Lead Pharma Holding B.V.

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IPC Class
C07C 317/32 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton 7
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates 7
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID] 5
A61P 37/00 - Drugs for immunological or allergic disorders 5
A61K 31/10 - SulfidesSulfoxidesSulfones 4
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05 - Pharmaceutical, veterinary and sanitary products 2
42 - Scientific, technological and industrial services, research and design 2
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Pending 2
Registered / In Force 16

1.

ESTROGEN-RELATED RECEPTOR ALPHA MODULATORS

      
Application Number 17754902
Status Pending
Filing Date 2020-10-16
First Publication Date 2024-05-09
Owner LEAD PHARMA HOLDING B.V. (Netherlands)
Inventor
  • Lemmers, Jaap Gerardus Henricus
  • Deretey, Eugen
  • Klomp, Johannes Petrus Gerardus
  • Cals, Joseph Maria Gerardus
  • Oubrie, Arthur

Abstract

The present invention is directed to compounds according to Formula I and the pharmaceutically acceptable salts thereof. The compounds can be used as modulators of Estrogen-related Receptor alpha (ERRα) and have utility in the treatment of ERRα-mediated diseases or conditions. (I) The present invention is directed to compounds according to Formula I and the pharmaceutically acceptable salts thereof. The compounds can be used as modulators of Estrogen-related Receptor alpha (ERRα) and have utility in the treatment of ERRα-mediated diseases or conditions. (I)

IPC Classes  ?

2.

ESTROGEN-RELATED RECEPTOR ALPHA MODULATORS

      
Application Number 17624297
Status Pending
Filing Date 2020-07-01
First Publication Date 2022-12-08
Owner LEAD PHARMA HOLDING B.V. (Netherlands)
Inventor
  • Lemmers, Jaap Gerardus Henricus
  • Deretey, Eugen
  • Klomp, Johannes Petrus Gerardus
  • Cals, Joseph Maria Gerardus Barbara
  • Oubrie, Arthur

Abstract

The present invention is directed to compounds according to Formula (I) and the pharmaceutically acceptable salts thereof. The compounds can be used as modulators of Estrogen-related Receptor alpha (ERRα) and have utility in the treatment of ERRα-mediated diseases or conditions. The present invention is directed to compounds according to Formula (I) and the pharmaceutically acceptable salts thereof. The compounds can be used as modulators of Estrogen-related Receptor alpha (ERRα) and have utility in the treatment of ERRα-mediated diseases or conditions.

IPC Classes  ?

  • A61K 31/437 - 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
  • C07D 471/04 - Ortho-condensed systems
  • A61P 35/00 - Antineoplastic agents
  • C07D 495/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
  • A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings

3.

LeadPharma

      
Application Number 1610159
Status Registered
Filing Date 2021-06-09
Registration Date 2021-06-09
Owner Lead Pharma Holding B.V. (Netherlands)
NICE Classes  ?
  • 05 - Pharmaceutical, veterinary and sanitary products
  • 42 - Scientific, technological and industrial services, research and design

Goods & Services

Pharmaceutical preparations and pharmaceutical products; pharmaceutical preparations and pharmaceutical products for the treatment and prevention of autoimmune diseases, cancer, metabolic diseases, cardiological diseases, haematological diseases, diabetes, urological diseases, eye diseases, osteoporosis, depression, mental illness, bone diseases, respiratory diseases, asthma, kidney diseases, gastrointestinal diseases. Research and development in the field of pharmaceuticals and medicines; pharmaceutical research and drug research advisory services; providing information on medical and scientific research in the field of pharmaceutical substances and clinical trials.

4.

ESTROGEN-RELATED RECEPTOR ALPHA (ERRα) MODULATORS

      
Application Number EP2020079166
Publication Number 2021/074365
Status In Force
Filing Date 2020-10-16
Publication Date 2021-04-22
Owner LEAD PHARMA HOLDING B.V. (Netherlands)
Inventor
  • Lemmers, Jaap Gerardus Henricus
  • Deretey, Eugen
  • Klomp, Johannes Petrus Gerardus
  • Cals, Joseph Maria Gerardus
  • Oubrie, Arthur

Abstract

The present invention is directed to compounds according to Formula I and the pharmaceutically acceptable salts thereof. The compounds can be used as modulators of Estrogen-related Receptor alpha (ERRα) and have utility in the treatment of ERRα-mediated diseases or conditions. (I)

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/437 - 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
  • A61P 35/00 - Antineoplastic agents

5.

LeadPharma

      
Application Number 018450932
Status Registered
Filing Date 2021-04-12
Registration Date 2023-08-22
Owner Lead Pharma Holding B.V. (Netherlands)
NICE Classes  ?
  • 05 - Pharmaceutical, veterinary and sanitary products
  • 42 - Scientific, technological and industrial services, research and design

Goods & Services

pharmaceutical preparations and pharmaceutical products; pharmaceutical preparations and pharmaceutical products for the treatment and prevention of autoimmune diseases, cancer, metabolic diseases, cardiological diseases, haematological diseases, diabetes, urological diseases, eye diseases, osteoporosis, depression, mental illness, bone diseases, respiratory diseases, asthma, kidney diseases, gastrointestinal diseases; all the above-mentioned goods, excluding hygienic products for medical purposes, dietetic substances for medical use, foods for babies, plasters, materials for dressings, essences of dill or turpentine for medical use, glycerin, gums, balms, cold creams for medical use and tooth filling material, disinfectants, soaps for medical use. Research and development in the field of pharmaceuticals and medicines; pharmaceutical research and drug research advisory services; providing information on medical and scientific research in the field of pharmaceutical substances and clinical trials.

6.

ESTROGEN-RELATED RECEPTOR ALPHA (ERRα) MODULATORS

      
Application Number EP2020068574
Publication Number 2021/001453
Status In Force
Filing Date 2020-07-01
Publication Date 2021-01-07
Owner LEAD PHARMA HOLDING B.V. (Netherlands)
Inventor
  • Lemmers, Jaap Gerardus Henricus
  • Deretey, Eugen
  • Klomp, Johannes Petrus Gerardus
  • Cals, Joseph Maria Gerardus Barbara
  • Oubrie, Arthur

Abstract

The present invention is directed to compounds according to Formula (I) and the pharmaceutically acceptable salts thereof. The compounds can be used as modulators of Estrogen-related Receptor alpha (ERRα) and have utility in the treatment of ERRα-mediated diseases or conditions.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • C07D 495/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • A61P 35/00 - Antineoplastic agents
  • A61K 31/437 - 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
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone

7.

ROR gamma (RORγ) modulators

      
Application Number 15579111
Grant Number 10315996
Status In Force
Filing Date 2016-06-03
First Publication Date 2018-06-21
Grant Date 2019-06-11
Owner
  • LEAD PHARMA HOLDING B.V. (Netherlands)
  • SANOFI (France)
Inventor
  • Cals, Joseph Maria Gerardus Barbara
  • De Kimpe, Vera
  • Nabuurs, Sander Bernardus

Abstract

Compounds according to Formula I: 13 being C(1-6)alkyl or C(2-6)alkenyl. The RORγ compounds can treat RORγ mediated diseases.

IPC Classes  ?

  • C07C 311/20 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
  • C07C 317/44 - SulfonesSulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
  • C07C 317/50 - SulfonesSulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the nitrogen atoms being part of any of the groups X being a hetero atom, Y being any atom
  • C07D 207/06 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
  • C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
  • C07D 211/16 - 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
  • C07D 211/26 - 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
  • C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
  • C07D 213/82 - AmidesImides in position 3
  • C07D 215/08 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
  • C07D 217/02 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines
  • C07D 223/16 - BenzazepinesHydrogenated benzazepines
  • C07D 231/40 - Acylated on said nitrogen atom
  • C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
  • C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • C07D 277/46 - Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
  • C07D 285/135 - Nitrogen atoms
  • C07D 295/13 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
  • C07D 295/192 - Radicals derived from carboxylic acids from aromatic carboxylic acids
  • C07D 307/52 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
  • C07D 333/36 - Nitrogen atoms
  • C07D 417/04 - 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 containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 495/04 - Ortho-condensed systems

8.

ROR gamma (RORy) modulators

      
Application Number 15579075
Grant Number 10428018
Status In Force
Filing Date 2016-06-03
First Publication Date 2018-06-14
Grant Date 2019-10-01
Owner
  • LEAD PHARMA HOLDING B.V. (Netherlands)
  • SANOFI (France)
Inventor
  • Cals, Joseph Maria Gerardus Barbara
  • De Kimpe, Vera
  • Nabuurs, Sander Bernardus

Abstract

The present invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof. The compounds can be used as inhibitors of RORy and are useful for the treatment of RORy mediated diseases such as autoimmune and inflammatory diseases.

IPC Classes  ?

  • C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
  • C07D 215/08 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
  • C07D 231/40 - Acylated on said nitrogen atom
  • C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • C07D 261/14 - Nitrogen atoms
  • C07D 207/325 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
  • C07D 277/46 - Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
  • C07D 285/135 - Nitrogen atoms
  • C07D 211/16 - 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
  • C07D 307/52 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
  • C07C 317/32 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
  • C07C 317/44 - SulfonesSulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/415 - 1,2-Diazoles
  • A61K 31/42 - Oxazoles
  • A61K 31/433 - Thiadiazoles
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/4402 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
  • A61K 31/4406 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
  • A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
  • A61K 31/47 - QuinolinesIsoquinolines
  • C07D 207/06 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
  • C07D 213/71 - Sulfur atoms to which a second hetero atom is attached
  • C07D 307/14 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
  • C07D 307/22 - Nitrogen atoms not forming part of a nitro radical

9.

ROR gamma (RORγ) modulators

      
Application Number 15579164
Grant Number 10556866
Status In Force
Filing Date 2016-06-03
First Publication Date 2018-06-14
Grant Date 2020-02-11
Owner
  • LEAD PHARMA HOLDING B.V. (Netherlands)
  • SANOFI (France)
Inventor
  • Cals, Joseph Maria Gerardus Barbara
  • Nabuurs, Sander Bernardus

Abstract

Novel compounds according to Formula I 16 is C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl. The compounds can be used as inhibitors of RORγ and are useful for the treatment of RORγ mediated diseases.

IPC Classes  ?

  • C07C 317/32 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
  • C07D 213/81 - AmidesImides
  • C07C 311/46 - Y being a hydrogen or a carbon atom
  • A61P 37/00 - Drugs for immunological or allergic disorders
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

10.

ROR gamma (RORy) modulators

      
Application Number EP2017081489
Publication Number 2018/104288
Status In Force
Filing Date 2017-12-05
Publication Date 2018-06-14
Owner
  • LEAD PHARMA HOLDING B.V. (Netherlands)
  • SANOFI (France)
Inventor
  • Cals, Joseph Maria Gerardus Barbara
  • Machnik, David
  • Nabuurs, Sander Bernardus
  • Sabuco, Jean-François

Abstract

The present application relates to compounds according to (Formula IA) or (Formula IB): (Formula IA) (Formula IB) or a pharmaceutically acceptable salt thereof. The compounds can be used as inhibitors of RORγ and are useful for the treatment of RORγ mediated diseases.

IPC Classes  ?

  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • C07C 317/44 - SulfonesSulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
  • C07C 317/46 - SulfonesSulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
  • C07C 317/32 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
  • A61K 31/10 - SulfidesSulfoxidesSulfones

11.

ROR gamma (RORγ) modulators

      
Application Number 15578997
Grant Number 10118895
Status In Force
Filing Date 2016-06-03
First Publication Date 2018-05-24
Grant Date 2018-11-06
Owner
  • LEAD PHARMA HOLDING B.V. (Netherlands)
  • SANOFI (France)
Inventor
  • Cals, Joseph Maria Gerardus Barbara
  • Machnik, David
  • Nabuurs, Sander Bernardus
  • Sabuco, Jean-Francois
  • Schio, Laurent

Abstract

Novel compounds according to Formula I 16 is C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkyl-C(1-3)alkyl.

IPC Classes  ?

  • C07D 213/71 - Sulfur atoms to which a second hetero atom is attached
  • C07D 237/18 - Sulfur atoms
  • C07D 239/38 - One sulfur atom
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 31/50 - PyridazinesHydrogenated pyridazines
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
  • A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
  • C07D 241/18 - Oxygen or sulfur atoms

12.

ROR GAMMA (RORY) MODULATORS

      
Application Number EP2016062696
Publication Number 2016/193459
Status In Force
Filing Date 2016-06-03
Publication Date 2016-12-08
Owner
  • LEAD PHARMA HOLDING B.V. (Netherlands)
  • SANOFI (France)
Inventor
  • Cals, Joseph Maria Gerardus Barbara
  • De Kimpe, Vera
  • Nabuurs, Sander Bernardus

Abstract

The present invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof. The compounds can be used as inhibitors of RORy and are useful for the treatment of RORy mediated diseases such as autoimmune and inflammatory diseases.

IPC Classes  ?

  • C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
  • C07D 215/08 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
  • C07D 231/40 - Acylated on said nitrogen atom
  • C07C 317/32 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
  • C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • C07D 261/14 - Nitrogen atoms
  • C07D 207/325 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
  • C07D 277/46 - Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
  • C07D 285/135 - Nitrogen atoms
  • C07D 211/16 - 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
  • C07D 307/52 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
  • A61K 31/10 - SulfidesSulfoxidesSulfones
  • A61P 37/00 - Drugs for immunological or allergic disorders
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

13.

ROR GAMMA (RORY) MODULATORS

      
Application Number EP2016062708
Publication Number 2016/193468
Status In Force
Filing Date 2016-06-03
Publication Date 2016-12-08
Owner
  • LEAD PHARMA HOLDING B.V. (Netherlands)
  • SANOFI (France)
Inventor
  • Cals, Joseph Maria Gerardus Barbara
  • Machnik, David
  • Nabuurs, Sander Bernardus
  • Sabuco, Jean-Francois
  • Schio, Laurent

Abstract

The present invention relates to novel compounds according to Formula (I) or a pharmaceutically acceptable salt thereof

IPC Classes  ?

  • C07D 213/71 - Sulfur atoms to which a second hetero atom is attached
  • C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
  • C07D 241/18 - Oxygen or sulfur atoms
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/4965 - Non-condensed pyrazines
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • A61P 37/00 - Drugs for immunological or allergic disorders

14.

ROR GAMMA (RORγ) MODULATORS

      
Application Number EP2016062688
Publication Number 2016/193452
Status In Force
Filing Date 2016-06-03
Publication Date 2016-12-08
Owner
  • LEAD PHARMA HOLDING B.V. (Netherlands)
  • SANOFI (France)
Inventor
  • Cals, Joseph Maria Gerardus Barbara
  • De Kimpe, Vera
  • Nabuurs, Sander Bernardus

Abstract

The present invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof. The compounds can be used as inhibitors of RORy and are useful for the treatment of RORy mediated diseases.

IPC Classes  ?

  • C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
  • C07D 213/82 - AmidesImides in position 3
  • C07D 215/08 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
  • C07D 217/02 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines
  • C07D 223/16 - BenzazepinesHydrogenated benzazepines
  • C07D 231/40 - Acylated on said nitrogen atom
  • C07D 333/36 - Nitrogen atoms
  • C07C 311/20 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
  • C07C 317/32 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
  • C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
  • C07D 417/04 - 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 containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • C07D 207/06 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
  • C07D 495/04 - Ortho-condensed systems
  • C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring

15.

ROR GAMMA (RORγ) MODULATORS

      
Application Number EP2016062701
Publication Number 2016/193461
Status In Force
Filing Date 2016-06-03
Publication Date 2016-12-08
Owner
  • LEAD PHARMA HOLDING B.V. (Netherlands)
  • SANOFI (France)
Inventor
  • Cals, Joseph Maria Gerardus Barbara
  • Nabuurs, Sander Bernardus

Abstract

The present invention relates to novel compounds according to Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used as inhibitors of RORγ and are useful for the treatment of RORγ mediated diseases.

IPC Classes  ?

  • C07D 213/81 - AmidesImides
  • C07C 317/32 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
  • A61K 31/10 - SulfidesSulfoxidesSulfones
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • A61P 37/00 - Drugs for immunological or allergic disorders

16.

ROR GAMMA (RORY) MODULATORS

      
Application Number EP2016062712
Publication Number 2016/193470
Status In Force
Filing Date 2016-06-03
Publication Date 2016-12-08
Owner
  • LEAD PHARMA HOLDING B.V. (Netherlands)
  • SANOFI (France)
Inventor
  • Cals, Joseph Maria Gerardus Barbara
  • De Kimpe, Vera
  • Nabuurs, Sander Bernardus
  • Cadicamo, Cosimo Damiano
  • Lemmers, Jaap Gerardus Henricus

Abstract

The present invention relates to compounds according to Formula (I): or a pharmaceutically acceptable salt thereof. The compounds can be used as inhibitors of RORy and are useful for the treatment of RORy mediated diseases.

IPC Classes  ?

  • C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
  • C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • C07D 333/36 - Nitrogen atoms
  • C07D 233/61 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
  • C07C 311/20 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
  • C07C 317/32 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
  • C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 249/08 - 1,2,4-TriazolesHydrogenated 1,2,4-triazoles
  • C07D 263/32 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles
  • C07D 277/46 - Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
  • A61K 31/10 - SulfidesSulfoxidesSulfones
  • A61K 31/18 - Sulfonamides
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • A61P 37/00 - Drugs for immunological or allergic disorders

17.

ROR gamma (RORγ) modulators

      
Application Number 15102098
Grant Number 09738600
Status In Force
Filing Date 2014-12-03
First Publication Date 2016-10-20
Grant Date 2017-08-22
Owner
  • LEAD PHARMA CEL MODELS IP B.V. (Netherlands)
  • LEAD PHARMA HOLDING B.V. (Netherlands)
Inventor
  • Cals, Joseph Maria Gerardus Barbara
  • Nabuurs, Sander Bernardus

Abstract

15-16 are independently H, C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl, all groups optionally substituted with F, Cl, C(1-2)alkyl, C(1-2)alkoxy or cyano.

IPC Classes  ?

  • C07C 317/44 - SulfonesSulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
  • A61K 31/18 - Sulfonamides
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • C07C 311/16 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
  • C07C 311/20 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
  • C07C 317/46 - SulfonesSulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

18.

PROVISION OF NEW CARDIOMYOCYTE PROGENITOR CELLS AND CARDIOMYOCYTES DERIVED THEREFROM

      
Application Number EP2008000119
Publication Number 2008/083962
Status In Force
Filing Date 2008-01-09
Publication Date 2008-07-17
Owner LEAD PHARMA HOLDING B.V. (Netherlands)
Inventor
  • Goumans, Marie, José
  • Doevendans, Pieter

Abstract

The present invention relates to cardiomyocyte progenitor cells (CMPCs), to methods for their isolation and to the use of this CMPCs for the provision of cardiomyocytes, by way of differentiating the obtained CMPCs with a demethylating agent. The present invention also relates to pharmaceuticals compositions comprising cardiomyocytes for use in a cardiomyocyte replacement therapy and/or for the treatment in myocardial infarctation or for ameliorating the effects of myocardial infarctation.

IPC Classes  ?

  • A61K 35/34 - MusclesSmooth muscle cellsHeartCardiac stem cellsMyoblastsMyocytesCardiomyocytes
  • C12N 5/077 - Mesenchymal cells, e.g. bone cells, cartilage cells, marrow stromal cells, fat cells or muscle cells