BR0016530A - Bloqueadores do canal de cálcio de piperazina e piperidina substituìda - Google Patents
Bloqueadores do canal de cálcio de piperazina e piperidina substituìdaInfo
- Publication number
- BR0016530A BR0016530A BR0016530-1A BR0016530A BR0016530A BR 0016530 A BR0016530 A BR 0016530A BR 0016530 A BR0016530 A BR 0016530A BR 0016530 A BR0016530 A BR 0016530A
- Authority
- BR
- Brazil
- Prior art keywords
- calcium channel
- channel blockers
- alkyl
- chain
- trivalent straight
- Prior art date
Links
- 229940127291 Calcium channel antagonist Drugs 0.000 title abstract 2
- 239000000480 calcium channel blocker Substances 0.000 title abstract 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical class C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 title 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N diethylenediamine Natural products C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 title 1
- 150000004885 piperazines Chemical class 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000520 N-substituted aminocarbonyl group Chemical group [*]NC(=O)* 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- HDCXQTPVTAIPNZ-UHFFFAOYSA-N n-({[4-(aminosulfonyl)phenyl]amino}carbonyl)-4-methylbenzenesulfonamide Chemical compound C1=CC(C)=CC=C1S(=O)(=O)NC(=O)NC1=CC=C(S(N)(=O)=O)C=C1 HDCXQTPVTAIPNZ-UHFFFAOYSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4515—Non condensed piperidines, e.g. piperocaine having a butyrophenone group in position 1, e.g. haloperidol
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- 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
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- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
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- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D211/08—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/10—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
- C07D211/14—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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- 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
- C07D211/08—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/10—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
- C07D211/16—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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- 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
- C07D211/40—Oxygen atoms
- C07D211/44—Oxygen atoms attached in position 4
- C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
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- 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
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- C07D295/02—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
- C07D295/027—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
- C07D295/03—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to acyclic carbon atoms
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- C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
- C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
- C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
- C07D317/60—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
"BLOQUEADORES DO CANAL DE CáLCIO DE PIPERAZINA E PIPERIDINA SUBSTITUìDA". Compostos de fórmula (1) e seus sais, em que Cy representa ciclohexila; y é CH=CH<237>L, CH<237>~ 2~, <237> OU Cy X é alquileno de cadeia linear trivalente (3-10C) ou 1-alquenileno de cadeia linear trivalente (3-10C) opcionalmente substituído por oxo no N do carbono adjacente quando n é 0 e Y é <237>~ 2CH~; e é diferentemente alquileno de cadeia linear trivalente (5-10C) ou 1-alquenileno de cadeia linear trivalente (5-10C) opcionalmente substituído com oxo no N do carbono adjacente; Z é N, NCO, CHNCOR^ 1^ ou CHNR^ 1^, em que R^ 1^ é alquila (C1-6); e n é 0-5; em que cada <237> e Cy independentemente, podem ser opcionalmente substituídos por alquila (C1-6) ou por halo, CF~ 3~, OCF~ 3~, NO~ 2~, NR~ 2~,OR, SR, COR, COOR, CONR~ 2~, NROCR ou OOCR em que R é H ou alquila (C14) ou dois substituintes podem formar um anel de 5-7 membros. com a condição de que os compostos de fórmula (1) contenham pelo menos uma porção aromática, de utilidade como bloqueadores do canal de cálcio.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US17283199P | 1999-12-20 | 1999-12-20 | |
US09/476,927 US6387897B1 (en) | 1998-06-30 | 1999-12-30 | Preferentially substituted calcium channel blockers |
PCT/CA2000/001557 WO2001045709A1 (en) | 1999-12-20 | 2000-12-20 | Substituted piperazine and piperidine calcium channel blockers |
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Family Applications (1)
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BR0016530-1A BR0016530A (pt) | 1999-12-20 | 2000-12-20 | Bloqueadores do canal de cálcio de piperazina e piperidina substituìda |
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US (2) | US6387897B1 (pt) |
EP (1) | EP1244451B1 (pt) |
JP (1) | JP2003518064A (pt) |
KR (1) | KR100823889B1 (pt) |
CN (1) | CN100477992C (pt) |
AT (1) | ATE333878T1 (pt) |
AU (1) | AU784206B2 (pt) |
BR (1) | BR0016530A (pt) |
CA (1) | CA2394327C (pt) |
DE (1) | DE60029634T2 (pt) |
DK (1) | DK1244451T3 (pt) |
ES (1) | ES2269220T3 (pt) |
HK (1) | HK1049969B (pt) |
IL (1) | IL150117A0 (pt) |
MX (1) | MXPA02006138A (pt) |
NO (1) | NO323724B1 (pt) |
PT (1) | PT1244451E (pt) |
WO (1) | WO2001045709A1 (pt) |
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JP2008534630A (ja) * | 2005-04-08 | 2008-08-28 | ニューロメッド ファーマシューティカルズ リミテッド | 疼痛の軽減のためのn型カルシウムチャネルブロッカーを含む組み合わせ治療の方法 |
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JP2010540629A (ja) * | 2007-10-04 | 2010-12-24 | メルク・シャープ・エンド・ドーム・コーポレイション | カルシウムチャネル遮断薬としての置換アリールスルホン誘導体 |
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-
1999
- 1999-12-30 US US09/476,927 patent/US6387897B1/en not_active Expired - Lifetime
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2000
- 2000-12-20 MX MXPA02006138A patent/MXPA02006138A/es active IP Right Grant
- 2000-12-20 KR KR1020027007951A patent/KR100823889B1/ko not_active IP Right Cessation
- 2000-12-20 JP JP2001546648A patent/JP2003518064A/ja active Pending
- 2000-12-20 CN CNB008174369A patent/CN100477992C/zh not_active Expired - Fee Related
- 2000-12-20 EP EP00988531A patent/EP1244451B1/en not_active Expired - Lifetime
- 2000-12-20 AU AU24956/01A patent/AU784206B2/en not_active Ceased
- 2000-12-20 DK DK00988531T patent/DK1244451T3/da active
- 2000-12-20 AT AT00988531T patent/ATE333878T1/de active
- 2000-12-20 DE DE60029634T patent/DE60029634T2/de not_active Expired - Lifetime
- 2000-12-20 ES ES00988531T patent/ES2269220T3/es not_active Expired - Lifetime
- 2000-12-20 IL IL15011700A patent/IL150117A0/xx active IP Right Grant
- 2000-12-20 BR BR0016530-1A patent/BR0016530A/pt not_active Application Discontinuation
- 2000-12-20 PT PT00988531T patent/PT1244451E/pt unknown
- 2000-12-20 CA CA2394327A patent/CA2394327C/en not_active Expired - Fee Related
- 2000-12-20 WO PCT/CA2000/001557 patent/WO2001045709A1/en active IP Right Grant
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AU2495601A (en) | 2001-07-03 |
US20030045530A1 (en) | 2003-03-06 |
DK1244451T3 (da) | 2006-10-30 |
NO323724B1 (no) | 2007-06-25 |
CA2394327A1 (en) | 2001-06-28 |
US6617322B2 (en) | 2003-09-09 |
DE60029634T2 (de) | 2007-07-05 |
KR100823889B1 (ko) | 2008-04-22 |
NO20022947D0 (no) | 2002-06-19 |
DE60029634D1 (de) | 2006-09-07 |
JP2003518064A (ja) | 2003-06-03 |
WO2001045709A1 (en) | 2001-06-28 |
IL150117A0 (en) | 2002-12-01 |
CN100477992C (zh) | 2009-04-15 |
EP1244451B1 (en) | 2006-07-26 |
ATE333878T1 (de) | 2006-08-15 |
CA2394327C (en) | 2012-01-24 |
KR20020075874A (ko) | 2002-10-07 |
EP1244451A1 (en) | 2002-10-02 |
ES2269220T3 (es) | 2007-04-01 |
US6387897B1 (en) | 2002-05-14 |
NO20022947L (no) | 2002-08-09 |
HK1049969B (zh) | 2006-12-29 |
AU784206B2 (en) | 2006-02-23 |
MXPA02006138A (es) | 2002-12-05 |
CN1411374A (zh) | 2003-04-16 |
HK1049969A1 (en) | 2003-06-06 |
PT1244451E (pt) | 2006-10-31 |
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