Tuesday 17 March 2015

KHK 7580 structure cracked

WP_000286


KHK 7580 .....example no 3.001  R1-X- group\
  Figure imgb0352 Figure imgb0353 Figure imgb0354
HCl salt
MS · APCI: 361 [M+H] +
Figure imgb0350
in EP1757582
4-(3S-(1R-(1-naphthyl)ethylamino)pyrrolidin-1- yl)phenylacetic acid
4-​[(3S)​-​3-​[[(1R)​-​1-​(1-​naphthalenyl)​ethyl]​amino]​-​1-​pyrrolidinyl]​-Benzeneacetic acid,
cas will be updated
BASE ....870964-67-3
DI HCL SALT .......870856-31-8
MF C24 H26 N2 O2 BASE
MW 374.48 BASE
KHK-7580
KHK-7580; MT-4580
Mitsubishi Tanabe Pharma Corp... innovator
Kyowa Hakko Kirin Co Ltd.. licencee
4-(3S-(1R-(1-naphthyl)ethylamino)pyrrolidin-1-yl)phenylacetic acid,
useful as calcium-sensitive receptor (CaSR) agonists for treating hyperparathyroidism.  a CaSR agonist, being developed by Kyowa Hakko Kirin, under license from Mitsubishi Tanabe, for treating secondary hyperparathyroidism (phase 2 clinical, as of March 2015).
WILL BE UPDATED
WO2005115975,/EP1757582
http://www.google.co.in/patents/EP1757582A1?cl=en
Example no 3.001  R1-X- group Figure imgb0352 Figure imgb0353 Figure imgb0354
HCl salt
MS · APCI: 361 [M+H] +
Figure imgb0350



WO 2015034031A1
http://worldwide.espacenet.com/publicationDetails/biblio?DB=worldwide.espacenet.com&II=0&ND=3&adjacent=true&locale=en_EP&FT=D&date=20150312&CC=WO&NR=2015034031A1&KC=A1
Mitsubishi Tanabe Pharma Corporation
The present invention provides a novel crystal form of an arylalkylamine
compound. Specifically, a novel crystal form of
4-(3S-(1R-(1-naphthyl)ethylamino)pyrrolidin-1- yl)phenylacetic acid has
excellent stability, and is therefore useful as an active ingredient for
a medicine. The present invention also provides an industrially
advantageous method for producing an arylalkylamine compound.
WP_000287
WO 2015034031A1
http://worldwide.espacenet.com/publicationDetails/biblio?DB=worldwide.espacenet.com&II=0&ND=3&adjacent=true&locale=en_EP&FT=D&date=20150312&CC=WO&NR=2015034031A1&KC=A1
Mitsubishi Tanabe Pharma Corporation
The present invention provides a novel crystal form of an arylalkylamine compound. Specifically, a novel crystal form of 4-(3S-(1R-(1-naphthyl)ethylamino)pyrrolidin-1- yl)phenylacetic acid has excellent stability, and is therefore useful as an active ingredient for a medicine. The present invention also provides an industrially advantageous method for producing an arylalkylamine compound.

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see all at   http://drugpatentsint.blogspot.in/2015/03/wo-2015034031.html
see all at   http://drugpatentsint.blogspot.in/2015/03/wo-2015034031.html
see all at   http://drugpatentsint.blogspot.in/2015/03/wo-2015034031.html
see all at   http://drugpatentsint.blogspot.in/2015/03/wo-2015034031.html
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 http://www.kyowa-kirin.com/research_and_development/pipeline/
KHK7580 -Secondary Hyperparathyroidism
JP
CompanyMitsubishi Tanabe Pharma Corp.
DescriptionCalcium receptor agonist
Molecular Target
Mechanism of ActionCalcium-sensing receptor (CaSR) agonist
Therapeutic ModalitySmall molecule
Latest Stage of DevelopmentPhase II
Standard IndicationThyroid disease
Indication DetailsTreat hyperparathyroidism in patients receiving hemodialysis; Treat secondary hyperparathyroidism (SHPT)
Regulatory Designation
Partner
August 29, 2014

Kyowa Hakko Kirin Announces Commencement of Phase 2b Clinical Study of KHK7580 in Patients with Secondary Hyperparathyroidism in Japan

Tokyo, Japan, August 29, 2014 --- Kyowa Hakko Kirin Co., Ltd. (Tokyo: 4151, President and CEO: Nobuo Hanai, "Kyowa Hakko Kirin") today announced the initiation of a phase 2b clinical study evaluating KHK7580 for secondary hyperparathyroidism patients receiving hemodialysis in Japan.
This randomized, placebo-controlled, double-blind, parallel-group, multi-center study is designed to evaluate efficacy and safety in cohorts comprising KHK7580, its placebo and cinacalcet and initial dose of KHK7580 for secondary hyperparathyroidism patients receiving hemodialysis.
KHK7580 is a small molecular compound produced by Mitsubishi Tanabe Pharma Corporation (President & Representative Director, CEO: Masayuki Mitsuka, "Mitsubishi Tanabe Pharma"). Kyowa Hakko Kirin signed a license agreement of KHK7580 with Mitsubishi Tanabe Pharma for the rights to cooperative research, develop, market and manufacture the product in Japan and some part of Asia on March 2008.
The Kyowa Hakko Kirin Group is contributing to the health and prosperity of the world's people by pursuing advances in life sciences and technology and creating new value.
Outline of this study
ClinicalTrials.gov IdentifierNew window opensNCT02216656
Target PopulationSecondary hyperparathyroidism patients receiving hemodialysis
Trial DesignRandomized, placebo-controlled, double-blind (included open arm of cinacalcet), parallel-group, multi-center study
Administration GroupKHK7580, Placebo, cinacalcet
Target Number of Subjects150
Primary ObjectiveEfficacy
Trial LocationJapan
Trial DurationJul. 2014 to Jun. 2015

Contact:

Kyowa Hakko Kirin
Media Contact:
+81-3-3282-1903
or
Investors:
+81-3-3282-0009




Update on march 2016

New comment waiting approval on New Drug Approvals

M.F. Balandrin commented on KHK 7580 structure cracked
KHK 7580 .....example 3.008 2HCl MS · APCI: 375[M + H]+ in …
The calcimimetic agent, KHK-7580, currently entering Phase III clinical trials, has now been given the INN (WHO) generic name, evocalcet. Its chemical structure has also now been published and it is, in fact, correct as proposed by Dr. Crasto (Well Done!!):
http://www.drugspider.com/drug/evocalcet
https://tripod.nih.gov/ginas/app/substance/f580b9fd
http://www.medkoo.com/products/6729
(Etymologically, in classical Latin, "evolutio" refers to "the unrolling of a scroll" and "evocare" refers to a "call out"...).

http://www.medkoo.com/products/6729
img
Name: Evocalcet
CAS#: 870964-67-3
Chemical Formula: C24H26N2O2
Exact Mass: 374.19943
Evocalcet is a calcium-sensing receptor agonist. The calcium-sensing receptor (CaSR) is a Class C G-protein coupled receptor which senses extracellular levels of calcium ion. The calcium-sensing receptor controls calcium homeostasis by regulating the release of parathyroid hormone (PTH). CaSR is expressed in all of the organs of the digestive system. CaSR plays a key role in gastrointestinal physiological function and in the occurrence of digestive disease. High dietary Ca2+ may stimulate CaSR activation and could both inhibit tumor development and increase the chemotherapeutic sensitivity of cancer cells in colon cancer tissues. (Last update: 12/15/2015).
Synonym: MT-4580; MT 4580; MT4580; KHK-7580; KHK7580; KHK 7580; Evocalcet
IUPAC/Chemical Name: 2-(4-((S)-3-(((R)-1-(naphthalen-1-yl)ethyl)amino)pyrrolidin-1-yl)phenyl)acetic acid

2
https://tripod.nih.gov/ginas/app/substance/f580b9fd
Structure of EVOCALCET
http://www.drugspider.com/drug/evocalcet
INN name
Evocalcet
Lab Code(s)
MT-4580
KHK-7580
Chemical name
{4-[(3S)-3-{[(1R)-1-(Naphthalen-1-yl)ethyl]amino}pyrrolidin-1-yl]phenyl}acetic acid
Chemical structure
Molecular formula
C24H26N2O2
SMILES
O=C(O)CC1=CC=C(N2C[C@@H](N[C@@H](C3=C4C=CC=CC4=CC=C3)C)CC2)C=C1
CAS registry number
870964-67-3
Orphan Drug Status
No
On Fast track
No
New Molecular Entity
Yes
Originator
Developer(s)
Class
Mechanism of action
WHO ATC code(s)
EPhMRA code(s)
Clinical trial(s)
ConditionsInterventionsPhasesRecruitmentSponsor/Collaborators
Secondary HyperparathyroidismDrug: KHK7580Phase 3RecruitingKyowa Hakko Kirin Company, Limited
Secondary HyperparathyroidismDrug: KHK7580Phase 3RecruitingKyowa Hakko Kirin Company, Limited
Secondary HyperparathyroidismDrug: KHK7580|Drug: KRN1493Phase 2|Phase 3RecruitingKyowa Hakko Kirin Company, Limited
Secondary HyperparathyroidismDrug: Placebo|Drug: KHK7580 low dose|Drug: KHK7580 middle dose|Drug: KHK7580 high dose|Drug: KRN1493Phase 2CompletedKyowa Hakko Kirin Company, Limited
HyperparathyroidismDrug: KHK7580Phase 1|Phase 2CompletedKyowa Hakko Kirin Company, Limited
Secondary HyperparathyroidismDrug: KHK7580Phase 1CompletedKyowa Hakko Kirin Company, Limited
Updated on
11 Oct 2015
///////////////
SMILES Code: O=C(O)CC1=CC=C(N2C[C@@H](N[C@@H](C3=C4C=CC=CC4=CC=C3)C)CC2)C=C1

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