JP2008537741A5 - - Google Patents
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- Publication number
- JP2008537741A5 JP2008537741A5 JP2008503245A JP2008503245A JP2008537741A5 JP 2008537741 A5 JP2008537741 A5 JP 2008537741A5 JP 2008503245 A JP2008503245 A JP 2008503245A JP 2008503245 A JP2008503245 A JP 2008503245A JP 2008537741 A5 JP2008537741 A5 JP 2008537741A5
- Authority
- JP
- Japan
- Prior art keywords
- triazabicyclo
- trien
- deca
- adamantyl
- acetamide
- Prior art date
- Legal status (The legal status 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 status listed.)
- Withdrawn
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- -1 amino, cyano, sulfo, sulfanyl Chemical group 0.000 claims 585
- CKBZJTAMRPPVSR-UHFFFAOYSA-N adamantane-1-carboxamide Chemical compound C1C(C2)CC3CC2CC1(C(=O)N)C3 CKBZJTAMRPPVSR-UHFFFAOYSA-N 0.000 claims 217
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 190
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 121
- 150000001875 compounds Chemical class 0.000 claims 47
- 150000003857 carboxamides Chemical class 0.000 claims 29
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 27
- 239000008194 pharmaceutical composition Substances 0.000 claims 19
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 18
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 18
- 125000004210 cyclohexylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 16
- 208000004296 neuralgia Diseases 0.000 claims 16
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 15
- 208000002193 Pain Diseases 0.000 claims 13
- 125000003118 aryl group Chemical group 0.000 claims 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims 13
- 125000002252 acyl group Chemical group 0.000 claims 12
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 12
- 201000010099 disease Diseases 0.000 claims 12
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 11
- 125000001475 halogen functional group Chemical group 0.000 claims 11
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 11
- 125000001424 substituent group Chemical group 0.000 claims 11
- 206010061218 Inflammation Diseases 0.000 claims 10
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 10
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 10
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 230000004054 inflammatory process Effects 0.000 claims 10
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 9
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 9
- 125000000547 substituted alkyl group Chemical group 0.000 claims 9
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 8
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 8
- 125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims 7
- 208000023275 Autoimmune disease Diseases 0.000 claims 7
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims 7
- 125000003107 substituted aryl group Chemical group 0.000 claims 7
- 125000006833 (C1-C5) alkylene group Chemical group 0.000 claims 6
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 6
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 6
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 6
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 6
- 208000020925 Bipolar disease Diseases 0.000 claims 6
- 208000014644 Brain disease Diseases 0.000 claims 6
- 208000003251 Pruritus Diseases 0.000 claims 6
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 6
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 6
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 208000037765 diseases and disorders Diseases 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- 125000004404 heteroalkyl group Chemical group 0.000 claims 6
- 230000001404 mediated effect Effects 0.000 claims 6
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 6
- 150000003457 sulfones Chemical class 0.000 claims 6
- 150000003462 sulfoxides Chemical class 0.000 claims 6
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 5
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 5
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims 5
- 206010029240 Neuritis Diseases 0.000 claims 5
- 125000004442 acylamino group Chemical group 0.000 claims 5
- 125000003282 alkyl amino group Chemical group 0.000 claims 5
- 125000004947 alkyl aryl amino group Chemical group 0.000 claims 5
- 125000004414 alkyl thio group Chemical group 0.000 claims 5
- 125000003710 aryl alkyl group Chemical group 0.000 claims 5
- 125000004663 dialkyl amino group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 5
- 208000021722 neuropathic pain Diseases 0.000 claims 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 5
- 201000008482 osteoarthritis Diseases 0.000 claims 5
- 125000001476 phosphono group Chemical group [H]OP(*)(=O)O[H] 0.000 claims 5
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 5
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 5
- 208000024891 symptom Diseases 0.000 claims 5
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 5
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims 4
- 125000003762 3,4-dimethoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C(OC([H])([H])[H])C([H])=C1* 0.000 claims 4
- 208000019695 Migraine disease Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 208000018737 Parkinson disease Diseases 0.000 claims 4
- 206010043269 Tension headache Diseases 0.000 claims 4
- 208000008548 Tension-Type Headache Diseases 0.000 claims 4
- DGYIJVNZSDYBOE-UHFFFAOYSA-N [CH2]C1=CC=NC=C1 Chemical group [CH2]C1=CC=NC=C1 DGYIJVNZSDYBOE-UHFFFAOYSA-N 0.000 claims 4
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 4
- 150000001408 amides Chemical class 0.000 claims 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims 4
- 150000001540 azides Chemical class 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 claims 4
- 206010015037 epilepsy Diseases 0.000 claims 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 4
- 238000001727 in vivo Methods 0.000 claims 4
- 208000014674 injury Diseases 0.000 claims 4
- 206010027599 migraine Diseases 0.000 claims 4
- 210000002307 prostate Anatomy 0.000 claims 4
- 208000023504 respiratory system disease Diseases 0.000 claims 4
- 208000004371 toothache Diseases 0.000 claims 4
- 125000003287 1H-imidazol-4-ylmethyl group Chemical group [H]N1C([H])=NC(C([H])([H])[*])=C1[H] 0.000 claims 3
- 125000006479 2-pyridyl methyl group Chemical group [H]C1=C([H])C([H])=C([H])C(=N1)C([H])([H])* 0.000 claims 3
- VTXNOVCTHUBABW-UHFFFAOYSA-N 3,4-dichlorobenzoyl chloride Chemical group ClC(=O)C1=CC=C(Cl)C(Cl)=C1 VTXNOVCTHUBABW-UHFFFAOYSA-N 0.000 claims 3
- 125000002981 3-(trifluoromethyl)benzoyl group Chemical group FC(C=1C=C(C(=O)*)C=CC1)(F)F 0.000 claims 3
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 3
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims 3
- 208000019901 Anxiety disease Diseases 0.000 claims 3
- 201000001320 Atherosclerosis Diseases 0.000 claims 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 3
- 208000000094 Chronic Pain Diseases 0.000 claims 3
- 208000006561 Cluster Headache Diseases 0.000 claims 3
- 208000030814 Eating disease Diseases 0.000 claims 3
- 208000034347 Faecal incontinence Diseases 0.000 claims 3
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 3
- 206010019233 Headaches Diseases 0.000 claims 3
- 206010020751 Hypersensitivity Diseases 0.000 claims 3
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 3
- 206010065390 Inflammatory pain Diseases 0.000 claims 3
- 206010022998 Irritability Diseases 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 3
- 208000008589 Obesity Diseases 0.000 claims 3
- 201000004681 Psoriasis Diseases 0.000 claims 3
- 206010039085 Rhinitis allergic Diseases 0.000 claims 3
- 206010046543 Urinary incontinence Diseases 0.000 claims 3
- 206010046851 Uveitis Diseases 0.000 claims 3
- 208000027418 Wounds and injury Diseases 0.000 claims 3
- 230000001154 acute effect Effects 0.000 claims 3
- 208000005298 acute pain Diseases 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 201000009961 allergic asthma Diseases 0.000 claims 3
- 208000026935 allergic disease Diseases 0.000 claims 3
- 201000010105 allergic rhinitis Diseases 0.000 claims 3
- 230000036506 anxiety Effects 0.000 claims 3
- 206010003246 arthritis Diseases 0.000 claims 3
- 208000006673 asthma Diseases 0.000 claims 3
- 208000028683 bipolar I disease Diseases 0.000 claims 3
- 230000036772 blood pressure Effects 0.000 claims 3
- 229910052794 bromium Inorganic materials 0.000 claims 3
- 208000018912 cluster headache syndrome Diseases 0.000 claims 3
- 208000010877 cognitive disease Diseases 0.000 claims 3
- 210000001072 colon Anatomy 0.000 claims 3
- NKLCHDQGUHMCGL-UHFFFAOYSA-N cyclohexylidenemethanone Chemical group O=C=C1CCCCC1 NKLCHDQGUHMCGL-UHFFFAOYSA-N 0.000 claims 3
- 230000006378 damage Effects 0.000 claims 3
- 235000014632 disordered eating Nutrition 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 230000004064 dysfunction Effects 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 206010014599 encephalitis Diseases 0.000 claims 3
- 150000002148 esters Chemical class 0.000 claims 3
- 231100000869 headache Toxicity 0.000 claims 3
- 230000009610 hypersensitivity Effects 0.000 claims 3
- 230000002757 inflammatory effect Effects 0.000 claims 3
- 230000007803 itching Effects 0.000 claims 3
- 150000002632 lipids Chemical class 0.000 claims 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- 201000006417 multiple sclerosis Diseases 0.000 claims 3
- 208000010125 myocardial infarction Diseases 0.000 claims 3
- 230000000926 neurological effect Effects 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 239000000651 prodrug Substances 0.000 claims 3
- 229940002612 prodrug Drugs 0.000 claims 3
- 150000003254 radicals Chemical class 0.000 claims 3
- 102000005962 receptors Human genes 0.000 claims 3
- 108020003175 receptors Proteins 0.000 claims 3
- 230000008085 renal dysfunction Effects 0.000 claims 3
- 230000000241 respiratory effect Effects 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 201000000980 schizophrenia Diseases 0.000 claims 3
- 208000019116 sleep disease Diseases 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 208000020431 spinal cord injury Diseases 0.000 claims 3
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 3
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 3
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 3
- 229940124530 sulfonamide Drugs 0.000 claims 3
- 150000003456 sulfonamides Chemical class 0.000 claims 3
- 230000000472 traumatic effect Effects 0.000 claims 3
- 210000003932 urinary bladder Anatomy 0.000 claims 3
- 125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 claims 2
- 125000006276 2-bromophenyl group Chemical group [H]C1=C([H])C(Br)=C(*)C([H])=C1[H] 0.000 claims 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 2
- QOXOZONBQWIKDA-UHFFFAOYSA-N 3-hydroxypropyl Chemical group [CH2]CCO QOXOZONBQWIKDA-UHFFFAOYSA-N 0.000 claims 2
- 125000006201 3-phenylpropyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 2
- 206010006482 Bronchospasm Diseases 0.000 claims 2
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 claims 2
- 208000021965 Glossopharyngeal Nerve disease Diseases 0.000 claims 2
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 2
- 208000018569 Respiratory Tract disease Diseases 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 230000007885 bronchoconstriction Effects 0.000 claims 2
- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000004851 cyclopentylmethyl group Chemical group C1(CCCC1)C* 0.000 claims 2
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 2
- 230000006806 disease prevention Effects 0.000 claims 2
- 206010013990 dysuria Diseases 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 201000005442 glossopharyngeal neuralgia Diseases 0.000 claims 2
- 125000005226 heteroaryloxycarbonyl group Chemical group 0.000 claims 2
- 201000001119 neuropathy Diseases 0.000 claims 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- IZWHQUZOPBEYKY-AATRIKPKSA-N (e)-3-[4-[[4-[[2-(1-adamantyl)acetyl]amino]-6,8-dihydro-5h-pyrido[3,4-d]pyrimidin-7-yl]methyl]phenyl]prop-2-enoic acid Chemical compound C1=CC(/C=C/C(=O)O)=CC=C1CN1CC(N=CN=C2NC(=O)CC34CC5CC(CC(C5)C3)C4)=C2CC1 IZWHQUZOPBEYKY-AATRIKPKSA-N 0.000 claims 1
- 125000000980 1H-indol-3-ylmethyl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C(C([H])([H])[*])C2=C1[H] 0.000 claims 1
- 125000000579 2,2-diphenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(C1=C([H])C([H])=C([H])C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000001617 2,3-dimethoxy phenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C(OC([H])([H])[H])=C1[H] 0.000 claims 1
- 125000006334 2,4-difluoro benzoyl group Chemical group [H]C1=C([H])C(C(*)=O)=C(F)C([H])=C1F 0.000 claims 1
- 125000004098 2,6-dichlorobenzoyl group Chemical group O=C([*])C1=C(Cl)C([H])=C([H])C([H])=C1Cl 0.000 claims 1
- GXKAVGBEDMNAHX-UHFFFAOYSA-N 2-(1-adamantyl)-n-(7-benzyl-6,8-dihydro-5h-1,7-naphthyridin-4-yl)acetamide Chemical compound C1C(C2)CC(C3)CC2CC13CC(=O)NC(C=1CC2)=CC=NC=1CN2CC1=CC=CC=C1 GXKAVGBEDMNAHX-UHFFFAOYSA-N 0.000 claims 1
- RIVCPBYSDNUPTD-UHFFFAOYSA-N 2-(1-adamantyl)-n-[2-[(4-fluorophenyl)methyl]-1h-isoquinolin-5-yl]acetamide Chemical compound C1=CC(F)=CC=C1CN1C=CC2=C(NC(=O)CC34CC5CC(CC(C5)C3)C4)C=CC=C2C1 RIVCPBYSDNUPTD-UHFFFAOYSA-N 0.000 claims 1
- 125000003070 2-(2-chlorophenyl)ethyl group Chemical group [H]C1=C([H])C(Cl)=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000002995 2-(trifluoromethyl)benzoyl group Chemical group FC(C1=C(C(=O)*)C=CC=C1)(F)F 0.000 claims 1
- 125000003541 2-chlorobenzoyl group Chemical group ClC1=C(C(=O)*)C=CC=C1 0.000 claims 1
- 125000006176 2-ethylbutyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(C([H])([H])*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000005916 2-methylpentyl group Chemical group 0.000 claims 1
- 125000001216 2-naphthoyl group Chemical group C1=C(C=CC2=CC=CC=C12)C(=O)* 0.000 claims 1
- 125000006275 3-bromophenyl group Chemical group [H]C1=C([H])C(Br)=C([H])C(*)=C1[H] 0.000 claims 1
- 125000002999 4-(trifluoromethyl)benzoyl group Chemical group FC(C1=CC=C(C(=O)*)C=C1)(F)F 0.000 claims 1
- 125000001999 4-Methoxybenzoyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1OC([H])([H])[H])C(*)=O 0.000 claims 1
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims 1
- 125000000242 4-chlorobenzoyl group Chemical group ClC1=CC=C(C(=O)*)C=C1 0.000 claims 1
- 125000004860 4-ethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 206010003399 Arthropod bite Diseases 0.000 claims 1
- ZYUZLEUJKZZXNN-UHFFFAOYSA-N C1=CC(CC(N)C(O)=O)=CC=C1OS(=O)(=O)C1=CC=C(C=CC=C2)C2=C1 Chemical group C1=CC(CC(N)C(O)=O)=CC=C1OS(=O)(=O)C1=CC=C(C=CC=C2)C2=C1 ZYUZLEUJKZZXNN-UHFFFAOYSA-N 0.000 claims 1
- 208000001387 Causalgia Diseases 0.000 claims 1
- 206010008334 Cervicobrachial syndrome Diseases 0.000 claims 1
- 208000023890 Complex Regional Pain Syndromes Diseases 0.000 claims 1
- 208000013586 Complex regional pain syndrome type 1 Diseases 0.000 claims 1
- 208000001640 Fibromyalgia Diseases 0.000 claims 1
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims 1
- 206010020880 Hypertrophy Diseases 0.000 claims 1
- 208000006877 Insect Bites and Stings Diseases 0.000 claims 1
- 206010049949 Intercostal neuralgia Diseases 0.000 claims 1
- 206010049567 Miller Fisher syndrome Diseases 0.000 claims 1
- 208000002472 Morton Neuroma Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 206010068106 Occipital neuralgia Diseases 0.000 claims 1
- 208000004983 Phantom Limb Diseases 0.000 claims 1
- 206010056238 Phantom pain Diseases 0.000 claims 1
- 206010036105 Polyneuropathy Diseases 0.000 claims 1
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims 1
- 201000001947 Reflex Sympathetic Dystrophy Diseases 0.000 claims 1
- 208000008765 Sciatica Diseases 0.000 claims 1
- 206010040744 Sinus headache Diseases 0.000 claims 1
- 208000004078 Snake Bites Diseases 0.000 claims 1
- 208000003589 Spider Bites Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- WLYPBMBWKYALCG-UHFFFAOYSA-N [2,4-bis(trifluoromethyl)phenyl]boronic acid Chemical group OB(O)C1=CC=C(C(F)(F)F)C=C1C(F)(F)F WLYPBMBWKYALCG-UHFFFAOYSA-N 0.000 claims 1
- ZUSWDTWYONAOPH-UHFFFAOYSA-N [2-(trifluoromethyl)phenyl]hydrazine;hydrochloride Chemical group [Cl-].[NH3+]NC1=CC=CC=C1C(F)(F)F ZUSWDTWYONAOPH-UHFFFAOYSA-N 0.000 claims 1
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 150000007513 acids Chemical class 0.000 claims 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000004619 benzopyranyl group Chemical group O1C(C=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000004622 benzoxazinyl group Chemical group O1NC(=CC2=C1C=CC=C2)* 0.000 claims 1
- 230000002146 bilateral effect Effects 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 229960002504 capsaicin Drugs 0.000 claims 1
- 235000017663 capsaicin Nutrition 0.000 claims 1
- 230000035606 childbirth Effects 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 208000014439 complex regional pain syndrome type 2 Diseases 0.000 claims 1
- 208000012790 cranial neuralgia Diseases 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 239000007789 gas Substances 0.000 claims 1
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Families Citing this family (89)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE447572T1 (de) * | 2005-01-26 | 2009-11-15 | Hoffmann La Roche | Phenylmethanonderivate und ihre verwendung als glycin-transporter-1-hemmer |
| WO2007002701A2 (en) * | 2005-06-27 | 2007-01-04 | Amgen Inc. | Anti-inflammatory aryl nitrile compounds |
| DK2774925T3 (en) | 2005-11-08 | 2017-02-27 | Vertex Pharma | Heterocyclic modulators of ATP binding cassette transporters |
| EP2001474B1 (en) * | 2006-03-16 | 2016-03-09 | Second Genome, Inc. | Bicycloheteroaryl compounds as p2x7 modulators and uses thereof |
| ES2596532T3 (es) * | 2006-03-16 | 2017-01-10 | Second Genome, Inc. | Compuestos de bicicloheteroarilo como moduladores de P2X7 y usos de los mismos |
| TWI464148B (zh) | 2006-03-16 | 2014-12-11 | Evotec Us Inc | 作為p2x7調節劑之雙環雜芳基化合物與其用途 |
| US7645789B2 (en) | 2006-04-07 | 2010-01-12 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| USRE50453E1 (en) | 2006-04-07 | 2025-06-10 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| ES2882684T3 (es) | 2006-04-07 | 2021-12-02 | Vertex Pharma | Preparación de moduladores de transportadores del casete de unión a ATP |
| US7754739B2 (en) * | 2007-05-09 | 2010-07-13 | Vertex Pharmaceuticals Incorporated | Modulators of CFTR |
| KR20090094336A (ko) * | 2006-11-27 | 2009-09-04 | 하. 룬트벡 아크티에 셀스카브 | 헤테로아릴 아미드 유도체 |
| DK2124562T3 (en) * | 2007-03-09 | 2016-08-01 | Second Genome Inc | BICYCLOHETEROARYLFORBINDELSER AS P2X7 modulators and uses thereof |
| CA2682925A1 (en) * | 2007-04-10 | 2008-10-16 | David C. Ihle | Heteroaryl amide analogues |
| CA2682692A1 (en) * | 2007-04-17 | 2008-10-30 | Renovis, Inc. | 2-cyanophenyl fused heterocyclic compounds, and compositions and uses thereof |
| NZ581259A (en) | 2007-05-09 | 2012-07-27 | Vertex Pharma | Modulators of cystic fibrosis transmembrane conductance regulator |
| WO2009019503A2 (en) * | 2007-08-03 | 2009-02-12 | Astrazeneca Ab | P2x7 antagonists for use in the treatment of mood disorders |
| CN103626744B (zh) | 2007-12-07 | 2016-05-11 | 沃泰克斯药物股份有限公司 | 3-(6-(1-(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)环丙烷甲酰氨基)-3-甲基吡啶-2-基)苯甲酸的固体形式 |
| AU2008335440B2 (en) | 2007-12-07 | 2013-11-07 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxamido-pyridine benzoic acids |
| JP5523352B2 (ja) | 2008-02-28 | 2014-06-18 | バーテックス ファーマシューティカルズ インコーポレイテッド | Cftr修飾因子としてのへテロアリール誘導体 |
| EP2105164B1 (en) | 2008-03-25 | 2011-01-12 | Affectis Pharmaceuticals AG | Novel P2X7R antagonists and their use |
| ES2376092T3 (es) * | 2008-04-22 | 2012-03-08 | Janssen Pharmaceutica, N.V. | Antagonistas de p2x7 sustituidos con quinolina o isoquinolina. |
| WO2010080503A1 (en) * | 2008-12-19 | 2010-07-15 | Genentech, Inc. | Heterocyclic compounds and methods of use |
| ATE541832T1 (de) | 2009-04-14 | 2012-02-15 | Affectis Pharmaceuticals Ag | Neuartige p2x7r-antagonisten und ihre verwendung |
| US8802868B2 (en) | 2010-03-25 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide |
| AR081069A1 (es) | 2010-04-07 | 2012-06-06 | Vertex Pharma | Formas solidas del acido 3-(6-(1-(2,2-difluorbenzo[d][1,3]dioxol-5-il)ciclopropancarboxamido)-3-metilpiridin-2-il)benzoico |
| EP2555755B2 (en) | 2010-04-07 | 2019-07-10 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyriodin-2-yl)benzoic acid and administration thereof |
| RU2569678C2 (ru) | 2010-04-22 | 2015-11-27 | Вертекс Фармасьютикалз Инкорпорейтед | Способ получения циклоалкилкарбоксамидо-индольных соединений |
| EP2386541A1 (en) | 2010-05-14 | 2011-11-16 | Affectis Pharmaceuticals AG | Novel methods for the preparation of P2X7R antagonists |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| WO2012110190A1 (en) | 2011-02-17 | 2012-08-23 | Affectis Pharmaceuticals Ag | Novel p2x7r antagonists and their use |
| WO2012163456A1 (en) | 2011-05-27 | 2012-12-06 | Affectis Pharmaceuticals Ag | Novel p2x7r antagonists and their use |
| WO2012163792A1 (en) | 2011-05-27 | 2012-12-06 | Affectis Pharmaceuticals Ag | Novel p2x7r antagonists and their use |
| MX2014000894A (es) | 2011-07-22 | 2014-02-27 | Actelion Pharmaceuticals Ltd | Derivados de amidas heterociclicas como antagonistas de receptores p2x7. |
| TWI561521B (en) * | 2011-10-14 | 2016-12-11 | Abbvie Inc | Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases |
| US9254291B2 (en) | 2011-11-08 | 2016-02-09 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| BR112014017735B1 (pt) | 2012-01-20 | 2022-06-28 | Idorsia Pharmaceuticals Ltd | Compostos derivados de amida heterocíclicos como antagonistas do receptor de p2x7, composição farmacêutica, e, uso de um composto |
| PE20190736A1 (es) | 2012-06-13 | 2019-05-23 | Incyte Holdings Corp | Compuestos triciclicos sustituidos como inhibidores del receptor del factor de crecimiento de fibroblastos (fgfr) |
| US9012496B2 (en) | 2012-07-16 | 2015-04-21 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions of (R)-1-(2,2-difluorobenzo[D][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide and administration thereof |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| EP2931717B1 (en) | 2012-12-12 | 2016-12-07 | Actelion Pharmaceuticals Ltd. | Indole carboxamide derivatives as p2x7 receptor antagonists |
| CA2891499C (en) | 2012-12-18 | 2021-07-06 | Actelion Pharmaceuticals Ltd | Indole carboxamide derivatives as p2x7 receptor antagonists |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| JP6282017B2 (ja) | 2013-01-22 | 2018-02-21 | イドーシア ファーマシューティカルズ リミテッドIdorsia Pharmaceuticals Ltd | P2x7受容体アンタゴニストとしての複素環アミド誘導体 |
| CN104918617B (zh) | 2013-01-22 | 2017-05-10 | 埃科特莱茵药品有限公司 | 作为p2x7受体拮抗剂的杂环酰胺衍生物 |
| JP6294953B2 (ja) | 2013-03-14 | 2018-03-14 | ヤンセン ファーマシューティカ エヌ.ベー. | P2x7調節物質 |
| ES2689526T3 (es) | 2013-03-14 | 2018-11-14 | Janssen Pharmaceutica Nv | Moduladores de P2X7 |
| TWI627174B (zh) | 2013-03-14 | 2018-06-21 | 比利時商健生藥品公司 | P2x7調控劑 |
| TWI599567B (zh) | 2013-03-14 | 2017-09-21 | 健生藥品公司 | P2x7調節劑 |
| KR102269032B1 (ko) | 2013-04-19 | 2021-06-24 | 인사이트 홀딩스 코포레이션 | Fgfr 저해제로서 이환식 헤테로사이클 |
| HRP20210516T2 (hr) | 2013-11-12 | 2021-10-01 | Vertex Pharmaceuticals Incorporated | Postupak proizvodnje farmaceutskih pripravaka za liječenje bolesti koje su posredovane putem cftr |
| PT3131582T (pt) | 2014-04-15 | 2018-10-08 | Vertex Pharma | Composições farmacêuticas para o tratamento de doenças mediadas pelo regulador de condutância transmembranar da fibrose quística |
| WO2016039983A1 (en) | 2014-09-12 | 2016-03-17 | Janssen Pharmaceutica Nv | P2x7 modulating n-acyl-triazolopyrazines |
| EP3191492B1 (en) | 2014-09-12 | 2019-01-09 | Janssen Pharmaceutica NV | P2x7 modulators |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| DK3221692T3 (da) | 2014-11-18 | 2021-08-23 | Vertex Pharma | Fremgangsmåde til udførsel af tests med høj kapacitet ved hjælp af højtryksvæskekromatografi |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| ES2895769T3 (es) | 2015-02-20 | 2022-02-22 | Incyte Corp | Heterociclos bicíclicos como inhibidores de FGFR |
| HK1255034A1 (zh) | 2015-07-01 | 2019-08-02 | Crinetics Pharmaceuticals, Inc. | 生长抑素调节剂及其用途 |
| CN105198810B (zh) * | 2015-07-16 | 2018-01-05 | 西安交通大学 | 2‑苄基‑1‑异喹啉酮类化合物及其合成方法和用途 |
| CN105503724B (zh) * | 2016-01-20 | 2018-01-30 | 湘潭大学 | 一种多取代2‑苄基‑1‑异喹啉酮类化合物的制备方法 |
| EP3495363B1 (en) | 2016-07-28 | 2023-08-23 | Shionogi & Co., Ltd | Nitrogen-containing condensed ring compounds having dopamine d3 receptor antagonistic effect |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| WO2019023278A1 (en) | 2017-07-25 | 2019-01-31 | Crinetics Pharmaceuticals, Inc. | MODULATORS OF SOMATOSTATIN AND USES THEREOF |
| JP7065951B2 (ja) | 2017-09-22 | 2022-05-12 | ジュビラント エピパッド エルエルシー | Pad阻害剤としての複素環式化合物 |
| WO2019077631A1 (en) | 2017-10-18 | 2019-04-25 | Jubilant Biosys Limited | IMIDAZO-PYRIDINE COMPOUNDS FOR USE AS PAD INHIBITORS |
| EP3707135A1 (en) | 2017-11-06 | 2020-09-16 | Jubilant Prodel LLC | Pyrimidine derivatives as inhibitors of pd1/pd-l1 activation |
| IL274762B2 (en) | 2017-11-24 | 2023-10-01 | Jubilant Episcribe Llc | Novel heterocyclic compounds as prmt5 inhibitors |
| KR20200112910A (ko) | 2018-01-26 | 2020-10-05 | 시오노기 앤드 컴파니, 리미티드 | 도파민 d3 수용체 길항 작용을 갖는 축환 화합물 |
| WO2019175897A1 (en) | 2018-03-13 | 2019-09-19 | Jubilant Biosys Limited | Bicyclic compounds as inhibitors of pd1/pd-l1 interaction/activation |
| SI3788047T1 (sl) | 2018-05-04 | 2024-11-29 | Incyte Corporation | Trdne oblike inhibitorja fgfr in postopki priprave le-teh |
| SG11202010882XA (en) | 2018-05-04 | 2020-11-27 | Incyte Corp | Salts of an fgfr inhibitor |
| CA3111309A1 (en) | 2018-09-28 | 2020-04-02 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| CN113164459B (zh) | 2018-09-28 | 2024-09-03 | 詹森药业有限公司 | 单酰基甘油脂肪酶调节剂 |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CA3156100A1 (en) | 2019-09-30 | 2021-04-08 | Janssen Pharmaceutica Nv | Radiolabelled mgl pet ligands |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US11607416B2 (en) | 2019-10-14 | 2023-03-21 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2021113462A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Derivatives of an fgfr inhibitor |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CA3176946A1 (en) | 2020-03-26 | 2021-09-30 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| WO2022221170A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| EP4496797A1 (en) * | 2022-03-21 | 2025-01-29 | Gasherbrum Bio, Inc. | 5,8-dihydro-1,7-naphthyridine derivatives as glp-1 agonists for the treatment of diabetes |
| CN118908892B (zh) * | 2024-07-18 | 2025-10-31 | 武汉大学 | 氨基异喹啉类衍生物及其在制备抗病毒药物中的应用 |
Family Cites Families (60)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2640829A (en) | 1950-11-10 | 1953-06-02 | Smith Kline French Lab | Isoquinolyl heterocyclic ethers |
| US3978066A (en) | 1973-11-06 | 1976-08-31 | Ayerst, Mckenna And Harrison Ltd. | Certain 4,6-dihydropyrrolotriazoline-quinoline derivatives |
| US5034393A (en) * | 1989-07-27 | 1991-07-23 | Dowelanco | Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives |
| KR920008026A (ko) | 1990-10-24 | 1992-05-27 | 오노 화아마슈티칼 캄파니 리미팃드 | 이소퀴놀리논 유도체 또는 이의 무독성 산부가염 또는 이의 수화물, 이의 제조방법 및 이를 포함하는 약제 조성물 |
| JPH04224580A (ja) | 1990-12-25 | 1992-08-13 | Nippon Soda Co Ltd | ピリミジン誘導体、その製造方法及び農園芸用殺菌剤 |
| DK0968206T3 (da) | 1997-02-19 | 2007-03-26 | Berlex Inc | N-heterocykliske derivater som NOS-inhibitorer |
| CA2307030A1 (en) | 1997-10-24 | 1999-05-06 | Mervyn Thompson | Substituted isoquinoline derivatives and their use as anticonvulsants |
| US6380193B1 (en) | 1998-05-15 | 2002-04-30 | Guilford Pharmaceuticals Inc. | Fused tricyclic compounds, methods and compositions for inhibiting PARP activity |
| GB9816984D0 (en) * | 1998-08-05 | 1998-09-30 | Smithkline Beecham Plc | Novel compounds |
| PL210415B1 (pl) | 1999-01-11 | 2012-01-31 | Agouron Pharma | Pochodne indolu, środek farmaceutyczny i zastosowanie pochodnych indolu |
| CA2366858A1 (en) | 1999-04-01 | 2000-10-12 | Margaret Yuhua Chu-Moyer | Sorbitol dehydrogenase inhibitors |
| AU1071301A (en) | 1999-11-01 | 2001-05-14 | Eli Lilly And Company | Pharmaceutical compounds |
| PL359340A1 (en) | 2000-05-19 | 2004-08-23 | Triazole derivatives | |
| AU2001296871A1 (en) | 2000-09-15 | 2002-03-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| HUP0400639A3 (en) | 2000-12-21 | 2010-03-29 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them |
| ES2241891T3 (es) | 2001-01-02 | 2005-11-01 | F. Hoffmann-La Roche Ag | Derivados de quinazolona como antagonistas de receptores adrenergicos alfa-1a/b. |
| US7105667B2 (en) | 2001-05-01 | 2006-09-12 | Bristol-Myers Squibb Co. | Fused heterocyclic compounds and use thereof |
| WO2002088079A2 (en) | 2001-05-01 | 2002-11-07 | Bristol-Myers Squibb Company | Dual inhibitors of pde 7 and pde 4 |
| WO2002094790A1 (en) | 2001-05-23 | 2002-11-28 | Mitsubishi Pharma Corporation | Fused heterocyclic compound and medicinal use thereof |
| WO2002098426A1 (en) * | 2001-06-06 | 2002-12-12 | Aventis Pharma Limtied | Substituted tetrahydroisoquinolines for use in the treatment of inflammatory diseases |
| CA2455181C (en) | 2001-08-01 | 2010-04-06 | Merck & Co., Inc. | Benzimidazo[4,5-f]isoquinolinone derivatives |
| MXPA04005510A (es) | 2001-12-07 | 2006-02-24 | Vertex Pharma | Compuestos basados en pirimidina utiles como inhibidores de gsk-3. |
| US6924290B2 (en) | 2002-01-23 | 2005-08-02 | Bayer Pharmaceuticals Corporation | Rho-kinase inhibitors |
| CA2476936A1 (en) * | 2002-02-20 | 2003-08-28 | Chih-Hung Lee | Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (vr1) receptor |
| GB0206033D0 (en) | 2002-03-14 | 2002-04-24 | Pfizer Ltd | Compounds useful in therapy |
| GB0206876D0 (en) | 2002-03-22 | 2002-05-01 | Merck Sharp & Dohme | Therapeutic agents |
| SE0200920D0 (sv) * | 2002-03-25 | 2002-03-25 | Astrazeneca Ab | Novel compounds |
| DE10215316C1 (de) | 2002-04-02 | 2003-12-18 | Schering Ag | Chinolin- und Isochinolin-Derivate, ein pharmazeutisches Mittel und ihre Verwendung als Entzündungshemmer |
| RS95404A (sr) | 2002-05-03 | 2006-10-27 | Schering Aktiengesellschaft | Tiazolidinoni i njihova primena kao inhibitora polo like kinaze |
| MY140680A (en) | 2002-05-20 | 2010-01-15 | Bristol Myers Squibb Co | Hepatitis c virus inhibitors |
| WO2003104230A1 (ja) | 2002-06-07 | 2003-12-18 | 協和醱酵工業株式会社 | 二環性ピリミジン誘導体 |
| WO2004007468A1 (en) | 2002-07-15 | 2004-01-22 | Merck & Co., Inc. | Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes |
| AU2003301443A1 (en) * | 2002-10-18 | 2004-05-04 | E.I. Du Pont De Nemours And Company | Azolecarboxamide herbicides |
| US6933311B2 (en) * | 2003-02-11 | 2005-08-23 | Abbott Laboratories | Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor |
| GB0303439D0 (en) | 2003-02-14 | 2003-03-19 | Pfizer Ltd | Antiparasitic terpene alkaloids |
| KR100751604B1 (ko) | 2003-03-03 | 2007-08-22 | 에프. 호프만-라 로슈 아게 | 5-ht6 조절자로서 사용되는 2,5- 및 2,6-치환된테트라하이드로아이소퀴놀린 |
| EP1608631A4 (en) | 2003-03-28 | 2008-08-20 | Scios Inc | BICYCLIC PYRIMIDININHIBITORS OF TGF BETA |
| GB0312609D0 (en) * | 2003-06-02 | 2003-07-09 | Astrazeneca Ab | Novel compounds |
| US7160894B2 (en) | 2003-06-06 | 2007-01-09 | Asahi Kasei Pharma Corporation | Tricyclic compound |
| CN1566099A (zh) * | 2003-06-13 | 2005-01-19 | 中国科学院上海药物研究所 | 异喹啉-1,3,4-三酮类化合物、制备方法及其用途 |
| JP2009513504A (ja) | 2003-07-02 | 2009-04-02 | エフ.ホフマン−ラ ロシュ アーゲー | 5−置換キナゾリノン誘導体 |
| AR045445A1 (es) | 2003-08-05 | 2005-10-26 | Vertex Pharma | Compuestos ihinibidores de canales ionicos regulados por voltaje |
| DE502004002403D1 (de) | 2003-10-08 | 2007-02-01 | Schering Ag | Tetrahydronaphthalinderivate, verfahren zu ihrer herstellung und ihre verwendung als entzündungshemmer |
| JP2007008816A (ja) | 2003-10-15 | 2007-01-18 | Ube Ind Ltd | 新規イソキノリン誘導体 |
| US7419978B2 (en) | 2003-10-22 | 2008-09-02 | Bristol-Myers Squibb Company | Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors |
| MY141220A (en) | 2003-11-17 | 2010-03-31 | Astrazeneca Ab | Pyrazole derivatives as inhibitors of receptor tyrosine kinases |
| US7312330B2 (en) | 2003-12-24 | 2007-12-25 | Renovis, Inc. | Bicycloheteroarylamine compounds as ion channel ligands and uses thereof |
| TW200530235A (en) | 2003-12-24 | 2005-09-16 | Renovis Inc | Bicycloheteroarylamine compounds as ion channel ligands and uses thereof |
| JP2007524673A (ja) | 2004-01-23 | 2007-08-30 | アムジエン・インコーポレーテツド | バニロイド受容体リガンドと治療におけるその使用 |
| SE0400284D0 (sv) | 2004-02-10 | 2004-02-10 | Astrazeneca Ab | Novel compounds |
| WO2005105814A1 (en) | 2004-04-28 | 2005-11-10 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
| US20050267202A1 (en) | 2004-05-19 | 2005-12-01 | Konrad Krolikiewicz | Chromanol derivatives, a process for their production and their use as anti-inflammatory agents |
| GB0420722D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| BRPI0516751A (pt) | 2004-09-30 | 2008-09-16 | Tibotec Pharm Ltd | pirimidinas bicìclicas que inibem hcv |
| DE102004055633A1 (de) | 2004-11-12 | 2006-05-18 | Schering Ag | 5-substituierte Chinolin- und Isochinolin-Derivate, ein Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer |
| JPWO2006057270A1 (ja) | 2004-11-26 | 2008-06-05 | 旭化成ファーマ株式会社 | 含窒素3環化合物 |
| US20060128710A1 (en) | 2004-12-09 | 2006-06-15 | Chih-Hung Lee | Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof |
| DE102004063227A1 (de) | 2004-12-22 | 2006-07-06 | Schering Ag | Tricylische Aminoalkohole, Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer |
| US8211929B2 (en) | 2004-12-30 | 2012-07-03 | Exelixis, Inc. | Pyrimidine derivatives as kinase modulators and method of use |
| ES2596532T3 (es) * | 2006-03-16 | 2017-01-10 | Second Genome, Inc. | Compuestos de bicicloheteroarilo como moduladores de P2X7 y usos de los mismos |
-
2006
- 2006-03-17 US US11/384,045 patent/US7297700B2/en not_active Expired - Fee Related
- 2006-03-17 US US11/384,199 patent/US7402596B2/en not_active Expired - Fee Related
- 2006-03-24 WO PCT/US2006/010774 patent/WO2006102588A1/en not_active Ceased
- 2006-03-24 CA CA002602718A patent/CA2602718A1/en not_active Abandoned
- 2006-03-24 EP EP06739589A patent/EP1860942A4/en not_active Withdrawn
- 2006-03-24 JP JP2008503245A patent/JP2008537741A/ja not_active Withdrawn
- 2006-03-24 CA CA002602717A patent/CA2602717A1/en not_active Abandoned
- 2006-03-24 EP EP06739520A patent/EP1865774A4/en not_active Withdrawn
- 2006-03-24 MX MX2007011855A patent/MX2007011855A/es active IP Right Grant
- 2006-03-24 MX MX2007011854A patent/MX2007011854A/es active IP Right Grant
- 2006-03-24 WO PCT/US2006/010880 patent/WO2006102610A2/en not_active Ceased
- 2006-03-24 JP JP2008503223A patent/JP2008534511A/ja not_active Withdrawn
-
2007
- 2007-07-03 US US11/773,106 patent/US20080039478A1/en not_active Abandoned
-
2008
- 2008-07-16 US US12/218,620 patent/US20090170838A1/en not_active Abandoned
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