AR039891A1 - Compuestos tiofen-amidinas, sus composiciones farmaceuticas y su uso para la preparacion de medicamentos para tratar enfermedades y trastornos mediados por c1s - Google Patents

Compuestos tiofen-amidinas, sus composiciones farmaceuticas y su uso para la preparacion de medicamentos para tratar enfermedades y trastornos mediados por c1s

Info

Publication number
AR039891A1
AR039891A1 ARP030101873A ARP030101873A AR039891A1 AR 039891 A1 AR039891 A1 AR 039891A1 AR P030101873 A ARP030101873 A AR P030101873A AR P030101873 A ARP030101873 A AR P030101873A AR 039891 A1 AR039891 A1 AR 039891A1
Authority
AR
Argentina
Prior art keywords
alkyl
phenyl
hydrogen
alkenyl
alkoxy
Prior art date
Application number
ARP030101873A
Other languages
English (en)
Original Assignee
Dimensional Pharm 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 Dimensional Pharm Inc filed Critical Dimensional Pharm Inc
Publication of AR039891A1 publication Critical patent/AR039891A1/es

Links

Classifications

    • 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
    • C07D417/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/34—Sulfur atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/08—Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/22—Radicals substituted by doubly bound hetero atoms, or by two hetero atoms other than halogen singly bound to the same carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/38—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
    • 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
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
    • C07F9/655345—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a five-membered ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)

Abstract

Un compuesto tiofen-amidina de fórmula (1): o un solvato, hidrato o sal farmacéuticamente aceptable del mismo; en donde: Z es -S(O)- o -S(O2)-; R1 es alquilo C1-4, halo, amino, alquiltio C1-6, alqueniltio C2-6, alcoxi C1-6, trifluormetilo, metilsulfonilo, o benciltio; Ar es fenilo, naftilo, piridilo, imidazolilo, tiazolilo, furanilo, tienilo, benzotiazolilo, pirazolilo, pirimidinilo, bencimidazolilo, benzofuranilo, indolilo, benzotiofenilo o benzo[c]cromenilo, cualquiera de los cuales está opcionalmente sustituido; R2, R3 y R4 son independientemente hidrógeno, alquilo C1-4, arilo C6-10, hidroxialquilo C1-4, aminoalquilo C1-4, mono alquilamino(C1-4)alquilo(C2-6), di(C1-4)alquilamino(C2-6)alquilo, carboxi(C1-4)alquilo, ciano, amino, nitro, C1-4 alcoxi, o hidroxi o BCO2Rw, donde Rw es hidrógeno, hidroxi, C1-4 alcoxi, ciano, C1-4alcoxicarbonilo, C1-4 alquilo, C3-8 cicloalquilo, fenilo, bencilo, representado por las fórmulas (2) o (3): donde Rd y Re son independientemente hidrógeno, C1-6 alquilo, C2-6 alquenilo o fenilo, Rf es hidrógeno, C1-6 alquilo, C2-6 alquenilo, o fenilo, Rg es hidrógeno, C1-6 alquilo, C2-6 alquenilo o fenilo, y Rh es C6-10 ar(C1-4)alquilo o C1-6 alquilo; y R7 es hidrógeno, cloro, fluoro o amino. Composiciones farmacéuticas que los comprenden, el uso de dichos compuestos para la preparación de un medicamento para tratar los síntomas de un desorden agudo o crónico mediado por la ruta clásica de la cascada del complemento.
ARP030101873A 2002-05-28 2003-05-28 Compuestos tiofen-amidinas, sus composiciones farmaceuticas y su uso para la preparacion de medicamentos para tratar enfermedades y trastornos mediados por c1s AR039891A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US38313002P 2002-05-28 2002-05-28

Publications (1)

Publication Number Publication Date
AR039891A1 true AR039891A1 (es) 2005-03-09

Family

ID=29584510

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030101873A AR039891A1 (es) 2002-05-28 2003-05-28 Compuestos tiofen-amidinas, sus composiciones farmaceuticas y su uso para la preparacion de medicamentos para tratar enfermedades y trastornos mediados por c1s

Country Status (23)

Country Link
US (2) US7138530B2 (es)
EP (1) EP1549632A4 (es)
JP (1) JP2005538953A (es)
KR (1) KR20050009720A (es)
CN (1) CN100412073C (es)
AR (1) AR039891A1 (es)
AU (1) AU2003251384B2 (es)
BR (1) BR0311419A (es)
CA (1) CA2484822A1 (es)
CO (1) CO5640081A2 (es)
HK (1) HK1081187A1 (es)
HR (1) HRP20041220A2 (es)
IL (1) IL164890A0 (es)
MX (1) MX249034B (es)
MY (1) MY137509A (es)
NO (1) NO20045403L (es)
NZ (1) NZ537346A (es)
PL (1) PL372246A1 (es)
RU (1) RU2359967C2 (es)
TW (1) TW200406395A (es)
UA (1) UA80131C2 (es)
WO (1) WO2003099805A1 (es)
ZA (1) ZA200408711B (es)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR0210357A (pt) * 2001-06-11 2004-06-29 Shire Biochem Inc Composto e métodos para o tratamento ou a prevenção de infecções pelo flavivìrus
DE10162114A1 (de) * 2001-12-12 2003-06-26 Schering Ag Neue Amidin-Derivate und deren Verwendung in Arzneimitteln
MY137509A (en) 2002-05-28 2009-02-27 Dimensional Pharm Inc Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
CN100413861C (zh) 2002-12-10 2008-08-27 维勒凯姆制药股份有限公司 用于治疗或预防黄病毒感染的化合物
GB0305575D0 (en) * 2003-03-11 2003-04-16 Glaxo Group Ltd Novel compounds
US7482376B2 (en) * 2003-07-03 2009-01-27 3-Dimensional Pharmaceuticals, Inc. Conjugated complement cascade inhibitors
BRPI0512988A (pt) * 2004-07-08 2008-04-22 Novo Nordisk As método para aumentar a meia-vida plasmática de uma molécula, composto, uso do mesmo, e, composição farmacêutica
CA2584342C (en) * 2004-10-20 2013-04-30 The Regents Of The University Of California Improved inhibitors for the soluble epoxide hydrolase
WO2006122150A1 (en) 2005-05-10 2006-11-16 Incyte Corporation Modulators of indoleamine 2,3-dioxygenase and methods of using the same
EA016071B1 (ru) * 2005-05-13 2012-01-30 Вирокем Фарма Инк. Соединения и способы лечения или предотвращения флавивирусных инфекций
EP1971583B1 (en) * 2005-12-20 2015-03-25 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
MX335993B (es) * 2005-12-30 2016-01-07 Anacor Pharmaceuticals Inc Moleculas pequeñas que contienen boro.
CA2933994A1 (en) 2006-02-16 2007-08-23 Anacor Pharmaceuticals, Inc. Boron-containing small molecules as anti-inflammatory agents
CL2007002650A1 (es) 2006-09-19 2008-02-08 Incyte Corp Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras.
US20080146624A1 (en) * 2006-09-19 2008-06-19 Incyte Corporation Amidines as modulators of indoleamine 2,3-dioxygenase
JP5319532B2 (ja) 2006-09-19 2013-10-16 インサイト・コーポレイション インドールアミン２，３−ジオキシゲナーゼのモジュレーターとしてのｎ−ヒドロキシアミジノヘテロサイクル
AU2007321677B2 (en) * 2006-11-15 2013-04-11 Vertex Pharmaceuticals (Canada) Incorporated Thiophene analogues for the treatment or prevention of flavivirus infections
PL2148691T3 (pl) 2007-02-05 2015-12-31 Apellis Pharmaceuticals Inc Analogi kompstatyny do stosowania w leczeniu stanów zapalnych układu oddechowego
JO3396B1 (ar) * 2007-06-20 2019-10-20 Anacor Pharmaceuticals Inc جزيئات صغيرة تحتوي على البورون
WO2009081970A1 (ja) * 2007-12-26 2009-07-02 Eisai R & D Management Co., Ltd. ヘテロ環置換ピリジン誘導体の製造方法
LT2824100T (lt) 2008-07-08 2018-05-10 Incyte Holdings Corporation 1,2,5-oksadiazolai, kaip indolamino 2,3-dioksigenazės inhibitoriai
WO2011090929A1 (en) 2010-01-19 2011-07-28 Theravance, Inc. Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents
AU2012272706B2 (en) 2011-06-22 2017-07-06 Apellis Pharmaceuticals, Inc. Methods of treating chronic disorders with complement inhibitors
AU2013292519B2 (en) 2012-07-19 2017-12-07 Drexel University Sigma receptor ligands for modulating cellular protein homeostasis
IN2015DN02542A (es) 2012-09-27 2015-09-11 Bayer Cropscience Ag
LT2953942T (lt) 2013-02-06 2018-02-12 Bayer Cropscience Aktiengesellschaft Halogenpakeistieji pirazolo dariniai kaip pesticidai
EP3628661A1 (en) * 2013-06-27 2020-04-01 Lg Chem, Ltd. Biaryl derivatives as gpr120 agonists
AR098343A1 (es) 2013-11-08 2016-05-26 Incyte Holdings Corp Proceso para la síntesis de un inhibidor de indolamina 2,3-dioxigenasa
MD3259253T2 (ro) 2015-02-16 2020-06-30 Univ Queensland Sulfoniluree și compuși înrudiți și utilizări ale acestora
ES2906280T3 (es) 2017-07-07 2022-04-18 Inflazome Ltd Nuevos compuestos de sulfonamida carboxamida
US11370776B2 (en) 2017-07-07 2022-06-28 Inflazome Limited Sulfonylureas and sulfonylthioureas as NLRP3 inhibitors
WO2019034693A1 (en) 2017-08-15 2019-02-21 Inflazome Limited SULFONYLURATES AND SULFONYLTHIOURES AS INHIBITORS OF NLRP3
US20200361895A1 (en) * 2017-08-15 2020-11-19 Inflazome Limited Novel sulfonamide carboxamide compounds
UY37848A (es) 2017-08-15 2019-03-29 Inflazome Ltd Sulfonilureas y sulfoniltioureas útiles como inhibidores de nlrp3
EP3668840A1 (en) 2017-08-15 2020-06-24 Inflazome Limited Novel sulfonamide carboxamide compounds
AU2018317798A1 (en) 2017-08-15 2020-02-13 Inflazome Limited Sulfonylureas and sulfonylthioureas as NLRP
US11117870B2 (en) 2017-11-01 2021-09-14 Drexel University Compounds, compositions, and methods for treating diseases
EP3707134A1 (en) 2017-11-09 2020-09-16 Inflazome Limited Novel sulfonamide carboxamide compounds
WO2019166619A1 (en) 2018-03-02 2019-09-06 Inflazome Limited Novel compounds
WO2021067526A1 (en) 2019-10-02 2021-04-08 Alexion Pharmaceuticals, Inc. Complement inhibitors for treating drug-induced complement-mediated response
WO2021231720A1 (en) 2020-05-15 2021-11-18 Alexion Pharmaceuticals, Inc. Method of using extracellular vesicles to detect complement activation, and uses thereof to assess and/or monitor treatment of a complement-mediated disease
CN115884969A (zh) 2020-09-01 2023-03-31 江苏恒瑞医药股份有限公司 稠合咪唑类衍生物、其制备方法及其在医药上的应用

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59139357A (ja) * 1983-01-28 1984-08-10 Torii Yakuhin Kk アミジン誘導体
US4510130A (en) * 1983-05-20 1985-04-09 Genetic Diagnostics Corporation Promoting animal and plant growth with leupeptin
US4727064A (en) * 1984-04-25 1988-02-23 The United States Of America As Represented By The Department Of Health And Human Services Pharmaceutical preparations containing cyclodextrin derivatives
GB8506792D0 (en) * 1985-03-15 1985-04-17 Janssen Pharmaceutica Nv Derivatives of y-cyclodextrin
US4916219A (en) * 1985-03-28 1990-04-10 University Of Iowa Research Foundation Oligosaccharide heparin fragments as inhibitors of complement cascade
US4722890A (en) * 1985-08-27 1988-02-02 The United States Of America As Represented By The Department Of Health And Human Services Quantitative assay for human terminal complement cascade activation
US5002935A (en) * 1987-12-30 1991-03-26 University Of Florida Improvements in redox systems for brain-targeted drug delivery
US5256642A (en) * 1988-04-01 1993-10-26 The Johns Hopkins University Compositions of soluble complement receptor 1 (CR1) and a thrombolytic agent, and the methods of use thereof
US5268363A (en) * 1989-09-12 1993-12-07 The Beth Israel Hospital Association Method of treatment to inhibit the undesirable activation of the complement cascade with factor J, an inhibitor of complement C1
ZA928276B (en) * 1991-10-31 1993-05-06 Daiichi Seiyaku Co Aromatic amidine derivates and salts thereof.
US5466811A (en) * 1994-07-18 1995-11-14 Merck & Co., Inc. Dioxolenylmethyl carbamates pro moieties for amine drugs
DE19650196A1 (de) * 1996-12-04 1998-06-10 Bayer Ag Thienylsulfonylamino(thio)carbonylverbindungen
WO1998046588A2 (en) * 1997-04-11 1998-10-22 Neorx Corporation Compounds and therapies for the prevention of vascular and non-vascular pathologies
GB9721964D0 (en) 1997-10-16 1997-12-17 Pfizer Ltd Isoquinolines
US6291514B1 (en) 1998-02-09 2001-09-18 3-Dimensional Pharmaceuticals, Inc. Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors
JP2002502852A (ja) * 1998-02-09 2002-01-29 ３−ディメンショナル ファーマシューティカルズ， インコーポレイテッド プロテアーゼ阻害剤、特にウロキナーゼ阻害剤としてのヘテロアリールアミジン、メチルアミジンおよびグアニジン
US6727238B2 (en) * 1998-06-11 2004-04-27 Pfizer Inc. Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
DE19840319A1 (de) 1998-09-04 2000-03-09 Bayer Ag Verfahren zur Herstellung von aromatischen oder heteroaromatischen Sulfonsäurechloriden
FR2783519B1 (fr) * 1998-09-23 2003-01-24 Sod Conseils Rech Applic Nouveaux derives d'amidines, leur preparation, leur application a titre de medicaments et les compositions pharmaceutiques les contenant
JP3450724B2 (ja) * 1998-11-06 2003-09-29 キヤノン株式会社 画像形成装置
EP1152759A2 (en) * 1999-02-09 2001-11-14 3-Dimensional Pharmaceuticals, Inc. METHODS OF TREATING C1s-MEDIATED DISEASES AND CONDITIONS, AND COMPOUNDS AND COMPOSITIONS THEREFOR
EA200100882A1 (ru) * 1999-02-09 2002-04-25 3-Дименшенл Фамэсьютикэлс, Инк. Гетероарильные производные амидина, метиламидина и гуанидина (варианты), способ их получения, фармацевтическая композиция (варианты), способ ингибирования протеазы (варианты) и способ лечения различных заболеваний (варианты)
CA2421548C (en) 2000-09-11 2007-10-30 Genentech, Inc. Amidine inhibitors of serine proteases
DE10112041A1 (de) * 2001-03-14 2002-09-26 Aventis Pharma Gmbh p-Thienylbenzyl-Amide als Agonisten von Angiotensin-(1-7)-Rezeptoren, Verfahren zu ihrer Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate
MY137509A (en) 2002-05-28 2009-02-27 Dimensional Pharm Inc Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
TWI299664B (en) * 2003-01-06 2008-08-11 Osi Pharm Inc (2-carboxamido)(3-amino)thiophene compounds

Also Published As

Publication number Publication date
IL164890A0 (en) 2005-12-18
AU2003251384B2 (en) 2009-01-29
RU2004138787A (ru) 2005-07-10
US7109354B2 (en) 2006-09-19
EP1549632A1 (en) 2005-07-06
NO20045403L (no) 2004-12-10
CA2484822A1 (en) 2003-12-04
MXPA04011671A (es) 2005-03-07
PL372246A1 (en) 2005-07-11
TW200406395A (en) 2004-05-01
NZ537346A (en) 2006-12-22
KR20050009720A (ko) 2005-01-25
ZA200408711B (en) 2006-10-25
HK1081187A1 (en) 2006-05-12
UA80131C2 (en) 2007-08-27
JP2005538953A (ja) 2005-12-22
US20050234081A1 (en) 2005-10-20
MY137509A (en) 2009-02-27
US20040009995A1 (en) 2004-01-15
AU2003251384A1 (en) 2003-12-12
CN1665800A (zh) 2005-09-07
BR0311419A (pt) 2005-04-05
EP1549632A4 (en) 2005-11-09
RU2359967C2 (ru) 2009-06-27
CN100412073C (zh) 2008-08-20
HRP20041220A2 (hr) 2006-04-30
CO5640081A2 (es) 2006-05-31
WO2003099805A1 (en) 2003-12-04
US7138530B2 (en) 2006-11-21
MX249034B (es) 2007-09-14

Similar Documents

Publication Publication Date Title
AR039891A1 (es) Compuestos tiofen-amidinas, sus composiciones farmaceuticas y su uso para la preparacion de medicamentos para tratar enfermedades y trastornos mediados por c1s
JP5406716B2 (ja) インドール化合物
ES2435799T3 (es) Un método de inhibición del virus de la hepatitis C mediante combinación de una 5,6-dihidro-1H-piridin-2-ona y de uno o más compuestos antivirales adicionales
ES2977656T3 (es) Inhibidores de KDM1A para el tratamiento de enfermedades
ES2548228T3 (es) Derivados de bencimidazol e imidazopiridina como moduladores de canal de sodio
ES2884067T3 (es) Derivados de indolina sustituidos como inhibidores de la replicación viral del dengue
BR112021002327A2 (pt) derivados de 6-(4-amino-3-metil-2-oxa-8-azaespiro[4,5]decan-8-il)-3-(2,3-diclorofenil)-2-metilpirimidin-4(3h)-ona e compostos relacionados como inibidores de ptpn11(shp2) para o tratamento do câncer
AR064561A1 (es) Derivados de 2-aza-biciclo[3.1.0]hexano y su uso en la preparacion de un medicamento para el tratamiento de enfermedades relacionadas con disfunciones generales del sistema de la orexina.
NO20045589L (no) Nye forbindelser
UY28132A1 (es) Derivados de pirrolopirimidina
US20070203209A1 (en) Useful indole compounds
CA2963681A1 (en) Induction of gata2 by hdac1 and hdac2 inhibitors
EA200500018A1 (ru) Бензконденсированные гетероариламидные производные тиенопиридинов, применяемые в качестве терапевтических агентов, фармацевтические композиции, включающие их, и способы их применения
BR0206955A (pt) Ligantes de receptores de canabinóides
CY1110977T1 (el) Υποκατεστημενα παραγωγα ινδολης για φαρμακευτικη συνθεση για θεραπεια ασθενειων του αναπνευστικου
RU2007120454A (ru) Производные хинуклидина и их применение в качестве антагонистов мускариновых рецепторов м3
NO20064151L (no) Nye forbindelser
DE60224172D1 (de) Formanilid-derivative als beta2-adrenorezeptor-agonisten
BRPI0513433A (pt) derivados de hidantoìna para o tratamento de distúrbios inflamatórios
EA200600892A1 (ru) Новые хинолиновые производные
ES2920888T3 (es) Derivado de sulfonamida y método de preparación y uso del mismo
CA3018316C (en) Griseofulvin compound
DE60206911D1 (de) Imidazol-2-carbonsäureamid derivate als raf-kinase-inhibitoren
AR056321A1 (es) COMBINACIONES TERAPÉUTICAS PARA EL TRATAMIENTO O LA PREVENCIoN DE TRASTORNOS PSICoTICOS
JP2022003063A (ja) 置換ｎ−アセチル−ｌ−システイン誘導体及び関連化合物

Legal Events

Date Code Title Description
FB Suspension of granting procedure