ZA200608738B - Combinations comprising alpha-2-delta ligands and EP4 receptor antagonists - Google Patents
Combinations comprising alpha-2-delta ligands and EP4 receptor antagonists Download PDFInfo
- Publication number
- ZA200608738B ZA200608738B ZA200608738A ZA200608738A ZA200608738B ZA 200608738 B ZA200608738 B ZA 200608738B ZA 200608738 A ZA200608738 A ZA 200608738A ZA 200608738 A ZA200608738 A ZA 200608738A ZA 200608738 B ZA200608738 B ZA 200608738B
- Authority
- ZA
- South Africa
- Prior art keywords
- ethyl
- amino
- phenyl
- chloro
- carbonyl
- Prior art date
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- 239000003446 ligand Substances 0.000 title claims description 30
- 101150109738 Ptger4 gene Proteins 0.000 title claims description 16
- 239000002464 receptor antagonist Substances 0.000 title claims description 16
- 229940044551 receptor antagonist Drugs 0.000 title claims description 16
- 150000003839 salts Chemical class 0.000 claims description 18
- -1 3,5-dimethyl-4-phenyl-1H-pyrazol-1 -yl Chemical group 0.000 claims description 15
- 208000002193 Pain Diseases 0.000 claims description 15
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Natural products CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 14
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims description 13
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 11
- 239000002253 acid Substances 0.000 claims description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
- 229960002870 gabapentin Drugs 0.000 claims description 5
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- JXEHXYFSIOYTAH-SFYZADRCSA-N imagabalin Chemical compound CCC[C@@H](C)C[C@H](N)CC(O)=O JXEHXYFSIOYTAH-SFYZADRCSA-N 0.000 claims description 4
- AYXYPKUFHZROOJ-ZETCQYMHSA-N pregabalin Chemical compound CC(C)C[C@H](CN)CC(O)=O AYXYPKUFHZROOJ-ZETCQYMHSA-N 0.000 claims description 4
- 229960001233 pregabalin Drugs 0.000 claims description 4
- RGFRGRZSMVXTLF-ONGXEEELSA-N (2s,4s)-4-[(3-fluorophenyl)methyl]pyrrolidine-2-carboxylic acid Chemical compound C1N[C@H](C(=O)O)C[C@@H]1CC1=CC=CC(F)=C1 RGFRGRZSMVXTLF-ONGXEEELSA-N 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 208000004296 neuralgia Diseases 0.000 claims description 3
- 208000021722 neuropathic pain Diseases 0.000 claims description 3
- LUANXJIOUGKVRZ-UWVGGRQHSA-N (2s,4s)-4-(3-chlorophenoxy)pyrrolidine-2-carboxylic acid Chemical compound C1N[C@H](C(=O)O)C[C@@H]1OC1=CC=CC(Cl)=C1 LUANXJIOUGKVRZ-UWVGGRQHSA-N 0.000 claims description 2
- KKXFMWXZXDUYBF-BDAKNGLRSA-N (3s,5r)-3-(aminomethyl)-5-methyloctanoic acid Chemical compound CCC[C@@H](C)C[C@H](CN)CC(O)=O KKXFMWXZXDUYBF-BDAKNGLRSA-N 0.000 claims description 2
- GUEQOLSQPOTTME-RQJHMYQMSA-N (3s,5r)-3-amino-5-methylheptanoic acid Chemical compound CC[C@@H](C)C[C@H](N)CC(O)=O GUEQOLSQPOTTME-RQJHMYQMSA-N 0.000 claims description 2
- XKWDZEJCUWTBOM-BDAKNGLRSA-N (3s,5r)-3-amino-5-methylnonanoic acid Chemical compound CCCC[C@@H](C)C[C@H](N)CC(O)=O XKWDZEJCUWTBOM-BDAKNGLRSA-N 0.000 claims description 2
- 206010065390 Inflammatory pain Diseases 0.000 claims description 2
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 16
- 239000005711 Benzoic acid Substances 0.000 claims 8
- 235000010233 benzoic acid Nutrition 0.000 claims 8
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 6
- 125000000590 4-methylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- FULSIHOOFUQXTB-UHFFFAOYSA-N (2-chlorophenyl)sulfonylcarbamic acid Chemical compound OC(=O)NS(=O)(=O)C1=CC=CC=C1Cl FULSIHOOFUQXTB-UHFFFAOYSA-N 0.000 claims 2
- VATAIZDYZPAXOX-UHFFFAOYSA-N (4-methylphenyl)sulfonylcarbamic acid Chemical compound CC1=CC=C(S(=O)(=O)NC(O)=O)C=C1 VATAIZDYZPAXOX-UHFFFAOYSA-N 0.000 claims 2
- KHBQMWCZKVMBLN-UHFFFAOYSA-N Benzenesulfonamide Chemical compound NS(=O)(=O)C1=CC=CC=C1 KHBQMWCZKVMBLN-UHFFFAOYSA-N 0.000 claims 2
- 238000009109 curative therapy Methods 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 238000002638 palliative care Methods 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 230000000069 prophylactic effect Effects 0.000 claims 2
- 238000011321 prophylaxis Methods 0.000 claims 2
- VRSJQMXCCLVETK-UHFFFAOYSA-N 1-[2-[4-(2-ethyl-4-phenylimidazol-1-yl)phenyl]ethyl]-3-(4-methylphenyl)sulfonylurea Chemical compound CCC1=NC(C=2C=CC=CC=2)=CN1C(C=C1)=CC=C1CCNC(=O)NS(=O)(=O)C1=CC=C(C)C=C1 VRSJQMXCCLVETK-UHFFFAOYSA-N 0.000 claims 1
- KFDAZUZDUCNSCO-UHFFFAOYSA-N 1-[2-[4-(3,5-dimethyl-4-phenylpyrazol-1-yl)phenyl]ethyl]-3-(4-methylphenyl)sulfonylurea Chemical compound CC1=NN(C=2C=CC(CCNC(=O)NS(=O)(=O)C=3C=CC(C)=CC=3)=CC=2)C(C)=C1C1=CC=CC=C1 KFDAZUZDUCNSCO-UHFFFAOYSA-N 0.000 claims 1
- GFMMZVFKQDQZHJ-UHFFFAOYSA-N 1-[2-[4-[2-ethyl-5-(2-hydroxypropan-2-yl)benzimidazol-1-yl]phenyl]ethyl]-3-(4-methylphenyl)sulfonylurea Chemical compound CCC1=NC2=CC(C(C)(C)O)=CC=C2N1C(C=C1)=CC=C1CCNC(=O)NS(=O)(=O)C1=CC=C(C)C=C1 GFMMZVFKQDQZHJ-UHFFFAOYSA-N 0.000 claims 1
- IFQJIRWSTAXGLB-UHFFFAOYSA-N 2-[4-[2-(2-methylpropyl)-4-phenylimidazol-1-yl]phenyl]ethyl n-(2-chlorophenyl)sulfonylcarbamate Chemical compound CC(C)CC1=NC(C=2C=CC=CC=2)=CN1C(C=C1)=CC=C1CCOC(=O)NS(=O)(=O)C1=CC=CC=C1Cl IFQJIRWSTAXGLB-UHFFFAOYSA-N 0.000 claims 1
- VFGIXMWNVHDPQH-UHFFFAOYSA-N 2-[4-[5,7-dimethyl-2-(methylamino)imidazo[4,5-b]pyridin-3-yl]phenyl]ethyl n-(4-methylphenyl)sulfonylcarbamate Chemical compound CNC1=NC2=C(C)C=C(C)N=C2N1C(C=C1)=CC=C1CCOC(=O)NS(=O)(=O)C1=CC=C(C)C=C1 VFGIXMWNVHDPQH-UHFFFAOYSA-N 0.000 claims 1
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 1
- MOEZPHHJIZLEKX-UHFFFAOYSA-N 3-[[1-(aminomethyl)cyclohexyl]methyl]-2h-1,2,4-oxadiazol-5-one Chemical compound N=1OC(=O)NC=1CC1(CN)CCCCC1 MOEZPHHJIZLEKX-UHFFFAOYSA-N 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 1
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims 1
- JYZIHLWOWKMNNX-UHFFFAOYSA-N benzimidazole Chemical compound C1=C[CH]C2=NC=NC2=C1 JYZIHLWOWKMNNX-UHFFFAOYSA-N 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 description 65
- 125000004432 carbon atom Chemical group C* 0.000 description 64
- 125000003118 aryl group Chemical group 0.000 description 33
- 125000001072 heteroaryl group Chemical group 0.000 description 27
- 125000003545 alkoxy group Chemical group 0.000 description 22
- 125000000753 cycloalkyl group Chemical group 0.000 description 14
- 125000001424 substituent group Chemical group 0.000 description 14
- 125000005843 halogen group Chemical group 0.000 description 12
- 239000011575 calcium Substances 0.000 description 11
- 125000004093 cyano group Chemical group *C#N 0.000 description 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 9
- 229910052717 sulfur Inorganic materials 0.000 description 9
- 150000001875 compounds Chemical class 0.000 description 8
- 125000001153 fluoro group Chemical group F* 0.000 description 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 8
- 229910052757 nitrogen Inorganic materials 0.000 description 8
- 229910052760 oxygen Inorganic materials 0.000 description 8
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 description 7
- 125000004414 alkyl thio group Chemical group 0.000 description 7
- 125000002947 alkylene group Chemical group 0.000 description 7
- 125000005842 heteroatom Chemical group 0.000 description 7
- 125000002950 monocyclic group Chemical group 0.000 description 7
- 125000004430 oxygen atom Chemical group O* 0.000 description 7
- 229910052739 hydrogen Inorganic materials 0.000 description 6
- 239000001257 hydrogen Substances 0.000 description 6
- 125000004434 sulfur atom Chemical group 0.000 description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 5
- 125000003342 alkenyl group Chemical group 0.000 description 5
- 125000000304 alkynyl group Chemical group 0.000 description 5
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- 125000004429 atom Chemical group 0.000 description 5
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- 125000003282 alkyl amino group Chemical group 0.000 description 3
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- 125000000392 cycloalkenyl group Chemical group 0.000 description 3
- 206010015037 epilepsy Diseases 0.000 description 3
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- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 2
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Classifications
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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| SI0934061T1 (en) | 1996-07-24 | 2003-10-31 | Warner-Lambert Company Llc | Isobutylgaba and its derivatives for the treatment of pain |
| CA2613522A1 (en) | 2005-06-27 | 2007-01-04 | Exelixis, Inc. | Imidazole based lxr modulators |
| EP2025672B1 (en) * | 2006-05-31 | 2013-09-18 | Daiichi Sankyo Company, Limited | Process for producing 1-carbamoyl-3,7-dioxo-1,4-diazepane compounds |
| AU2007283404B2 (en) * | 2006-08-11 | 2013-04-18 | Merck Canada Inc. | Thiophenecarboxamide derivatives as EP4 receptor ligands |
| US8598355B2 (en) * | 2008-05-14 | 2013-12-03 | Astellas Pharma Inc. | Amide compound |
| CA2754702C (en) * | 2009-04-22 | 2016-06-07 | Yukinori Take | Selective ep4 antagonistic substance for treatment of cancer |
| CA2789665C (en) * | 2010-02-22 | 2020-06-16 | Raqualia Pharma Inc. | Use of ep4 receptor antagonists in the treatment of il-23 mediated diseases |
| UA115576C2 (uk) | 2012-12-06 | 2017-11-27 | Байєр Фарма Акцієнгезелльшафт | Похідні бензимідазолу як антагоністи ер4 |
| CN107496421A (zh) * | 2013-03-19 | 2017-12-22 | 株式会社ＡｓｋＡｔ | Ep4受体拮抗剂在软骨疾病的治疗中的用途 |
| US10391086B2 (en) | 2013-03-19 | 2019-08-27 | Askat Inc. | Use of EP4 receptor antagonists in the treatment of cartilage disease |
| MA38661A1 (fr) | 2013-06-27 | 2017-03-31 | Pfizer | Composés hétéro-aromatiques et leur utilisation en tant que ligands d1 de la dopamine |
| TW201607943A (zh) | 2013-12-19 | 2016-03-01 | 拜耳製藥公司 | 作為ｅｐ４配體之新穎苯并咪唑衍生物 |
| CA2941008C (en) * | 2014-03-06 | 2022-07-26 | Aratana Therapeutics, Inc. | Compositions of grapiprant and methods for using the same |
| US10342785B2 (en) | 2016-11-04 | 2019-07-09 | Askat Inc. | Use of EP4 receptor antagonists for the treatment of NASH-associated liver cancer |
| WO2018162562A1 (en) | 2017-03-10 | 2018-09-13 | Bayer Pharma Aktiengesellschaft | Use of an ep4 antagonist for the treatment of inflammatory pain |
| WO2019038156A1 (en) | 2017-08-22 | 2019-02-28 | Bayer Pharma Aktiengesellschaft | USE OF AN EP4 ANTAGONIST FOR THE TREATMENT OF ARTHRITIS |
| US10239885B1 (en) * | 2018-06-18 | 2019-03-26 | Avista Pharma Solutions, Inc. | Compound 1-[2-[4-(2-ethyl-6,8-dimethylimidazo[1,2-α]pyrazin-3-yl)phenyl]ethyl]-3-(p-tolylsulfonyl)urea as a prostaglandin EP4 receptor antagonist |
| EP3820469A4 (en) * | 2018-07-11 | 2022-04-13 | Arrys Therapeutics, Inc. | EP4 INHIBITORS AND USE THEREOF |
| US11254675B2 (en) * | 2019-08-12 | 2022-02-22 | Cadila Healthcare Limited | Process for preparation of grapiprant |
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| CA2206119C (en) * | 1994-12-12 | 2008-05-13 | Omeros Medical Systems, Inc. | Irrigation solution and method for inhibition of pain, inflammation and spasm |
| TWI249520B (en) * | 1998-07-15 | 2006-02-21 | Ono Pharmaceutical Co | 5-Thia-omega-substituted phenyl prostaglandin E derivatives, method for producing the same and medicines containing the same as the active ingredient |
| EP1202730B1 (en) * | 1999-08-10 | 2004-08-04 | Glaxo Group Limited | Use of ep4 receptor ligands in the treatment of neuropathic pain |
| HN2001000224A (es) * | 2000-10-19 | 2002-06-13 | Pfizer | Compuestos de imidazol condensado con arilo o heteroarilo como agentes anti - inflamatorios y analgesicos. |
| GB0030541D0 (en) * | 2000-12-14 | 2001-01-31 | Glaxo Group Ltd | Medical uses |
| GB0031295D0 (en) * | 2000-12-21 | 2001-01-31 | Glaxo Group Ltd | Naphthalene derivatives |
| GB0031302D0 (en) * | 2000-12-21 | 2001-01-31 | Glaxo Group Ltd | Napthalene derivatives |
| HUP0400183A2 (hu) * | 2001-06-11 | 2004-07-28 | Xenoport Inc. | Gaba-analóg prodrugok csökkentett toxicitású orális dózisformái |
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| US20090036495A1 (en) | 2009-02-05 |
| RU2006137076A (ru) | 2008-04-27 |
| WO2005102389A2 (en) | 2005-11-03 |
| CA2563356A1 (en) | 2005-11-03 |
| JP2007533723A (ja) | 2007-11-22 |
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| AR049029A1 (es) | 2006-06-21 |
| BRPI0509993A (pt) | 2007-10-16 |
| CN1946391A (zh) | 2007-04-11 |
| NO20065271L (no) | 2006-12-12 |
| TW200539861A (en) | 2005-12-16 |
| KR20070000495A (ko) | 2007-01-02 |
| WO2005102389A3 (en) | 2006-08-17 |
| EP1740211A2 (en) | 2007-01-10 |
| MXPA06012172A (es) | 2007-01-17 |
| IL178609A0 (en) | 2007-02-11 |
| AU2005235248A1 (en) | 2005-11-03 |
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