JP2013545791A5 - - Google Patents
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- Publication number
- JP2013545791A5 JP2013545791A5 JP2013543816A JP2013543816A JP2013545791A5 JP 2013545791 A5 JP2013545791 A5 JP 2013545791A5 JP 2013543816 A JP2013543816 A JP 2013543816A JP 2013543816 A JP2013543816 A JP 2013543816A JP 2013545791 A5 JP2013545791 A5 JP 2013545791A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- substituted
- ring
- cycloalkyl
- 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
- 125000001424 substituent group Chemical group 0.000 claims description 32
- 229910052799 carbon Inorganic materials 0.000 claims description 31
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 30
- -1 1,2,3,6-tetrahydro-pyridin-4-yl ring Chemical group 0.000 claims description 28
- 125000003118 aryl group Chemical group 0.000 claims description 23
- 229910052717 sulfur Inorganic materials 0.000 claims description 21
- 229910052760 oxygen Inorganic materials 0.000 claims description 19
- 125000001072 heteroaryl group Chemical group 0.000 claims description 18
- 125000002837 carbocyclic group Chemical group 0.000 claims description 17
- 150000001875 compounds Chemical class 0.000 claims description 17
- 125000000217 alkyl group Chemical group 0.000 claims description 16
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 15
- 125000000623 heterocyclic group Chemical group 0.000 claims description 15
- 125000005842 heteroatom Chemical group 0.000 claims description 13
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 8
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 6
- 125000001153 fluoro group Chemical group F* 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 125000003342 alkenyl group Chemical group 0.000 claims description 4
- 125000000304 alkynyl group Chemical group 0.000 claims description 4
- 125000001624 naphthyl group Chemical group 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 4
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims description 4
- 239000000969 carrier Substances 0.000 claims description 3
- 239000003085 diluting agent Substances 0.000 claims description 3
- 201000010099 disease Diseases 0.000 claims description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- 125000006432 1-methyl cyclopropyl group Chemical group [H]C([H])([H])C1(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 claims description 2
- 101000996752 Homo sapiens Glucose-dependent insulinotropic receptor Proteins 0.000 claims description 2
- 230000004913 activation Effects 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 125000002971 oxazolyl group Chemical group 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 125000000335 thiazolyl group Chemical group 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- 229920001577 copolymer Chemical class 0.000 claims 1
- YAEXNBGOCUGYHW-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCC1C(C1)Oc(nc2)c1cc2-c(cc1)ccc1S(C)(O)=O)=O Chemical compound CC(C)(C)OC(N(CC1)CCC1C(C1)Oc(nc2)c1cc2-c(cc1)ccc1S(C)(O)=O)=O YAEXNBGOCUGYHW-UHFFFAOYSA-N 0.000 description 1
- PZCMKJKGSWYCBG-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCC1C(C1)Oc2c1cc(-c(cc1)ccc1S(C)(O)=O)nn2)=O Chemical compound CC(C)(C)OC(N(CC1)CCC1C(C1)Oc2c1cc(-c(cc1)ccc1S(C)(O)=O)nn2)=O PZCMKJKGSWYCBG-UHFFFAOYSA-N 0.000 description 1
- 0 CC(C)(CC(CC1)C2(*)OC(**=*C([Al])=I)=C(*)C2)CN1C(O*)=O Chemical compound CC(C)(CC(CC1)C2(*)OC(**=*C([Al])=I)=C(*)C2)CN1C(O*)=O 0.000 description 1
- GBDYAPQZIGXIOC-UHFFFAOYSA-N CC(C)OC(N(CC1)CCC1C(C1)Oc(cc2)c1cc2-c(c(C)c1)ncc1S(C)(=O)=O)=O Chemical compound CC(C)OC(N(CC1)CCC1C(C1)Oc(cc2)c1cc2-c(c(C)c1)ncc1S(C)(=O)=O)=O GBDYAPQZIGXIOC-UHFFFAOYSA-N 0.000 description 1
- YTPCWZXAOUDNBY-UHFFFAOYSA-N CC(C)OC(N(CC1)CCC1C(C1)Oc(cc2)c1cc2-c(c(C)c1)ncc1S(C)=O)=O Chemical compound CC(C)OC(N(CC1)CCC1C(C1)Oc(cc2)c1cc2-c(c(C)c1)ncc1S(C)=O)=O YTPCWZXAOUDNBY-UHFFFAOYSA-N 0.000 description 1
- HLFPHPBEPQBUTB-UHFFFAOYSA-N CC(C)OC(N(CC1)CCC1C(C1)Oc(cc2)c1cc2-c(cc1)ccc1C(NC)=O)=O Chemical compound CC(C)OC(N(CC1)CCC1C(C1)Oc(cc2)c1cc2-c(cc1)ccc1C(NC)=O)=O HLFPHPBEPQBUTB-UHFFFAOYSA-N 0.000 description 1
- LZCLRPYCYCEKBS-UHFFFAOYSA-N CC1(CN(C)CC1)O Chemical compound CC1(CN(C)CC1)O LZCLRPYCYCEKBS-UHFFFAOYSA-N 0.000 description 1
- KPGFWZMUGOLTFK-UHFFFAOYSA-N CN(C1)CC1(F)[F]C Chemical compound CN(C1)CC1(F)[F]C KPGFWZMUGOLTFK-UHFFFAOYSA-N 0.000 description 1
- NVBHAFAVARZYFO-UHFFFAOYSA-N CN(C1)CC1OC Chemical compound CN(C1)CC1OC NVBHAFAVARZYFO-UHFFFAOYSA-N 0.000 description 1
- FLVFPAIGVBQGET-UHFFFAOYSA-N CN(CC1)CC1O Chemical compound CN(CC1)CC1O FLVFPAIGVBQGET-UHFFFAOYSA-N 0.000 description 1
- VJUDVVHGQMPPEI-UHFFFAOYSA-N CNCC1OCCC1 Chemical compound CNCC1OCCC1 VJUDVVHGQMPPEI-UHFFFAOYSA-N 0.000 description 1
- VCVSKQNPBCXRAM-UHFFFAOYSA-N CNCc1c[o]cn1 Chemical compound CNCc1c[o]cn1 VCVSKQNPBCXRAM-UHFFFAOYSA-N 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10195814.8 | 2010-12-17 | ||
| EP10195814 | 2010-12-17 | ||
| PCT/EP2011/073067 WO2012080476A1 (en) | 2010-12-17 | 2011-12-16 | Fused dihydropyrans as gpr119 modulators for the treatment of diabetes, obesity and related diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013545791A JP2013545791A (ja) | 2013-12-26 |
| JP2013545791A5 true JP2013545791A5 (enExample) | 2015-02-05 |
| JP6011543B2 JP6011543B2 (ja) | 2016-10-19 |
Family
ID=45470522
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013543816A Active JP6011543B2 (ja) | 2010-12-17 | 2011-12-16 | 糖尿病、肥満および関連疾患の治療のためのｇｐｒ１１９モジュレーターとしての縮合ジヒドロフラン |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8669271B2 (enExample) |
| EP (1) | EP2651931B1 (enExample) |
| JP (1) | JP6011543B2 (enExample) |
| AR (1) | AR084349A1 (enExample) |
| UY (1) | UY33805A (enExample) |
| WO (1) | WO2012080476A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201113269A (en) | 2009-06-24 | 2011-04-16 | Boehringer Ingelheim Int | New compounds, pharmaceutical composition and methods relating thereto |
| UY33805A (es) | 2010-12-17 | 2012-07-31 | Boehringer Ingelheim Int | ?Derivados de dihidrobenzofuranil-piperidinilo, aza-dihidrobenzofuranilpiperidinilo y diaza-dihidrobenzofuranil-piperidinilo, composiciones farmacéuticas que los contienen y usos de los mismos?. |
| CA2825124A1 (en) * | 2011-01-21 | 2012-07-26 | Boehringer Ingelheim International Gmbh | Fused dihydrofurans as gpr119 modulators for the treatment of diabetes, obesity and related disorders |
| US8822471B2 (en) | 2011-03-14 | 2014-09-02 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical compositions and uses thereof |
| US8921398B2 (en) | 2011-06-09 | 2014-12-30 | Boehringer Ingelheim International Gmbh | N-cyclopropyl-N-piperidinyl-amide derivatives, pharmaceutical compositions and uses thereof |
| WO2012170867A1 (en) * | 2011-06-09 | 2012-12-13 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of gpr-119 |
| US8853239B2 (en) | 2011-12-09 | 2014-10-07 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical compositions and uses thereof |
| US9012456B2 (en) * | 2012-02-28 | 2015-04-21 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical compositions and uses thereof |
| US8809361B2 (en) * | 2012-05-07 | 2014-08-19 | Boehringer Ingelheim International Gmbh | 2,3-dihydrofuro[2,3-c]pyridines, their use as modulators of the G-protein-coupled receptor GPR119 and pharmaceutical compositions thereof |
| US8975277B2 (en) | 2012-06-12 | 2015-03-10 | Boehringer Ingelheim International Gmbh | 2,3-dihydrofuro[2,3-c]pyridin-2-ylpiperidine derivatives |
| JP2015522080A (ja) | 2012-07-11 | 2015-08-03 | エルセリクス セラピューティクス インコーポレイテッド | スタチン、ビグアナイド、およびさらなる薬剤を含む心血管代謝性リスクを減少させるための組成物 |
| WO2014167008A1 (en) | 2013-04-12 | 2014-10-16 | Bayer Cropscience Ag | Novel triazolinthione derivatives |
| EP2984081B1 (en) | 2013-04-12 | 2017-08-09 | Bayer CropScience Aktiengesellschaft | Novel triazole derivatives |
| KR20150140381A (ko) | 2013-04-12 | 2015-12-15 | 바이엘 크롭사이언스 악티엔게젤샤프트 | 신규 트리아졸 유도체 |
| TW201613860A (en) | 2014-02-13 | 2016-04-16 | Incyte Corp | Cyclopropylamines as LSD1 inhibitors |
| SI3105218T1 (sl) | 2014-02-13 | 2019-11-29 | Incyte Corp | Ciklopropilamini kot inhibitorji LSD1 |
| WO2015123437A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| ES2750956T3 (es) | 2014-02-13 | 2020-03-30 | Incyte Corp | Ciclopropilaminas como inhibidores de LSD1 |
| WO2016007731A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
| US9695167B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| WO2016007736A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyrazines as lsd1 inhibitors |
| US20180339976A1 (en) | 2015-04-02 | 2018-11-29 | Bayer Cropscience Aktiengesellschaft | Novel triazole derivatives |
| US9944647B2 (en) | 2015-04-03 | 2018-04-17 | Incyte Corporation | Heterocyclic compounds as LSD1 inhibitors |
| SI3334709T1 (sl) | 2015-08-12 | 2025-03-31 | Incyte Holdings Corporation | Soli zaviralca lsd1 |
| US10526345B2 (en) * | 2016-04-08 | 2020-01-07 | Mankind Pharma Ltd. | Compounds as GPR119 agonists |
| US10208030B2 (en) | 2016-04-08 | 2019-02-19 | Mankind Pharma Ltd. | GPR119 agonist compounds |
| US10954229B2 (en) | 2016-04-08 | 2021-03-23 | Mankind Pharma Ltd. | GPR119 agonist compounds |
| EP3445339B1 (en) | 2016-04-22 | 2023-08-23 | Incyte Corporation | Formulations of an lsd1 inhibitor |
| US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
| CA3173731A1 (en) | 2020-02-28 | 2021-09-02 | Kallyope, Inc. | Gpr40 agonists |
| CN116323608A (zh) | 2020-05-19 | 2023-06-23 | 卡尔优普公司 | Ampk活化剂 |
| CA3183575A1 (en) | 2020-06-26 | 2021-12-30 | Iyassu Sebhat | Ampk activators |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007003961A2 (en) * | 2005-06-30 | 2007-01-11 | Prosidion Limited | Gpcr agonists |
| EP2059516A1 (en) * | 2006-08-30 | 2009-05-20 | BIOVITRUM AB (publ) | Pyridine compounds for treating gpr119 related disorders |
| EP2325182A1 (en) * | 2006-12-06 | 2011-05-25 | Glaxosmithkline LLC | Bicyclic compounds and use as antidiabetics |
| JP2010526145A (ja) * | 2007-05-04 | 2010-07-29 | ブリストル−マイヤーズ スクイブ カンパニー | ［６，６］および［６，７］−二環式ｇｐｒ１１９ｇタンパク質結合受容体アゴニスト |
| PE20090213A1 (es) * | 2007-05-04 | 2009-02-28 | Bristol Myers Squibb Co | Agonistas del receptor acoplado a la proteina g gpr119 [6,5]-biciclicos |
| NZ583495A (en) * | 2007-09-20 | 2011-11-25 | Irm Llc | Compounds and compositions as modulators of gpr119 activity |
| WO2009106565A1 (en) * | 2008-02-27 | 2009-09-03 | Biovitrum Ab (Publ) | Agonists of gpr119 |
| WO2009150144A1 (en) * | 2008-06-10 | 2009-12-17 | Inovacia Ab | New gpr119modulators |
| TW201031668A (en) * | 2009-01-22 | 2010-09-01 | Mitsubishi Tanabe Pharma Corp | Novel pyrrolo[2,3-d] pyrimidine compound |
| EP2399914A4 (en) * | 2009-02-18 | 2012-08-29 | Takeda Pharmaceutical | FUSED HETEROCYCLIC CORE COMPOUND |
| JP5467151B2 (ja) | 2009-06-24 | 2014-04-09 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規化合物、医薬組成物及びそれに関する方法 |
| TW201113269A (en) | 2009-06-24 | 2011-04-16 | Boehringer Ingelheim Int | New compounds, pharmaceutical composition and methods relating thereto |
| WO2011140161A1 (en) * | 2010-05-06 | 2011-11-10 | Bristol-Myers Squibb Company | Benzofuranyl analogues as gpr119 modulators |
| EP2566864B1 (en) | 2010-05-07 | 2014-09-03 | Boehringer Ingelheim International GmbH | Pyridazinones as gpr119 agonists |
| UY33805A (es) | 2010-12-17 | 2012-07-31 | Boehringer Ingelheim Int | ?Derivados de dihidrobenzofuranil-piperidinilo, aza-dihidrobenzofuranilpiperidinilo y diaza-dihidrobenzofuranil-piperidinilo, composiciones farmacéuticas que los contienen y usos de los mismos?. |
| CA2825124A1 (en) | 2011-01-21 | 2012-07-26 | Boehringer Ingelheim International Gmbh | Fused dihydrofurans as gpr119 modulators for the treatment of diabetes, obesity and related disorders |
| US8822471B2 (en) | 2011-03-14 | 2014-09-02 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical compositions and uses thereof |
-
2011
- 2011-12-15 UY UY0001033805A patent/UY33805A/es not_active Application Discontinuation
- 2011-12-16 EP EP11807666.0A patent/EP2651931B1/en active Active
- 2011-12-16 US US13/327,823 patent/US8669271B2/en active Active
- 2011-12-16 JP JP2013543816A patent/JP6011543B2/ja active Active
- 2011-12-16 AR ARP110104756A patent/AR084349A1/es unknown
- 2011-12-16 WO PCT/EP2011/073067 patent/WO2012080476A1/en not_active Ceased