BRPI0415862A - processo para preparar um composto - Google Patents

processo para preparar um composto

Info

Publication number
BRPI0415862A
BRPI0415862A BRPI0415862-8A BRPI0415862A BRPI0415862A BR PI0415862 A BRPI0415862 A BR PI0415862A BR PI0415862 A BRPI0415862 A BR PI0415862A BR PI0415862 A BRPI0415862 A BR PI0415862A
Authority
BR
Brazil
Prior art keywords
pyran
tetrahydro
trifluoromethyl
methoxy
isopropyl
Prior art date
Application number
BRPI0415862-8A
Other languages
English (en)
Inventor
Dongwei Cai
Fred Fleitz
Min Ge
Scott Hoerrner
Gary Javadi
Mark Jensen
Robert Larsen
Wenjie Li
Dorian Nelson
Elizabeth Szumigala
Lihu Yang
Changyou Zhou
Original Assignee
Merck & Co 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 Merck & Co Inc filed Critical Merck & Co Inc
Publication of BRPI0415862A publication Critical patent/BRPI0415862A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/24—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/36—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids
    • C07C303/40—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/325—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • C07D207/327—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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/10—Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

"PROCESSO PARA PREPARAR UM COMPOSTO". A presente invenção proporciona uma sintese eficiente para a preparação de ((1R,3S)-3-isopropil-3-{¢3-(trifluorometil)-7,8-di-hidro-1,6naftiridin-6(5H )-i1!-carboni1}-ciclo-penti1)¢(3S,4S)-3-metóxi-tetra-hidro-2Hpiran-4-i1 !-amina e seu sal de succinato. A presente invenção adicionalmente proporciona uma sintese eficiente para a preparação de intermediários (3R)-3metóxi-tetra-hidro-4H-piran-4-ona; ácido (lS,4S)-4-(2,5-dimeti1-1H-pirro1-1i1)-1-isopropi1-ciclo-pent-2-eno-1-c arboxílico; e 3-(trifluorometi1)-5,6,7,8tetra-hidro-1,6-naftiridina; e para a preparação do precursor (3S,4S)-N((1S,4S)-4-isopropi1-4-{¢3-trifluorometi1)-7,8-di-hidro-1,6-na ftiridin-6(5H)i1!-carboni1}-ciclo-pent-2-en-1-i1)-3-metóxi-tetra-hidro-2 H-piran-4-amina. A invenção adicionalmente reside nas propriedades superiores do sal de succinato de ((1R,3S)-3-isopropi1-3-{¢3-(trifluorometi1)-7,8-di-hidro-1,6naftiridin-6(5 H)-i1!-carboni1}-ciclo-penti1)¢(3S,4S)-3-metóxi-tetra-hidro-2Hpiran-4-i 1!-amina.
BRPI0415862-8A 2003-10-27 2004-10-25 processo para preparar um composto BRPI0415862A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US51475403P 2003-10-27 2003-10-27
PCT/US2004/035294 WO2005044795A1 (en) 2003-10-27 2004-10-25 Process for the preparation of ccr-2 antagonist

Publications (1)

Publication Number Publication Date
BRPI0415862A true BRPI0415862A (pt) 2007-01-09

Family

ID=34572776

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0415862-8A BRPI0415862A (pt) 2003-10-27 2004-10-25 processo para preparar um composto

Country Status (11)

Country Link
US (1) US7361765B2 (pt)
EP (1) EP1682500A1 (pt)
JP (1) JP4551405B2 (pt)
CN (1) CN101160286B (pt)
AR (1) AR045875A1 (pt)
AU (1) AU2004287810B2 (pt)
BR (1) BRPI0415862A (pt)
CA (1) CA2543250C (pt)
IS (1) IS8416A (pt)
TW (1) TWI294426B (pt)
WO (1) WO2005044795A1 (pt)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004050024A2 (en) 2002-11-27 2004-06-17 Incyte Corporation 3-aminopyrrolidine derivatives as modulators of chemokine receptors
WO2004082616A2 (en) * 2003-03-18 2004-09-30 Merck & Co. Inc. Tetrahydropyranyl cyclopentyl heterocylic amide modulators of chemokine receptor activity
RU2317295C1 (ru) * 2003-10-27 2008-02-20 Мерк Энд Ко., Инк. Соль антагониста ccr-2
CA2550596C (en) 2003-12-18 2011-03-15 Incyte Corporation 3-cycloalkylaminopyrrolidine derivatives as modulators of chemokine receptors
CN1950085A (zh) 2004-05-11 2007-04-18 因赛特公司 作为趋化因子受体调节剂的3－(4－杂芳基环己基氨基)环戊烷羧酰胺
WO2012125663A2 (en) * 2011-03-17 2012-09-20 Merck Sharp & Dohme Corp. Cyclohexane substituted amino cyclopentane derivatives as useful ccr2 antagonists
US8822460B2 (en) * 2012-04-06 2014-09-02 Janssen Pharmaceutica Nv Fused cyclopentyl antagonists of CCR2
CN104418769A (zh) * 2013-09-03 2015-03-18 苏州安尼康药物研发有限公司 一种化合物及其制备方法
US20180072945A1 (en) 2015-04-27 2018-03-15 Konica Minolta, Inc. Material for organic electroluminescent elements, organic electroluminescent element, display device and lighting device
RU2726206C2 (ru) 2015-05-21 2020-07-09 Кемосентрикс, Инк. Модуляторы ccr2
CN105968055B (zh) * 2016-07-26 2018-08-28 中国科学院长春应用化学研究所 一种芳基嘧啶及其衍生物的制备方法
EP3687525B1 (en) 2017-09-25 2025-10-29 ChemoCentryx, Inc. Combination therapy using a chemokine receptor 2 (ccr2) antagonist and a pd-1/pd-l1 inhibitor
US20190269664A1 (en) 2018-01-08 2019-09-05 Chemocentryx, Inc. Methods of treating solid tumors with ccr2 antagonists
CN112105353B (zh) 2018-01-08 2024-04-19 凯莫森特里克斯股份有限公司 Ccr2拮抗剂治疗实体瘤的方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH09291034A (ja) * 1996-02-27 1997-11-11 Yoshitomi Pharmaceut Ind Ltd 縮合ピリジン化合物およびその医薬としての用途
WO2002013824A1 (en) * 2000-08-17 2002-02-21 Merck & Co., Inc. Cyclopentyl modulators of chemokine receptor activity
JP2004529943A (ja) * 2001-05-15 2004-09-30 イー・アイ・デュポン・ドウ・ヌムール・アンド・カンパニー 殺菌・殺カビ剤としてのピリジニル縮合二環式アミド
JP3780291B2 (ja) * 2002-04-29 2006-05-31 メルク エンド カムパニー インコーポレーテッド テトラヒドロピラニルシクロペンチルテトラヒドロピリドピリジン系のケモカイン受容体活性調節剤
RU2317295C1 (ru) * 2003-10-27 2008-02-20 Мерк Энд Ко., Инк. Соль антагониста ccr-2

Also Published As

Publication number Publication date
CA2543250C (en) 2011-03-29
EP1682500A1 (en) 2006-07-26
CN101160286B (zh) 2012-07-04
US20070135475A1 (en) 2007-06-14
CN101160286A (zh) 2008-04-09
AU2004287810A1 (en) 2005-05-19
AU2004287810B2 (en) 2011-01-06
JP2007509944A (ja) 2007-04-19
US7361765B2 (en) 2008-04-22
WO2005044795A1 (en) 2005-05-19
WO2005044795A8 (en) 2006-06-22
TW200530233A (en) 2005-09-16
TWI294426B (en) 2008-03-11
AR045875A1 (es) 2005-11-16
CA2543250A1 (en) 2005-05-19
IS8416A (is) 2006-04-12
JP4551405B2 (ja) 2010-09-29

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Legal Events

Date Code Title Description
B25D Requested change of name of applicant approved

Owner name: MERCK SHARP AND DOHME CORP. (US)

Free format text: ALTERADO DE: MERCK AND CO., INC.

B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 7A ANUIDADE.

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 AO DESPACHO 8.6 PUBLICADO NA RPI 2144 DE 07/02/2012.