PE78898A1 - Derivados de 2,4-diaminopirimidinas - Google Patents

Derivados de 2,4-diaminopirimidinas

Info

Publication number
PE78898A1
PE78898A1 PE1997000356A PE00035697A PE78898A1 PE 78898 A1 PE78898 A1 PE 78898A1 PE 1997000356 A PE1997000356 A PE 1997000356A PE 00035697 A PE00035697 A PE 00035697A PE 78898 A1 PE78898 A1 PE 78898A1
Authority
PE
Peru
Prior art keywords
formula
compounds
iii
compound
metoxyl
Prior art date
Application number
PE1997000356A
Other languages
English (en)
Inventor
Henri Stalder
Philippe Guerry
Pierre-Charles Wyss
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE78898A1 publication Critical patent/PE78898A1/es

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/06—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with the ring nitrogen atom acylated by carboxylic or carbonic acids, or with sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • C07D401/10—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 aromatic rings
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D409/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/14—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 three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIEREN A COMPUESTOS DE FORMULA (I) Y A LOS COMPUESTOS INTERMEDIOS DE FORMULA (III), EN DONDE: R1 Y R2 SON DE PREFERENCIA METOXILO; R3 ES H, CICLOALQUILO C3-C6, FENILO, PIRIDILO O TIENILO, ENTRE OTROS, LOS CUALES ESTAN OPCIONALMENTE SUSTITUIDOS; R4 Y R5 SON H, ALQUILO C1-C6 O ALCOXILO C1-C6, ENTRE OTROS; "Q" ES ETILENO O VINILENO. TAMBIEN SE REFIERE AL PROCEDIMIENTO DE PREPARACION DE LOS COMPUESTOS DE FORMULA (I), QUE COMPRENDE: HACER REACCIONAR UN COMPUESTO (II), EN DONDE Y ES UN GRUPO PARTIENTE, CON UN COMPUESTO DE FORMULA (III), EN PRESENCIA DE UNA BASE TAL COMO UN CARBONATO DE METAL ALCALINO. LOS COMPUESTOS OBTENIDOS ACTUAN INHIBIENDO LA DEHIDROFOLATO REDUCTASA BACTERIAL (DHFR) Y POTENCIANDO LA ACTIVIDAD ANTIBACTERIANA DE SULFONAMIDAS Y OTROS INHIBIDORES DE ENZIMAS QUE ESTAN IMPLICADAS EN BIOSINTESIS DE ACIDOS FOLICOS, SIENDO UTILES COMO ANTIBIOTICOS PARTICULARMENTE EFECTIVOS CONTRA CEPAS GRAMPOSITIVAS MULTIRRESISTENTES Y CONTRA PATOGENOS OPORTUNISTAS TAL COMO PNEUMOCYSTIS CARINII
PE1997000356A 1996-05-15 1997-05-07 Derivados de 2,4-diaminopirimidinas PE78898A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP96107739 1996-05-15

Publications (1)

Publication Number Publication Date
PE78898A1 true PE78898A1 (es) 1998-11-13

Family

ID=8222784

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1997000356A PE78898A1 (es) 1996-05-15 1997-05-07 Derivados de 2,4-diaminopirimidinas

Country Status (29)

Country Link
US (1) US5866583A (es)
EP (1) EP0901488B1 (es)
JP (1) JP3098259B2 (es)
KR (1) KR100295509B1 (es)
CN (1) CN1098260C (es)
AR (1) AR007088A1 (es)
AT (1) ATE227282T1 (es)
AU (1) AU726416B2 (es)
BR (1) BR9709251A (es)
CA (1) CA2254117C (es)
CO (1) CO4840509A1 (es)
CY (1) CY2425B1 (es)
CZ (1) CZ364698A3 (es)
DE (1) DE69716901T2 (es)
DK (1) DK0901488T3 (es)
ES (1) ES2184089T3 (es)
HR (1) HRP970260A2 (es)
IL (1) IL126702A0 (es)
MA (1) MA24182A1 (es)
NO (1) NO985335L (es)
NZ (1) NZ332481A (es)
PE (1) PE78898A1 (es)
PL (1) PL330277A1 (es)
PT (1) PT901488E (es)
TR (1) TR199802331T2 (es)
TW (1) TW438796B (es)
WO (1) WO1997043277A1 (es)
YU (1) YU51498A (es)
ZA (1) ZA973984B (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0966464B1 (en) * 1997-03-03 2003-05-28 Basilea Pharmaceutica AG Substituted 2,4-diaminopyrimidines
CA2281642C (en) * 1997-03-03 2008-02-05 F. Hoffmann-La Roche Ag Substituted 2,4-diaminopyrimidines
US6277860B1 (en) * 1999-10-29 2001-08-21 Pfizer Inc Furopyridine antibacterials
US6544555B2 (en) 2000-02-24 2003-04-08 Advancis Pharmaceutical Corp. Antibiotic product, use and formulation thereof
US20020068078A1 (en) 2000-10-13 2002-06-06 Rudnic Edward M. Antifungal product, use and formulation thereof
WO2005011677A1 (en) * 2003-06-13 2005-02-10 Arena Pharmaceuticals, Inc. 5-substituted 2h-pyrazole-3-carboxylic acid derivatives as agonists for the nicotinic acid receptor rup25 for the treatment of dyslipidemia and related diseases
CN1832741A (zh) * 2003-08-07 2006-09-13 默克公司 作为11－β－羟甾类脱氢酶－1抑制剂的吡唑甲酰胺类
CA2535398C (en) 2003-08-12 2013-11-12 Advancis Pharmaceuticals Corporation Antibiotic product, use and formulation thereof
DE102005062987A1 (de) * 2005-12-28 2007-07-05 Grünenthal GmbH Substituierte Propiolsäureamide und ihre Verwendung zur Herstellung von Arzneimitteln
JP5341084B2 (ja) * 2007-08-03 2013-11-13 エフ．ホフマン−ラ ロシュ アーゲー Ｔａａｒ１リガンドとしてのピリジンカルボキシアミド及びベンズアミド誘導体
RU2528406C2 (ru) * 2008-11-21 2014-09-20 Раквалиа Фарма Инк. Новое производное пиразол-3-карбоксамида, обладающее антагонистической активностью в отношении рецептора 5-нт2в
CA2750047A1 (en) * 2009-01-21 2010-07-29 Basilea Pharmaceutica Ag Novel bicyclic antibiotics
JP5753856B2 (ja) * 2009-12-15 2015-07-22 バイエル・クロップサイエンス・アーゲーＢａｙｅｒ Ｃｒｏｐｓｃｉｅｎｃｅ Ａｇ １−アルキル−／１−アリール−５−ピラゾールカルボン酸誘導体を調製する方法
BR112013025792A2 (pt) 2011-04-05 2018-04-24 Pfizer Ltd Inibidores de quinase relacionada à pirrolo[2,3-d] pirimidina tropomisina
DE102013208484B4 (de) 2013-05-08 2018-04-26 Wirtgen Gmbh Vorrichtung zum Bearbeiten von Straßen- oder Bodenoberflächen, sowie Verfahren zum Lenken einer Straßenfräsmaschine
AR117169A1 (es) * 2018-11-28 2021-07-14 Bayer Ag (tio)amidas de piridazina como compuestos fungicidas

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3485840A (en) * 1964-11-12 1969-12-23 Hoffmann La Roche 2,4-diamino - 5 - (2',4',5'-substituted benzyl) pyrimidines,intermediates and processes
US4515948A (en) * 1973-09-12 1985-05-07 Hoffmann-La Roche Inc. 2,4-Diamino-5-(4-amino and 4-dimethylamino-3,5-dimethoxy benzyl)pyrimidines
US4013644A (en) * 1976-03-15 1977-03-22 G. D. Searle & Co. [8 α(E), 13aβ]-5,8,13,13a-tetrahydro-2,3,10,11-tetramethoxy-8-(2-phenylethenyl)-6H-dibenzo[a,g]quinolizines and intermediates thereto
US4444770A (en) * 1980-05-29 1984-04-24 Bayer Aktiengesellschaft New imidazoazole-alkenoic acid amide compounds, intermediate products for their production, their production, and their medicinal use
US4594199A (en) * 1983-09-19 1986-06-10 E. R. Squibb & Sons, Inc. Method for making phosphinic acid intermediates
EP0639075A1 (en) * 1990-11-14 1995-02-22 Chiron Corporation Specific inhibition of dihydrofolate reductase and compounds therefor
MX9703687A (es) * 1994-11-24 1997-08-30 Hoffmann La Roche Nuevas bencil pirimidinas.
EP0832069B1 (en) * 1995-06-07 2003-03-05 Pfizer Inc. BIPHENYL-2-CARBOXYLIC ACID-TETRAHYDRO-ISOQUINOLIN-6-YL AMIDE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND/OR APOLIPOPROTEIN B (Apo B) SECRETION
ES2169272T3 (es) * 1995-12-04 2002-07-01 Arpida Ag Diaminopirimidinas, composiciones farmaceuticas que las contienen y su utilizacion como agente antibacteriano.

Also Published As

Publication number Publication date
JPH11511749A (ja) 1999-10-12
ATE227282T1 (de) 2002-11-15
CA2254117A1 (en) 1997-11-20
AR007088A1 (es) 1999-10-13
PT901488E (pt) 2003-03-31
ES2184089T3 (es) 2003-04-01
WO1997043277A1 (en) 1997-11-20
AU726416B2 (en) 2000-11-09
EP0901488A1 (en) 1999-03-17
MA24182A1 (fr) 1997-12-31
CO4840509A1 (es) 1999-09-27
BR9709251A (pt) 1999-08-10
IL126702A0 (en) 1999-08-17
DE69716901T2 (de) 2003-09-18
DK0901488T3 (da) 2003-03-03
CN1098260C (zh) 2003-01-08
HRP970260A2 (en) 1998-04-30
PL330277A1 (en) 1999-05-10
CZ364698A3 (cs) 1999-02-17
ZA973984B (en) 1997-11-17
NO985335D0 (no) 1998-11-16
EP0901488B1 (en) 2002-11-06
AU2894297A (en) 1997-12-05
KR20000011053A (ko) 2000-02-25
DE69716901D1 (de) 2002-12-12
US5866583A (en) 1999-02-02
CN1218465A (zh) 1999-06-02
NO985335L (no) 1999-01-15
NZ332481A (en) 2000-04-28
YU51498A (en) 1999-11-22
JP3098259B2 (ja) 2000-10-16
KR100295509B1 (ko) 2001-09-17
TW438796B (en) 2001-06-07
TR199802331T2 (xx) 1999-04-21
CA2254117C (en) 2003-03-11
CY2425B1 (en) 2004-11-12

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Legal Events

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FG Grant, registration
FD Application declared void or lapsed