chemical compound OC(=O)C(N)CCCC(O)=O OYIFNHCXNCRBQI-UHFFFAOYSA-N 0.000 claims description 6
RDFMDVXONNIGBC-UHFFFAOYSA-N 2-aminoheptanoic acid Chemical compound CCCCCC(N)C(O)=O RDFMDVXONNIGBC-UHFFFAOYSA-N 0.000 claims description 6
PECYZEOJVXMISF-UHFFFAOYSA-N 3-aminoalanine Chemical compound [NH3+]CC(N)C([O-])=O PECYZEOJVXMISF-UHFFFAOYSA-N 0.000 claims description 6
208000000094 Chronic Pain Diseases 0.000 claims description 6
229930194542 Keto Natural products 0.000 claims description 6
CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims description 6
HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims description 6
KSPIYJQBLVDRRI-UHFFFAOYSA-N N-methylisoleucine Chemical compound CCC(C)C(NC)C(O)=O KSPIYJQBLVDRRI-UHFFFAOYSA-N 0.000 claims description 6
239000002253 acid Substances 0.000 claims description 6
QWCKQJZIFLGMSD-UHFFFAOYSA-N alpha-aminobutyric acid Chemical compound CCC(N)C(O)=O QWCKQJZIFLGMSD-UHFFFAOYSA-N 0.000 claims description 6
125000005428 anthryl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C3C(*)=C([H])C([H])=C([H])C3=C([H])C2=C1[H] 0.000 claims description 6
235000003704 aspartic acid Nutrition 0.000 claims description 6
229960005261 aspartic acid Drugs 0.000 claims description 6
OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims description 6
XVOYSCVBGLVSOL-UHFFFAOYSA-N cysteic acid Chemical compound OC(=O)C(N)CS(O)(=O)=O XVOYSCVBGLVSOL-UHFFFAOYSA-N 0.000 claims description 6
PMMYEEVYMWASQN-UHFFFAOYSA-N dl-hydroxyproline Natural products OC1C[NH2+]C(C([O-])=O)C1 PMMYEEVYMWASQN-UHFFFAOYSA-N 0.000 claims description 6
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229910052740 iodine Inorganic materials 0.000 claims description 6
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IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 5
235000008206 alpha-amino acids Nutrition 0.000 claims description 5
229910052801 chlorine Inorganic materials 0.000 claims description 5
239000000460 chlorine Substances 0.000 claims description 5
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125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 5
PMJHHCWVYXUKFD-UHFFFAOYSA-N piperylene Natural products CC=CC=C PMJHHCWVYXUKFD-UHFFFAOYSA-N 0.000 claims description 5
238000002560 therapeutic procedure Methods 0.000 claims description 5
LRANPJDWHYRCER-UHFFFAOYSA-N 1,2-diazepine Chemical compound N1C=CC=CC=N1 LRANPJDWHYRCER-UHFFFAOYSA-N 0.000 claims description 4
125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 claims description 4
206010019233 Headaches Diseases 0.000 claims description 4
230000001154 acute effect Effects 0.000 claims description 4
150000001371 alpha-amino acids Chemical class 0.000 claims description 4
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229910052794 bromium Inorganic materials 0.000 claims description 4
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 4
WCZVZNOTHYJIEI-UHFFFAOYSA-N cinnoline Chemical compound N1=NC=CC2=CC=CC=C21 WCZVZNOTHYJIEI-UHFFFAOYSA-N 0.000 claims description 4
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208000004296 neuralgia Diseases 0.000 claims description 4
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Classifications

- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
- 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
- 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
- A61K31/403—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 condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- 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
- A61K31/41—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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
- 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
- A61K31/41—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
- A61K31/4245—Oxadiazoles
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents

Landscapes

Health & Medical Sciences (AREA)
General Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Public Health (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Epidemiology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Organic Chemistry (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Pain & Pain Management (AREA)
Rheumatology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Paper (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

OA1200500046A 2002-08-17 2003-08-05 Use of IKB-kinase inhibitors for the treatment of pain. OA12907A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
DE10237723A DE10237723A1 (de)	2002-08-17	2002-08-17	Verwendung von IKappaB-Kinase Inhibitoren in der Schmerztherapie

Publications (1)

Publication Number	Publication Date
OA12907A true OA12907A (en)	2006-10-13

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OA1200500046A OA12907A (en)	2002-08-17	2003-08-05	Use of IKB-kinase inhibitors for the treatment of pain.

Country Status (33)

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EP (1)	EP1531819B1 (fr)
JP (1)	JP4504811B2 (fr)
KR (2)	KR20110135428A (fr)
CN (1)	CN100398107C (fr)
AR (1)	AR043045A1 (fr)
AT (1)	ATE418336T1 (fr)
AU (1)	AU2003271555B2 (fr)
BR (1)	BR0313555A (fr)
CA (1)	CA2495455C (fr)
CO (1)	CO5690585A2 (fr)
CR (1)	CR7716A (fr)
CY (1)	CY1108874T1 (fr)
DE (2)	DE10237723A1 (fr)
DK (1)	DK1531819T3 (fr)
EC (1)	ECSP055609A (fr)
ES (1)	ES2320118T3 (fr)
HR (1)	HRP20050041B1 (fr)
IL (1)	IL166780A (fr)
MA (1)	MA27334A1 (fr)
MX (1)	MXPA05001218A (fr)
MY (1)	MY138059A (fr)
NO (1)	NO334309B1 (fr)
OA (1)	OA12907A (fr)
PL (1)	PL212356B1 (fr)
PT (1)	PT1531819E (fr)
RS (1)	RS51878B (fr)
RU (1)	RU2320338C2 (fr)
SI (1)	SI1531819T1 (fr)
TN (1)	TNSN05044A1 (fr)
TW (1)	TWI325782B (fr)
UA (1)	UA80837C2 (fr)
WO (1)	WO2004022057A1 (fr)
ZA (1)	ZA200500323B (fr)

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US7718644B2 (en)	2004-01-22	2010-05-18	The Trustees Of Columbia University In The City Of New York	Anti-arrhythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2) and uses thereof
DE10237722A1 (de) *	2002-08-17	2004-08-19	Aventis Pharma Deutschland Gmbh	Indol- oder Benzimidazolderivate zur Modulation der IKappaB-Kinase
US7544678B2 (en)	2002-11-05	2009-06-09	The Trustees Of Columbia University In The City Of New York	Anti-arrythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2)
JP2007525165A (ja)	2003-03-07	2007-09-06	トラスティーズ・オブ・コロンビア・ユニバーシティ・イン・ザ・シティ・オブ・ニューヨーク	タイプ１ライアノジン受容体に基づく方法
US8710045B2 (en)	2004-01-22	2014-04-29	The Trustees Of Columbia University In The City Of New York	Agents for preventing and treating disorders involving modulation of the ryanodine receptors
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US7781478B2 (en)	2004-07-14	2010-08-24	Ptc Therapeutics, Inc.	Methods for treating hepatitis C
JP2008506702A (ja)	2004-07-14	2008-03-06	ピーティーシーセラピューティクス，インコーポレーテッド	Ｃ型肝炎を治療するための方法
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US7704990B2 (en)	2005-08-25	2010-04-27	The Trustees Of Columbia University In The City Of New York	Agents for preventing and treating disorders involving modulation of the RyR receptors
EP2025674A1 (fr)	2007-08-15	2009-02-18	sanofi-aventis	Tetrahydronaphthaline substituée, son procédé de fabrication et son utilisation en tant que médicament
AR072297A1 (es)	2008-06-27	2010-08-18	Novartis Ag	Derivados de indol-2-il-piridin-3-ilo, composicion farmaceutica que los comprende y su uso en medicamentos para el tratamiento de enfermedades mediadas por la sintasa aldosterona.
WO2011107494A1 (fr)	2010-03-03	2011-09-09	Sanofi	Nouveaux dérivés aromatiques de glycoside, médicaments contenants ces composés, et leur utilisation
EP2582709B1 (fr)	2010-06-18	2018-01-24	Sanofi	Dérivés d'azolopyridin-3-one en tant qu'inhibiteurs de lipases et de phospholipases
TW201221505A (en)	2010-07-05	2012-06-01	Sanofi Sa	Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215388A (en)	2010-07-05	2012-04-16	Sanofi Sa	(2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en)	2010-07-05	2012-04-16	Sanofi Aventis	Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
JP5790440B2 (ja)	2010-12-01	2015-10-07	住友化学株式会社	ピリミジン化合物およびその有害生物防除用途
US8828994B2 (en)	2011-03-08	2014-09-09	Sanofi	Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
EP2766349B1 (fr)	2011-03-08	2016-06-01	Sanofi	Dérivés d'oxathiazine substitués par des carbocycles ou des hétérocycles, leur procédé de préparation, médicaments contenant ces composés et leur utilisation
EP2683704B1 (fr)	2011-03-08	2014-12-17	Sanofi	Dérivés oxathiazine ramifiés, procédé pour leur préparation, utilisation en tant que médicament, agents pharmaceutiques contenant ces dérivés et leur utilisation
US8710050B2 (en)	2011-03-08	2014-04-29	Sanofi	Di and tri- substituted oxathiazine derivatives, method for the production, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
US8871758B2 (en)	2011-03-08	2014-10-28	Sanofi	Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof
EP2532755A1 (fr) *	2011-06-10	2012-12-12	Sanofi-Aventis	Procédés et utilisations basés sur l'expression de Slfn2 et liés à l'identification et au profilage de composés pour une utilisation dans le traitement ou la prévention de la douleur
WO2013045413A1 (fr)	2011-09-27	2013-04-04	Sanofi	Dérivés d'amide d'acide 6-(4-hydroxyphényl)-3-alkyl-1h-pyrazolo[3,4-b] pyridine-4-carboxylique utilisés comme inhibiteurs de kinase
WO2013083553A1 (fr)	2011-12-06	2013-06-13	Sanofi	Formes cristallines du [(s)-1-carbamoyl-2-(phénylpyrimidin-2-ylamino)éthyl]amide de l'acide 2-(2-méthylaminopyrimidin-4-yl)-1h-indole-5-carboxylique
EP2805705B1 (fr)	2013-05-23	2016-11-09	IP Gesellschaft für Management mbH	Emballage comprenant des unités d'administration des sels de sodium de l'acide (R)-3-[6-amino-pyridin-3-yl]-2-(1-cyclohexyl-1 H-imidazol-4-yl)-propionique
JO3425B1 (ar)	2013-07-15	2019-10-20	Novartis Ag	مشتقات البابيريدينيل-اندول واستخدامها كعامل متمم لمثبطات b
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PT1194425E (pt) *	1999-06-23	2005-10-31	Aventis Pharma Gmbh	Benzimidazoles substituidos
DE19951360A1 (de) *	1999-10-26	2001-05-03	Aventis Pharma Gmbh	Substituierte Indole
DE10237722A1 (de) *	2002-08-17	2004-08-19	Aventis Pharma Deutschland Gmbh	Indol- oder Benzimidazolderivate zur Modulation der IKappaB-Kinase

2002
- 2002-08-17 DE DE10237723A patent/DE10237723A1/de not_active Withdrawn
2003
- 2003-05-08 UA UAA200502388A patent/UA80837C2/uk unknown
- 2003-08-05 SI SI200331531T patent/SI1531819T1/sl unknown
- 2003-08-05 AU AU2003271555A patent/AU2003271555B2/en not_active Ceased
- 2003-08-05 PL PL373568A patent/PL212356B1/pl unknown
- 2003-08-05 CN CNB038195429A patent/CN100398107C/zh not_active Expired - Fee Related
- 2003-08-05 EP EP03753349A patent/EP1531819B1/fr not_active Expired - Lifetime
- 2003-08-05 BR BR0313555-1A patent/BR0313555A/pt not_active Application Discontinuation
- 2003-08-05 MX MXPA05001218A patent/MXPA05001218A/es active IP Right Grant
- 2003-08-05 DE DE50310980T patent/DE50310980D1/de not_active Expired - Lifetime
- 2003-08-05 CA CA2495455A patent/CA2495455C/fr not_active Expired - Fee Related
- 2003-08-05 DK DK03753349T patent/DK1531819T3/da active
- 2003-08-05 JP JP2004533318A patent/JP4504811B2/ja not_active Expired - Fee Related
- 2003-08-05 OA OA1200500046A patent/OA12907A/en unknown
- 2003-08-05 KR KR1020117028345A patent/KR20110135428A/ko not_active Withdrawn
- 2003-08-05 WO PCT/EP2003/008628 patent/WO2004022057A1/fr not_active Ceased
- 2003-08-05 HR HRP20050041AA patent/HRP20050041B1/hr not_active IP Right Cessation
- 2003-08-05 AT AT03753349T patent/ATE418336T1/de active
- 2003-08-05 KR KR1020057002712A patent/KR101119845B1/ko not_active Expired - Fee Related
- 2003-08-05 RS YU20050070A patent/RS51878B/sr unknown
- 2003-08-05 PT PT03753349T patent/PT1531819E/pt unknown
- 2003-08-05 RU RU2005107419/15A patent/RU2320338C2/ru not_active IP Right Cessation
- 2003-08-05 ES ES03753349T patent/ES2320118T3/es not_active Expired - Lifetime
- 2003-08-14 AR ARP030102944A patent/AR043045A1/es not_active Application Discontinuation
- 2003-08-14 TW TW092122310A patent/TWI325782B/zh not_active IP Right Cessation
- 2003-08-15 MY MYPI20033112A patent/MY138059A/en unknown
2005
- 2005-01-13 ZA ZA200500323A patent/ZA200500323B/xx unknown
- 2005-02-09 IL IL166780A patent/IL166780A/en not_active IP Right Cessation
- 2005-02-15 MA MA28107A patent/MA27334A1/fr unknown
- 2005-02-15 CO CO05013333A patent/CO5690585A2/es not_active Application Discontinuation
- 2005-02-16 TN TNP2005000044A patent/TNSN05044A1/en unknown
- 2005-02-17 EC EC2005005609A patent/ECSP055609A/es unknown
- 2005-03-07 CR CR7716A patent/CR7716A/es unknown
- 2005-03-15 NO NO20051339A patent/NO334309B1/no not_active IP Right Cessation
2009
- 2009-03-17 CY CY20091100291T patent/CY1108874T1/el unknown

Also Published As

Publication number	Publication date
HRP20050041A2 (hr)	2006-04-30
BR0313555A (pt)	2005-07-12
HRP20050041B1 (hr)	2013-07-31
EP1531819B1 (fr)	2008-12-24
PT1531819E (pt)	2009-02-18
SI1531819T1 (sl)	2009-06-30
KR20110135428A (ko)	2011-12-16
MY138059A (en)	2009-04-30
ATE418336T1 (de)	2009-01-15
AU2003271555A1 (en)	2004-03-29
KR101119845B1 (ko)	2012-02-28
MA27334A1 (fr)	2005-05-02
JP2005539053A (ja)	2005-12-22
CA2495455C (fr)	2011-01-11
CA2495455A1 (fr)	2004-03-18
TW200417370A (en)	2004-09-16
KR20050058339A (ko)	2005-06-16
WO2004022057A1 (fr)	2004-03-18
HK1079426A1 (en)	2006-04-07
CN1674899A (zh)	2005-09-28
ZA200500323B (en)	2006-02-22
NO20051339L (no)	2005-05-03
CY1108874T1 (el)	2014-07-02
CR7716A (es)	2008-11-25
PL212356B1 (pl)	2012-09-28
RS51878B (sr)	2012-02-29
NO334309B1 (no)	2014-02-03
CN100398107C (zh)	2008-07-02
EP1531819A1 (fr)	2005-05-25
RU2005107419A (ru)	2005-08-10
DE10237723A1 (de)	2004-07-08
ECSP055609A (es)	2005-04-18
AR043045A1 (es)	2005-07-13
MXPA05001218A (es)	2005-05-16
TNSN05044A1 (en)	2007-05-14
JP4504811B2 (ja)	2010-07-14
CO5690585A2 (es)	2006-10-31
AU2003271555B2 (en)	2009-03-26
PL373568A1 (en)	2005-09-05
ES2320118T3 (es)	2009-05-19
DE50310980D1 (de)	2009-02-05
UA80837C2 (uk)	2007-11-12
RS20050070A (sr)	2007-06-04
DK1531819T3 (da)	2009-04-20
IL166780A (en)	2011-11-30
IL166780A0 (en)	2006-01-15
TWI325782B (en)	2010-06-11
RU2320338C2 (ru)	2008-03-27

Publication	Publication Date	Title
OA12907A (en)	2006-10-13	Use of IKB-kinase inhibitors for the treatment of pain.
US8809358B2 (en)	2014-08-19	Use of IκB-kinase inhibitors in pain therapy
EP1261601B1 (fr)	2009-07-29	Indols substitues pour moduler l'activite du facteur de transcription nfkb
DE10237722A1 (de)	2004-08-19	Indol- oder Benzimidazolderivate zur Modulation der IKappaB-Kinase
RS50340B (sr)	2009-11-10	Supstituisani benzimidazoli
NZ538297A (en)	2007-02-23	Use of IkB kinase inhibitors for the treatment of pain
HK1079426B (en)	2009-07-31	USE OF IκB KINASE INHIBITORS FOR THE TREATMENT OF PAIN
RU2415134C9 (ru)	2011-05-27	Способ лечения или профилактики физиологических и/или патофизиологических состояний, опосредуемых рецепторами, стимулирующими секрецию гормона роста, триазолы и фармацевтическая композиция на их основе