PE20140592A1 - Proceso para la preparacion de derivados de benzoimidazol-2-il pirimidina - Google Patents

Proceso para la preparacion de derivados de benzoimidazol-2-il pirimidina

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Publication number
PE20140592A1
PE20140592A1 PE2013001866A PE2013001866A PE20140592A1 PE 20140592 A1 PE20140592 A1 PE 20140592A1 PE 2013001866 A PE2013001866 A PE 2013001866A PE 2013001866 A PE2013001866 A PE 2013001866A PE 20140592 A1 PE20140592 A1 PE 20140592A1
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PE
Peru
Prior art keywords
compound
preparation
methyl
refers
benzoimidazole
Prior art date
Application number
PE2013001866A
Other languages
English (en)
Inventor
Neelakandha S Mani
Christopher M Mapes
David C Palmer
Daniel J Pippel
Tong Xiao
Diego Broggini
Susanne Lochner
Sergio Cesco-Cancian
Jeffrey S Grimm
Original Assignee
Janssen Pharmaceutica Nv
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Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41426846&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20140592(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of PE20140592A1 publication Critical patent/PE20140592A1/es

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    • 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
    • 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Cardiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Otolaryngology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A UN HEMITARTRATO CRISTALINO DEL COMPUESTO [5-(4,6-DIMETIL-1H-BENZOIMIDAZOL-2-IL)-4-METIL-PIRIMIDIN-2-IL]-[3-(1-METIL-PIPERIDIN-4-IL)-PROPIL]-AMINA DE FORMULA (I-A) CUYO ESPECTRO DE DIFRACCION DE RAYOS X EN POLVO COMPRENDE LOS SIGUIENTES PICOS EXPRESADOS EN GRADOS 2O: 6.49, 8.58, 9.17, 10.35, 10.75, 16.72, 17.46, 18.89 Y 23.60. TAMBIEN SE REFIERE A UN PROCESO DE PREPARACION DEL HEMITARTRATO CRISTALINO QUE COMPRENDE: A) DISOLVER EL COMPUESTO DE FORMULA (I-A) EN UN SOLVENTE ORGANICO; B) CALENTAR LA SOLUCION A UNA PRIMERA TEMPERATURA DE 50 �C; C) ANADIR ACIDO L-TARTARICO PARA FORMAR UNA SOLUCION DE TARTRATO; Y D) CALENTAR LA SOLUCION DE TARTRATO A UNA SEGUNDA TEMPERATURA DE 70 A 75 �C PARA FORMAR UNA MEZCLA CALIENTE. DICHO COMPUESTO ES MODULADOR DEL RECEPTOR H4 DE HISTAMINA SIENDO UTIL EN EL TRATAMIENTO DE LA INFLAMACION
PE2013001866A 2008-06-30 2009-06-29 Proceso para la preparacion de derivados de benzoimidazol-2-il pirimidina PE20140592A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US7675908P 2008-06-30 2008-06-30

Publications (1)

Publication Number Publication Date
PE20140592A1 true PE20140592A1 (es) 2014-05-16

Family

ID=41426846

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2013001866A PE20140592A1 (es) 2008-06-30 2009-06-29 Proceso para la preparacion de derivados de benzoimidazol-2-il pirimidina

Country Status (27)

Country Link
US (3) US20100029942A1 (es)
EP (2) EP2865678A3 (es)
JP (2) JP2011526911A (es)
KR (1) KR20110022721A (es)
CN (2) CN102137857A (es)
AR (1) AR072397A1 (es)
AU (1) AU2009267159B2 (es)
BR (1) BRPI0913989A2 (es)
CA (1) CA2729703A1 (es)
CL (1) CL2010001639A1 (es)
CO (1) CO6341626A2 (es)
CR (1) CR20110057A (es)
EA (1) EA020090B1 (es)
EC (1) ECSP11010744A (es)
IL (1) IL210213A (es)
MX (1) MX2011000081A (es)
MY (1) MY157197A (es)
NI (1) NI201000233A (es)
NZ (2) NZ590169A (es)
PE (1) PE20140592A1 (es)
SG (1) SG192446A1 (es)
SV (1) SV2011003789A (es)
TW (2) TW201018668A (es)
UA (1) UA102855C2 (es)
UY (1) UY31951A (es)
WO (1) WO2010002777A2 (es)
ZA (1) ZA201100760B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101054325B1 (ko) 2006-03-31 2011-08-04 얀센 파마슈티카 엔.브이. 히스타민 ｈ４ 수용체 조절제로서의 벤조이미다졸―２―일 피리미딘 및 피라진
ME02154B (me) * 2008-06-30 2015-10-20 Janssen Pharmaceutica Nv Proces za pripremu supstituisanih derivata pirimidina
BRPI0913989A2 (pt) 2008-06-30 2015-10-20 Janssen Pharmaceutica Nv processo para preparação de derivados de benzoimidazol-2-il pirirmidina
US9371311B2 (en) 2008-06-30 2016-06-21 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidine derivatives
WO2011133920A1 (en) 2010-04-23 2011-10-27 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
AR081331A1 (es) * 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
AR081626A1 (es) 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
NZ710640A (en) * 2013-03-06 2019-03-29 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidine modulators of the histamine h4 receptor
WO2017076888A1 (en) 2015-11-03 2017-05-11 Janssen Pharmaceutica Nv 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides and methods of making the same

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KR101054325B1 (ko) * 2006-03-31 2011-08-04 얀센 파마슈티카 엔.브이. 히스타민 ｈ４ 수용체 조절제로서의 벤조이미다졸―２―일 피리미딘 및 피라진
BRPI0913989A2 (pt) 2008-06-30 2015-10-20 Janssen Pharmaceutica Nv processo para preparação de derivados de benzoimidazol-2-il pirirmidina

Also Published As

Publication number Publication date
EP2865678A3 (en) 2015-05-27
NZ590169A (en) 2012-05-25
WO2010002777A2 (en) 2010-01-07
SV2011003789A (es) 2011-04-08
CR20110057A (es) 2013-01-25
IL210213A0 (en) 2011-03-31
EP2865678A2 (en) 2015-04-29
WO2010002777A3 (en) 2010-06-24
EA201170114A1 (ru) 2011-08-30
US20120178932A1 (en) 2012-07-12
SG192446A1 (en) 2013-08-30
US8921550B2 (en) 2014-12-30
KR20110022721A (ko) 2011-03-07
UY31951A (es) 2010-01-29
CN103319459A (zh) 2013-09-25
AR072397A1 (es) 2010-08-25
US20120184740A1 (en) 2012-07-19
TWI485147B (zh) 2015-05-21
NZ599747A (en) 2013-03-28
JP2014040426A (ja) 2014-03-06
BRPI0913989A2 (pt) 2015-10-20
TW201422609A (zh) 2014-06-16
CA2729703A1 (en) 2010-01-07
TW201018668A (en) 2010-05-16
EA020090B1 (ru) 2014-08-29
MY157197A (en) 2016-05-13
NI201000233A (es) 2011-11-09
AU2009267159B2 (en) 2014-05-15
US20100029942A1 (en) 2010-02-04
JP2011526911A (ja) 2011-10-20
CL2010001639A1 (es) 2011-06-24
AU2009267159A1 (en) 2010-01-07
UA102855C2 (ru) 2013-08-27
CN102137857A (zh) 2011-07-27
US8835633B2 (en) 2014-09-16
CO6341626A2 (es) 2011-11-21
ECSP11010744A (es) 2011-02-28
EP2303869A2 (en) 2011-04-06
ZA201100760B (en) 2012-07-25
MX2011000081A (es) 2011-03-02
IL210213A (en) 2015-08-31

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