EA018198B1 - Диаминопиридиновые, пиримидиновые и пиридазиновые модуляторы гистаминового рецептора h - Google Patents

Диаминопиридиновые, пиримидиновые и пиридазиновые модуляторы гистаминового рецептора h Download PDF

Info

Publication number
EA018198B1
EA018198B1 EA201170005A EA201170005A EA018198B1 EA 018198 B1 EA018198 B1 EA 018198B1 EA 201170005 A EA201170005 A EA 201170005A EA 201170005 A EA201170005 A EA 201170005A EA 018198 B1 EA018198 B1 EA 018198B1
Authority
EA
Eurasian Patent Office
Prior art keywords
amine
methylamino
pyrimidin
pyridin
pyrrolidin
Prior art date
Application number
EA201170005A
Other languages
English (en)
Russian (ru)
Other versions
EA201170005A1 (ru
Inventor
Хой Цай
Франк Чавез
Пол Дж. Данфорд
Эндрю Дж. Гринспан
Стивен П. Медуна
Джордж А. Куироз
Брэд М. Савалль
Кевин Л. Тайс
Робин Л. Турмонд
Дзяньмэй Вэй
Рональд Л. Волин
Сяоху Чжан
Original Assignee
Янссен Фармацевтика Нв
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41417123&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA018198(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Янссен Фармацевтика Нв filed Critical Янссен Фармацевтика Нв
Publication of EA201170005A1 publication Critical patent/EA201170005A1/ru
Publication of EA018198B1 publication Critical patent/EA018198B1/ru

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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P13/12—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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • A61P25/04—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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • 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
    • 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
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • 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
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three 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
    • C07D237/20—Nitrogen 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
    • C07D401/04—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
    • C07D401/14—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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
EA201170005A 2008-06-12 2009-06-11 Диаминопиридиновые, пиримидиновые и пиридазиновые модуляторы гистаминового рецептора h EA018198B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US6103908P 2008-06-12 2008-06-12
US11441608P 2008-11-13 2008-11-13
US11442508P 2008-11-13 2008-11-13
PCT/US2009/047033 WO2009152325A1 (en) 2008-06-12 2009-06-11 Diamino-pyridine, pyrimidine, and pyridazine modulators of the histamine h4 receptor

Publications (2)

Publication Number Publication Date
EA201170005A1 EA201170005A1 (ru) 2011-08-30
EA018198B1 true EA018198B1 (ru) 2013-06-28

Family

ID=41417123

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201170005A EA018198B1 (ru) 2008-06-12 2009-06-11 Диаминопиридиновые, пиримидиновые и пиридазиновые модуляторы гистаминового рецептора h

Country Status (20)

Country Link
US (3) US8841287B2 (enExample)
EP (1) EP2315521B1 (enExample)
JP (1) JP5658662B2 (enExample)
KR (1) KR101600278B1 (enExample)
CN (1) CN102118969B (enExample)
AU (1) AU2009257434B2 (enExample)
BR (1) BRPI0915720A2 (enExample)
CA (1) CA2727684C (enExample)
CO (1) CO6321192A2 (enExample)
CR (1) CR20110029A (enExample)
EA (1) EA018198B1 (enExample)
EC (1) ECSP10010675A (enExample)
IL (1) IL209593A (enExample)
MX (1) MX2010013726A (enExample)
MY (1) MY158927A (enExample)
NI (1) NI201000214A (enExample)
NZ (1) NZ589532A (enExample)
PE (1) PE20110061A1 (enExample)
WO (1) WO2009152325A1 (enExample)
ZA (1) ZA201100298B (enExample)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS51423B (sr) 2006-03-31 2011-02-28 Janssen Pharmaceutica N.V. Benzoimidazol-2-il pirimidini i pirazini kao modulatori histaminskog h4 receptora
PE20110061A1 (es) 2008-06-12 2011-01-31 Janssen Pharmaceutica Nv Derivados de diamino-piridina, pirimidina y piridazina como moduladores del receptor h4 de histamina
AU2009257486B2 (en) * 2008-06-12 2015-01-22 Janssen Pharmaceutica Nv Use of histamine H4 antagonist for the treatment of post-operative adhesions
US9371311B2 (en) 2008-06-30 2016-06-21 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidine derivatives
BRPI1011058A2 (pt) * 2009-05-19 2015-08-25 Dow Agrosciences Llc Compostos e metodos controlar fungos
WO2011078143A1 (ja) * 2009-12-22 2011-06-30 塩野義製薬株式会社 ピリミジン誘導体およびそれらを含有する医薬組成物
BR112014028006A2 (pt) * 2012-05-30 2017-06-27 Hoffmann La Roche heterociclos de pirrolidino
JO3516B1 (ar) 2013-03-06 2020-07-05 Janssen Pharmaceutica Nv مُعدِّلات بنزإيميدازول-2-يل بيريميدين لمستقبل الهستامين h4
WO2014147586A1 (en) * 2013-03-22 2014-09-25 Novartis Ag 1-(2-(ethylamino)pyrimidin-4-yl)pyrrolidin-2-ones as inhibitors of mutant idh
CN104903312B (zh) * 2013-10-07 2019-01-29 卡德门企业有限公司 Rho激酶抑制剂
PL3174858T3 (pl) 2014-07-31 2019-10-31 Basf Se Sposób wytwarzania pirazoli
PE20180327A1 (es) 2015-05-11 2018-02-13 Basf Se Proceso para preparar 4-amino-piridazinas
US20190216790A1 (en) * 2016-10-13 2019-07-18 The Regents Of The University Of California Methods for Treating Pruritis
WO2018082964A1 (en) 2016-11-04 2018-05-11 Basf Se Process for the production of pyridazinyl-amides in a one-pot synthesis
JP2022165429A (ja) * 2019-10-02 2022-11-01 Ｍｅｉｊｉ Ｓｅｉｋａファルマ株式会社 ヒスタミンｈ４受容体調節作用を有する新規トリアジン誘導体
CN117642395A (zh) * 2021-07-01 2024-03-01 爱瑞制药公司 氮杂环丁烷基嘧啶及其用途
CN116354937B (zh) * 2021-12-27 2025-07-11 江苏恩华药业股份有限公司 吡啶(嘧啶)胺类衍生物及其应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003076430A1 (en) * 2002-03-13 2003-09-18 Janssen Pharmaceutica N.V. Amino-derivatives as novel inhibitors of histone deacetylase
WO2003076438A1 (en) * 2002-03-13 2003-09-18 Janssen Pharmaceutica N.V. Piperazinyl-, piperidinyl- and morpholinyl-derivatives as novel inhibitors of histone deacetylase
WO2007082878A1 (en) * 2006-01-19 2007-07-26 Janssen Pharmaceutica N.V. Aminophenyl derivatives as novel inhibitors of histone deacetylase

Family Cites Families (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE759371A (fr) 1969-11-24 1971-05-24 Bristol Myers Co Azaspirodecanediones heterocycliques et procedes pour leur preparation
GB8609630D0 (en) 1986-04-19 1986-05-21 Pfizer Ltd Anti-arrhythmia agents
HU206337B (en) 1988-12-29 1992-10-28 Mitsui Petrochemical Ind Process for producing pyrimidine derivatives and pharmaceutical compositions
CA2071529C (en) 1989-12-28 2001-03-20 Donna Lee Romero Diaromatic substituted anti-aids compounds
WO1992019602A1 (de) * 1991-04-26 1992-11-12 Byk Gulden Lomberg Chemische Fabrik Gmbh Neue pyridazine
CA2346659A1 (en) * 1998-10-06 2000-04-13 Michiyo Gyoten Condensed pyridazine compounds, their production and use
JP2003519143A (ja) 1999-12-28 2003-06-17 ファーマコピーア，インコーポレーティッド ピリミジン及びトリアジン系キナーゼ阻害剤
WO2002022605A1 (en) 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
SE0004245D0 (sv) 2000-11-20 2000-11-20 Pharmacia Ab Novel compounds and their use
JP4544820B2 (ja) 2001-03-09 2010-09-15 オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド 複素環化合物
US6825198B2 (en) 2001-06-21 2004-11-30 Pfizer Inc 5-HT receptor ligands and uses thereof
MXPA04004178A (es) * 2001-11-01 2004-09-06 Janssen Pharmaceutica Nv Heteroarilaminas como inhibidores de glucogeno cintasa cinasa 3beta.
EP1485378B1 (en) 2002-03-13 2008-06-18 Janssen Pharmaceutica N.V. Piperazinyl-, piperidinyl- and morpholinyl-derivatives as novel inhibitors of histone deacetylase
WO2004052862A1 (ja) 2002-12-10 2004-06-24 Ono Pharmaceutical Co., Ltd. 含窒素複素環化合物およびその医薬用途
EP1437348A1 (fr) 2003-01-13 2004-07-14 L'oreal Dérivés de de la 6-méthyl-pyrimidine-2,4-diamine, procédé de synthèse, compositions les comprenant et utilisations comme agents neutralisants basiques
EP1505064A1 (en) 2003-08-05 2005-02-09 Bayer HealthCare AG 2-Aminopyrimidine derivatives
WO2005054239A1 (en) * 2003-12-05 2005-06-16 Bayer Healthcare Ag 2-aminopyrimidine derivatives
CA2556239A1 (en) * 2004-02-11 2005-08-25 Amgen Inc. Vanilloid receptor ligands and their use in treatments
AU2005303893A1 (en) 2004-11-11 2006-05-18 Argenta Discovery Ltd Pyrimidine compounds as histamine modulators
DE602005010744D1 (de) 2004-12-16 2008-12-11 Hoffmann La Roche Piperazinylpyridinderivate als mittel gegen adipositas
RU2008114378A (ru) * 2005-09-13 2009-10-20 Палау Фарма, С.А. (Es) Производные 2-аминопиримидина как модуляторы активности н4-рецептора гистамина
EP1767537A1 (en) 2005-09-21 2007-03-28 Cellzome (UK) Ltd. Pyrimidine compounds for the treatment of inflammatory disorders
NL2000323C2 (nl) * 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine-derivaten.
WO2007090853A1 (en) 2006-02-10 2007-08-16 Cellzome (Uk) Ltd. Enantiomers of amino pyrimidine compounds for the treatment of inflammatory disorders
WO2007090854A1 (en) 2006-02-10 2007-08-16 Cellzome (Uk) Ltd. Azetidine amino pyrimidine compounds for the treatment of inflammatory disorders
EP1829879A1 (en) 2006-02-10 2007-09-05 Cellzome (UK) Ltd. Amino pyrimidine compounds for the treatment of inflammatory disorders
RS51423B (sr) 2006-03-31 2011-02-28 Janssen Pharmaceutica N.V. Benzoimidazol-2-il pirimidini i pirazini kao modulatori histaminskog h4 receptora
GB0610909D0 (en) * 2006-06-05 2006-07-12 Merck Sharp & Dohme Therapeutic treatment
US20100035863A1 (en) * 2006-09-12 2010-02-11 Ucb Pharma, S.A. 2 Amino-Pyrimidine Derivatives As H4 Receptor Antagonists, Processes For Preparing Them And Their Use In Pharmaceutical Compositions
EP1920654A1 (en) 2006-09-13 2008-05-14 Syngeta Participations AG Novel pyridopyrazine N-oxides
US7985745B2 (en) 2006-10-02 2011-07-26 Abbott Laboratories Method for pain treatment
WO2008074445A1 (en) 2006-12-18 2008-06-26 Ucb Pharma, S.A. Novel tricyclic and heterotricyclic derivatives, processes for preparing them, pharmaceutical compositions thereof
TW200904437A (en) 2007-02-14 2009-02-01 Janssen Pharmaceutica Nv 2-aminopyrimidine modulators of the histamine H4 receptor
US20100168077A1 (en) 2007-04-04 2010-07-01 Ucb Pharma, S.A. Novel Pyridine Derivatives, Processes for Preparing Them, Pharmaceutical Compositions Thereof
WO2009068512A1 (en) 2007-11-30 2009-06-04 Palau Pharma, S. A. 2 -amino-pyrimidine derivatives as histamine h4 antagonists
PE20110061A1 (es) 2008-06-12 2011-01-31 Janssen Pharmaceutica Nv Derivados de diamino-piridina, pirimidina y piridazina como moduladores del receptor h4 de histamina
AR072084A1 (es) 2008-06-12 2010-08-04 Sanofi Aventis Derivados de azacarbolinas, su preparacion y su utilizacion terapeutica como inhibidores de las quinasas pim
JO2870B1 (en) 2008-11-13 2015-03-15 ميرك شارب اند دوهم كورب Amino Tetra Hydro Pirans as Inhibitors of Peptide Dipeptide IV for the Treatment or Prevention of Diabetes
PL2356123T3 (pl) 2008-11-13 2013-03-29 Hoffmann La Roche Spiro-5,6-dihudro-4h-2,3,5,10b- tetraazabenzo[e]azuleny

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003076430A1 (en) * 2002-03-13 2003-09-18 Janssen Pharmaceutica N.V. Amino-derivatives as novel inhibitors of histone deacetylase
WO2003076438A1 (en) * 2002-03-13 2003-09-18 Janssen Pharmaceutica N.V. Piperazinyl-, piperidinyl- and morpholinyl-derivatives as novel inhibitors of histone deacetylase
WO2007082878A1 (en) * 2006-01-19 2007-07-26 Janssen Pharmaceutica N.V. Aminophenyl derivatives as novel inhibitors of histone deacetylase

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SHIN et al. Molecular Modeling and Site-Specific Mutagenesis of the Histamine-Binding Site of the Histamine H4 Receptor. Molecular Pharmacology, 2002, Vol 62(1), pp 38-47, Abstract; pg 42-pg 46; Fig. 2 *

Also Published As

Publication number Publication date
MX2010013726A (es) 2011-01-14
CA2727684A1 (en) 2009-12-17
HK1157569A1 (en) 2012-07-06
NZ589532A (en) 2012-02-24
IL209593A (en) 2015-02-26
ECSP10010675A (es) 2011-01-31
JP5658662B2 (ja) 2015-01-28
CN102118969A (zh) 2011-07-06
EP2315521A4 (en) 2012-04-25
IL209593A0 (en) 2011-01-31
CR20110029A (es) 2011-07-06
US20170298022A1 (en) 2017-10-19
EA201170005A1 (ru) 2011-08-30
JP2011524363A (ja) 2011-09-01
PE20110061A1 (es) 2011-01-31
CA2727684C (en) 2017-01-31
EP2315521B1 (en) 2014-05-21
KR20110017441A (ko) 2011-02-21
AU2009257434B2 (en) 2014-12-11
NI201000214A (es) 2011-08-01
ZA201100298B (en) 2012-06-27
CN102118969B (zh) 2017-03-08
WO2009152325A1 (en) 2009-12-17
US9732087B2 (en) 2017-08-15
KR101600278B1 (ko) 2016-03-08
AU2009257434A1 (en) 2009-12-17
US20140357614A1 (en) 2014-12-04
US8841287B2 (en) 2014-09-23
CO6321192A2 (es) 2011-09-20
BRPI0915720A2 (pt) 2015-08-04
EP2315521A1 (en) 2011-05-04
US20110092474A1 (en) 2011-04-21
MY158927A (en) 2016-11-30

Similar Documents

Publication Publication Date Title
EA018198B1 (ru) Диаминопиридиновые, пиримидиновые и пиридазиновые модуляторы гистаминового рецептора h
KR102329162B1 (ko) 카이네이즈 저해제로서의 피라졸로피리미딘 유도체
JP7514025B2 (ja) Ｊａｋ阻害剤化合物及びその使用
US20240208947A1 (en) Jak1 selective inhibitors
JP5281586B2 (ja) ヒスタミンｈ４受容体の２−アミノピリミジン系モジュレーター
KR20160144378A (ko) 브루톤 티로신 키나제 억제제로서 작용하는 폴리플루오로화 화합물
IL259862A (en) Inhibitors of bruton's tyrosine kinase and methods of their use
JP2024527623A (ja) 癌の治療のためのｈｐｋ１阻害剤としての置換ピラジン－２－カルボキサミド阻害剤
HK1157569B (en) Diamino-pyridine, pyrimidine, and pyridazine modulators of the histamine h 4 receptor
HK40053464A (en) Pyrazolopyrimidine derivatives as kinase inhibitor
WO2021066088A1 (ja) 新規トリアジン誘導体
HK1260670A1 (en) Pyrazolopyrimidine derivatives as kinase inhibitor

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM