WO2011159852A1 - Piperidinyl compound as a modulator of chemokine receptor activity - Google Patents

Piperidinyl compound as a modulator of chemokine receptor activity Download PDF

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Publication number
WO2011159852A1
WO2011159852A1 PCT/US2011/040605 US2011040605W WO2011159852A1 WO 2011159852 A1 WO2011159852 A1 WO 2011159852A1 US 2011040605 W US2011040605 W US 2011040605W WO 2011159852 A1 WO2011159852 A1 WO 2011159852A1
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WO
WIPO (PCT)
Prior art keywords
compound
patient
effective amount
therapeutically effective
administering
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
PCT/US2011/040605
Other languages
English (en)
French (fr)
Inventor
Robert J. Cherney
John V. Duncia
Daniel S. Gardner
Joseph B. Santella
Zhongyu Wang
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.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
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 to BR112012031768A priority Critical patent/BR112012031768A2/pt
Priority to CA2802714A priority patent/CA2802714A1/en
Priority to JP2013515497A priority patent/JP5795797B2/ja
Priority to EA201270790A priority patent/EA022395B1/ru
Priority to KR1020137001026A priority patent/KR20130032357A/ko
Priority to SG2012085353A priority patent/SG186064A1/en
Priority to CN201180039590.3A priority patent/CN103068800B/zh
Priority to MA35558A priority patent/MA34377B1/fr
Priority to AU2011268373A priority patent/AU2011268373B2/en
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Priority to EP11728134.5A priority patent/EP2582670B1/en
Priority to NZ605741A priority patent/NZ605741A/en
Priority to MX2012014068A priority patent/MX2012014068A/es
Publication of WO2011159852A1 publication Critical patent/WO2011159852A1/en
Priority to IL223368A priority patent/IL223368A0/en
Priority to TNP2012000581A priority patent/TN2012000581A1/en
Anticipated expiration legal-status Critical
Priority to ZA2013/00380A priority patent/ZA201300380B/en
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/36—Heterocyclic 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
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/52—Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
    • 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
    • A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • 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
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    • 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
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • 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]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
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    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/02—Immunomodulators
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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

Definitions

  • Step 3 3S,4S)-tert-butyl 4-(4-chlorophenyl)-3,4-dihydroxy-3- methylpiperidine- 1 -carboxylate
  • the mixture was then cooled to 5 °C and treated with solid sodium sulfite, and the mixture was stirred for 1 hour, during which time a clear solution was observed.
  • the mixture was extracted with ethyl acetate (3 x), then the combined organic phases were washed twice with water, and once with brine, dried over sodium sulfate, and concentrated in vacuo.
  • Step 5 tert-butyl (R)-l-((35,45)-4-(4-chlorophenyl)-3,4-dihydroxy-3- methylpiperidin- 1 -yl)-3 -methyl- 1 -oxobutan-2-ylcarbamate
  • Step 8 (R)-3,3-difluorocyclopentanecarboxylic acid
  • Test compound is received as 20 mM in DMSO.
  • Compound is diluted to create a 300 ⁇ acetonitrile (ACN) solution containing 1.5% DMSO, which is then used as a lOOx stock for incubation with microsomes.
  • ACN acetonitrile
  • Each compound is tested in duplicate separately in each of three species in the Metabolic Stability -Human, Rat, Mouse assay suite or individual species in the Metabolic Stability-Dog or Metabolic Stability-Monkey suites.
  • Compound, NADPH and liver microsome solutions are combined for incubation in three steps:
  • the compound is typically administered in admixture with suitable pharmaceutical diluents, excipients, or carriers (collectively referred to herein as pharmaceutical carriers) suitably selected with respect to the intended form of administration, that is, oral tablets, capsules, elixirs, syrups and the like, and consistent with conventional pharmaceutical practices.
  • suitable pharmaceutical diluents, excipients, or carriers suitably selected with respect to the intended form of administration, that is, oral tablets, capsules, elixirs, syrups and the like, and consistent with conventional pharmaceutical practices.
  • Dosage forms suitable for administration may contain from about 1 milligram to about 100 milligrams of active ingredient per dosage unit.
  • the active ingredient will ordinarily be present in an amount of about 0.5-95% by weight based on the total weight of the composition.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Molecular Biology (AREA)
  • Psychiatry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Diabetes (AREA)
  • AIDS & HIV (AREA)
PCT/US2011/040605 2010-06-16 2011-06-16 Piperidinyl compound as a modulator of chemokine receptor activity Ceased WO2011159852A1 (en)

Priority Applications (15)

Application Number Priority Date Filing Date Title
AU2011268373A AU2011268373B2 (en) 2010-06-16 2011-06-16 Piperidinyl compound as a modulator of chemokine receptor activity
JP2013515497A JP5795797B2 (ja) 2010-06-16 2011-06-16 ケモカイン受容体活性の調整薬としてのピペリジニル化合物
EP11728134.5A EP2582670B1 (en) 2010-06-16 2011-06-16 Piperidinyl compound as a modulator of chemokine receptor activity
KR1020137001026A KR20130032357A (ko) 2010-06-16 2011-06-16 케모카인 수용체 활성의 조절제로서의 피페리디닐 화합물
SG2012085353A SG186064A1 (en) 2010-06-16 2011-06-16 Piperidinyl compound as a modulator of chemokine receptor activity
CN201180039590.3A CN103068800B (zh) 2010-06-16 2011-06-16 作为趋化因子受体活性调节剂的哌啶基化合物
MA35558A MA34377B1 (fr) 2010-06-16 2011-06-16 Composé de pipéridinyle en tant que modulateur de l'activité des récepteurs des chimiokines
BR112012031768A BR112012031768A2 (pt) 2010-06-16 2011-06-16 composto de piperidinila como um modulador de atividade receptora de quimiocina
EA201270790A EA022395B1 (ru) 2010-06-16 2011-06-16 Соединение пиперидинила в качестве модулятора активности хемокинового рецептора
CA2802714A CA2802714A1 (en) 2010-06-16 2011-06-16 Piperidinyl compound as a modulator of chemokine receptor activity
NZ605741A NZ605741A (en) 2010-06-16 2011-06-16 Piperidinyl compound as a modulator of chemokine receptor activity
MX2012014068A MX2012014068A (es) 2010-06-16 2011-06-16 Compuestos de piperidinilo como modulador de la actividad de receptor de quimiocinas.
IL223368A IL223368A0 (en) 2010-06-16 2012-11-29 Piperidinyl compounds as a modulator of chemokine receptor activity
TNP2012000581A TN2012000581A1 (en) 2010-06-16 2012-12-07 Piperidinyl compound as a modulator of chemokine receptor activity
ZA2013/00380A ZA201300380B (en) 2010-06-16 2013-01-15 Piperidinyl compound as a modulator of chemokine receptor activity

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US35522510P 2010-06-16 2010-06-16
US61/355,225 2010-06-16

Publications (1)

Publication Number Publication Date
WO2011159852A1 true WO2011159852A1 (en) 2011-12-22

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ID=44278764

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2011/040605 Ceased WO2011159852A1 (en) 2010-06-16 2011-06-16 Piperidinyl compound as a modulator of chemokine receptor activity

Country Status (20)

Country Link
US (1) US8642622B2 (https=)
EP (1) EP2582670B1 (https=)
JP (1) JP5795797B2 (https=)
KR (1) KR20130032357A (https=)
CN (1) CN103068800B (https=)
AR (1) AR081943A1 (https=)
AU (1) AU2011268373B2 (https=)
BR (1) BR112012031768A2 (https=)
CL (1) CL2012003521A1 (https=)
CO (1) CO6650362A2 (https=)
EA (1) EA022395B1 (https=)
IL (1) IL223368A0 (https=)
MA (1) MA34377B1 (https=)
MX (1) MX2012014068A (https=)
NZ (1) NZ605741A (https=)
SG (1) SG186064A1 (https=)
TN (1) TN2012000581A1 (https=)
TW (1) TW201206435A (https=)
WO (1) WO2011159852A1 (https=)
ZA (1) ZA201300380B (https=)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9783540B2 (en) 2015-05-21 2017-10-10 Chemocentryx, Inc. Substituted tetrahydropyrans as CCR2 modulators
WO2019117550A1 (en) * 2017-12-11 2019-06-20 Cj Healthcare Corporation Intermediates for optically active piperidine derivatives and preparation methods thereof
US11154556B2 (en) 2018-01-08 2021-10-26 Chemocentryx, Inc. Methods of treating solid tumors with CCR2 antagonists
US11304952B2 (en) 2017-09-25 2022-04-19 Chemocentryx, Inc. Combination therapy using a chemokine receptor 2 (CCR2) antagonist and a PD-1/PD-L1 inhibitor
WO2024099908A1 (en) 2022-11-09 2024-05-16 Boehringer Ingelheim International Gmbh Cyclic pyridine derivatives as cgas inhibitors
US11986466B2 (en) 2018-01-08 2024-05-21 Chemocentryx, Inc. Methods of treating solid tumors with CCR2 antagonists
US12611409B2 (en) 2022-03-15 2026-04-28 Chemocentryx, Inc. Combination therapy using a chemokine receptor 2 (CCR2) antagonist and a PD-1/PD-L1 inhibitor

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102648193A (zh) * 2009-10-07 2012-08-22 百时美施贵宝公司 作为趋化因子受体活性调节剂的螺环化合物
TWI511967B (zh) 2010-06-16 2015-12-11 Takeda Pharmaceutical 醯胺化合物之結晶
CN109983012B (zh) 2016-09-16 2023-12-01 莱特豪斯制药公司 赖氨酸牙龈蛋白酶的酮抑制剂
EP3375778A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aryl-piperidine derivatives

Citations (4)

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Publication number Priority date Publication date Assignee Title
WO2007092681A2 (en) 2006-01-27 2007-08-16 Bristol-Myers Squibb Company Piperidinyl derivatives as modulators of chemokine receptor activity
WO2009015164A2 (en) * 2007-07-24 2009-01-29 Bristol-Myers Squibb Company Piperidinyl derivatives as modulators of chemokine receptor activity
WO2009015166A1 (en) * 2007-07-24 2009-01-29 Bristol-Myers Squibb Company Piperidine derivatives as modulators of chemokine receptor activity
WO2009158452A1 (en) * 2008-06-25 2009-12-30 Bristol-Myers Squibb Company Piperidinyl derivative as a modulator of chemokine receptor activity

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