JP2012501334A5 - - Google Patents
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- Publication number
- JP2012501334A5 JP2012501334A5 JP2011525147A JP2011525147A JP2012501334A5 JP 2012501334 A5 JP2012501334 A5 JP 2012501334A5 JP 2011525147 A JP2011525147 A JP 2011525147A JP 2011525147 A JP2011525147 A JP 2011525147A JP 2012501334 A5 JP2012501334 A5 JP 2012501334A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- methyl
- hydrogen
- thiophen
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 24
- 229910052739 hydrogen Inorganic materials 0.000 claims 21
- 239000001257 hydrogen Substances 0.000 claims 21
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 239000003085 diluting agent Substances 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 3
- XOMZJWSIQIBUQR-QAQDUYKDSA-N S1C(C)=CC=C1CN(CCC(O)=O)C1=NC([C@@H]2CC[C@H](CC2)C(C)(C)C)=CS1 Chemical compound S1C(C)=CC=C1CN(CCC(O)=O)C1=NC([C@@H]2CC[C@H](CC2)C(C)(C)C)=CS1 XOMZJWSIQIBUQR-QAQDUYKDSA-N 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 230000004584 weight gain Effects 0.000 claims 2
- 235000019786 weight gain Nutrition 0.000 claims 2
- YOOZBJQEMOPTJW-UHFFFAOYSA-N 3-[(5-methylthiophen-2-yl)methyl-[4-(4-propan-2-ylcyclohexyl)-1,3-thiazol-2-yl]amino]propanoic acid Chemical compound C1CC(C(C)C)CCC1C1=CSC(N(CCC(O)=O)CC=2SC(C)=CC=2)=N1 YOOZBJQEMOPTJW-UHFFFAOYSA-N 0.000 claims 1
- FGGSHTCNGFCULE-UHFFFAOYSA-N 3-[(5-methylthiophen-2-yl)methyl-[4-(4-propylcyclohexyl)-1,3-thiazol-2-yl]amino]propanoic acid Chemical compound C1CC(CCC)CCC1C1=CSC(N(CCC(O)=O)CC=2SC(C)=CC=2)=N1 FGGSHTCNGFCULE-UHFFFAOYSA-N 0.000 claims 1
- IEOGVWBPUKXEQF-UHFFFAOYSA-N 3-[(5-methylthiophen-2-yl)methyl-[4-[4-(trifluoromethyl)cyclohexyl]-1,3-thiazol-2-yl]amino]propanoic acid Chemical compound S1C(C)=CC=C1CN(CCC(O)=O)C1=NC(C2CCC(CC2)C(F)(F)F)=CS1 IEOGVWBPUKXEQF-UHFFFAOYSA-N 0.000 claims 1
- PPVPBVSDDKTQRT-UHFFFAOYSA-N 3-[[4-(4,4-difluorocyclohexyl)-1,3-thiazol-2-yl]-[(5-methylthiophen-2-yl)methyl]amino]propanoic acid Chemical compound S1C(C)=CC=C1CN(CCC(O)=O)C1=NC(C2CCC(F)(F)CC2)=CS1 PPVPBVSDDKTQRT-UHFFFAOYSA-N 0.000 claims 1
- ZRZZQCNAIDQHNS-UHFFFAOYSA-N 3-[[4-(4,4-dimethylcyclohexyl)-1,3-thiazol-2-yl]-[(5-methylthiophen-2-yl)methyl]amino]propanoic acid Chemical compound S1C(C)=CC=C1CN(CCC(O)=O)C1=NC(C2CCC(C)(C)CC2)=CS1 ZRZZQCNAIDQHNS-UHFFFAOYSA-N 0.000 claims 1
- UGOGHKGNOQEGPJ-UHFFFAOYSA-N 3-[[4-(4-ethylcyclohexyl)-1,3-thiazol-2-yl]-[(5-methylthiophen-2-yl)methyl]amino]propanoic acid Chemical compound C1CC(CC)CCC1C1=CSC(N(CCC(O)=O)CC=2SC(C)=CC=2)=N1 UGOGHKGNOQEGPJ-UHFFFAOYSA-N 0.000 claims 1
- QBCAGJGPWFAZDH-UHFFFAOYSA-N 3-[[4-(4-methoxycyclohexyl)-1,3-thiazol-2-yl]-[(5-methylthiophen-2-yl)methyl]amino]propanoic acid Chemical compound C1CC(OC)CCC1C1=CSC(N(CCC(O)=O)CC=2SC(C)=CC=2)=N1 QBCAGJGPWFAZDH-UHFFFAOYSA-N 0.000 claims 1
- XOMZJWSIQIBUQR-UHFFFAOYSA-N 3-[[4-(4-tert-butylcyclohexyl)-1,3-thiazol-2-yl]-[(5-methylthiophen-2-yl)methyl]amino]propanoic acid Chemical compound S1C(C)=CC=C1CN(CCC(O)=O)C1=NC(C2CCC(CC2)C(C)(C)C)=CS1 XOMZJWSIQIBUQR-UHFFFAOYSA-N 0.000 claims 1
- FRFAQMKDIVZURC-UHFFFAOYSA-N 3-[[4-[4-(4-fluorophenyl)cyclohexyl]-1,3-thiazol-2-yl]-[(5-methylthiophen-2-yl)methyl]amino]propanoic acid Chemical compound S1C(C)=CC=C1CN(CCC(O)=O)C1=NC(C2CCC(CC2)C=2C=CC(F)=CC=2)=CS1 FRFAQMKDIVZURC-UHFFFAOYSA-N 0.000 claims 1
- 206010057671 Female sexual dysfunction Diseases 0.000 claims 1
- 206010057672 Male sexual dysfunction Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Substances CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 1
- ASTROQQYUQIBSQ-MXVIHJGJSA-N S1C(C)=CC=C1CN(CCC(O)=O)C1=NC([C@@H]2CC[C@H](CC2)C=2C=CC=CC=2)=CS1 Chemical compound S1C(C)=CC=C1CN(CCC(O)=O)C1=NC([C@@H]2CC[C@H](CC2)C=2C=CC=CC=2)=CS1 ASTROQQYUQIBSQ-MXVIHJGJSA-N 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000004580 weight loss Effects 0.000 claims 1
- -1 —phenyl Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9284408P | 2008-08-29 | 2008-08-29 | |
| US61/092,844 | 2008-08-29 | ||
| PCT/US2009/054920 WO2010025142A1 (en) | 2008-08-29 | 2009-08-25 | Substituted aminothiazole derivatives, pharmaceutical compositions, and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012501334A JP2012501334A (ja) | 2012-01-19 |
| JP2012501334A5 true JP2012501334A5 (enExample) | 2012-05-17 |
Family
ID=41721863
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011525147A Pending JP2012501334A (ja) | 2008-08-29 | 2009-08-25 | 置換アミノチアゾール誘導体、医薬組成物、および使用の方法 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8563742B2 (enExample) |
| EP (1) | EP2320738A4 (enExample) |
| JP (1) | JP2012501334A (enExample) |
| CA (1) | CA2731442A1 (enExample) |
| WO (1) | WO2010025142A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3988108A1 (en) | 2011-12-29 | 2022-04-27 | Rhythm Pharmaceuticals, Inc. | Method of treating melanocortin-4 receptor-associated disorders in heterozygous carriers |
| US10960046B2 (en) | 2015-09-30 | 2021-03-30 | Rhythm Pharmaceuticals, Inc. | Method of treating melanocortin-4 receptor pathway-associated disorders |
| EP3773897A1 (en) | 2018-04-06 | 2021-02-17 | Rhythm Pharmaceuticals, Inc. | Compositions for treating kidney disease |
| EP3846793B1 (en) * | 2018-09-07 | 2024-01-24 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
| AU2021230289A1 (en) | 2020-03-03 | 2022-09-29 | PIC Therapeutics, Inc. | eIF4E inhibitors and uses thereof |
| CA3229560A1 (en) | 2021-08-25 | 2023-03-02 | Christopher L. Vandeusen | Eif4e inhibitors and uses thereof |
| JP2024532276A (ja) | 2021-08-25 | 2024-09-05 | ピク セラピューティクス， インコーポレイテッド | ｅＩＦ４Ｅ阻害剤及びその使用 |
| PE20242044A1 (es) | 2022-01-07 | 2024-10-14 | V Mane Fils | Compuestos y composiciones refrescantes |
Family Cites Families (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2607369B2 (ja) | 1987-02-20 | 1997-05-07 | 興和株式会社 | 新規な複素環化合物 |
| US5502025A (en) | 1987-08-13 | 1996-03-26 | Monsanto Company | Safening herbicidal pyrazolylsulfonylureas |
| YU48319B (sh) | 1988-08-01 | 1998-05-15 | Monsanto Company | Bezbednosni herbicidni derivati benzoeve kiseline |
| US5201933A (en) | 1988-08-01 | 1993-04-13 | Monsanto Company | Safening herbicidal benzoic acid derivatives |
| FR2656610B1 (fr) | 1989-12-29 | 1992-05-07 | Sanofi Sa | Derives d'amino-2 phenyl-4 thiazole, leur procede de preparation et leur application therapeutique. |
| JPH0532662A (ja) | 1990-11-09 | 1993-02-09 | Nissan Chem Ind Ltd | 置換ピラゾール誘導体および農園芸用殺菌剤 |
| TW311136B (enExample) | 1990-11-30 | 1997-07-21 | Otsuka Pharma Co Ltd | |
| DE4124942A1 (de) | 1991-07-27 | 1993-01-28 | Thomae Gmbh Dr K | 5-gliedrige heterocyclen, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
| WO1993015060A1 (fr) | 1992-01-22 | 1993-08-05 | Nissan Chemical Industries, Ltd. | Derive de pyrazole substitue et bactericide agrohorticole |
| US5326776A (en) | 1992-03-02 | 1994-07-05 | Abbott Laboratories | Angiotensin II receptor antagonists |
| US6310034B1 (en) | 1993-05-21 | 2001-10-30 | Ut-Battelle, Llc | Agouti polypeptide compositions |
| JPH07149745A (ja) | 1993-11-30 | 1995-06-13 | Hisamitsu Pharmaceut Co Inc | 新規な２−アミノチアゾール誘導体 |
| US5627131A (en) | 1995-01-09 | 1997-05-06 | Zeneca Limited | Herbicidal compositions of 4-benzoylisoxazole and antidotes therefor |
| US5766877A (en) | 1996-05-10 | 1998-06-16 | Amgen Inc. | Genes encoding art, an agouti-related transcript |
| WO1997047299A1 (en) | 1996-06-12 | 1997-12-18 | 3-Dimensional Pharmaceuticals, Inc. | Amidino and guanidino heterocyclic protease inhibitors |
| FR2754258B1 (fr) | 1996-10-08 | 1998-12-31 | Sanofi Sa | Derives d'aminothiazole, leur procede de preparation et les compositions pharmaceutiques les contenant |
| US6011048A (en) | 1997-01-28 | 2000-01-04 | Merck & Co., Inc. | Thiazole benzenesulfonamides as β3 agonists for treatment of diabetes and obesity |
| WO1999050295A2 (en) | 1998-03-30 | 1999-10-07 | Gryphon Sciences | Agouti-related protein analogs and methods of use |
| US6689873B1 (en) | 1998-04-29 | 2004-02-10 | Merck & Co., Inc. | Nucleic acid encoding rat agouti related protein |
| US6699896B1 (en) | 1998-05-12 | 2004-03-02 | Wyeth | Oxazole-aryl-carboxylic acids useful in the treatment of insulin resistance and hyperglycemia |
| WO1999058514A1 (en) | 1998-05-12 | 1999-11-18 | American Home Products Corporation | (2-acylaminothiazole-4-yl)acetic acid derivatives |
| CN1308618A (zh) | 1998-05-12 | 2001-08-15 | 美国家用产品公司 | 用于治疗胰岛素抗性和高血糖的噁唑芳基－羧酸 |
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| EP2308833A3 (en) | 1999-04-15 | 2011-09-28 | Bristol-Myers Squibb Company | Cyclic protein tyrosine kinase inhibitors |
| US7291641B2 (en) | 1999-10-11 | 2007-11-06 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) | Derivatives of heterocycles with 5 members, their preparation and their use as medicaments |
| US20040132788A1 (en) | 1999-10-11 | 2004-07-08 | Chabrier De Lassauniere Pierre-Etienne | Derivatives of heterocycles with 5 members, their preparation and their use as medicaments |
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| DE10006453A1 (de) | 2000-02-14 | 2001-08-16 | Bayer Ag | Piperidylcarbonsäuren als Integrinantagonisten |
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| HUP0202719A3 (en) | 2001-08-21 | 2006-01-30 | Pfizer Prod Inc | Pharmaceutical compositions for the treatment of female sexual dysfunctions |
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| JP4879165B2 (ja) * | 2004-04-20 | 2012-02-22 | トランス テック ファーマ，インコーポレイテッド | メラノコルチン受容体の調節因子としての置換チアゾール及びピリミジン誘導体 |
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-
2009
- 2009-08-25 EP EP09810508A patent/EP2320738A4/en not_active Withdrawn
- 2009-08-25 WO PCT/US2009/054920 patent/WO2010025142A1/en not_active Ceased
- 2009-08-25 CA CA2731442A patent/CA2731442A1/en not_active Abandoned
- 2009-08-25 US US12/547,018 patent/US8563742B2/en not_active Expired - Fee Related
- 2009-08-25 JP JP2011525147A patent/JP2012501334A/ja active Pending