AR110382A1 - SMALL MOLECULES INHIBITORS OF THE JAK QUINASAS FAMILY - Google Patents

SMALL MOLECULES INHIBITORS OF THE JAK QUINASAS FAMILY

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Publication number
AR110382A1
AR110382A1 ARP170103537A ARP170103537A AR110382A1 AR 110382 A1 AR110382 A1 AR 110382A1 AR P170103537 A ARP170103537 A AR P170103537A AR P170103537 A ARP170103537 A AR P170103537A AR 110382 A1 AR110382 A1 AR 110382A1
Authority
AR
Argentina
Prior art keywords
pyrrolo
cyclohexyl
cyanomethyl
pyridin
dihydroimidazo
Prior art date
Application number
ARP170103537A
Other languages
Spanish (es)
Original Assignee
Janssen Pharmaceutica Nv
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
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR110382A1 publication Critical patent/AR110382A1/en

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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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • 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
    • A61K31/4353—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
    • 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
    • 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
    • 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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • 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
    • 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
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • 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
    • A—HUMAN NECESSITIES
    • 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
    • A61P9/10—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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)

Abstract

Compuestos de 2-((1r,4r)-4-(imidazo[4,5-d]pirrolo[2,3-b]piridin-1(6H)-il)ciclohexil)acetonitrilo, composiciones farmacéuticas que los contienen, métodos para fabricarlos y métodos de uso de estos que incluyen los métodos para tratar estados de enfermedad, trastornos y afecciones mediadas por JAK, tal como la enfermedad intestinal inflamatoria. Reivindicación 1: Un compuesto seleccionado del grupo que consiste en 2-(1-((1r,4r)-4-(cianometil)ciclohexil)-1,6-dihidroimidazo[4,5-d]pirrolo[2,3-b]piridin-2-il)-N-(2-hidroxi-2-metilpropil)acetamida; 2-((1r,4r)-4-(2-(1H-imidazol-4-il)imidazo[4,5-d]pirrolo[2,3-b]piridin-1(6H)-il)ciclohexil)acetonitrilo; 2-(1-((1r,4r)-4-(cianometil)ciclohexil)-1,6-dihidroimidazo[4,5-d]pirrolo[2,3-b]piridin-2-il)-N-(ciclopropilmetil)acetamida; N-(2-cianoetil)-2-(1-((1r,4r)-4-(cianometil)ciclohexil)-1,6-dihidroimidazo[4,5-d]pirrolo[2,3-b]piridin-2-il)acetamida; 2-(1-((1r,4r)-4-(cianometil)ciclohexil)-1,6-dihidroimidazo[4,5-d]pirrolo[2,3-b]piridin-2-il)-N-(tetrahidro-2H-piran-4-il)acetamida; 2-(1-((1r,4r)-4-(cianometil)ciclohexil)-1,6-dihidroimidazo[4,5-d]pirrolo[2,3-b]piridin-2-il)-N-((tetrahidro-2H-piran-4-il)metil)acetamida; N-(2-ciano-2-metilpropil)-2-(1-((1r,4r)-4-(cianometil)ciclohexil)-1,6-dihidroimidazo[4,5-d]pirrolo[2,3-b]piridin-2-il)acetamida; 2-(1-((1r,4r)-4-(cianometil)ciclohexil)-1,6-dihidroimidazo[4,5-d]pirrolo[2,3-b]piridin-2-il)-N-((1-hidroxiciclobutil)metil)acetamida; 2-(1-((1r,4r)-4-(cianometil)ciclohexil)-1,6-dihidroimidazo[4,5-d]pirrolo[2,3-b]piridin-2-il)-N-(1-metil-1H-pirazol-4-il)acetamida; N-(4-(cianometil)biciclo[2.2.1]heptan-1-il)-2-(1-((1r,4r)-4-(cianometil)ciclohexil)-1,6-dihidroimidazo[4,5-d]pirrolo[2,3-b]piridin-2-il)acetamida; 2-(1-((1r,4r)-4-(cianometil)ciclohexil)-1,6-dihidroimidazo[4,5-d]pirrolo[2,3-b]piridin-2-il)-N-(1H-pirazol-3-il)acetamida; 2-(1-((1r,4r)-4-(cianometil)ciclohexil)-1,6-dihidroimidazo[4,5-d]pirrolo[2,3-b]piridin-2-ii)-N-((1-hidroxiciclopropil)metil)acetamida; y sales farmacéuticamente aceptables, y combinaciones de estos.Compounds of 2 - ((1r, 4r) -4- (imidazo [4,5-d] pyrrolo [2,3-b] pyridin-1 (6H) -yl) cyclohexyl) acetonitrile, pharmaceutical compositions containing them, methods to manufacture them and methods of use of these that include the methods to treat disease states, disorders and conditions mediated by JAK, such as inflammatory bowel disease. Claim 1: A compound selected from the group consisting of 2- (1 - ((1r, 4r) -4- (cyanomethyl) cyclohexyl) -1,6-dihydroimidazo [4,5-d] pyrrolo [2,3-b ] pyridin-2-yl) -N- (2-hydroxy-2-methylpropyl) acetamide; 2 - ((1r, 4r) -4- (2- (1H-imidazol-4-yl) imidazo [4,5-d] pyrrolo [2,3-b] pyridin-1 (6H) -yl) cyclohexyl) acetonitrile; 2- (1 - ((1r, 4r) -4- (cyanomethyl) cyclohexyl) -1,6-dihydroimidazo [4,5-d] pyrrolo [2,3-b] pyridin-2-yl) -N- ( cyclopropylmethyl) acetamide; N- (2-cyanoethyl) -2- (1 - ((1r, 4r) -4- (cyanomethyl) cyclohexyl) -1,6-dihydroimidazo [4,5-d] pyrrolo [2,3-b] pyridine- 2-yl) acetamide; 2- (1 - ((1r, 4r) -4- (cyanomethyl) cyclohexyl) -1,6-dihydroimidazo [4,5-d] pyrrolo [2,3-b] pyridin-2-yl) -N- ( tetrahydro-2H-pyran-4-yl) acetamide; 2- (1 - ((1r, 4r) -4- (cyanomethyl) cyclohexyl) -1,6-dihydroimidazo [4,5-d] pyrrolo [2,3-b] pyridin-2-yl) -N- ( (tetrahydro-2H-pyran-4-yl) methyl) acetamide; N- (2-cyano-2-methylpropyl) -2- (1 - ((1r, 4r) -4- (cyanomethyl) cyclohexyl) -1,6-dihydroimidazo [4,5-d] pyrrolo [2,3- b] pyridin-2-yl) acetamide; 2- (1 - ((1r, 4r) -4- (cyanomethyl) cyclohexyl) -1,6-dihydroimidazo [4,5-d] pyrrolo [2,3-b] pyridin-2-yl) -N- ( (1-hydroxycyclobutyl) methyl) acetamide; 2- (1 - ((1r, 4r) -4- (cyanomethyl) cyclohexyl) -1,6-dihydroimidazo [4,5-d] pyrrolo [2,3-b] pyridin-2-yl) -N- ( 1-methyl-1H-pyrazol-4-yl) acetamide; N- (4- (cyanomethyl) bicyclo [2.2.1] heptan-1-yl) -2- (1 - ((1r, 4r) -4- (cyanomethyl) cyclohexyl) -1,6-dihydroimidazo [4,5 -d] pyrrolo [2,3-b] pyridin-2-yl) acetamide; 2- (1 - ((1r, 4r) -4- (cyanomethyl) cyclohexyl) -1,6-dihydroimidazo [4,5-d] pyrrolo [2,3-b] pyridin-2-yl) -N- ( 1H-pyrazol-3-yl) acetamide; 2- (1 - ((1r, 4r) -4- (cyanomethyl) cyclohexyl) -1,6-dihydroimidazo [4,5-d] pyrrolo [2,3-b] pyridin-2-ii) -N- ( (1-hydroxycyclopropyl) methyl) acetamide; and pharmaceutically acceptable salts, and combinations thereof.

ARP170103537A 2016-12-16 2017-12-15 SMALL MOLECULES INHIBITORS OF THE JAK QUINASAS FAMILY AR110382A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201662435609P 2016-12-16 2016-12-16

Publications (1)

Publication Number Publication Date
AR110382A1 true AR110382A1 (en) 2019-03-20

Family

ID=65895700

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP170103537A AR110382A1 (en) 2016-12-16 2017-12-15 SMALL MOLECULES INHIBITORS OF THE JAK QUINASAS FAMILY

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AR (1) AR110382A1 (en)
MA (1) MA50430B1 (en)

Also Published As

Publication number Publication date
MA50430B1 (en) 2022-06-30
MA50430A (en) 2020-09-02

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