Processing

Please wait...

Settings

Settings

Goto Application

1. WO2016145935 - OPTIMISED COMBINATION THERAPY AND USE THEREOF TO TREAT CANCER AND AUTOIMMUNE DISEASE

Publication Number WO/2016/145935
Publication Date 22.09.2016
International Application No. PCT/CN2016/000149
International Filing Date 18.03.2016
IPC
C07D 487/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/519 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61K 45/06 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 37/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
A61P 29/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
A61P 5/14 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
14of the thyroid hormones, e.g. T3, T4
CPC
A61K 2300/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
2300Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
A61K 31/4162
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
4151,2-Diazoles
4162condensed with heterocyclic ring systems
A61K 31/436
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
436the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
A61K 31/454
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
445Non condensed piperidines, e.g. piperocaine
4523containing further heterocyclic ring systems
454containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/519
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61K 31/52
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
52Purines, e.g. adenine
Applicants
  • 浙江导明医药科技有限公司 ZHEJIANG DTRM BIOPHARMA CO., LTD. [CN]/[CN]
Inventors
  • 何伟 HE, Wei
Priority Data
201510119944.519.03.2015CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) OPTIMISED COMBINATION THERAPY AND USE THEREOF TO TREAT CANCER AND AUTOIMMUNE DISEASE
(FR) POLYTHÉRAPIE OPTIMISÉE ET SON UTILISATION POUR LE TRAITEMENT DU CANCER ET DE MALADIES AUTO-IMMUNES
(ZH) 优化的联合用药及其治疗癌症和自身免疫疾病的用途
Abstract
(EN)
Provided is a series of new poly-fluorosubstituted pyrazolopyrimidine compounds or salts. The compounds are Bruton's tyrosine kinase (BTK) inhibitors. The compounds have better kinase inhibition selectivity and pharmokinetic properties. Also provided is a preparation method for the compounds. Also provided is a combination therapy including the compounds in combination with another targeted drug composition or another drug. The optimised combination therapy has a cooperative effect, inhibits the existence of a tumour better than a single targeted drug, and causes certain tumours to completely disappear. The optimised combination therapy treats drug resistance and cancer recurrence of a tumour better than a single targeted drug, and the treatment cycle is shorter. The present invention also relates to a combined compound and a pharmaceutical preparation wherein said combined compound acts as an active ingredient, said pharmaceutical preparation being safer at a lower dosage and having a cooperative effect efficacy. Also provided is a method of using the compounds and a preparation thereof to treat and inhibit an autoimmune disease or illness, a heterogeneous autoimmune disease or illness, an inflammatory disease, a cancer or an illness.
(FR)
La présente invention concerne une série de nouveaux composés ou sels de pyrazolopyrimidine polyfluorés. Les composés sont des inhibiteurs de la tyrosine kinase de Bruton (BTK). Les composés ont une meilleure sélectivité d'inhibition des kinases et de meilleures propriétés pharmacocinétiques. L'invention concerne également une méthode de préparation des composés. L'invention concerne également une polythérapie comprenant les composés en association avec une autre composition de médicament ciblée ou un autre médicament. La polythérapie optimisée a un effet de coopération, inhibe mieux l'existence d'une tumeur qu'un seul médicament ciblé, et amène certaines tumeurs à disparaître complètement. La polythérapie optimisée traite mieux la résistance aux médicaments et la récidive cancéreuse d'une tumeur qu'un seul médicament ciblé, et le cycle de traitement est plus court. La présente invention concerne également un composé combiné et une préparation pharmaceutique où ledit composé combiné joue le rôle de principe actif, ladite préparation pharmaceutique étant d'utilisation plus sûre à une dose plus faible et possédant une efficacité de type effet coopératif. L'invention concerne également une méthode d'utilisation des composés et une préparation de ceux-ci pour traiter et inhiber une affection ou maladie auto-immune, une affection ou maladie auto-immune hétérogène, une maladie inflammatoire, un cancer ou une maladie.
(ZH)
本发明提供一系列新的多氟取代的吡唑并嘧啶类化合物或盐。这类化合物是酪氨酸激酶(BTK)的抑制剂。这类化合物可具有更好的激酶抑制选择性和药代药谢性质。本发明公开了所述化合物的制备方法。本发明也公开了包含所属化合物与其他靶向药物组合物或其他药物相互组合的联合用药。优化的联合用药具有协同作用、比单一靶向药物能更好地抑制肿瘤的生存,可造成某些肿瘤完全消失。优化的联合用药比单一靶向药物能更好治疗肿瘤的耐药性和癌症复发,治疗周期更短。本发明还涉及组合化合物及其作为活性成分的药物制剂,在更低剂量下更安全并有协同效应的疗效。本发明还包括使用这些化合物和它们的制剂来治疗和抑制自身免疫性疾病或病症、异种免疫性疾病或病症、炎性疾病以及癌症或病症的方法。
Latest bibliographic data on file with the International Bureau