CN106414435A - 氨基‑取代的异噻唑 - Google Patents

氨基‑取代的异噻唑 Download PDF

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Publication number
CN106414435A
CN106414435A CN201580017711.2A CN201580017711A CN106414435A CN 106414435 A CN106414435 A CN 106414435A CN 201580017711 A CN201580017711 A CN 201580017711A CN 106414435 A CN106414435 A CN 106414435A
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CN
China
Prior art keywords
methyl
amino
group
alkyl
thiazole
Prior art date
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Pending
Application number
CN201580017711.2A
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English (en)
Chinese (zh)
Inventor
L.贝法克
G.西迈斯特
T.海因里希
S.普雷希特尔
D.施特基希特
A.罗特曼
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.)
Bayer Pharma AG
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Bayer Pharma AG
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
Priority claimed from EP14178680.6A external-priority patent/EP2980088A1/en
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of CN106414435A publication Critical patent/CN106414435A/zh
Pending legal-status Critical Current

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    • 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
    • C07D417/14—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 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic 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
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
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    • A61P35/00—Antineoplastic agents
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    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201580017711.2A 2014-01-29 2015-01-26 氨基‑取代的异噻唑 Pending CN106414435A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP14153031.1 2014-01-29
EP14153031 2014-01-29
EP14178680.6A EP2980088A1 (en) 2014-07-28 2014-07-28 Amino-substituted isothiazoles
EP14178680.6 2014-07-28
PCT/EP2015/051440 WO2015113920A1 (en) 2014-01-29 2015-01-26 Amino-substituted isothiazoles

Publications (1)

Publication Number Publication Date
CN106414435A true CN106414435A (zh) 2017-02-15

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ID=52434789

Family Applications (1)

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CN201580017711.2A Pending CN106414435A (zh) 2014-01-29 2015-01-26 氨基‑取代的异噻唑

Country Status (6)

Country Link
US (1) US20170334899A1 (enExample)
EP (1) EP3099682A1 (enExample)
JP (1) JP2017512184A (enExample)
CN (1) CN106414435A (enExample)
CA (1) CA2937989A1 (enExample)
WO (1) WO2015113920A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110475791A (zh) * 2017-03-29 2019-11-19 伊士曼化工公司 区域选择性取代的纤维素酯
CN114174273A (zh) * 2019-03-22 2022-03-11 优曼尼蒂治疗公司 化合物和其用途

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Hdac抑制劑與pd-l1抑制劑之組合治療
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
EP3529245A4 (en) 2016-10-24 2020-12-23 Yumanity Therapeutics, Inc. COMPOUNDS AND USES OF THE LATEST
MA47212A (fr) 2017-01-06 2019-11-13 Yumanity Therapeutics Inc Méthodes de traitement de troubles neurologiques
WO2019084157A1 (en) 2017-10-24 2019-05-02 Yumanity Therapeutics, Inc. COMPOUNDS AND USES THEREOF
ES3043183T3 (en) 2018-03-23 2025-11-25 Janssen Pharmaceutica Nv Compounds and uses thereof
MA54829A (fr) 2019-01-24 2021-12-01 Yumanity Therapeutics Inc Composés et leurs utilisations
EA202192047A1 (ru) 2019-11-13 2021-12-08 Юманити Терапьютикс, Инк. Соединения и их применение

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101965336A (zh) * 2008-01-04 2011-02-02 英特利凯恩股份有限公司 某些化学实体、组合物和方法
CN103153970A (zh) * 2010-04-15 2013-06-12 诺瓦提斯公司 作为ksp抑制剂的*唑和噻唑化合物
WO2014118186A1 (en) * 2013-01-30 2014-08-07 Bayer Pharma Aktiengesellschaft Amino-substituted isothiazoles

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101965336A (zh) * 2008-01-04 2011-02-02 英特利凯恩股份有限公司 某些化学实体、组合物和方法
CN103153970A (zh) * 2010-04-15 2013-06-12 诺瓦提斯公司 作为ksp抑制剂的*唑和噻唑化合物
WO2014118186A1 (en) * 2013-01-30 2014-08-07 Bayer Pharma Aktiengesellschaft Amino-substituted isothiazoles

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BURAK K,等: "Synthesis of isothiazole Derivatives with potential biological activity", 《DIE PHARMAZIE》 *
URSZULA LIPNICKA,等: "New Amides of 5-Acylamino-3-Methyl-4-Isothiazolecarboxylic Acid and their Immunotropic Activity", 《ARCH. PHARM. CHEM. LIFE SCI.》 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110475791A (zh) * 2017-03-29 2019-11-19 伊士曼化工公司 区域选择性取代的纤维素酯
CN110475791B (zh) * 2017-03-29 2021-12-21 伊士曼化工公司 区域选择性取代的纤维素酯
CN114174273A (zh) * 2019-03-22 2022-03-11 优曼尼蒂治疗公司 化合物和其用途

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JP2017512184A (ja) 2017-05-18
CA2937989A1 (en) 2015-08-06
EP3099682A1 (en) 2016-12-07
US20170334899A1 (en) 2017-11-23
WO2015113920A1 (en) 2015-08-06

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