AU2013299557B2 - Heteroaromatic compounds as Bruton's tyrosine kinase (BTK) inhibitors - Google Patents

Heteroaromatic compounds as Bruton's tyrosine kinase (BTK) inhibitors Download PDF

Info

Publication number
AU2013299557B2
AU2013299557B2 AU2013299557A AU2013299557A AU2013299557B2 AU 2013299557 B2 AU2013299557 B2 AU 2013299557B2 AU 2013299557 A AU2013299557 A AU 2013299557A AU 2013299557 A AU2013299557 A AU 2013299557A AU 2013299557 B2 AU2013299557 B2 AU 2013299557B2
Authority
AU
Australia
Prior art keywords
mmol
pharmaceutically acceptable
chosen
tautomers
mixture
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
AU2013299557A
Other languages
English (en)
Other versions
AU2013299557A1 (en
Inventor
Joerg Martin Bentzien
Angela Kay BERRY
Todd Bosanac
Michael Jason Burke
Darren Todd Disalvo
Joshua Courtney Horan
Shuang Liang
Can Mao
Wang Mao
Yue Shen
Fariba Soleymanzadeh
Renee M. Zindell
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim International GmbH
Original Assignee
Boehringer Ingelheim International GmbH
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=49029216&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AU2013299557(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim International GmbH filed Critical Boehringer Ingelheim International GmbH
Publication of AU2013299557A1 publication Critical patent/AU2013299557A1/en
Application granted granted Critical
Publication of AU2013299557B2 publication Critical patent/AU2013299557B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • C07D417/08—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 carbon chain containing alicyclic 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
    • A61K31/435—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
    • 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
    • A61P11/02—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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or 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
    • C07D231/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or 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
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • 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
    • C07D401/02—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
    • C07D401/06—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 carbon chain containing only aliphatic carbon 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
    • C07D401/14—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
    • 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
    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/08—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 linked by a carbon chain containing alicyclic rings
    • 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
    • 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
    • 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
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
AU2013299557A 2012-08-10 2013-08-08 Heteroaromatic compounds as Bruton's tyrosine kinase (BTK) inhibitors Ceased AU2013299557B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261681684P 2012-08-10 2012-08-10
US61/681,684 2012-08-10
PCT/US2013/054096 WO2014025976A1 (en) 2012-08-10 2013-08-08 Heteroaromatic compounds as bruton's tyrosine kinase (btk) inhibitors

Publications (2)

Publication Number Publication Date
AU2013299557A1 AU2013299557A1 (en) 2015-01-29
AU2013299557B2 true AU2013299557B2 (en) 2017-06-22

Family

ID=49029216

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2013299557A Ceased AU2013299557B2 (en) 2012-08-10 2013-08-08 Heteroaromatic compounds as Bruton's tyrosine kinase (BTK) inhibitors

Country Status (24)

Country Link
US (5) US20140045813A1 (enExample)
EP (1) EP2882741B1 (enExample)
JP (1) JP6348492B2 (enExample)
KR (1) KR20150040292A (enExample)
CN (1) CN104603124B (enExample)
AP (1) AP2015008203A0 (enExample)
AU (1) AU2013299557B2 (enExample)
BR (1) BR112015002590A2 (enExample)
CA (1) CA2881519A1 (enExample)
CL (1) CL2015000256A1 (enExample)
EA (1) EA029210B1 (enExample)
EC (1) ECSP15008851A (enExample)
GE (1) GEP201706748B (enExample)
IL (1) IL236495A0 (enExample)
IN (1) IN2015DN00524A (enExample)
MA (1) MA37830B1 (enExample)
MX (1) MX2015001802A (enExample)
NZ (1) NZ703607A (enExample)
PE (1) PE20150756A1 (enExample)
PH (1) PH12015500294B1 (enExample)
SA (1) SA515360007B1 (enExample)
SG (1) SG11201500499TA (enExample)
TN (1) TN2015000029A1 (enExample)
WO (1) WO2014025976A1 (enExample)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104603124B (zh) 2012-08-10 2018-04-17 勃林格殷格翰国际有限公司 用作布鲁顿酪氨酸激酶(btk)抑制剂的杂芳族化合物
US20150291554A1 (en) 2012-11-02 2015-10-15 Pfizer Inc. Bruton's Tyrosine Kinase Inhibitors
CN103848810A (zh) * 2012-11-30 2014-06-11 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
WO2014151620A1 (en) * 2013-03-14 2014-09-25 Boehringer Ingelheim International Gmbh 5-thiazolecarboxamide dervatives and their use as btk inhibitors
WO2014152114A1 (en) 2013-03-15 2014-09-25 Boehringer Ingelheim International Gmbh Heteroaromatic compounds as btk inhibitors
EP2970291B1 (en) * 2013-03-15 2022-05-11 Janssen Pharmaceutica, N.V. Processes and intermediates for preparing a medicament
RU2677884C2 (ru) 2013-09-30 2019-01-22 Гуанчжоу Иннокэа Фарма Тек Ко., Лтд. Замещенные никотинимидные ингибиторы втк, их получение и применение в терапии раковых, воспалительных и аутоиммунных заболеваний
US9512084B2 (en) 2013-11-29 2016-12-06 Novartis Ag Amino pyrimidine derivatives
JP6486954B2 (ja) * 2014-01-29 2019-03-20 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｂｔｋ阻害剤としてのピラゾール化合物
WO2015185998A2 (en) * 2014-04-11 2015-12-10 Acerta Pharma B.V. Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bone marrow x kinase
CN105085474B (zh) * 2014-05-07 2018-05-18 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
CN105884747B (zh) * 2014-08-28 2021-01-05 首药控股(北京)有限公司 一种制备布鲁顿酪氨酸激酶(btk)激酶抑制剂的制备方法
GB201519352D0 (en) 2015-11-02 2015-12-16 Heptares Therapeutics Ltd Pharmaceutical compounds
HRP20211845T1 (hr) * 2015-12-16 2022-03-04 Boehringer Ingelheim International Gmbh Derivati bipirazolila korisni za liječenje autoimunih bolesti
CN114605327B (zh) * 2015-12-16 2025-03-11 洛克索肿瘤学股份有限公司 可用作激酶抑制剂的化合物
CN105646318A (zh) * 2015-12-30 2016-06-08 武汉药明康德新药开发有限公司 一种2-叔丁氧羰基-5-氮杂螺环[3.3]庚烷-6-羧酸的合成方法
US10570118B2 (en) 2016-01-13 2020-02-25 Boehringer Ingelheim International Gmbh Isoquinolones as BTK inhibitors
CN107226805A (zh) * 2016-03-24 2017-10-03 北京天诚医药科技有限公司 芳香族酰胺类衍生物、其制备方法及其在医药上的应用
EP4252847A3 (en) 2016-08-15 2023-11-15 Novartis AG Regimens and methods of treating multiple sclerosis using ofatumumab
CN107759602B (zh) * 2016-08-17 2020-04-21 中国科学院上海药物研究所 含有共轭联烯结构的化合物、其药物组合物和用途
JOP20190113A1 (ar) * 2016-11-18 2019-05-15 Biocad Joint Stock Co مثبطات بروتون تيروزين كيناز
EP3824906A1 (en) 2016-12-21 2021-05-26 Amgen Inc. Anti-tnf alpha antibody formulations
CN110944999A (zh) 2017-08-01 2020-03-31 勃林格殷格翰国际有限公司 中间体化合物和方法
TWI767148B (zh) * 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
AU2019387370A1 (en) 2018-11-30 2021-06-10 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
GB201819961D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
CN113227077B (zh) * 2018-12-13 2024-10-29 英特维特国际股份有限公司 一种制备1-[(3r,4s)-4-氰基四氢吡喃-3-基]-3-[(2-氟-6-甲氧基-4-吡啶基)氨基]吡唑-4-甲酰胺的方法
KR102200032B1 (ko) * 2019-03-13 2021-01-08 전남대학교산학협력단 호흡기 질환의 예방 또는 치료용 조성물
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
JP7475370B2 (ja) * 2019-05-10 2024-04-26 河南知微生物医薬有限公司 ブルトン型チロシンキナーゼ阻害剤としての置換されている１－アミノ－１ｈ－イミダゾール－５－カルボキサミド
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
EP4741018A3 (en) * 2020-06-19 2026-07-15 Anaxis Pharma Pty Ltd Sulphonamide compounds
CN114573586B (zh) * 2020-11-28 2023-11-03 杭州和正医药有限公司 一种抑制布鲁顿酪氨酸激酶活性的多环化合物、药物组合物及其应用
EP4448523A1 (en) 2021-12-14 2024-10-23 Crossfire Oncology Holding B.V. Macrocyclic btk inhibitors
WO2023110936A1 (en) 2021-12-14 2023-06-22 Netherlands Translational Research Center Holding B.V Reversible macrocyclic kinase inhibitors
CN116554102B (zh) * 2022-01-28 2025-10-03 深圳海博为药业有限公司 一种作为btk抑制剂的化合物及其制备方法和应用
CR20250069A (es) * 2022-08-04 2025-05-26 Nxera Pharma Uk Ltd Formas cristalinas y sales de un agonista del receptor muscarínico

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008121742A2 (en) * 2007-03-28 2008-10-09 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9608435D0 (en) * 1996-04-24 1996-06-26 Celltech Therapeutics Ltd Chemical compounds
HRP20040098B1 (en) 2001-08-13 2012-08-31 Janssen Pharmaceutica N.V. 2,4,5-TRlSUBSTITUTED THIAZOLYL DERIVATIVES AND THEIR ANTIINFLAMMATORY ACTIVITY
WO2003072541A2 (en) 2001-09-27 2003-09-04 Smithkline Beecham Corporation Chemical compounds
FR2881426B1 (fr) * 2005-02-03 2007-03-30 Aventis Pharma Sa Pyrolles et imidazoles substitues, compositions les contenant, procede de frabrication et utilisation
ATE534632T1 (de) * 2006-04-11 2011-12-15 Vertex Pharma Thiazole, imidazole und pyrazole als proteinkinasehemmer
AR063706A1 (es) 2006-09-11 2009-02-11 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
EP2529621B1 (en) * 2006-09-22 2016-10-05 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
PE20100851A1 (es) 2008-06-24 2011-01-31 Hoffmann La Roche PIRIDIN-2-ONAS Y PIRIDAZIN-3-ONAS SUSTITUIDAS COMO INHIBIDORES DE Btk
DK2310528T3 (da) 2008-07-29 2013-12-02 Univ Liege Genetisk markør-test til brachyspina og frugtbarhed hos kvæg
GB0820819D0 (en) * 2008-11-13 2008-12-24 Sareum Ltd Pharmaceutical compounds
JP2012516329A (ja) * 2009-01-30 2012-07-19 ミレニアム ファーマシューティカルズ， インコーポレイテッド Ｐｉ３ｋ阻害剤としてのヘテロアリールおよびその使用
US8299077B2 (en) 2009-03-02 2012-10-30 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
BR112012014884A2 (pt) 2009-12-17 2016-03-22 Merck Patent Gmbh inibidores de esfingosina quinase
US8940725B2 (en) 2010-05-31 2015-01-27 Ono Pharmaceutical Co., Ltd. Purinone derivative
US8859768B2 (en) * 2010-08-11 2014-10-14 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
AR082590A1 (es) 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
ES2590491T3 (es) 2011-05-17 2016-11-22 F. Hoffmann-La Roche Ag Inhibidores de la tirosina quinasa de Bruton
KR20140052032A (ko) 2011-08-17 2014-05-02 에프. 호프만-라 로슈 아게 브루톤 티로신 키나아제의 억제제
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
EP2809673B1 (en) 2012-01-31 2016-11-02 Nanjing Allgen Pharma Co. Ltd. Spirocyclic molecules as bruton's tyrosine kinase inhibitors
CN104662018B (zh) 2012-04-20 2017-10-24 阿迪维纳斯治疗有限公司 取代的杂双环化合物、组合物及其医疗应用
CN104603124B (zh) 2012-08-10 2018-04-17 勃林格殷格翰国际有限公司 用作布鲁顿酪氨酸激酶(btk)抑制剂的杂芳族化合物
US9499548B2 (en) 2012-09-13 2016-11-22 Hoffmann-La Roche Inc. Inhibitors of bruton's tyrosine kinase
US20150291554A1 (en) 2012-11-02 2015-10-15 Pfizer Inc. Bruton's Tyrosine Kinase Inhibitors
CN103848810A (zh) 2012-11-30 2014-06-11 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
WO2014152114A1 (en) 2013-03-15 2014-09-25 Boehringer Ingelheim International Gmbh Heteroaromatic compounds as btk inhibitors
AU2014316247A1 (en) 2013-09-03 2016-03-31 Carna Biosciences, Inc. Novel 2,6-diaminopyrimidine derivative
JP6486954B2 (ja) 2014-01-29 2019-03-20 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｂｔｋ阻害剤としてのピラゾール化合物
HRP20211845T1 (hr) 2015-12-16 2022-03-04 Boehringer Ingelheim International Gmbh Derivati bipirazolila korisni za liječenje autoimunih bolesti

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008121742A2 (en) * 2007-03-28 2008-10-09 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase

Also Published As

Publication number Publication date
EA029210B1 (ru) 2018-02-28
IN2015DN00524A (enExample) 2015-06-26
SG11201500499TA (en) 2015-03-30
EA201500207A1 (ru) 2015-08-31
IL236495A0 (en) 2015-02-26
PH12015500294A1 (en) 2015-04-20
NZ703607A (en) 2018-02-23
JP6348492B2 (ja) 2018-06-27
KR20150040292A (ko) 2015-04-14
CL2015000256A1 (es) 2015-07-03
CN104603124A (zh) 2015-05-06
ECSP15008851A (es) 2015-12-31
BR112015002590A2 (pt) 2019-08-06
US10138229B2 (en) 2018-11-27
US20170320867A1 (en) 2017-11-09
US20160031872A1 (en) 2016-02-04
JP2015524480A (ja) 2015-08-24
US20140045813A1 (en) 2014-02-13
EP2882741B1 (en) 2018-10-24
CN104603124B (zh) 2018-04-17
TN2015000029A1 (en) 2016-06-29
PH12015500294B1 (en) 2015-04-20
GEP201706748B (en) 2017-10-10
US20180086748A1 (en) 2018-03-29
US20190112302A1 (en) 2019-04-18
HK1210161A1 (en) 2016-04-15
WO2014025976A1 (en) 2014-02-13
MX2015001802A (es) 2015-05-07
MA20150290A1 (fr) 2015-08-31
US10875852B2 (en) 2020-12-29
EP2882741A1 (en) 2015-06-17
AP2015008203A0 (en) 2015-01-31
CA2881519A1 (en) 2014-02-13
SA515360007B1 (ar) 2016-09-04
PE20150756A1 (es) 2015-06-03
MA37830B1 (fr) 2018-09-28
AU2013299557A1 (en) 2015-01-29

Similar Documents

Publication Publication Date Title
US10875852B2 (en) Heteroaromatic compounds as BTK inhibitors
US8940893B2 (en) Heteroaromatic compounds as BTK inhibitors
EP3099674B1 (en) Pyrazole compounds as btk inhibitors
CA3005268C (en) Heteroaromatic compounds as btk inhibitors
US10570118B2 (en) Isoquinolones as BTK inhibitors
EP2970163B1 (en) 5-thiazolecarboxamide dervatives and their use as btk inhibitors
IL271104A (en) The traumatic compounds as inhibitors and fines
OA17161A (en) Heteroaromatic compounds as bruton's tyrosine kinase (BTK) inhibitors
HK1256795B (en) Bipyrazolyl derivatives useful for the treatment of autoimmune diseases

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired