JPWO2020038435A5 - - Google Patents
Download PDFInfo
- Publication number
- JPWO2020038435A5 JPWO2020038435A5 JP2021509988A JP2021509988A JPWO2020038435A5 JP WO2020038435 A5 JPWO2020038435 A5 JP WO2020038435A5 JP 2021509988 A JP2021509988 A JP 2021509988A JP 2021509988 A JP2021509988 A JP 2021509988A JP WO2020038435 A5 JPWO2020038435 A5 JP WO2020038435A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- cooh
- compound according
- propyl
- 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.)
- Granted
Links
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 15
- -1 frill Chemical group 0.000 claims 15
- 239000002207 metabolite Substances 0.000 claims 9
- 150000001204 N-oxides Chemical class 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 239000000651 prodrug Substances 0.000 claims 6
- 229940002612 prodrug Drugs 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims 3
- 208000002193 Pain Diseases 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 125000001624 naphthyl group Chemical group 0.000 claims 3
- 125000002971 oxazolyl group Chemical group 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000000168 pyrrolyl group Chemical group 0.000 claims 3
- 125000005493 quinolyl group Chemical group 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000003831 tetrazolyl group Chemical group 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 125000001544 thienyl group Chemical group 0.000 claims 3
- 125000001425 triazolyl group Chemical group 0.000 claims 3
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 2
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 2
- 208000019901 Anxiety disease Diseases 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 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
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000005936 piperidyl group Chemical group 0.000 claims 2
- 125000004368 propenyl group Chemical group C(=CC)* 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 208000007848 Alcoholism Diseases 0.000 claims 1
- 201000004384 Alopecia Diseases 0.000 claims 1
- 208000000044 Amnesia Diseases 0.000 claims 1
- 206010002942 Apathy Diseases 0.000 claims 1
- 208000036487 Arthropathies Diseases 0.000 claims 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 206010008874 Chronic Fatigue Syndrome Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 1
- 206010020710 Hyperphagia Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 241000208125 Nicotiana Species 0.000 claims 1
- 235000002637 Nicotiana tabacum Nutrition 0.000 claims 1
- 206010029897 Obsessive thoughts Diseases 0.000 claims 1
- 206010034912 Phobia Diseases 0.000 claims 1
- 208000008348 Post-Concussion Syndrome Diseases 0.000 claims 1
- 206010036618 Premenstrual syndrome Diseases 0.000 claims 1
- 206010041250 Social phobia Diseases 0.000 claims 1
- 230000003213 activating effect Effects 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 201000007930 alcohol dependence Diseases 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 230000036528 appetite Effects 0.000 claims 1
- 235000019789 appetite Nutrition 0.000 claims 1
- 208000030963 borderline personality disease Diseases 0.000 claims 1
- 230000001066 destructive effect Effects 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 208000024963 hair loss Diseases 0.000 claims 1
- 230000003676 hair loss Effects 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 201000001881 impotence Diseases 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 230000000938 luteal effect Effects 0.000 claims 1
- 230000006984 memory degeneration Effects 0.000 claims 1
- 208000023060 memory loss Diseases 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 208000029766 myalgic encephalomeyelitis/chronic fatigue syndrome Diseases 0.000 claims 1
- 230000002981 neuropathic effect Effects 0.000 claims 1
- 208000019899 phobic disease Diseases 0.000 claims 1
- 230000002028 premature Effects 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- GECHUMIMRBOMGK-UHFFFAOYSA-N sulfapyridine Chemical compound C1=CC(N)=CC=C1S(=O)(=O)NC1=CC=CC=N1 GECHUMIMRBOMGK-UHFFFAOYSA-N 0.000 claims 1
- 229960002211 sulfapyridine Drugs 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 208000004371 toothache Diseases 0.000 claims 1
Claims (15)
Lは、-C(=O)-、-C(=S)-又は-S(=O)2-であり、
R1は、C1～C6アルキル、C3～C8シクロアルキル、3～8員のヘテロシクリル、C6～C10アリール又は5～10員のヘテロアリールであり、R1は、R1a、R1b、R1c、R1d及びR1eから独立して選択される1つ、2つ、3つ、4つ又は5つの置換基により場合により置換されており、
R1a、R1b、R1c、R1d及びR1eはそれぞれ、独立して、H、F、Cl、Br、I、-CN、-NO2、-NH2、-OH、-SH、-COOH、-C(=O)NH2、-C(=O)NHCH3、-C(=O)N(CH3)2、-C(=O)-(C1～C6アルキル)、-C(=O)-(C1～C6アルコキシ)、C1～C6アルキル、C2～C6アルケニル、C2～C6アルキニル、C1～C6ハロアルキル、C1～C6アルコキシ、C1～C6ハロアルコキシ、C1～C6アルキルチオ、C1～C6アルキルアミノ、ヒドロキシ-置換C1～C6アルキル、C3～C8シクロアルキル、3～8員のヘテロシクリル、C6～C10アリール又は5～10員のヘテロアリールであり、
R2は、H、F、Cl、Br、I、-CN、-NO2、-NH2、-OH、-COOH、-C(=O)NH2、C1～C6アルキル、C1～C6ハロアルキル、C1～C6アルコキシ、C1～C6ハロアルコキシ又はヒドロキシ-置換C1～C6アルキルであり、
R3、R4及びR5はそれぞれ、独立して、H、F、Cl、Br、I、-CN、-NO2、-NH2、-OH、-COOH、-C(=O)NH2、C1～C6アルキル、C1～C6ハロアルキル、C1～C6アルコキシ、C1～C6ハロアルコキシ又はヒドロキシ-置換C1～C6アルキルであり、
R6は、H、F、Cl、Br又はIであり、
R7は、H、F、Cl、Br、I、-CN、-NO2、-NH2、-OH、-COOH、-C(=O)NH2、C1～C6アルキル、C1～C6ハロアルキル、C1～C6アルコキシ、C1～C6ハロアルコキシ又はヒドロキシ-置換C1～C6アルキルであり、
R8は、H、F、Cl、Br、I、-CN、-NO2、-NH2、-OH、-SH、-COOH、-C(=O)NH2、-C(=O)NHCH3、-C(=O)N(CH3)2、-C(=O)-(C1～C6アルキル)、-C(=O)-(C1～C6アルコキシ)、C1～C6アルキル、C2～C6アルケニル、C2～C6アルキニル、C1～C6ハロアルキル、C1～C6アルコキシ、C1～C6ハロアルコキシ、C1～C6アルキルチオ、C1～C6アルキルアミノ、ヒドロキシ-置換C1～C6アルキル、C3～C8シクロアルキル、3～8員のヘテロシクリル、C6～C10アリール又は5～10員のヘテロアリールである)。 Compounds having formula (I), or their stereoisomers, metavariants, N-oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs:
L is -C (= O)-, -C (= S)-or -S (= O) 2- ,
R 1 is C 1 to C 6 alkyl, C 3 to C 8 cycloalkyl, 3 to 8 membered heterocyclyl, C 6 to C 10 aryl or 5 to 10 membered heteroaryl, and R 1 is R 1a , It is optionally substituted with one, two, three, four or five substituents independently selected from R 1b , R 1c , R 1d and R 1e .
R 1a , R 1b , R 1c , R 1d and R 1e are independent of H, F, Cl, Br, I, -CN, -NO 2 , -NH 2 , -OH, -SH, -COOH, respectively. , -C (= O) NH 2 , -C (= O) NHCH 3 , -C (= O) N (CH 3 ) 2 , -C (= O)-(C 1 to C 6 alkyl), -C (= O)-(C 1 to C 6 alkoxy), C 1 to C 6 alkyl, C 2 to C 6 alkenyl, C 2 to C 6 alkynyl, C 1 to C 6 haloalkyl, C 1 to C 6 alkoxy, C 1 to C 6 haloalkoxy, C 1 to C 6 alkylthio, C 1 to C 6 alkylamino, hydroxy-substituted C 1 to C 6 alkyl, C 3 to C 8 cycloalkyl, 3 to 8 member heterocyclyl, C 6 to C 10 aryl or 5-10 membered heteroaryl,
R 2 is H, F, Cl, Br, I, -CN, -NO 2 , -NH 2 , -OH, -COOH, -C (= O) NH 2 , C 1 to C 6 alkyl, C 1 to C 6 haloalkyl, C 1 to C 6 alkoxy, C 1 to C 6 haloalkoxy or hydroxy-substituted C 1 to C 6 alkyl.
R 3 , R 4 and R 5 are independently H, F, Cl, Br, I, -CN, -NO 2 , -NH 2 , -OH, -COOH, -C (= O) NH 2 , C 1 to C 6 alkyl, C 1 to C 6 haloalkyl, C 1 to C 6 alkoxy, C 1 to C 6 haloalkoxy or hydroxy-substituted C 1 to C 6 alkyl.
R 6 is H, F, Cl, Br or I,
R 7 is H, F, Cl, Br, I, -CN, -NO 2 , -NH 2 , -OH, -COOH, -C (= O) NH 2 , C 1 to C 6 alkyl, C 1 to C 6 haloalkyl, C 1 to C 6 alkoxy, C 1 to C 6 haloalkoxy or hydroxy-substituted C 1 to C 6 alkyl.
R 8 is H, F, Cl, Br, I, -CN, -NO 2 , -NH 2 , -OH, -SH, -COOH, -C (= O) NH 2 , -C (= O) NHCH 3 , -C (= O) N (CH 3 ) 2 , -C (= O)-(C 1 to C 6 alkyl), -C (= O)-(C 1 to C 6 alkoxy), C 1 to C 6 alkyl, C 2 to C 6 alkoxy, C 2 to C 6 alkynyl, C 1 to C 6 haloalkyl, C 1 to C 6 alkoxy, C 1 to C 6 haloalkoxy, C 1 to C 6 alkylthio, C 1 to C 6 alkylamino, hydroxy-substituted C 1 to C 6 alkyl, C 3 to C 8 cycloalkyl, 3 to 8 membered heterocyclyl, C 6 to C 10 aryl or 5 to 10 membered heteroaryl).
R1a、R1b、R1c、R1d及びR1eがそれぞれ、独立して、H、F、Cl、Br、I、-CN、-NO2、-NH2、-OH、-SH、-COOH、-C(=O)NH2、-C(=O)NHCH3、-C(=O)N(CH3)2、-C(=O)-(C1～C4アルキル)、-C(=O)-(C1～C4アルコキシ)、C1～C4アルキル、C2～C4アルケニル、C2～C4アルキニル、C1～C4ハロアルキル、C1～C4アルコキシ、C1～C4ハロアルコキシ、C1～C4アルキルチオ、C1～C4アルキルアミノ、ヒドロキシ-置換C1～C4アルキル、C3～C6シクロアルキル、3～6員のヘテロシクリル、C6～C10アリール又は5～10員のヘテロアリールである、
請求項1に記載の化合物。 R 1 is C 1 to C 4 alkyl, C 3 to C 6 cycloalkyl, 3 to 6 member heterocyclyl, C 6 to C 10 aryl or 5 to 10 member heteroaryl, and R 1 is R 1a , It is optionally substituted with one, two, three, four or five substituents independently selected from R 1b , R 1c , R 1d and R 1e .
R 1a , R 1b , R 1c , R 1d and R 1e are independent of H, F, Cl, Br, I, -CN, -NO 2 , -NH 2 , -OH, -SH, -COOH, respectively. , -C (= O) NH 2 , -C (= O) NHCH 3 , -C (= O) N (CH 3 ) 2 , -C (= O)-(C 1 to C 4 alkyl), -C (= O)-(C 1 to C 4 alkoxy), C 1 to C 4 alkyl, C 2 to C 4 alkenyl, C 2 to C 4 alkynyl, C 1 to C 4 haloalkyl, C 1 to C 4 alkoxy, C 1 to C 4 haloalkoxy, C 1 to C 4 alkylthio, C 1 to C 4 alkylamino, hydroxy-substituted C 1 to C 4 alkyl, C 3 to C 6 cycloalkyl, 3 to 6 member heterocyclyl, C 6 to C 10 aryl or 5-10 membered heteroaryl,
The compound according to claim 1.
R1a、R1b、R1c、R1d及びR1eがそれぞれ、独立して、H、F、Cl、Br、I、-CN、-NO2、-NH2、-OH、-SH、-COOH、-C(=O)NH2、-C(=O)NHCH3、-C(=O)N(CH3)2、-C(=O)-CH3、-C(=O)-OCH3、メチル、エチル、n-プロピル、i-プロピル、アリル、プロペニル、プロパルギル、プロピニル、-CHF2、-CF3、-CHFCH2F、-CF2CHF2、-CH2CF3、-CH2CF2CHF2、メトキシ、エトキシ、n-プロポキシ、i-プロポキシ、-OCHF2、-OCF3、-OCHFCH2F、-OCF2CHF2、-OCH2CF3、-OCH2CF2CHF2、メチルチオ、エチルチオ、メチルアミノ、ジメチルアミノ、エチルアミノ、ヒドロキシメチル、2-ヒドロキシエチル、シクロプロピル、シクロブチル、シクロペンチル、シクロヘキシル、アゼチジニル、ピロリジニル、テトラヒドロフラニル、ピペリジル、ピペラジニル、モルホリニル、フェニル、インデニル、ナフチル、ピロリル、ピラゾリル、イミダゾリル、トリアゾリル、テトラゾリル、フラニル、チエニル、チアゾリル、オキサゾリル、ピリジル、ピリミジル、ピラジニル、ピリダジル、ベンゾイミダゾリル、インドリル又はキノリルである、
請求項1又は2に記載の化合物。 R 1 is phenyl, indenyl, naphthyl, pyrrolyl, pyrazolyl, imidazolyl, triazolyl, tetrazolyl, frill, thienyl, thiazolyl, oxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzoimidazolyl, indrill or quinolyl, and R 1 is R 1a . , R 1b , R 1c , R 1d and R 1e , optionally substituted with one, two, three, four or five substituents.
R 1a , R 1b , R 1c , R 1d and R 1e are independent of H, F, Cl, Br, I, -CN, -NO 2 , -NH 2 , -OH, -SH, -COOH, respectively. , -C (= O) NH 2 , -C (= O) NHCH 3 , -C (= O) N (CH 3 ) 2 , -C (= O) -CH 3 , -C (= O) -OCH 3 , Methyl, Ethyl, n-propyl, i-propyl, Allyl, Propenyl, Propyl, Propinyl, -CHF 2 , -CF 3 , -CHFCH 2 F, -CF 2 CHF 2 , -CH 2 CF 3 , -CH 2 CF 2 CHF 2 , methoxy, ethoxy, n-propoxy, i-propoxy, -OCHF 2 , -OCF 3 , -OCHFCH 2 F, -OCF 2 CHF 2 , -OCH 2 CF 3 , -OCH 2 CF 2 CHF 2 , Methylthio, ethylthio, methylamino, dimethylamino, ethylamino, hydroxymethyl, 2-hydroxyethyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, azetidinyl, pyrrolidinyl, tetrahydrofuranyl, piperidyl, piperazinyl, morpholinyl, phenyl, indenyl, naphthyl, pyrrolyl , Pyrazolyl, imidazolyl, triazolyl, tetrazolyl, furanyl, thienyl, thiazolyl, oxazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazol, benzoimidazolyl, indrill or quinolyl.
The compound according to claim 1 or 2.
R3、R4及びR5がそれぞれ、独立して、H、F、Cl、Br、I、-CN、-NO2、-NH2、-OH、-COOH、-C(=O)NH2、C1～C4アルキル、C1～C4ハロアルキル、C1～C4アルコキシ、C1～C4ハロアルコキシ又はヒドロキシ-置換C1～C4アルキルであり、
R7が、H、F、Cl、Br、I、-CN、-NO2、-NH2、-OH、-COOH、-C(=O)NH2、C1～C4アルキル、C1～C4ハロアルキル、C1～C4アルコキシ、C1～C4ハロアルコキシ又はヒドロキシ-置換C1～C4アルキルである、
請求項1から3のいずれか一項に記載の化合物。 R 2 is H, F, Cl, Br, I, -CN, -NO 2 , -NH 2 , -OH, -COOH, -C (= O) NH 2 , C 1 to C 4 alkyl, C 1 to C 4 haloalkyl, C 1 to C 4 alkoxy, C 1 to C 4 haloalkoxy or hydroxy-substituted C 1 to C 4 alkyl.
R 3 , R 4 and R 5 are independently H, F, Cl, Br, I, -CN, -NO 2 , -NH 2 , -OH, -COOH, -C (= O) NH 2 , C 1 to C 4 alkyl, C 1 to C 4 haloalkyl, C 1 to C 4 alkoxy, C 1 to C 4 haloalkoxy or hydroxy-substituted C 1 to C 4 alkyl.
R 7 is H, F, Cl, Br, I, -CN, -NO 2 , -NH 2 , -OH, -COOH, -C (= O) NH 2 , C 1 to C 4 alkyl, C 1 to C 4 haloalkyl, C 1 to C 4 alkoxy, C 1 to C 4 haloalkoxy or hydroxy-substituted C 1 to C 4 alkyl,
The compound according to any one of claims 1 to 3.
R3、R4及びR5がそれぞれ、独立して、H、F、Cl、Br、I、-CN、-NO2、-NH2、-OH、-COOH、-C(=O)NH2、メチル、エチル、n-プロピル、i-プロピル、-CF3、-CH2CF3、メトキシ、エトキシ、n-プロポキシ又はi-プロポキシであり、
R7が、H、F、Cl、Br、I、-CN、-NO2、-NH2、-OH、-COOH、-C(=O)NH2、メチル、エチル、n-プロピル、i-プロピル、-CF3、-CH2CF3、メトキシ、エトキシ、n-プロポキシ又はi-プロポキシである、
請求項1から4のいずれか一項に記載の化合物。 R 2 is H, F, Cl, Br, I, -CN, -NO 2 , -NH 2 , -OH, -COOH, -C (= O) NH 2 , methyl, ethyl, n-propyl, i- Propyl, -CF 3 , -CH 2 CF 3 , methoxy, ethoxy, n-propoxy or i-propoxy,
R 3 , R 4 and R 5 are independently H, F, Cl, Br, I, -CN, -NO 2 , -NH 2 , -OH, -COOH, -C (= O) NH 2 , Methyl, ethyl, n-propyl, i-propyl, -CF 3 , -CH 2 CF 3 , methoxy, ethoxy, n-propoxy or i-propoxy,
R 7 is H, F, Cl, Br, I, -CN, -NO 2 , -NH 2 , -OH, -COOH, -C (= O) NH 2 , methyl, ethyl, n-propyl, i- Propyl, -CF 3 , -CH 2 CF 3 , methoxy, ethoxy, n-propoxy or i-propoxy,
The compound according to any one of claims 1 to 4.
薬学的に許容される添加剤、担体若しくはジュバント又はそれらの組合せを場合により更に含む、医薬組成物。 Contains the compound according to any one of claims 1 to 12.
A pharmaceutical composition, optionally further comprising a pharmaceutically acceptable additive, carrier or juvant or a combination thereof.
前記5-HT 1F 受容体関連疾患が、偏頭痛、一般疼痛、三叉神経痛、歯痛又は顎関節機能障害疼痛、自閉症、強迫観念、恐怖症、うつ病、社会恐怖症、不安症、全般性不安障害、睡眠の障害、外傷後症候群、慢性疲労症候群、月経前症候群又は後期黄体期症候群、境界型人格障害、破壊的行動障害、衝動制御障害、注意欠陥多動性障害、アルコール依存症、タバコ乱用症、無言症、抜毛癖、過食症、神経性食欲不振症、早漏、勃起機能不全、記憶喪失又は認知症である、医薬組成物。 The compound according to any one of claims 1 to 12 or the pharmaceutical composition according to claim 13 for use in the prevention, treatment or alleviation of 5-HT 1F receptor-related diseases in a subject .
The 5-HT 1F receptor-related diseases include migraine, general pain, trigeminal pain, tooth pain or jaw joint dysfunction pain, autism, obsession, phobia, depression, social phobia, anxiety, and generality. Anxiety disorders, sleep disorders, post-traumatic syndrome, chronic fatigue syndrome, premenstrual syndrome or late luteal syndrome, borderline personality disorders, destructive behavior disorders, impulsive control disorders, attention deficit hyperactivity disorders, alcohol dependence, tobacco A pharmaceutical composition that is abusive, apathy, hair loss, hyperphagia, neuropathic appetite, premature leakage, erectile dysfunction, memory loss or dementia .
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810969837 | 2018-08-24 | ||
| CN201810969837.5 | 2018-08-24 | ||
| PCT/CN2019/101985 WO2020038435A1 (en) | 2018-08-24 | 2019-08-22 | Pyridinylmethylenepiperidine derivatives and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021536433A JP2021536433A (en) | 2021-12-27 |
| JPWO2020038435A5 true JPWO2020038435A5 (en) | 2022-07-04 |
| JP7405834B2 JP7405834B2 (en) | 2023-12-26 |
Family
ID=68437065
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021509988A Active JP7405834B2 (en) | 2018-08-24 | 2019-08-22 | Pyridinylmethylenepiperidine derivatives and their uses |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US11858910B2 (en) |
| EP (1) | EP3841096A4 (en) |
| JP (1) | JP7405834B2 (en) |
| CN (1) | CN110437205B (en) |
| AU (1) | AU2019323450A1 (en) |
| CA (1) | CA3107145A1 (en) |
| WO (1) | WO2020038435A1 (en) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111187252B (en) * | 2019-11-22 | 2023-06-09 | 广东东阳光药业有限公司 | Pyridinoyl azaspiroheptane derivatives and their use |
| CN111187251B (en) * | 2019-11-22 | 2023-06-09 | 广东东阳光药业有限公司 | Pyridinoylpiperidine derivatives and their use |
| CN111943930B (en) * | 2020-08-25 | 2022-11-01 | 南京三元阳普医药科技有限公司 | Synthesis process of Lasmidinan |
| CN114685441B (en) * | 2020-12-29 | 2023-07-18 | 广东东阳光药业有限公司 | Salts of pyridyleiperidine derivatives and uses thereof |
| EP4271671A1 (en) * | 2020-12-29 | 2023-11-08 | Sunshine Lake Pharma Co., Ltd. | Salts of pyridinylmethylenepiperidine derivatives and uses thereof |
| CN114685443B (en) * | 2020-12-29 | 2023-07-18 | 广东东阳光药业有限公司 | Salts of pyridyleiperidine derivatives and uses thereof |
| CN114685444B (en) * | 2020-12-29 | 2023-07-18 | 广东东阳光药业有限公司 | Salts of pyridyleiperidine derivatives and uses thereof |
| CN114685440B (en) * | 2020-12-29 | 2023-07-18 | 广东东阳光药业有限公司 | Salts of pyridyleiperidine derivatives and uses thereof |
| CN112898276A (en) * | 2021-02-02 | 2021-06-04 | 深圳市第二人民医院(深圳市转化医学研究院) | Chalcone derivative and application thereof |
| CN112939952A (en) * | 2021-02-02 | 2021-06-11 | 深圳市第二人民医院(深圳市转化医学研究院) | 3-hydroxy chalcone derivative and application thereof |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA979961B (en) | 1996-11-15 | 1999-05-05 | Lilly Co Eli | 5-HT1F agonists |
| US6133290A (en) | 1998-07-31 | 2000-10-17 | Eli Lilly And Company | 5-HT1F agonists |
| US6777428B1 (en) | 1999-02-10 | 2004-08-17 | Eli Lilly And Company | 5-HT1f agonist |
| TWI263497B (en) | 2002-03-29 | 2006-10-11 | Lilly Co Eli | Pyridinoylpiperidines as 5-HT1F agonists |
| JP2006523692A (en) * | 2003-04-18 | 2006-10-19 | イーライ リリー アンド カンパニー | (Piperidinyloxy) phenyl, (piperidinyloxy) pyridinyl, (piperidinylsulfanyl) phenyl, and (piperidinylsulfanyl) pyridinyl compounds as 5-HT1F agonists |
| UA82711C2 (en) * | 2003-09-12 | 2008-05-12 | Эли Лилли Энд Компани | Substituted 2-carbonylamino-6-piperidinaminopyridines and substituted 1-carbonylamino-3-piperidinaminobenzenes as 5-ht1f agonists |
| CA2549007A1 (en) | 2003-12-17 | 2005-07-07 | Eli Lilly And Company | Substituted (4-aminocyclohexen-1-yl)phenyl and (4-aminocyclohexen-1-yl)pyridinyl compounds as 5-ht1f agonists |
| MX2009004233A (en) * | 2006-10-18 | 2009-08-12 | Pfizer Prod Inc | Biaryl ether urea compounds. |
| CN101602708B (en) | 2008-06-10 | 2012-11-21 | 江苏国华投资有限公司 | Aryl alkanol piperidine derivative and application thereof as antidepressive medicine |
| TW201028421A (en) | 2009-01-15 | 2010-08-01 | Abbott Lab | Novel benzenesulfonamides as calcium channel blockers |
| GB201114448D0 (en) | 2011-08-22 | 2011-10-05 | Takeda Pharmaceutical | Compounds and their use |
| CN107001259B (en) | 2014-08-27 | 2019-12-06 | 豪夫迈·罗氏有限公司 | Substituted azetidine derivatives as TAAR ligands |
| GB201416513D0 (en) * | 2014-09-18 | 2014-11-05 | Astex Therapeutics Ltd And Cancer Res Technology Ltd | Pharmaceutical compounds |
-
2019
- 2019-08-22 CA CA3107145A patent/CA3107145A1/en active Pending
- 2019-08-22 JP JP2021509988A patent/JP7405834B2/en active Active
- 2019-08-22 US US17/263,177 patent/US11858910B2/en active Active
- 2019-08-22 AU AU2019323450A patent/AU2019323450A1/en active Pending
- 2019-08-22 CN CN201910778613.0A patent/CN110437205B/en active Active
- 2019-08-22 WO PCT/CN2019/101985 patent/WO2020038435A1/en unknown
- 2019-08-22 EP EP19851618.9A patent/EP3841096A4/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2023027269A5 (en) | ||
| JPWO2020038435A5 (en) | ||
| JP2022034029A5 (en) | ||
| RU2498983C2 (en) | Phenylaminopyrimidine compounds and uses thereof | |
| CA2565852A1 (en) | 3- or 4-monosubstituted phenol and thiophenol derivatives useful as h3 ligands | |
| JP2017530199A5 (en) | ||
| JP2018527336A5 (en) | ||
| JP2020505356A5 (en) | ||
| JP2016526576A5 (en) | ||
| JP2012236838A5 (en) | ||
| JP2017525757A5 (en) | ||
| JP2018528192A5 (en) | ||
| JP2012519693A5 (en) | ||
| RU2009126624A (en) | 2- (PIPERIDIN-4-IL) -4-PHENOXY-OR Phenylinopyrimidine Derivatives as Non-nucleoside Inhibitors of Reverse Transcriptase | |
| RU2010120682A (en) | HISTONDESECETHYLASE INHIBITORS | |
| JP2013523710A5 (en) | ||
| JPWO2020033828A5 (en) | ||
| JP2018522823A5 (en) | ||
| CA2526866A1 (en) | Substituted 3-sulfur indoles for treating a disease mediated by crth2 | |
| TW201443057A (en) | Organic compounds | |
| RU2007101236A (en) | NEW HYDANTOINE DERIVATIVES FOR TREATMENT OF OBSTRUCTIVE RESPIRATORY DISEASES | |
| JP2009520021A5 (en) | ||
| JP2017501237A5 (en) | ||
| RU2011149360A (en) | SUBSTITUTED Phenylureas and Phenylamides as Vanilloid Receptor Ligands | |
| RU2006126974A (en) | AMID DERIVATIVE AND MEDICINE |