JP2008517913A5 - - Google Patents
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- JP2008517913A5 JP2008517913A5 JP2007537951A JP2007537951A JP2008517913A5 JP 2008517913 A5 JP2008517913 A5 JP 2008517913A5 JP 2007537951 A JP2007537951 A JP 2007537951A JP 2007537951 A JP2007537951 A JP 2007537951A JP 2008517913 A5 JP2008517913 A5 JP 2008517913A5
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- JP
- Japan
- Prior art keywords
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- compound according
- compound
- amino
- thieno
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000000166 1,3-dioxalanyl group Chemical group 0.000 claims 1
- APVXECALWXWTBQ-UHFFFAOYSA-N 3-amino-5-chloro-N-cyclopropyl-4-methyl-6-(2-morpholin-4-ylethoxy)thieno[2,3-b]pyridine-2-carboxamide Chemical compound N=1C=2SC(C(=O)NC3CC3)=C(N)C=2C(C)=C(Cl)C=1OCCN1CCOCC1 APVXECALWXWTBQ-UHFFFAOYSA-N 0.000 claims 1
- NJBOUQLKCGARJL-UHFFFAOYSA-N 3-amino-5-chloro-N-cyclopropyl-4-methyl-6-oxo-7H-thieno[2,3-b]pyridine-2-carboxamide Chemical compound NC=1C=2C(C)=C(Cl)C(O)=NC=2SC=1C(=O)NC1CC1 NJBOUQLKCGARJL-UHFFFAOYSA-N 0.000 claims 1
- CTEGQKDJTBWFHW-UHFFFAOYSA-N 3-amino-5-chloro-N-cyclopropyl-6-methoxy-4-methylthieno[2,3-b]pyridine-2-carboxamide Chemical compound NC=1C=2C(C)=C(Cl)C(OC)=NC=2SC=1C(=O)NC1CC1 CTEGQKDJTBWFHW-UHFFFAOYSA-N 0.000 claims 1
- ZUUXEGXLNZNKNQ-UHFFFAOYSA-N C1(CC1)NC(=O)C1=CC=2C(=NC=CC=2)S1 Chemical group C1(CC1)NC(=O)C1=CC=2C(=NC=CC=2)S1 ZUUXEGXLNZNKNQ-UHFFFAOYSA-N 0.000 claims 1
- 102000014415 Muscarinic acetylcholine receptor family Human genes 0.000 claims 1
- 108050003473 Muscarinic acetylcholine receptor family Proteins 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Claims (13)
- 式(I)の化合物、又はその薬学的に許容される塩。
(式中、mは1又は2であり、nは0、1又は2であり、Xは結合、−O−、−SOp−、−C(O)−、−NR2−、−C(O)−NR2−、又は−NR2−C(O)−であり、pは0、1又は2であり;
R1は、水素原子、ヒドロキシル基、C1−C4アルキル基、フェニル基、ピリジル基、ピロリジニル基、ピペラジニル基、モルフォリノ基、チアゾリル基、イミダゾリル基又は1,3−ジオキサラニル基であり、フェニル基、ピペラジニル基又はチアゾリル基は、ハロゲン原子又はC1−C2アルキル基からなる群から選択される1つの置換基によって、任意に置換されてよく、pが0であるとき、又はXが−O−、−NR2、若しくは−NR2−C(O)−であるときはnが0でなく;
R2は水素原子又はC1−C2アルキル基であり、C1−C2アルキル基は、1つのヒドロキシル基によって任意に置換されてよい。) - Xが結合である、請求項1記載の化合物。
- nが0である、請求項1又は2のいずれか一項記載の化合物。
- mが1である、請求項1から3のいずれか一項記載の化合物。
- R1が水素原子である、請求項4記載の化合物。
- mが2である、請求項1から3のいずれか一項記載の化合物。
- R1がモルフォリノ基である、請求項6記載の化合物。
- 3−アミノ−5−クロロ−6−メトキシ−4−メチル−チエノ[2,3−b]ピリジン2−カルボン酸シクロプロピルアミドである、請求項1記載の化合物。
- 3−アミノ−5−クロロ−4−メチル−6−(2−モルフォリン−4−イル−エトキシ)−チエノ[2,3−b]ピリジン−2−カルボン酸シクロプロピルアミドである、請求項1に記載の化合物。
- 3−アミノ−5−クロロ−6−ヒドロキシ−4−メチル−チエノ[2,3−b]ピリジン−2−カルボン酸シクロプロピルアミド又は3−アミノ−5−クロロ−6−イソプロポキシ−4−メチル−チエノ[2,3−b]ピリジン−2−カルボン酸シクロプロピルアミドである化合物。
- 治療用の、請求項1から9のいずれか一項記載の化合物。
- 請求項1から9のいずれかに記載の化合物の、M4ムスカリン性受容体活性と関連する障害の治療のための薬剤の製造における使用。
- 請求項1記載の化合物又はその薬学的に許容される塩を、薬学的に許容される担体、賦形剤又は希釈剤と組み合わせて含む医薬組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US62178504P | 2004-10-25 | 2004-10-25 | |
US60/621,785 | 2004-10-25 | ||
PCT/US2005/037271 WO2006047124A1 (en) | 2004-10-25 | 2005-10-18 | Thienopyridines as allosteric potentiators of the m4 muscarinic receptor |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2008517913A JP2008517913A (ja) | 2008-05-29 |
JP2008517913A5 true JP2008517913A5 (ja) | 2008-10-23 |
JP4945453B2 JP4945453B2 (ja) | 2012-06-06 |
Family
ID=36021809
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2007537951A Expired - Fee Related JP4945453B2 (ja) | 2004-10-25 | 2005-10-18 | M4ムスカリン性受容体のアロステリック増強剤としてのチエノピリジン |
Country Status (16)
Country | Link |
---|---|
US (1) | US8071776B2 (ja) |
EP (1) | EP1807434B1 (ja) |
JP (1) | JP4945453B2 (ja) |
CN (1) | CN100577666C (ja) |
AT (1) | ATE478876T1 (ja) |
AU (1) | AU2005299957B2 (ja) |
BR (1) | BRPI0517438A (ja) |
CA (1) | CA2583550C (ja) |
CY (1) | CY1111477T1 (ja) |
DE (1) | DE602005023197D1 (ja) |
DK (1) | DK1807434T3 (ja) |
ES (1) | ES2349416T3 (ja) |
MX (1) | MX2007004794A (ja) |
PL (1) | PL1807434T3 (ja) |
PT (1) | PT1807434E (ja) |
WO (1) | WO2006047124A1 (ja) |
Families Citing this family (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9493481B2 (en) | 2012-02-23 | 2016-11-15 | Vanderbilt University | Substituted 5-aminothieno[2,3—C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4 |
WO2014035829A1 (en) * | 2012-08-31 | 2014-03-06 | Vanderbilt University | Substituted 3-aminothieno[2,3-c]pyridine-2-carboxamide analogs as positive allosteric modulators |
EP3008073B1 (en) | 2013-06-11 | 2020-01-01 | Latvian Institute Of Organic Synthesis | Thieno[2,3-b]pyridines as multidrug resistance modulators |
WO2015027214A1 (en) | 2013-08-23 | 2015-02-26 | Vanderbilt University | Substituted thieno[2,3-c]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
WO2017107089A1 (en) | 2015-12-23 | 2017-06-29 | Merck Sharp & Dohme Corp. | 3- (1h-pyrazol-4-yl) pyridineallosteric modulators of the m4 muscarinic acetylcholine receptor |
ES2789756T3 (es) | 2015-12-23 | 2020-10-26 | Merck Sharp & Dohme | Moduladores alostéricos de 6,7-dihidro-5H-pirrolo[3,4-b]piridin-5-ona del receptor de acetilcolina muscarínico M4 |
JOP20180114B1 (ar) | 2016-06-22 | 2022-09-15 | Univ Vanderbilt | عوامل تعديل متباينة التجاسم موجبة من مستقبل الأسيتيل كولين المسكاريني m4 |
KR102470497B1 (ko) | 2016-07-01 | 2022-11-23 | 화이자 인코포레이티드 | 신경계 및 신경변성 질환을 치료하기 위한 5,7-디히드로-피롤로-피리딘 유도체 |
GB201616839D0 (en) | 2016-10-04 | 2016-11-16 | Takeda Pharmaceutical Company Limited | Therapeutic compounds |
BR112018013882A2 (pt) | 2016-11-07 | 2018-12-18 | Vanderbilt University | moduladores alostéricos positivos do receptor muscarínico de acetilcolina m4 |
WO2018085808A1 (en) | 2016-11-07 | 2018-05-11 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
MA46899A (fr) | 2016-11-07 | 2021-04-14 | Univ Vanderbilt | Modulateurs allostériques positifs du récepteur muscarinique de l'acétylcholine m4 |
WO2018112842A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | 6,6-fused heteroaryl piperidine ether allosteric modulators of m4 muscarinic acetylcholine receptor |
WO2018112840A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | 6, 5-fused heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor |
WO2018112843A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor |
WO2018234953A1 (en) | 2017-06-22 | 2018-12-27 | Pfizer Inc. | DIHYDRO-PYRROLO-PYRIDINE DERIVATIVES |
WO2019000238A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | 5- (PYRIDIN-3-YL) OXAZOLE ALLOSTERIC MODULATORS OF M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
WO2019000236A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
WO2019000237A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
TW201930311A (zh) | 2017-12-05 | 2019-08-01 | 泛德比爾特大學 | 蕈毒鹼型乙醯膽鹼受體m4之正向別構調節劑 |
WO2019113174A1 (en) | 2017-12-05 | 2019-06-13 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB9924962D0 (en) * | 1999-10-21 | 1999-12-22 | Mrc Collaborative Centre | Allosteric sites on muscarinic receptors |
CN1249051C (zh) * | 2000-04-28 | 2006-04-05 | 阿卡蒂亚药品公司 | 毒蕈碱性激动剂 |
AU2003214936A1 (en) * | 2002-02-20 | 2003-09-09 | Pharmacia And Upjohn Company | Azabicyclic compounds with alfa7 nicotinic acetylcholine receptor activity |
US6974870B2 (en) * | 2002-06-06 | 2005-12-13 | Boehringer Ingelheim Phamaceuticals, Inc. | Substituted 3-amino-thieno [2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses |
-
2005
- 2005-10-18 CN CN200580036624A patent/CN100577666C/zh not_active Expired - Fee Related
- 2005-10-18 JP JP2007537951A patent/JP4945453B2/ja not_active Expired - Fee Related
- 2005-10-18 PT PT05812144T patent/PT1807434E/pt unknown
- 2005-10-18 AT AT05812144T patent/ATE478876T1/de active
- 2005-10-18 DK DK05812144.3T patent/DK1807434T3/da active
- 2005-10-18 AU AU2005299957A patent/AU2005299957B2/en not_active Ceased
- 2005-10-18 ES ES05812144T patent/ES2349416T3/es active Active
- 2005-10-18 MX MX2007004794A patent/MX2007004794A/es active IP Right Grant
- 2005-10-18 US US11/577,508 patent/US8071776B2/en not_active Expired - Fee Related
- 2005-10-18 EP EP05812144A patent/EP1807434B1/en not_active Not-in-force
- 2005-10-18 BR BRPI0517438-4A patent/BRPI0517438A/pt not_active IP Right Cessation
- 2005-10-18 WO PCT/US2005/037271 patent/WO2006047124A1/en active Application Filing
- 2005-10-18 CA CA2583550A patent/CA2583550C/en not_active Expired - Fee Related
- 2005-10-18 DE DE602005023197T patent/DE602005023197D1/de active Active
- 2005-10-18 PL PL05812144T patent/PL1807434T3/pl unknown
-
2010
- 2010-10-14 CY CY20101100921T patent/CY1111477T1/el unknown
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