ES2527467T3 - Nuevas bencenosulfonamidas como bloqueantes de canales de calcio - Google Patents
Nuevas bencenosulfonamidas como bloqueantes de canales de calcio Download PDFInfo
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- ES2527467T3 ES2527467T3 ES10701070.4T ES10701070T ES2527467T3 ES 2527467 T3 ES2527467 T3 ES 2527467T3 ES 10701070 T ES10701070 T ES 10701070T ES 2527467 T3 ES2527467 T3 ES 2527467T3
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- alkyl
- nrc
- heteroaryl
- aryl
- alkoxy
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- 229940127291 Calcium channel antagonist Drugs 0.000 title 1
- 150000008331 benzenesulfonamides Chemical class 0.000 title 1
- 239000000480 calcium channel blocker Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract description 3
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 3
- 125000003725 azepanyl group Chemical group 0.000 abstract 2
- 125000002393 azetidinyl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000002757 morpholinyl group Chemical group 0.000 abstract 2
- 125000003386 piperidinyl group Chemical group 0.000 abstract 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 101150093826 par1 gene Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 101000932804 Homo sapiens Voltage-dependent T-type calcium channel subunit alpha-1H Proteins 0.000 description 3
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 2
- 102000054636 human CACNA1H Human genes 0.000 description 2
- 239000005557 antagonist Substances 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
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- C07D—HETEROCYCLIC COMPOUNDS
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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Abstract
Un compuesto de fórmula (I) o (II),**Fórmula** o una sal farmacéuticamente aceptable del mismo, donde R1 es X y R2 es Y; X es (i) o (ii): m y n, en cada caso, son independientemente 1 o 2; G1 es azetidinilo, pirrolidinilo, piperidinilo, morfolinilo, tiomorfolinilo o azepanilo, donde G1 está conectado a través del átomo de nitrógeno de dicho azetidinilo, pirrolidinilo, piperidinilo, morfolinilo, tiomorfolinilo o azepanilo; Y es -NRcAr1, -NRcAr2-Ar1, -NRcCH(Ar1)2, -NRc(CRaRb)pAr1, -NRc(CRaRb)pCH(Ar1)2, -NRc-G2, -NRc-G2-Ar1, (iii), (iv), (v) o (vi): Ar1, en cada caso, es independientemente arilo o heteroarilo, donde dicho arilo y heteroarilo están sin sustituir o sustituidos con 1, 2, 3 o 4 o 5 sustituyentes seleccionados entre alcoxi, alquilo, ciano, haloalquilo, halógeno o -N(alquilo)2; Ar2 es arilo o heteroarilo, donde dicho arilo y heteroarilo están sin sustituir o sustituidos con 1, 2, 3 o 4 sustituyentes seleccionados entre alcoxi, alquilo, ciano, haloalquilo o halógeno; G2 es cicloalquilo; Ra y Rb son en cada caso independientemente hidrógeno, alquilo o hidroxialquilo; Rc es hidrógeno o alquilo; p es 1, 2, 3 o 4; y R3, R4, R5 y R6 son cada uno independientemente hidrógeno, alcoxi, alquilo o halógeno.
Description
E10701070
07-01-2015
concentraciones en aumento de antagonista a las células individuales en un formato de multi-adición con 5 minutos en cada concentración de prueba. Para cada célula, las respuestas se normalizaron a control de vehículo de dimetil sulfóxido para generar curvas de respuesta a concentración.
La Tabla 1 lista los valores de CI50 para los compuestos 1-49, 57-59, 61-64, 66, 67, 70 y 74 de la presente invención; los demás compuestos en la tabla no forman parte de la presente invención.
Tabla 1. Determinación electrofisiológica para canales Cav3.2 humanos
- Ejemplo
- Calificador CI50 (μM) de Cav3.2 humana -77 mV GeoMean Ejemplo Calificador CI50 (μM) de Cav3.2 humana -77 mV GeoMean
- 1
- > 10 43 4,9
- 2
- 10,6 44 4,9
- 3
- 5,9 45 > 10
- 4
- 7,7 46 1,8
- 5
- 1,8 47 3,8
- 6
- 1,9 48 > 10
- 7
- 6,5 49 1,3
- 8
- 2,1 50 0,6
- 9
- 7,3 51 0,9
- 10
- 1,5 52 0,6
- 11
- 6,6 53 0,5
- 12
- 4,7 54 1,2
- 13
- 5,6 55 1,8
- 14
- 3,7 56 4,1
- 15
- > 10 57 48
- 16
- 6,0 58 4,6
- 17
- > 10 59 9,0
- 18
- 9,3 60 5,0
- 19
- 2,4 61 > 10
- 20
- 6 62 > 10
- 21
- 5,9 63 > 10
- 22
- 1,4 64 1,7
- 23
- 2,5 65 1,84
- 24
- 1,0 66 5,9
- 25
- 8,9 67 3,18
- 26
- 1,5 68 10,9
- 27
- > 10 69 > 10
- 28
- 1,9 70 7,2
- 29
- 2,1 71 10
- 30
- 1,8 72 > 10
- 31
- 3,3 73 1,8
- 32
- 8,4 74 2
- 33
- 5,7 75 6,5
- 34
- 6,2 76 6,4
- 35
- 4,8 77 > 10
- 36
- 4,7 78 > 10
- 37
- 1,1 79 8,5
- 38
- 4,6 80 2
- 39
- 4,1 81 > 10
- 40
- 4,1 82 2,6
- 41
- 5,0 83 > 10
- 42
- 5,8
15
Claims (1)
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imagen1 imagen2 imagen3 imagen4
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US14489909P | 2009-01-15 | 2009-01-15 | |
US144899P | 2009-01-15 | ||
PCT/US2010/020964 WO2010083264A1 (en) | 2009-01-15 | 2010-01-14 | Novel benzenesulfonamides as calcium channel blockers |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2527467T3 true ES2527467T3 (es) | 2015-01-26 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES10701070.4T Active ES2527467T3 (es) | 2009-01-15 | 2010-01-14 | Nuevas bencenosulfonamidas como bloqueantes de canales de calcio |
Country Status (22)
Country | Link |
---|---|
US (3) | US8101614B2 (es) |
EP (1) | EP2382191B1 (es) |
JP (1) | JP5619773B2 (es) |
KR (1) | KR20110110299A (es) |
CN (1) | CN102282131B (es) |
AR (1) | AR077440A1 (es) |
AU (1) | AU2010204753A1 (es) |
BR (1) | BRPI1005675A2 (es) |
CA (1) | CA2747752A1 (es) |
CL (1) | CL2011001714A1 (es) |
CO (1) | CO6400194A2 (es) |
DO (1) | DOP2011000217A (es) |
ES (1) | ES2527467T3 (es) |
IL (1) | IL213500A0 (es) |
MX (1) | MX337190B (es) |
PE (1) | PE20120126A1 (es) |
RU (1) | RU2011134052A (es) |
SG (1) | SG172308A1 (es) |
TW (1) | TW201028421A (es) |
UY (1) | UY32384A (es) |
WO (1) | WO2010083264A1 (es) |
ZA (1) | ZA201104715B (es) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP5501226B2 (ja) | 2008-04-24 | 2014-05-21 | Msd株式会社 | アリールスルホニル誘導体を有効成分とする長鎖脂肪酸伸長酵素阻害剤 |
TW201028421A (en) * | 2009-01-15 | 2010-08-01 | Abbott Lab | Novel benzenesulfonamides as calcium channel blockers |
KR20140091522A (ko) * | 2011-09-15 | 2014-07-21 | 타이페이 메디컬 유니이버시티 | 심부전증 또는 신경 손상을 치료하기 위한 인돌릴 및 인돌리닐 하이드록사메이트의 용도 |
US8648074B2 (en) | 2011-09-29 | 2014-02-11 | Abbvie Inc. | Substituted octahydropyrrolo[1,2-a]pyrazine sulfonamides as calcium channel blockers |
US8669255B2 (en) | 2011-09-29 | 2014-03-11 | Abbvie Inc. | Substituted octahydropyrrolo[1,2-a]pyrazines as calcium channel blockers |
WO2013103867A1 (en) | 2012-01-05 | 2013-07-11 | Abbvie Inc. | Benzenesulfonamide derivative for use in the treatment of diabetic neuropathy |
MX2015007460A (es) | 2012-12-12 | 2015-09-04 | Abbvie Inc | Agentes para el tratamiento del dolor y usos de los mismos. |
CN105873913B (zh) * | 2013-09-10 | 2019-12-03 | 得克萨斯系统大学评议会 | 靶向截短的腺瘤性结肠息肉(apc)蛋白的治疗法 |
US9700549B2 (en) | 2013-10-03 | 2017-07-11 | David Wise | Compositions and methods for treating pelvic pain and other conditions |
US10082496B2 (en) | 2014-09-10 | 2018-09-25 | Board Of Regents Of The University Of Texas System | Targeting emopamil binding protein (EBP) with small molecules that induce an abnormal feedback response by lowering endogenous cholesterol biosynthesis |
FI3364993T3 (fi) | 2015-10-22 | 2023-01-13 | Menetelmiä angelmanin oireyhtymän hoitamiseksi | |
AU2018221722B2 (en) | 2017-02-15 | 2022-02-03 | Cavion, Inc. | Calcium channel inhibitors |
EP3615521A4 (en) | 2017-04-26 | 2021-02-17 | Cavion, Inc. | MEMORY AND COGNITION IMPROVEMENT, AND TREATMENT OF MEMORY AND COGNITIVE DISORDERS |
EP3737382A1 (en) | 2018-01-10 | 2020-11-18 | Cura Therapeutics, LLC | Pharmaceutical compositions comprising phenylsulfonamides, and their therapeutic applications |
CA3107145A1 (en) | 2018-08-24 | 2020-02-27 | Sunshine Lake Pharma Co., Ltd. | Pyridinylmethylenepiperidine derivatives and uses thereof |
US20220016095A1 (en) | 2018-10-03 | 2022-01-20 | Cavion, Inc. | Treating essential tremor using (r)-2-(4-isopropylphenyl)-n-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide |
US20200131156A1 (en) * | 2018-10-30 | 2020-04-30 | H. Lundbeck A/S | ARYLSULFONYLPYROLECARBOXAMIDE DERIVATIVES AS Kv3 POTASSIUM CHANNEL ACTIVATORS |
CN114340670A (zh) | 2019-07-11 | 2022-04-12 | 普拉克西斯精密药物股份有限公司 | T-型钙通道调节剂的制剂及其使用方法 |
EP3997068A1 (en) * | 2019-07-11 | 2022-05-18 | Cura Therapeutics, LLC | Sulfone compounds and pharmaceutical compositions thereof, and their therapeutic applications for the treatment of neurodegenerative diseases |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1165508B1 (en) | 1999-04-07 | 2004-06-23 | The University of Virginia Patent Foundation | Anticancer calcium channel blockers |
TW200503994A (en) * | 2003-01-24 | 2005-02-01 | Novartis Ag | Organic compounds |
US7223754B2 (en) | 2003-03-10 | 2007-05-29 | Dynogen Pharmaceuticals, Inc. | Thiazolidinone, oxazolidinone, and imidazolone derivatives for treating lower urinary tract and related disorders |
EP1615698B1 (en) * | 2003-04-11 | 2010-09-29 | High Point Pharmaceuticals, LLC | New amide derivatives and pharmaceutical use thereof |
DE602004012083T2 (de) * | 2003-04-15 | 2009-04-23 | Astrazeneca Ab | Neue Verbindungen, die als Verstärker von Glutamatrezeptoren dienen |
WO2006105127A2 (en) * | 2005-03-31 | 2006-10-05 | Takeda San Diego, Inc. | Hydroxysteroid dehydrogenase inhibitors |
WO2007052843A1 (ja) * | 2005-11-04 | 2007-05-10 | Takeda Pharmaceutical Company Limited | 複素環アミド化合物およびその用途 |
CA2666275A1 (en) * | 2006-10-13 | 2008-04-17 | Neuromed Pharmaceuticals Ltd. | Cyclopropyl-piperazine compounds as calcium channel blockers |
WO2008151184A1 (en) * | 2007-06-03 | 2008-12-11 | Vanderbilt University | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
JP5501226B2 (ja) | 2008-04-24 | 2014-05-21 | Msd株式会社 | アリールスルホニル誘導体を有効成分とする長鎖脂肪酸伸長酵素阻害剤 |
TW201028421A (en) * | 2009-01-15 | 2010-08-01 | Abbott Lab | Novel benzenesulfonamides as calcium channel blockers |
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EP2382191B1 (en) | 2014-11-12 |
AR077440A1 (es) | 2011-08-31 |
JP2012515209A (ja) | 2012-07-05 |
RU2011134052A (ru) | 2013-02-20 |
KR20110110299A (ko) | 2011-10-06 |
US8101614B2 (en) | 2012-01-24 |
MX2011007496A (es) | 2011-08-04 |
UY32384A (es) | 2010-08-31 |
IL213500A0 (en) | 2011-07-31 |
US8741899B2 (en) | 2014-06-03 |
WO2010083264A1 (en) | 2010-07-22 |
JP5619773B2 (ja) | 2014-11-05 |
CL2011001714A1 (es) | 2011-11-11 |
AU2010204753A1 (en) | 2011-08-11 |
ZA201104715B (en) | 2014-01-29 |
CO6400194A2 (es) | 2012-03-15 |
EP2382191A1 (en) | 2011-11-02 |
PE20120126A1 (es) | 2012-03-18 |
TW201028421A (en) | 2010-08-01 |
MX337190B (es) | 2016-02-16 |
CN102282131B (zh) | 2015-08-26 |
SG172308A1 (en) | 2011-07-28 |
US8404719B2 (en) | 2013-03-26 |
US20100197693A1 (en) | 2010-08-05 |
US20120083499A1 (en) | 2012-04-05 |
BRPI1005675A2 (pt) | 2017-06-13 |
CA2747752A1 (en) | 2010-07-22 |
CN102282131A (zh) | 2011-12-14 |
DOP2011000217A (es) | 2011-07-31 |
US20130210827A1 (en) | 2013-08-15 |
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