DOP2016000270A - Inhibidores espirocíclicos sustituidos de la autotaxina y su preparación y uso en el tratamiento de enfermedades dependientes o mediadas por lpa - Google Patents
Inhibidores espirocíclicos sustituidos de la autotaxina y su preparación y uso en el tratamiento de enfermedades dependientes o mediadas por lpaInfo
- Publication number
- DOP2016000270A DOP2016000270A DO2016000270A DO2016000270A DOP2016000270A DO P2016000270 A DOP2016000270 A DO P2016000270A DO 2016000270 A DO2016000270 A DO 2016000270A DO 2016000270 A DO2016000270 A DO 2016000270A DO P2016000270 A DOP2016000270 A DO P2016000270A
- Authority
- DO
- Dominican Republic
- Prior art keywords
- mediated
- treatment
- autotaxin
- lpa
- replaced
- Prior art date
Links
- 201000010099 disease Diseases 0.000 title abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 3
- 230000001404 mediated effect Effects 0.000 title abstract 2
- 102100021977 Ectonucleotide pyrophosphatase/phosphodiesterase family member 2 Human genes 0.000 title 1
- 108050004000 Ectonucleotide pyrophosphatase/phosphodiesterase family member 2 Proteins 0.000 title 1
- 230000001419 dependent effect Effects 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 206010064190 Cholestatic pruritus Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000007536 Thrombosis Diseases 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 208000037976 chronic inflammation Diseases 0.000 abstract 1
- 230000006020 chronic inflammation Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000003176 fibrotic effect Effects 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 210000004698 lymphocyte Anatomy 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 208000004296 neuralgia Diseases 0.000 abstract 1
- 208000021722 neuropathic pain Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
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- A—HUMAN NECESSITIES
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- 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
-
- A—HUMAN NECESSITIES
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- 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
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
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- 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
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- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
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- 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
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Organic Chemistry (AREA)
- Epidemiology (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)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Transplantation (AREA)
- Ophthalmology & Optometry (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Gastroenterology & Hepatology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente invención se refiere a compuestos según la fórmula I: y sales farmacéuticamente aceptables, síntesis, intermedios, formulaciones, y métodos de tratamiento con las mismas enfermedades, incluyendo cáncer, homing de linfocitos, inflamación crónica, dolor neuropático, enfermedades fibróticas, trombosis, y prurito colestásico, mediados al menos en parte por ATX.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201461975123P | 2014-04-04 | 2014-04-04 |
Publications (1)
Publication Number | Publication Date |
---|---|
DOP2016000270A true DOP2016000270A (es) | 2016-12-15 |
Family
ID=54241341
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DO2016000270A DOP2016000270A (es) | 2014-04-04 | 2016-10-03 | Inhibidores espirocíclicos sustituidos de la autotaxina y su preparación y uso en el tratamiento de enfermedades dependientes o mediadas por lpa |
Country Status (21)
Country | Link |
---|---|
US (3) | US10011601B2 (es) |
EP (1) | EP3125895A4 (es) |
JP (2) | JP6616821B2 (es) |
KR (1) | KR20160133004A (es) |
CN (1) | CN107106559A (es) |
AP (1) | AP2016009496A0 (es) |
AU (2) | AU2015240519B2 (es) |
CA (1) | CA2943874A1 (es) |
CL (1) | CL2016002516A1 (es) |
CR (1) | CR20160496A (es) |
CU (1) | CU24442B1 (es) |
DO (1) | DOP2016000270A (es) |
EA (1) | EA201691840A1 (es) |
EC (1) | ECSP16084293A (es) |
IL (1) | IL248050A0 (es) |
MD (1) | MD20160116A2 (es) |
MX (1) | MX2016013049A (es) |
PE (1) | PE20170206A1 (es) |
PH (1) | PH12016501922A1 (es) |
SG (1) | SG11201607920RA (es) |
WO (1) | WO2015154023A1 (es) |
Families Citing this family (26)
Publication number | Priority date | Publication date | Assignee | Title |
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MX358310B (es) | 2012-06-13 | 2018-08-14 | Hoffmann La Roche | Nuevos diazaespirocicloalcanos y azaespirocicloalcanos. |
KR102179599B1 (ko) | 2012-09-25 | 2020-11-19 | 에프. 호프만-라 로슈 아게 | 이환형 유도체 |
AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
CN105764905B (zh) | 2013-11-26 | 2019-06-07 | 豪夫迈·罗氏有限公司 | 新的八氢-环丁二烯并[1,2-c;3,4-c’]二吡咯-2基 |
WO2015144609A1 (en) | 2014-03-26 | 2015-10-01 | F. Hoffmann-La Roche Ag | Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
CN110204550B (zh) | 2014-03-26 | 2022-05-17 | 豪夫迈·罗氏有限公司 | 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的二环化合物 |
CU24442B1 (es) | 2014-04-04 | 2019-09-04 | X Rx Inc | Derivados de n-(1-(espirocíclico)oxo) amida sustituidos como inhibidores de autotaxina |
MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
AU2016316717B2 (en) | 2015-09-04 | 2021-02-18 | F. Hoffmann-La Roche Ag | Phenoxymethyl derivatives |
AU2016328436B2 (en) | 2015-09-24 | 2020-05-14 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual ATX/CA inhibitors |
BR112018006024A2 (pt) | 2015-09-24 | 2020-05-12 | F. Hoffmann-La Roche Ag | Compostos bicíclicos como inibidores de atx |
KR20180054635A (ko) | 2015-09-24 | 2018-05-24 | 에프. 호프만-라 로슈 아게 | 오토탁신(atx) 억제제로서 이환형 화합물 |
MX2017015034A (es) | 2015-09-24 | 2018-04-13 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores duales de autotaxina (atx)/anhidrasa carbonica (ca). |
JP2019510752A (ja) | 2016-03-04 | 2019-04-18 | ギリアード サイエンシーズ, インコーポレイテッド | オートタキシン阻害剤の組成物及び合剤 |
JOP20190107A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
CN108456208B (zh) * | 2017-02-22 | 2021-04-16 | 广州市恒诺康医药科技有限公司 | 氮杂螺环类化合物及其制备方法和应用 |
JP7090099B2 (ja) | 2017-03-16 | 2022-06-23 | エフ.ホフマン-ラ ロシュ アーゲー | Atxインヒビターとしての新規二環式化合物 |
EP3596059B1 (en) | 2017-03-16 | 2024-04-24 | F. Hoffmann-La Roche AG | Heterocyclic compounds useful as dual atx/ca inhibitors |
US10961242B2 (en) | 2017-05-17 | 2021-03-30 | Legochem Biosciences, Inc. | Compounds as autotaxin inhibitors and pharmaceutical compositions comprising the same |
KR101798840B1 (ko) | 2017-05-17 | 2017-11-17 | 주식회사 레고켐 바이오사이언스 | 신규 오토탁신 저해 화합물 및 이를 함유하는 약제학적 조성물 |
BR112020005720A2 (pt) | 2017-09-29 | 2020-10-20 | Takeda Pharmaceutical Company Limited | composto ou sal, medicamento, métodos para inibir monoacilglicerol lipase e para a profilaxia ou o tratamento de doença de alzheimer, doença de parkinson, doença de huntington, esclerose lateral amiotrófica, esclerose múltipla, distúrbio de ansiedade, dor, epilepsia ou depressão, e, uso do composto ou sal. |
WO2020051230A1 (en) * | 2018-09-04 | 2020-03-12 | X-Rx, Inc. | Amorphous pharmaceutical compositions and uses thereof |
TW202229255A (zh) | 2020-11-13 | 2022-08-01 | 丹麥商H 朗德貝克公司 | Magl抑制劑 |
CN112675308B (zh) * | 2020-12-09 | 2023-05-05 | 中国人民解放军军事科学院军事医学研究院 | 抑制enpp2基因和/或蛋白表达的物质在制备治疗多发性骨髓瘤的药物中的应用 |
CN116806150A (zh) * | 2021-01-05 | 2023-09-26 | 载度思生命科学有限公司 | 新的自分泌运动因子抑制剂 |
WO2024073658A1 (en) * | 2022-09-30 | 2024-04-04 | Genentech, Inc. | Hydantoin modulators of cholesterol biosynthesis and their use for promoting remyelination |
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2015
- 2015-04-03 CU CU2016000150A patent/CU24442B1/es unknown
- 2015-04-03 EA EA201691840A patent/EA201691840A1/ru unknown
- 2015-04-03 CR CR20160496A patent/CR20160496A/es unknown
- 2015-04-03 AP AP2016009496A patent/AP2016009496A0/en unknown
- 2015-04-03 KR KR1020167030589A patent/KR20160133004A/ko unknown
- 2015-04-03 EP EP15773254.6A patent/EP3125895A4/en not_active Withdrawn
- 2015-04-03 PE PE2016001885A patent/PE20170206A1/es unknown
- 2015-04-03 CA CA2943874A patent/CA2943874A1/en not_active Abandoned
- 2015-04-03 AU AU2015240519A patent/AU2015240519B2/en not_active Ceased
- 2015-04-03 JP JP2017503794A patent/JP6616821B2/ja not_active Expired - Fee Related
- 2015-04-03 US US15/300,762 patent/US10011601B2/en not_active Expired - Fee Related
- 2015-04-03 MD MDA20160116A patent/MD20160116A2/ro not_active Application Discontinuation
- 2015-04-03 WO PCT/US2015/024338 patent/WO2015154023A1/en active Application Filing
- 2015-04-03 MX MX2016013049A patent/MX2016013049A/es unknown
- 2015-04-03 CN CN201580028170.3A patent/CN107106559A/zh active Pending
- 2015-04-03 SG SG11201607920RA patent/SG11201607920RA/en unknown
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2016
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- 2016-09-28 PH PH12016501922A patent/PH12016501922A1/en unknown
- 2016-10-03 DO DO2016000270A patent/DOP2016000270A/es unknown
- 2016-10-04 CL CL2016002516A patent/CL2016002516A1/es unknown
- 2016-10-26 EC ECIEPI201684293A patent/ECSP16084293A/es unknown
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2018
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2019
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- 2019-11-08 JP JP2019203023A patent/JP2020040960A/ja active Pending
- 2019-11-15 AU AU2019264641A patent/AU2019264641A1/en not_active Abandoned
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MD20160116A2 (ro) | 2017-04-30 |
US20170166568A1 (en) | 2017-06-15 |
CU20160150A7 (es) | 2017-02-02 |
US20180282332A1 (en) | 2018-10-04 |
JP6616821B2 (ja) | 2019-12-04 |
CR20160496A (es) | 2017-01-02 |
EA201691840A1 (ru) | 2017-03-31 |
AU2015240519A1 (en) | 2016-10-20 |
CL2016002516A1 (es) | 2017-05-12 |
EP3125895A1 (en) | 2017-02-08 |
MX2016013049A (es) | 2017-04-27 |
AP2016009496A0 (en) | 2016-10-31 |
JP2020040960A (ja) | 2020-03-19 |
CU24442B1 (es) | 2019-09-04 |
AU2019264641A1 (en) | 2019-12-05 |
CA2943874A1 (en) | 2015-10-08 |
EP3125895A4 (en) | 2017-08-30 |
KR20160133004A (ko) | 2016-11-21 |
CN107106559A (zh) | 2017-08-29 |
SG11201607920RA (en) | 2016-10-28 |
US10233182B2 (en) | 2019-03-19 |
IL248050A0 (en) | 2016-11-30 |
PE20170206A1 (es) | 2017-04-09 |
WO2015154023A1 (en) | 2015-10-08 |
ECSP16084293A (es) | 2017-01-31 |
JP2017513932A (ja) | 2017-06-01 |
AU2015240519B2 (en) | 2019-08-15 |
PH12016501922A1 (en) | 2016-12-19 |
US10011601B2 (en) | 2018-07-03 |
US20190225611A1 (en) | 2019-07-25 |
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