BRPI0510951A - derivados de piperidina como antagonistas de nk1 e nk3 - Google Patents

derivados de piperidina como antagonistas de nk1 e nk3

Info

Publication number
BRPI0510951A
BRPI0510951A BRPI0510951-5A BRPI0510951A BRPI0510951A BR PI0510951 A BRPI0510951 A BR PI0510951A BR PI0510951 A BRPI0510951 A BR PI0510951A BR PI0510951 A BRPI0510951 A BR PI0510951A
Authority
BR
Brazil
Prior art keywords
alkyl
aryl
heteroaryl
heterocycloalkyl
independently selected
Prior art date
Application number
BRPI0510951-5A
Other languages
English (en)
Inventor
Brian Thomas O'neill
Vinod Dipak Parikh
Willard Mickowan Welch Jr
Original Assignee
Pfizer Prod Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of BRPI0510951A publication Critical patent/BRPI0510951A/pt

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D211/36—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D211/36—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D211/36—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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

DERIVADOS DE PIPERIDINA COMO ANTAGONISTAS DE NKl E NK3 A invenção está relacionada a compostos de acordo com a fórmula I que exibem propriedades inibitórias de neurocinina, uma composição farmacêutica compreendendo, o mesmo e um método de tratamento para condições mediadas por neurocinina. Fórmula (I) ou um sal farmaceuticamente aceitável ou solvato da mesma onde: m = 0 ou 1; n = 0 ou 1; 5 = 0 ou 1; L é -O- ou -N(R¬ 4¬)-; R¬ 1¬ e R¬ 2¬ são, cada um, independentemente H, arila, heteroarila, -alquila (C~ 1~-C~ 6~) heterocicloalquila, -alquila (C~ 1~-C~ 6~) heterocicloalquila, -alquila (C~ 1~-C~ 6~) heteroarila, -alquila (C~ 1~-C~ 6~) - O-arila, alquila (C~ 1~-C~ 6~) arila, e -H~ 2~N(R¬ 4¬) (R¬ 5¬), onde cada uma das referidas heterocicloalquila, -alquila (C~ 1~-C~ 6~) hetzerocicloalquila, -alquila (C~ 1~-C~ 6~) heteroarila, -alquila (C~ 1~-C~ 6~) -0-arila, arila, -alquila (C~ 1~-C~ 6~) arila, heteroarila, e -CH~ 2~N (R¬ 4¬) (R¬ 5¬), é opcionalmente substituída com 1 a 3 frações independentemente selecionadas de X<39>, Y<39> ou Z <39>; R¬ 3¬ é H, CF~ 3~, OH, ou -alquila (C~ 1~-C~ 6~); R¬ 4¬, e R¬ 5¬, são, cada um, independentemente selecionados de H, -alquila (C~ 1~-C~ 6~), ou - (C~ 1~-C~ 6~) (C=O) R¬ 7¬; R¬ 7¬ é alquila (C~ 1~-C~ 6~ ), OH, -N(R¬ 4¬) (R¬ 5¬), ou -OR¬ 4¬; R¬ 8¬ e R~ 9¬ são, cada um, independentemente alquila (C~ 1~-C~ 6~); X, Y, X<39>, Y<39> e Z<39> são, cada um, independentemente selecionados de H, -alquila (C~ 1~-C~ 6~), -alquila (C~ 1~-C~ 6~) -NR¬ 4¬R¬ 5¬, CF~ 3~, OH, -O-alquila (C~ 1~-C~ 6~), -alquila (C~ 1~-C~ 6~) - C(=O) R¬ 7¬, arila, heteroarila, cicloalquila, -NO~ 2~, -alquila (C~ 1~-C~6~) arila, -O-arila, halogênio, CN, -CH~ 3~N(R¬ 4¬) (R¬ 5¬), -C(=O)R¬ 7¬, -C(=O)R¬ 7¬, -R¬ 6¬C(=O)R¬ 7¬ ou -R¬ 6¬C(=O) NR¬ 4¬R¬ 5~; e R¬ 6¬ é uma ligação, -CH~ 2~-, -O-, ou -NR¬ 4¬-.
BRPI0510951-5A 2004-05-12 2005-04-29 derivados de piperidina como antagonistas de nk1 e nk3 BRPI0510951A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US57050804P 2004-05-12 2004-05-12
PCT/IB2005/001198 WO2005110987A1 (en) 2004-05-12 2005-04-29 Piperidine derivatives as nk1 and nk3 antagonists

Publications (1)

Publication Number Publication Date
BRPI0510951A true BRPI0510951A (pt) 2007-11-20

Family

ID=34966231

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0510951-5A BRPI0510951A (pt) 2004-05-12 2005-04-29 derivados de piperidina como antagonistas de nk1 e nk3

Country Status (7)

Country Link
US (1) US20050256164A1 (pt)
EP (1) EP1748984A1 (pt)
JP (1) JP2007537233A (pt)
BR (1) BRPI0510951A (pt)
CA (1) CA2565953A1 (pt)
MX (1) MXPA06013162A (pt)
WO (1) WO2005110987A1 (pt)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
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WO2006057921A2 (en) * 2004-11-22 2006-06-01 Merck & Co., Inc. Piperidinyl piperidine tachykinin receptor antagonists
TW200716603A (en) * 2005-04-21 2007-05-01 Takeda Pharmaceuticals Co Piperidine derivative crystal, process for producing the same, and use
WO2006115285A1 (ja) * 2005-04-21 2006-11-02 Takeda Pharmaceutical Company Limited 医薬組成物
WO2007015588A1 (en) * 2005-08-04 2007-02-08 Takeda Pharmaceutical Company Limited Piperidine derivative as tachykinin receptor antagonist
JP2009523170A (ja) * 2006-01-11 2009-06-18 メルク エンド カムパニー インコーポレーテッド 縮合トリアゾールタキキニン受容体アンダニスト
MX2009013115A (es) * 2007-06-07 2010-01-15 Hoffmann La Roche Derivados de prolinamida como antagonistas de nk3.
AR069526A1 (es) * 2007-12-03 2010-01-27 Takeda Pharmaceutical Compuesto heterociclico que contiene nitrogeno y su uso
US8063075B2 (en) * 2008-06-10 2011-11-22 Hoffmann-La Roche Inc. Pyrrolidine ether derivatives as NK3 receptor antagonists
USRE48334E1 (en) 2008-09-19 2020-12-01 Takeda Pharmaceutical Company Limited Nitrogen-containing heterocyclic compound and use of same
JP2012505173A (ja) 2008-10-09 2012-03-01 エフ．ホフマン−ラ ロシュ アーゲー ピロリジンｎ−ベンジル誘導体
EP2391615B1 (en) * 2009-01-30 2013-01-16 F. Hoffmann-La Roche AG Piperidine derivatives as nk3 receptor antagonists
US9446029B2 (en) * 2010-07-27 2016-09-20 Colorado State University Research Foundation Use of NK-1 receptor antagonists in management of visceral pain
GB201116335D0 (en) * 2011-09-21 2011-11-02 Novaremed Ltd A method of treating or preventing affective disorders
JP6420074B2 (ja) * 2013-06-27 2018-11-07 国立大学法人京都大学 プテロシン誘導体を含む軟骨欠損、軟骨変性、および／または軟骨菲薄疾患治療剤
HUE047732T2 (hu) 2015-05-18 2020-05-28 Nerre Therapeutics Ltd NK-1/NK-3 receptor antagonista vértolulások kezeléséhez
UA128159C2 (uk) 2018-03-14 2024-04-24 Канді Терап'Ютікс Лімітед Фармацевтичний препарат для капсули з м'якого желатину, який містить подвійний антагоніст рецептора nk-1/nk-3

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CH485756A (de) * 1966-10-07 1970-02-15 Sandoz Ag Verfahren zur Herstellung neuer Naphthyridin-Derivate
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Also Published As

Publication number Publication date
WO2005110987A1 (en) 2005-11-24
MXPA06013162A (es) 2007-02-13
JP2007537233A (ja) 2007-12-20
CA2565953A1 (en) 2005-11-24
US20050256164A1 (en) 2005-11-17
EP1748984A1 (en) 2007-02-07

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Legal Events

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B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 5A E 6A ANUIDADE(S).

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE A 8.6 NA RPI 2099 DE 29/03/2011.