EA201300436A1 - Совместные кристаллы и соли ингибиторов ccr3 - Google Patents

Совместные кристаллы и соли ингибиторов ccr3

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Publication number
EA201300436A1
EA201300436A1 EA201300436A EA201300436A EA201300436A1 EA 201300436 A1 EA201300436 A1 EA 201300436A1 EA 201300436 A EA201300436 A EA 201300436A EA 201300436 A EA201300436 A EA 201300436A EA 201300436 A1 EA201300436 A1 EA 201300436A1
Authority
EA
Eurasian Patent Office
Prior art keywords
salts
ccr3 inhibitors
crystals
ccr3
joint crystals
Prior art date
Application number
EA201300436A
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English (en)
Other versions
EA201300436A8 (ru
EA029097B1 (ru
Inventor
Маркус Франк
Ханс Хеберле
Манюэль Анри
Томас Пахур
Марко Сантагостино
Уве Штертц
Томас Требинг
Ульрике Вертманн
Original Assignee
Бёрингер Ингельхайм Интернациональ Гмбх
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.)
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Publication date
Application filed by Бёрингер Ингельхайм Интернациональ Гмбх filed Critical Бёрингер Ингельхайм Интернациональ Гмбх
Publication of EA201300436A1 publication Critical patent/EA201300436A1/ru
Publication of EA201300436A8 publication Critical patent/EA201300436A8/ru
Publication of EA029097B1 publication Critical patent/EA029097B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Virology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

В заявке описаны совместные кристаллы и соли ингибиторов CCR3 формулы (1)содержащие их фармацевтические композиции и способы их применения в качестве средств, предназначенных для лечения и/или предупреждения заболеваний, связанных с рецептором CCR3.
EA201300436A 2010-10-07 2011-10-06 Совместные кристаллы и соли ингибиторов ccr3 EA029097B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10186901 2010-10-07
PCT/EP2011/067437 WO2012045803A1 (en) 2010-10-07 2011-10-06 Co-crystals and salts of ccr3-inhibitors

Publications (3)

Publication Number Publication Date
EA201300436A1 true EA201300436A1 (ru) 2013-08-30
EA201300436A8 EA201300436A8 (ru) 2018-01-31
EA029097B1 EA029097B1 (ru) 2018-02-28

Family

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EA201300436A EA029097B1 (ru) 2010-10-07 2011-10-06 Совместные кристаллы и соли ингибиторов ccr3

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US (3) US8742115B2 (ru)
EP (1) EP2625174B1 (ru)
JP (1) JP5794713B2 (ru)
KR (3) KR101844215B1 (ru)
CN (1) CN103140486B (ru)
AP (1) AP3268A (ru)
AR (1) AR083353A1 (ru)
AU (1) AU2011311530B2 (ru)
BR (2) BR122021010665B1 (ru)
CA (1) CA2807255C (ru)
CL (1) CL2013000488A1 (ru)
CO (1) CO6710910A2 (ru)
CY (1) CY1116168T1 (ru)
DK (1) DK2625174T3 (ru)
EA (1) EA029097B1 (ru)
EC (1) ECSP13012600A (ru)
ES (1) ES2535264T3 (ru)
GE (1) GEP20166488B (ru)
HR (1) HRP20150419T1 (ru)
HU (1) HUE024540T2 (ru)
IL (1) IL224269A (ru)
MA (1) MA34545B1 (ru)
ME (1) ME02040B (ru)
MX (1) MX2013003785A (ru)
MY (1) MY167898A (ru)
NZ (1) NZ605827A (ru)
PE (1) PE20140188A1 (ru)
PL (1) PL2625174T3 (ru)
PT (1) PT2625174E (ru)
RS (1) RS53858B1 (ru)
SG (1) SG188949A1 (ru)
SI (1) SI2625174T1 (ru)
TW (1) TWI546294B (ru)
UA (1) UA109290C2 (ru)
UY (1) UY33655A (ru)
WO (1) WO2012045803A1 (ru)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8278302B2 (en) 2009-04-08 2012-10-02 Boehringer Ingelheim International Gmbh Substituted piperidines as CCR3 antagonists
UA109290C2 (uk) 2010-10-07 2015-08-10 Спільні кристали і солі інгібіторів ccr3
US8680280B2 (en) * 2012-04-02 2014-03-25 Boehringer Ingelheim International Gmbh Process for the manufacturing of CRR inhibitors
US20130261153A1 (en) * 2012-04-03 2013-10-03 Boehringer Ingelheim International Gmbh Use of ccr3-inhibitors
US10213421B2 (en) 2012-04-04 2019-02-26 Alkahest, Inc. Pharmaceutical formulations comprising CCR3 antagonists
AU2018248425B2 (en) 2017-04-05 2024-03-28 Alkahest Inc. Methods and compositions for treating retina-associated disease using CCR3-inhibitors
US20200054622A1 (en) * 2017-04-05 2020-02-20 Alkahest, Inc. Methods and Compositions for Treating Aging-Associated Impairments Using CCR3-Inhibitors
BR112019020798A2 (pt) * 2017-04-05 2020-04-28 Alkahest Inc métodos e composições para tratamento de danos associados ao envelhecimento usando inibidores de ccr3
JP2020536929A (ja) * 2017-10-13 2020-12-17 アルカヘスト,インコーポレイテッド Ccr3阻害剤を用いた、そう痒症、乾皮症、及び関連疾患を治療するための方法及び組成物
WO2019222265A1 (en) 2018-05-15 2019-11-21 Alkahest, Inc. Treatment of aging-associated disease with modulators of leukotriene a4 hydrolase
BR112021004938A2 (pt) * 2018-09-26 2021-06-01 Alkahest, Inc. métodos e composições para tratamento de danos associados com o envelhecimento usando inibidores de ccr3
AU2021287906A1 (en) * 2020-06-11 2022-12-15 Alkahest Inc. Methods of improving retina-associated disease outcome using CCR3-inhibitors
US11957671B2 (en) 2021-11-01 2024-04-16 Alkahest, Inc. Benzodioxane modulators of leukotriene A4 hydrolase (LTA4H) for prevention and treatment of aging-associated diseases

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US8278302B2 (en) 2009-04-08 2012-10-02 Boehringer Ingelheim International Gmbh Substituted piperidines as CCR3 antagonists
UA109290C2 (uk) 2010-10-07 2015-08-10 Спільні кристали і солі інгібіторів ccr3
US8680280B2 (en) 2012-04-02 2014-03-25 Boehringer Ingelheim International Gmbh Process for the manufacturing of CRR inhibitors
US20130261153A1 (en) 2012-04-03 2013-10-03 Boehringer Ingelheim International Gmbh Use of ccr3-inhibitors
US10213421B2 (en) 2012-04-04 2019-02-26 Alkahest, Inc. Pharmaceutical formulations comprising CCR3 antagonists

Also Published As

Publication number Publication date
DK2625174T3 (da) 2015-02-02
CA2807255A1 (en) 2012-04-12
PE20140188A1 (es) 2014-02-26
CN103140486B (zh) 2016-08-03
KR20130118313A (ko) 2013-10-29
US20120264729A1 (en) 2012-10-18
EA201300436A8 (ru) 2018-01-31
SG188949A1 (en) 2013-05-31
ES2535264T3 (es) 2015-05-07
CN103140486A (zh) 2013-06-05
EA029097B1 (ru) 2018-02-28
AU2011311530A1 (en) 2013-01-31
EP2625174A1 (en) 2013-08-14
BR112013008211A2 (pt) 2016-06-21
AR083353A1 (es) 2013-02-21
JP2013542207A (ja) 2013-11-21
CL2013000488A1 (es) 2013-07-05
ME02040B (me) 2015-05-20
BR122021010665B1 (pt) 2022-03-15
ECSP13012600A (es) 2013-07-31
KR102163874B1 (ko) 2020-10-12
KR20180005717A (ko) 2018-01-16
AP2013006679A0 (en) 2013-01-31
KR20190104645A (ko) 2019-09-10
GEP20166488B (en) 2016-06-10
US20140135307A1 (en) 2014-05-15
US9233950B2 (en) 2016-01-12
WO2012045803A1 (en) 2012-04-12
RS53858B1 (en) 2015-08-31
AU2011311530B2 (en) 2015-04-09
TWI546294B (zh) 2016-08-21
KR101844215B1 (ko) 2018-04-03
KR102239690B1 (ko) 2021-04-13
JP5794713B2 (ja) 2015-10-14
CY1116168T1 (el) 2017-02-08
PL2625174T3 (pl) 2015-06-30
UA109290C2 (uk) 2015-08-10
MA34545B1 (fr) 2013-09-02
CA2807255C (en) 2018-11-13
SI2625174T1 (sl) 2015-03-31
NZ605827A (en) 2015-09-25
BR112013008211B1 (pt) 2021-08-24
UY33655A (es) 2012-04-30
HUE024540T2 (hu) 2016-01-28
US8742115B2 (en) 2014-06-03
HRP20150419T1 (hr) 2015-05-22
MX2013003785A (es) 2013-06-05
US20150105371A1 (en) 2015-04-16
CO6710910A2 (es) 2013-07-15
PT2625174E (pt) 2015-03-09
MY167898A (en) 2018-09-26
IL224269A (en) 2017-08-31
BR112013008211A8 (pt) 2017-10-10
AP3268A (en) 2015-05-31
TW201305134A (zh) 2013-02-01
EP2625174B1 (en) 2015-01-21

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