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ES2105920A1 - Procedimiento para preparar compuestos de benzo-y piridopiridazinona y piridazinationa. - Google Patents

Procedimiento para preparar compuestos de benzo-y piridopiridazinona y piridazinationa.

Info

Publication number
ES2105920A1
ES2105920A1 ES09201998A ES9201998A ES2105920A1 ES 2105920 A1 ES2105920 A1 ES 2105920A1 ES 09201998 A ES09201998 A ES 09201998A ES 9201998 A ES9201998 A ES 9201998A ES 2105920 A1 ES2105920 A1 ES 2105920A1
Authority
ES
Spain
Prior art keywords
benzo
pde
inhibiting activity
hydrogen
carbon
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
ES09201998A
Other languages
English (en)
Other versions
ES2105920B1 (es
Inventor
Robert S Wilhelm
Bradley E Loe
Bruce H Devens
Robert Alvarez
Michael Martin
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Syntex USA LLC
Original Assignee
Syntex USA LLC
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 Syntex USA LLC filed Critical Syntex USA LLC
Publication of ES2105920A1 publication Critical patent/ES2105920A1/es
Application granted granted Critical
Publication of ES2105920B1 publication Critical patent/ES2105920B1/es
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/76—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • C07D213/80—Acids; Esters in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30—Phthalazines
    • C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

PROCEDIMIENTO PARA PREPARAR COMPUESTOS DE BENZO- Y PIRIDOPIRIDAZINONA Y PIRIDAZINATIONA. BENZO- O PIRIDO-PIRIDAZINONAS Y PIRIDAZINATIONAS DE FORMULA FORMULA EN LA QUE: X E Y SON NITROGENO O CARBONO, CON LA CONDICION DE QUE POR LO MENOS UNO SEA CARBONO, Y Z ES OXIGENO O AZUFRE; R1 ES HIDROGENO, ALQUILO INFERIOR, ARILO, HETEROARILO, O HETEROCICLOALQUILENO INFERIOR; R2, R3, R4, R5 Y R6 SE SELECCIONAN INDEPENDIENTEMENTE DE HIDROGENO, ALQUILO INFERIOR, HALO, CARBOXI, ALCOXI-CARBONILO, CARBAMOILO, ACILO, HALOGENURO DE ACILO, TIO-METILO, TRI-FLUORO-METILO, CIENO O NITRO; O UN ESTER, UN ETER O UNA SAL FARMACEUTICAMENTE ACEPTABLE DEL MISMO, SE HAN HALLADO UTILES COMO AGENTES ANTI-INFLAMATORIOS, ANTIASMATICOS, INMUNOSUPRESORES, ANTI-RECHAZO DE ALOINJERTO, ANTI-RECHAZO DE INJERTO FRENTE A HOSPEDANTE, ENFERMEDAD AUTOINMUNE O ANALGESICOS.
ES09201998A 1991-10-09 1992-10-08 Procedimiento para preparar compuestos de benzo-y piridopiridazinona y piridazinationa. Expired - Fee Related ES2105920B1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US77567991A 1991-10-09 1991-10-09

Publications (2)

Publication Number Publication Date
ES2105920A1 true ES2105920A1 (es) 1997-10-16
ES2105920B1 ES2105920B1 (es) 1998-07-01

Family

ID=25105161

Family Applications (2)

Application Number Title Priority Date Filing Date
ES92922090T Expired - Lifetime ES2135416T3 (es) 1991-10-09 1992-10-08 Compuestos de piridopiridazinonas y piridazintionas con actividad inhibidora de la pde iv.
ES09201998A Expired - Fee Related ES2105920B1 (es) 1991-10-09 1992-10-08 Procedimiento para preparar compuestos de benzo-y piridopiridazinona y piridazinationa.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES92922090T Expired - Lifetime ES2135416T3 (es) 1991-10-09 1992-10-08 Compuestos de piridopiridazinonas y piridazintionas con actividad inhibidora de la pde iv.

Country Status (20)

Country Link
EP (1) EP0612321B1 (es)
JP (1) JP3245165B2 (es)
KR (1) KR100263494B1 (es)
AT (1) ATE183745T1 (es)
AU (1) AU670544B2 (es)
CA (1) CA2117059C (es)
DE (1) DE69229874T2 (es)
DK (1) DK0612321T3 (es)
ES (2) ES2135416T3 (es)
FI (1) FI108229B (es)
GR (1) GR3030969T3 (es)
HU (2) HUT66969A (es)
IL (1) IL103388A (es)
MX (1) MX9205794A (es)
NO (1) NO302888B1 (es)
NZ (1) NZ244660A (es)
PT (1) PT100938B (es)
TW (1) TW365606B (es)
WO (1) WO1993007146A1 (es)
ZA (1) ZA927755B (es)

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US5665754A (en) * 1993-09-20 1997-09-09 Glaxo Wellcome Inc. Substituted pyrrolidines
US5466697A (en) * 1994-07-13 1995-11-14 Syntex (U.S.A.) Inc. 8-phenyl-1,6-naphthyridin-5-ones
AU3265695A (en) * 1994-08-29 1996-03-22 Yamanouchi Pharmaceutical Co., Ltd. Novel naphthyridine derivative and medicinal composition thereof
US6069151A (en) * 1996-11-06 2000-05-30 Darwin Discovery, Ltd. Quinolines and their therapeutic use
GB9712761D0 (en) * 1997-06-17 1997-08-20 Chiroscience Ltd Quinolines and their therapeutic use
ES2137113B1 (es) * 1997-07-29 2000-09-16 Almirall Prodesfarma Sa Nuevos derivados de triazolo-piridazinas heterociclicos.
CA2314111A1 (en) * 1997-12-15 1999-06-24 Byk Gulden Lomberg Chemische Fabrik Gmbh Dihydrobenzofurans
EP0934933A1 (en) * 1998-02-06 1999-08-11 Byk Gulden Lomberg Chemische Fabrik GmbH Phthalazinones
IT1303272B1 (it) * 1998-10-29 2000-11-06 Zambon Spa Derivati triciclici inibitori della fosfodiesterasi 4
JP3270834B2 (ja) 1999-01-27 2002-04-02 ファイザー・プロダクツ・インク 抗がん剤として有用なヘテロ芳香族二環式誘導体
UA71945C2 (en) 1999-01-27 2005-01-17 Pfizer Prod Inc Substituted bicyclic derivatives being used as anticancer agents
ATE447952T1 (de) 1999-08-21 2009-11-15 Nycomed Gmbh Synergistische kombination von pumafentrine und salmeterol
IL156812A0 (en) * 2001-02-15 2004-02-08 Altana Pharma Ag Phthalazinone-piperidino derivatives and pharmaceutical compositions containing the same
HUP0303469A3 (en) 2001-04-25 2004-04-28 Altana Pharma Ag Phtalazinon-derivatives, their use and pharmaceutical compositions containing them
NZ529221A (en) * 2001-04-25 2005-04-29 Altana Pharma Ag Phthalazinones with PDE-inhibiting properties for treatment of airway disorders and other inflammatory conditions
ES2195785B1 (es) 2002-05-16 2005-03-16 Almirall Prodesfarma, S.A. Nuevos derivados de piridazin-3(2h)-ona.
AU2003260371A1 (en) * 2002-08-10 2004-03-11 Altana Pharma Ag Piperidine-n-oxide-derivatives
PL372926A1 (en) 2002-08-10 2005-08-08 Altana Pharma Ag Piperidine-pyridazones and phthalazones as pde4 inhibitors
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US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
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WO2008151257A2 (en) 2007-06-04 2008-12-11 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
PL383550A1 (pl) * 2007-10-15 2009-04-27 Uniwersytet Łódzki Nowe pochodne benzeno- i pirydopirydazynonów
EP3239170B1 (en) 2008-06-04 2019-03-20 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
CA2730603C (en) 2008-07-16 2019-09-24 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
MX357121B (es) 2011-03-01 2018-06-27 Synergy Pharmaceuticals Inc Star Proceso de preparacion de agonistas c de guanilato ciclasa.
US20130116241A1 (en) * 2011-11-09 2013-05-09 Abbvie Inc. Novel inhibitor compounds of phosphodiesterase type 10a
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
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WO1991012251A1 (en) * 1990-02-19 1991-08-22 Chugai Seiyaku Kabushiki Kaisha Novel fused heterocyclic compound and antiasthmatic agent prepared therefrom

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CSAMPAI et al. Bromoalkylphthalazinones..., Tetrahedron Vol. 45, n‘ 17, pßginas 5539-5548, 1989 *
EPSZTAJN et al. Application of organolithium and related reagents in synthesis, Vol. 121, pßginas 909-921, 1990 *
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Also Published As

Publication number Publication date
DE69229874T2 (de) 1999-12-09
AU2781592A (en) 1993-05-03
MX9205794A (es) 1993-04-01
NO302888B1 (no) 1998-05-04
IL103388A (en) 1997-09-30
GR3030969T3 (en) 1999-11-30
EP0612321A1 (en) 1994-08-31
HUT66969A (en) 1995-01-30
ZA927755B (en) 1994-04-08
HU9400949D0 (en) 1994-06-28
NO941210D0 (no) 1994-04-05
JPH07500321A (ja) 1995-01-12
DK0612321T3 (da) 1999-12-13
PT100938A (pt) 1993-10-29
NO941210L (no) 1994-04-05
ES2135416T3 (es) 1999-11-01
FI108229B (fi) 2001-12-14
IL103388A0 (en) 1993-03-15
CA2117059C (en) 2003-05-20
KR940702868A (ko) 1994-09-17
FI941567A0 (fi) 1994-04-06
DE69229874D1 (de) 1999-09-30
WO1993007146A1 (en) 1993-04-15
JP3245165B2 (ja) 2002-01-07
AU670544B2 (en) 1996-07-25
KR100263494B1 (ko) 2000-08-01
NZ244660A (en) 1995-05-26
PT100938B (pt) 1999-10-29
CA2117059A1 (en) 1993-04-15
EP0612321B1 (en) 1999-08-25
HU210814A9 (en) 1995-08-28
ES2105920B1 (es) 1998-07-01
ATE183745T1 (de) 1999-09-15
FI941567A (fi) 1994-04-06
TW365606B (en) 1999-08-01

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